密毛乳香树根中的拉蒂烷二萜及其生物活性。

Lathyrane diterpenoids from the roots of Euphorbia micractina and their biological activities.

机构信息

State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, and Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.

出版信息

J Nat Prod. 2011 May 27;74(5):1221-9. doi: 10.1021/np2001489. Epub 2011 May 2.

DOI:10.1021/np2001489

PMID:21534583

Abstract

Seventeen new lathyrane diterpenoids (1-17) and two known analogues have been isolated from an ethanolic extract of Euphorbia micractina roots. Their structures including absolute configurations were determined by spectroscopic data interpretation and single-crystal X-ray crystallography. Compound 10 showed activity against HIV-1 replication in vitro, with an IC50 value of 8.2 μM. Compounds 6, 7, 11, 14, 15, and 18, at 10(-6) M, showed significant vascular-relaxing activities against phenylephrine-induced vasoconstriction with relaxation rates of 48%, 41%, 42%, 48%, 50%, and 53%, respectively.

摘要

从 Micractinina 属植物 Micractinina 根的乙醇提取物中分离得到了 17 种新的拉蒂烷二萜类化合物（1-17）和两种已知类似物。通过光谱数据分析和单晶 X 射线晶体学确定了它们的结构包括绝对构型。化合物 10 对 HIV-1 复制具有体外抑制活性，IC50 值为 8.2 μM。化合物 6、7、11、14、15 和 18 在 10(-6) M 时对苯肾上腺素诱导的血管收缩具有显著的血管舒张活性，其舒张率分别为 48%、41%、42%、48%、50%和 53%。