scholarly journals EVALUATION OF DOSE-DEPENDENT ACTIVITY OF BISPHENOL F ON VIABILITY PARAMETERS AND STEROIDOGENESIS IN H295R CELLS

2021 ◽  
Vol 11 (2) ◽  
Author(s):  
Nikola Knížatová
Keyword(s):  
Bisphenol F ◽  
Dependent Activity ◽  
H295r Cells ◽  
Dose Dependent

scholarly journals Biological Effect of Different Spinach Extracts in Comparison with the Individual Components of the Phytocomplex

Foods ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 382
Author(s):  
Laura Arru ◽  
Francesca Mussi ◽  
Luca Forti ◽  
Annamaria Buschini
Keyword(s):  
Antioxidant Defense ◽  
Extraction Methods ◽  
Oxidizing Agent ◽  
Endogenous Reactive Oxygen Species ◽  
Dependent Activity ◽  
Main Components ◽  
The Individual ◽  
Dose Dependent ◽  
Higher Doses ◽  
Oxidative Insult

The Mediterranean-style diet is rich in fruit and vegetables and has a great impact on the prevention of major chronic diseases, such as cardiovascular diseases and cancer. In this work we investigated the ability of spinach extracts obtained by different extraction methods and of the single main components of the phytocomplex, alone or mixed, to modulate proliferation, antioxidant defense, and genotoxicity of HT29 human colorectal cells. Spinach extracts show dose-dependent activity, increasing the level of intracellular endogenous reactive oxygen species (ROS) when tested at higher doses. In the presence of oxidative stress, the activity is related to the oxidizing agent involved (H2O2 or menadione) and by the extraction method. The single components of the phytocomplex, alone or mixed, do not alter the intracellular endogenous level of ROS but again, in the presence of an oxidative insult, the modulation of antioxidant defense depends on the oxidizing agent used. The application of the phytocomplex extracts seem to be more effective than the application of the single phytocomplex components.

scholarly journals In VivoPharmacodynamic Evaluation of an FtsZ Inhibitor, TXA-709, and Its Active Metabolite, TXA-707, in a Murine Neutropenic Thigh Infection Model

2015 ◽  
Vol 59 (10) ◽  
pp. 6568-6574 ◽  
Author(s):  
Alexander J. Lepak ◽  
Ajit Parhi ◽  
Michaela Madison ◽  
Karen Marchillo ◽  
Jamie VanHecker ◽  
...  
Keyword(s):  
Active Metabolite ◽  
Methicillin Resistance ◽  
Dose Fractionation ◽  
Infection Model ◽  
Time Curve ◽  
Cellular Division ◽  
Content Type ◽  
Concentration Time ◽  
Dependent Activity ◽  
Dose Dependent

ABSTRACTAntibiotics with novel mechanisms of action are urgently needed. Processes of cellular division are attractive targets for new drug development. FtsZ, an integral protein involved in cell cytokinesis, is a representative example. In the present study, the pharmacodynamic (PD) activity of an FtsZ inhibitor, TXA-709, and its active metabolite, TXA-707, was evaluated in the neutropenic murine thigh infection model against 5Staphylococcus aureusisolates, including both methicillin-susceptible and methicillin-resistant isolates. The pharmacokinetics (PK) of the TXA-707 active metabolite were examined after oral administration of the TXA-709 prodrug at 10, 40, and 160 mg/kg of body weight. The half-life ranged from 3.2 to 4.4 h, and the area under the concentration-time curve (AUC) and maximum concentration of drug in serum (Cmax) were relatively linear over the doses studied. All organisms exhibited an MIC of 1 mg/liter. Dose fractionation demonstrated the area under the concentration-time curve over 24 h in the steady state divided by the MIC (AUC/MIC ratio) to be the PD index most closely linked to efficacy (R2= 0.72). Dose-dependent activity was demonstrated against all 5 isolates, and the methicillin-resistance phenotype did not alter the pharmacokinetic/pharmacodynamic (PK/PD) targets. Net stasis was achieved against all isolates and a 1-log10kill level against 4 isolates. PD targets included total drug 24-h AUC/MIC values of 122 for net stasis and 243 for 1-log10killing. TXA-709 and TXA-707 are a promising novel antibacterial class and compound forS. aureusinfections. These results should prove useful for design of clinical dosing regimen trials.

scholarly journals Antifeedant Activity of Anticopalic Acid Isolated from Vitex hemsleyi

2009 ◽  
Vol 64 (7-8) ◽  
pp. 502-508 ◽  
Author(s):  
Clarisa Villegas Gómez ◽  
Mariano Martínez-Vázquez ◽  
Baldomero Esquivel
Keyword(s):  
Spodoptera Frugiperda ◽  
Antifeedant Activity ◽  
First Report ◽  
Aerial Parts ◽  
Dependent Activity ◽  
Dose Dependent

The known labdane-type diterpenoids anticopalic acid (1) and 3β-hydroxyanticopalic acid (2) were isolated from extracts of the aerial parts of Vitex hemsleyi Briq. (Labiatae). The acid 1 showed an antifeedant, dose-dependent activity against Spodoptera frugiperda (J. E. Smith) (Lepidoptera:Noctuidae). To our knowledge this is the first report on the antifeedant activity of a labdane-type diterpene against S. frugiperda.

scholarly journals Anti-inflammatory and Anti-arthritic Activities ofMerremia tridentate(L.) Hall. f.

2009 ◽  
Vol 6 (4) ◽  
pp. 943-948 ◽  
Author(s):  
M. Kamalutheen ◽  
S. Gopalakrishnan ◽  
T. Syed Ismail
Keyword(s):  
Ethanol Extract ◽  
Albino Rats ◽  
Standard Drug ◽  
Arthritis Model ◽  
Paw Oedema ◽  
Dependent Activity ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Dose Dependent ◽  
Rat Paw Oedema

The various extracts ofMerremia tridentatewere investigated for its anti-inflammatory and anti-arthritic activities in male albino rats. The anti-inflammatory activity was carried out using carrageenan-induced rat paw oedema model and the anti-arthritic activity was carried out using complete Freund’s adjuvant induced arthritis model. Indomethacin (10 mg/kg bw) was used as a standard drug. The ethanol extract ofM. tridentateexhibited significant dose dependent activity in acute inflammation and the doses of 100 mg/kg bw and 200 mg/kg bw produced 38.3% and 42.8% inhibition respectively after 3 h as compared with that of the standard drug which showed 48.5% inhibition. In arthritis model, the doses of 100 mg/kg bw and 200 mg/kg bw of the ethanol extract produced 49.0% and 51.7% inhibition respectively after 19 days when compared with that of the standard drug (55.5%). Both doses of the ethanol extract ofM. tridentateexhibit significant anti-inflammatory and anti-arthritic activities.

scholarly journals Preclinical Appraisal of Hematinic Potential of Mandura Bhasma for Treating Anemia

2021 ◽  
pp. 207-214
Author(s):  
Deepak S. Khobragade ◽  
Mrunali S. Potbhare ◽  
Awdhut Pimpale ◽  
Sagar B. Wankhede ◽  
Chandrashekhar R. Tempe
Keyword(s):  
Body Weight ◽  
Ferrous Sulphate ◽  
Standard Drug ◽  
Dependent Activity ◽  
Daily Dose ◽  
Study Institute ◽  
Dose Dependent ◽  
Pharmaceutical Education ◽  
Different Doses

Aims: To evaluate hematinic potential of mandura bhasma. Study Design: Experimental study. Place and Duration of Study: Institute of Pharmaceutical Education and Research, Wardha, Maharashtra, India. 6 Months. Methodology: The anti-anaemic potential of Mandura bhasma in Wistar rats was investigated. Anaemia was induced in rats with phenyl hydrazine hydrochloride at a dose of 10        mg kg-1 body weight by oral administration. Anaemia was treated with mandura bhasma administered in three different doses based on body weight. Results: In vivo investigation showed that though the dose of 6mg kg-1 body weight of mandura bhasm produced only a minimal antianaemic (hematinic) effect, oral daily dose of 11 mg kg-1 body weight and 22mg kg-1 body weight a produced a significant (P < 0.05) antianaemic effect when compared to standard drug ferrous sulphate indicating dose dependent activity. Conclusions: The results indicate that Mandura Bhasm have very potential dose dependant hematinic activity and can be a safe and effective drug for treating anemia.

scholarly journals Inhibition of glycogen synthase kinase-3-beta (GSK3β) blocks nucleocapsid phosphorylation and SARS-CoV-2 replication

2022 ◽  
Author(s):  
Tirosh Shapira ◽  
Celine Rens ◽  
Virginia Pichler ◽  
William Rees ◽  
Theodor Steiner ◽  
...  
Keyword(s):  
Glycogen Synthase ◽  
Host Cells ◽  
N Protein ◽  
Kinase Substrate ◽  
Protein Levels ◽  
Dependent Activity ◽  
Multiple Cell ◽  
Low Toxicity ◽  
Dose Dependent ◽  
Targeted Library

Abstract GSK3β has been proposed to have an essential role in Coronaviridae infection. Screening of a targeted library of GSK3β inhibitors against SARS-CoV-2 and HCoV-229E resulted in identification of high proportion of active compounds with low toxicity to host cells. A select lead compound, T-1686568, showed dose-dependent activity against SARS-CoV-2 transcription, translation and viral particle release in multiple cell lines and primary organoids. A protein kinase substrate profiling assay combined with western blot analysis showed that SARS-CoV-2 nucleocapsid is phosphorylated by GSK3β on S180/S184, S190/S194 and T198 which have already been primed in the adjacent phospho-sites S188, T198 and S206 respectively. Inhibition by T-1686568 resulted in reduction of the S1 Spike protein levels, an accumulation of the Nucleocapsid (N) protein and maintenance of the non-structural (NSP2) level in infected Huh-7.5.1 cells, indicating that N phosphorylation might serve as a critical precursor for processing and release of mature viruses.

scholarly journals LARVICIDAL ACTIVITY OF ESSENTIAL OIL OF GLIRICIDIA SEPIUM LEAF

2020 ◽  
pp. 26-27
Author(s):  
UMADEVI A. ◽  
ABDUL JALEEL
Keyword(s):  
Biological Activity ◽  
Essential Oil ◽  
Larvicidal Activity ◽  
Aqueous Extract ◽  
Lethal Effect ◽  
Gliricidia Sepium ◽  
Fourth Instar ◽  
Dependent Activity ◽  
The Relationship ◽  
Dose Dependent

Objective: This study focus at the larvicidal activity of essential oil of Gliricidia sepium leaf Methods: Pharmacological evaluation of leaf was carried out for larvicidal activity. Household mosquitoes of fourth instar larvae were used for the study. The study was carried out for 5 different concentrations for aqueous extract. Results: The aqueous extract shown dose-dependent activity with the maximum larvicidal potential was seen with leaf of essential oil (250 mg/ml). Conclusion: The study is designed to evaluate the larvicidal activity of essential oil of leaf of G. sepium. The relationship between the chemical composition and biological activity of essential oil of G. sepium is confirmed by lethal effect.

scholarly journals Antitumor and anti-inflammatory activities of polysaccharides isolated from Ganoderma lucidum

2011 ◽  
Vol 61 (3) ◽  
pp. 335-342 ◽  
Author(s):  
Soniamol Joseph ◽  
Baby Sabulal ◽  
Varughese George ◽  
Kuttikkadan Antony ◽  
Kainoor Janardhanan
Keyword(s):  
Ganoderma Lucidum ◽  
Tumour Volume ◽  
Carcinoma Cells ◽  
Tumour Mass ◽  
Dependent Activity ◽  
Tumour Implantation ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Potential Antitumor

Antitumor and anti-inflammatory activities of polysaccharides isolated fromGanoderma lucidumIn this study, polysaccharides were isolated fromGanoderma lucidum (Polyporaceae)and their antitumor and anti-inflammatory activities were investigated usingin vivomodels. Potential antitumor activity was shown byG. lucidumpolysaccharides (GLP) against solid tumor induced by Ehrlich's ascites carcinoma cells. GLP at 100 mg kg-1body mass showed 80.8 and 77.6 % reduction in tumour volume and tumour mass, respectively, when administered 24 h after tumour implantation. Again, GLP at the same dose but when administered prior to tumour inoculation, showed 79.5 and 81.2 % inhibition of tumour volume and tumour mass, respectively. GLP showed significant dose-dependent activity in carrageenean-induced (acute) and formalin-induced (chronic) inflammation assays. At 100 mg kg-1, GLP exhibited 57.6 and 58.2 % inhibition in carrageenean-induced and formalin-induced assays, respectively.

NEUROTOXICOLOGICAL PROFILE OF 5-НТ2А-ANTAGONIST OF IMIDAZOBENZIMIDAZOLE DERIVATIVE

2019 ◽  
pp. 23-28
Author(s):  
A. A. Spasov ◽  
D. S. Yakovlev ◽  
D. V. Maltsev ◽  
M. V. Miroshnikov ◽  
K. T. Sultanova ◽  
...  
Keyword(s):  
Oral Administration ◽  
Effective Dose ◽  
Control Group ◽  
Compound I ◽  
Toxic Dose ◽  
Test Parameters ◽  
Dependent Activity ◽  
High Doses ◽  
Dose Dependent ◽  
Average Effective Dose

Thearticlepresentstheresultsofastudyoftheneurotoxicologicalprofileofanew5-HT2A-antagonist(compoundI) using the method of multi-test observation by «S. Irwin». The test parameters were evaluated in parallel groups, receiving the compound in doses beginning with the average effective dose (ED50) and with a multiple increase of 2, 5, 7.5 and 10 times.The study revealed that the neurotoxicological properties of compound I are characterized by dose-dependent activity. It has been shown that neurotoxicological changes in the behavior of the animals did not occur with the administration of compound I at average effective dose of 10 mg / kg and doses, exceeding the effective by 2 and 5 times; the animals welfare corresponds to that of the control group. The most significant effects by the administration of the studied compound developed in high doses, exceeding the effective by 7.5 and 10 times. The limits of the minimum toxic dose (TDmin) for compound I by oral administration has been found to be 50 mg / kg <TDmin≤75 mg / kg.

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