pterostilbene has been researched along with 3-3--4-5--tetrahydroxystilbene* in 2 studies
2 other study(ies) available for pterostilbene and 3-3--4-5--tetrahydroxystilbene
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Protective effect of piceatannol and bioactive stilbene derivatives against hypoxia-induced toxicity in H9c2 cardiomyocytes and structural elucidation as 5-LOX inhibitors.
Stilbenes with well-known antioxidant and antiradical properties are beneficial in different pathologies including cardiovascular diseases. The present research was performed to investigate the potential protective effect of resveratrol (1) and piceatannol (2), against hypoxia-induced oxidative stress in the H9c2 cardiomyoblast cell line, and the underlying mechanisms. Compounds 1 and 2 significantly inhibited the release of peroxynitrite and thiobarbituric acid levels at na no- or submicromolar concentrations, and this effect was more evident in piceatannol-treated cells, that significantly increased MnSOD protein level in a concentration dependent manner. Furthermore, since piceatannol, which is far less abundant in natural sources, displayed a higher bioactivity than the parent compound, we hereby report on a very fast synthesis and detailed structure-based design of a focused stilbene library. Finally, taking into account that hypoxia-induced ROS accumulation also increases expression and activity of 5-lipoxygenase (5-LOX) with production of leukotrienes, we have disclosed structural key factors crucial for 5-LOX activity. Among the synthesized analogues ( 3-7), compound 7 was the most effective in improving cardiomyocytes viability and in 5-LOX inhibition. In conclusion, modeling and experimental studies provided the basis for further optimization of stilbene analogues as multi-target inhibitors of the inflammatory and oxidative pathway. Topics: Animals; Arachidonate 5-Lipoxygenase; Cell Proliferation; Cells, Cultured; Dose-Response Relationship, Drug; Hypoxia; Lipoxygenase Inhibitors; Molecular Structure; Myocytes, Cardiac; Protective Agents; Rats; Stilbenes; Structure-Activity Relationship | 2019 |
The quorum-sensing inhibiting effects of stilbenoids and their potential structure-activity relationship.
Stilbenoids, known an important phytoalexins in plants, were renowned for their beneficial effects on cardiovascular, neurological and hepatic systems. In the present study, quorum sensing inhibition activity of ten stilbenoids were tested using Chromobacterium violaceum CV026 as the bio-indicator strain and the structure-activity relationship was also investigated. Among them, resveratrol (1), piceatannol (2) and oxyresveratrol (3) showed potential anti-QS activities. At the sub-MIC concentrations, 1-3 demonstrated a statistically significant reduction of violacein in C. violaceum CV026 in a concentration dependent manner. Furthermore, the effects of 1-3 on QS regulated virulence factors in Pseudomonas aeruginosa PAO1 were also evaluated. Our results showed that the stilbenoids 1-3 can markedly decreased the production of pyocyanin and swarming motility of P. aeruginosa PAO1. Further transcriptome analyses showed that 1-3 suppressed the expression of QS-induced genes: lasR, lasI, rhlR and rhlI. Topics: Anti-Bacterial Agents; Cell Movement; Chromobacterium; Genes, Bacterial; Plant Extracts; Pseudomonas aeruginosa; Pyocyanine; Quorum Sensing; Stilbenes; Structure-Activity Relationship | 2015 |