Effects of Chemical Components Obtained from Plants on the Aorta with Endothelium

植物化学成分对主动脉内皮细胞的影响

基本信息

批准号：
06672117
负责人：
NAGAI Masahiro
金额：
$ 1.34万
依托单位：
Hoshi University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (C)
财政年份：
1994
资助国家：
日本
起止时间：
1994 至 1995
项目状态：
已结题

项目摘要

Tanjin and takuran originate from Labiatae plants, and have been used as crude drugs promoting blood circulation (ku-oketsu) in Chinese medicine. We searched thetwo drugs for vasodilating components to rat aortic strips with endothelium.(1) Tanjin, dried root of Salvia miltiorrhiza, contains lithospermic acids (LSA and LSA-B) as its chemical constituents. We reported that LSA-B is an endothelium-dependent vasodilator and that it induces hypotensive effects in rats through endothelium-dependent vasodilation of a resistance artery such as a mesenteric arterial bed.In our continuing research for active ingredients of tanjin, the presenceof another effective vasodilator was presumed, which seemed to be an unknown component of this crude drug. On the basis of chemical and spectral results obtained during the period of this grant-in aid, the effective vasodilator was identified as (2S, 3S)-4-[(E)-2carboxy-ethenyl]-2-(3,4-dihydroxyphenyl)-2, 3-dihydro-7-hydroxy-3-benzofurancarboxylic acid (de … More PL-LSA=8-epiblechnic acid), and was chemically derived from LSA and LSA-B by alkaline hydrolysis. In addition, dePL-LSA caused a sustained, slowly developing relaxation of rat aortic strips precontracted with norepinephrine (NE) in preparations with or without endothelium at a concentration 10^<-7>M.Taking into consideration the results of other four kinds of pharmacological experiments, we presume that dePL-LSA inhibits NE-induced contraction of the aortic strips through reduction in Ca^<2+> mobilization. DePL-LSA may be useful in the tretmanet of hypertension, because this agent inhibits NE-induced, sustained contraction.(2)Since commercially-available takuran mostly comes from upper-ground part of Eupatorium fortunei (Compositae), we cultivated Lycopus lucidus in 1994 to get a harvest enough to investigate its vasodilating components. Through the chemical and chromatographic separation of a water-extract from the plant material, three compounds were isolated, which showed vasodilating activities. Any of them seemed to be an endothelium-independent vasodilator. Identification, efficiency and mechanism of them should further be investigated. Less

Tanjin和Takaran起源于Labiatae植物，并被用作促进血液循环（Ku-Oketsu）中药的原始药物。我们搜索了两种药物，以发现带有内皮的大鼠主动脉条的血管散发成分。（1）Tanjin，salvia miltiorrhiza的干燥根，含有岩性乳酸（LSA和LSA-B）作为其化学构成。我们报道说，LSA-B是一种依赖内皮的血管扩张剂，它通过抗电阻动脉等内皮依赖性血管舒张（例如肠系膜动脉床）引起大鼠的降压作用。我们继续进行Tanjin的持续研究，对Tanjin的活跃物质进行了研究，这似乎是另一种有效的血管造成的药物，这似乎是众所周知的，这是一个不知所措的构成。根据在此授予帮助期间获得的化学和光谱结果，有效的血管扩张剂被确定为（2s，3s）-4-- [（E（e）-2-羧基 - 乙基] -2-（3,4-二羟基苯基）-2 PL-LSA = 8-元素酸），并通过葡萄糖水解从LSA和LSA-B化学得出。此外，DEPL-LSA引起了持续的，缓慢发展的大鼠主动脉条的放松，在有或不浓度的情况下，在有或没有原始的10^<-7> M.的制备过程中，用去甲肾上腺素（NE）进行了预取的持续松弛动员。 DEPL-LSA可能在高血压的心理中很有用，因为该药物会抑制NE引起的持续收缩。（2）由于商业上可用的Takaran主要来自Fortarei（Compositae）的上层一部分（Compositae），因此我们在1994年在1994年培养了足够的lycopusucusus，以进行足够的收获来调查其vasonents的vasonentsodeentsodillating。通过从植物材料中提取水的化学和色谱分离，分离了三种化合物，显示了血管生嘴活性。他们中的任何一个似乎都是独立于内皮的血管扩张剂。应进一步研究它们的识别，效率和机制。较少的