Anti-diabetic xanthones from the bark of Garcinia xanthochymus

IF 2.2 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2017-08-01 DOI:10.1016/j.bmcl.2017.06.021

Chi N. Nguyen , Binh T.D. Trinh , Toan B. Tran , Le-Thu T. Nguyen , Anna K. Jäger , Lien-Hoa D. Nguyen

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引用次数: 25

Abstract

An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards α-glucosidase and PTP1B with IC₅₀ values of 0.3 ± 0.1 μg/mL and 2.3 ± 0.4 μg/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (3–12), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards α-glucosidase with IC₅₀ value of 4.1 ± 0.3 μM (compared with acarbose, IC₅₀ = 900.0 ± 3.0 μM) whilst xanthochymusxanthone B (2) exhibited remarkable activity towards PTP1B with IC₅₀ value of 8.0 ± 0.6 μM (compared with RK682, IC₅₀ = 4.4 ± 0.3 μM).

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黄藤黄树皮中抗糖尿病的山酮类化合物

藤黄树皮乙酸乙酯提取物对α-葡萄糖苷酶和PTP1B具有较强的抑制作用，IC50值分别为0.3±0.1 μg/mL和2.3±0.4 μg/mL。对其化学成分进行了分析，分离得到两个新化合物:黄酮(xanthochymusxanthones) A(1)和B(2)，以及10个已知的黄酮(3-12)。它们的结构用波谱方法确定，主要是一维和二维核磁共振。亚belliptenone F(12)对α-葡萄糖苷酶的IC50值为4.1±0.3 μM(与阿卡波糖相比，IC50值为900.0±3.0 μM)，黄糖蜜山酮B(2)对PTP1B的IC50值为8.0±0.6 μM(与RK682相比，IC50值为4.4±0.3 μM)具有显著的抑制活性。

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.