Vasodilator Effects of Des (α-carboxy-3,4-dihydroxyphenethyl) lithospermic Acid (8-Epiblechnic Acid), a Derivative of Lithospermic Acids in Salviae Miltiorrhizae Radix
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概要
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A potent vasodilator substance (compound III), [α]_D +141°, was isolated from salviae miltiorrhizae radix (dan-shen). This substance was determined to be des (α-carboxy-3,4-dihydroxyphenethyl) lithospermic acid on the basis of spectrometric and chemical evidence, and was identified with an authentic sample of 8-epiblechnic acid. However, comp. III seemed to be formed from lithospermic acid (LSA) and LSA-B during a chemical procedure to separate active ingredients. It caused a sustained, slowly developing relaxation of rat aortic strips precontracted with norepinephrine (NE) in preparations with or without endothelium. The NE-induced concentration-dependent contraction of aortic strips was significantly attenuated by pretreatment with comp. III. Concentration-response curves for Ca^<2+>-induced contracture of depolarized aortic strips with isotonic high K^+ (60mM) were not affected by comp. III. Ca^<2+>-induced contraction of aortic strips, preincubated with 10^<-6>M NE in the presence of 10^<-6>M nicardipine and 0.01mM EGTA in Ca^<2+>-free solution, was slightly inhibited by comp. III. Pretreatment of aortic strips with comp. III slightly inhibited the phorbol ester (PMA)-induced contraction. These results suggest that comp. III inhibits NE-induced contraction of the aortic strips through reduction in Ca^<2+> mobilization. Since comp. III inhibits NE-induced sustained contraction, this agent may be useful in the treatment of hypertension.
- 公益社団法人日本薬学会の論文
- 1996-02-15
著者
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Kamata Katsuo
Physiology And Morphology Institute Of Medicinal Chemistry Hoshi University
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OTANI Kazuyo
Department of Pharmacognosy, Faculty of Pharmaceutical Sciences
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Otani Kazuyo
Department Of Pharmacognosy Faculty Of Pharmaceutical Sciences