Hu Yu, Li Jianxin, Chang Alan K, Li Yanan, Tao Xia, Liu Wenbao, Wang Zhina, Su Weiping, Li Zehao, Liang Xiao
College of Pharmacy, Liaoning University, 66 Chongshan Road, Shenyang 110036, Liaoning Province, PR China.
College of Pharmacy, Liaoning University, 66 Chongshan Road, Shenyang 110036, Liaoning Province, PR China; College of Chemistry, Liaoning University, 66 Chongshan Road, Shenyang 110036, Liaoning Province, PR China.
Food Chem. 2021 Apr 9;357:129759. doi: 10.1016/j.foodchem.2021.129759.
Garcinia mangostana L. (mangosteen) is a tropical fruit that is rich in xanthones and is thought to have an anti-diabetic effect. In this study, we screened for the xanthones in mangosteen that could inhibit the activity of protein tyrosine phosphatase 1B (PTP1B), an enzyme that is targeted by diabetic drugs. Mice were orally administered mangosteen extract and blood samples were screened for the presence of PTP1B-interacting xanthones. Six such compounds (1-6) were identified by UF-HPLC-QTOF-MS and their inhibition against PTP1B was confirmed by activity assay. Among them, garcinone E (5) was found to be the most effective PTP1B inhibitor (IC = 0.43 μM). Tissue distribution analysis showed that the six compounds were distributed in eleven tissues, including the liver, muscle, fat, stomach, large intestine, small intestine, brain, kidney, heart, lung, and spleen. The results demonstrated that mangosteen might be a promising source of natural compounds with high PTP1B-inhibitory activity.
山竹（Garcinia mangostana L.）是一种富含氧杂蒽酮的热带水果，被认为具有抗糖尿病作用。在本研究中，我们筛选了山竹中能够抑制蛋白酪氨酸磷酸酶1B（PTP1B）活性的氧杂蒽酮，PTP1B是一种糖尿病药物的作用靶点。给小鼠口服山竹提取物，并对血样进行筛选，以检测与PTP1B相互作用的氧杂蒽酮的存在。通过超高效液相色谱-四极杆飞行时间质谱（UF-HPLC-QTOF-MS）鉴定出六种此类化合物（1-6），并通过活性测定证实了它们对PTP1B的抑制作用。其中，藤黄酮E（5）被发现是最有效的PTP1B抑制剂（IC = 0.43 μM）。组织分布分析表明，这六种化合物分布于肝脏、肌肉、脂肪、胃、大肠、小肠、脑、肾、心脏、肺和脾脏等11种组织中。结果表明，山竹可能是具有高PTP1B抑制活性的天然化合物的一个有前景的来源。
