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Part 1: Antiplasmodial, Cytotoxic, Radical Scavenging and Antioxidant Activities of Thai Plants in the Family Acanthaceae
Abstract
Crude extracts (CH(2)Cl(2) and MeOH) of 20 plants in the family Acanthaceae were screened for their antiplasmodial, cytotoxic, antioxidant, and radical scavenging activities. These plants included Asystasia nemorum, Barleria cristata, B. strigosa, Dicliptera burmanni, Eranthemum tetragonum, Hygrophila ringens, Justicia balansae, J. procumbens, Lepidagathis incurva, Peristrophe lanceolaria, Phaulopsis dorsiflora, Ruellia kerrii, Strobilanthes auriculata, S. corrugata, S. cusia, S. dimorphotricha, S. karensium, S. maxwellii, S. pateriformis, and S. brandisii. CH(2)Cl(2) extracts of A. nemorum, S. corrugata, S. cusia, S. maxwellii, S. pateriformis, and S. brandisii, as well as MeOH extracts of J. balansae and J. procumbens, showed antiplasmodial activity with IC(50) values of 10-100 µg/mL. CH(2)Cl(2) extracts of nine plants including D. burmanni, H. ringens, J. balansae, J. procumbens, L. incurva, P. lanceolaria, P. dorsiflora, S. corrugata, and S. maxwellii showed cytotoxic activity with IC(50) values of 3.5-46.0 µg/mL. MeOH extracts (at 100 µg/mL) of R. kerrii and S. auriculata could effectively scavenge DPPH free radicals (82-83% inhibition) and superoxide anion radicals (79% and 88% inhibition). In the ORAC antioxidant assay, MeOH extracts of B. cristata, J. procumbens, R. kerrii, and S. auriculata exhibited activity with ORAC units of 3.1-3.9.
... These were widely used as traditional Chinese medicine to remove heat from blood and eliminate toxicity in the human body [27]. Pharmacological studies have shown that Nan-Ban-Lan-Gen has many biological activities, such as antibacterial [28], antiviral [29,30], immunomodulatory [31,32] and anti-inflammatory activities [33]. Previous clinical studies indicated that Indigo Naturalis is good for the treatment of acute promyelocytic leukemia [34,35], ulcerative colitis [36,37], and psoriatic lesions [38]. ...
... We identified 196 and 73 DEGs remarkably enriched in fourteen and three KEGG pathways in CL-VS-TL and CR-VS-TR, respectively. In CL-VS-TL, the DEGs were mostly associated with phenylpropanoid biosynthesis (46), starch and sucrose metabolism (28), pentose and glucuronate interconversions (18), DNA replication (17) and terpenoid backbone biosynthesis (12) ( Table 2). Most of the DEGs were down-regulated, such as photosystem I subunit IV (PsaE), photosystem I subunit VI (PsaH), photosystem I subunit X (PsaK), photosystem I subunit PsaN (PsaN), photosystem I subunit PsaO (PsaO) on ko00195 (S1 Fig Indican is the precursor of indigo and indirubin (Fig 3). ...
Baphicacanthus cusia (Nees) Bremek (B. cusia) is an effective herb for the treatment of acute promyelocytic leukemia and psoriasis in traditional Chinese medicine. Methyl jasmonate (MeJA) is a well-known signaling phytohormone that triggers gene expression in secondary metabolism. Currently, MeJA-mediated biosynthesis of indigo and indirubin in B. cusia is not well understood. In this study, we analyzed the content of indigo and indirubin in leaf and root tissues of B. cusia with high-performance liquid chromatography and measured photosynthetic characteristics of leaves treated by MeJA using FluorCam6 Fluorometer and chlorophyll fluorescence using the portable photosynthesis system CIRAS-2. We performed de novo RNA-seq of B. cusia leaf and root transcriptional profiles to investigate differentially expressed genes (DEGs) in response to exogenous MeJA application. The amount of indigo in MeJA-treated leaves were higher than that in controled leaves (p = 0.004), and the amounts of indigo in treated roots was higher than that in controlled roots (p = 0.048); Chlorophyll fluorescence of leaves treated with MeJA were significantly decreased. Leaves treated with MeJA showed lower photosynthetic rate compared to the control in the absence of MeJA. Functional annotation of DEGs showed the DEGs related to growth and development processes were down-regulated in the treated leaves, while most of the unigenes involved in the defense response were up-regulated in treated roots. This coincided with the effects of MeJA on photosynthetic characteristics and chlorophyll fluorescence. The qRT-PCR results showed that MeJA appears to down-regulate the gene expression of tryptophan synthase β-subunits (trpA-β) in leaves but increased the gene expression of anthranilate synthase (trp 3) in roots responsible for increased indigo content. The results showed that MeJA suppressed leaf photosynthesis for B. cusia and this growth-defense trade-off may contribute to the improved adaptability of B. cusia in changing environments.
... It is used as a Thai traditional medicine for treating glossitis, infected wounds, smallpox, rashes, and fever [1]. The extract of P. lanceolaria showed cytotoxic, antiplasmodial and antioxidant activities [2][3]. Previous phytochemical investigations on this plant revealed the present of two alkaloids, peristrophine and the butyl acetal derivative of 1,6benzoxazocine-5-one [3], and an anthocyanin, pelargonidin-3-glucoside [4][5]. ...
... Previous phytochemical investigations on this plant revealed the present of two alkaloids, peristrophine and the butyl acetal derivative of 1,6benzoxazocine-5-one [3], and an anthocyanin, pelargonidin-3-glucoside [4][5]. In the current study we isolated lutein (1) and lutein 3′-methyl ether (2). Lutein is the main xanthophyll found in the major light-harvesting pigment-protein complex of higher plants, and is involved in energy-transfer mechanisms during photosynthesis. ...
Two carotenoids, lutein (1) and lutein 3'-methyl ether (2), have been isolated from the EtOAc fraction of the MeOH extract of Peristrophe lanceolaria, growing in Thailand. The structures of these compounds were elucidated from their 1D and 2D NMR spectroscopic data and from comparisons made with the literature data. This is the first report of the isolation of lutein-3'-methyl ether as a natural product.
... Methanol extracts (at 100µg/ml) of Ruelliakerrii and Strobilanthesauriculata showed antioxidant activity. Methanolextracts of Barleriacristata, Justiciaprocumbens, Ruelliakerrii and Strobilanthesaureculata showed antioxidant activity [27]. ...
... O-β-D-gluco-pyranosyl-2H-1,4benzoxazin-3(4H)-one (23),(2R)-2-O-β-D-glucopyranosyl-4hydroxy-2H-1,4-benzoxazin-3(4H)-one (24), (2R)-2-O-β-Dglucopyranosyl-7-hydroxy-2H-1,4-benzoxazin-3(4H)-one (25), 7chloro-(2R)-2-O-β-D-glucopyranosyl-2H-1,4-benzoxazin-3(4H)-one (26) and (2R)-2-O-β-D-glucopyranosyl-5-hydroxy-2H-1,4benzoxazin-3(4H)-one(27) have been isolated[31].Salidroside(28),benzyl β-D-glucopyranoside(29), (6S,9R)roseoside(30), asysgangoside(31), ajugol(32), apigenin 7-O-β-Dglucopyranoside(33), apigenin 7-O-neohesperidoside (34) and apigenin 7-O-β-Dglucopyranosy (1 → 6) -β-D-glucopyranoside(35) have been reported in Asystasiagangeticawhich belongs to family Acanthaceae [32]. Olean-12-ene-1β,3β,11α,28-tetraol-28-O-β-D-glucopyranosyl-(1→2) -β-D-glucopyranoside (36), olean-12-ene-1β,3β,11α,28-tetraol-28-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-(1→2)-β-D-gluco pyranoside(37), 11α-methoxy-olean-12-ene-1β,3β,28-triol-28-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranoside ...
Aphelandra belong to family Acanthaceae. We have reviewed traditional uses, pharmacological potential and phytochemical study of family Acanthaceae and genus Aphelandra. Traditionally the most important part use in Acanthaceae is the leaves and they are used externally for wounds. We have found that Acanthaceae possess antifungal, cytotoxic, anti-inflammatory, anti-pyretic, anti-oxidant, insecticidal, hepatoprotective, immunomodulatory, Anti- platelet aggregation and anti-viral potential. Phytochemical reports on family Acanthaceae are glycosides, flavonoids, benzonoids, phenolic compounds, naphthoquinone and triterpenoids. We have also document genus Aphelandra, its phytochemical and pharmacological potential.
... Indeed, many of saponin components from Polygala species are reported to have neuroprotective potential against Aβ-induced neurotoxicity in PC 12 cells suggesting a potential therapeutic value for Polygala in neurodegenerative disorders [56,57]. Limited available data revealed that E. capense has been ethnopharmacologically used as anti-inflammatory and antioxidant agents [29]. These activities have key role in developing anti-AD agents. ...
... Triterpenes, flavonoids, phenolic compounds, iridoids, and phenylethanoid glycoside have all been identified in the phytochemical profile of Barlerai cristata [19,20].Biological activities exhibited by Barleria cristata included hepatoprotective, antiplasmodial, antibacterial, antifungal, antidiabetic, anti-inflammatory, and antioxidant activities [21]. As a result, the purpose of this review was to emphasise the significance of Barleria cristata as a possible an origin of bioactive chemicals and to summarise the therapeutic applications as well as phytopharmacological investigations to emphasise this plant's potential for the future. ...
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... Pharmacological studies reported that this plant possesses several biological activities, including anti-inflammatory, antibacterial, anti-diabetic, anti-oxidant, anti-fungal, hepato-protective, anti-plasmodial, anti-oxidant, and cytotoxic properties [8]. This plant is of significant value and lacking in standardization parameters based on the literature; therefore, detailed morphological estimation, physicochemical evaluation, and phytochemical group screening are required. ...
Background: Barleria cristata Linn. belongs to the family Acanthaceae and is commonly known as Raktajhinti and VajraDanti. It is widely distributed in countries, such as India, Nepal, Bangladesh, Pakistan, and Asian tropical regions. This plant has been observed to bear multifarious ethnomedical uses in treating lung disorders, inflammatory conditions, toothache, anemia, and snakebite. A wide range of major chemical constituents, such as triterpenes, phenolic compounds, flavonoids, and glycosides are reported to be present in this plant. The plant exhibited diverse pharmacological actions, such as anti-inflammatory, antibacterial, antifungal, and antioxidant activities. The literature revealed insufficient information concerning the standardization of Barleria cristata Linn. Objectives: The present study aimed to explore the pharmacognostic and phytochemical characteristics of Barleria cristata Linn. (leaf). Methods: The present study addressed quality control parameters, including loss on drying, ash values, extractive values, pharmacognostic parameters (e.g. macroscopic & microscopic characters and powder microscopy) as per the World Health Organization (WHO) guidelines. Results: Biochemical analysis revealed total ash (16.11±0.38), acid insoluble ash (1.50±0.18), water-soluble ash (11.10±0.23), alcohol-soluble extractive (19.34±0.79), and water-soluble extractive (25.06±0.17), respectively. The transverse section of the leaf revealed the presence of the epidermis, covering trichomes, vascular bundle, and so on. The other parameters such as phytochemical investigation, fluorescence analysis, and thin-layer chromatography were also performed to explore the crucial values of these examinations. Conclusion: The obtained data would be useful in the future for preparing a monograph for the authentication and standardization of this crude drug.
... The Flora of Kinmen records that the whole plant is used as medicine to treat sore throat and lower back pain. The known pharmacological activities of this species are antioxidant (Charoenchai et al., 2010), antiviral (Xu et al., 2019), antibacterial (Zhang et al., 2007), and anticancer activity (Day et al., 2002;Wang et al., 2015). It is worth noting that this plant is widely used by people in Kinmen because of its efficacy in clearing heat and removing toxicity, as documented in different literature and studies. ...
Kinmen is an outlying island that has the richest plant resources in Taiwan. The objective of this study was to record the methods that people in Kinmen use medicinal plants and to analyze the cultural characteristics of their use. Field investigations were carried out in various towns and villages in Kinmen, and 80 respondents were included in the survey. The search for respondents was conducted through local elderly people and medicinal plant groups. Semi-structured interviews were conducted with the local people to obtain their knowledge of medicinal plants and how they disseminate this information. Informed consent was obtained prior to the interviews, and the following was determined: plant use value (UV), frequency of citation (FC), and factor of informant consensus (Fic). These parameters were used to quantify the data and measure the agreement among the respondents on using plants to treat different diseases. Finally, the survey results were compared with the representative ethnobotanical literature in neighboring areas to evaluate the similarity between plant usage in Kinmen and neighboring areas as well as to determine whether there are new species or novel usages in the study area. In the Kinmen area, phytotherapy is generally used by elderly people with low educational attainments. According to the survey results, 83 medicinal plants belonging to 48 families were collected. These medicinal plants were mainly distributed in the Compositae, Lamiaceae, and Solanaceae families. Eighteen novel uses that have not been previously documented were found, four of which were related to newly recorded medicinal plant species in the Kinmen area. The results showed that 93.98 and 65.06% of the species collected in the present study were also recorded in literature from Taiwan and Fujian, respectively. This study showed that Kinmen’s ethnobotanical knowledge is closely related to the Catalogue of Medicinal Plant Resources in Taiwan, and local people indeed shared similar uses of medicinal species with people in Taiwan and Fujian (46.99%). The results from this study highlighted the importance of traditional medicine in the Kinmen area, where people have a specific understanding of using medicinal plants and communication with people in Taiwan and Fujian Province in China. It was found that Kinmen shares ethnobotanical knowledge with Taiwan and Fujian.
... The flowering plant commonly known as kamanabillu balli, appertains to the Acanthaceae species and Thunbergioideae subfamily, innate to Evergreen Forests, extended to Southern Western Ghats. The earlier explorations specified that the Acanthaceae family preserve cytotoxic, antiplasmodial, antioxidant [23] , antifungal [24] , hepatoprotective [25] , immunomodulatory [26] , anti-viral [27] characteristics. Iridoid glycosides are the core sort of molecules proclaimed from the Thunbergioideae family. ...
Practicing the aqueous Thunbergia mysorensis stem and flower essences for obtaining the silver oxide nanoparticles (Ag2O-NPs) advances over chemical and physical processes since the extracts fiddle a dualistic role as reducing and stabilizing agents. The UV-Visible, FTIR, TEM, SEM, and XRD were realized to validate and mark the green synthesized Ag2O-NPs. TEM pictures exposed the quasi-spherical Ag2O-NPs shape with average sizes 15 nm and 120 nm respectively for Ag2O-NPs of flower (F-Ag2O-NPs) and the stem extracts (S-Ag2O- NPs). Antioxidant activity of Ag2O-NPs investigated by DPPH, ABTS cation radical and ferric ion reduction routes manifest enhanced antioxidant activity with F-Ag2O-NPs compared to S-Ag2O-NPs. Hemolytic assay results elicited that S-Ag2O-NPs and F-Ag2O-NPs, respectively showed 1.4% and 1% hemolysis. Additionally, the synthesized F-Ag2O-NPs showed potent antibacterial activity against Gram-negative and Gram-positive bacteria compared to S-Ag2O-NPs and were effective against human MDA-MB-468-triple negative breast cancer cell lines with an IC50 of 480 µM.
... 15414/agrobiodiversity.2019.2585-8246.186-194 *Corresponding author: Kateryna Lystvan, Institute of Cell Biology and Genetic Engineering of National Academy of Sciences of Ukraine, Academika Zabolotnogo 148, 03680 Kyiv, Ukraine species (Shinwari et al., 2017); show antiplasmodial, antitumor and antioxidant activities (Charoenchai et al., 2010), etc. ...
In this work we described a procedure of Fittonia albivenis (Lindl. ex Veitch) Brummitt in vitro conservation and microclonal propagation by enhanced bud proliferation from shoot tips as well as studying some biochemical characteristics of plants cultured both in vivo and in vitro. Multiple shoot formation from apical and axillary buds started in 4 months on MS/2 medium without growth regulators. Multiplication coefficients ranged from 6.0 ±1.9 to 14.7 ±2.6 for different plant clones. So, as a result of our work, the effective system of microclonal propagation of F.albiviens on hormone-free media was elaborated. It have been shown that application of plant growth regulators seems just to shorten the time period of Fittonia in vitro microclonal propagation but does not have any significant effect on multiplication coefficients. The total content of bioactive substances (flavonoids and phenolics) was about 0.2–0.45 % of dry weight, that is significantly less than its amount in known sources of polyphenols (e.g., ground coffee ). However, the data indicate the significant differences in the content of these bioactive substances between in vivo growing plants with dark-green (clone #1) and light-green leaves (clone #2) as well as different reactions to the transfer to the in vitro conditions. For some clones the significant increase in both phenolics and flavonoids amount was observed after such transfer. The clones with highest productivity have been identified and will be used in further researches.
... Besides these compounds, researchers have found 4-hydroxy-trans-cinnamate derivatives and oleanolic acid (109) in this plant [74]. Biological investigations of this plant showed anti-inflammatory [69,75], and antioxidant properties [76,77]. There are few phytochemistry and biological studies of this species; therefore, it seems to be interesting for further investigation of new lead products. ...
Medicinal plants are a reservoir of biologically active compounds with therapeutic properties that over time have been reported and used by diverse groups of people for treatment of various diseases. This review covers 15 selected medicinal plants distributed in Myanmar, including Croton oblongifolius and Glycomis pentaphylla. Investigation of the phytochemical constituents, biological and pharmacological activities of the selected medicinal plants is reported. This study aims at providing a collection of publications on the species of selected medicinal plants in Myanmar along with a critical review of the literature data. As a country, Myanmar appears to be a source of traditional drugs that have not yet been scientifically investigated. This review will be support for further investigations on the pharmacological activity of medicinal plant species in Myanmar.
... [14,18,19] Some recent pharmacological studies have reported that B. cristata possesses several biological activity including anti-inflammatory, antibacterial, antidiabetic, antioxidant, antifungal, hepatoprotective, antiplasmodial and antioxidant activity. [20] Therefore, the aim of this review was to highlight the importance of B. cristata as a potential source of bioactive compounds and to summarize the medicinal uses as well as phytopharmacological studies to highlight the future prospects of this plant. Critical evaluation of pharmacological studies undertaken in relation to ethnobotanical use was also performed. ...
Objectives:
Barleria cristata (Family: Acanthaceae), commonly known as Philippine violet, is used in different ethnomedical systems for the treatment of a wide range of ailments. This review aimed to provide a scientific overview of B. cristata with reference to its ethnobotanical aspects, geographical distribution, medicinal uses, phytochemistry and pharmacological activity, and critical analyses research gaps and future research opportunities for investigations on this plant.
Key findings:
Ethnomedical uses of the plant have been observed in lungs disorders, inflammatory conditions, toothache, anaemia, snake bite, diabetes and tuberculosis. The exhaustive bibliographic research carried out on this plant revealed that the plant parts are rich in various phytochemical constituents including triterpenes, phenolic compounds, glycosides and flavonoids type phenolic compounds. Furthermore, the plant was also investigated in terms of its anti-inflammatory, antibacterial, antidiabetic, antifungal, hepatoprotective and antioxidant activity.
Conclusions:
This review confirms that B. cristata is a potential herb for the treatment of a wide range of diseases especially lung disorders and inflammatory conditions. Modern pharmacological studies have also validated many ethnobotanical uses of B. cristata, though data regarding many aspects of this plant such as mechanism of action, adverse effects of extracts and active compounds are still limited which call for additional studies.
... Other medicinal uses of lepidagathis plants include skin infections, malaria, migraine, cardiovascular diseases and gastric problems (Hassan-Abdallah et al., 2013;Mollik et al., 2009;Ravikanth et al., 2001;Richard et al., 2011). Previous studies have shown they possess excellent larvicidal, anti-inflammatory, analgesic, antipyretic and cytotoxic properties (Charoenchai et al., 2010;Obomanu et al., 2006;Richard et al., 2011). Despite having a number of traditional claims and uses in management of kidney stones, very few species of this genus have been studied for antiurolithiatic activity. ...
Oxidative stress acts as an essential mediator in the pathophysiology of urolithiasis. Lepidagathis prostrata Dalz. (Acanthaceae) is a Pashanbhed plant that is recommended for the management of urolithiasis; however, no scientific validation has been reported.
To evaluate the antiurolithiatic and antioxidant potential of L. prostrata.
Methanol extract (LPM) and fractions; petroleum ether (LPPE), ethyl acetate (LPEA), n-butanol (LPBU) and aqueous (LPAQ) were prepared. In vitro antiurolithiatic activity was evaluated by the capacity to inhibit calcium oxalate (CaOx) nucleation and aggregation at different concentrations of extract/fractions (0.04-3 mg/mL) for 30 min. Total phenol and flavonoid content and antioxidant potential were determined. A validated HPTLC method was performed to quantify lupeol and β-sitosterol.
LPEA exhibited the highest dose-dependent inhibition of CaOx nucleation (IC50: 336.23 ± 30.79 µg/mL) and aggregation (IC50: 149.63 ± 10.31 µg/mL), which was significantly (p < 0.05) better than standard Cystone®. The polar LPBU fraction was enriched with phenols (47.34 ± 0.19 mg GAE/g) and flavonoids (20.38 ± 0.05 mg QE/g), which correlates with its highest antioxidant potential in DPPH, ABTS, nitric oxide scavenging and iron chelating activities (IC50: 1.18-87.34 µg/mL). To our knowledge, this is the first study reporting the presence of lupeol and β-sitosterol in L. prostrata.
The antiurolithiatic activity of L. prostrata is probably mediated through the inhibition of CaOx crystallization. In addition to its free radical scavenging and antioxidant activities, it would act as an excellent agent for the prevention of urolithiasis.
... 4 The biological investigation of the plant showed anti-inflammatory, anti-anaemic and anti-toothache, 5 anti-plasmodial and antioxidant properties. 6 Previous phytochemical studies with the plant led to the isolation and structure elucidation of flavonoids, phenolic compounds, iridoidal 7 and phenylethanoid glycosides. 8 The present study has been undertaken to isolate and identify biologically active secondary metabolites and we, herein, report 4-hydroxy-transcinnamate derivatives (1-3) and a triterpene, namely oleanolic acid (4). ...
Barleria cristata is an important medicinal plant of Bangladesh. Many compounds of diverse biological activities were isolated from different Barleria species, including irridoids, flavonoids and phenylethanoid derivatives in addition to other groups of chemical constituents. This paper presents the chemical investigation of the whole plants of B.cristata. Classic phytochemical investigation of organic extracts of the whole plants of B. cristata together with spectroscopic methods led to the isolation and characterization of 4-hydroxy-trans-cinnamate derivatives (1-3) and a triterpene, namely oleanolic acid (4).
... A previous report on the bioactivity of the CH 2 Cl 2 extract of P. lanceolaria showed cytotoxic activity against a T-lymphoblast cell line and the ability to scavenge TPAinduced superoxide anion radical formation in differentiated HL-60 cells, whereas the MeOH extract was able to inhibit the superoxide anion radical. Both the CH 2 Cl 2 and MeOH extracts showed antiplasmodial and antioxidant activities in an oxygen radical antioxidant capacity assay [2]. Previous phytochemical investigations of this plant revealed the presence of pelargonidin-3β-glucoside [3][4]. ...
A new 1,6-benzoxazocine-5-one alkaloid has been isolated as its butyl acetal derivative (1) along with peristrophine from the n-BuOH and EtOAc fractions of the crude MeOH extract of the aerial parts of Peristrophe lanceolaria growing in Thailand. The structures of these compounds were elucidated on the basis of their spectroscopic data. These compounds were isolated for the first time from P. lanceolaria. The EtOAc and n-BuOH fractions also possessed significant antioxidant activity with IC50 values of 57 and 50 μg/mL, respectively (DPPH method), whereas 1 had an IC50 value of 23 μg/mL.
... The complete egg hatching inhibition and larval development inhibition for leaf and seed ethyl acetate, acetone and methanol extracts of S. torvum indicated in vitro anthelmintic activity against the parasitic nematode of small ruminants Haemonchus contortus (Kamaraj et al. 2010d). The dichloromethane and methanol crude extracts of Acanthaceae family plants, Justicia procumbens and Justicia balansae were screened for their antiplasmodial, cytotoxic, antioxidant and radical scavenging activities against P. falciparum (Charoenchai et al. 2010). Kamaraj et al. (2010b) reported the adulticidal, repellent and larvicidal activity of the crude hexane, ethyl acetate and methanol extracts of J. procumbens which were tested against adult and early fourth-instar larvae of C. gelidus and C. quinquefasciatus. ...
The emergence and spread of Plasmodium falciparum with resistance to chloroquine (CQ), the safest and cheapest anti-malarial drug, coupled with the increasing cost of alternative drugs especially in developing countries have necessitated the urgent need to tap the potential of plants for novel anti-malarials. The present study investigates the anti-malarial activity of the methanolic extracts of 13 medicinal plants from the Malaiyur and Javadhu hills of South India against blood stage CQ-sensitive (3D7) and CQ-resistant (INDO) strains of P. falciparum in culture using the fluorescence-based SYBR Green I assay. Sorbitol-synchronized parasites were incubated under normal culture conditions at 2% hematocrit and 1% parasitemia in the absence or presence of increasing concentrations of plant extracts. CQ and artemisinin were used as positive controls, while 0.4% DMSO was used as the negative control. The cytotoxic effects of extracts on host cells were assessed by functional assay using HeLa cells cultured in RPMI containing 10% fetal bovine serum, 0.21% sodium bicarbonate and 50 μg/mL gentamycin (complete medium). Plant extracts (bark methanol extracts of Annona squamosa (IC(50), 30 μg/mL), leaf extracts of Ocimum gratissimum (IC(50), 32 μg/mL), Ocimum tenuiflorum (IC(50), 31 μg/mL), Solanum torvum (IC(50), 31 μg/mL) and Justicia procumbens (IC(50), 63 μg/mL), showed moderate activity. The leaf extracts of Aristolochia indica (IC(50), 10 μg/mL), Cassia auriculata (IC(50), 14 μg/mL), Chrysanthemum indicum (IC(50), 20 μg/mL) and Dolichos biflorus (IC(50), 20 μg/mL) showed promising activity and low activity was observed in the flower methanol extracts of A. indica , leaf methanol extract of Catharanthus roseus, and Gymnema sylvestre (IC(50), >100 μg/mL). These four extracts exhibited promising IC(50) (μg/mL) of 17, 24, 19 and 24 respectively also against the CQ resistant INDO strain of P. falciparum. The high TC(50) in mammalian cell cytotoxicity assay and the low IC(50) in anti-malarial P. falciparum assay indicates selectivity and good resistance indices in the range of 0.9-1.7 for leaf extracts of A. indica, C. auriculata, C. indicum and D. biflorus suggests that these may serve as anti-malarial agents even in their crude form. These results indicate a possible explanation of the traditional use of some of these medicinal plants against malaria or malaria-like conditions.
Justicia procumbens L. a perennial herb belonging to the Acanthaceae family, has been used in traditional medicine for centuries to treat various ailments. The plant has been found to possess a wide range of pharmacological properties, including anti-platelet aggregation, anti-retro viral disease (RVD), antiasthmatic, anti-inflammatory, antibacterial, antifungal, antiviral, anti-diabetic, antihelminthic, antiplasmodial, antioxidant and radical scavenging activities. For instance, DW2008, an ethanol extract of Justicia procumbens, demonstrated effective anti-asthmatic properties in mouse models. The plant's extracts have also been shown to exhibit cytotoxic effects against various cancer cell lines, including bladder, colorectal, leukemia and liver cancers, indicating its potential as an anti-cancer agent. Additionally, the plant has been found to possess fungicide and insecticide properties, making it a potential natural pesticide. The phytochemical analysis of Justicia procumbens has revealed the presence of lignans (primary bioactive compound), flavonoids, alkaloids and phenolic compounds, which are responsible for its diverse pharmacological properties. Anti-platelet aggregation studies reveal that aryl naphthalene lignans from Justicia procumbens inhibit platelet aggregation by modulating key signaling pathways, suggesting potential therapeutic applications for thrombotic diseases. This review aims to provide a comprehensive overview of the phytochemical and pharmacological investigations of Justicia procumbens, highlighting its potential as a source of novel therapeutic agents for various diseases. Further research is warranted to fully exploit the plant's therapeutic potential and to develop evidence-based remedies for human health.
Hygrophila salicifolia (Vahl) Nees is a traditional Chinese herbal medicine widely circulated in the Chinese medicinal materials market. It has gained significant popularity for its therapeutic effects in clearing heat and reducing swelling. The present study evaluated the chemical composition, antioxidant capacity, acetylcholinesterase, and α-glucosidase inhibitory effect of this species’ essential oil. The major compounds of H. salicifolia
essential oil were 1-octen-3-ol (29.0 %), phytol (5.7 %), phytone (4.6 %), cubebol (3.7 %), estragole (3.5 %), 7-epi-silphiperfol-5-ene (3.3 %), and ylangenol (3.1 %). The essential oil of H. salicifolia revealed antioxidant activity against both 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals with half-maximal inhibitory concentration (IC50) values of 2.13 ± 0.17 and 0.22 ±
0.02 mg/mL. The ferric reducing antioxidant power (FRAP) value was 170.97 ± 3.68 μmol⋅g− 1. The essential oil has moderate activity against acetylcholinesterase (IC50 = 360.4 ± 12.7 μg/mL) and weak activity against α-glucosidase (14.2 % inhibition at 500 μg/mL). Moreover, we conducted in silico network pharmacology
analysis and molecular docking to evidence the results of in vitro tests, providing a theoretical foundation for future drug development. The presented results suggest that the essential oil of H. salicifolia possesses the potential to be used in cosmetics, food, and pharmacological industries, emphasizing the need for further investigation.
The leaves of the species of Acanthceae have been traditionally used as herbal medicines by the native and nomadic communities mainly to alleviate the poisonous bites of insects and reptiles and for the treatment of external wounds and ulcers. The pharmacological activities reported from these species are antibacterial, antifungal, anti-pyretic, hepatoprotective, anti-inflammatory, cytotoxic, antioxidant, anti-platelet aggression and insecticidal. The traditional use, chemical constituents and pharmacological activities from family Acanthaceae have been selected for study. In literature, from this family phytochemicals mainly flavonoids, alkaloids, lignans, saponins, triterpenoids, steroids and fatty acids are recorded. The species of Acanthaceae has emerged as good source of traditional medicines. The chemical compounds isolated from these species have been reported for their pharmacological effects. Although, few experimental studies validated their traditional claim, but uncharacterized crude extract was employed in most of the activities. Such species need to be explored properly for their bioactive principle and exploited as potential drug. The review will help the researchers to select medicinally potential species of Acanthaceae for future research.
The present study was undertaken to evaluate the antidiabetic and hypolipidemic action of leaf extract of Barleria cristata Linn in rats. Diabetes was induced in the rats by a single intraperitoneal (IP) injection of alloxan (150 mg/kg) and randomly divided into 7 groups. Animals were treated with low (250 mg/kg) and high (500 mg/kg) doses of ethyl acetate leaf extract (EALE) and hydro-alcoholic leaf extract (HALE) up to 21 days. The body weight and blood glucose level (BGL) were measured on weekly basis. The rats were killed under mild ether anesthesia on 21st day, blood and the vital organ were collected to estimate biochemical parameters and to study histopathological changes. A single-dose administration of alloxan induced hyperglycemia in all the groups. A regular increase in BGL was observed in toxic control groups when compared with the normal control. Daily oral administration of rats with extracts (HALE and EALE) and standard drug (Glimepiride, 5 mg/kg), reduced elevated BGL significantly (p < 0.001), and body weight was regained in diabetic rats. The extract treatment also improved the normal functioning of the liver and kidneys as evidenced by the restoration of the biochemical profile. The study revealed that B. cristata possesses promising antidiabetic and hypolipidemic activity.
The present article deals with ethnopharmacological study of Madia tribe of Gadchiroli district of Maharashtra state, India. The ethnomedicinal plants were collected from the field. The uses were verified on the basis of earlier published pharmacological and phytochemical data
Barleria plant of family Acanthaceae is used traditionally for a wide variety of biomedical properties such as anemia, toothache, cough, hypoglycemic agent, anti inflammatory agent. Owing to the multiple pharmacological properties, the compounds were investigated for the treatment of autoimmune disorders by in silico approach. Phytochemical analysis, spectral characterization by GC-MS followed by Molecular Docking of the characterized compound were performed. ADMET and DFT studies were carried out to select the suitability of drug compounds. Totally nineteen compounds were obtained and depending upon the highest mass percentage five compounds were selected. i) 6-Amino-1,2,3,4tetrahydroindan-5,7-Dione ii) 9, 12, 15-Octadecatrienoicacid, methyl ester, iii) 1,2-Benzenedicarboxylic acid, butyl 2-methyl propyl ester iv) p-Decylphenoxsy acetic acid and v) 2,6,6-Trimethyl-2-3-[3-Oxo-3-phenylpropenyl) cyclohexane for further studies. The selected five compounds qualified the Lipinski rule of five and were non-mutagenic and non-carcinogenic. Thus the compound p-Decylphenoxy acetic acid was found to be a potent and safe against HLA-DR4 associated with rheumatoid arthritis.
This research is meant for the isolation of the compounds out from the methanolic extract of the Hygrophila auriculata. This herb was customarily used as a diuretic to cure the inflammation, pain, urinal infections, and the gout. To isolate the compounds from methanolic extract of Hygrophila auriculata which was taken from Bihar’s Koshi river belt, open silica gel column chromatographic methods with different solvent mixtures were applied. The elucidation of the structure of the different separated phytoconstituent was accomplished through spectral data analysis, chemical reactions and their literary comparisons. Phytochemical analysis of methanolic extract of Hygrophila auriculata gave a new compound identified as n-octa-triacontan-3-one-19α, 31α-diol (4) and along with the four known aliphatic ester compounds n-hexacos-21-one-1-ol (1), trans-tetracont-7-en-1-ol (2), n–octacosan-8-one (3) and n-heptacosan-11α-ol (5). A new compound was found with four other known compounds as aliphatic esters from H. auriculata extract.
Two phenolic compounds (P- Coumaric acid and α-Tocopherol), two flavonoidal compounds (luetoline and 7-methoxy luetoline) and two iridoidal glycosides (barlerin and schanshiside methyl ester) have been isolated from leaves of Barleria cristata their structure were established by spectral analysis. This is the first report of occurrence of these compounds from Barleria cristata Linn plant.
The anticancer activity of leaf extracts of Peristrophe bicalyculata was evaluated. Results showed that the methanolic ethylacetate fraction with an IC50 of 15.60 ± 0.52 μg/ml was potentially very toxic against human mouth epidermal carcinoma (KB) cells. After partial purification of the methanolic ethylacetate fraction, seven fractions were obtained; five of which were inactive (IC50 values above 500 μg/ml) and one moderately toxic (IC50 = 235 ± 33.05 μg/ml), hence not considered. The IC50 value of the most cytotoxic fraction (fraction 5) (3.50 ± 0.21 μg/ml) was not different from that of cisplastin (3.32 ± 0.09 μg/ml), but was significantly (P<0.05) higher than the value obtained for doxorubicin (0.43 ± 0.02 μg /ml) and vincristine (0.05 ± 0.01μg/ml). The partially-purified fraction induced apoptosis in KB cells after 24 and 48 hours in a dose-dependent manner. The percentage of apoptotic cells in cultures treated with this fraction was significantly (P<0.05) higher than that in control cultures, but lower than cultures treated with cisplastin. The GC-MS analysis of the fraction indicated an abundance of andrographolide 2(3H)-furanone and aromadendrene oxide, both of which possess anticancer properties. The results provide scientific evidence supporting the anticancer activity of the methanolic ethylacetate fraction of the plant. In conclusion, the methanolic ethylacetate fraction of Peristrophe bicalyculata is a potential source of chemotherapeutic agent.
Living organisms in Thailand are very diverse due to the unique geographical location of Thailand. The diversity of Thai bioresources has proven to be a rich source of biologically active compounds. The present review covers bioactive substances from Thai endophytic, marine-derived, insect pathogenic fungi and medicinal plants. Many new compounds isolated from Thai bioresources have diverse skeletons belonging to various classes of natural products. These compounds exhibited an array of biological activities, and some are of pharmaceutical interest. Bioactive compounds from Thai bioresources have not only attracted organic chemists to develop strategies for total synthesis, but also attracted (chemical) biologists to investigate the mechanisms of action. The chemistry and biology of some selected compounds are also discussed in this review.
The anticancer activity of leaf extracts of Peristrophe bicalyculata was evaluated. Results showed that the methanolic ethylacetate fraction with an IC 50 of 15.60 ± 0.52 µg/ml was potentially very toxic against human mouth epidermal carcinoma (KB) cells. After partial purification of the methanolic ethylacetate fraction, seven fractions were obtained; five of which were inactive (IC 50 values above 500 μg/ml) and one moderately toxic (IC 50 = 235 ± 33.05 µg/ml), hence not considered. The IC 50 value of the most cytotoxic fraction (fraction 5) (3.50 ± 0.21 µg/ml) was not different from that of cisplastin (3.32 ± 0.09 µg/ml), but was significantly (P<0.05) higher than the value obtained for doxorubicin (0.43 ± 0.02 µg /ml) and vincristine (0.05 ± 0.01µg/ml). The partially-purified fraction induced apoptosis in KB cells after 24 and 48 hours in a dose-dependent manner. The percentage of apoptotic cells in cultures treated with this fraction was significantly (P<0.05) higher than that in control cultures, but lower than cultures treated with cisplastin. The GC-MS analysis of the fraction indicated an abundance of andrographolide 2(3H)-furanone and aromadendrene oxide, both of which possess anticancer properties. The results provide scientific evidence supporting the anticancer activity of the methanolic ethylacetate fraction of the plant. In conclusion, the methanolic ethylacetate fraction of Peristrophe bicalyculata is a potential source of chemotherapeutic agent.
Medicinal plants used by tribal medicinal practitioners of three clans of the Chakma tribe residing in Rangamati district, Bangladesh ABSTRACT The Chakmas are the largest tribe inhabiting the forested hilly regions in the Chittagong Hill Tracts, which lies in the southeastern part of Bangladesh. Although they are scattered in all four districts of the Chittagong Hill Tracts, they are mostly concentrated in the districts of Rangamati and Khagrachari. The tribal population is currently estimated at around 300,000. The Chakmas are distinguished by having their own language with alphabets and their own distinctive culture, which includes their own rituals and own tribal medicinal practitioners. More than 30 clans (which are further sub-divided into over 50 sects) exist within the tribe. It was the objective of the present study to conduct an ethnomedicinal survey among the tribal medicinal practitioners of Baburo, Haduga, and Larma clans of the Chakma tribe inhabiting the Rangamati district of Bangladesh as to their traditional formulations for treatment of various ailments. The survey was conducted with the help of a semi-structured questionnaire and the guided field-walk method. One practitioner from each clan was interviewed. It was observed that the three tribal practitioners, among themselves, used a total of 73 plants distributed into 42 families for treatment of ailments. The Rubiaceae family contributed 7 plants followed by the Apocynaceae, Euphorbiaceae and Lamiaceae families with four plants each. Leaves constituted the major plant part used, forming 60.2% of total uses. Leaves were followed by barks, roots, fruits and stems, which respectively, formed 12.9, 8.6, 7.5 and 5.4% of total uses. Respiratory disorders (coughs, mucus), skin diseases, gastrointestinal disorders, hemorrhoids, fever, eye disorders, urinary tract disorders, helminthiasis, stomach and kidney stones, paralysis, pain, rheumatism and jaundice were ailments treated by the tribal medicinal practitioners. However, the practitioners also recognized and claimed to treat successfully diseases like diabetes, cancer, and hypertension. Diabetes was treated with 9 different plants and hypertension with 5 different plants. The practitioners treated two types of cancer, namely skin cancer and throat cancer. Chittagong Hill Tracts is widely known for the existence of a diverse variety of medicinal plants, most of which are yet to be studied scientifically. It is expected that the present survey can provide insights into the ancient medicinal practices of the Chakma tribe, which in turn can lead to successful discoveries of efficacious medicines against difficult to cure diseases like cancer, hypertension, diabetes, and rheumatism.
Apples ( MALUS sp., Rosaceae) are a rich source of nutrient as well as non-nutrient components and contain high levels of polyphenols and other phytochemicals. Main structural classes of apple constituents include hydroxycinnamic acids, dihydrochalcones, flavonols (quercetin glycosides), catechins and oligomeric procyanidins, as well as triterpenoids in apple peel and anthocyanins in red apples. Several lines of evidence suggest that apples and apple products possess a wide range of biological activities which may contribute to health beneficial effects against cardiovascular disease, asthma and pulmonary dysfunction, diabetes, obesity, and cancer (reviewed by Boyer and Liu, Nutr J 2004). The present review will summarize the current knowledge on potential cancer preventive effects of apples, apple juice and apple extracts (jointly designated as apple products). In brief, apple extracts and components, especially oligomeric procyanidins, have been shown to influence multiple mechanisms relevant for cancer prevention in IN VITRO studies. These include antimutagenic activity, modulation of carcinogen metabolism, antioxidant activity, anti-inflammatory mechanisms, modulation of signal transduction pathways, antiproliferative and apoptosis-inducing activity, as well as novel mechanisms on epigenetic events and innate immunity. Apple products have been shown to prevent skin, mammary and colon carcinogenesis in animal models. Epidemiological observations indicate that regular consumption of one or more apples a day may reduce the risk for lung and colon cancer.
Acute respiratory infections represent a significant cause of over-prescription of antibiotics and are one of the major reasons for absence from work. The leaves of Andrographis paniculata (Burm. f.) Wall ex Nees (Acanthaceae) are used as a medicinal herb in the treatment of infectious diseases. Systematic literature searches were conducted in six computerised databases and the reference lists of all papers located were checked for further relevant publications. Information was also requested from manufacturers, the spontaneous reporting schemes of the World Health Organisation and national drug safety bodies. No language restrictions were imposed. Seven double-blind, controlled trials (n = 896) met the inclusion criteria for evaluation of efficacy. All trials scored at least three, out of a maximum of five, for methodological quality on the Jadad scale. Collectively, the data suggest that A. paniculata is superior to placebo in alleviating the subjective symptoms of uncomplicated upper respiratory tract infection. There is also preliminary evidence of a preventative effect. Adverse events reported following administration of A. paniculata were generally mild and infrequent. There were few spontaneous reports of adverse events. A. paniculata may be a safe and efficacious treatment for the relief of symptoms of uncomplicated upper respiratory tract infection; more research is warranted.
The natural product justicidin A, an arylnaphthalide lignan isolated from Justicia procumbens, significantly inhibited the growth of human colorectal cancer cells HT-29 and HCT 116 at day 6 post-treatment. Further study revealed that justicidin A-treated HT-29 and HCT 116 colorectal cancer cells died of apoptosis. Justicidin A treatment caused DNA fragmentation and an increase in phosphatidylserine exposure of the cells. The number of cells in the sub-G1 phase was also increased upon justicidin A treatment. Caspase-9 but not caspase-8 was activated, suggesting that justicidin A treatment damaged mitochondria. The mitochondrial membrane potential was altered and cytochrome c and Smac were released from mitochondria to the cytoplasm upon justicidin A treatment. The level of Ku70 in the cytoplasm was decreased, but that of Bax in mitochondria was increased by justicidin A. Since Ku70 normally binds and sequesters Bax, these results suggest that justicidin A decreases the level of Ku70 leading to translocation of Bax from the cytosol to mitochondria to induce apoptosis. Oral administration of justicidin A was shown to suppress the growth of HT-29 cells transplanted into NOD-SCID mice, suggesting chemotherapeutic potential of justicidin A on colorectal cancer cells.
The in vitro cytotoxicities of the ethanol extract of Andrographis paniculata (APE) and its main diterpenoid components were evaluated in various cancer cells. APE was found to be significantly growth inhibitory to human acute myeloid leukemic HL-60 cells with an IC50 value of 14.01 μg/mL after 24 h of treatment. Among the three main diterpenoids in A. paniculata, andrographolide exhibited the highest degree of cytotoxicity followed by deoxyandrographolide while neoandrographolide was the least effective. Laser confocal microscopy and gel electrophoresis studies revealed chromosomal DNA fragmentations suggesting the occurrence of apoptosis. An increase of G0/G1 phase cells from 51.88 % to 78.69 % was noted after andrographolide treatment for 36 h. The G0/G1 phase arrest and apoptosis were associated with disappearance of mitochondrial cytochrome c and increased expression of Bax but decreased expression of Bcl-2 proteins in the inhibited cells. Although the order of all these events has not been determined, it is concluded that APE and andrographolide induce cell cycle arrest and affect an intrinsic mitochondria-dependent pathway of apoptosis by regulating the expression of some pro-apoptotic markers in HL-60 cells.
Abbreviations
APE:extract of Andrographis paniculata
DSAM:deoxyandrographolide succinic acid monoester
HIV:human immunodeficiency virus
MTT:3-[4,5-dimethylthiazol-2-yl]-3,5-diphenyl-tetrazolium bromide
AO/EB:acridine orange/ethidium bromide
PBS:phosphate buffer saline
FACS:fluorescence-activated Cell Sorting system
PI:propidium iodide
SDS-PAGE:sodium dodecyl polyacrylamide gel electrophoresis
ECL:enhance dchemiluminescence
The stability of andrographolide in powdered Andrographis Herb--the aerial part of Andrographis paniculata (Burm. f.) Nees (Acanthaceae)--was determined using a heat-accelerated experiment to reveal a second-order kinetics of degradation. The fast decomposition was observed regardless of the method of analysis. The rate constant of the decomposition of andrographolide at 25 degrees C ( K(25)( degrees C)), predicted from the Arrhenius plot, was 6.58 x 10 (-6) d (-1).
We previously observed that rhinacanthins-C, -N and -Q, three main naphthoquinone esters isolated from the roots of Thai medicinal plant; Rhinacanthus nasutus KURZ. (Acanthaceae) induced apoptosis of human cervical carcinoma HeLaS3 cells. Since these rhinacanthins showed limited solubility in aqueous medium, we attempted to entrap them into liposomal membrane: Liposomalization enabled injection of the drugs and the drugs were expected to transfer to lipoproteins in the bloodstream. Liposomal formulations of rhinacanthins-C, -N and -Q showed strong antiproliferative activity against HeLaS3 cells with the IC50 values of 32, 17, 70 microM; 19, 17, 52 microM and 2.7, 2.0 and 5.0 microM for the exposure time of 24, 48, and 72 h, respectively. These liposomes suppressed the tumor growth in Meth-A sarcoma-bearing BALB/c mice at the dose of 5.0 mg/kg/d for 10 d. Among rhinacanthins, liposomal rhinacanthin-N significantly suppressed solid tumor growth. Based on these results, our findings demonstrated that rhinacanthin-N suppressed tumor growth in vivo, and suggested that liposomes are useful for preparing injectable formulation of hydrophobic drugs.
Plants have evolved multiple mechanisms to selectively suppress pathogens by production of secondary metabolites with antimicrobial activities. Therefore, direct selections for antiviral compounds from plants can be used to identify new agents with potent antiviral activity but not toxic to hosts. Here, we provide evidence that a class of compounds, seco-pregnane steroid glaucogenin C and its monosugar-glycoside cynatratoside A of Strobilanthes cusia and three new pantasugar-glycosides of glaucogenin C of Cynanchum paniculatum, are effective and selective inhibitors to alphavirus-like positive-strand RNA viruses including plant-infecting tobacco mosaic virus (TMV) and animal-infecting Sindbis virus (SINV), eastern equine encephalitis virus, and Getah virus, but not to other RNA or DNA viruses, yet they were not toxic to host cells. In vivo administration of the compounds protected BALB/c mice from lethal SINV infection without adverse effects on the mice. Using TMV and SINV as models, studies on the action mechanism revealed that the compounds predominantly suppress the expression of viral subgenomic RNA(s) without affecting the accumulation of viral genomic RNA. Our work suggested that the viral subgenomic RNA could be a new target for the discovery of antiviral drugs, and that seco-pregnane steroid and its four glycosides found in the two medicinal herbs have the potential for further development as antiviral agents against alphavirus-like positive-strand RNA viruses.
• antiviral drugs
• Strobilanthes cusia
• Cynanchum atratum
Andrographolide (Andro) is a potentially anti-inflammatory diterpenoid lactone isolated from the traditional herbal medicine Andrographis paniculata, which has been effectively used for the treatment of infection, inflammation, cold, fever and diarrhea in China for centuries. In the current study, we found that Andro significantly decreased the number of surviving hepatoma-derived Hep3B cells in the MTT assay and induced cell apoptosis. Further study showed that Andro induced activation of mitogen-activated protein kinases (MAPKs) including p38 kinase, c-Jun N-terminal kinase (JNK) and extracellular signal-related kinases (ERK1/2), but had no significant effect on caspase-3, Bcl-xL and Bcl-2, which are apoptosis-related proteins. Moreover, inhibition of JNK activation partially rescued the toxic effect of Andro on Hep3B cells. Therefore, our results indicate that the JNK signaling pathway plays an important role in the toxic effect of Andro on Hep3B cells.
Abbreviations
Andro:andrographolide
CDK:cyclin-dependent kinase
ELISA:enzyme-linked immunosorbent assay
ERK1/2:extracellular signal-related kinases
FBS:fetal bovine serum
HCC:hepatocellular carcinoma
HPLC:high pressure liquid chromatography
JNK:c-Jun N-terminal kinase
MAPK:mitogen-activated protein kinase
MEM:modified Eagle's medium
RTKs:receptor tyrosine kinases
This article has no abstract
Six new diarylbutane lignans, namely, justin A (1), (-)-dihydroclusin diacetate (2), secoisolariciresinol dimethyl ether diacetate (3), 5-methoxy-4,4'-di-O-methylsecolariciresinol diacetate (4), justin B (5), and justin C (6), together with three known diarylbutane lignans [2,3-demethoxysecisolintetralin acetate (7), secoisolariciresinol dimethyl ether (8), and 5-methoxy-4,4'-di-O-methylsecolariciresinol (9)], were isolated from the whole plant of Justicia procumbens. Their structures were established by spectral analysis.
The aim of this work is to clarify the antioxidant abilities of phenolic and enolic hydroxyl groups in curcumin. 1,7-bis(4-benzyloxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (BEC), 1,7-bis(4-hydroxy-3-methoxyphenyl)heptane-3,5-diol (OHC), 1,7-bis(4-hydroxy-3-methoxyphenyl)heptane-3,5-dione (THC), and 1,7-bis(3,4-dihydroxyphenyl)-1,6-heptadiene-3,5-dione (BDC) are synthesized to determine the antioxidant activities by using antiradical assays against 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical, galvinoxyl radical, and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonate) cation radical (ABTS*+) and by protecting DNA and erythrocyte against 2,2'-azobis(2-amidinopropane hydrochloride) (AAPH) induced oxidation. The phenolic hydroxyl is the main group for curcumin to trap DPPH, galvinoxyl, and ABTS*+ radicals. The conjugative system between enolic and phenolic hydroxyl groups is beneficial for curcumin to protect erythrocytes against hemin-induced hemolysis and to protect DNA against AAPH-induced oxidation, but is not beneficial for curcumin to protect erythrocytes against AAPH-induced hemolysis. More hydroxyl groups enhance the antioxidant effectiveness of curcumin in the experimental systems employed herein. Therefore, curcumin acts as an antioxidant through the phenolic hydroxyl group.
Rhinacanthone, a main bioactive naphthoquinone, isolated from roots of Rhinacanthus nasutus KURZ, (family Acanthaceae), a Thai traditional medicine, has been reported to possess anticancer effects, although the anticancer mechanism is still unclear. Therefore, we investigated the effects of rhinacanthone on cell proliferation, cell cycle progression and apoptosis induction in human cervical carcinoma (HeLa) cells. beta-Lapachone, an anticancer drug having a chemical structure related to rhinacanthone, was used as a positive control. The results demonstrated that rhinacanthone inhibited proliferation of HeLa cells in a dose-dependent manner and had greater efficacy than that of beta-lapachone: IC(50) values of the compound ranged from 1.2+/-0.1 to 5.5+/-0.86 muM for 2-24 h time periods. Rhinacanthone-treated HeLa cells displayed several apoptotic features as evidenced by the appearance of chromatin condensation, internucleosomal DNA fragmentation, increase in the proportion of sub G(1) apoptotic cells, and externalization of annexin-V. The apoptotic processes by the treatment with rhinacanthone involved in a marked increase in the level of pro-apoptotic protein Bax and decrease in the levels of anti-apoptotic proteins Bcl-2 and survivin as well as subsequent activation of caspase-9 and caspase-3. Moreover, rhinacanthone increased the expression of apoptosis-inducing factor (AIF) which would translocate from mitochondria to nucleus through cytosol, and induce apoptosis through caspase independent signaling pathway. Taken together, our findings for the first time demonstrate that rhinacanthone-induced apoptosis in HeLa cells is mediated primarily through the mitochondria-dependent signaling pathway, suggesting that it may be a promising agent for the treatment of human cervical cancer.
Resveratrol is a well-known natural antioxidant and cancer chemopreventive agent that has attracted much interest in the past decade. Resveratrol-directed compounds were synthesized, and their antioxidant effects against reactive oxygen species (ROS)-induced DNA damage, their prooxidant effects on DNA damage in the presence cupric ions, and their cytotoxic and apoptosis-inducing effects on human promyelocytic leukemia (HL-60) cells were investigated in vitro. It was found that the compounds bearing o-diphenoxyl groups exhibited remarkably higher activities in inhibiting ROS-induced DNA damage, accelerating DNA damage in the presence cupric ions, and inducing apoptosis of HL-60 cells compared with the ones bearing no such groups. The detail mechanism of the structure-activity relationship was also studied by the oxidative product analysis of resveratrol and its analogues with galvinoxyl radical or cupric ions and UV-visible spectra change in the presence cupric ions. This study reveals a good and interesting correlation between antioxidant and prooxidant activity, as well as cytotoxicity and apoptosis-inducing activity against HL-60 cells, and provides an idea for designing antioxidant-based cancer chemoprevention agents.
The immunomodulatory activity of HN-02, an extract containing a mixture of andrographolides (i.e., andrographolide [88 +/- 5 %] plus 14-deoxyandrographolide and 14-deoxy-11,12-didehydroandrographolide together [12 +/- 3 %]) in a pure powder form was evaluated at 1.0, 1.5, and 2.5 mg/kg on different in vivo and in vitro experimental models. In a delayed-type hypersensitivity (DTH) mouse model, potentiation of the DTH reaction was observed after treatment with cyclophosphamide (CYP) and HN-02 individually. However, CYP potentiation of the DTH reaction was reversed by HN-02 pretreatment. Furthermore, HN-02 treatment elevated the depressed hemagglutination antibody (HA) titer and increased the number of plaque-forming cells (PFCs) in the spleen cells of mice that had been treated with CYP and challenged with sheep red blood cells (SRBC). Further, it was also found that HN-02 treatment stimulated phagocytosis in mice. A significant increase in total WBC count and relative weight of spleen and thymus was observed in mice during 30 days of treatment with HN-02. The present experimental findings demonstrate that HN-02 has the ability to enhance immune function, possibly through modulation of immune responses altered during antigen interaction, and to reverse the immunosuppression induced by CYP.
Isolation of a broth extract of the endophytic fungus Corynespora cassiicola L36 afforded three compounds, corynesidones A (1) and B (3), and corynether A (5), together with a known diaryl ether 7. Compounds 1, 3, 5, and 7 were relatively non-toxic against cancer cells, and inactive toward normal cell line, MRC-5. Corynesidone B (3) exhibited potent radical scavenging activity in the DPPH assay, whose activity was comparable to ascorbic acid. Based on the ORAC assay, compounds 1, 3, 5, and 7 showed potent antioxidant activity. However, the isolated natural substances and their methylated derivatives (1-8) neither inhibited superoxide anion radical formation in the XXO assay nor suppressed TPA-induced superoxide anion generation in HL-60 cell line. Corynesidone A (1) inhibited aromatase activity with an IC(50) value of 5.30 microM.
From the leaves of Strobilanthes cusia, a folk remedy for athlete's foot in Okinawa, tryptanthrin was isolated as a strong antifungal substance against dermatophytes.
Ten antiviral lignans, seven known (justicidins A, B, C and D, diphyllin, diphyllin apioside and diphyllin apioside-5-acetate) and three new compounds, justicidinosides A (justicidin C 6'-O-glucoside), B (justicidin A 6'-O-glucoside) and C (justicidin B 6'-O-glucoside), were isolated from a methanolic extract of the aerial parts of Justicia procumbens var. leucantha. Justicidins A and B, diphyllin, diphyllin apioside and diphyllin apioside-5-acetate showed strong antiviral activity (the MIC were less than 0.25 microgram ml-1, respectively) against vesicular stomatitis virus and low cytotoxicity (the MTC were larger than 31 micrograms ml-1, respectively) against cultured rabbit lung cells (RL-33).
Fractionation of the EtOH extract of Justicia procumbens, guided by antiplatelet bioassay, led to the isolation of nine known arylnaphthalide lignans, neojusticin A (1), justicidin B (2), justicidin A (3), taiwanin E methyl ether (4), neojusticin B (5), chinensinaphthol methyl ether (6), taiwanin E (8), chinensinaphthol (9), and diphyllin (10), and a new arylnaphthalide lignan that was characterized by spectral means as 4'-demethylchinensinaphthol methyl ether (7). Compounds 1, 2, 4, and 8 significantly inhibited platelet aggregation.
A new lignan glycoside, 4-O-alpha-L-arabinopyranosyl-(1' "-->2' ')-beta-D-apiofuranosyldiphyllin (2), named procumbenoside A, and 11 known compounds were isolated from the whole plant of Justicia procumbens. The structure of 2 was established by spectral analysis and chemical methods. The known compounds justicidin A (1), diphyllin (3), and tuberculatin (4) showed potent cytotoxic effects against a number of cancer cells in vitro. Compounds 1 and 4 also strongly enhanced tumor-necrosis factor-alpha (TNF-alpha) generation from mouse macrophage-like RAW 264.7 cells stimulated with lipopolysaccharide (LPS).
The leaf of Strobilanthes cusia (Acanthaceae), popularly known as Da-Ching-Yeh, has been commonly used in traditional Chinese medicine. It is used for influenza, epidemic cerebrospinal meningitis, encephalitis B, viral pneumonia and mumps. It is also used to treat sore throat, aphthae and inflammatory diseases with redness of skin, etc. In this study, we evaluated the antinociceptive, anti-inflammatory and antipyretic effects of methanol extract of Strobilanthes cusia leaf. The results showed that the extract significantly inhibited the writhing responses of mice and decreased the licking time on both the early and late phases of the formalin test in a dose-dependent manner. It also reduced the paw edema induced by carrageenan in rats. In addition, it potently attenuated pyrexia induced by lipopolysaccharide.
The human bronchial epithelial cells are the primary sites of influenza virus infection. In this study, the effect of indirubin on the expression of the chemokine regulated on activation, normal T cell expressed and secreted (RANTES) by the influenza virus-infected H292 human epithelial cell line was examined. The expression of RANTES mRNA was analyzed using reverse transcription polymerase chain reaction and the concentration of RANTES production was determined by the enzyme-linked immunosorbent assay. At the non-cytotoxic concentrations, indirubin was found to reduce both the expression and production of RANTES in influenza A/NWS/33-infected H292 cells. Inhibition was also observed in influenza virus B/Lee-infected cells. Significant reduction of the expression of IL-8 was not observed after the infection. Indirubin-3'-oxime, a recently developed derivative with kinase inhibitory activity, also mediates a potent inhibitory effect on the expression of RANTES. The influenza virus infection-induced phosphorylation of the nuclear transcription NF-kB regulatory molecule IkBalpha and the p38 MAP kinase were also found to be inhibited by indirubin-3'-oxime. This finding suggests that indirubin is one of the components in the Chinese medicinal herbs Isatis indigotica and Strobilanthes cusia with immunomodulatory activity on the expression of RANTES.
Two new arylnaphthalide lignans, procumphthalide A (1) and 4-O-beta-D-glucopyranosyl-(1"'-->2")-beta-D-apiofuranosyldiphyllin, named procumbenoside B (2), along with cilinaphthalide B (3) and several other known compounds were isolated from the methanolic extracts of Justicia procumbens. By using NMR and other spectral methods, the structures of 1 and 2 were elucidated. Cilinaphthalide B (3), justicidin A (4), and taiwan E methyl ether (5) were shown to have an antiplatelet effect in human plateletrich plasma. In human citrated PRP, 5 showed a strong inhibitory effect on platelet aggregation induced by adrenaline in a concentration-dependent manner, with an IC(50) value of about 27.6 microM.
Exposure of macrophages to lipopolysaccharide (LPS) induces release of tumor necrosis factor-alpha (TNF-alpha), which is initially synthesized as a 26-kDa pro-TNF-alpha followed by proteolytic processing to a 17-kDa secreted form. In this study, justicidin A, an arylnaphthalide lignan isolated from Justicia procumbens, was found to inhibit LPS-stimulated TNF-alpha release from RAW 264.7 macrophages in a concentration- and time-dependent manner, and the underlying mechanism was investigated. In the presence of justicidin A, challenge with LPS increased the steady-state level of the 26-kDa membrane-bound form of TNF-alpha protein, whereas justicidin A had little effect on the expression of TNF-alpha mRNA and on the synthesis of pro-TNF-alpha protein. Results of the pulse-chase experiment, revealed that the conversion of pro-TNF-alpha to mature TNF-alpha was inhibited by justicidin A. Moreover, justicidin A suppressed the transport of TNF-alpha to cell surface as analyzed by flow cytometry. The immunofluorescence analysis demonstrated that large amounts of LPS-induced TNF-alpha accumulated primarily within Golgi complex. These results indicate that justicidin A inhibits TNF-alpha release at the step of transport of pro-TNF-alpha to cell surface, and this leads to the accumulation of TNF-alpha in Golgi complex in RAW 264.7 macrophages.
The root of Strobilanthes cusia BREMEK. (Acanthaceae), popularly known as Da-Ching-Yeh, has been commonly used in traditional Chinese medicine. It is used to treat influenza, epidemic cerebrospinal meningitis, encephalitis B, viral pneumonia, mumps, and severe acute respiratory syndrome (SARS). In this study, we found a new lignan glycoside (6) and two new phenylethanoid glycosides (7, 8) together with five known compounds as chemical constituents of Strobilanthes cusia root. Some samples were examined for anti-herpes simplex virus type-1 (HSV-1) activity. Among the tested samples, lupeol showed anti-HSV-1 activity (EC(50): 11.7 microM) and showed 100% inhibition of virus plaque formation at 58.7 microM.
Andrographolide is the main labdane diterpene present in Andrographis paniculata. Two lines of evidence report immunostimulant and anti-inflammatory properties for andrographolide in different models. Using murine T-cells in vitro we demonstrated that andrographolide and to a lesser extent, 14-deoxyandrographolide (14-DAP), reduced significantly, in a dose-dependent manner, the IFN-gamma production induced by concanavaline A (CON-A), with an IC50 of 1.7 +/- 0.07 microM and 35.8 +/- 0.50 microM, respectively. Andrographolide, but not 14-DAP, inhibited partially the IL-2 production induced by CON-A. Andrographolide at doses of 5 and 10 microM reduced the extracellular-signal-regulated protein kinase (ERK1/2) phosphorylation induced by CON-A, whereas 14-DAP only reduced ERK1 and partially the ERK2 phosphorylation. The inhibition of ERK1/2 phosphorylation was associated to a decrease in the IFN-gamma production, due that UO126, a specific ERK1/2 inhibitor, also reduced the IFN-gamma production in murine T-cells induced by CON-A. Additionally, andrographolide and to a lesser extent 14-DAP, at doses of 50 microM and 100 microM, respectively, reduced the apoptosis induced by hydrocortisone and PMA in thymocytes, which was associated to a decrease in caspase-3 like activity. We conclude that both diterpenic labdanes isolated from A. paniculata can exert potent immunosuppressant effects without affecting the viability of the cells.
Justicia procumbens is a traditional Taiwanese herbal remedy used to treat fever, pain, and cancer. Justicidin A, isolated from Justicia procumbens, has been reported to suppress in vitro growth of several tumor cell lines as well as hepatoma cells. In this study, justicidin A activated caspase-8 to increase tBid, disrupted mitochondrial membrane potential (Delta psi(m)), and caused the release of cytochrome c and Smac/DIABLO in Hep 3B and Hep G2 cells. Justicidin A also reduced Bcl-x(L) and increased Bax and Bak in mitochondria. Caspase-8 inhibitor (Z-IETD) attenuated the justicidin A-induced disruption of Delta psi(m). Growth of Hep 3B implanted in NOD-SCID mice was suppressed significantly by oral justicidin A (20 mg/kg/day). These results indicate that justicidin A-induced apoptosis in these cells proceeds via caspase-8 and is followed by mitochondrial disruption.
Andrographis paniculata has been widely used as a traditional medicine for the treatment of common cold, diarrhea and hypertension. The three major active diterpenoids are andrographolide (AP1), 14-deoxy-11,12-didehydroandrographolide (AP3) and neoandrographolide (AP4). It has been reported that AP3 has hypotensive and vasorelaxation effects. However, there is only limited information on the cardiovascular effects of the other diterpenoids and crude extracts containing different levels of AP3. Therefore, the present study investigated the effects of these diterpenoids, AP1, AP3, and AP4, isolated from A. paniculata, and different aqueous plant extracts on blood pressure, vascular and chronotropic responses by using conscious rats and their isolated aortas and right atria as the test models. Among the three major diterpenoids, AP3 was the most potent compound for inducing vasorelaxation and decreasing heart rate. In addition, Extract B (high level of AP3) had greater hypotensive effect in conscious rats than Extract A (low level of AP3). Verapamil, a Ca2+ channel blocker, also had a hypotensive effect less than that of Extract C containing a high level of AP3. At the doses and durations of Extract A and B which produced hypotension, the responses of the Extract A-treated aorta to norepinephrine, and the vascular muscarinic responses to acetylcholine of both extracts were decreased. However, repeated doses of both extracts did not alter cardiac beta-adrenoceptor and muscarinic responses of extract-treated rats to NE and ACh, respectively. The results of this study suggest that vascular smooth muscle is the major site of these hypotensive effects of both AP3 and A. paniculata extracts. Furthermore, the consumption of A. paniculata products containing high levels of AP3 may be responsible for causing hypotension in some patients taking this herbal drug.
Five 2,4,6-prenylated phloroglucinols, garcinielliptones HA (1), HB (2), HC (3), HD (4) and HE (5), were isolated from the heartwood of Garcinia subelliptica Merr. Their structures, including relative configurations, were elucidated by means of spectroscopic data analysis. The ability of phloroglucinols, 1-5 and lignans, tuberculatin (8), justicidin A (9), procumbenoside A (10) and ciliatosides A (11) and B (12), isolated from Justicia ciliata and Justicia procumbens, to induce DNA-cleavage activity was examined using pBR322, a supercoiled, covalently closed circular DNA, and it was analyzed by agarose gel electrophoresis. In the presence of Cu (II), compounds 3, 8, 10 and 11 caused significant breakage of supercoiled plasmid pBR322. The products were relaxed circles with no detectable linear forms. In the Cu(II)-mediated DNA damage of 3 and selective compound 8, Cu(I) was shown not to be an essential intermediate by using the Cu(I)-specific sequestering reagent neocuproine.
Inhibition of RANTES expression by indirubin in influenza virus-infected human bronchial epithelial cells
- Nk Mak
- Cy Leung
- Xy Wei
- Xl Shen
- Rn Wong
- Kn Leung
- Mc Fung
Mak NK, Leung CY, Wei XY, Shen XL, Wong RN, Leung KN, Fung MC. Inhibition of RANTES expression by indirubin in influenza virus-infected human bronchial epithelial cells. Biochem Pharmacol 2004; 67: 167–174
Studies on the Acanthaceae of Thailand
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Hansen B. Studies on the Acanthaceae of Thailand. Fl Males Bull 1985;
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A Textbook of botany: angiosperms
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