Antihypertensive Effect of Peptides from Sesame, Almond, and Pumpkin Seeds: In-silico and In-vivo Evaluation

2018 ◽  
Vol 30 (1) ◽  
Keyword(s):  
In Silico ◽  
Antihypertensive Effect ◽  
In Vivo Evaluation ◽  
Pumpkin Seeds

scholarly journals A New Symmetrical Thiazolidinedione Derivative: In Silico Design, Synthesis, and In Vivo Evaluation on a Streptozotocin- Induced Rat Model of Diabetes

Processes ◽  
2021 ◽  
Vol 9 (8) ◽  
pp. 1294
Author(s):  
Samuel Álvarez-Almazán ◽  
Gabriel Navarrete-Vázquez ◽  
Itzia Irene Padilla-Martínez ◽  
José Correa-Basurto ◽  
Diana Alemán-González-Duhart ◽  
...  
Keyword(s):  
Rat Model ◽  
In Silico ◽  
Female Rats ◽  
Therapeutic Effects ◽  
Acute Oral Toxicity ◽  
Oral Toxicity ◽  
In Vivo Evaluation ◽  
Docking Simulations ◽  
Ppar Γ

By activating PPAR-γ, thiazolidinediones normalize glucose levels in animal models of type 2 diabetes and in patients with this pathology. The aim of the present study was to analyze 219 new derivatives in silico and select the best for synthesis, to be evaluated for acute oral toxicity in female rats and for control of diabetes-related parameters in a rat model of streptozotocin-induced diabetes. The best compound was chosen based on pharmacokinetic, pharmacodynamic, and toxicological parameters obtained in silico and binding orientation observed by docking simulations on PPAR-γ. Compound 1G was synthesized by a quick and easy Knoevenagel condensation. Acute oral toxicity was found at a dose greater than 2000 mg/Kg. Compound 1G apparently produces therapeutic effects similar to those of pioglitazone, decreasing glycaemia and triglyceride levels in diabetic animals, without liver damage. Moreover, it did not cause a significant weight gain and tended to reduce polydipsia and polyphagia, while diminishing systemic inflammation related to TNF-α and IL-6. It lowered the level of endogenous antioxidant molecules such as reduced glutathione and glutathione reductase. In conclusion, 1G may be a candidate for further testing as an euglycemic agent capable of preventing the complications of diabetes.

Synthesis and characterization of Chitosan-Catechol conjugates: Development and in vitro, in silico and in vivo evaluation of mucoadhesive pellets of lafutidine

2021 ◽  
pp. 088391152199784
Author(s):  
Loveleen Kaur ◽  
Ajay Kumar Thakur ◽  
Pradeep Kumar ◽  
Inderbir Singh
Keyword(s):  
Drug Release ◽  
In Silico ◽  
Ex Vivo ◽  
Strong Interactions ◽  
Dissolution Time ◽  
Sem Images ◽  
In Vivo Evaluation ◽  
Release Studies

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

scholarly journals Antihyperuricemic, Anti-Inflammatory and Antihypertensive Effect of a Dry Extract from Solidago virgaurea L. (Asteraceae)

2021 ◽  
Vol 89 (2) ◽  
pp. 27
Author(s):  
Mircea Tămaş ◽  
Oliviu Vostinaru ◽  
Loredana Soran ◽  
Ildiko Lung ◽  
Ocsana Opris ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Rat Model ◽  
Antihypertensive Effect ◽  
Chemical Constituents ◽  
In Vivo Evaluation ◽  
Dry Extract ◽  
The Balkans ◽  
Solidago Virgaurea ◽  
Anti Inflammatory

Solidago virgaurea L. is a perennial plant used in European traditional medicine as a diuretic or a remedy for inflammatory conditions of the urinary tract but also for gout, especially in the Balkans. The present study was focused on a preclinical, in vivo evaluation of antihyperuricemic, anti-inflammatory, and antihypertensive effects of a dry extract from S. virgaurea L. (ESV). Colorimetric and HPLC–MS techniques were used to identify the main chemical constituents of ESV. Antihyperuricemic effect of ESV was assessed in a rat model of hyperuricemia induced by the administration of potassium oxonate. Antihypertensive effect of ESV was evaluated in hyperuricemic rats by monitoring systolic blood pressure with a non-invasive blood-pressure recording system. The anti-inflammatory effect of ESV was tested using a rat model of paw edema. The main chemical constituents of ESV were rutin and phenolic acids represented by chlorogenic and caffeic acid. ESV demonstrated significant antihyperuricemic effects in rats due to an uricosuric mechanism. Additionally, ESV reduced the progression of arterial hypertension in hyperuricemic rats and also showed anti-inflammatory properties slightly inferior to diclofenac. The results suggest that ESV could be a natural remedy for the treatment of gout and protection against endothelial dysfunction caused by hyperuricemia.

N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro,in silico and in vivo evaluation

2018 ◽  
Vol 93 (3) ◽  
pp. 364-372 ◽  
Author(s):  
Ajmer Singh Grewal ◽  
Rajeev Kharb ◽  
Deo Nandan Prasad ◽  
Jagdeep Singh Dua ◽  
Viney Lather
Keyword(s):  
In Silico ◽  
In Vivo Evaluation ◽  
Design Synthesis

scholarly journals In vitro and in vivo Evaluation of in silico Predicted Pneumococcal UDPG:PP Inhibitors

2020 ◽  
Vol 11 ◽  
Author(s):  
Freya Cools ◽  
Dhoha Triki ◽  
Nele Geerts ◽  
Peter Delputte ◽  
Denis Fourches ◽  
...  
Keyword(s):  
In Silico ◽  
In Vivo Evaluation

Novel phthalamide derivatives as antihypertensive agents: rapid and clean synthesis, in silico and in vivo evaluation

2019 ◽  
Vol 28 (5) ◽  
pp. 681-695
Author(s):  
Erik Andrade-Jorge ◽  
Jessica E. Rodríguez ◽  
José Bribiesca-Carlos ◽  
Itzell A. Gallardo-Ortíz ◽  
José G. Trujillo-Ferrara ◽  
...  
Keyword(s):  
In Silico ◽  
Antihypertensive Agents ◽  
In Vivo Evaluation ◽  
Clean Synthesis

Gastrointestinal transfer: In vivo evaluation and implementation in in vitro and in silico predictive tools

2014 ◽  
Vol 63 ◽  
pp. 233-242 ◽  
Author(s):  
Bart Hens ◽  
Joachim Brouwers ◽  
Bart Anneveld ◽  
Maura Corsetti ◽  
Mira Symillides ◽  
...  
Keyword(s):  
In Silico ◽  
In Vivo Evaluation ◽  
Predictive Tools
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