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来自糙叶斑鸠菊的格劳科内酯D和E对子宫和主动脉平滑肌的舒张作用。

Relaxation of uterine and aortic smooth muscle by glaucolides D and E from Vernonia liatroides.

作者信息

Campos María, Oropeza Martha, Ponce Héctor, Fernández Jaquelina, Jimenez-Estrada Manuel, Torres Héctor, Reyes-Chilpa Ricardo

机构信息

Unit of Medical Research in Pharmacology, National Medical Center S. XXI, Mexican Institute of Social Security, San Francisco 350-502, Col. Del Valle, Mexico City 03100, Mexico.

出版信息

Biol Pharm Bull. 2003 Jan;26(1):112-5. doi: 10.1248/bpb.26.112.

DOI:10.1248/bpb.26.112
PMID:12520187
Abstract

Vernonia spp. (Asteraceae) are used in herbolaria in Latin America in menstrual and stomach disorders, suggesting smooth muscle relaxing properties of some of their chemical constituents. For pharmacological support for this belief, sesquiterpene lactones glaucolides D and E were assayed on isolated rat smooth muscle. Glaucolide E proved more potent than glaucolide D to relax high KCl- or noradrenaline-induced contractions in aorta and to relax the high KCl-contraction in uterus. Hirsutinolide-type sesquiterpene lactone also was tested but displayed no effect. Relaxation of smooth muscle by structurally related sesquiterpene lactone parthenolide has been attributed mainly to the alpha-methylene gamma-lactone moiety; because glaucolides D and E lack this functional group, their relaxant properties may rely on other alkylating sites such as C10 of the germacra-1(10),4-diene-4-epoxide skeleton.

摘要

斑鸠菊属植物(菊科)在拉丁美洲的草药中用于治疗月经和胃部疾病,这表明其某些化学成分具有平滑肌松弛特性。为了从药理学上支持这一观点,对倍半萜内酯类化合物格劳可苷D和E在离体大鼠平滑肌上进行了测定。结果表明,格劳可苷E在舒张主动脉中高钾或去甲肾上腺素诱导的收缩以及舒张子宫中高钾诱导的收缩方面比格劳可苷D更有效。还测试了水苏素型倍半萜内酯,但未显示出效果。结构相关的倍半萜内酯类化合物小白菊内酯对平滑肌的舒张作用主要归因于α-亚甲基γ-内酯部分;由于格劳可苷D和E缺乏该官能团,它们的舒张特性可能依赖于其他烷基化位点,如吉马-1(10),4-二烯-4-环氧化物骨架的C10位。

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