scholarly journals EVALUATION OF XANTHINE OXIDASE INHIBITORY ACTIVITY BY FLAVONOIDS FROM PONGAMIA PINNATA LINN

2017 ◽  
Vol 10 (3) ◽  
pp. 360 ◽  
Author(s):  
Vanishree Bambrana ◽  
Dayanand Cd ◽  
Sheela Sr
Keyword(s):  
Xanthine Oxidase ◽  
Plant Extracts ◽  
Inhibitory Activity ◽  
Mangifera Indica ◽  
Zingiber Officinale ◽  
Pongamia Pinnata ◽  
Morinda Citrifolia ◽  
Dried Fruit ◽  
Fruit Powder ◽  
Inhibitory Potential

ABSTRACTObjective: Flavonoids from the crude seeds extract of Pongamia pinnata L., dried fruit powder of Morinda citrifolia L., bark of Mangifera indica L., andrhizome of Zingiber officinale Rosc. were screened for xanthine oxidase (XO) inhibition at different concentration. The inhibitory potential of quercetinand allopurinol were used for the determination of 50% inhibitory concentration (IC50) and Ki values.Methods: Isolation of flavonoids from the plant extracts was processed by column chromatography and tested for XO inhibitory activity in the rangeof 6-800 μg/ml.Results: The results demonstrated that optimized flavonoids extract of P. pinnata L. exhibited promising XO inhibition. P. pinnata L., M. indica L., andZ. officinale Rosc. had IC50 in the concentration of 8.74 mM, 1.09 mM, 5.4 mM and Ki 0.35 mM, 1.73 mM, 2.7 mM, respectively.Conclusion: The study showed that plant species under investigation exhibited XO inhibition by optimized flavonoid extract. P. pinnata L. indicatedpromising XO inhibition compared to other plant extracts. Flavonoids can be used as a potent inhibitor of XO an alternative to allopurinol.Keywords: Xanthine oxidase, Quercetin, Allopurinol, Pongamia pinnata, Oxidative stress.

scholarly journals Shortlisting Phytochemicals Exhibiting Inhibitory Activity against Major Proteins of SARS-CoV-2 through Virtual Screening

2020 ◽  
Author(s):  
Saranya Nallusamy ◽  
Jayakanthan Mannu ◽  
Caroline Ravikumar ◽  
Kandavelmani Angamuthu ◽  
Bharathi Nathan ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Inhibitory Activity ◽  
Mangifera Indica ◽  
Herbal Medicines ◽  
Genomic Analysis ◽  
Zingiber Officinale ◽  
Major Protein ◽  
Synthetic Drugs ◽  
Cissus Quadrangularis ◽  
Control And Management

Abstract Severe Acute Respiratory Syndrome Corona Virus 2 (SARS-CoV-2) declared as a pandemic by WHO that has affected more than 40 lakh peoples and caused death of more than 2 lakh individuals across the globe. Limited availability of genomic information of SARS-CoV-2 and non-availability of vaccines and effective drugs are major problems responsible for the ineffective control and management of this pandemic. Several attempts have been made to explore repurposing existing drugs known for their anti-viral activities, and test the traditional herbal medicines known for their health benefiting and immune boosting activity against SARS-CoV-2.In this study, efforts were made to examine the potential of 721 phytochemicals of 37 plant species in inhibiting major protein targets namely, spike glycoprotein, main protease (MPro), NSP3, NSP9, NSP15, NSP10-NSP16 and RNA dependent RNA polymerase of SARS-CoV-2 through virtual screening approach. Results of our experiments revealed that SARS-CoV-2 MPro shared significant dissimilarities against SARS-CoVMPro and MERS-CoVMPro indicating the need for discovering novel drugs. This study has identified the phytochemical cyanin (Zingiber officinale) exhibiting broad spectrum inhibitory activity against main proteases of all the three Coronaviruses. Amentoflavone, agathisflavone, catechin-7-o-gallate and chlorogeninwere shown to exhibit multi target inhibitory activity. This study has identified Mangifera indica, Anacardium occidentale, Vitex negundo, Solanum nigrum, Pedalium murex, Terminalia chebula, Azadirachta indica, Cissus quadrangularis, Clerodendrum serratum and Ocimum basilicum as potential sources of phytochemicals combating nCOVID-19. More interestingly, this study has generated evidences for the anti-viral properties of the traditional herbal formulation “Kabasura kudineer” recommended by AYUSH, a unit of Government of India. Testing of short listed phytochemicals through clinical trials will help in developing effective formulation for management of this pandemic disease. Genomic analysis of identified herbal plants will help in unravelling molecular complexity of therapeutic and anti-viral properties and will pave way for designing synthetic drugs.

scholarly journals Exploring Phytochemicals of Traditional Medicinal Plants Exhibiting Inhibitory Activity Against Main Protease, Spike Glycoprotein, RNA-dependent RNA Polymerase and Non-Structural Proteins of SARS-CoV-2 Through Virtual Screening

2021 ◽  
Vol 12 ◽  
Author(s):  
Saranya Nallusamy ◽  
Jayakanthan Mannu ◽  
Caroline Ravikumar ◽  
Kandavelmani Angamuthu ◽  
Bharathi Nathan ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Inhibitory Activity ◽  
Mangifera Indica ◽  
Herbal Medicines ◽  
Genomic Analysis ◽  
Zingiber Officinale ◽  
Binding Energies ◽  
New Drugs ◽  
Cissus Quadrangularis ◽  
Scientific Attention

Severe Acute Respiratory Syndrome Corona Virus 2 (SARS-CoV-2) being a causative agent for global pandemic disease nCOVID’19, has acquired much scientific attention for the development of effective vaccines and drugs. Several attempts have been made to explore repurposing existing drugs known for their anti-viral activities, and test the traditional herbal medicines known for their health benefiting and immune-boosting activity against SARS-CoV-2. In this study, efforts were made to examine the potential of 605 phytochemicals from 37 plant species (of which 14 plants were endemic to India) and 139 antiviral molecules (Pubchem and Drug bank) in inhibiting SARS-CoV-2 multiple protein targets through a virtual screening approach. Results of our experiments revealed that SARS-CoV-2 MPro shared significant disimilarities against SARS-CoV MPro and MERS-CoV MPro indicating the need for discovering novel drugs. This study has screened the phytochemical cyanin (Zingiber officinale) which may exhibit broad-spectrum inhibitory activity against main proteases of SARS-CoV-2, SARS-CoV and MERS-CoV with binding energies of (−) 8.3 kcal/mol (−) 8.2 kcal/mol and (−) 7.7 kcal/mol respectively. Amentoflavone, agathisflavone, catechin-7-o-gallate and chlorogenin were shown to exhibit multi-target inhibitory activity. Further, Mangifera indica, Anacardium occidentale, Vitex negundo, Solanum nigrum, Pedalium murex, Terminalia chebula, Azadirachta indica, Cissus quadrangularis, Clerodendrum serratum and Ocimum basilicumaree reported as potential sources of phytochemicals for combating nCOVID’19. More interestingly, this study has highlighted the anti-viral properties of the traditional herbal formulation “Kabasura kudineer” recommended by AYUSH, a unit of Government of India. Short listed phytochemicals could be used as leads for future drug design and development. Genomic analysis of identified herbal plants will help in unraveling molecular complexity of therapeutic and anti-viral properties which proffer lot of chance in the pharmaceutical field for researchers to scout new drugs in drug discovery.

In SilicoDesign and Synthesis of Targeted Curcumin Derivatives as Xanthine Oxidase Inhibitors

2019 ◽  
Vol 20 (5) ◽  
pp. 593-603
Author(s):  
Neelam Malik ◽  
Priyanka Dhiman ◽  
Anurag Khatkar
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Pyrimidine Ring ◽  
Inhibitory Potency ◽  
Curcumin Derivatives ◽  
Xanthine Oxidase Inhibitors ◽  
Excess Production ◽  
Ic50 Values ◽  
Inhibitory Potential ◽  
Potent Inhibitory Activity

Background: Curcumin is a well-known pharmacophore and some of its derivatives are shown to target xanthine oxidase (XO) to alleviate disorders caused by the excess production of uric acid. </p><p> Objective: Curcumin based derivatives were designed, synthesized and evaluated for their antioxidant and xanthine oxidase inhibitory potential. </p><p> Method: In this report, we designed and synthesized two series of curcumin derivatives modified by inserting pyrazole and pyrimidine ring to central keto group. The synthesized compounds were evaluated for their antioxidant and xanthine oxidase inhibitory potential. </p><p> Results: Results showed that pyrazole analogues of curcumin produced excellent XO inhibitory potency with the IC50 values varying from 06.255 &#181;M to 10.503 &#181;M. Among pyrimidine derivatives compound CU3a1 having ortho nitro substitution exhibited more potent xanthine oxidase inhibitory activity than any other curcumin derivative of this series. </p><p> Conclusion: Curcumin derivatives CU5b1, CU5b2, CU5b3, and CU3a1 showed a potent inhibitory activity against xanthine oxidase along with good antioxidant potential.

scholarly journals In vitro and in vivo inhibition of xanthine oxidase by the flowers of Chrysanthemum morifolium Ramat.

2020 ◽  
Author(s):  
Teng Lit Ng ◽  
Khye Er Loh ◽  
Sheri-Ann Shu Wei Tan ◽  
Hui Yin Tan ◽  
Sze Ping Wee
Keyword(s):  
Gene Expression ◽  
Uric Acid ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Competitive Inhibition ◽  
Chrysanthemum Morifolium ◽  
Inhibitory Potential ◽  
Tof Ms

Abstract Background: Xanthine oxidase (XO) plays an important role in human’s purine degradation. Excessive uric acid formation results in hyperuricemia and gout. The study aimed to determine the XO inhibitory potential of Chrysanthemum morifolium Ramat. dried flower and its effect on XO gene expression in animal models.Methods: In vitro XO inhibitory assay was employed to investigate the XO inhibitory potential of C. morifolium flowers. The bioactive sub-fraction was investigated further to give additional insight on its uric acid lowering potential via animal study and XO gene expression analysis. HPLC-Q-TOF-MS/MS was utilized to identify the putative compounds in the sub-fraction.Results: Among the fractions, EtOAc fraction exhibited the highest in vitro XO inhibitory potency (51.77 ± 0.98%; IC50 = 10.64 ± 0.51 µg/mL) and it was further fractionated into 15 sub-fractions through open column chromatography. EtOAc F7, F8, F9, F10, and F11 possessed >75% XO inhibition. F9 and F10 exhibited high in vitro XO inhibitory activity, cellular pro-proliferative effect and intracellular antioxidant activity among the sub-fractions tested. These two sub-fractions were also non-cytotoxic at the concentration range of 0.1 – 10 µg/mL. F10 was shown to be very effective in both serum and urine uric acid lowering properties in rats model upon oral consumption. It was subjected to further fractionation and a total of 11 sub-fractions were obtained. F10-4, F10-8, F10-9, and F10-10 possessed >90% XO inhibition. These sub-fractions were subjected to HPLC-Q-TOF-MS/MS analysis. A total of nine known compounds have been identified and 26 unknown compounds were detected. Conclusions: The possible mechanisms contributed to the anti-hyperuricemic effect of F10 were suggested to be non-competitive inhibition of XO enzyme, XO gene expression down regulation, and enhancement of uric acid excretion. Structure elucidation of the unknown compounds and the evaluation of the XO inhibitory activity of a single or a mixture of these compounds are recommended to identify possible synergism between them.

Screening of Hungarian mushrooms for xanthine-oxidase inhibitory activity

Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
A Ványolós ◽  
O Orbán-Gyapai ◽  
T Támadi ◽  
J Hohmann
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity

Polyphenols from Cyclopia genistoides and their xanthine oxidase inhibitory activity

Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
O Roza ◽  
A Martins ◽  
J Hohmann ◽  
WC Lai ◽  
FR Chang ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity

ANTIOESTROGENIC ACTIVITY IN FAHLI CLOVER HAY AND OAT HAY

1965 ◽  
Vol 49 (1) ◽  
pp. 90-96 ◽  
Author(s):  
J. H. Adler
Keyword(s):  
Plant Extracts ◽  
Avena Sativa ◽  
Inhibitory Activity ◽  
Weight Increase ◽  
Trifolium Alexandrinum ◽  
Uterine Weight ◽  
Extraction Procedures ◽  
Fodder Plants

ABSTRACT The presence of oestrogen inhibitory activity in oat hay (Avena sativa) and Fahli clover hay (Trifolium alexandrinum var. Fahli) has been established. The antioestrogenic effect was demonstrated by the inhibition of uterine weight increase in rats (Astwood test) in response to oestradiol injected together with the above mentioned plant extracts. The extraction procedures are described in detail and the possible biological implications of antioestrogenic and oestrogenic activity in fodder plants is discussed.

Antioxidant, Xanthine Oxidase and Monoamine Oxidase Inhibitory Potential of Coumarins: A Review

2017 ◽  
Vol 21 (4) ◽  
pp. 294-304 ◽  
Author(s):  
Priyanka Dhiman ◽  
Neelam Malik ◽  
Anurag Khatkar ◽  
Mahesh Kulharia
Keyword(s):  
Monoamine Oxidase ◽  
Xanthine Oxidase ◽  
Inhibitory Potential

2,4-Dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic Acid Derivatives: In Vitro Antidiabetic Activity, Molecular Modeling and In silico ADMET Screening

2019 ◽  
Vol 15 (2) ◽  
pp. 186-195 ◽  
Author(s):  
Samridhi Thakral ◽  
Vikramjeet Singh
Keyword(s):  
Molecular Docking ◽  
Benzoic Acid ◽  
Inhibitory Activity ◽  
In Silico ◽  
Computational Study ◽  
Antidiabetic Activity ◽  
Standard Drug ◽  
Benzoic Acid Derivatives ◽  
In Silico Admet ◽  
Inhibitory Potential

Background: Postprandial hyperglycemia can be reduced by inhibiting major carbohydrate hydrolyzing enzymes, such as α-glucosidase and α-amylase which is an effective approach in both preventing and treating diabetes. Objective: The aim of this study was to synthesize a series of 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl] benzoic acid derivatives and evaluate α-glucosidase and α-amylase inhibitory activity along with molecular docking and in silico ADMET property analysis. Method: Chlorosulfonation of 2,4-dichloro benzoic acid followed by reaction with corresponding anilines/amines yielded 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic acid derivatives. For evaluating their antidiabetic potential α-glucosidase and α-amylase inhibitory assays were carried out. In silico molecular docking studies of these compounds were performed with respect to these enzymes and a computational study was also carried out to predict the drug-likeness and ADMET properties of the title compounds. Results: Compound 3c (2,4-dichloro-5-[(2-nitrophenyl)sulfamoyl]benzoic acid) was found to be highly active having 3 fold inhibitory potential against α-amylase and 5 times inhibitory activity against α-glucosidase in comparison to standard drug acarbose. Conclusion: Most of the synthesized compounds were highly potent or equipotent to standard drug acarbose for inhibitory potential against α-glucosidase and α-amylase enzyme and hence this may indicate their antidiabetic activity. The docking study revealed that these compounds interact with active site of enzyme through hydrogen bonding and different pi interactions.

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