Cardiovascular pharmacology of 3-n-butylphthalide in spontaneously hypertensive rats

Abstract

The hypotensive and vasorelaxant effects of 3‐n ‐butylphthalide (BuPh) and its possible mechanisms of action were investigated in spontaneously hypertensive rats (SHR) for the first time. A 13‐day intraperitoneal infusion of BuPh at doses of 2.0 and 4.0 mg/day produced a transient hypotensive effect while a dose of 0.5 mg/day showed a significant hypotensive effect only on day 12. BuPh at 0.5 mg/day had no effect on the plasma and tissue angiotensin converting enzyme (ACE) activities, or on the tissue lipid peroxidation index. BuPh relaxed endothelium‐intact and denuded aortic rings precontracted with phenylephrine and KCl. NG‐nitro‐L‐arginine methyl ester, an inhibitor of nitric oxide synthase, did not attenuate the vasorelaxant activity of BuPh. The cumulative concentration response curves of phenylephrine and Ca2+ (in CaCl2‐free, high KCl medium) were non‐competitively inhibited by BuPh. However, BuPh did not interfere with the caffeine‐induced release of intracellular Ca2+. It appears that the vasorelaxant effect of BuPh could be attributed to the blockade of Ca2+ entry, possibly through voltage‐ and receptor‐operated Ca2+ channels, thereby lowering the systolic blood pressure of SHR. © 1997 John Wiley & Sons, Ltd.

Anti-hypertensive medicinal plants and their mode of action

“…Intraperitoneal administration of BuPh resulted in hypotensive and relaxing effect in the case of contraction induced by phenylephrine and KCl in rat aortic rings, however, no alteration in ACE activity was observed. Blockade of voltageand receptor-operated Ca 2+ channels was suggested to be the probable mechanism (Tsi and Tan, 1997). In another study the hypotensive effect of the plant extract was suggested to be through stimulation of muscarinic receptors (Branković et al , 2010).…”

“…North America, Europe Blockage of calcium channel, stimulation of muscarinic receptor (Dianat, Veisi, 2015;Chai, Tian, 2010;Supari, 2002;Moghadam, Imenshahidi, 2013;Jorge, Ángel, 2013;Tsi and Tan, 1997;Branković, Kitić, 2010) 4…”

Cardioactive Agents from Plants

“…All compounds have been shown to possess hypotensive and vasorelaxant effects. Treatment with 3-n-Butylphthalide at doses of 2.0 and 4.0 mg/day for thirteen days produced a transient hypotensive effect [75]. In another study brazilein is a compound with a non-steroidal skeleton, obtained in a large amount from Caesalpinia sappan ethanol extracts.…”

3-(3-Methoxyanilino)isobenzofuran-1(3H)-one

“…Data collection: X-AREA (Stoe & Cie, 2002); cell refinement: X-AREA; data reduction: X-RED32 (Stoe & Cie, 2002); program(s) used to solve structure: SHELXS97 (Sheldrick, 1997); program(s) used to refine structure: SHELXL97 (Sheldrick, 1997); molecular graphics: ORTEP-3 for Windows (Farrugia, 1997); software used to prepare material for publication: WinGX (Farrugia, 1999 (Aoki et al, 1973;Lacova, 1973;Elderfield, 1951;Tsi & Tan, 1997;Bellasio, 1974;Roy & Sarkar, 2005). As part of a continuing study of the interplay between molecular conformation and supramolecular aggregation in 3-substituted phthalides, we now report the structure of the title compound, 3-(3-methoxyphenylamino)isobenzofuran-1(3H)-one, (I) (Fig.…”