MyMedR

Displaying all 9 publications

Abstract:

Sort:

Anti-mycobacterial Constituents from Medicinal Plants; A Review

Sarkar N, Dey YN, Kumar D, Rajagopal M

Mini Rev Med Chem, 2021;21(19):3037-3051.
PMID: 34036911 DOI: 10.2174/1389557521666210525120325

Effective treatment of tuberculosis has been hampered by the emergence of drug-resistant strains of Mycobacterium therapeutic facilities tuberculosis. With the global resurgence of tuberculosis with the development of multidrug-resistant cases, there is a call for the development of new drugs to combat these diseases. Throughout history, natural products have afforded a rich source of compounds that have found many applications in the fields of medicine, pharmacy and biology, and continued to play a significant role in the drug discovery and development process. This review article depicts the various potential plant extracts as well as plant derived phytoconstituents against the H37rv, the most persistent strains of Mycobacterium tuberculosis and its multidrug strains.
Beneficial effect of Amorphophallus paeoniifolius tuber on experimental ulcerative colitis in rats

Dey YN, Sharma G, Wanjari MM, Kumar D, Lomash V, Jadhav AD

Pharm Biol, 2017 Dec;55(1):53-62.
PMID: 27600166

CONTEXT: The tuber of Amorphophallus paeoniifolius (Dennst.) Nicolson (Araceae), commonly called Suran or Jimmikand, has high medicinal value and is used ethnomedicinally for the treatment of different gastrointestinal and inflammatory disorders.
OBJECTIVE: The present study evaluated the effects of extracts of Amorphophallus paeoniifolius tubers on acetic acid-induced ulcerative colitis (UC) in rats.
MATERIALS AND METHODS: Wistar rats were orally administered methanol extract (APME) or aqueous extract (APAE) (250 and 500 mg/kg) or standard drug, prednisolone (PRDS) (4 mg/kg) for 7 days. On 6th day of treatment, UC was induced by transrectal instillation of 4% acetic acid (AA) and after 48 h colitis was assessed by measuring colitis parameters, biochemical estimations and histology of colon.
RESULTS: APME or APAE pretreatment significantly (p
Curative effect of Amorphophallus paeoniifolius tuber on experimental hemorrhoids in rats

Dey YN, Wanjari MM, Kumar D, Lomash V, Jadhav AD

J Ethnopharmacol, 2016 Nov 04;192:183-191.
PMID: 27426509 DOI: 10.1016/j.jep.2016.07.042

ETHNOPHARMACOLOGICAL RELEVANCE: Amorphophallus paeoniifolius (Dennst.) Nicolson (Family- Araceae) is a crop of south East Asian origin. In India, its tuber is widely used in ethnomedicinal practices by different tribes for the treatment of piles (hemorrhoids).
AIM: The present study evaluated the effect of methanolic and aqueous extract of Amorphophallus paeoniifolius tuber on croton oil induced hemorrhoids in rats.
MATERIALS AND METHODS: The methanolic extract was standardized with the major phenolic compound, betulinic acid, by HPLC. The hemorrhoids were induced by applying 6% croton oil preparation in the ano-rectal region. Rats were orally administered methanolic and aqueous extract at doses of 250 and 500mg/kg, each for 7 days. Pilex (200mg/kg) was used as reference anti-hemorrhoidal drug. Hemorrhoids were assessed on eighth day by measuring hemorrhoidal and biochemical parameters along with histology of ano-rectal tissue.
RESULTS: Croton oil application caused induction of hemorrhoids as indicated by significant (p<0.001) increase in plasma exudation of Evans blue in ano-rectal tissue, macroscopic severity score and ano-rectal coefficient as compared to normal rats. It significantly (p<0.001) elevated lactate dehydrogenase and cytokines (TNF-α and IL-6) levels in serum and increased myeloperoxidase activity and lipid peroxidation in ano-rectal tissue along with marked histological damage as compared to normal rats. Treatment with tuber extracts and pilex significantly (p<0.05-p<0.001) ameliorated Evans blue exudation, hemorrhoidal parameters and other biochemical parameters with attenuation of tissue damage compared to hemorrhoid control rats. The results indicate that tuber extracts exhibited curative action on hemorrhoids. The aqueous extract showed more pronounced effect than methanolic extract. The effects may be attributed to anti-inflammatory and antioxidant properties.
CONCLUSION: Results indicate that tuber of Amorphophallus paeoniifolius exhibited curative action on hemorrhoids through anti-inflammatory and antioxidant properties. The study validates the ethnomedicinal use of tuber in hemorrhoids and implicates its therapeutic potential as an anti-hemorrhoidal agent.
Fulltext Inhibitory activity of Enhydra fluctuans Lour. on calcium oxalate crystallisation through in silico and in vitro studies

Chattaraj B, Nandi A, Das A, Sharma A, Dey YN, Kumar D, et al.

Front Pharmacol, 2022;13:982419.
PMID: 36744215 DOI: 10.3389/fphar.2022.982419

The decoction of the whole plant of Enhydra fluctuans is used ethno medicinally by various tribes for the treatment of kidney stones and urinary problems. However, no scientific studies were carried out to delineate its influence on urinary stone formation and crystallisation. Hence, the present study is proposed to investigate the effect of the aqueous extract of Enhydra fluctuans extract on in vitro crystallisation of calcium oxalate. The present study also evaluated. in silico studies of the metabolites with the target proteins present in the renal calcium oxalate stone matrix. The plant material was subjected to decoction to obtain an aqueous extract. The effect of the extract on calcium oxalate crystallization was evaluated by in vitro nucleation and aggregation assays. Further, the metabolites present in E. fluctuans were mined from the existing literature and their number was found to be 35. The selected 35 metabolites of E. fluctuans were subjected to molecular docking with the 5 proteins which are known to be responsible for calcium oxalate crystal growth. Results of in vitro studies indicated that the extract (50, 100, and 200 μg/mL) and standard drug cystone (1,000 μg/mL) exhibited an inhibitory role in the nucleation process where the percentage inhibitions were 52.69, 43.47, 21.98, and 31.67 μg/mL respectively. The results of molecular docking studies revealed that 2 out of 35 metabolites i.e. Baicalein-7-O-diglucoside and 4',5,6,7-Tetrahydroxy-8-methoxy isoflavone-7-O-beta-D- galactopyranosyl-(1→3)-O-beta-D-xylopyranosyl-(1→4)- O-alpha-L-rhamnopyranoside showed modulatory effects on the four renal stone matrix-associated protein (Human CTP: Phosphoethanolamine Cytidylyltransferase (Protein Data Bank ID: 3ELB), UDP glucose: glycoprotein glucosyltransferase 2 (Gene: UGGT2) (AlphaFold) and RIMS-binding protein 3A (Gene: RIMBP3) (AlphaFold), and Ras GTPase activating-like protein (PDB: 3FAY) based on their docking scores which indicates that they may inhibit the crystallization process. Findings from this study show that Enhydra fluctuans may be effective in the prevention of the crystallization of calcium oxalate. However, further, in vivo studies as well as molecular studies are needed to be conducted to confirm and strengthen its anti-urolithiatic activity and to elucidate the possible mechanism of action involved therein.
The Potential of Mur Enzymes as Targets for Antimicrobial Drug Discovery

Kumar D, Sarkar N, Roy KK, Bisht D, Kumar D, Mandal B, et al.

Curr Drug Targets, 2023;24(8):627-647.
PMID: 37291783 DOI: 10.2174/1389450124666230608150759

The extensive development in the strains of resistant bacteria is a potential hazard to public health worldwide. This necessitates the development of newer agents with the antibacterial property having new mechanisms of action. Mur enzymes catalyze the steps related to the biosynthesis of peptidoglycan, which constitutes a major part of the cell wall in bacteria. Peptidoglycan increases the stiffness of the cell wall, helping it to survive in unfavorable conditions. Therefore, the inhibition of Mur enzymes may lead to novel antibacterial agents that may help in controlling or overcoming bacterial resistance. Mur enzymes are classified into MurA, MurB, MurC, MurD, MurE, and MurF. Until-date, multiple inhibitors are reported for each class of the Mur enzymes. In this review, we have summarized the development of Mur enzyme inhibitors as antibacterial agents in the last few decades.
Fulltext Gastrokinetic activity of Amorphophallus paeoniifolius tuber in rats

Dey YN, Mahor S, Kumar D, Wanjari M, Gaidhani S, Jadhav A

J Intercult Ethnopharmacol, 2016;5(1):36-42.
PMID: 27069720 DOI: 10.5455/jice.20151211063819

AIM: The tuber of Amorphophallus paeoniifolius (Family-Araceae), commonly called suran or jimikand, has medicinal and food value. It is used in ethnomedicinal practices for correction of gastrointestinal disturbances such as constipation and hemorrhoids. The present study evaluated the effect of A. paeoniifolius tuber on gastrointestinal motor functions.
MATERIALS AND METHODS: The tuber was collected in December 2011, and its methanolic extract was standardized with the major phenolic compound, betulinic acid, by high-performance liquid chromatography. Rats were orally administered methanolic (APME) or aqueous (APAE) extract (250 and 500 mg/kg, each) of tuber for 7 days. Metoclopramide (MET) (3 mg/kg, orally) was used a reference prokinetic drug. The gastrointestinal parameters viz. number of feces, wet and dry weight and moisture content of feces, gastric emptying, and intestinal transit were evaluated. The isolated tissue preparations were used to check the effect of the extracts on fundus and intestinal contractility. The glucomannan and total phenolic and flavonoid contents were determined spectrophotometrically.
RESULTS: The pre-treatment of extracts significantly increased the number of feces, wet and dry weight of feces, moisture content, gastric emptying, and intestinal transit. Results were comparable to MET. Further, APME and APAE showed a contraction of fundus and ileum in isolated preparations. APME and APAE were also found to have fair amount of glucomannan, total phenolics, and flavonoids. The results indicate the gastrokinetic potential of the tuber extracts. This may be attributed to the presence of glucomannan and betulinic acid present in the extracts.
CONCLUSION: In conclusion, the tuber of A. paeoniifolius exhibits gastrokinetic activity and substantiates its traditional use in gastrointestinal motor disturbances.
Fulltext Beneficial effect of standardized extracts of Amorphophallus paeoniifolius tuber and its active constituents on experimental constipation in rats

Dey YN, Wanjari MM, Srivastava B, Kumar D, Sharma D, Sharma J, et al.

Heliyon, 2020 May;6(5):e04023.
PMID: 32509986 DOI: 10.1016/j.heliyon.2020.e04023

The tubers of Amorphophallus paeoniifolius (Elephant foot yam), principally consumed as crop food and vegetables, are used in ethno-medicinal practices in mitigation of constipation and piles. Hence, present study evaluated the effect of tubers of A. paeoniifolius and its active constituents glucomannan and betulinic acid on experimentally-induced constipation. The tuber and its extracts were standardized as per Ayurvedic Pharmacopoeia of India and physicochemical constants were found within the pharmacopoeial limit. HPTLC fingerprint profile of extracts has been developed using suitable mobile phase. Methanolic extract was subjected to column chromatography. The isolated phytoconstituents were characterized by FT-IR, NMR and MS and identified as betulinic acid and β-sitosterol. Functional constipation was induced in rats by oral administration of loperamide (3 mg/kg) for first 3 consecutive days. The rats were orally treated with methanolic and aqueous tuber extracts in the doses of 125, 250 and 500 mg/kg, glucomannan (300 mg/kg) and betulinic acid (1.5 mg/kg) for 7 days. The parameters viz. number of stools, wet weight of stools and moisture content of stools and intestinal transit were studied. Treatment with tuber extracts, glucomannan and betulinic acid showed significant (p < 0.05) increase in fecal parameters and intestinal transit in constipated rats. The effects were comparable to standard laxative drug, sodium picosulfate (5 mg/kg, orally). The results indicated that tuber extracts and its active constituents showed laxative effect and relieved constipation. It is concluded that tuber of A. paeoniifolius exhibited beneficial effect in functional constipation possibly through its laxative action. The study validates its ethno-medicinal use in correction of constipation. The principal constituents, betulinic acid and glucomannan in tuber extracts might have played important role in relieving the constipation.
Fulltext Potential of histone deacetylase inhibitors in the control and regulation of prostate, breast and ovarian cancer

Pramanik SD, Kumar Halder A, Mukherjee U, Kumar D, Dey YN, R M

Front Chem, 2022;10:948217.
PMID: 36034650 DOI: 10.3389/fchem.2022.948217

Histone deacetylases (HDACs) are enzymes that play a role in chromatin remodeling and epigenetics. They belong to a specific category of enzymes that eliminate the acetyl part of the histones' -N-acetyl lysine, causing the histones to be wrapped compactly around DNA. Numerous biological processes rely on HDACs, including cell proliferation and differentiation, angiogenesis, metastasis, gene regulation, and transcription. Epigenetic changes, specifically increased expression and activity of HDACs, are commonly detected in cancer. As a result, HDACi could be used to develop anticancer drugs. Although preclinical outcomes with HDACs as monotherapy have been promising clinical trials have had mixed results and limited success. In both preclinical and clinical trials, however, combination therapy with different anticancer medicines has proved to have synergistic effects. Furthermore, these combinations improved efficacy, decreased tumor resistance to therapy, and decreased toxicity. In the present review, the detailed modes of action, classification of HDACs, and their correlation with different cancers like prostate, breast, and ovarian cancer were discussed. Further, the different cell signaling pathways and the structure-activity relationship and pharmaco-toxicological properties of the HDACi, and their synergistic effects with other anticancer drugs observed in recent preclinical and clinical studies used in combination therapy were discussed for prostate, breast, and ovarian cancer treatment.
Fulltext Integration of System Biology Tools to Investigate Huperzine A as an Anti-Alzheimer Agent

Khanal P, Zargari F, Far BF, Kumar D, R M, Mahdi YK, et al.

Front Pharmacol, 2021;12:785964.
PMID: 34966281 DOI: 10.3389/fphar.2021.785964

Aim: The present study aimed to investigate huperzine A as an anti-Alzheimer agent based on the principle that a single compound can regulate multiple proteins and associated pathways, using system biology tools. Methodology: The simplified molecular-input line-entry system of huperzine A was retrieved from the PubChem database, and its targets were predicted using SwissTargetPrediction. These targets were matched with the proteins deposited in DisGeNET for Alzheimer disease and enriched in STRING to identify the probably regulated pathways, cellular components, biological processes, and molecular function. Furthermore, huperzine A was docked against acetylcholinesterase using AutoDock Vina, and simulations were performed with the Gromacs package to take into account the dynamics of the system and its effect on the stability and function of the ligands. Results: A total of 100 targets were predicted to be targeted by huperzine A, of which 42 were regulated at a minimum probability of 0.05. Similarly, 101 Kyoto Encyclopedia of Genes and Genomes pathways were triggered, in which neuroactive ligand-receptor interactions scored the least false discovery rate. Also, huperzine A was predicted to modulate 54 cellular components, 120 molecular functions, and 873 biological processes. Furthermore, huperzine A possessed a binding affinity of -8.7 kcal/mol with AChE and interacted within the active site of AChE via H-bonds and hydrophobic interactions.