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Diuretic Activity of Ethanol Extract of Piper attenuatum Leaves Might Be Due to the Inhibition of Carbonic Anhydrase Enzyme: An in vivo and in silico Investigation
... shown that P. attenuatum exhibits antibacterial, anticancer, antidiabetic, anti-inflammatory, antipyretic, diuretic, hepatoprotective, and hyperlipidemic activities [7]. ...
... nigrum) [4,5]. The leaves and roots of P. attenuatum are traditionally used to treat malaria, headache, hepatitis, mechanical injury, muscular pain, and pulmonary and urinary disorders [6][7][8]. ...
... The studies of the chemical composition of P. attenuatum have identified alkaloids, amides lignans, neolignans, and terpenes [7,9]. A few research groups have investigated the biological activities of P. attenuatum extracts, but there have been no systematic studies on the chemical identification of its biological activities. ...
Piper attenuatum Buch-Ham, a perennial woody vine belonging to the Piperaceae family, is traditionally used in Southeast Asia for treating various ailments such as malaria, headache, and hepatitis. This study described the isolation and identification of three new compounds, piperamides I-III (1–3), which belong to the maleimide-type alkaloid skeletons, along with fifteen known compounds (4–18) from the methanol extract of the aerial parts of P. attnuatum. Their chemical structures were elucidated using spectroscopic methods (UV, IR, ESI-Q-TOF-MS, and 1D/2D NMR). All the isolates were evaluated for their ability to inhibit IL-6 activity in the human embryonic kidney-Blue™ IL-6 cell line and their cytotoxic activity against ovarian cancer cell lines (SKOV3/SKOV3-TR) and chemotherapy-resistant variants (cisplatin-resistant A2780/paclitaxel-resistant SKOV3). The compounds 3, 4, 11, 12, 17, and 18 exhibited IL-6 inhibition comparable to that of the positive control bazedoxifene. Notably, compound 12 displayed the most potent anticancer effect against all the tested cancer cell lines. These findings highlight the importance of researching the diverse activities of both known and newly discovered natural products to fully unlock their potential therapeutic benefits.
In Ayurveda, polyherbal preparations appear to be an unavoidable medicinal approach. Many polyherbal medicines are prepared by local medical practitioners from rural regions of Thiruvananthapuram district, who follow their ethnic customs. The current study was an investigation of their medical system in order to determine the types of plants and plant parts that are used as main components in medicinal compositions. In this study, fifty plants from 34 distinct families were found to be used in the preparation of various Ayurvedic medicines. Solanaceae, Fabaceae, Zingiberaceae, and Piperaceae were the most important among the 34 families studied in terms of the number of herbal medications produced. The most prevalent constituent in 66 percent of currently investigated formulations is Zingiber officinale, followed by Piper longum and Aegle marmelos. The root was found to be the most commonly used plant portion, and harvesting the entire plant could lead to the natural depletion of supply materials. Many of the plants are also becoming threatened. This leads to drug adulteration, necessitating the development of procedures for detecting contaminated products.
Applying restriction site-associated DNA sequencing (RADseq) and target capture for Piper species from species-rich South America and India, Southeast Asia, and Africa will highlight the origin and evolution of Sri Lankan endemics, P. zeylanicum, P. walkerii, and P. trineuron. Looking into the genetic diversity of cultivated P. nigrum from different agroclimatic regions and available germplasm in Sri Lanka using RADseq will give an overview of the existing genetic diversity of black pepper, which is economically important and needs genetic improvement. Variation in flower composition (male, female or bisexual) across the spikes and their shape is of major interest to evolutionary and pollination biologists and plant systematists. The 3D shape models of flowers obtained by computed tomography of the wild species of Piper from Sri Lanka and cultivated P. nigrum will play an important role in revising the taxonomy and understanding the pollination biology of the genus.
Tea (Camellia sinensis L.) is considered as to be one of the most consumed beverages globally and a reservoir of phytochemicals with immense health benefits. Despite numerous advantages, tea compounds lack a robust multi-disease target study. In this work, we presented a unique in silico approach consisting of molecular docking, multivariate statistics, pharmacophore analysis, and network pharmacology approaches. Eight tea phytochemicals were identified through literature mining, namely gallic acid, catechin, epigallocatechin gallate, epicatechin, epicatechin gallate (ECG), quercetin, kaempferol, and ellagic acid, based on their richness in tea leaves. Further, exploration of databases revealed 30 target proteins related to the pharmacological properties of tea compounds and multiple associated diseases. Molecular docking experiment with eight tea compounds and all 30 proteins revealed that except gallic acid all other seven phytochemicals had potential inhibitory activities against these targets. The docking experiment was validated by comparing the binding affinities (Kcal mol⁻¹) of the compounds with known drug molecules for the respective proteins. Further, with the aid of the application of statistical tools (principal component analysis and clustering), we identified two major clusters of phytochemicals based on their chemical properties and docking scores (Kcal mol⁻¹). Pharmacophore analysis of these clusters revealed the functional descriptors of phytochemicals, related to the ligand–protein docking interactions. Tripartite network was constructed based on the docking scores, and it consisted of seven tea phytochemicals (gallic acid was excluded) targeting five proteins and ten associated diseases. Epicatechin gallate (ECG)-hepatocyte growth factor receptor (PDB id 1FYR) complex was found to be highest in docking performance (10 kcal mol⁻¹). Finally, molecular dynamic simulation showed that ECG-1FYR could make a stable complex in the near-native physiological condition.
Graphical abstract
The purpose of this review is to summarize the available antidiabetic medicinal plants in the Kingdom of Saudi Arabia with its phytoconstituents and toxicological findings supporting by the latest literature. Required data about medicinal plants having antidiabetic activities and growing in the Kingdom of Saudi Arabia were searched/collected from the online databases including Wiley, Google, PubMed, Google Scholar, ScienceDirect, and Scopus. Keywords used in search are in vivo antidiabetic activities, flora of Saudi Arabia, active ingredients, toxicological evaluations, and medicinal plants. A total of 50 plant species belonging to 27 families were found in the flora of Saudi Arabia. Dominant family was found Lamiaceae with 5 species (highest) followed by Moraceae with 4 species. β-Amyrin, β-sitosterol, stigmasterol, oleanolic acid, ursolic acid, rutin, chlorogenic acid, quercetin, and kaempferol are the very common bioactive constituents of these selected plant species. This paper has presented a list of antidiabetic plants used in the treatment of diabetes mellitus. Bioactive antidiabetic phytoconstituents which showed that these plants have hypoglycemic effects and highly recommended for further pharmacological purposes and to isolate/identify antidiabetes mellitus (anti-DM) active agents also need to investigate the side effects of active ingredients.
In continuation of phytochemical investigations of the methanolic extract of Dictyopteris hoytii, we have obtained twelve compounds (1–12) through column chromatography. Herein, three compounds, namely, dimethyl 2-bromoterepthalate (3), dimethyl 2,6-dibromoterepthalate (4), and (E)-3-(4-(dimethoxymethyl)phenyl) acrylic acid (5) are isolated for the first time as a natural product, while the rest of the compounds (1, 2, 6–12) are known and isolated for the first time from this source. The structures of the isolated compounds were elucidated by advanced spectroscopic 1D and 2D NMR techniques including 1H, 13C, DEPT, HSQC, HMBC, COSY, NEOSY, and HR-MS and comparison with the reported literature. Furthermore, eight compounds (13–20) previously isolated by our group from the same source along with the currently isolated compounds (1–12) were screened against the CA-II enzyme. All compounds, except 6, 8, 14, and 17, were evaluated for in vitro bovine carbonic anhydrase-II (CA-II) inhibitory activity. Eventually, eleven compounds (1, 4, 5, 7, 9, 10, 12, 13, 15, 18, and 19) exhibited significant inhibitory activity against CA-II with IC50 values ranging from 13.4 to 71.6 μM. Additionally, the active molecules were subjected to molecular docking studies to predict the binding behavior of those compounds. It was observed that the compounds exhibit the inhibitory potential by specifically interacting with the ZN ion present in the active site of CA-II. In addition to ZN ion, two residues (His94 and Thr199) play an important role in binding with the compounds that possess a carboxylate group in their structure.
Background: West Bengal is a state rich in floral biodiversity, with a high occurrence of medicinal plants being used. The state is populated by several ethnic communities, which still rely on various ethnomedical practises. Unfortunately information relating to the medicinally useful species is not holistic or is fraganmentory. We thus felt for a meta-analysis and abridged the available information of the state
Methods: The purpose of the present study was to annotate the published information on ethnomedicinal plants used by various indigenous communities of West Bengal, India. We therefore searched the published Journal articles, book chapters, and scientific reports using Web of Science, Scopus, Google, Google Scholar, individual journal databases and personal communication to review the ethnomedicinal information of the state.
Resutls: The meta-analysis resulted to a repository of 377 plant species represented by 99 families and 278 genera which were utilized for folk medicinal purposes. These ethnomedicinal plant species were used to treat a total of 126 different ailments and diseases. Stomach related problems were found common among the ethnic groups for which about half of the listed plant species were used for its treatment. Santal ethnic group was found richest with traditional knowledge related to folk medicinal purposes of 195 plant species. Some plant species Aerva lanata and Aristolochia indica were found commonly utilized by the communities. Leaves were prominently used plant part for folk therapies. Harvesting of the plants or their parts was largely unsustainable and is a matter of concern which needs urgent conservation action. Moreover, neglect and disregard to traditional culture and lores by the younger generation of the traditional communities is causing rapid decline and making the traditional knowledge system of these communities obsolete.
Conclusion: Documentation of ethnomedicinal plant species and the associated traditional knowledge is vital for well being of future generation as well as their conservation. This meta-analysis will be useful as baseline information for research on new drug development which will give national and global recognition to the traditional knowledge system of these ethnic societies while, will boost their healthcare, ecological, socio-economic and bio-cultural perspectives.
For evaluating the anti-pyretic effect of Ethanolic seed extract at a dose of 200mg/kg & 400mg/kg of plant Piper attenuatum (Buch Ham) obtained from Tropical botanic garden & research institute, Palode, Trivandrum, Kerala & authenticated by Dr. Mathew Dan, detailed study were carried out by using brewer yeast induced pyretic model. Rats were made pyretic by single subcutaneous injection of 20% yeast suspension in 0.9% saline at a dose of 1 ml. /100 g body weight. Paracetamol (150mg/kg) was used as standard drug. Oral administration of Ethanolic extract of plant causes decrease in rectal temperature of rats. Piperine, the amide present in extract is responsible for anti-pyretic activity by inhibiting the inflammatory mediator like tissue necrosis factor-α. The result in this study demonstrated the anti-pyretic effect of Piper attenuatum (B. Ham).
Piper attenuatum is a potent medicinal plant in the Indian systems of medicine. Piper attenuatum having Piperine, Piperlonguminine and other active constituents which are used as muscle relaxant, central nervous system depressant, in headache and as insecticide agent against Musca domestica. Piperine reduced the total body temperature and display analgesic, and anti-inflammatory activities. The aim of present study is to determine the Anti-Hyperlipidemic activity of Ethanolic seed extract of plant Piper attenuatum (Linn.) B. Ham. (Fam. Piperaceae). Piperine was the first amide to be isolated from Piper species. Ethanolic extracts of Piper attenuatum with a dose of 200 mg/kg exhibited significant Anti-Hyperlipidemic activity in Triton X-100 Induced Hyperlipidemia in rats (P<.05). It was found that Piperine & Piperlonguminine the active constituent of the plant was responsible for the Anti-Hyperlipidemic activity because this constituent have the ability to reduce the Total Cholesterol & Total Triglyceride level in rats. Fenofibrate was used as standard drug (65 mg/kg). The total time period of this study was one week.
Medicinal plants are potential source of therapeutic aids and they have attained a significant role for both human and animals, not only in diseased conditions but also for maintaining health. The increasing interest in plants derived medicines is mainly due to the current widespread belief that "Green medicine" is safe while costly synthetic drugs have serious side effects. Various tropical and subtropical plant species had been used from ancient time and placed in the various system of medicine like Indian Ayurvedic system as a medicine. Piper attenuatum (B. Ham) an important Piper species mainly found in the southern regions of India. Caesalpinia crista (linn) of family Fabaceae is a moderately size deciduous tree, growing wild throughout the deciduous forest of India. They are popular in indigenous system of medicine like Ayurveda, Siddha, Unani and Homoeopathy. There are insufficient research about the mechanisms behind the medicinal action Piper attenuatum (B. Ham) & Caesalpinia crista (linn) but they have diverse pharmacological activities like antibacterial, anti-inflammatory, anti-hyperglycemic, antioxidant any many more are reported from various extracts of the plant. Piper attenuatum (B. Ham) contain alkaloids like Piperine and Piperlonguminine which are responsible for therapeutic efficacy while Caesalpinia crista (linn) has carbohydrates, alkaloids, Glycosides, tannins, flavonoids & Coumarins. The current article provides an updated review on recent advancement on Pharmacognosy, chemistry and pharmacological activities of Piper attenuatum (B. Ham) & Caesalpinia crista (linn).
medicine that the phytochemical constituents present in P. attenuatum (B. Ham) have Antioxidant and skeletal muscle relaxant activity. So the present study aimed to evaluate anti–oxidant and skeletal muscle relaxant activity of ethanolic, aqueous and ethanolic leaf extract of plant P. attenuatum (B. Ham), respectively. Antioxidant activity was evaluated by in vitro as well as in vivo methods. Invitro method we used DPPH (2, 2-diphenyl-1-picrylhydrazyl) free radical scavenging assay and H2O2 (Hydrogen Peroxide) scavenging assay while in vivo methods antioxidant enzymes like Superoxide Dismutase (SOD) and reduced glutathione (GSH) were assayed by using animal models. Anti-oxidant activity of following concentrations 10μg/mL, 20μg/mL, 30μg/mL, 40μg/mL and 50μg/mL were measured for both extracts. Ethanolic extract of P. attenuatum (B. Ham) was evaluated at dose of 100mg/kg & 200 mg/kg b.w. for skeletal muscle relaxant activity by using rota rod apparatus. The high antioxidant activity was found in the ethanolic extract of P. attenuatum (B. Ham) compared to aqueous one. For muscle relaxation, 200 mg/kg b.w. showed a significant reduction in the time spent by the animals on the revolving rod compared to the control. From the above study it may be concluded that both extract of P. attenuatum (B. Ham) having Anti – oxidant and skeletal muscle relaxant activity.
Keywords: Anti – oxidant activity, DPPH, P. attenuatum (B. Ham), Skeletal muscle relaxant activity.
Indian J. Pharm. Biol. Res. (2020): https://doi.org/10.30750/ijpbr.8.4.1
Piper attenuatum B. Ham and Caesalpinia crista Linn are traditional medicinal plants in India. It has been claimed in traditional Indian system of medicine that the phytochemical constituents present in both plants having hepatoprotective activity. So, the aim of the present study was to evaluate hepatoprotective potential of ethanolic leaf extract of plant Piper attenuatum B. Ham and Caesalpinia crista Linn. Hepatoprotective potential of ethanolic leaf extract of Piper attenuatum B. Ham and Caesalpinia crista Linn were evaluated by using D-Galactosamine (400 mg/kg) induced liver toxicity model in rats. 100 mg/kg and 200 mg/kg dose selected for evaluation of hepatoprotective potential for both plants. Various biochemical parameters like AST/SGOT, ALT/SGPT, ALP, Total protein and Serum bilirubin were analyzed for different groups. Liver histopathology was also carried out for various groups. Silymarin (50 mg/kg) used as standard drug. Both the plant ethanolic extracts showed significant hepatoprotective potential. Piper attenuatum B. Ham ethanolic extract 200 mg/kg showed best hepatoprotective activity among all other groups. From the above study it may be possible that Piperine and flavonoids present in ethanolic leaf extracts of Piper attenuatum B. Ham and Caesalpinia crista Linn respectively responsible for hepatoprotective potential.
New derivatives were synthesised by reaction of amino-containing aromatic sulphonamides with mono-, bi-, and tricyclic anhydrides. These sulphonamides were investigated as human carbonic anhydrases (hCAs, EC 4.2.1.1) I, II, IX, and XII inhibitors. hCA I was inhibited with inhibition constants (Kis) ranging from 49 to >10,000 nM. The physiologically dominant hCA II was significantly inhibited by most of the sulphonamide with the Kis ranging between 2.4 and 4515 nM. hCA IX and hCA XII were inhibited by these sulphonamides in the range of 9.7 to 7766 nM and 14 to 316 nM, respectively. The structure–activity relationships (SAR) are rationalised with the help of molecular docking studies.
A 60 year married female from Chennai presented with pain and restricted abduction, adduction, external rotation and flexion of right shoulder both in active and passive movements for 2 months. She was diagnosed to be affected by adhesive capsulitis which is equated to Kumbavatham, one of the vatha diseases mentioned in Siddha system of medicine. She was treated with Siddha Varmam therapy and thokkanam with Vathakesari thylam. After 15 days of hospital stay the patient was discharged and was followed for 6 months. There were no adverse reactions/events observed during the course of treatment. The combination therapy has provided the reduction in pain and restricted movements which was measured using goniometer and SPADI index.
The “tail-approach” has become a milestone in human carbonic anhydrase inhibitor (hCAI) design for various therapeutics, including antiglaucoma agents. Beside the classical hydrophobic/hydrophilic division of hCAs active site, several subpockets have been importantly identified at the medium/outer active sites rim which could be targeted to increase CAI isoform-selectivity. This postulate is explored here by three-tailed benzenesulfonamide CAIs (TTI) to fully exploit the such amino acid differences among hCAs. In this proof-of-concept study, an extensive structure-activity-relationship (SAR) study was carried out with thirty-two such benzenesulfonamides differing for tails combination, that were assayed for hCAs I, II, IV, and XII inhibition. A structural study was undertaken by X-ray crystallography and in silico tools to assess the ligand/target interaction mode. The most active and selective inhibitors against isoforms implicated in glaucoma were assessed in a rabbit model of the disease achieving an intraocular pressure lowering action comparable to the clinically used dorzolamide.
Background: Macrothelypteris torresiana (Gaudich) is a species of fern having a wide range of reputed medicinal properties for the treatment of inflammation, fever, renal failure, stomach problems, etc. Objective: The present investigation focused on the evaluation of toxicity profile and diuretic and laxative activities of ethanol extract from M. torresiana aerial parts (EEMTAP), with in silico docking studies of polyphenolic compounds on carbonic anhydrase (CA)-II, an enzyme target for diuretic activity. Materials and Methods: Acute and subacute toxicity was performed according to the Organization for Economic Cooperation and Development guidelines. EEMTAP at doses of 200, 400, and 600 mg/kg, p.o., employed for the assessment of diuretic and laxative activities with loperamide-induced constipation in Wistar albino rats. Furosemide (10 mg/kg, p.o.), agar-agar (300 mg/kg, p.o.), and sodium picosulfate (5 mg/kg, p.o) were used as reference standards, respectively, for activity comparison. During saluretic activity study, total urine volume, body weight before and after the experiment, and urinary levels of Na + , K + (by flame photometry), and Cl − (by titrimetry) were estimated. Polyphenolic compounds such as caffeic acid and quercetin were successfully detected through chromatographic method of EEMTAP, and to rationalize the results obtained in diuretic activities, we carried out docking studies of the natural phenolic compounds against CA-II enzyme co-complexed with furosemide (Protein Data Bank ID: 1Z9Y CA-II in complex with furosemide as sulfonamide inhibitor). Results: In acute toxicity study, no mortality was observed at 2000 mg/kg, p.o., and in subacute toxicity study, the extract-treated group did not show any significant changes in body weight and organ weights. The hematological and biochemical parameters did not show any significant changes in the sample-treated groups when compared with the control group animals. The laxative activity of the extract was found to be in a dose-dependent increase in fecal output of rats at selected dose levels; similarly, EEMTAP significantly increased the urinary output as well as urinary electrolyte concentration in a dose-dependent manner. The molecular docking studies of phenolic compounds (caffeic acid and quercetin) into the binding site of CA II enzyme reveals that these analogues are having more favourable interaction when compared to the furosemide with better docking scores and hydrogen bonding interactions. Conclusion: The result demonstrated that the EEMTAP possesses a reasonable safety profile and shows promising diuretic and laxative activities in a dose-dependent manner.
Piper attenuatum is used as a traditional medicinal plant in India. One of the substances in P. attenuatum has been suggested to have anti-inflammatory effects. However, there is insufficient research about the anti-inflammatory mechanisms of action of P. attenuatum . The effects of P. attenuatum methanol extract (Pa-ME) on the production of inflammatory mediators nitric oxide (NO) and prostaglandin E 2 (PGE 2 ), the expression of proinflammatory genes, the translocation level of transcription factors, and intracellular signaling activities were investigated using macrophages. Pa-ME suppressed the production of NO and PGE 2 in lipopolysaccharide- (LPS-), pam3CSK4-, and poly(I:C)-stimulated RAW264.7 cells without displaying cytotoxicity. The mRNA expression levels of inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) were decreased by Pa-ME. P-ME reduced the translocation of p50/NF- κ B and AP-1 (c-Jun and c-Fos), as well as the activity of their upstream enzymes Src, Syk, and TAK1. Immunoprecipitation analysis showed failure of binding between their substrates, phospho- (p-) p85 and p-MKK3/6. p-p85 and p-MKK3/6, which were induced by overexpression of Src, Syk, and TAK1, were also reduced by Pa-ME. Therefore, these results suggest that Pa-ME exerts its anti-inflammatory effects by targeting Src and Syk in the NF- κ B signaling pathway and TAK1 in the AP-1 signaling pathway.
diversity of medicinal plants among the Adi community in four settlements which are located nearby area of Daying Ering Memorial Wild Life Sanctuary, Arunachal Pradesh, North East India.
The information was obtained through open and face-to-face interviews with the local knowledgeable people. A total of 73 plant species belonging to 66 genera and 44 families were documented in the study. The dominant family in the survey was Asteraceae (eight species) followed by Euphorbiaceae (seven species). Of the collected ethno medicinal plants, 46% herbs followed by 36% shrubs, 11% trees and 7% climbers. Among the different plant parts used for the
preparation of medicine, leaves were mostly used and predominantly used herbal preparations were taking raw materials directly followed by decoction. The herbal medicines to treat variety of ailments such as to heal cuts and wounds (eight species), jaundice (six species), bone fracture and gastritis (six species each), blood pressure, and ring worm (four species each), diarrhoea, headache, snake bite and toothache (three species each), anaemia, antidote, asthma, diabetes,
expel worms, gynaecological problems, loose motion, malaria, sinusitis, skin disease and stomach problems (two species each) and other diseases containing one species each were recorded. The plants like Alstonia scholaris, Diplazium esculentum, and Hydrocotyle
sibthorpioides should be given priority in conservation point of view, since these plants eroding rapidly in study area due to over- exploitation. The usage of plants by the Adi community reflects
their interest in herbal medicine and further investigation on these species may lead to the discovery of novel bioactive molecules.
The present ethno-botanical exploration conducted in the forest area of Japali Hanuman Theertham a sacred grove of Tirumala hills during the period of 2010-2013 resulted in the information about the uses of traditional medicinal plants of 85 species belonging to 47 families to treat 46 types of ailmentsand utilization of different forest plant resources. Out of 85 plant species the dominant life forms of herbs (40), shrubs (17), trees (17), climbers (08), lianas (02) and creepers (01).The grove having endemic medicinal plants and owing to anthropogenic pressures, they are in extreme state of vulnerability. The information gathered from Japali Hanuman Theertham indicates that the tribal people of this region possess good knowledge of herbal drugs. The ethnomedicinal information has been eradicating day by day due to lack of proper interest in the younger generations of ethnic groups. Hence the present study had been focused on the ethnic groups of Tirumala who are collecting medicinal plants from Japali Hanuman Theertham, a sacred grove located in Tirumala- Seshachalam hill range of Chittoor District, Andhra Pradesh, India.The further research will be carried out on isolation of active ingredients from medicinal plant species for effective treatment of particular diseases and measures should be taken to conserve the endangering ethnomedicinal knowledge of Chenchu and Nakkala tribes for future generations and endangered medicinal plants for ecological balance and sustainable environmentdevelopment.
PubChem (https://pubchem.ncbi.nlm.nih.gov) is a public repository for information on chemical substances and their biological activities, launched in 2004 as a component
of the Molecular Libraries Roadmap Initiatives of the US National Institutes of Health (NIH). For the past 11 years, PubChem
has grown to a sizable system, serving as a chemical information resource for the scientific research community. PubChem consists
of three inter-linked databases, Substance, Compound and BioAssay. The Substance database contains chemical information deposited
by individual data contributors to PubChem, and the Compound database stores unique chemical structures extracted from the
Substance database. Biological activity data of chemical substances tested in assay experiments are contained in the BioAssay
database. This paper provides an overview of the PubChem Substance and Compound databases, including data sources and contents,
data organization, data submission using PubChem Upload, chemical structure standardization, web-based interfaces for textual
and non-textual searches, and programmatic access. It also gives a brief description of PubChem3D, a resource derived from
theoretical three-dimensional structures of compounds in PubChem, as well as PubChemRDF, Resource Description Framework (RDF)-formatted
PubChem data for data sharing, analysis and integration with information contained in other databases.
Background:
In ayurvedic system of medicine a vast number of medicinal plants are reported to possess with antiurolithic activity.
Aim:
To study the antiurolithic activity of alcoholic extract of roots of Cissampelos pareira (AERCP) in chemicals induced urolithiasis in albino rats.
Materials and methods:
Nine Groups of albino rats (n=6) were used to evaluate the antiurolithic activity of alcoholic extract of roots of C.Pareira. Group I received with rat chow diet, Group II with 2% Ammonium chloride (AC) and 0.75% Ethylene glycol (EG) Group III with EG plus AC and cystone (5 ml/kg), Groups IV, V, VI with low (100 mg/kg), medium (200 mg/kg), and high (400 mg/kg) doses of root extract, Groups VII, VIII, IX with EG plus AC and low (100 mg/kg), medium (200 mg/kg), and high (400 mg/kg) doses of root extract respectively for 10 days. Urolithiasis was induced by supplying drinking water mixed with 2% Ammonium chloride and 0.75% Ethylene glycol for 10 days. On 11th day three rats from each Group were kept in one metabolic cage and urine (pooled) collected for 24h was subjected for estimation of biochemical parameters like urinary calcium, uric acid and magnesium. Blood was collected on the same day and analysed for various parameters. Kidneys were observed for the histopathological changes.
Results:
The rats treated with alcoholic extract of roots of C. pareira at 03 different doses significantly (p≤ 0.05) reduced urinary calcium, uric acid and increased urinary magnesium levels, reduced serum calcium, creatinine and increased serum magnesium. Rats treated with 200 mg/kg and 400 mg/kg doses revealed less tissue damage and the cytology of the nephrotic tissue was almost similar to normal control Group I rats.
Conclusion:
RESULTS showed that alcoholic extract of roots of C. pareira has exhibited a significant antiurolithic effect against urolithiasis in experimental rats.
Indian traditional medicinal plant Piper attenuatum (Buch-Ham) was investigated for its antioxidant and anticancer activity. Three extracts were prepared using ethyl acetate, ethanol and methanol. In vitro antioxidant activity was performed by ABTS {2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)} free radical scavenging method. All three extracts reduced the free radicals produced by ABTS in a concentration dependent manner which could be compared to the standard (Gallic acid). Invitro anticancer activity of all extracts was carried out by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay method against MCF7 (Michigan Cancer Foundation-7) cell lines. None of the extract showed anticancer activity when compared with the standard (Mitomycin-C) indicating that p. attenuatum is deprived of antiproliferative or cytotoxic components.
The present study was aimed to investigate the diuretic effects of aqueous and crude ethanol extracts of Bombax ceiba L. fruits (family, Bombacaceae) using acute model in rats. A single individual dose of aqueous and ethanol extract of B. ceiba fruit (200 mg/kg and 400 mg/kg, p.o., each), frusemide and hydrochlorothiazide, (25 mg/kg, p.o., each) as reference diuretic drugs, were administered orally to dehydrated rats. Control group rats were fed with normal saline (25 ml/kg, p.o.). All rats were caged in metabolic cages in pairs and their urine output was monitored at 5 and 24 h intervals. Both extracts significantly increased the urine output in higher doses. Although, the onset of this diuretic action was gradual (within 5 h), it lasted throughout the studied period (up to 24 h). Further, the intensity of diuresis induced by aqueous extract (400 mg/kg) in 5 h was almost similar to that of frusemide and hydrochlothiazide. Aqueous extract of B. ceiba fruit also caused marked increase in urinary Na(+) and K(+) levels. However, the routine urinalysis showed non-significant alterations in pH and specific gravity by either dose of crude extracts of B. ceiba fruits. These effects demonstrate possible diuretic actions of B. ceiba fruit extracts and support its folklore use in various urinary ailments. Further studies need to be done to characterize the active phytoconstituents from fruits.
The secondary metabolites isolated from Piper species for the period 1907 to June 1996 have been reviewed. Nearly six hundred chemical constituents belonging to different classes of bioactive compounds are listed together with their source(s) and references. © 1997 Elsevier Science Ltd
Current chemotherapeutic options for African trypanosomiasis in humans and livestock are very limited. In the present study, a total of 71 medicinal plant specimens from 60 plant species collected in Myanmar were screened for antitrypanosomal activity against trypomastigotes of Trypanosoma evansi and cytotoxicity against MRC-5 cells in vitro. The methanol extract of dried rootbark of Vitis repens showed the highest antitrypanosomal activity with IC(50) value of 8.6 +/- 1.5 microg/ml and the highest selectivity index of 24.4. The extracts of Brucea javanica, Vitex arborea, Eucalyptus globulus and Jatropha podagrica had also remarkable activity with IC(50) values and selectivity indices in the range of 27.2-52.6 microg/ml and 11.4-15.1 respectively.
Aristolactams, having a phenanthrene chromophore are a small group of compounds mainly found in the Aristolochiaceae together with the aristolochic acids and 4,5-dioxoaporphines. In this report, these three important classes of natural products are reviewed and classified on the basis of their oxygenation pattern. In addition the biological activities of these compounds and their general chemistry are discussed.
Steroid and painkiller abuse induced peptic ulcer disease, which causes abdominal pain, fullness, heartburn, and nausea. Medicinal plants have treated ulcers for centuries. We used Piper attenuatum ethanolic plant extracts for aspirin to induce ulcers in Wistar rats to test the leaf ethanolic extract's antiulcer properties. The control group is normal saline, the standard group is ranitidine (20 mg/kg), and the extract-treated groups are 100 mg/kg and 200 mg/kg ethanolic plant extracts. Ulcer Score, gastric juice volume, free and total acidity, ulcer index, ulcer protection, and pH were measured. The ulcer score was determined via rat stomach biopsies. Plant ethanolic extracts are gastroprotective. Only pH increased compared to the control group. Piper attenuatum ethanolic extract is the most gastroprotective at 200 mg/kg. Extracts were phytochemically and analytically assessed. Phytochemical screening demonstrates that plant extracts contain alkaloids, amides, glucose, proteins, glycosides, steroids, flavonoids, etc. This research suggests that phytoconstituents may have anti-ulcer potential, although structural elucidation of bioactive chemicals is needed. Molecular docking showed better binding affinity versus the 3D structure of pig gastric H+/K+ ATPase isoforms phytoconstituents Cepharadione A, Cepharadione B, Guineensine, Norcepharadione B, and Piperlonguminine. With these significant results, it may be a drug in the future.
The tropical plant species of family Piperaceae had been consumed from ancient time and has reputed place in the Indian Ayurvedic system as a medicine and as a spice in foods. Piper species are also an important part in folklore medicine of Latin America and West Indies. Piper attenuatum Buch.-Ham. ex Miq., an important Piper species, mainly found in the southern tropical and sub-tropical regions of India and is much used in the Ayurvedic system of medicine. However, there is insufficient research about the mechanisms behind the medicinal action of P. attenuatum but diverse pharmacological activities like antibacterial, anti-inflammatory, anti-hyperglycaemic and antioxidant are reported from various extracts of this plant. It contains various important phytochemicals like crotepoxide, piperine, guineensine and piperlonguminine which are responsible for its therapeutic efficacy. Crotepoxide is reported to exhibit significant antitumor activity. The seed extract is reported to have antioxidant activity. Piperine is reported to increase the bioavailability of other drugs by interacting with various enzymes responsible for metabolism. The current article provides an updated literature review on recent advancement on pharmacognosy, chemistry and pharmacological activities of P. attenuatum.
Background:
One of the most challenging effects of diabetes is diabetic foot ulceration (DFU). DFU may occur in up to one-third of individuals with diabetes mellitus (D.M.) at some point in their lives. The major cause of morbidity in D.M. patients is DFU. The length of treatment is difficult, and DFU recurrence is common.
Objective:
The most crucial element for the treatment and prevention of DFUs require a multidisciplinary approach. Patients who are at risk should be identified, depending on the type of risk, prophylactic actions etc. It is imperative to identify at-risk patients and take preventative measures accordingly.
Method:
The at-risk diabetes-related foot ulcer was identified based on the risk category classification, while the foot ulcers were evaluated using Wagner's classification system.
Results:
Literature reported that patients with lower limb vascular insufficiency, loss of vibratory sensation, or protective sensation loss have an increased risk of developing foot ulcers. Proper categorization and therapeutic measures will be implemented after the DFU has been formed. The appropriate assessment and management of general health status should include glycemic control, the diagnosis and treatment of vascular disease, standard care for wounds, diagnosis, and infection treatments.
Conclusion:
The review reflects the updated awareness of the treatment and management of DFU based on the current and past literature and patent analysis.
The genus Piper, a member of the Piperaceae family, comprises >2000 species, of which many are well known to possess considerable economic and medicinal values. Lignans are essential ingredients and are rich in Piper plants. Although many phytochemical studies have reported many lignans identified from Piper plants, comprehensive research has not reviewed these compounds. Hence, the present review reports on natural lignans from the genus Piper and their pharmacological activities. At least 275 lignans have been discovered from the Piper genus until October 2022, including traditional lignans, neolignans, oxyneolignans, norlignans, secolignans, and polyneolignans, especially some neolignans and norlignans with novel and complex scaffolds. In addition, these lignans have been reported to show various pharmacological activities, such as antimicrobial, anti-inflammatory, neuroprotective, antioxidative, anti-platelet aggregation, cytotoxic, antiparasitic, CYP3A4 inhibitory activities, and so on. The current work presents an up-to-date critical review and a systematic summary of publications on lignans from the genus Piper to lay the groundwork and show better insights for further investigations.
Quantification of bioactive markers through modern analytical methods is very essential for establishing the authenticity and creditability of prescription and usage of herbal drugs formulations. In the present study, simultaneous quantification of rosmarinic acid (RA), quercetin (Q), glycyrrhizin (G) and betulinic acid (BA), in polyherbal formulation by high-performance thin-layer chromatography (HPTLC) method was developed. Mobile phase of ethyl acetate‒toluene‒methanol‒formic acid (7:1:0.5:0.5, V/V) was used on pre-coated plate of silica gel 60F254 and quantified by densitometric method. Validation of the method was done to demonstrate its selectivity, linearity, precision and accuracy as per the International Council for Harmonization (ICH) guidelines. Intra-day assay and inter-day assay precision of the analytes were less than 2%, and the average recovery rates obtained were in the range of 98.11‒101.14% for all with percent relative standard deviation (%RSD) below 2%. Correlation coefficient shows that the developed method was accurate and precise. This method can be used in the routine analysis of polyherbal formulations.
Piper species are aromatic plants used as spices in the kitchen, but their secondary metabolites have also shown biological effects on human health. These plants are rich in essential oils, which can be found in their fruits, seeds, leaves, branches, roots and stems. Some Piper species have simple chemical profiles, while others, such as Piper nigrum, Piper betle, and Piper auritum, contain very diverse suites of secondary metabolites. In traditional medicine, Piper species have been used worldwide to treat several diseases such as urological problems, skin, liver and stomach ailments, for wound healing, and as antipyretic and anti-inflammatory agents. In addition, Piper species could be used as natural antioxidants and antimicrobial agents in food preservation. The phytochemicals and essential oils of Piper species have shown strong antioxidant activity, in comparison with synthetic antioxidants, and demonstrated antibacterial and antifungal activities against human pathogens. Moreover, Piper species possess therapeutic and preventive potential against several chronic disorders. Among the functional properties of Piper plants/extracts/active components the antiproliferative, anti-inflammatory, and neuropharmacological activities of the extracts and extract-derived bioactive constituents are thought to be key effects for the protection against chronic conditions, based on preclinical in vitro and in vivo studies, besides clinical studies. Habitats and cultivation of Piper species are also covered in this review. In this current work, available literature of chemical constituents of the essential oils Piper plants, their use in traditional medicine, their applications as a food preservative, their antiparasitic activities and other important biological activities are reviewed.
The present paper explores the dependence of local population of Seijosa circle of Pakke-Kessang district, Arunachal Pradesh on the phytoresources available here. Local population of Sejiosa circle has their unique system of resource management. They are directly dependent on their surroundings for timber forest products (TFPs) and non-timber forest products (NTFPs). This area is rich in vascular plant diversity which direcly or indirectly supports wild life also. In present study total 365 plant species belonging to 272 genera and 95 families have been recorded, which are utilized by natives of this area in the form of beverage, broom making, canes, condiment / spices, craft, dye, edible (fruit), fiber, fodder, fuel, medicinal, oil, ornamental, paper pulp, resin, tannin, timber, vegetable, etc.
Acetazolamide (Diamox) was one of the first synthetic nonmercurial diuretics. The mode of action was found to be inhibition of carbonic anhydrase. Carbonic anhydrase is a zinc-containing enzyme that catalyzes the reversible hydration (or hydroxylation) of CO2 to form H2CO3 which dissociates nonenzymatically into HCO3− and H+. The enzyme is located within the cytoplasm and at the apical and basolateral membranes of proximal tubules as well as on the apical (lumenal) surface of distal tubules and in the thick ascending limb of the loop of Henle. Its primary function is to enhance H+ secretion into the urine. At least three isoenzymes, designated as I, II, and II or A, B, and C, are known to exist.
Arunachal Pradesh, falling under Easter Himalayan region one of the global mega-diversity centers, is a botanical paradise and the home of 110 ethnic communities (tribes) most of which are still forest dwellers and so diverse that they can not understand each others language. Hindi is gradually becoming popular among the persons, who are near townships. The paper throws light on different uses of 108 species of plants in day-to-day life of the people belonging to Adi ethnic community of Arunachal Pradesh.
Piper attenuatum is a potent medicinal plant in the Indian systems of medicine. Piper attenuatum having Piperine, Piperlonguminine and other active constituents which are used as muscle relaxant, central nervous system depressant, in headache and as insecticide agent against Musca domestica. Piperine reduced the total body temperature and display analgesic, and anti-inflammatory activities. The aim of present study is to determine the Anti-Hyperlipidemic activity of Ethanolic seed extract of plant Piper attenuatum (Linn.) B. Ham. (Fam. Piperaceae). Piperine was the first amide to be isolated from Piper species. Ethanolic extracts of Piper attenuatum with a dose of 200 mg/kg exhibited significant Anti-Hyperlipidemic activity in Triton X-100 Induced Hyperlipidemia in rats (P<.05). It was found that Piperine & Piperlonguminine the active constituent of the plant was responsible for the Anti-Hyperlipidemic activity because this constituent have the ability to reduce the Total Cholesterol & Total Triglyceride level in rats. Fenofibrate was used as standard drug (65 mg/kg). The total time period of this study was one week.
Objective: The aim of the present work was to perform complete pharmacognostic evaluation of Piper attenuatum. Antibacterial activity was performed to explore the possible inhibitory property of dry fruit extract of Piper attenuatum against different microorganisms. Methods: Extensive pharmacognostic evaluation of dry fruits of P. attenuatum was performed which includes morphology, microscopy, phytochemical screening, physicochemical parameters (loss on drying, extractive values, ash values and pH) and high performance thin layer chromatography (HPTLC) profile. We also performed antibacterial activity for methanol, ethanol and ethyl acetate extracts of dry fruit powder of P. attenuatum by agar diffusion method. Results: The morphology of fruits of P. attenuatum was found similar to that of Piper nigrum with less folding on the fruits of P. attenuatum. The fruits have bland taste unlike the dry fruits of P. nigrum which are pungent. Powder microscopy showed the presence of different cellular structures. Phytochemical screening tests revealed the presence of different chemical constituents like alkaloids, tannins, carbohydrates, steroids and volatile oil. The HPTLC profile of crude sample showed many spots indicating its chemical diversity. Conclusion: All these tests gave the valuable data which may be helpful for its qualitative identification and further study. Antibacterial activity did not show prominent inhibitory property except at higher concentrations in methanol extract.
Background: Crotepoxide is a potent molecule for the development of anticancer pharmacodynamics therefore; estimation process for such novel compound is highly desired for future research work in the field of natural products. Introduction: Piper attenuatum is an important species used as a drug in Ayurvedic system of medicine. Pipoxide chlorohydrin, galbelgin, 8-hentriacontanol, several aristolactams, and 4,5-dioxaporphines are the main chemical constituents reported from this plant. Method: Methods based on HPTLC and HPLC with PDA detector for rapid quantitative estimation of crotepoxide in the methanolic extract of Piper attenuatum fruits has been described. Result: The linearity for crotepoxide was found to be in the concentration range of 0.2 to 1.2 μg/spot with coefficient of determination 0.9988 for HPTLC and 1 to 32 μg/mL with coefficient of determination 0.9990 for HPLC with respect to peak area. Limit of detection (LOD) and limit of quantification (LOQ) were found to be 60 ng/spot and 198 ng/spot, for HPTLC and 15 ng/mL and 50 ng/mL for HPLC, respectively. Repeatability studies have shown 0.14% RSD and SE 2.06 for HPTLC and 0.65% RSD for HPLC. Recovery values of 96.06 to 103.02% for HPTLC and 98.05 to 100.09% for HPLC indicate excellent accuracy of the methods. Conclusion: HPTLC and HPLC analyses of the fruit extract had shown percent content of crotepoxide 2.5 and 2.43, respectively, which appears to be the highest from any plant source. The developed methods are accurate, precise, cost-effective, and can be successfully applied for the estimation of crotepoxide.
The aim was to study and identify free radicals scavenging and antihyperglycemic principles in fruit of Piper attenuatum.
Bioassay guided identification of extracts possessing potent free radical scavenging activity, and isolation of compounds was done. Chloroform extract of P. attenuatum possessing potent radical scavenging activity was also evaluated for antihyperglycemic activity following oral glucose tolerance test in rats.
Nine neolignans namely, denudatin B (1), iso-4', 5'-dimethoxy-3, 4-methylenedioxy-2'-oxo-Δ(3',5',8')-8.1'-lignan (2), lancifolin D (3), denudatin A (4), wallichinin (5), piperenone (6), lancifolin C (7), 2-oxo-piperol B (8), piperkadsin A (9) and a crotepoxide (10) was identified in Chloroform extract of P. attenuatum. Neolignans (1-9) displayed potent 2, 2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) radical and piperkadsin A (9) also displayed 1, 1-diphenyl-2-picrylhydrazyl radical scavenging activity. Analysis of structure-activity relationship revealed that presence of furan ring and methoxy groups is an important criterion to influence 2, 2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) radical scavenging potentials. Chloroform extract of P. attenuatum fruit could not display antihyperglycemic activity following oral glucose tolerance test in rats.
Neolignans present in P. attenuatum fruits are potent free radical scavengers and this is the first report identifying these compounds and activities in this fruit.
THE FOLLOWING study on the treatment of glaucoma with the carbonic anhydrase inhibitor acetazoleamide ( 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide; Diamox) was initiated in October, 1953, and covers a four-month period of observation.
Inhibition of carbonic anhydrase by acetazoleamide is a new and useful means of lowering the intraocular pressure. Acetazoleamide, a heterocyclic sulfonamide, was developed by Roblin and associates, in 1950,* as a diuretic agent whose action was based on inhibition of carbonic anhydrase in the renal tubular epithelium. Carbonic anhydrase catalyzes the hydration of carbon dioxide to form carbonic acid: H2O+CO2⇄ H2CO3. The carbonic acid dissociates to form H+ and HCO3-. Thus, the level of hydrogen ions and bicarbonate ions is affected by this enzyme. In the kidney there ensues a hydrogen-sodium exchange between the tubular epithelium and the glomerular filtrate, resulting in the normal conservation of base and the formation of an acid urine.
New cyclohexyl epoxide and crotepoxide were isolated from the fruits of Piper attenuatum. The structure of the new metabolite was characterized as (2-benzoyl-1, 6-epoxy-3, 4, 5,-trihydroxy cyclohexyl) methanol benzoate along with crotepoxide using spectroscopic techniques.
The present communication deals with the macroscopical, microscopical & preliminary phytochemical screening on the aerial parts of Suaeda maritima Linn. (Chenopodiaceae). Suaeda maritima Linn. is widely used in traditional medicine in many parts of India for the treatment of various diseases & ailments viz. hepatoprotective, antioxidant, antifungal etc. No reports are available on the pharmacognostic nature of different parts of plant, hence, the present study was undertaken to investigate the same. All the parameters were studied according to the WHO & Pharmacopoeial guidelines. The qualitative chemical tests on the successive solvent extract revealed the presence of steroids, triterpenoids, proteins & carbohydrates.
A stereoselective synthesis procedure for lignans of the all-trans αα'-diaryl-ββ'-dimethyltetrahydrofurans is described. The lignans, galbelgin (4) and grandisin (37) were synthesized by routine reduction of the tetrahydrofuran dicarboxylic esters (24 and 34), obtained by mild acid treatment of the readily available diaryl dilactones (23 and 33).
Thirty eight compounds of different types have been isolated from twelve Piper species. The ether extract of the leaves of P. aduncum yielded eleven compounds, out of which 2,6-dimethoxy-4-(2-propenyl)phenol was isolated for the first time from the genus Piper and 2-acetoxy-1,3-dimethoxy-5-(2-propenyl)benzene is a new compound. The petrol extract of the stems and leaves of P. attenuatum furnished a novel long chain alcohol, 14-benzo[1, 3]dioxol-5-yl-tetradecan-2-ol. From P. betle, β-sitosteryl palmitate was isolated for the first time from the genus Piper. A novel amide, 3-(3,4-dimethoxyphenyl)propanoyl pyrrole has been obtained from P. brachystachyum. Nerolidol was isolated for the first time from P. falconeri. From the methanol extract of the stems and leaves of P. khasiana, piperlonguminine, piperine, apigenin dimethyl ether and β-sitosterol were obtained. Retrofractamide A was obtained for the first time from P. longum; the structure of (+)-asarinin, isolated from P. longum, was confirmed by X-ray crystallographic studies. Retrofractamide A, apigenin dimethyl ether, tetratriacontanol and tectochrysin were isolated from P. manii. P. pedicellosum furnished β-sitosterol, pellitorine, piperlonguminine, cepharadione A and furacridone, the last compound being isolated for the first time from the genus Piper.
Pipoxide chlorohydrin, (−)-galbelgin and a new aliphatic alcohol, 8-hentriacontanol have been isolated from the leaves of Piper attenuatum.
Ethno-medico-botanical investigations of seven primitive tribals, Cholanaikken, Pathinaikken, Paniyan, Kuruman, Irular, Adiyan and Kurichan, living in the densely forested high-lands of western ghats in Kerala were carried out. One of the tribes, Cholanaikken, is the most primitive tribe known in the Indian subcontinent. Ethnically they appear close to the Australian aboriginals. All other tribes of Kerala have mixed features of Veddoids, Negroids, Australian aboriginals and Dravidian races suggesting the mixing of these races at various periods of Kerala's historical past. All the tribals investigated practice their own traditional system of medicine. The medical treatment of diseases of most of these tribals involves mysticism, magical incantations, sacrificial practices and divining. They also utilize a wide variety of herbs in treating the physical symptoms. These medicinal herbs were collected, identified and some of the interesting plants for which new medicinal uses were claimed by the tribals are described here.