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来自维菊属植物的贝壳杉烷型和半日花烷型二萜类化合物可抑制血管平滑肌收缩性。

Kaurane and pimarane-type diterpenes from the Viguiera species inhibit vascular smooth muscle contractility.

作者信息

Ambrosio Sergio R, Tirapelli Carlos R, da Costa Fernando B, de Oliveira Ana M

机构信息

Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto - Universidade de São Paulo (USP), Ribeirão Preto, Brazil.

出版信息

Life Sci. 2006 Aug 1;79(10):925-33. doi: 10.1016/j.lfs.2006.05.015. Epub 2006 May 23.

Abstract

The research, development and use of natural products as therapeutic agents, especially those derived from plants, have been increasing in recent years. Despite the fact that plants provide a rich source of novel biologically active compounds, only a small percentage have been phytochemically investigated and studied for their medical potential. Viguiera is a genus that belongs to the family Asteraceae and to the sunflower tribe Heliantheae, which is widespread mostly in Mexico and in other areas of the Andes and upland areas of Brazil. A review on the secondary metabolites pointed out that sesquiterpene lactones and diterpenes, of the kaurane and pimarane-type, are the main compounds produced by these plants. Some reports have shown that kaurane- and pimarane-type diterpenes exert several biological activities such as anti-inflammatory action, antimicrobial and antispasmodic activities. Kaurenoic and pimaradienoic acids, which are the main secondary metabolites isolated by our research group from the roots of Viguiera robusta and V. arenaria, respectively, have been evaluated on vascular smooth muscle contractility. We showed that these diterpenoids are able to inhibit the vascular contractility mainly by blocking extracellular Ca(2+) influx. Additionally, in this review we discuss the structure-activity relationship of the diterpenes regarding their inhibitory activity on vascular contractility.

摘要

近年来,天然产物作为治疗剂,尤其是植物来源的天然产物的研究、开发和应用不断增加。尽管植物提供了丰富的新型生物活性化合物来源,但只有一小部分经过了植物化学研究并对其医学潜力进行了研究。维菊属属于菊科向日葵族,主要分布在墨西哥以及安第斯山脉的其他地区和巴西的高地地区。一篇关于次生代谢产物的综述指出,倍半萜内酯和贝壳杉烷型及半日花烷型二萜是这些植物产生的主要化合物。一些报告表明,贝壳杉烷型和半日花烷型二萜具有多种生物活性,如抗炎作用、抗菌和抗痉挛活性。我们研究小组分别从粗壮维菊和沙地维菊的根中分离出的主要次生代谢产物贝壳杉烯酸和半日花二烯酸,已对血管平滑肌收缩性进行了评估。我们发现这些二萜类化合物主要通过阻断细胞外Ca(2+)内流来抑制血管收缩。此外,在本综述中,我们讨论了二萜类化合物对血管收缩抑制活性的构效关系。

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