scholarly journals IN VITRO HEPATOPROTECTIVE EFFECT OF ECHINOCHLOA COLONA ON ETHANOL-INDUCED OXIDATIVE DAMAGE IN HEPG2 CELLS

2017 ◽  
Vol 10 (9) ◽  
pp. 259 ◽  
Author(s):  
Praneetha Pallerla ◽  
Durgaih G ◽  
Narsimha Reddy Y ◽  
Ravi Kumar B
Keyword(s):  
Hepg2 Cell ◽  
Hepatoprotective Activity ◽  
Standard Drug ◽  
Cytoprotective Activity ◽  
Cytotoxicity Studies ◽  
Maximum Protection ◽  
Diphenyl Tetrazolium Bromide ◽  
Hepg2 Cell Lines ◽  
Dose Dependent

  Objective: The current study was aimed to evaluate the methanolic extract of caryopses of Echinochloa colona (ECME) for its in vitro hepatoprotective activity against ethanol in HepG2 cell lines.Methods: In this regard, the cytotoxicity studies were conducted for the extract, ECME using 3-(4,5-dimethythiazol- 2-yl)-2,5-diphenyl tetrazolium bromide assay to determine the inhibitory concentration 50% value based on which, the doses 50, 100, and 200 μg/ml were selected for the hepatoprotective studies in HepG2 cell lines. The toxicity was induced using ethanol (100 mM). The in vitro hepatoprotective activity of the extract was assessed based on the changes in the level of biochemical parameters such as aspartate aminotransferase, alanine aminotransferase, and lactate dehydrogenase.Results: The extract, ECME has shown a dose-dependent cytoprotective activity with maximum protection at 200 μg/ml. The percentage cell viability of the extract, ECME at 200 μg/ml was more, i.e., 69.33% which was well comparable to that of standard drug, silymarin (100 μg/ml).Conclusion: The study revealed that the extract had shown significant hepatoprotective activity at all the test doses against ethanol-induced cytotoxity assay.

scholarly journals e-Pharmacophore model-guided design of potential DprE1 inhibitors: synthesis, in vitro antitubercular assay and molecular modelling studies

2021 ◽  
Author(s):  
Avinash Kumar ◽  
Revathi Rajappan ◽  
Suvarna G. Kini ◽  
Ekta Rathi ◽  
Sriram Dharmarajan ◽  
...  
Keyword(s):  
Pharmacophore Model ◽  
Antitubercular Activity ◽  
Stable Complex ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Standard Drug ◽  
Docking Score ◽  
Mycobacterium Tuberculosis H37rv ◽  
Cytotoxicity Studies

AbstractTuberculosis continues to wreak havoc worldwide and caused around 1.4 million deaths in 2019. Hence, in our pursuit of developing novel antitubercular compounds, we are reporting the e-Pharmacophore-based design of DprE1 (decaprenylphosphoryl-ribose 2′-oxidase) inhibitors. In the present work, we have developed a four-feature e-Pharmacophore model based on the receptor–ligand cavity of DprE1 protein (PDB ID 4P8C) and mapped our previous reported library of compounds against it. The compounds were ranked on phase screen score, and the insights obtained from their alignment were used to design some novel compounds. The designed compounds were docked with DprE1 protein in extra-precision mode using Glide module of Maestro, Schrodinger. Some derivatives like B1, B2, B4, B5 and B12 showed comparable docking score (docking score > − 6.0) with respect to the co-crystallized ligand. The designed compounds were synthesized and characterized. In vitro antitubercular activity was carried out on Mycobacterium tuberculosis H37Rv (ATCC27294) strain using the agar dilution method, and minimum inhibitory concentration (MIC) was determined. The compound B12 showed a MIC value of 1.56 μg/ml which was better than the standard drug ethambutol (3.125 μg/ml). Compounds B7 and B11 were found to be equipotent with ethambutol. Cytotoxicity studies against Vero cell lines proved that these compounds were non-cytotoxic. Molecular dynamic simulation study also suggests that compound B12 will form a stable complex with DprE1 protein and will show the crucial H-bond interaction with LYS418 residue. Further in vitro enzyme inhibition studies are required to validate these findings.

scholarly journals IN VITRO ANTI-INFLAMMATORY AND ANTIOXIDANT ACTIVITIES OF HINGULESWARA RASABASED HERBOMINERAL FORMULATIONS

2018 ◽  
Vol 11 (14) ◽  
pp. 24
Author(s):  
Abhishek Chatterjee ◽  
Dileep Singh Baghel ◽  
Bimlesh Kumar ◽  
Saurabh Singh ◽  
Narendra Kumar Pandey ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Standard Drug ◽  
Three Samples ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Antioxidant Effects ◽  
Made In ◽  
In Vitro Antioxidant Activity

Objective: The aims of the present investigation were to develop the herbal and/or herbomineral formulations of Hinguleswara rasa and to compare their anti-inflammatory and antioxidant activities, in vitro, with that of standard drug samples.Methods: This study was an interventional investigation in three samples: In the first sample, Hinguleswara rasa (HR1) was prepared as per methodology described in Rasatarangini using Shuddha Hingula (10 g), Shuddha Vatsanabha (10 g), and Pippali (10 g). In the second and third sample, respectively, Hinguleswara rasa was prepared by replacing Shuddha Hingula with Kajjali where Kajjali made from Hingulotha parada and Sodhita parada constitutes two varieties of Hinguleswara rasa, i.e. HR2 and HR3. In vitro antioxidant activity was studied using 2,2-diphenyl-1-picrylhydrazyl, and the absorbance was recorded at 517 nm. For evaluating the in vitro anti-inflammatory studies, the inhibition of albumin denaturation technique was performed.Results: The results showed that the formulation of Hinguleswara rasa has shown dose-dependent activity which was observed in 100 μg concentration. HR1, HR2, and HR3 showed 36.11, 17.22, and 16.11% radical scavenging activity.Conclusion: It could be concluded that the changes made in the formulations did not affect the in vitro anti-inflammatory and antioxidant effects of the herbomineral formulations.

scholarly journals EVALUATION AND COMPARISON OF CYTOTOXIC EFFECT OF VILAZODONE HYDROCHLORIDE WITH 5-FLUOROURACIL IN HT-29 BOWEL CANCER CELL LINE

2019 ◽  
pp. 124-127
Author(s):  
LATHA PRIYA A ◽  
ANUSHA D ◽  
DARLING CHELLATHAI K ◽  
HEMALATHA A ◽  
JEGAN MOHAN Y
Keyword(s):  
Cell Line ◽  
Cytotoxic Effect ◽  
Depressive Disorders ◽  
Cancer Cell Line ◽  
Test Sample ◽  
Standard Drug ◽  
Drug Sample ◽  
Diphenyl Tetrazolium Bromide ◽  
Ht 29

Objectives: Vilazodone hydrochloride is a novel selective serotonin reuptake inhibitor (SSRI) used to treat major depressive disorders. There are only sparse data available to know about the SSRI’s and its association with colon cancer. This study aims to evaluate and compare the in vitro cytotoxic effect of vilazodone with 5-fluorouracil (5-FU) in HT-29 cell line. Methods: Cell viability was tested by the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay (Mosmann, 1983). Test sample and standard drug in variable concentrations were added to the HT-29 cell lines for incubation over 24 h under ideal conditions. After washing the test and standard drug sample from the well with saline, MTT was added and incubated for 4 h. Dimethyl sulfoxide of 1 ml was added in all wells after incubation with MTT. The absorbance at 570 nm was measured with an ultraviolet - spectrophotometer. Results: The values were tabulated, and the graph was plotted to find the IC-50 value (inhibitory concentration at 50%) which was struck at 28.5 μg/ml and12. 8 μg/ml for vilazodone hydrochloride and 5-FU, respectively. Conclusion: The results show that vilazodone hydrochloride has good anticancer property comparable with 5-FU, which would probably play a role as a cytotoxic agent in tumor cells. The proposed mechanism of action could be by activation of caspase-3 enzyme, thereby increasing apoptosis and indicates its use in coexisting depression and colon carcinoma. Other mechanism includes suppression of oncogene p53, which can be confirmed by future studies.

Evaluation of Hepatoprotective activity of Methanol extract of Persicaria hydropiper: An in vivo screening

2021 ◽  
pp. 5819-5824
Author(s):  
Pooja Kamra ◽  
Mahaveer Singh ◽  
Hardarshan Singh Lamba ◽  
Birendra Srivastava
Keyword(s):  
Carbon Tetrachloride ◽  
Intraperitoneal Administration ◽  
Hepatoprotective Activity ◽  
Dependent Manner ◽  
Standard Drug ◽  
Whole Plant ◽  
Dose Dependent ◽  
Histopathological Investigation ◽  
Different Doses

The present study aimed to evaluate the hepatoprotective potential of methanolic whole plant extract of Persicaria hydropiper in carbon tetrachloride (CCl4) induced hepatotoxicity model. Hepatotoxicity was induced in rats by intraperitoneal administration of carbon tetrachloride (CCl4) for seven days. The extract was thereafter administered at two different doses of 200 mg/kg and 400 mg/kg body weight for next seven days. Silymarin was used as a reference standard. The extract revealed hepatoprotective activity in dose dependent manner. The dose of 400 mg/kg exhibited maximum hepatoprotective ability as apparent from several evaluation parameters including liver function profile, bilirubin, antioxidant enzymes as well as histopathological investigation which was comparable to the standard drug Silymarin respectively. These findings sustenance the use of the extract as an adjuvant with existing therapy for treatment of liver ailments.

Green Synthesis of Silver Nanocomposites of Nigella sativa Seeds Extract for Hepatocellular Carcinoma

2019 ◽  
Vol 4 (3) ◽  
pp. 191-200 ◽  
Author(s):  
Afreen Usmani ◽  
Anuradha Mishra ◽  
Asif Jafri ◽  
Md Arshad ◽  
Mohd Aftab Siddiqui
Keyword(s):  
Hepatocellular Carcinoma ◽  
Green Synthesis ◽  
Hepg2 Cell ◽  
Cell Lines ◽  
Nigella Sativa ◽  
Uv Spectroscopy ◽  
Silver Nanocomposites ◽  
Natural Drugs ◽  
Hepg2 Cell Lines

Background: Silver nanoparticles play a significant role in bioavailability and refining the compatibility of natural drugs in the treatment of various chronic diseases including different types of cancer. Objective: Green synthesis of silver nanocomposites of Nigella sativa seeds extract to evaluate the anticancer effects against hepatocellular carcinoma using HepG2 cell lines. Methods: The AgNCs were developed by treating aqueous extract of N. sativa seeds treated with silver nitrate (1mM) solution and were used to test its efficacy against hepatocellular carcinoma using HepG2 cell lines. Results and Discussion: The Surface Plasmon Resonance (SPR) of prepared AgNCs showed a peak at 432 nm via UV spectroscopy. The selected N. sativa AgNCs were characterized for polydispersity, surface charge and size and the results showed 0.215±0.093 polydispersity index (PDI), zeta potential 18.8±0.372 mV and size range 10-20 nm, respectively. The Fourier transform infrared spectroscopy (FTIR) also showed various peak of functional groups that are possibly involved in the reduction of silver ion and synthesized the N. sativa silver nanocomposites, respectively. N. sativa AgNCs showed 89.954% drug release while in the case of extract release, it was only 33.821% in 24 hrs. Further, in vitro studies of N. sativa AgNCs against hepatocellular carcinoma showed good cytotoxic effect p<0.05 with 7.16 µg/ml IC50 value. Conclusion: Thus, the present results revealed that green synthesis of N. sativa AgNCs can be an alternative tool for clinical application in cancer therapy; however, there is a need to find the mechanism and role of AgNCs inside the individual.

scholarly journals INVESTIGATION ON PHARMACOGNOSY AS WELL AS THE ANTIOXIDANT, ANTI-INFLAMMATORY POTENTIAL OF THE KATHA POWDER

2021 ◽  
pp. 125-132
Author(s):  
PANKAJ SHARMA ◽  
RAJU L
Keyword(s):  
Diclofenac Sodium ◽  
In Vitro Study ◽  
Alcoholic Solution ◽  
Hot Water ◽  
Dependent Manner ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Acacia Catechu ◽  
Dose Dependent

Objective: The objective of the study was to investigate the pharmacognosy as well as the antioxidant, anti-inflammatory potential of the Katha powder. Methods: The Coarsely dried chips of Acacia catechu heartwood were treated with 10 % hydro-alcoholic solution to obtain Katha as the final product. The powdered Katha was standardized through pharmacognostic parameters. This Katha power is showing the good solubility in the hot water having astringent in the taste. The powder microscopy of the Katha powder is to be demonstrated fragments of acicular crystals, fibers, and bordered pitted vessels. Katha powder antioxidant potential is to be accessed by using the 2, 2-diphenyl-1-picryl hydrazyl assay and NO Scavenging assay using ascorbic acid as a standard drug. Further, the Katha powder is to be subjected for the assessment of its anti-inflammatory potential by the use of heat-induced hemolysis as well as hypotonicity-induced hemolysis approach by the use of the aspirin or diclofenac sodium as a standard drug. Results: Microscopical investigations were showed that Katha showing the presence of fragments of acicular crystals, fibers, and bordered pitted vessels. In vitro study shows that the Katha powder has excellent antioxidant as well as anti-inflammatory potential in a dose-dependent manner in comparison of the result of heartwood of A. catechu. Conclusion: So from this investigation, it is to be suggested that the Katha powder is rich in the phenolic compound and the experimentation study shows that the drug is to possess a good antioxidant as well as anti-inflammatory property.

scholarly journals Ethanolic extract of ocimum kilimandscharicum linnleaves: phytochemical and in vitro pharmacological activity

2021 ◽  
pp. 106-109
Author(s):  
Yamini N ◽  
Lahari S ◽  
Phani deepthi V
Keyword(s):  
In Vitro Model ◽  
Ethanolic Extract ◽  
Clinical Development ◽  
Dependent Manner ◽  
Thrombolytic Activity ◽  
Standard Drug ◽  
Ethanolic Extracts ◽  
Vitro Model ◽  
Dose Dependent

Using an in vitro model, the anti-thrombolytic efficacy of ethanolic extracts of Ocimum kilimandscharicum Linn was investigated. The researchers discovered that different concentrations of the extract had significant anti-thrombolytic activity in a dose-dependent manner , which was comparable to a standard drug. As a result of the presence of flavonoids and polyphenols in the plant extract, it can be concluded that it has a promising future in the treatment of thrombosis. This knowledge will be useful in the clinical development of thrombolytic therapeutics by identifying more potent anti-thrombolytic principles from natural resources..    

scholarly journals Identification of Suitable Agents against Adenine Phosphoribosyl Transferase for the Management of Leishmaniasis: Synthesis, Characterization and Computational Studies

2021 ◽  
Vol 12 (6) ◽  
pp. 7503-7522
Keyword(s):  
Leishmania Donovani ◽  
Antileishmanial Activity ◽  
Standard Drug ◽  
Docking Analysis ◽  
Equivalent Number ◽  
In Silico Admet ◽  
Drug Score ◽  
Diphenyl Tetrazolium Bromide ◽  
Genus Leishmania

A leishmaniasis is a group of diseases attributable to protozoan parasites of the genus Leishmania. It is a potential disease mostly occurring in developing nations. Various quinoline substituted derivatives (11a-f, 12a-f, and 13a-f) were synthesized by refluxing amino quinolines with an equivalent number of different alkylaminoethyl chlorides and evaluated for their in vitro antileishmanial activity against promastigotes forms of Leishmania donovani by using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] reduction assay. Compounds 11f (IC50 = 13.61μg/mL), 12f (IC50 = 11.92 μg/mL) and 13f (IC50 =10.41 μg/mL) have shown significant antileishmanial activity when compared with standard sitamaquine (IC50= 10.09 μg/mL). Furthermore, the molecular docking analysis targeting adenine phosphoribosyltransferase of Leishmania donovani exhibits significant binding interactions. In silico, ADMET predictions revealed that these compounds, i.e., 11f, 12f, and 13f, demonstrated good absorption as well as solubility characteristics with good drug-likeness and drug score values compared to the standard drug.

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