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

Evaluation of the anti-ulcer activity of seeds of Syzyzium cumini on experimental animal models

Syzyzium cumini (Myrtaceae) is an evergreen tropical tree mostly found in South East Asia. Extracts of fruits and seeds are extensively used in the treatment of diabetes. Other folkloric uses include treatment of cold, cough, fever, skin problem and genitourinary tract ulcer. The present study evaluated the anti-ulcer activity of the seeds of S. cumini against different ulcer models in rats. The anti-ulcer activity of the methanol extract and ethyl acetate fraction of methanol extract of S. cumini seed was evaluated in ethanol, pylorus ligation, Aspirin + pylorus ligation and stress-induced gastric ulcer model. The study biomarkers used were gastric volume, pH, ulcer index and free acidity. The extract and fraction at the dose level of 200 mg/kg caused a significant (P <0.05) reduction in the ulcer index, free acidity while there was an increase in the pH value of the test in comparison to the solvent control group. Experimentally, it was observed that animals who received ethyl acetate fraction had relatively improved protection of gastric ulcer as demonstrated by different biomarkers. The present study showed that the ethyl acetate fraction of methanol extract of S. cumini seed possesses potential anti-ulcer activity. This may be due to a linear relationship between the antioxidant value of the seeds as reported earlier by several authors due to rich in phenolic compounds, which in turn is responsible for mucosal cytoprotection of the stomach and hence, participate in the enhancement of mucosal defence mechanism

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

COVID‐19 vaccines and their underbelly: Are we going the right way?

Abstract Background Historically, a critical aetiological agent of health concern stays till eternity after its discovery, so shall it be with the COVID‐19 outbreak. It has transformed human life to a ‘new normal’ with huge tolls on the social, psychological, intellectual and financial spheres. Aim This perspective aimed to collate numerous reported COVID‐19 vaccine‐associated adverse events and the predisposing factors. It focussed on the efficacy of mix‐n‐match (cocktail) vaccines to effectively counter COVID‐19 infection to facilitate future research and possible interventions. Material and Methods Databases like Scopus, Pubmed and the Web‐of‐science were searched for published literature on ‘adverse events associated with COVID‐19 vaccine’. The reports and updates from health agencies like the WHO and CDC were also considered for the purpose. The details with respect to the adverse events associated with COVID‐19 vaccination and the predisposing factors were compiled to obtain insights and suggest possible future directions in vaccine research. Results India stood strong to manage its health resources in time and turned into a dominant global vaccine supplier at a time when healthcare infrastructure of many countries was still significantly challenged. Developing indigenous vaccines and the vaccination drive in India were its major achievements during the second and the subsequent COVID‐19 waves. The fully indigenous Covaxin vaccine, primarily as an emergency intervention, was successfully rapidly launched. Similar such vaccines for emergency use were developed elsewhere as well. However, all of these reached the marketplace with a ‘emergency use only’ tag, without formal clinical trials and other associated formalities to validate and verify them as these would require much longer incubation time before they are available for human use. Discussion Many adverse events associated with either the first or the second/booster vaccination doses were reported. Evidently, these associated adverse events were considered as ‘usually rare’ or were often underreported. Without the additional financial or ethical burden on the vaccine companies, fortunately, the Phase IV (human) clinical trials of their manufactured vaccines are occurring by default as the human population receives these under the tag ‘emergency use’. Thus, focused and collaborative strategies to unveil the molecular mechanisms in vaccine‐related adverse events in a time‐bound manner are suggested. Conclusion Reliable data particularly on the safety of children is lacking as majority of the current over‐the‐counter COVID‐19 vaccines were for emergency use. Many of these were still in their Phase III and Phase IV trials. The need for a mutant‐proof, next‐gen COVID‐19 vaccine in the face of vaccine‐associated adverse events is opined