The present work describes the mechanisms involved in the vasorelaxant effect of harmine and harmaline. These alkaloids induce in a dose-dependent manner the relaxation in the aorta precontracted with noradrenaline or KCl. However, the removal of endothelium or pre-treatment of intact aortic ring with L-NAME (inhibitor of NOSe synthetase) or with indomethacin (non-specific inhibitor of cyclo-ox...

(+/-)-(E)-4-Ethyl-2-[(E)-hydroxyimino]-5-nitro-3-hexenamide (FK409) shows both potent in vitro vasorelaxant and antiplatelet activities via nitric oxide (NO) generated spontaneously from the compound. In this study, we measured spontaneous NO-releasing rates of a series of FK409 derivatives, of which chain lengths or substituents were systematically modified, in sodium-phosphate buffer solution...

fects, such as methyl brevifolincarboxylate, from the leaves of Phyllanthus niruri, ebricoic acid from the extract of Phellinus givus, and forsythiaside from the fruit of Forsythia suspensa. In our attempts to search for compounds with vasorelaxant effects from various plants, in the present study we isolated three constituents from the heartwood of Acer nikoense (Aceraceae): A. nikoense is a J...

Isosteviol (1) has been reported to exhibit moderate vasorelaxant activity. In order to enhance the bioactivity of this compound, chemical modification of 1 to the dihydro analog, ent-16β-hydroxybeyeran-19-oic acid (2), was undertaken. Compound 2 was then converted to the corresponding acetate derivative, ent-16β-acetoxybeyeran-19-oic acid (3). Biotransformation of compounds 1-3 by the fungus C...

Effects of ER-001533 (ER), a newly synthesized vasorelaxant, on the membrane currents were examined in single ventricular cells of guinea pigs. The patch-clamp technique was used in the "whole-cell" and "inside-out" patch configurations. In the whole-cell clamp condition, ER induced a time-independent K'-dominant current, which was inhibited by glibenclamide (1-3 ,uM), suggesting that ER activa...

drug design is generally achieved through trial and error methods, which is a time and resource consuming process and novel methods are needed to improve it. mathematical modelling is one of the possible solutions to speed up this process. in this study, we have presented box-jenkins model, to predict the vasorelaxant activity (pec50) of a set of benzopyrane compounds. we used the hyperchem sof...

introduction: our previous studies showed that hydroalcoholic extract of leaf of vitis vinifera relaxes the phenylephrine-induced contraction in rat thoracic aorta. this effect was dependent on endothelial integrity and no-cgmp system. the vasorelaxant effect of extract was much lesser on kcl-induced contraction. we, therefore, postulated that k+ channels are involved. the main aim of the prese...

Chemical constituents investigation on the seeds of Machilus yunnanensis led to two new phenolic compounds 8-O-acetyl-phenylethanoid-4-O-β-D-glucopyranoside (1) and (E)-2,3-bis(4-hydroxyphenyl)acrylaldehyde (2), together with 16 known compounds. Their structures were elucidated on the basis of spectroscopic data analysis (IR, MS, 1D, and 2D NMR). Meanwhile, compounds 1-3, 6-13, 17, and 18 were ...

A new indole alkaloid, naucline (1) together with four known alkaloids, angustine (2), angustidine (3), nauclefine (4) and naucletine (5), were isolated from the bark of Nauclea officinalis. The structures of all isolated compounds were elucidated with various spectroscopic methods such as 1D- and 2D- NMR, IR, UV and LCMS-IT-TOF. In addition to that of alkaloid 1, the complete 13C-NMR data of n...

Dodoneine (Ddn) is one of the active compounds identified from Agelanthusdodoneifolius, which is a medicinal plant used in African pharmacopeia and traditional medicine for the treatment of hypertension. In the context of a scientific program aiming at discovering new hypotensive agents through the original combination of natural product discovery and superacid chemistry diversification, and af...