提高胰岛素的敏感性是寻找治疗糖尿病药物的重要手段之一。从传统中药或生物资源中寻找能够提高胰岛素敏感性的天然新型活性物质一直是科学家的努力目标,对寻找治疗糖尿病创新药物或药物先导具有重要意义。
在国家科技部973项目、国家基金委重点项目及云南省科技厅的资助下,中国科学院昆明植物研究所刘吉开课题组与上海营养所翟奇巍课题组等合作,从传统中药乌药中发现能提高胰岛素敏感性的天然活性分子。这些活性分子结构新颖奇特,具有风车状化学结构。相关结果近日相继发表在《有机快报》上。
该团队的王飞、朱华结博士等研究人员在发表的该论文中解决了手性拆分问题、确定了绝对构型,并首次提出了这类分子的生物合成途径以及乌药中存在[4+4]环加成酶的假说。这类新骨架结构类型分子的发现为有机化学家发展该类化合物新的合成策略和方法提出了新的挑战。(生物谷Bioon.com)
生物谷推荐原文出处:
Org.Lett. DOI: 10.1021/ol1011289
A Pair of Windmill-Shaped Enantiomers from Lindera aggregata with Activity toward Improvement of Insulin Sensitivity
Fei Wang?§, Yuan Gao§, Ling Zhang?, Bing Bai?, Ya Nan Hu?, Ze Jun Dong?, Qi Wei Zhai*?, Hua Jie Zhu*? and Ji Kai Liu*?
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, People’s Republic of China, BioBioPha Co. Ltd., Kunming 650204, People’s Republic of China, and Institute for Nutritional Science, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 294 Tai-Yuan Road, Shanghai 200031, People’s Republic of China
(+)-Linderaspirone A and (?)-linderaspirone A, a pair of natural windmill-shaped enantiomers, were isolated from the traditional Chinese medicine plant Lindera aggregate by HPLC using a chiral column, achieving over 98% ee. Their structures and absolute configurations were determined on the basis of extensive analysis of NMR spectra, crystal X-ray diffraction, and calculation of the optical rotations (OR). They have an unprecedented carbon skeleton and showed significant activity against glucosamine-induced insulin resistance.