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

• 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
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-06672117/
• 关键词: Salvia miltiorrhiza; Lycopus Incidus; Lithospermic acid derivative; Smooth muscle relaxation; Vasodilator; 血管弛緩物質; 丹参; リゾスペルミン酸誘導体; シネロ; リソスペルミン酸誘導体

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

丹参和takuran源于唇形科植物，在中医中被用作促进血液循环的原料药。用大鼠带内皮主动脉条研究两种药物的扩血管活性成分。(1)丹金为丹参的干燥根，其化学成分为紫草酸（LSA和LSA-B）。本文报道LSA-B是一种内皮依赖性血管扩张剂，它通过内皮依赖性血管扩张阻力动脉（如肠系膜动脉床）而引起大鼠的血管扩张作用，在我们对丹参活性成分的进一步研究中，推测存在另一种有效的血管扩张剂，这似乎是该生药的一种未知成分。根据在资助期间获得的化学和光谱结果，有效的血管扩张剂被鉴定为（2S，3S）-4-[（E）-2羧基-乙烯基]-2-（3，4-二羟基苯基）-2，3-二氢-7-羟基-3-苯并呋喃羧酸（de ...更多信息 PL-LSA=8-表亚麻酸），并通过碱水解从LSA和LSA-B化学衍生。此外，dePL-LSA在浓度为10 μ M时，可引起去甲肾上腺素（NE）预收缩的大鼠主动脉条的持续的、缓慢发展的舒张<-7>。考虑到其他四种药理学实验的结果，我们推测dePL-LSA通过减少Ca^2+动员来抑制NE诱导的主动脉条的收缩。DePL-LSA可用于治疗高血压，因为该药物抑制NE诱导的持续收缩。（2）由于目前市售的泽兰主要来源于菊科植物佩兰的地上部分，因此我们于1994年对泽兰进行了栽培，以获得足够的收获量来研究泽兰的扩血管活性成分。通过化学和色谱分离，从该植物的水提取物中分离出三个化合物，它们具有扩血管活性。它们中的任何一种似乎都是非内皮依赖性血管扩张剂。其识别、效率和作用机制有待进一步研究。少

项目成果

鎌田 勝雄: "Hypotensive Effects of Lithospermic Acid B Isolated from the Extract of Salviae Miltiorrhizae Radix in the Rat" General Pharmacology. 25. 69-73 (1994)

Katsuo Kamata：“从丹参提取物中分离出的紫精酸 B 对大鼠的降压作用”普通药理学 25. 69-73 (1994)。

永井正博: "Vasodilator Effects of Des(α-carboxy-3,4-dihydroxy-phenethyl)lithospermic Acid(8-Epiblechnic Acid),a Derivative of Lithospermic Acids in Salviae Miltionhizae Radix." Biological a Pharmaceutical Bulletin. 19. 228-232 (1996)

Masahiro Nagai：“Des(α-羧基-3,4-二羟基-苯乙基)紫精酸(8-Epiblechnic Acid)的血管舒张作用，紫精酸是丹参中的一种衍生物，生物药物通报19。228-”。 232 (1996)

Katsuo Kamata, Tohru Iizuka, Masahiro Nagai and Yutaka Kasuya: "Endothelium-Dependent Vasodilator Effects of the Extract from Salviae Miltiorrhizae Radix. A study on the Identification of lithospermic Acid B in the Extracts." General Pharmacology. 24. 977

Katsuo Kamata、Tohru Iizuka、Masahiro Nagai 和 Yutaka Kasuya：“丹参提取物的内皮依赖性血管舒张作用。提取物中紫精酸 B 的鉴定研究。”

Katsuo Kamata, Mariko Noguchi and Masahiro Nagai: "Hypotensive Effects of Lithospermic Acid B Isolated from the Extract of Salviae Miltiorrhizae Radix in the Rat." General Pharmacology. 25. 69-73 (1994)

Katsuo Kamata、Mariko Noguchi 和 Masahiro Nagai：“从丹参提取物中分离出的紫精酸 B 对大鼠的降血压作用。”

鎌田勝雄: "Endothelium-Dependent Vasodilator Effects of the Extrat from Salviae Miltiorrhizae Radix. A Study on the Identification of Lithospermic Acid B in the Extracts." Generla Pharmacology. 24. 977-981 (1993)

Katsuo Kamata：“丹参提取物的内皮依赖性血管舒张作用。提取物中紫草酸 B 的鉴定研究。药理学概要 24. 977-981 (1993)”