EVALUATION OF HEPATOPROTECTIVE ACTIVITY OF THE AERIAL PARTS OF PHYLLANTHUS RETICULATES AGAINST PARACETAMOL INDUCED HEPATIC DAMAGE IN RATS

ABSTRACTObjective: The present study deals with evaluation of hepatoprotective effect against paracetamol induced hepatitis in rats and in-vitro antioxidantactivity of aerial parts of ethanolic extract (70%) of Phyllanthus reticulates.Methods: Alteration in the levels of biochemical markers of hepatic damage like AST, ALT, ALP and total Bilirubin were tested in both treated anduntreated groups.Results: Treatment with ethanolic extract of Phyllanthus reticulates (400 mg/kg) has brought back the altered levels of biochemical markers to thenear normal level which is comparable with the standard drug Silymarin.Conclusion: Further the in-vitro antioxidant activity and total phenolic content showed significant result which in turn encourages further evaluationof this plant in future.Keywords: Phyllanthus, Hepatitis, Biochemical markers, Antioxidant activity, Total phenolic content

SYNTHESIS, CHARACTERIZATION AND ANTIOXIDANT ACTIVITY OF POTASSIUM CIS-DIAQUA-BIS (OXALATO) CHROMATE (III) WITH LEVODOPA AND CARBIDOPA

Objective: These studies focus on the interaction between two clinically active antiparkinsonian drugs L-dopa (L) and carbidopa (C) with the cis-[Cr(C2O4)2(H2O)2]-and evaluation of the synthesized product from a coordination chemistry aspect with respect to the possibility of its antioxidant activity and its therapeutic application in the treatment of Parkinson disease.Methods: The resulting synthesized complexes were characterized by UV-VIS and FTIR spectroscopy. Evaluation of antioxidant activities of this cis-[Cr(C2O4)2(H2O)2]--L-dopa(ML), cis-[Cr(C2O4)2(H2O)2]--carbidopa(MC) and standard butylated hydroxytoluene (BHT) were carried out by using 1,1-diphenyl-1-picrylhydrazyl free radical (DPPH), 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cations and hydrogen peroxide method.Results: The results of spectral analysis of the synthesized products indicate that complexes have a Cr(III) ion coordinated via the carboxylic and amino group. In the reduction of radical DPPH· and the formation of radical monocation ABTS·+the ability to scavenge radical was measured in these experiments by the discoloration of the solution. However, in hydrogen peroxide method, the increased in absorbance showing its scavenging potential. The scavenging capacity of the test compounds and standard on the DPPH, ABTS·+, H2O2 decreased in the order BHT>ML>MC>C>L which were 98.4, 96.4, 86.4, 68.3, 49.7% for DPPH, BHT>ML>L>MC>C which were 99.3, 96.9, 96.3,66.6, 53.4% for ABTS·+, BHT>ML>MC>L>C which were 68.8%, 52.4%, 49.6%, 43.1% and 37.7% for H2O2 at the concentration of 50 µg/ml, respectively.Conclusion: The experimental findings showed that cis-[Cr(C2O4)2(H2O)2]--levodopa and cis-[Cr(C2O4)2(H2O)2]--carbidopa are having higher antioxidant potential than Levodopa and carbidopa although not superior to that of standard compound

Anthelmintic and anti-filarial coumarins of natural and synthetic origin: Chemical and biological intervention

Coumarin is a bicyclic system with a lactone-(hetero)aryl motif and a critical structural unit of many natural and synthetic pharmaceutical compounds. The coumarins possess a broad spectrum of biological activities and have successful clinical applications. Several coumarin-based natural compounds like osthol, isopimpinellin, umbelliferon, scopoletin, scopoline, cleomiscosin A to D, and inophyllum E have been isolated with anthelmintic and antifilarial activities. The ability of coumarin to interact with various active sites through noncovalent interactions like van der Waals forces, metal coordination, electrostatic and hydrophobic interaction, as well as hydrogen bonding, have led to the synthesis of different coumarins with significant anthelmintic and anti-filarial activities. The SAR studies of parasitic coumarins revealed that a hydroxy group at C-4 and C-7 positions has a deciding role in the anthelmintic and anti-filarial activity. The careful structure–activity studies could be effectively employed in the structural optimization of the bicyclic coumarin ring, allowing it to have many derivatives that could be screened for helminthiases. We hope this review will provide a structure-based input to researchers to design and develop novel coumarin hybrids to treat helminthiasis and filariasis

SYNTHESIS, CHARACTERIZATION AND ANTIOXIDANT ACTIVITY OF POTASSIUM CIS-DIAQUA-BIS (OXALATO) CHROMATE (III) WITH LEVODOPA AND CARBIDOPA

Objective: These studies focus on the interaction between two clinically active antiparkinsonian drugs L-dopa (L) and carbidopa (C) with the cis-[Cr(C2O4)2(H2O)2]-and evaluation of the synthesized product from a coordination chemistry aspect with respect to the possibility of its antioxidant activity and its therapeutic application in the treatment of Parkinson disease.Methods: The resulting synthesized complexes were characterized by UV-VIS and FTIR spectroscopy. Evaluation of antioxidant activities of this cis-[Cr(C2O4)2(H2O)2]--L-dopa(ML), cis-[Cr(C2O4)2(H2O)2]--carbidopa(MC) and standard butylated hydroxytoluene (BHT) were carried out by using 1,1-diphenyl-1-picrylhydrazyl free radical (DPPH), 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cations and hydrogen peroxide method.Results: The results of spectral analysis of the synthesized products indicate that complexes have a Cr(III) ion coordinated via the carboxylic and amino group. In the reduction of radical DPPH· and the formation of radical monocation ABTS·+the ability to scavenge radical was measured in these experiments by the discoloration of the solution. However, in hydrogen peroxide method, the increased in absorbance showing its scavenging potential. The scavenging capacity of the test compounds and standard on the DPPH, ABTS·+, H2O2 decreased in the order BHT>ML>MC>C>L which were 98.4, 96.4, 86.4, 68.3, 49.7% for DPPH, BHT>ML>L>MC>C which were 99.3, 96.9, 96.3,66.6, 53.4% for ABTS·+, BHT>ML>MC>L>C which were 68.8%, 52.4%, 49.6%, 43.1% and 37.7% for H2O2 at the concentration of 50 µg/ml, respectively.Conclusion: The experimental findings showed that cis-[Cr(C2O4)2(H2O)2]--levodopa and cis-[Cr(C2O4)2(H2O)2]--carbidopa are having higher antioxidant potential than Levodopa and carbidopa although not superior to that of standard compound

In Silico Design & Development of Some Selected Flavonols Against Beta–Glucuronidase Inhibitory Activity

Drug discovery process develops faster due to more advances in computational techniques. The protein ligand interaction well predicted due to the in-silico approach study. The present investigation focused towards the development of lead structure for treatment of hepatic disorders. An increase in serum acid hydrolase, including β-glucuronidase has been reported in numbers of pathological conditions such as arthritis, renal diseases and epilepsies. Enhancement of this enzyme β–glucuronidase in blood has been found to correlate significantly with liver damage. β-glucuronidase inhibitor is a novel approach which is different from the available hepatoprotective drug therapies. Method: The current study is based on in-silico ligand screening and in-vitro estimation of the three flavonols [Naringenin, Quercetin and 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one] compounds with enzyme β-glucuronidase. Molecular docking software Py Rex and Py Mol was used to dock the selected ligand in the binding site of the crystal structure of protein. Results: Docking results are based on the least binding energy of the selected flavonols compounds. Further attempt has been made towards in-vitro estimation of this enzyme with those selected compounds. The binding affinity with existence of hydrogen bonds leads to find out the mechanism which was well correlated with the findings of in-vitro inhibitory activity. Conclusion: The result outcome of the binding orientation of 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one linked with the active amino acid residue of the protein and the binding affinity leads to find out the mechanism for its potential in-vitro inhibitory activity

In Silico Design & Development of Some Selected Flavonols Against Beta–Glucuronidase Inhibitory Activity

Drug discovery process develops faster due to more advances in computational techniques. The protein ligand interaction well predicted due to the in-silico approach study. The present investigation focused towards the development of lead structure for treatment of hepatic disorders. An increase in serum acid hydrolase, including β-glucuronidase has been reported in numbers of pathological conditions such as arthritis, renal diseases and epilepsies. Enhancement of this enzyme β–glucuronidase in blood has been found to correlate significantly with liver damage. β-glucuronidase inhibitor is a novel approach which is different from the available hepatoprotective drug therapies. Method: The current study is based on in-silico ligand screening and in-vitro estimation of the three flavonols [Naringenin, Quercetin and 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one] compounds with enzyme β-glucuronidase. Molecular docking software Py Rex and Py Mol was used to dock the selected ligand in the binding site of the crystal structure of protein. Results: Docking results are based on the least binding energy of the selected flavonols compounds. Further attempt has been made towards in-vitro estimation of this enzyme with those selected compounds. The binding affinity with existence of hydrogen bonds leads to find out the mechanism which was well correlated with the findings of in-vitro inhibitory activity. Conclusion: The result outcome of the binding orientation of 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one linked with the active amino acid residue of the protein and the binding affinity leads to find out the mechanism for its potential in-vitro inhibitory activity

Abstracts of National Conference on Research and Developments in Material Processing, Modelling and Characterization 2020

This book presents the abstracts of the papers presented to the Online National Conference on Research and Developments in Material Processing, Modelling and Characterization 2020 (RDMPMC-2020) held on 26th and 27th August 2020 organized by the Department of Metallurgical and Materials Science in Association with the Department of Production and Industrial Engineering, National Institute of Technology Jamshedpur, Jharkhand, India. Conference Title: National Conference on Research and Developments in Material Processing, Modelling and Characterization 2020Conference Acronym: RDMPMC-2020Conference Date: 26–27 August 2020Conference Location: Online (Virtual Mode)Conference Organizer: Department of Metallurgical and Materials Engineering, National Institute of Technology JamshedpurCo-organizer: Department of Production and Industrial Engineering, National Institute of Technology Jamshedpur, Jharkhand, IndiaConference Sponsor: TEQIP-