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三叶花椒果实中的具有α-葡萄糖苷酶抑制活性的二萜类化合物

Diterpenoids with α-glucosidase inhibitory activities from the fruits of Vitex trifolia Linn.

机构信息

School of Pharmacy, State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China.

School of Pharmacy, State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China.

出版信息

Fitoterapia. 2022 Sep;161:105248. doi: 10.1016/j.fitote.2022.105248. Epub 2022 Jun 29.

Abstract

Viticis Fructus, known as "Man-jing-zi", are the fruits of the traditional Chinese medicine Vitex trifolia Linn. and its variant Vitex trifolia Linn. var. simplicifolia. These fruits are used as folk medicines to treat various diseases. Although V. trifolia is useful for treating diabetes, the antidiabetic effect of its purified constituents is still under investigation. The phytochemical investigation on the ethanol extract of the fruits of V. trifolia yielded four new labdane diterpenoids vitetrolins A-D (1-4), together with seven (5-11) known analogs. The structures of these compounds were elucidated by spectroscopy techniques and the absolute configuration of 4 was determined by electronic circular dichroism (ECD) calculations. The isolated diterpenoids were evaluated for their α-glucosidase inhibitory activities. Compounds 5, 6, 8, and 9 exhibited moderate inhibitory activities against α-glucosidase with IC values ranging from 44.9 ± 6.1 to 70.5 ± 5.5 μM.

摘要

山茱萸,又称“蔓荆子”,是传统中药三叶蔓荆 Vitex trifolia Linn. 和其变种三叶蔓荆 Vitex trifolia Linn. var. simplicifolia 的果实。这些果实被民间用作药物治疗各种疾病。虽然三叶蔓荆对治疗糖尿病有一定作用,但对其纯化成分的降血糖作用仍在研究中。对三叶蔓荆果实的乙醇提取物进行的植物化学研究得到了四个新的半日花烷二萜类化合物 vitetrolins A-D(1-4),以及七个(5-11)已知类似物。通过光谱技术阐明了这些化合物的结构,通过电子圆二色性(ECD)计算确定了 4 的绝对构型。对分离得到的二萜类化合物进行了α-葡萄糖苷酶抑制活性评价。化合物 5、6、8 和 9 对α-葡萄糖苷酶表现出中等抑制活性,IC 值范围为 44.9±6.1 至 70.5±5.5μM。

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