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A review of traditional uses, phytochemistry and pharmacology of the genus Indigofera
Abstract
Ethnopharmacological relevance:
Indigofera is the third-largest genus in the family of Fabaceae, with approximately 750 species. It is distributed across all tropical regions. Indigofera species are widely employed in traditional medicine all around the world, against many ailments. Thus, based on these medicinal properties, various investigations have been undertaken in order to appraise the pharmacological activities and the chemical composition of these species. A recent paper provides a summary of the phytochemistry and pharmacology of the genus Indigofera. Consequently, this review is a continuation of this previous study by updating some data and adding information about the phylogeny and traditional uses of the genus.
Aim of the study:
To provide an overview of the phylogeny, traditional uses, phytochemistry, pharmacology and toxicity of the genus Indigofera, and to identify the remaining gaps and thus supply a basis for further investigations.
Materials and methods:
A review of the literature was performed by consulting scientific databases such as 'ScienceDirect', 'PubMed', 'Google Scholar' and 'SpringerLink' and using the keyword Indigofera.
Results:
Over 60 Indigofera species are reported in traditional medicine. The uses depend on the country and the species, but similarities have been noticed. Indeed, treatments of gastrointestinal disorders, inflammatory conditions and pain, skin ailments, and respiratory and infectious diseases are recurring. Phytochemical studies have led to the identification of more than 200 compounds, notably flavonoids and terpenoids. Many pharmacological activities have been demonstrated, particularly antimicrobial, cytotoxic and anti-inflammatory activities, and thus allowed to assert most of the traditional uses of the genus. Some active compounds have been isolated and have shown remarkable therapeutic potential, like the alkaloid indirubin, which is currently being clinically trialed.
Conclusions:
The data on the genus Indigofera are extensive, but gaps still remain. Indeed, some promising species have not been assessed for their phytochemistry and/or pharmacology and thus remain unexplored. Moreover, relatively few active compounds have been isolated and tested for their biological activity, and studies to explain their mechanism of action are nearly inexistent. Furthermore, some pharmacological studies have inappropriate methodologies that make the results difficult to interpret. Consequently, further in-depth and relevant research is required to supplement the knowledge on this wide-ranging genus and to confirm its reported therapeutic potential.
... Numerous medicinal plants have been shown to have antioxidant, anticancer, and antitumor effects in earlier research [10,11] One of such plants whose therapeutic properties have been reported is Indigofera macrophylla. The genus Indigofera, comprising approximately 750 species, is widely used in traditional medicine for various ailments [12]. Phytochemical studies have identified over 200 compounds in the Indigofera species, primarily flavonoids and terpenoids [12]. ...
... The genus Indigofera, comprising approximately 750 species, is widely used in traditional medicine for various ailments [12]. Phytochemical studies have identified over 200 compounds in the Indigofera species, primarily flavonoids and terpenoids [12]. These plants exhibit diverse pharmacological activities, including antimicrobial, cytotoxic, and anti-inflammatory effects [12,13]. ...
... Phytochemical studies have identified over 200 compounds in the Indigofera species, primarily flavonoids and terpenoids [12]. These plants exhibit diverse pharmacological activities, including antimicrobial, cytotoxic, and anti-inflammatory effects [12,13]. Specific Indigofera species, such as I. colutea, I. tinctoria, I. nigritana, and I. macrocalyx, have demonstrated significant antioxidant properties, correlating with their high phenolic content [14]. ...
Background
Prostate cancer (Pca) is a deadly disease prevalent among men, and it accounts for about 7–8 % of mortality globally. Synthetic drugs have proved effective but have limitations and severe side effects. There is, therefore, a need to discover a less expensive, natural therapeutic agent with no side effects in treating the ailment.
Aim
The study aims to investigate the anti-prostate cancer activity of extracts of Indigofera macrophylla (I. macrophylla) at the physiological and molecular levels in experimental animals.
Method
Polyphenol-rich extract of I. macrophylla was subjected to HPLC analysis to identify the plant's phytochemical constituent. Adult Wistar rats were orally administered 2mls of 50, 100 and 200 PPM of the cacodylic acid solution for 28 days to induce prostate cancer, while treatment was carried out by orally administering extract of I. macrophylla at doses of 50, 100 and 200 mg/kg for up to 28 days. The anti-inflammatory and apoptotic properties of the extract in experimental animals were investigated by the expression levels of various genetic biomarkers such as Bax-2, TNF-α, IL-6, COX2, IL-1β, β-Catenin, APC, Bcl2, CEA, Caspase 3 and β-Catenin using reverse transcriptase polymerase chain reaction (RT-PCR).
Result
HPLC analysis shows that I. macrophylla has 21 bioactive components which are categorized into seven groups: flavonoid, terpenes, phenols, isoflavonoid, phytosterols, quinone and glycosides. Administration of the drug shows inconsistencies in the mean body weights of the experimental animals. Further investigation revealed that I. macrophylla increased TNF-α upregulation and expression, significantly downregulated IL-1β, significantly decreased IL-6 expression, ameliorated COX2 expression, downregulated β-catenin expression and significantly reduced the expression of the APC gene. These results show that the drug activity modulates the investigated inflammatory and apoptotic genes in the prostate gland of PCa-induced rats, thus demonstrating its anti-PCa potential.
Conclusion
The results of this study suggest the potential of a novel treatment protocol of I. macrophylla plant extract to improve therapeutic outcomes for patients with aggressive PCa, which reportedly claims hundreds of thousands of lives yearly.
... The genus Indigofera (Fabaceae) includes approximately 750 species, distributed across all tropical regions and possessing a wide range of pharmacological activities such as antimicrobial, cytotoxic and antiinflammatory properties (Gerometta et al., 2020). More than 200 metabolites are reported in this genus, including flavonoids, terpenoids and alkaloids (Gerometta et al., 2020). ...
... The genus Indigofera (Fabaceae) includes approximately 750 species, distributed across all tropical regions and possessing a wide range of pharmacological activities such as antimicrobial, cytotoxic and antiinflammatory properties (Gerometta et al., 2020). More than 200 metabolites are reported in this genus, including flavonoids, terpenoids and alkaloids (Gerometta et al., 2020). Some compounds have shown a potent therapeutic potential, like the anticancer bis-indole alkaloid indirubin (Gerometta et al., 2020). ...
... More than 200 metabolites are reported in this genus, including flavonoids, terpenoids and alkaloids (Gerometta et al., 2020). Some compounds have shown a potent therapeutic potential, like the anticancer bis-indole alkaloid indirubin (Gerometta et al., 2020). The species Indigofera ammoxylum (DC.) ...
... The genus has some species which produce indigo dye and are useful for crop shading, erosion control, soil protection and ornamental plants [70]. All parts of the plant are used as medicine for the treatment of skin diseases, swellings and wounds, digestive disorders and relief of pain [264]. Indigofera species have been used in several ways as decoctions for oral administration, and poultices for topical applications [264]. ...
... All parts of the plant are used as medicine for the treatment of skin diseases, swellings and wounds, digestive disorders and relief of pain [264]. Indigofera species have been used in several ways as decoctions for oral administration, and poultices for topical applications [264]. In Uganda and India, inhalation of the steam is common while in many countries they are used as an exclusive toothbrush for oral hygiene [264]. ...
... Indigofera species have been used in several ways as decoctions for oral administration, and poultices for topical applications [264]. In Uganda and India, inhalation of the steam is common while in many countries they are used as an exclusive toothbrush for oral hygiene [264]. Crude extracts and purified fractions of Indigofera species have anti-arthritic [265], antidiabetic and antidyslipidaemic [264], anticonvulsant [266] anthelmintic [267] and anticancer properties [268]. ...
Legumes are a major food crop in many developing nations. However, orphan or underutilized legumes are domesticated legumes that have valuable properties but are less significant than main legumes due to use and supply restrictions. Compared to other major legumes, they are better suited to harsh soil and climate conditions, and their great tolerance to abiotic environmental circumstances like drought can help to lessen the strains brought on by climate change. Despite this, their economic significance in international markets is relatively minimal. This article is aimed at carrying out a comprehensive review of the nutritional and pharmacological benefits of orphan legumes from eight genera in the sub-family Faboidea, namely Psophocarpus Neck. ex DC., Tylosema (Schweinf.) Torre Hillc., Vigna Savi., Vicia L., Baphia Afzel. ex G. Lodd., Mucuna Adans, Indigofera L. and Macrotyloma (Wight & Arn.) Verdc, and the phytoconstituents that have been isolated and characterized from these plants. A literature search was conducted using PubMed, Google Scholar, and Science Direct for articles that have previously reported the relevance of underutilized legumes. The International Union for Conservation of Nature (IUCN) red list of threatened species was also conducted for the status of the species. References were scrutinized and citation searches were performed on the study. The review showed that many underutilized legumes have a lot of untapped potential in terms of their nutritional and pharmacological activities. The phytoconstituents from plants in the subfamily Faboideae could serve as lead compounds for drug discovery for the treatment of a variety of disorders, indicating the need to explore these plant species.
... Antibacterial, antifungal, anticancer, anti-inflammatory and antioxidant [149] Flemingia grahamiana Alkaloids, flavonoids, glycosides, phenolics, saponins, steroids, tannins and volatile oils Antibacterial and anticancer [150,151] Indigofera arrecta Alkaloids, flavonoids, glycosides, phenols, saponins, tannins and terpenoids Antibacterial, antiviral and anticancer [152,153] Indigofera astragalina Saponins and tannins Antioxidant and cytotoxic [154] Indigofera hirsuta Alkaloids, flavonoids and phenolics Antidiabetic, anti-inflammatory and antioxidant [153] Indigofera spicata ...
... Antibacterial, antifungal, anticancer, anti-inflammatory and antioxidant [149] Flemingia grahamiana Alkaloids, flavonoids, glycosides, phenolics, saponins, steroids, tannins and volatile oils Antibacterial and anticancer [150,151] Indigofera arrecta Alkaloids, flavonoids, glycosides, phenols, saponins, tannins and terpenoids Antibacterial, antiviral and anticancer [152,153] Indigofera astragalina Saponins and tannins Antioxidant and cytotoxic [154] Indigofera hirsuta Alkaloids, flavonoids and phenolics Antidiabetic, anti-inflammatory and antioxidant [153] Indigofera spicata ...
... Benzofuran, fatty acids, flavonoids, phthalate, rotenoids, saponins, steroids and triterpenes Anticancer, antidiabetic, antidiarrhoeal, antiplasmodial and cytotoxicity [153,155] Julbernardia globiflora Fatty acids, lignin, proanthocyanidins and tannins Anticancer [112,156] Lessertia frutescens Amino acids, flavonoids, pinitol and triterpenes Analgesic, antibacterial, anticonvulsant, antidiabetic, anti-HIV, anti-inflammatory, antiproliferative, antistress and antithrombotic [157] Leucaena leucocephala Coumarins, flavonoids, phytol, sterols and triterpenes Antimicrobial, diuretic, antiviral, cytotoxic, antioxidant and anti-inflammatory [158][159][160][161] Mucuna coriacea None found Bacterial and antiviral [162,163] Mundulea sericea Coumarins, flavonoids, phenolic, saponins, steroids, tannins and volatile oils Analgesic, antibacterial, antifungal, antioxidant and insecticidal [164,165] Neorautanenia mitis Alkaloids, flavonoids, glycosides, saponins and tannins Antibacterial, antifungal and antinociceptive [166,167] Ormocarpum kirkii Coumarins, flavonoids and triterpenoids Antibacterial, antifungal, antimalarial, antiplasmodial and cytotoxicity [168] Ormocarpum trichocarpum Aliphatic hydrocarbons, coumarins, diterpenoids, steroids and triterpenes Antimicrobial, antiplasmodial, antioxidant and antimutagenic [169][170][171] Peltophorum africanum ...
The current study is aimed at providing a systematic review of the ethnomedicinal, phytochemical and pharmacological properties of Fabaceae species used as sources of traditional medicinies in Zimbabwe. Fabaceae is one of the well-known plant families of ethnopharmacological importance. Of the approximately 665 species of the Fabaceae family occurring in Zimbabwe, about 101 are used for medicinal purposes. Many communities in the country, mainly in peri-urban, rural and marginalized areas with limited access to healthcare facilities, rely on traditional medicines as their primary healthcare. The study reviewed research studies undertaken on Zimbabwe’s Fabaceae species during 1959 to 2022. Information was gathered from literature sourced from Google Scholar, Science Direct, Scopus, PubMed, books, dissertations, theses and scientific reports. This study showed that 101 species are traditionally used to manage human and animal diseases in Zimbabwe. The genera with the highest number of medicinal uses are Indigofera, Senna, Albizia, Rhynchosia and Vachellia. Species of these genera are used as traditional medicines against 134 medical conditions, mainly gastrointestinal conditions, female reproductive conditions, respiratory conditions and sexually transmitted infections. Shrubs (39.0%), trees (37.0%) and herbs (18.0%) are the primary sources of traditional medicines, while roots (80.2%), leaves (36.6%), bark (27.7%) and fruits (8.9%) are the most widely used plant parts. Many of Zimbabwe’s Fabaceae species used as sources of traditional medicines have been assessed for their phytochemical and pharmacological properties, corroborating their medicinal uses. However, there is a need to unravel the therapeutic potential of the family through further ethnopharmacological research focusing on toxicological studies, in vitro and in vivo models, biochemical assays and pharmacokinetic studies.
... A study [28] recorded renal toxicity in albino rats after the repetition of oral administration of AgNPs and explained the direct impact of nanoparticles on cellular construction through raising reactive oxygen species generation leading to necrotic and fibrotic alterations. On the other hand, many research confirmed the treatment influence of I. oblgofola on the prevention the inducing renal and hepatic toxicity as it enjoys anti-oxidative, anti-inflammatory, antifibrotic, and antiapoptotic properties [29]. The recent analysis agrees with the previous explanation due to the combination of AgNPs and I. oblgofola relieving the stressful impact on the cellular oxidative species. ...
... The treated experimental rats with I. oblgofola AgNPs showed refinement symptoms to a severe nephrotic syndrome caused by Plasmodium. The present data revealed that the I. oblgofola treatment had well imprint on acute kidney injury of malaria [11,29]. I. oblgofola has been used for its analgesic and anti-inflammatory properties to alleviate pain. ...
The study aimed to verify the pathogenic malarial kidney infections and histopathological pictures in mice infected with Plasmodium chabaudi using Indigofera oblongifolia leaf extract silver nanoparticles (IOLEAgNPs). Fifty healthy adult female mice C57BL/6 were used. Animals were divided into five groups, with each group of ten mice. The first control non-infected group was given distilled water for 7 days. The second group was orally given 50 mg/kg of IOLEAgNPs. The third, fourth, and fifth groups were injected intraperitoneally with 10⁵ parasitized erythrocytes of P. chabaudi. After 1 h, the fourth group received 50 mg/kg of IOLEAgNPs, while the fifth group orally received 10 mg/kg chloroquine phosphate. The histopathology of the kidney was studied by routine histology method with hematoxylin–eosin staining. The kidney revealed cerebral microvessel congestion, hemorrhages, and necrosis. Cast formation, glomerulonephritis, tubular necrosis, and congestion were observed in the kidney cortex. Consequently, the targeted medical IOLEAgNPs reduced this degeneration impact on renal tissue. Proven that plant-source synthesized IOLEAgNPs play a preventive role as antimalarial agents in female mice infected with P. chabaudi.
... Indigofera sp. contains phenol as an antimicrobial agent (Gerometta et al., 2020), whereas Gliricidia sp. has 1% tannin, 0.04% condensed tannins (Santos et al., 2017), and 17 mg/g saponins (Molina-Botero et al., 2019). ...
... Additionally, both the inclusion of legumes (Indigofera sp. + Gliricidia sp.) and BS4 spent substrate demonstrated potential in reducing methane production, which could be attributed to the activity of phenolic compounds, such as tannins and saponins, present in both legumes (Gerometta et al., 2020). ...
... In many countries, especially those of Africa and Asia, I. tinctoria has been used in traditional medicine to treat a wide range of maladies. The most well-documented uses include treating neurological disorders, dental problems, inflammation, and certain skin diseases, but there are many other known uses (Gerometta et al. 2020). It is also thought to have antimicrobial properties and can aid burn healing (Jisha and Benjamin 2009;Samanta, Basak, and Chattopadhyay 2014). ...
... Indigo was historically used as a cosmetic (eye shadow) in India (Lee 2010) and is still used as a hair dye, sometimes in conjunction with henna (Sri Bhuvaneswar et al. 2021). It can also act as an insect repellant (Zheng 2018), with documented activity against mosquito larvae (Gerometta et al. 2020). A recent use for indigo is as a biodegradable, organic semiconductor (Austrian Science Fund 2017; Krishnaswamy and Sundaresan 2013). ...
This EDIS publication is to introduce indigo as a new economic crop in south Florida. It highlights the historical and cultural background, including identification and distribution, uses, and history of indigo. The information included in this publication could be of interest to researchers, students, extension agents, growers, the dye industry, and the public.
... Indirubin will be tested for efficacy and safety as a potential therapeutic agent in these trials. As a result of the identification of numerous bioactive compounds, especially flavonoids and terpenoids, these Indigofera plants have been shown to have traditional uses (Gerometta et al., 2020). In spite of the extensive data available on Indigofera astragalina, there are still significant gaps in our knowledge of this plant. ...
... Numerous compounds have yet to be explored for their medicinal properties, suggesting vast untapped potential. Additionally, studies that consolidate the plant's activities and phytochemistry are lacking (Gerometta et al., 2020), as well as further exploration of active compounds. Therefore, the aim of this paper is to highlight a comprehensive overview of the pharmacological activities of I. astragalina, along with a comprehensive description of its phytochemistry. ...
Indigofera astragalina, a versatile medicinal plant, has gained significant attention because of its rich phytochemical composition and diverse therapeutic properties. I. astragalina contains sterols, phenolics, alkaloids, and flavonoids, making it ideal for a variety of therapeutic purposes. In this review, an in-depth look at the phytoconstituents and their biological activity is presented. The anti-microbial properties of the plant extracts have been demonstrated against drug-resistant Enterococcus and Staphylococcus aureus strains resistant to vancomycin and methicillin. Moreover, the plant exhibits moderate to potent anti-protozoal activity against Trypanosoma brucei and weak anti-protozoal activity against Plasmodium falciparum. In various cancer cell lines, astragalin extracts have demonstrated significant cytotoxic effects, suggesting their potential as anti-cancer agents. Due to its high phenolic content, the plant has an antioxidant effect, which has contributed to its traditional use for managing oxidative stress. In addition, I. astragalina is packed with essential amino acids, minerals (such as iron, manganese, and zinc), and vitamins. The comprehensive analysis of I. astragalina emphasizes its important role in drug discovery, nutrition, and healthcare, as well as its tremendous therapeutic potential.
... The extraction of essential oil from the berries of this plant is used to treat rheumatism [17,18] and the leaf essential-oil acts as an antiseptic agent [19]. The seed powder is used to treat skin boils, and, on the other hand, the root paste has the ability to poultice sprains and bruises, heal fever, swelling, and furunculosis [20]. Table 1 summarizes traditional uses of L. glutinosa. ...
... Root bark [24] Litseglutine A (2) Leaves and twigs [25] (7) Root bark [24] Glutinosine A (8) Root bark [27] Morphinane (9) - [13] Aporphine (10) [13] 1-benzylisoquinoline (11) [13] Phenanthrene (12) [13] N-methylactinodaphnine (13) Leaves [28] N-methyllaurotetanine (14) Leaves [28] Isoboldine (15) Leaves [28] Alcohols 1-heptadecanol (16) Bark [29] 1-eicosanol (17) Bark [29] Coclaurine (18) Root bark [30] Dihydrobuddlenol (19) Root bark [30] Ssioriside (20) Root bark [30] Carbohydrates Xylose (21) Leaves [31] Arabinose (22) Leaves [31] Glycosides Litseasins A (23) Root bark [32] Litseasins B (24) Root bark [32] Litseasins C (25) Root bark [32] Glutin (26) Leaves and twig [33] (7R,8S)-3,3 ′ ,5-trimethoxy-4 ′ ,7-epoxy-8,5 ′ -neolignan4,9,9-triol 9-β-D-xylopyranoside (27) Root bark [32] (6S, 7E, 9R)-6, 9-dihydroxy-4, 7-megastigmadien-3-one-9-O-[α-Larabinofuranosyl-(l→6)]-β-D-glucopyranoside (28) Leaves and twig [33] Roseoside (29) Leaves and twig [33] (30) Leaves and twig [33] ...
Litsea glutinosa (Lour.) C. B. Robinson, belonging to the family Lauraceae, is a multipurpose and fast-growing evergreen or deciduous tree that has been traditionally used for numerous purposes such as treatment for diarrhea, dysentery, abdominal pain, indigestion, gastroenteritis, edema, traumatic injuries, colds, arthritis, asthma, diabetes, pain relief, and poignant sexual power. This study aimed to summarize the chemical reports, folk values, and phytopharmacological activities of L. glutinosa, based on available information screened from diverse databases. An up-to-date electronic-based search was accomplished to obtain detailed information, with the help of several databases such as Google Scholar, Scopus, SpringerLink, Web of Science, ScienceDirect, Research-Gate, PubMed, ChemSpider, Elsevier, BioMed Central, and the USPTO, CIPO, INPI, Google Patents, and Espacenet, using relevant keywords. Outcomes advocate that, up to the present time, alka-loids, glycosides, and terpenoids are abundant in, and the most bioactive constituents of, this natural plant. Results demonstrated that L. glutinosa has various remarkable biological activities, including antioxidant, anti-inflammatory, anti-microbial, anticancer, antipyretic, anti-diabetic, analgesic, hep-atoprotective, and wound-healing activity. One study revealed that L. glutinosa exhibited significant aphrodisiac and anti-infertility activity. Nevertheless, no clinical studies have been cited. Taken together, L. glutinosa may be one of the significant sources of bioactive constituents that could potentially lead to different effective pharmacological activities. On the other hand, future research should focus on clinical studies and several toxicity evaluations, such as sub-chronic toxicity, teratogenicity, and genotoxicity.
... The genus Indigofera contains certain economically significant indigo dye-producing species, such as I. tinctoria and I. suffruticosa [9]. I. tinctoria belongs to the family of the Fabaceae, which is distributed across various tropical regions. ...
... It has been shown that indigotin, a colorless glycoside producing the blue color dye, possesses antiseptic and astringent properties [22]. However, no systemic toxicological data on I. tinctoria leaf powder has been reported in the literature [9]. In contrast, the neuroprotective role of aqueous extract of I. tinctoria was reported in Wistar rats [23]. ...
Background and Purpose: This research aimed to investigate the in vivo acute oral toxicity of aqueous extract of Indigofera tinctoria L. in different doses in Wistar rats.
Materials and Methods: Twenty-five male rats were divided into five groups (n=5 for each group). Group I served as the control, and the other four groups received I. tinctoria (100, 250, 500, and 1000mg/kg body weight) for 14 days. At the end of the experiment, all animals were killed, and the blood samples were collected for biochemical assay. The fourier transform infrared spectroscopy (FTIR), and histopathological analyses were done on different tissues.
Results: According to the results, rats who received I. tinctoria (100mg) had lower triglyceride than the control group. Moreover, I. tinctoria administration in all groups did not change the serum glucose, creatinine, urea, and high-density lipoprotein amounts. In addition, using 100mg of the extract resulted in a lower alanine transaminase level than the control. Also, histopathology data indicated no signs of tissue toxicity and degeneration in all experimental groups. Furthermore, FTIR indicated that I. tinctoria had not changed the tissues’ protein structure.
Conclusion: It can be concluded that I. tinctoria can be used as colorant food up to 1000mg/kg body weight.
... Moreover, 16 demonstrated remarkable cytotoxicity exclusively against CDK9-overexpressing cancer cells. Pomalidomide was employed in the synthesis of a novel conjugate of an indirubin analogue (an indole alkaloid from Indigofera species), which is a selective HDAC6 inhibitor by Cao et al. (Figure 6) [58,59]. HDAC6 has been related with many abnormalities including tumorigenesis due to its multiple roles in cells. ...
... Pomalidomide was employed in the synthesis of a novel conjugate of an indirubin analogue (an indole alkaloid from Indigofera species), which is a selective HDAC6 inhibitor by Cao et al. (Figure 6) [58,59]. HDAC6 has been related with many abnormalities including tumorigenesis due to its multiple roles in cells. ...
Cancer is one of the top leading causes of death worldwide. It is a heterogenous disease characterized by unregulated cell proliferation and invasiveness of abnormal cells. For the treatment of cancer, natural products have been widely used as a source of therapeutic ingredients since ancient times. Although natural compounds and their derivatives have demonstrated strong antitumor activity in many types of cancer, their poor pharmacokinetic properties, low cell selectivity, limited bioavailability and restricted efficacy against drug-resistant cancer cells hinder their wide clinical application. Conjugation of natural products with other bioactive molecules has given rise to a new field in drug discovery resulting to the development of novel, bifunctional and more potent drugs for cancer therapy to overcome the current drawbacks. This review discusses multiple categories of such bifunctional conjugates and highlights recent trends and advances in the development of natural product hybrids. Among them, ADCs, PDCs, ApDCs, PROTACs and AUTOTACs represent emerging therapeutic agents against cancer.
... Ipomine has anti-inflammatory activity (Kumar et al. 2022). Lupinisoflavone M is used in treating inflammatory conditions, gastrointestinal disorders, skin ailments, and respiratory infections (Gerometta et al. 2020). mepA inhibition mechanisms are the precise mechanisms by which these compounds inhibit mepA and require further investigation. ...
Helicobacter pylori is a Gram-negative bacterium that infects the human gastrointestinal mucosa and is a significant human pathogen, affecting 50% of the world’s population. Multidrug Efflux Pump mepA from the MATE family of proteins acts as a potential efflux pump target in Helicobacter pylori which exports multiple drugs outside the Helicobacter pylori and consists of 417 amino acids. This study aimed to identify potential inhibitors of the multidrug efflux pump mepA in Helicobacter pylori using in-silico approaches that employed molecular docking, drug-likeness evaluation, density functional theory [DFT], molecular dynamics (MD) simulations, and free energy calculations to analyze, the interactions between phytochemicals compounds and mepA protein. The best compounds exhibiting the highest binding affinities toward mepA were selected among all the screened phytochemical compounds from the database. Overall, this research identified three promising natural compounds Hinokiflavone (− 10.9 kcal/mol), Ipomine (− 10.7 kcal/mol), and Lupinisoflavone M (− 10.5 kcal/mol) from 30 top compounds based on binding affinity score, which demonstrated remarkable binding affinities toward mepA through molecular docking, suggesting their potential to block the efflux pump and potentiate antibiotic action with the potential to inhibit the multidrug efflux pump mepA in Helicobacter pylori. Besides, we select one complex for 3 compounds for an analysis of DFT and calculate the stability of protein and protein–ligand complex by Molecular Dynamics simulation along with this we calculate the binding free energy for the complex’s protein for selected Lupinisoflavone M complex (− 98.948 kJ/mol). The study highlights the promising capacity of the selected compounds to inhibit the mepA efflux pump, potentially paving the way for developing novel therapeutic strategies against multidrug-resistant pathogens.
... Two herbal drugs were selected by name-Indigofera prostrate (Fabaceae) and lantana camara (Verbenaceae)in the present study. I. prostrata has spread branches with unique features that make it a promising candidate for perennial crops [12]. Different species differ greatly from one another; this variation includes differences in fruit type, flowering shape, and pericarp thickness. ...
Objective: The present investigation explored the binding affinities of phytoconstituents present in Indigofera prostrata and lantana camara that acted as Anti-Alzheimer's drug. Also the phytoconstituents were identified by Gas chromatography–Mass spectrometry (GC-MS) against selected targets, i. e., β-amyloid and acetylcholinesterase (AchE). Methods: I. prostrata seeds and leaves of l. camara were macerated using methanol as a solvent, then analysed for phytoconstituents through GC–MS. The Chromatogram revealed the presence of 14 in I. prostrata and l. camara 19 novel phytoconstituents. These phytoconstituents were explored for their Anti-Alzheimer’s effect by iGEMDOCK software against selected targets, namely recombinant human acetylcholinesterase β-amyloid (protein data bank ID: 2LMN). Results: The docking analysis resulted in four and five phytoconstituents with the highest binding affinity towards the selected targets in I. prostrate and l. Camara, I, respectively. The bioactive compounds present in the methanolic extract of l. camara were, Heptane,4-ethyl-2,2,6,6-tetramethyl-‘N, N-Dinitro-1,3,5,7-tetrazabicyclo[3,3,1] nonane, Spiro[androst-5-ene-17,1'-cyclobutan]-2'-one,3-hydroxy-,(3. beta,17. beta.). ligPlot depicted hydrophobic bonds, hydrogen bonds, and their bond lengths in each of the in silico effective docking compounds, which were compared with their respective standards. Conclusion: From the results obtained it was concluded that the in silico analysis using computational approaches might become a prospective novel compound against the selected targets in Alzheimer's disease.
... Indigofera atropurpurea flowers are used for diarrhea and dysentery [15]. Similarly, Albizia julibrissin is used in Chinese medicine to treat ulcers, boils, bruises, fractures, insomnia, anxiety, and hemorrhoids [13,16]. ...
The Fabaceae is renowned for its diverse range of chemical compounds with significant biological activities, making it a valuable subject for pharmacological studies. The chemical composition and biological activities of three Fabaceae species were investigated using methanol separately and in combination with dimethyl sulfoxide (DMSO) and glycerol for extraction. The results revealed the highest phenolic (49.59 ± 0.38 mg gallic acid equivalent/g), flavonoid (29.16 ± 0.39 mg rutin equivalent/g), and alkaloid (14.23 ± 0.54 mg atropine equivalent/g) contents in the Caesalpinia decapetala methanol extracts. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and DNA protection activity were the highest (0.88 ± 0.43 µg/mL IC50 and 2149.26 band intensity) in Albizia julibrissin methanol extracts. The α-amylase activity was highest in all methanol extracts (< 15 µg/mL IC50 values), while the α-glucosidase inhibition potential was highest (< 1 µg/mL J o u r n a l P r e-p r o o f 2 IC50 value) in the methanol-glycerol and methanol-DMSO extracts. Pearson coefficient analysis showed a strong positive correlation between the DPPH and α-amylase assays and phytochemicals. Anti-leishmanial activity was observed in decreasing order: A. julibrissin (74.75 %) > C. decapetala (70.86 %) > Indigofera atropurpurea (65.34 %). Gas chromatography-mass spectrometry revealed 33 volatile compounds and, aamong these (Z)-9-octadecenamide was detected in the highest concentration ranging from 21.85 to 38.61 %. Only the methanol extracts of the examined species could be assessed for in vivo studies for immediate applications.
... The genus is characterised by a combination of the presence of medifixed 2-branched trichomes, pulvinate leaves, axillary simple racemes, anthers with appendiculate connective and flowers with an explosive pollen display (Hutchinson 1964;De Kort and Thijsse 1984). The genus includes economically important species with a variety of uses (Gerometta et al. 2020). Notably, I. tinctoria L. and I. suffruticosa Mill. ...
Indigofera jintongpenensis, a new species of the subfamily Papilionoideae of Fabaceae, is described and illustrated from Yunnan, southwest China. The new species is characterised by having a prostrate habit, flexible stems and branches, as well as spreading, sub-basifixed, asymmetrically 2-branched trichomes covering the entire plant, discoid calyx, and racemose inflorescences 6–8-flowered, short, 1–2 (–3.5) cm in length, apparently shorter than the leaf. A distribution map and comparison of morphological diagnostic characters with its morphologically similar species are provided. Additionally, a preliminary conservation assessment of I. jintongpenensis is proposed following IUCN criteria.
... Species of Indigofera used to treat skin diseases, swellings, wounds, digestive disorders, snakebites, headaches, chest pain, neurological disorders, diarrhea, dysentery and used as a diuretic, coolants, demulcents and pain killers [5][6][7][8][9][10] .Around 200 compounds have been identified so far, including phenolics, terpenoids, alkaloids and glucose esters of nitropropanoic acids. Crude extracts and purified fractions obtained from various parts of Indigofera species studied for their wide range of pharmacological activities 11 . Rusty Indigo (=Indigofera Viscosa Lam.) (figure 1) has been extensively used as folk medicine in various countries where it is found. ...
Species of Indigofera (Leguminosae) genus used as traditional medicines in different parts of the world, some of them are not studied for its chemical diversity. The present study was aimed to characterize the phytochemical potential of Indigofera Viscosa leaf. Nonpolar to polar solvents were used to successively extract the phytochemicals by using soxhlet apparatus. The extracts were tested for the secondary metabolite screening. Major bioactive compounds such as alkaloids, flavonoids, tannins, steroids, triterpenoids were detected from various extracts. Ethanol extract showed high positive results in the test of such biochemicals, so this extract only used for further study. High amount of total phenolic content was noted in the quantification of secondary metabolites. FTIR analysis indicated the presence of metabolically active alcohols, phenols, carboxylic acids, amino acids, alkynes, esters, nitro compounds, aromatic amines, etc. GC-MS analysis revealed that presence of 15 major compounds in leaf, most of them are well-known for their biological activities. The compound milbemycin B may highly present in the leaf sample because of its large area percentage.The present study will be helpful to the quality assessment of herbal remedies containing Indigofera species and chemotaxonomic justification of the species. Further investigations are required to study the biological activities of the plant in crude as well as elute form of extracts.
... Indigofera est le troisième plus grand genre de la famille Leguminosae et comprend environ 750 espèces dont environ 75% sont limitées à l'Afrique et à Madagascar Sud (Camara et al., 2019;Gerometta et al., 2020;Atta et al., 2022). Indigofera pulchra (Ip) Willd est une plante herbacée ou arbustive annuelle non grimpante qui peut atteindre 1 m de haut. ...
Indigofera eIndigofera pulchra (Ip) Willd est utilisé en médecine traditionnelle pour traiter l’anémie, le paludisme et la douleur, par des ingestions répétées. L’objectif de cette étude était d’évaluer la toxicité subaiguë des extraits hydro-méthanoliques de Ip. La constitution phytochimique de l’extrait a été déterminée. Quatre lots de cinq rats Wistar chacun ont été constitués dans lesquels étaient administrés quotidiennement de l’eau distillée (lot 1 : groupe témoin), l’extrait à 100 mg/kg de poids (lot 2), l’extrait à 200 mg/kg de poids (lot 3) et l’extrait à 400 mg/kg de poids (lot 4). Un hémogramme, une numération des réticulocytes (J0, J15 et J29) et des examens biochimiques (J0 et J29) ont été réalisés après gavage avec les extraits. L’extrait contenait des flavonoïdes, des tanins, des triterpènes et stérols, des saponosides et des coumarines. La variation de la numération des globules rouges (p=0,014) et l’urée sérique (p=0,019) était plus faible et celle du volume globulaire moyen (p=0,015) et de la teneur corpusculaire moyenne en hémoglobine (p=0,014) plus importante dans le lot 4 par rapport au lot 1 à J29. Il n’y avait pas de différence significative des valeurs et de la variation des paramètres biologiques étudiés. Ip n’est pas responsable de toxicité hématologique, hépatique ou rénale à la dose 100 à 400 mg d’extrait par kilogramme chez les rats. Indigofera pulchra (Ip) Wild is used as medicinal plant to treat anemia, malaria and pain, conditions that often require repeated doses. The aim of this work was to evaluate the subacute toxicity of Ip hydro-methonolic extracts. Four groups of five Wistar rats receiving orally every day and respectively distilled water (group 1: control group), 100 mg of extract per kilogram of weight (group 2), 200 mg/kg (group 3) and 400 mg/kg weight (group 4). A complete blood count with reticulocytes count (day0, day15 and day29) and biochemical tests (day0 and day29) were assessed after the extract administration. Flavonoids, tannins, triterpenes and sterols, saponins and coumarins were detected in the extract. The change in red blood cell count (p=0.014) and serum urea (p=0.019) was lesser and that of the mean corpuscular volume (p=0.015) and the mean corpuscular hemoglobin (p=0.014) greater in group 4 compared to group 1 at day29. The other hematological and biochemical parameters were not significantly different between the groups of rats. There was no significant difference in the absolute values and the variation of the assessed biological parameters. Ip is not responsible for hematological, liver or renal toxicity when administered orally at the dose of 100-400 mg extract per kilogram in rats.
... Follwing compounds have been isolated from various species of the genus. For E.g. (Kaempferitrin C 27 H 30 O 14 I. arrecta) [19], Indigoidin C 10 H 8 N 4 O 4 I. pseudomonas [20], Indigotin, C 16 H 10 N 2 O 2 I. tinctoria [21] (Singh B et al., 2006). While some reported compound based on different geographical terrian as compared to our study have been extracted from seed of I. heterantha following compounds have been isolated and there structures have been obtained by mass spectrometry, Carbon 13 NMR and Proton NMR. ...
Background
Multidrug-resistant bacterial strains cause several serious infections that can be fatal, such as Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacteriaceae (often referred to as ESKAPE pathogens). Since ancient times, several indigenous medical systems in India have utilized diverse medicinal plants (approximately 80,000 species) as conventional treatments for a variety of illnesses. A member of the Fabaceae family, also referred to as “Himalayan indigo,” Indigofera heterantha Wall, is well known for its therapeutic properties.
Methods
The present study investigated the antibacterial, antifungal and antihelmintic properties of the roots, bark, leaves, and flowers of I. heterantha from the Kashmir Himalayas. The effectiveness of the extracts against bacteria, fungi, and earthworms. Three of the tested organisms for bacteria were ESKAPE pathogens, as they are responsible for creating fatal bacterial infections. The antifungal potency of I. heterantha aqueous and methanolic extracts was evaluated using the Agar Well Diffusion Assay. The antihelmintic activity was carried out on an adult Pheretima posthuma Indian earth worm, which shares physiological and anatomical similarities with human intestinal roundworm parasites.
Results
The methanolic extracts of root and bark have shown prominent activity against all bacterial strains, whereas aqueous extracts of flower, root, and leaves have shown promising activity against Staphylococcus aureus. The aqueous extract demonstrated good activity against S. cerevisiae at a concentration of 200 mg/ml with a zone of inhibition of 16 mm, while the methanolic extract displayed comparable activity against the fungal strains. The remaining two strains, P. crysogenum and A. fumigatus, were only moderately active in response to the extracts. All the extracts have shown anthelmintic activity except aqueous flower.
Conclusion
These results will pave the way for the bioassay-guided isolation of bioactive constituents that may act as hits for further development as potential antibacterial agents against drug-resistant microbial and helminthic infections.
... It is a common plant in Gabon, Congo, and Nigeria, and the boiled seeds are generally eaten in India and Africa [151]. To prevent plaque and cavities, the powdered seeds are massaged into the teeth and gums [152]. The root has been used for treating elephantiasis in Congo [153] while the leaf decoction has been reported for treating hepatic diseases in Gabon [154]. ...
Underutilized legumes are common crops in developing countries with superior dietary potentials that could be useful sources of protein as well as some phytoconstituents. They are more tolerant of abiotic environmental conditions like drought than the major legumes. This makes them more adapted to harsh soil and climatic conditions, which helps to minimize the pressure brought on by climate change. However, despite their potential, underutilized legumes have been greatly overlooked compared to the major legumes due to supply constraints. Underutilized legumes in the subfamily Caesalpinioideae are better suited for use as animal feeds with little or no value as food for humans, and the extracts and infusions of the different parts of plant species in this subfamily are traditionally used for the treatment of different diseases. In addition, underutilized legumes in this subfamily contain phytoconstituents that are of pharmacological relevance, some of which have been isolated, characterized and evaluated for use in the treatment of a variety of disorders. Therefore, this review describes the medicinal activities of some selected underutilized legumes from five genera in the subfamily Caesalpinioideae as well as their phytoconstituents, which could be exploited as lead compounds for drug discovery.
... The major potential bioactive flavanone identified in Tephrosia species' aerial portions is (-) pseudosemiglabrin [20][21][22]. It was recently discovered to have pivotal potentialities, including anti-inflammatory, neuroprotective, analgesic, antioxidant, antiplatelet, antidyslipidemic, diuretic, anti-cancer, and anti-angiogenic properties [20-25]. ...
One prevalent neurological disorder is epilepsy. Modulating GABAergic/glutamatergic neurotransmission, Nrf2/HO-1, PI3K/Akt, and TLR-4/NF-B pathways might be a therapeutic strategy for epilepsy. Eight-week-old BALB/c mice were administered 12.5, 25, or 50 mg/kg (-) pseudosemiglabrin orally one hour before inducing epilepsy with an i.p. injection of 360 mg/kg pilocarpine. (-) Pseudosemiglabrin dose-dependently alleviated pilocarpine-induced epilepsy, as revealed by the complete repression of pilocarpine-induced convulsions and 100% survival rate in mice. Furthermore, (-) pseudosemiglabrin significantly enhanced mice's locomotor activities, brain GABA, SLC1A2, GABARα1 levels, glutamate decarboxylase activity, and SLC1A2 and GABARα1mRNA expression while decreasing brain glutamate, SLC6A1, GRIN1 levels, GABA transaminase activity, and SLC6A1 and GRIN1 mRNA expression. These potentials can be due to the suppression of the TLR-4/NF-κB and the enhancement of the Nrf2/HO-1 and PI3K/Akt pathways, as demonstrated by the reduction in TLR-4, NF-κB, IL-1β, TNF-α mRNA expression, MDA, NO, caspase-3, Bax levels, and Bax/Bcl-2 ratio, and the enhancement of Nrf2, HO-1, PI3K, Akt mRNA expression, GSH, Bcl-2 levels, and SOD activity. Additionally, (-) pseudosemiglabrin abrogated the pilocarpine-induced histopathological changes. Interestingly, the (-) pseudosemiglabrin intervention showed a comparable effect to the standard medication, diazepam. Therefore, (-) pseudosemiglabrin can be a promising medication for the management of epilepsy.
... Woad is grown in Western Asia, the Mediterranean, across Europe, and North America. Te largest family of medicinal plants is the Fabaceae, which has over 750 species and is utilized as a primary source of the blue color [40]. Among the Indigofera family, two species, namely, Indigofera tinctoria and Indigofera sufruticosa, are the plants that produce the blue colour in large quantities and they are the two economically important indigo dye-producing species known to exist today [41]. ...
The recent increasing consciousness for environment sustainability and health hazards is the motive for looking for alternative environment-friendly materials and manufacturing processes. Therefore, environmental compatibility and safety to the health manufacturing process are a worldwide concern. The use of excessive and toxic synthetic dyes in textile and apparel manufacturing processes lineages environment pollution and health hazards to the surroundings where they are sited. Consequently, penetrating for alternative eco-friendly dyes has been initiated in recent times by researchers and development motivators in order to reduce the excessive use of synthetic dyes. In this regard, natural indigo dye from the indigo plant is getting attention, and thus, it is preferred as good as synthetic indigo dye, owing to its inherited dyeing property. With natural indigo dye, it can be achieved eco-friendly dyeing without the application of mordant attaining commercially acceptable fastness properties. Owing to the popularity of blue jeans around the world, especially those that are naturally dyed indigo blue, indigo dye consumption is now rising. Furthermore, currently, natural indigo dye is demanding for functional textile finishing, cosmetics and food colouration, UV protection and deodorizing agents, and other applications. In general, because of its increasing demand and wide applications, natural indigo has become an important cash crop and is traded in the international market with a price range of 35 to 40 USD per kilogram as per its purity level. Indigo dye has therefore been revived with more applications than it had before the advent of man-made colourants. The revival of indigo presents a chance for underdeveloped nations with incorporated economic and social benefits. Ethiopia as a developing country and situated in tropical Africa will benefit from indigo revival because of its potentials with having a suitable climate, a young workforce, enough land resource, and its booming textile and apparel industries.
... Withania somnifera was another multipurpose MP (cited in four countries) used to control convulsions in Ethiopia, Lesotho, India, and in East African countries [107,110,111]. Moreover, Acacia seyal, Acalypha fruticosa, Allium sativum, Balanites aegyptica, Biophytum umbraculum, [105,106,108,109,118,[127][128][129][130][131][132][133][134][135][136][137]. The extensive use of MPs across different countries of the globe echoed the existence of shared ethnopharmacological knowledge among the THs, the importance of such MPs in the healthcare system of LMIC, especially in tropical and southern Africa, and more importantly, the pharmacological efficacy of the MPs in the treatment of epilepsy and related symptoms. ...
Epilepsy is a common central nervous system (CNS) disorder that affects 50 million people worldwide. Patients with status epilepticus (SE) suffer from devastating comorbidities and a high incidence of mortalities. Antiepileptic drugs (AEDs) are the mainstream treatment options for the symptomatic relief of epilepsy. The incidence of refractory epilepsy and the dose-dependent neurotoxicity of AEDs such as fatigue, cognitive impairment, dizziness, attention-deficit behavior, and other side effects are the major bottlenecks in epilepsy treatment. In low- and middle-income countries (LMICs), epilepsy patients failed to adhere to the AEDs regimens and consider other options such as complementary and alternative medicines (CAMs) to relieve pain due to status epilepticus (SE). Plant-based CAMs are widely employed for the treatment of epilepsy across the globe including Ethiopia. The current review documented around 96 plant species (PS) that are often used for the treatment of epilepsy in Ethiopia. It also described the in vivo anticonvulsant activities and toxicity profiles of the antiepileptic medicinal plants (MPs). Moreover, the phytochemical constituents of MPs with profound anticonvulsant effects were also assessed. The result reiterated that a lot has to be done to show the association between herbal-based epilepsy treatment and in vivo pharmacological activities of MPs regarding their mechanism of action (MOA), toxicity profiles, and bioactive constituents so that they can advance into the clinics and serve as a treatment option for epilepsy.
... Chemical constituents: [9] Apigenin, kaempferol, luteolin and quercetin, rotenoids, coumarins and flavonoids. ...
Introduction
Siddha system of medicine is an integrated part of Indian system, which is very potent and unique system. Treating disease with natural ingredient gives cost effective and less adverse drug reactions. Herbal formulations which are mentioned in Siddha text are helpful in the treatment of various diseases. Avuri Karpam is a poly herbal formulation which has 7 ingredients and it is mentioned in Siddha classical literature “ Pathartha Guna Vilakkam ”.
Materials and Methods
All ingredients of the drug Avuri Karpam is briefly explained here in Siddha aspects, Actions, Chemical constituents, Pharmacolgical aspects. All the above informations were collected from various scientific articles.
Results
This article provides a systematic review examined the effects of Siddha treatment for treating arthritis and also various diseases through Avuri Karpam and its active substances present in plants and their actions in a scientific way. However further clinical study is needed to prove the standard of the drug worldwide.
Conclusion
It could be a choice of drug for treating arthritis in cost effective less adverse drug reactions.
... 22,23 However, due to the existence of a hydrogenbonding framework in the structure of indirubin, the property of extremely poor solubility in most solvents has been observed, which is the main obstacle for the clinical application of indirubin. 21,[28][29][30][31][32][33][34][35][36] Up to now, much effort has been focused on indirubin and its derivatives; in particular, various cellular targets have been found including CDKs, 19,37,38 GSK-3b, 39 VEGFR-2, 40 c-Src, [41][42][43] Dyrk1A, 44 and other kinases. 15,45,46 Despite this, current research on indirubins is still mainly focused on the improvement of their water solubility and cytotoxicity. ...
Multi-drug-resistant microbial pathogens are a serious global health problem. New compounds with antibacterial activity serve as good candidates for developing novel antibacterial drugs which is very urgent and important. In this work, based on the unique scaffold of indirubin, an active ingredient of traditional Chinese medicine formulation Danggui Luhui Wan, we synthesized 29 indirubin-3'-monoximes and preliminarily evaluated their antibacterial activities. The antibacterial activity results demonstrated that the synthesized indirubin-3'-monoximes 5a-5z and 5aa-5ad displayed good potency against S. aureus ATCC25923 (MIC = 0.4-25.6 μg mL-1). Among them, we found that the 5-F, 5-Cl and 7-CF3 substituted indirubin-3'-monoximes 5r, 5s and 5aa also showed better antibacterial efficiency for S. aureus (MICs up to 0.4 μg mL-1) than the prototype natural product indirubin (MIC = 32 μg mL-1). More importantly, indirubin-3'-monoxime 5aa has certain synergistic effect with levofloxacin against clinic multidrug-resistant S. aureus (fractional inhibitory concentration index: 0.375). In addition, relevant experiments including electron microscopy observations, PI staining and the leakage of extracellular potassium ions and nucleic acid (260 nm) have been performed after treating S. aureus with indirubin-3'-monoxime 5aa, and the results revealed that indirubin-3'-monoximes could increase the cell membrane permeability of S. aureus. Although indirubin-3'-monoxime 5aa showed some cytotoxicity toward SH-SY5Y cells relative to compounds 5r and 5s, the skin irritation test of male mice after shaving showed that compound 5aa at a concentration of 12.8 μg mL-1 had no toxicity to mouse skin, and it could be used as a leading compound for skin antibacterial drugs.
... The most widely cultivated species was Indigofera tinctoria Mill. The large-scale cultivation of Indigofera tinctoria began in India in the 16th century and spread through the Mediterranean to southern Europe and northern Africa and then to Central America and the Antilles [37]. Persicaria tinctoria (Aiton) H. Gross (ex. ...
Since ancient times, indigo has been one of the most widely used natural pigments for textile dyeing. In Europe, the only source of indigo dye was from woad (Isatis tinctoria). Woad leaves were processed to obtain an insoluble indigo pigment, which had to be reduced to leuco-indigo to dye textiles. Today, most indigo comes from the chemical industry, the production of which raises public health and ecological problems. For the past few years, renewed interest in natural pigments has led to the revival of I. tinctoria cultivation for indigo pigment production. However, the woad blue is still obtained with uncontrolled and inconsistent yields. The aim of the following paper is to provide an overview of what is known about the production of the woad blue pigment, from the leaves of I. tinctoria to its use as a dye, from medieval times to the present day. Despite numerous studies, the behaviour of the woad indigogenic precursors and the mechanisms leading to indigo formation remain unclear.
Introduction:
Abundant evidence suggests that the overexpression of CDK2-cyclin A/E complex disrupts normal cell cycle regulation, leading to uncontrolled proliferation of cancer cells. Thus, CDK2 has become a promising therapeutic target for cancer treatment. In recent years, insights into the structures of the CDK2 catalytic site and allosteric pockets have provided notable opportunities for developing more effective clinical candidates of CDK2 inhibitors.
Area covered:
This article reviews the latest CDK2 inhibitors that have entered clinical trials and discusses the design and discovery of the most promising new preclinical CDK2 inhibitors in recent years. Additionally, it summarizes the development of allosteric CDK2 inhibitors and CDK2-targeting PROTACs. The review encompasses strategies for inhibitor and PROTAC design, structure-activity relationships, as well as in vitro and in vivo biological assessments.
Expert opinion:
Despite considerable effort, no CDK2 inhibitor has yet received FDA approval for marketing due to poor selectivity and observed toxicity in clinical settings. Future research must prioritize the optimization of the selectivity, potency, and pharmacokinetics of CDK2 inhibitors and PROTACs. Moreover, exploring combination therapies incorporating CDK2 inhibitors with other targeted agents, or the design of multi-target inhibitors, presents significant promise for advancing cancer treatment strategies.
This study was conducted to analyze the antiviral activity of flavonoid compounds of Fabaceae (Clitoria ternatea, Caesalpinia sappan, Leucaena leucocephala, Indigofera tinctoria) and Asteraceae (Eclipta prostrata, Artemisia vulgaris, Blumea balsamifera, Chromolaena odorata) against SARS-CoV-2 on spike protein, Mpro and RdRp receptors by molecular docking method in silico. The results of molecular docking with AutoDock Vina showed that the flavonoid compounds semiglabrin (-7,5 kcal/mol) and pseudosemiglabrin (-7,0 kcal/mol) has binding energy better than native ligand NAG (-4,9 kcal/mol) and ceftriaxone (-6,8 kcal/mol) as a standard drug against the spike protein receptor. Flavonoid compounds juglanin (-8,5 kcal/mol) and glabratephrin (-8,5 kcal/mol) has binding energy close to the native ligand 4WI/nirmatrelvir (-8,7 kcal/mol) against Mpro receptor. Flavonoid juglanin (-9,5 kcal/mol) has binding energy better than native ligan 1RP/favipiravir (-8,3 kcal/mol) and remdesivir (-8,7 kcal/mol) as a standard drug, while flavonoid apigetrin (-8,7 kcal/mol) has binding energy better than native ligand and has the same binding energy with remdesivir as a standard drug against RdRp receptor.
Background:
Makran is a semi-desert coastal strip that extends from southeastern Iran to Baluchestan, Pakistan, on the coast of the Oman Sea. This region has a special place in the country and enjoys the cultural diversity of the Baluch people.
Aim:
As no specific ethnopharmacological data are available for the Makran coastline, the present work was undertaken to document and analyze traditional knowledge of medicinal approaches used by Baluch communities (Chabahar and Konarak counties) during 2021-2023 in the Sistan and Baluchestan province.
Methods:
Data were collected through direct observations during comprehensive field surveys, comprehensive questionnaires, and interviews with local traditional practitioners, herbal healers, and grocery and itinerant sellers of medicinal plants and minerals.
Results:
Because of its strategic location, ethnomedicine knowledge of this area has been influenced by Indian and Pakistani medicine and has been endowed with a marvelous diversity of therapeutic approaches, such as Unani or Ayurvedic systems of traditional medication for the treatment of different diseases. Herbal integration, mineral (kushtas), mud, and music and heat therapy are examples of medicinal approaches utilized in the study area. A total of 74 potential medicinal plants belonging to 41 families and 6 mineral drugs have been identified to be traditionally used for remedial measures against special diseases. The inventory of medicinal plants showed that Fabaceae, Solanaceae, and Malvaceae dominated other plant families. Out of the total documented species in this area, some species were used as medicine in at least two or further forms in the local communities. The results have shown that musculoskeletal (SKE-L), digestive (GAS-D), and respiratory (RES-R) diseases have high ICF (>0.90). In terms of temperament, 37% of the medicinal plants used in this region have been found to be hot and dry, 28% hot and moist, and 25% cold and dry. Also, 77% of the medicinal plants have been found to have two degrees of toxicity. Spearman's correlation showed a moderate correlation between temperament and phytochemical compounds (r=0.31). Comparing our data with ethnopharmacological references in Iran revealed that applications of minerals (kushtas) have not been investigated in other provinces and are significant in this region.
Conclusion:
The culture of the coast of Makran is rich in the local knowledge of traditional medicine. In addition to herbal medicines, mineral substances are also used in this area, which are a good source for the treatment of various ailments. The Unani medical system and the composition of herbal medicine (multi-ingredients) are the main features of medicinal methods used at the Makran coastline. The variety of treatment methods used by the Baluch people can suggest a suitable candidate for finding drugs.
This study is the first to report the foliar and stem epidermal micro-morphology of 13 taxa of Indigofera L. (Fabaceae) using light (LM) and scanning electron microscopy (SEM). The micro-morphological characteristics studied here are related to the epidermal cell shape, size, frequency, anticlinal wall pattern, and stomatal complex types, size, position, frequency, and index. The study revealed 19 major normal stomatal types with eight subtypes and seven major abnormal stomatal types with 13 subtypes. The stomatal index was lower on the abaxial leaf surface than on the adaxial surface. Notably, the adaxial surface of I. hochstetteri had the highest stomatal index (27.46%), while the abaxial surface of I. oblongifolia had the lowest (9.95%). The adaxial surface of I. hochstetteri also displayed the highest average stomatal frequency (38.67), while the adaxial surface of I. spinosa had the lowest average frequency (9.37). SEM analysis revealed that most leaves had slightly sunken to sunken stomata, while stem stomata were positioned at the same level as epidermal cells in most taxa. Indigofera's foliar and stem epidermal anatomy recommends their application as baseline data coupled with other taxonomic data for the delimitation and differentiation of closely related taxa in the genus. The study provides a comprehensive description, illustrations, images, and micrographs of the stomatal types, as well as a taxonomic key for distinguishing the studied taxa of Indigofera.
The bioactive extracts of traditional medicinal plants are rich in polyphenols and help to rejuvenate skin. The study was designed to assess the skin rejuvenating effects of a stable cream enriched with 4% I. argentea (IaMe) extract. The quantity of polyphenols by spectrophotometric methods was TPC, 101.55 ± 0.03 mg GAE/g and total flavonoid content; 77.14 ± 0.13 mg QE/g, while HPLC-PDA revealed gallic acid; 4.91, chlorogenic acid 48.12, p-coumaric acid 0.43, and rutin 14.23 μg/g. The significant results of biological activities were observed as DPPH; 81.81% ± 0.05%, tyrosinase; 72% ± 0.23% compared to ascorbic acid (92.43% ± 0.03%), and kojic acid (78.80% ± 0.19%) respectively. Moreover, the promising sun protection effects Sun protection factor of extract (20.53) and formulation (10.59) were observed. The active cream formulation (w/o emulsion) was developed with liquid paraffin, beeswax, IaMe extract, and ABIL EM 90, which was stable for 90 days as shown by various stability parameters. The rheological results demonstrated the active formulation’s non-Newtonian and pseudo-plastic characteristics and nearly spherical globules by SEM. The IaMe loaded cream was further investigated on human trial subjects for skin rejuvenating effects and visualized in 3D skin images. Herein, the results were significant compared to placebo. IaMe formulation causes a substantial drop in skin melanin from −1.70% (2 weeks) to −10.8% (12 weeks). Furthermore, it showed a significant increase in skin moisture and elasticity index from 7.7% to 39.15% and 2%–30%, respectively. According to the findings, Indigofera argentea extract has promising bioactivities and skin rejuvenating properties, rationalizing the traditional use and encouraging its exploitation for effective and economical cosmeceuticals.
This contribution insight on the cytotoxic and anticancer activities and molecular mechanism of phyto‐reduced silver nanoparticles (AgNPs) in MCF‐7 breast cancer cell lines. A simple, entirely green synthesis process was optimized for the phyto‐reduction of AgNP (~12.7 nm) using aqueous leaf extracts of Indigofera heterantha . The structural and vibrational properties of biosynthesized AgNPs were extensively characterized using UV–Vis spectrophotometer, x‐ray diffraction (XRD), dynamic light scattering (DLS), and Fourier transform Infrared spectroscopy (FTIR), while their shape and morphology was studied through scanning electron microscopy (SEM). The 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) cell viability assay indicates concentration dependent inhibition with IC 50 , 27.93 ± 2.10 μg/mL against MCF‐7 cells and 294.38 ± 3.87 μg/mL against L929 cells. The manifested anticancer mechanism in MCF‐7 cells was extensively studied using Acridine orange/ethidium bromide (AO/EB), 4′,6‐diamidino‐2‐phenylindole (DAPI) and Annexin‐V/propedium iodide fluorescence microscopic assays. The level of reactive oxygen species (ROS) was measured using DCFH‐DA fluorescent spectroscopy. Overall, the results show that AgNPs exhibit cytotoxic and apoptotic effect on breast cancer MCF‐7 cells by damaging membrane integrity and nuclear fragmentation due to oxidative stress generated by elevated level of ROS.
Research Highlights
Biomimetic synthesis of nano dimension size silver nanoparticles (AgNPs).
Characterization of AgNPs through UV–Vis, DLS, XRD, FTIR, and SEM.
Cytotoxic and anticancer effects of the biosynthesized AgNPs in L929 fibroblast cells and MCF7 breast cancer respectively.
Determination of morphological, and nuclear changes triggered by AgNPs in MCF 7 breast cancer cells using fluorescent microscopy and flow cytometry.
Apoptosis induction by AgNPs in cancer cells through oxidative stress generated by reactive oxygen species (ROS).
Plants known as salaon ( Indigofera tinctoria L.) are commonly employed in conventional medicine. Salaon leaves have secondary metabolites sunch as alkaloid, flavonoid, tannin, glycoside, phenol, saponin and triterpenoid levels have benefit as antioxidants in counteracting free radicals. The aimed of this research was to investigate the Antioxidant properties of The EESL, NHFSL and EAFSL. Phytochemical investigation process was used on extracts and fractions. Antioxidant properties was determined using the DPPH technique and a UV/Vis spectrophotometer at 515 nm. The water level of salaon leaf simplicia was around 9.32%; water-soluble extract of 34.70%, ethanol-soluble extract of 23.94%, total ash of 8.57% and acid insoluble ash of 1.38%. Alkaloids, flavonoids, glycosides, tannins, saponins, steroids, and triterpenoids were found in the phytochemical investigation of EESL. The EESL, NHFSL and EAFSL which were tested for antioxidant properties revealed IC 50 values of (70.5046 ± 0.0409; 77.2190 ± 0.0021; 56.5593 ± 0.0120) µg/mL. IC 50 value of quercetin in the extremely strong category is 2.5424± 0.0010 µg/mL. The results of this investigation indicate that salaon leaf ethanol extract, n-hexane, and ethyl acetate fraction have potent antioxidant properties.
This review compiles diverse plant materials and their phytoconstituents, exploring their potential as antidiabetic agents. It aims to highlight recent advancements in the field, showcasing various plants and their bioactive compounds that have shown promise in managing diabetes.
Pharmacologically screened components from plants like Phyllanthus urinaria, Indigofera tinctoria, Trichosanthes kirilowii, Ziziphus jujuba, Curcuma longa, Gymnema sylvestre, Momordica charantia, Camellia sinensis (green tea), berberine-containing plants, quercetin sources, resveratrol-rich plants, and Allium genus extracts exhibit diverse mechanisms in regulating glucose metabolism. These mechanisms include enhancing insulin sensitivity, stimulating insulin secretion, inhibiting carbohydrate-digesting enzymes, and improving glucose uptake by cells.
Despite the potential benefits of these plant-derived compounds in managing diabetes, challenges arise when incorporating them into antidiabetic products, affecting attributes like color, taste, and texture. Thus, adjustments in processing parameters become essential for effectively integrating these materials into diabetic-friendly products. This review underscores the potential of plant-derived materials in diabetes management while acknowledging the need for further research to optimize their use in developing effective and palatable antidiabetic interventions.
Ethno-botanical survey was conducted during the month of October to December 2021 in 6 villages (Bhalabari, Simlibari, Khoirabari, Banseria, Angrajuli and Bagchai chuburi) of Udalguri district of BTR for a better understanding of local beliefs, habits and culinary practices regarding the use of medicinal plants for treatment of obesity. During the ethno-medicinal survey period the well known medicinal practitioners called as "Buwidw" were contacted and appraised regarding the purpose of the study and other ethno-medicinal information were gathered. Local healers or buwidw were interviewed using structured questionnaire. Owing to their prior experiences being exploited by business associates of pharmaceutical and drug companies, some respondents were occasionally reluctant to impart their knowledge of medicinal plants and less receptive to being the focus of outsiders' and visitors' investigations. Altogether 12 local healers or buwidw were interviewed from the randomly selected villages. From the survey, 15 medicinal plants were collected that are mainly used for treatmentof obesity. Out of these 15 plants most cited plants were found to be Alstonia scholaris (L.) R.Br. (Apocynaceae) and Syzygium cumini (L.) Skeels (Myrtaceae). This explorative survey underscores the importance of preserving and documentation of indigenous plants for further scientific investigations.
Blue color and medicinal plants – a few words about indigo and more Until the development of organic chemistry and the production of synthetic dyes in the second half of the 19th century, substances of natural origin were the only source of color compounds. These could be mineral, plant, and animal products, used in the form of raw products (e.g., crushed metals, minerals, animal fragments, or their excretions) and preparations derived from them. Among the plants we find many species that have been used as sources of coloring substances. They were valued primarily in the production of various utility or decorative fabrics and were used to dye natural fibers. Plant extracts or purified fractions of color compounds were also used as pigments in painting, in the illumination of books, and as substances that improve the look of medicines or foodstuffs. Some had medicinal significance per se. Among them, a small group of plant substances with a blue color is of special interest. The most famous natural raw material of this group is indigo (Indigo), obtained from Indigofera tinctoria L. and its substitutes. Noteworthy is also the less known wood of the logwood (Haematoxylum campechianum L.), known as the blue tree. This work presents the history, uses, and therapeutic importance of the abovementioned raw materials and their contemporary use.
Traditionally, selected plant sources have been explored for medicines to treat convulsions. This continues today, especially in countries with low-income rates and poor medical systems. However, in the low-income countries, plant extracts and isolated drugs are in high demand due to their good safety profiles. Preclinical studies on animal models of seizures/epilepsy have revealed the anticonvulsant and/or antiepileptogenic properties of, at least some, herb preparations or plant metabolites. Still, there is a significant number of plants known in traditional medicine that exert anticonvulsant activity but have not been evaluated on animal models. Zebrafish is recognized as a suitable in vivo model of epilepsy research and is increasingly used as a screening platform. In this review, the results of selected preclinical studies are summarized to provide credible information for the future development of effective screening methods for plant-derived antiseizure/ antiepileptic therapeutics using zebrafish models. We compared zebrafish vs. rodent data to show the translational value of the former in epilepsy research. We also surveyed caveats in methodology. Finally, we proposed a pipeline for screening new anticonvulsant plant-derived drugs in zebrafish ("from tank to bedside and back again").
Liver X receptor alpha (LXRα) is a nuclear receptor family member that is expressed in the liver, and has gained pharmacological interest for its role in the reduction of atherosclerosis, a long-term inflammatory disorder that affects the artery wall and is characterized by alterations in lipid metabolism. LXRα activators appear to be promising targets for preventing and/or treating these pathological conditions. The current work intends to perform a computational analysis of the IMPPAT database with LXRα. This comprehensive study will serve as a foundation for the investigation of novel plant-derived LXRα agonists against atherosclerosis. LXRα (PDB ID: 3IPU) was used as a target molecule for docking analysis. The docking scores of top five phytocompounds from the IMPAAT database, namely Betaxanthin, Adlumidiceine, Miraxanthin III S, Lupinisoflavone E, and p -Coumaroyl triacetic acid, ranged from - 35.88 kcal/mol to - 32.46 kcal/mol. The docking analysis was validated further by a 100 ns molecular dynamics study, which revealed fewer fluctuations in RMSD along with stable intermolecular interactions of lead phytocompounds with the targeted LXRα protein. The enrichment calculation metrics also validated the efficiency of the docking procedure. As evidenced by the MM-GBSA study, the binding free energies (ΔG bind ) score up to -71.219 kcal/mol, with no violations in terms of drug likeliness and ADMET predictions, indicated the promising nature of these phytocompounds as drug candidates against atherosclerosis. These in silico studies, in particular, aid in analyzing phytocompounds roles as potential lead drugs, paving the way for in vitro and in vivo assessments for the development of novel anti-atherosclerosis drugs.
Introduction
Indigofera L. is the third largest genus in Fabaceae and includes economically important species that are used for indigo dye-producing, medicinal, ornamental, and soil and water conservation. The genus is taxonomically difficult due to the high level of overlap in morphological characters of interspecies, fewer reliability states for classification, and extensive adaptive evolution. Previous characteristic-based taxonomy and nuclear ITS-based phylogenies have contributed to our understanding of Indigofera taxonomy and evolution. However, the lack of chloroplast genomic resources limits our comprehensive understanding of the phylogenetic relationships and evolutionary processes of Indigofera.
Methods
Here, we newly assembled 18 chloroplast genomes of Indigofera. We performed a series of analyses of genome structure, nucleotide diversity, phylogenetic analysis, species pairwise Ka/Ks ratios, and positive selection analysis by combining with allied species in Papilionoideae.
Results and discussion
The chloroplast genomes of Indigofera exhibited highly conserved structures and ranged in size from 157,918 to 160,040 bp, containing 83 protein-coding genes, 37 tRNA genes, and eight rRNA genes. Thirteen highly variable regions were identified, of which trnK-rbcL, ndhF-trnL, and ycf1 were considered as candidate DNA barcodes for species identification of Indigofera. Phylogenetic analysis using maximum likelihood (ML) and Bayesian inference (BI) methods based on complete chloroplast genome and protein-coding genes (PCGs) generated a well-resolved phylogeny of Indigofera and allied species. Indigofera monophyly was strongly supported, and four monophyletic lineages (i.e., the Pantropical, East Asian, Tethyan, and Palaeotropical clades) were resolved within the genus. The species pairwise Ka/Ks ratios showed values lower than 1, and 13 genes with significant posterior probabilities for codon sites were identified in the positive selection analysis using the branch-site model, eight of which were associated with photosynthesis. Positive selection of accD suggested that Indigofera species have experienced adaptive evolution to selection pressures imposed by their herbivores and pathogens. Our study provided insight into the structural variation of chloroplast genomes, phylogenetic relationships, and adaptive evolution in Indigofera. These results will facilitate future studies on species identification, interspecific and intraspecific delimitation, adaptive evolution, and the phylogenetic relationships of the genus Indigofera.
Background
A novel coronavirus COVID-19 outbreak causing infectious respiratory disorders. COVID-19 disease has no specific treatment. In the traditional medicinal system, different formulations are available for infectious diseases.
Objective
This review discusses the significance and utilization of Siddha and Ayurvedic herbal formulations for COVID-19 treatment and provides scientific information regarding the phytochemistry and pharmacological profiles of Indian medicinal plants used in the formulation.
Method
The information on medicine and medicinal plants was collected from research papers, review papers, and books available in several electronic databases, including Google Scholar, SpringerLink, and PubMed was explored as information sources.
Results
Traditional medicinal plants are potentially used in formulations due to their inevitable therapeutic properties. Phytochemistry and pharmacological properties of medicinal plants used in the formulations served as scientific proof for traditional medicine.
Conclusion
The present study explored the great importance of Siddha and Ayurvedic formulations for COVID-19 treatment. Further scientific investigations are a need to explore these formulations as widely acceptable.
[Abstract]
Objective
To explore the anti-inflammatory phytoconstituents from various plant sources as tumour necrosis factor-α (TNF-α)-inhibitor, a mediator involved in the inflammatory disorder, by in silico molecular docking.
Methods
Based on previous findings, we performed the in silico assessment of anti-inflammatory phytoconstituents from different medicinal plants to understand their binding patterns against TNF-α (PDB ID: 6OP0) using AutoDock Vina. Molecular docking was performed by setting a grid box (25 × 25 × 25) Å centered at [– 12.817 × (– 1.618) × 19.009] Å with 0.375 Å of grid spacing. Furthermore, Discovery Studio Client 2020 program was utilized to assess two- and three-dimensional (2D and 3D) hydrogen-bond interactions concerning an amino acid of target and ligand. Physicochemical properties were reported using the Lipinski’s rule and SwissADME database to support the in silico findings. Results From the selected medicinal plants, more than 200 phytocompounds were screened against TNF-α protein with binding scores in the range of – 12.3 to – 2.5 kcal/mol. Amongst them, emodin, aloe-emodin, pongamol, purpuritenin, semiglabrin, ellagic acid, imperatorin, α-tocopherol, and octanorcucurbitacin A showed good binding affinity as – 10.6, – 10.0, – 10.5, – 10.1, – 11.2, – 10.3, – 10.1, – 10.1, and – 10.0 kcal/mol, respectively. Also, the absorption, distribution, metabolism, excretion, and toxicology (ADMET) profiles were well within acceptable limits.
Conclusion
Based on our preliminary findings, we conclude that the selected phytoconstituents have the potential to be good anti-inflammatory candidates by inhibiting the TNF-α target. These compounds can be further optimized and validated as new therapeutic components to develop more effective and safe anti-inflammatory drugs.
Indigofera genus is the third biggest genus that has many commercial species. Indigo plants are also
famous for their protective and anti-inflammatory applications on gastrointestinal tract. In the
present investigation, ethanolic extracts of Indigofera cordifolia,andIndigoferaglandulosawere
investigated foracute oral toxicity and in-vivo anti-inflammatory activity usingCarrageenan-induced
rat paw edema.The results show that both plants displayed no significant abnormality even at
2,000mg/kg body weight. On the otherhand,Indigofera cordifolia demonstrated the highest
inhibition of inflammation of 65.384% thanIndigoferaglandulosa48.275%.The anti-inflammatory
activity of the ethanolic extracts of both plants may be attributed to flavonoids and alkaloids.
Covering: upto 2022Natural products have an embedded recognition of protein surfaces. They possess this property as they are produced by biosynthetic enzymes and are substrates for one or more enzymes in the biosynthetic pathway. The inherent advantages, compared to synthetic compound libraries, is this ligand-protein binding which is, in many cases, a function of the 3-dimensional properties. Protein degradation is a recent novel therapeutic approach with several compounds now in the clinic. This review highlights the potential of PROteolysis TArgeting Chimeras (PROTACs) in the area of natural products. The approach will complement existing approaches such as the direct use of a bioactive natural product or its analogues, pharmacophore development and drug-antibody conjugates. The chemical synthesis and challenges of using natural product-based PROTACs are summarised. The review also highlights methods to detect the ternary complexes necessary for PROTAC mechanism of action.
Cardiovascular diseases (CVDs) are the leading cause of global mortality, including deaths arising from non-communicable diseases in sub-Saharan Africa (SSA). Consequently, this study aimed to provide details of medicinal plants (MPs) employed in SSA for the treatment of CVDs and their related risk factors to open new avenues for the discovery of novel drugs. The extensive ethnopharmacological literature survey of these MPs in 41 SSA countries was based on studies from 1982 to 2021. It revealed 1,085 MPs belonging to 218 botanical families, with Fabaceae (9.61%), Asteraceae (6.77%), Apocynaceae (3.93%), Lamiaceae (3.75%), and Rubiaceae (3.66%) being the most represented. Meanwhile, Allium sativum L., Persea americana Mill., Moringa oleifera Lam., Mangifera indica L., and Allium cepa L. are the five most utilised plant species. The preferred plant parts include the leaves (36%), roots (21%), barks (14%), fruits (7%), and seeds (5%), which are mostly prepared by decoction. Benin, Mauritius, Nigeria, South Africa, and Togo had the highest reported use while most of the investigations were on diabetes and hypertension. Despite the nutraceutical advantages of some of these MPs, their general toxicity potential calls for caution in their human long-term use. Overall, the study established the need for governments of SSA countries to validate the efficacy/safety of these MPs as well as provide affordable, accessible, and improved modern healthcare services.
Importance of phenology has increased in view of global climate change. Reproductive phenology is responsible for success in seed production and thereby perpetuation of a species. Phenological studies were not given much importance,especially in the region of Holalkere and Hosadurga of chitraduga district of Karnataka state. Hence, attempt was made to study the phenological aspects of the genus Indigofera L. of sub family papilionoideae in the study area. The phenophases viz., leafing, flowering and fruiting and leaf fall are observed for 10 recorded species of the genus Indigofera. The regular Phenological period of the majority of genus was studied,variation in the phenophases of some small herbs and undershrubs was noticed with respect to its ecology. This investigation gives phenological database of the economically important genus Indigofera of the study area. This database can be also utilized, besides this importance, in future, in planning and management of conservational measures in the region.
A strategy that has the potential to contribute to the achievement of the targets established under SDG 8 (“Decent Work and Economic Growth”) involves the development of sustainable tourism to create productive job and livelihood opportunities and to promote local culture and products. In the province of East Nusa Tenggara (NTT), Indonesia, ikat weaving is an integral part of the cultural heritage of the region, with ikat characterized by unique design motives and the use of natural dyes. Unfortunately, in some areas, the use of natural dyes is diminishing as a result of competition with synthetic dyes and the limited availability of raw materials, particularly for the production of blue dye. The development of Indigofera spp. to produce natural, plant-based blue dye has significant potential to contribute to community incomes and employment. This study outlines a strategy for developing the use of Indigofera spp. as a natural dye and describes its potential for contributing to community incomes, especially on Timor Island, NTT. The study shows that weavers currently use indigo plants that grow naturally in gardens and yards. Although the community has a tradition of using these plants, informed by local wisdom, to develop the cultivation and processing of this plant through the application of the appropriate techniques, including innovative approaches to producing indigo paste, could enable the development of Indigofera spp. cultivation on a larger scale. The study shows that the availability of suitable land is high (±370 thousand ha), with 80% of the suitable land being categorized as critical. The study proposes a development based on the analysis of strengths, weaknesses, opportunities, and threats to assess the manner in which these opportunities could be leveraged with the support and participation of local communities and other stakeholders by leveraging the culture and wisdom of the community regarding the use of Indigofera spp.
Indigoferasuffruticosa Mill. (Fabaceae) is known as anil or anileira and also with other names, due to the production of a blue pigment, which is commonly used for yarn dyeing. It is distributed in some states of Brazil (Pernambuco, Paraíba, Mato Grosso, São Paulo, Bahia, Pará, and others) and is used in the popular medicine as a febrifuge, antispasmodic, diuretic, abortive, analgesic, purgative, or soothing agent against stomach and urinary problems, jaundice, and ulcers and also as an insecticide. In addition, I. suffruticosa can be used as animal feed. This review aimed at providing important data on the botanical, distribution, ethnopharmacology, phytochemical, pharmacological, and toxicity of I. suffruticosa based on the scientific literature. Information on I. suffruticosa was gathered via the Internet (from Elsevier, NCBI, and Sci-Hub) and libraries in the period from February to March 2016. More than 40 chemical compounds have been identified and a few compounds isolated, and the main origins are the essential oils, organic extracts, and aqueous extracts of different parts of the plant. I. suffruticosa and its active compounds possess wide pharmacological actions in the literature, such as anti-inflammatory, antibacterial, antifungal, antioxidative, antitumor, antimutagenic, anticonvulsant, gastroprotective, and hepatoprotective activities. Therefore, as an important traditional popular medicine, further studies on I. suffruticosa are required for the development of new drugs and therapeutics for various diseases.
Despite the use of ethnobotanical remedies to manage human immunodeficiency virus/acquired immune deficiency syndrome (HIV/AIDS), there is paucity of empirical data on the specific plant species used by traditional healers to manage HIV/AIDS opportunistic infections in Zambia. Therefore, this study documented putative plant species used to manage HIV and AIDS-related opportunistic diseases in Lusaka, Zambia. Exploratory, semi-structured interviews and detailed descriptive studies of 40 traditional healers were conducted. The following ethnobotanical data were recorded: plant species, parts used, modes of preparation, administration, and diseases treated. Data were analyzed by calculating percentage frequencies, familiarity index (Fi), and informant consensus factor (FIC). A total of 84 plant species from 38 families, mostly the Fabaceae, were used as ethnomedicines. Roots, leaves and stem bark were mostly harvested for the treatment of STIs including HIV, skin infections, diarrhea, malaria, tuberculosis, persistent cough, erectile dysfunction, oral infections, cancer and weight loss. Thirteen plants were used to manage three different diseases: Abrus precatorius, Albizia anthelmintica, Carica papaya, Cassia abbreviata, Combretum elaeagnoides, Flueggea virosa, Mimosa pigra, Mundulea sericea, Musa acuminata, Piliostigma thonningii, Ricinus communis, Securidaca longepedunculata, and Syzygium guineense. Garcinia livingstonei, Kigelia africana, Peltophorum africanum and Ziziphus mucronata were individually used to manage four different disease conditions. Only Plumbago zeylanica was used to manage five different disease conditions. These multi-use plants may have broad antimicrobial activities but risk over-exploitation. The results of this study urge a fundamental rethink of how patients and public health authorities view traditional plant medicines for HIV/AIDS management in Lusaka, Zambia.
In Tanzania, about 10% of the reported 12,000 species of higher plants are estimated to be used as medicine for treating different human health problems. Most of the medicinal plants are collected from wild populations, but their trade and quantities are not properly recorded. Monitoring of trade in wild-harvested medicinal plants is challenging as most materials are traded in various processed forms and most vendors practice informal trade. Yet, monitoring is important for conservation and sustainability. This study aims to assess the trade of wild-harvested medicinal plant species in local markets of Tanzania and its implications for conservation. Semi-structured interviews were used to record frequency, volume of trade and uses of wild-harvested medicinal plants in Arusha, Dodoma, Mbeya, Morogoro and Mwanza regions. Relative frequency of citation and informant consensus factor were calculated for each species and mentioned use category. Forty vendors were interviewed, and 400 out of 522 collected market samples were identified to 162 species from herbarium-deposited collections. Plant parts with the largest volume of trade were roots (3818 kg), bark (1163 kg) and leaves (492 kg). The most frequently traded species were Zanthoxylum chalybaeum Engl., Albizia anthelmintica Brongn., Zanha africana (Radlk.) Exell, Warburgia stuhlmannii and Vachellia nilotica (L.) P.J.H.Hurter & Mabb. The most popular medicinal plants in the markets are connected to local health problems including malaria, libido disorders or infertility. The high diversity of commercialized plants used for medicinal issues mainly relies on wild stock for local consumption and international trade, and this has significant implications for conservation concerns.
OBJECTIVE: To pool data on ethnobotanical medicine for the treatment of inflammatory disorders in Pakistan.
METHODS: We reviewed 237 research publications based on data from the six provinces in Pakistan (Punjab = 85, Khyber Pakhtunkhwa = 65, Sindh = 15, Balochistan = 8, Gilgit Baltistan = 22, Azad Jammu and Kashmir = 42) published until June 2015 in various journals. This was achieved using seven online databases: ScienceDirect, Google, Google
Scholar, PubMed, Wiley Online Library, SpringerLink, and MEDLINE. Data were analyzed from different perspectives.
RESULTS: People from Pakistan made use of 371 plant species belonging to 263 genera and 99 families for the treatment of inflammatory disorders. Plants from the Asteraceae family were used most often. Herbs were the dominant growth form. Leaves were the plant parts used most often. Decoctions were the main preparation method. Nine plant species were used most frequently in the dwellers of most regions of Pakistan. A total of 111 plants were shown experimentally to have neither anti-arthritic nor anti-inflammatory activities, and 148 plant species were threatened. Eighty-four species had commercial importance. Twelve plant species were imported, and 25 plant species were exported, from Pakistan.
CONCLUSION: This review provides baseline data for plant species in Pakistan that have potential anti-inflammatory/anti-arthritic activities.
The aim of this study was to screen the antimicrobial and acaricidal activity of 20 endemic or indigenous plants from Reunion Island (Indian Ocean). Plants were chosen on the basis of their traditional uses and their biocidal activities found in the literature. A survey was conducted in the local population to assess and supplement knowledge about the selected plants. The collected information confirmed and/or supplemented the data obtained for nine plants. Seven plants were described for the first time for their traditional uses in medicine and ethnoveterinary practices. To evaluate their biocidal activities, leaves or bark were treated with ethyl acetate using an accelerated solvent extraction method. Six bacteria and five fungi, frequently implicated in infectious diseases, were used to assess the antimicrobial activity of these extracts. A preliminary screening using the paper disk diffusion assay showed an effective antibacterial activity of 16 extracts. The minimum inhibitory concentration (MIC) of active plant extracts was then determined using a microdilution method. The leaf extract from Peperomia borbonensis displayed the widest spectrum of antibacterial activity and was the only one to act as a fungicide. In parallel, acaricidal bioassays were performed on the larvae of the tick Rhipicephalus microplus (Ixodidae), and plant extracts from Peperomia borbonensis and Zanthoxylum heterophyllum were the most effective. The preliminary studies of these plant extracts exhibited biocidal activities that were not described in the literature and that are congruent with traditional uses for some of them. Investigations are currently being conducted to isolate the active compound(s) and evaluate their potential for future developments and applications.
The search for new antimicrobial agents for the management of infections is of increasing interest because of the intense growing resistance of antibiotics to bacteria. Eighteen medicinal plants’ extracts, these plants belonging to different families were fractionated using different solvents with varying polarity (hexane, chloroform and methanol), with historical use against infections in a primary and secondary screening for activity against Candida albican, Aspergillus fumigatus, Crytococcus neoformans, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Vancomycin resistance enterococcus and Methicillin-resistance staphylococcus aureus in an in vitro assay. The methanol extract of leaves of Leptadenia hastata (IC50 (µg/mL) = 22.53 (MRS), 11.89 (VRE)) and chloroform extract of seeds of Parkia biglobosa (IC50 (µg/mL) = 28.25 (C. neoform.), 85.68 (VRE)) exhibited significant inhibition against the microbes. Though hexane fractions of P. biglobosa and Crotalaria mucronata show selective inhibition of IC50 (µg/mL) = 28.71 (C. neoform.) and 58.13 (C. alb) respectively. The antimicrobial nature of extracts from the seeds of P. biglobosa, leaves of B. ferruginea and T. preussi were ascertain in this study for the first time as far as we know. The positive results of these medicinal plants constitute vital reference for on-going phytoanalysis and biological studies.
This review is a comprehensive compilation of the ethnobotany of the Basotho (residing both in Lesotho and the Free State Province of South Africa) in its entirety. It includes all the known traditional uses ranging from food, through clothing, crafts, and textiles, to medicine and magic and is based on an extensive literature survey of both published and unpublished data from books, journals, dissertations, theses, available online databases, as well as past experiences of the authors. A total of 712 species is utilised for various purposes, comprising 22 pteridophytes and 690 flowering plants (509 dicotyledons, and 181 monocotyledons). The Asteraceae, with 115 species is the most commonly used family, followed by Poaceae (61) and Fabaceae (50). The largest number of plants (437 species) are utilised for all kinds of medical conditions (in both animals and humans) ranging from a simple cold to more complex ailments such as cancer and diabetes. There are 193 plant species utilised as food including staple food, vegetables, fruits, and beverages. Several species have functional uses such as thatching, clothing, textiles, building, cosmetics, crafts, fuel, musical instruments, and other cultural applications. 197 species are used for magic, mostly as a variety of charms, for example love charms, good luck charms, and protective charms.
Tribal community of Jhabua district uses the forest resources especially plants primarily for curing various ailments. Ethnobotanical practice has prevailed in this area since the ancient time and the invasive plants are not the exception. Thus, we documented the medicinal uses of the invasive plants. Exhaustive field surveys were conducted during 2008–2013 for the collection of the ethnobotanical data and voucher specimen. Information regarding ethnobotanical uses of plants was collected from the tribals using a semi-structured questionnaire. Several extensive reviews which studied invasive plant species are available. From this survey, a total of 102 plant species belonging to 38 families were reported for curing 37 types of ailments. Asteraceae was the dominant family and in lifeform category herbs stand dominant. Leaf is the most frequently used plant part, whereas decoction is the highly preferred preparatory method for medicine preparation in the study area. 56% of the invasive plants showed a use value of more than 0.50. This indicates the high acceptance of these plants in the primary health care. We also discussed the degree of invasiveness and habitat preference of these species. The use of invasive alien plant species relieves the pressure on the native plant species that leads to the native plant diversity conservation. Finding of this study can be used as an ethnopharmacological basis for selecting plants for future phytochemical pharmacological studies.
In this review, the existing literature data on the phytochemical and biological studies of the genus Indigofera are outlined with 71 references. Up till now, 65 compounds were secluded from various species of genus Indigofera. The chemical components are mostly terpenoids, flavonoids and nitro group containing compounds, together with steroids and others. The metabolites and crude extracts of the genus indigofera were found to exhibit various bioactivities including, antimicrobial, insecticidal, phytotoxic, antiulcergenic, hepatotoxic, teratogenic and cytotoxicity. Other constituents isolated from the genus Indigofera displayed inhibitory activity against the enzyme lipoxygenase and gastrointestinal activity. This review represents a brief description of the total Phytochemical and Pharmacological activities of genus Indigofera as well as chemotaxonomic classification of chemical constituents
Indigofera tinctoria and Scoparia dulcis are being widely used in Indian folk medicine for the treatment of various disorders. Environmental noise pollution is thought to be an important factor for many health problems and it causes immune abnormalities. In the present study immune-regulating potential of I. tinctoria and S. dulcis aqueous extracts on innate and adaptive immune system of wistar albino rats was evaluated during normal and chronic noise induced stress conditions. The results demonstrated that both I. tinctoria and S. dulcis aqueous extracts (200mg/kg b.w) showed immunostimulant effect on both innate and adaptive immune response of wistar albino rat compared to control group under normal condition. The noise stress (100dB for 1hour, 20 days) induced animals showed suppressive effects on immune response by decreasing macrophage phagocytosis, antibody secretion by spleen cells, humoral immune response, proliferation of lymphocytes, cytotoxicity, TNF α expression, granzyme B and perforin expression in splenic NK cells. Similarly, noise stress also caused DNA damage in tissues. However, the suppressed effects induced by noise stress on rat immune system were significantly prevented by oral administration of both I. tinctoria and S. dulcis aqueous extracts. Considering all these results it is suggested that the selected medicinal plant’s aqueous extracts have the potential to prevent the effects of noise stress induced rat immune system and explore a strong immunostimulant potential applicable to clinical practices.
Background
Indigo naturalis is a Traditional Chinese Medicine (TCM) ingredient long-recognized as a therapy for several inflammatory conditions, including psoriasis. However, its mechanism is unknown due to lack of knowledge about the responsible chemical entity. We took a different approach to this challenge by investigating the molecular profile of Indigo naturalis treatment and impacted pathways.
Methods
A randomized, double-blind, placebo-controlled clinical study was conducted using Indigo naturalis as topical monotherapy to treat moderate plaque psoriasis in a Chinese cohort (n = 24). Patients were treated with Indigo naturalis ointment (n = 16) or matched placebo (n = 8) twice daily for 8 weeks, with 1 week of follow-up.
Results
At week 8, significant improvements in Psoriasis Area and Severity Index (PASI) scores from baseline were observed in Indigo naturalis-treated patients (56.3% had 75% improvement [PASI 75] response) compared with placebo (0.0%). A gene expression signature of moderate psoriasis was established from baseline skin biopsies, which included the up-regulation of the interleukin (IL)-17 pathway as a key component; Indigo naturalis treatment resulted in most of these signature genes returning toward normal, including down-regulation of the IL-17 pathway. Using an in vitro keratinocyte assay, an IL-17-inhibitory effect was observed for tryptanthrin, a component of Indigo naturalis.
Conclusions
This study demonstrated the clinical efficacy of Indigo naturalis in moderate psoriasis, and exemplified a novel experimental medicine approach to understand TCM targeting mechanisms.
Trial registration
NCT01901705.
Electronic supplementary material
The online version of this article (10.1186/s12906-017-1947-1) contains supplementary material, which is available to authorized users.
Context: Indigofera suffruticosa Miller (Fabaceae) and I. truxillensis Kunth produce compounds, such as isatin (ISA) and indirubin (IRN), which possess antitumour properties. Their effects in mammalian cells are still not very well understood.
Objective: We evaluated the activities of ISA and/or IRN on cell viability and apoptosis in vitro, their genotoxic potentials in vitro and in vivo, and the IRN- and ISA-induced expression of ERCC1 or BAX genes.
Materials and methods: HeLa and/or CHO-K1 cell lines were tested (3 or 24 h) in the MTT, Trypan blue exclusion, acridine orange/ethidium bromide, cytokinesis-blocked micronucleus (CBMN) and comet (36, 24 and 72 h) tests after treatment with IRN (0.1 to 200 μM) or ISA (0.5 to 50 μM). Gene expression was measured by RT-qPCR in HeLa cells. Swiss albino mice received IRN (3, 4 or 24 h) by gavage (50, 100 and 150 mg/kg determined from the LD50 – 1 g/kg b.w.) and submitted to comet assay in vivo.
Results: IRN reduced the viability of CHO-K1 (24 h; 5 to 200 μM) and HeLa cells (10 to 200 μM), and was antiproliferative in the CBMN test (CHO-K1: 0.5 to 10 μM; HeLa: 5 and 10 μM). The drug did not induce apoptosis, micronucleus neither altered gene expression. IRN and ISA were genotoxic for HeLa cells (3 and 24 h) at all doses tested. IRN (100 and 150 mg/kg) also induced genotoxicity in vivo (4 h).
Conclusion: IRN and ISA have properties that make them candidates as chemotherapeutics for further pharmacological investigations.
Background
The Afar people inhabit the sub-arid and arid part of Ethiopia. Recurrent drought and invasive encroaching plants are taking out plants that have cultural importance, and threaten the biodiversity and the associated traditional knowledge. Thus, the aim of the current study is to conduct an ethnobotanical survey and document medicinal and edible plants in Yalo Woreda in Afar regional state.
Methods
A cross-sectional ethnobotanical study was carried out in eight kebeles of Yalo Woreda from October 2015 to December 2016. One hundred sixty informants were selected using purposive sampling. The data on diseases, medicinal and edible plants were collected using semi-structure interview and group discussion. The statistical methods, informant consensus factor, fidelity level, and preference ranking were conducted to analyze the data.
Results
One hundred and six plants were reported; gender and age differences had implication on the number of plants reported by informants. The knowledge of medicinal plants among informants of each kebele was not different (p < 0.5) and was not associated in particular with the religious establishment in the kebeles (informant*kebeles, Eta square = 0.19). Family Fabaceae was the major plant species, and shrubs (44%) were dominant plants reported. Leaf (52.94%) and oral (68%) were primary plant part used for remedy preparation and route of application, respectively. The plants with low fidelity values Indigofera articulata (0.25), Cadaba farinosa (0.22), Cadaba rotundifolia (0.19), and Acalypha fruticosa (0.15) were used to treat the category of diseases with high informant consensus value (0.69). Sixteen edible plants were identified that were consumed during wet and dry seasons. Balanites aegyptiaca, Balanites rotundifolia, and Dobera glabra were ‘famine food’ that were collected and stored for years.
Conclusion
People in Yalo Woreda are more dependent on natural resources of the area for their livelihood. The threat of climatic change and encroaching invasive plants on medicinal and edible plants affects the traditional use of plants in the Yalo Woreda. The conservation of the plants in the home garden and natural habitat and integration of edible plants into agroforestry development programs in sub-arid and arid regions has to be encouraged to conserve plants of medical and economic importance.
Electronic supplementary material
The online version of this article (doi:10.1186/s13002-017-0166-7) contains supplementary material, which is available to authorized users.
Malaria is a major health problem that still affects numerous countries. The current study aimed to identify the role of Indigofera oblongifolia leaf extract in regulating mouse spleen macrophages during the progression of Plasmodium chabaudi infection. Three doses of the leaf extract (100, 200, and 300mg/kg) were administered to mice inoculated with P. chabaudi infected erythrocytes. The weight of the infected mice improved after the treatment with I. oblongifolia. The infection causes disorganization of macrophage distribution in the spleen. After the mice had been treated with the leaf extract, the macrophages appeared to be reorganized in the white and red pulp areas. In addition, the I. oblongifolia leaf extract (IOLE) significantly increased the total antioxidant capacity of the mice spleens infected with P. chabaudi. The phagocytic activity of spleen macrophages was increased in the infected group as indicated by the significant decrease in the number of fluorescent particles in the spleen sections. This number increased in the mice spleens after treatment with IOLE. Based on these results, it is suggested that IOLE regulate macrophage response of the spleen during the blood stage of malaria in mice.
Currently, >35 Saudi Arabian medicinal plants are traditionally used for various liver disorders without a scientific rationale. This is the first experimental evaluation of the anti-hepatitis B virus (HBV) potential of the total ethanolic and sequential organic extracts of 60 candidate medicinal plants. The extracts were tested for toxicity on HepG2.2.15 cells and cytotoxicity concentration (CC50) values were determined. The extracts were further investigated on HepG2.2.15 cells for anti-HBV activities by analyzing the inhibition of HBsAg and HBeAg production in the culture supernatants, and their half maximal inhibitory concentration (IC50) and therapeutic index (TI) values were determined. Of the screened plants, Guiera senegalensis (dichloromethane extract, IC50=10.65), Pulicaria crispa (ethyl acetate extract, IC50=14.45), Coccinea grandis (total ethanol extract, IC50=31.57), Fumaria parviflora (hexane extract, IC50=35.44), Capparis decidua (aqueous extract, IC50=66.82), Corallocarpus epigeus (total ethanol extract, IC50=71.9), Indigofera caerulea (methanol extract, IC50=73.21), Abutilon figarianum (dichloromethane extract, IC50=99.76) and Acacia oerfota (total ethanol extract, IC50=101.46) demonstrated novel anti-HBV activities in a time- and dose-dependent manner. Further qualitative phytochemical analysis of the active extracts revealed the presence of alkaloids, tannins, flavonoids and saponins, which are attributed to antiviral efficacies. In conclusion, P. crispa, G. senegalensis and F. parviflora had the most promising anti-HBV potentials, including those of C. decidua, C. epigeus, A. figarianum, A. oerfota and I. caerulea with marked activities. However, a detailed phytochemical study of these extracts is essential to isolate the active principle(s) responsible for their novel anti-HBV potential.
Objective:
To report the indigenous people's uses of plants from a multidimensional perspective in a remote area where strong ethnobotanical cultural practices prevail.
Methods:
An ethnobotanical survey was conducted in the field during 2014-2016. Ethnobotanical data were gathered from 182 informants through oral interviews and semi-structured questionnaires. The distribution of plants was explored using both descriptive and graphical methods. Further, a Multinomial Logit Specification was applied to find out the probability of the occurrence of diverse utilization of plants in multipurpose domains.
Results:
The study identified 202 plant species distributed among 71 families and 156 genera. Ethnobotanical data indicate that there are more medicinal (36.96%) uses of plants as compared to all other use categories. The output from the Multinomial Logit Specifications (MLS) model reveals that perennial and non-woody plants are exploited more for medicinal and food uses than annual and woody plants. In the context of ethnomedicinal uses, aerial plant parts particularly leaves are more extensively used for the preparation of herbal recipes as compared to underground parts.
Conclusions:
The results of the study emphasize the need to create awareness among the local communities about the conservation status of plant species in order to maintain a sustainable resource of plant-derived materials into the future. The novel econometric approach employed in this study adds a new insightful methodology to the existing body of literature in the field of ethnobotany. We strongly recommend conservation measures, alongside phytochemical and pharmacological studies on the useful plant species identified in this study in order to ensure their sustainable and effective utilization.
Background
In addition to pharmacovigilance and pharmaco-economic concerns, resistance to anti-malarial medicines has been documented in all classes of anti-malarials and this is further worsened by resistance to common insecticides by malaria vector, which is a major threat to malaria control. As a means of facing the challenges of searching for new anti-malarial agents, the current study focused on evaluation of anti-malarial activity of root extract of Indigofera spicata.
Methods
Chloroquine-sensitive rodent malaria parasite, Plasmodium berghei (ANKA strain) was used to infect the Swiss Albino mice in 4-day suppressive and curative models. The crude hydromethanolic root extract of I. spicata at 200, 400 and 600 mg/kg doses was administered to a group of five mice. Important parameters, such as level of parasitaemia, packed cell volume (PCV), survival time, and body weight were determined and the significance of the differences between mean values of the five groups was analysed by one-way ANOVA followed by post hoc Tukey’s Multiple Comparison test.
Results
In both the suppressive and curative models, 400 and 600 mg/kg doses of the extract suppressed the level of parasitaemia significantly (p < 0.001) compared to the vehicle-treated groups, 34.93 and 53.42%, respectively. However, only the mice which were treated with the 600 mg/kg dose of the extract had significant difference in their mean survival time. In other parameters, namely PCV and mean body weight, there was no statistically significant difference between the extract-treated groups when compared to the negative control.
Conclusions
This study revealed that the root extract of I. spicata possesses anti-malarial activity and necessitates further scientific validation.
This study investigated the anticariogenic effect of 14 crude extracts from 7 medicinal plants and one isolated molecule on survival and growth of selected cariogenic bacteria. Antibacterial activity was performed against the selected organisms by disc diffusion method; minimum inhibitory concentration (MIC) was determined for purified compound. The most active extract from Jatropha gossypifolia (L.) was fractionated and fraction 3 showed broad spectrum activity against the tested cariogenic bacteria with MIC in the range of 125–500 µg/mL. Based on the anticariogenic activity fraction 3 was further purified and structure of active principle was elucidated based on spectroscopic analysis using proton and carbon NMR and comparison with reported literature. The isolated compound was identified as naringenin; it showed good anticariogenic activity with MIC value of 125 µg/mL against Escherichia coli and Enterococcus faecalis, 250 µg/mL against Klebsiella pneumoniae and Lactobacillus species and 500 µg/mL against Pseudomonas aeruginosa. Our results showed the potential of naringenin as a natural anticariogenic agent to control oral diseases. It can be further processed for pharmaceutical applications.
This review reports on natural compounds that derive from the isoxazolinone ring as well as the 3-nitropropanoic acid (3-NPA) moiety. These structural elements occur in compounds that have been identified in plants, insects, bacteria and fungi. In particular, plants belonging to the family of legumes produce such compounds. In the case of insects, isoxazolin-5-one and 3-NPA derivatives were found in leaf beetles of the subtribe Chrysomelina. A number of these natural products have been synthesized so far. In the case of the single compound 3-NPA, several synthetic strategies have been reported and some of the most efficient routes are reviewed. The toxicity of 3-NPA results from its ability to bind covalently to the catalytic center of succinate dehydrogenase causing irreversible inhibition of mitochondrial respiration. As a motif that is produced by many species of plants, leaf beetles and fungi, different detoxification mechanisms for 3-NPA have evolved in different species. These mechanisms are based on amide formation of 3-NPA with amino acids, reduction to b-alanine, ester formation or oxidation to malonic acid semialdehyde. The biosynthetic pathways of 3-NPA and isoxazolin-5-one moieties have been studied in fungi, plants and leaf beetles. In the case of fungi, 3-NPA derives from aspartate, while leaf beetles use essential amino acids such as valine as ultimate precursors. In the case of plants, it is supposed that malonate serves as a precursor of 3-NPA, as indicated by feeding of 14 C-labeled precursors to Indigofera spicata. In other leguminous plants it is suggested that asparagine is incorporated into compounds that derive from isoxazolin-5-one, which was indicated by 14 C-labeled compounds as well. In the case of leaf beetles it was demonstrated that detection of radioactivity after 14 C-labeling from a few precursors is not sufficient to unravel biosynthetic pathways.
Background:
The development of antivirals against herpes simplex virus 2 (HSV-2) has a major public health importance because of the wide spectrum of associated clinical disease in both immunocompetent and immunocompromised populations. Even with the extensive use of acyclovir, issues such as emergence of drug resistant strains, poor oral bioavailability, and low effectiveness in recurrent infections have highlighted the requirement for alternate therapies. Plants, which are rich in metabolites and active against viruses, are being explored as one such source. We had earlier reported specific and potent anti-HSV-2 activity from the roots of the plant Indigofera heterantha. Herein, we describe the mechanism by which it exerts this antiviral potential against HSV-2 virus.
Methods:
MTT, plaque reduction and immunofluorescence techniques were used for in vitro antiviral studies. Animal studies were carried out in HSV-2 infected mice followed by plaque reduction assays.
Results:
The extract was found to act at multiple steps of viral entry viz. attachment, adsorption and penetration by blocking binding sites present on the viral envelope glycoprotein's which eventually blocks it's binding with the cell surface receptors present on the host cells. We also showed efficacy of PP9706642 topical application in prohibiting HSV-2 invasion to nearby organs from the site of infection i.e. vagina in HSV-2 infected animals.
Conclusions:
The extract targets the early and late stages of HSV-2 viral life cycle and thus shows great promise as both a prophylactic as well as therapeutic phytopharmaceutical against HSV-2.
Lead (Pb) is one of the most common environmental toxicants, exposure to which can cause significant neurotoxicity and an associated decline in brain function. This study investigated the possible neuroprotec-tive role of Indigofera oblongifolia leaf methanolic extract (IOLME) against lead-induced neurotoxicity. Rats were intraperitoneally injected with lead acetate, with or without IOLME (intragastric administration for 5 days), and the neuroprotective effect of IOLME was assessed by measuring the lead concentration, redox status (lipid peroxidation, nitric oxide and glutathione), enzymatic antioxidant activities (superoxide dis-mutase, catalase, glutathione peroxidase and reductase), PCR assays of apoptosis markers (Bax and Bcl-2) and histopathology of the brain. The increases in the lipid peroxidation, nitric oxide, and apoptosis, the decreases in the glutathione level and the activity of antioxidant enzymes, and the altered histology of the brain induced by lead acetate were mitigated in the brain of rats pre-treated with IOLME. These findings indicate that IOLME has beneficial effects and it mitigates lead acetate-induced neurotoxicity via its antiox-idant and anti-apoptotic activities.
Scorpion sting envenoming poses major public health problems. The treatment modalities include antivenoms, chemical antidotes and phytotherapy, with varying degrees of effectiveness and side effects. In this investigation, we reviewed the use of Saudi medicinal plants for the treatment of scorpion sting patients. The relevant literature was collected using the online search engines including Science Direct, Google and PubMed with the help of specific keywords. We also used the printed and online resources at our institutional library to gather the relevant information on the use of medicinal plants for the treatment of scorpion sting patients. A descriptive statistics was used for data compilation and presentation. The results of this survey showed the use of at least 92 medicinal plants with beneficial effects for treating victims of stings of different scorpion species. These commonly used herbs spanned to 37 families while different parts of these plants were employed therapeutically for alleviation of envenomation symptoms. The application of leaves (41%) was preferred followed by roots (19%), whole plant (14%) and seeds (9%). The use of latex (4%), stem (3%), flowers (3%) and bark (3%) was also reported. In some cases, tannin (2%), rhizome (1%) and shoot (1%) were also used. In conclusion, herbal medicines are effectively used for the treatment of patients with scorpion envenomation. This type of medication is free from side effects as observed with chemical antidotes or antivenom therapy. It is important to identify the active ingredients of herbal drugs for improving their therapeutic potential in traditional medicine.
The review focuses on acetylcholinesterase (AChE) inhibition of extracts and compounds from southern African plants. We provide a detailed inventory of southern African plants used in the treatment of central nervous system (CNS) and memory-related disorders that are potential candidates for novel AChE inhibitors. This was achieved through a detailed literature search using web-based database searches including Google Scholar, Scopus and Web of Science (WoS) as well as ethnobotanical literature on southern African medicinal plants. Bibliometric analysis was performed on the data mined from WoS. In addition, we reviewed the methods used to determine AChE activity and highlighted the success and potential of alkaloids from the Amaryllidaceae. Our findings revealed about 200 southern African medicinal plants that are used for CNS and memory-related disorders. Approximately, 65 southern African plants have been evaluated for AChE inhibitory activity even though the majority of these plants do not have an ethnobotanical basis for such evaluation. Several extracts (e.g. Ammocharis coranica (KerGawl.) Herb., Lannea schweinfurthii Engl, Scadoxus puniceus (L.) Friis & Nordal, Xysmalobium undulatum (L.) W.T.Aiton.) have been found to demonstrate noteworthy (IC50 ≤ 1 μg/ml) AChE inhibitory activity. Moreover, 30 compounds have been isolated in an attempt to discover AChE inhibitors from southern African plants. The most active (IC50 ≤ 12 μM) compounds were isolated from Crinum moorei Hook. f., Scadoxus puniceus and Acacia nilotica (L.) Willd. ex Del. subspecies kraussiana (Benth.). Thus far, very few South African studies have looked at the ecological and environmental impact of both naturally occurring and applied AChE inhibitors (e.g. organophosphate and carbamate insecticides) and no studies have considered medical applications other than in Alzheimer's disease (AD) therapy. Furthermore, most of these studies have mainly used an in vitro approach directed at developing treatments of age-related dementia such as AD, despite the decline in pharmaceutical interest of AChE inhibitors in the treatment of AD. It is also apparent that no further steps are taken towards the investigation of in vivo studies and clinical trials. In addition to these existing gaps, the pharmacodynamic and pharmacokinetic studies also need to be adequately addressed in order to generate more coordinated and focused research.
Stachyodin A (1), a rearrangement product of pterocarpan featuring a 6/5/5/6 tetracyclic ring system with an unusual spirotetrahydrofuran ring, and stachyodin B (2), a new dihydrochalcone, along with five known analogues (3–7) were isolated from the roots of Indigofera stachyodes. The structures of 1 and 2 were elucidated on the basis of their HRESIMS and NMR spectroscopic data, and their absolute configurations were determined by X-ray crystallographic analysis and electronic circular dichroism (ECD) data, respectively. Compounds 2–4 showed inhibition of nitric oxide production in lipopolysaccharide-activated BV-2 microglial cells.