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来自马达加斯加哈伦加那的具有α-葡萄糖苷酶抑制活性的异戊烯基化邻氨基苯甲酸类化合物。

α-Glucosidase Inhibitory Prenylated Anthranols from Harungana madagascariensis.

作者信息

Johnson Oluwatosin O, Zhao Ming, Gunn Jordan, Santarsiero Bernard D, Yin Zhi-Qi, Ayoola Gloria A, Coker H A B, Che Chun-Tao

机构信息

Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago , Chicago, Illinois 60612, United States.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Lagos , CMUL Campus, Lagos 100254, Nigeria.

出版信息

J Nat Prod. 2016 Jan 22;79(1):224-9. doi: 10.1021/acs.jnatprod.5b00924. Epub 2016 Jan 4.

DOI:10.1021/acs.jnatprod.5b00924
PMID:26727375
Abstract

Four new prenylated anthranols, harunganols C-F (1-4), along with kenganthranol A (5), harunganin (6), and ferruginin A (7), were identified from the leaves of Harungana madagascariensis. The structures of compounds 2, 5, and 7 were confirmed by single-crystal X-ray diffraction analysis. Compound 1 is a unique symmetrical anthranol dimer connected via a CH2 group. Compound 4 possesses a unique C-10 hemiketal group. All anthranols were evaluated for their α-glucosidase inhibitory activities. They displayed a higher potency compared to acarbose except for 3 and 4. In particular, harunganol C (1) showed an IC50 value of 1.2 μM.

摘要

从马达加斯加哈伦加那树(Harungana madagascariensis)的叶子中鉴定出四种新的异戊烯基化邻氨基苯甲酸醇,即哈伦加诺醇C - F(1 - 4),以及肯甘邻氨基苯甲酸醇A(5)、哈伦加宁(6)和铁锈宁A(7)。化合物2、5和7的结构通过单晶X射线衍射分析得以确证。化合物1是一种通过CH₂基团连接的独特对称邻氨基苯甲酸醇二聚体。化合物4具有一个独特的C - 10半缩酮基团。对所有邻氨基苯甲酸醇进行了α - 葡萄糖苷酶抑制活性评估。除3和4外,它们表现出比阿卡波糖更高的活性。特别是,哈伦加诺醇C(1)的IC₅₀值为1.2 μM。

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