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绞股蓝(葫芦科绞股蓝属)中的达玛烷型三萜及其在 3T3-L1 细胞中对 AMPK 的激活作用。

Dammarane-type triterpenoids from Gynostemma compressum X. X. Chen & D. R. Liang (Cucurbitaceae) and their AMPK activation effect in 3T3-L1 cells.

机构信息

National Institute of Medicinal Materials (NIMM), 3B Quang Trung, Hoan Kiem, Hanoi, Viet Nam; National Hospital for Tropical Diseases, Dong Anh, Hanoi, Viet Nam.

National Institute of Medicinal Materials (NIMM), 3B Quang Trung, Hoan Kiem, Hanoi, Viet Nam.

出版信息

Phytochemistry. 2022 Aug;200:113218. doi: 10.1016/j.phytochem.2022.113218. Epub 2022 Apr 28.

DOI:10.1016/j.phytochem.2022.113218
PMID:35490775
Abstract

Bioassay-guided fractionation of the 80% ethanol extract of Gynostemma compressum X. X. Chen & D. R. Liang (Cucurbitaceae) resulted in the isolation and identification of eight undescribed triterpenoids, gycomol VN1, gycomol VN2, and gycomosides VN1-6 from the bioactive n-butanol fraction. The structures of these compounds were elucidated by one- and two-dimensional nuclear magnetic resonance spectroscopy, high-resolution electrospray ionisation mass spectrometry, and chemical methods. All isolated compounds were evaluated for their 5'-adenosine monophosphate-activated protein kinase (AMPK) and acetyl-coenzyme A carboxylase (ACC) activation effects on 3T3-L1 cells. Importantly, gycomol VN2, gycomoside VN1, and gycomosides VN3-5 activated the phosphorylation of AMPK and its downstream substrate ACC in 3T3-L1 cells at a dose of 10 μM. These effects imply that the activation of AMPK and ACC by active compounds from G. compressum has considerable potential for the prevention of obesity and its related disorders by activating AMPK signaling pathways.

摘要

生物活性正丁醇部位经柱层析分离,从绞股蓝 80%乙醇提取物(葫芦科绞股蓝属)中分离得到 8 个新三萜皂苷,分别命名为 gycomol VN1、gycomol VN2 和 gycomosides VN1-6。通过一维和二维核磁共振波谱、高分辨电喷雾电离质谱和化学方法鉴定了这些化合物的结构。所有分离得到的化合物均在 3T3-L1 细胞中进行了 5'-单磷酸腺苷激活的蛋白激酶(AMPK)和乙酰辅酶 A 羧化酶(ACC)的激活作用评价。重要的是,gycomol VN2、gycomoside VN1 和 gycomosides VN3-5 在 10 μM 剂量下可激活 3T3-L1 细胞中 AMPK 的磷酸化及其下游底物 ACC。这些结果表明,绞股蓝中活性化合物通过激活 AMPK 信号通路,对肥胖及其相关疾病的预防具有重要作用。

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