Background/aims: Total saponin extracted from Tribulus terrestris (TSETT) has been reported to protect against atherosclerosis. We here investigate the cellular and molecular mechanisms of TSETT underlying protection against atherosclerosis.
Methods: Cell proliferation was measured with Methyl thiazolyl tetrazolium (MTT); Intracellular H2O2 was measured with DCFH-DA, a fluorescent dye; Intracellular free Ca(2+) was measured with a confocal laser scanning microscopy; Genes expression was measured with gene array and real-time quantitative polymerase chain reaction (RT-PCR); Phosphorylation of extracellular signal-regulated kinase 1/2 (phospho-ERK1/2) was measured with cell-based enzyme-linked immunosorbent assay (ELISA) and western blotting.
Results: TSETT significantly suppressed the increase in cells proliferation induced by angiotensin II, significantly suppressed the increase in the intracellular production of H2O2 induced by angiotensin II, significantly inhibited the increase in intracellular free Ca(2+) induced by H2O2, significantly inhibited the increase in phospho-ERK1/2 induced by angiotensin II; significantly inhibited the increase in mRNA expression of c-fos, c-jun and pkc-α induced by angiotensin II.
Conclusion: These findings provide a new insight into the antiatherosclerotic properties of TSETT and provide a pharmacological basis for the clinical application of TSETT in anti-atherosclerosis.
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http://dx.doi.org/10.1159/000354528 | DOI Listing |
PLoS One
January 2025
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AHEPA Hospital, School of Medicine, Aristotle University of Thessaloniki, Thessaloniki, Greece.
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Laboratório de Imunofarmacologia, Instituto Oswaldo Cruz (IOC), Fundação Oswaldo Cruz (Fiocruz), Rio de Janeiro 21040-361, RJ, Brazil.
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December 2024
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi Arabia.
Angiotensin-converting enzyme (ACE) is a key regulator of blood pressure, and ACE inhibition is an essential part of the treatment of hypertension. We used a molecular docking approach to find the interaction of ACE with an active flavonoid isolated from Linn, , which leads to potential antihypertensive effects in methyl predenisolone-induced hypertensive rats. Additionally, the pharmacokinetic parameters of this compound are assessed.
View Article and Find Full Text PDFPharmaceutics
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Faculty of Pharmacy, "Victor Babeş" University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania.
Olmesartan medoxomil (OLM) is the prodrug of olmesartan, an angiotensin II type 1 receptor blocker that has antihypertensive and antioxidant activities and renal protective properties. It exhibits low water solubility, which leads to poor bioavailability and limits its clinical potential. To improve the solubility of OLM, a host-guest inclusion complex (IC) between heptakis(2,6-di-O-methyl)-β-cyclodextrin (DMβCD) and the drug substance was obtained.
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