Institute of Natural Medicine, University of Toyama, Toyama, Japan.
J Nat Med. 2013 Apr;67(2):264-70. doi: 10.1007/s11418-012-0674-7. Epub 2012 May 30.
We screened water and methanol extracts of 28 Indonesian medicinal plants for their protein tyrosine phosphatase 1B (PTP1B) inhibitory activities. Nine water extracts, i.e., Alstonia scholaris leaf, Blumea balsamifera, Cinnamomum burmannii, Cymbopogon nardus, Melaleuca leucadendra, Phyllanthus niruri, Piper nigrum, Syzygium aromaticum, and Sy. polyanthum, exhibited ≥70 % inhibition at 25 μg/mL, whereas 11 methanol extracts, i.e., Als. scholaris, Andrographis paniculata, B. balsamifera, Ci. burmannii, Curcuma heyneana, Glycyrrhiza glabra, M. leucadendra, Punica granatum, Rheum palmatum, Sy. polyanthum, and Z. aromaticum, exhibited ≥70 % inhibition at 25 μg/mL. Water extracts of B. balsamifera (IC50, 2.26 μg/mL) and M. leucadendra (IC50, 2.05 μg/mL), and methanol extracts of Ci. burmannii (IC50, 2.47 μg/mL), Pu. granatum (IC50, 2.40 μg/mL), and Sy. polyanthum (IC50, 1.03 μg/mL) exhibited strong inhibitory activity, which was comparable with that of the positive control, RK-682 (IC50, 2.05 μg/mL). The PTP1B inhibitory activity of the constituents of Ci. burmannii and Z. aromaticum was then evaluated. 5'-Hydroxy-5-hydroxymethyl-4″,5″-methylenedioxy-1,2,3,4-dibenzo-1,3,5-cycloheptatriene (2; IC50, 29.7 μM) and trans-cinnamaldehyde (5; IC50, 57.6 μM) were the active constituents of Ci. burmannii, while humulatrien-5-ol-8-one (21; IC50, 27.7 μM), kaempferol-3,4'-di-O-methyl ether (32; IC50, 17.5 μM), and (S)-6-gingerol (33; IC50, 28.1 μM) were those of Z. aromaticum. These results suggest that these medicinal plants may contribute to the treatment and/or prevention of type II diabetes and/or obesity through PTP1B inhibition.
我们筛选了 28 种印度尼西亚药用植物的水提物和甲醇提取物，以研究它们对蛋白酪氨酸磷酸酶 1B（PTP1B）的抑制活性。9 种水提取物，即醉茄叶、白花丹、肉桂、香茅草、千层塔、鸡骨草、黑胡椒、八角茴香和多花山姜，在 25μg/mL 时表现出≥70%的抑制活性，而 11 种甲醇提取物，即醉茄、穿心莲、白花丹、肉桂、莪术、甘草、千层塔、石榴、大黄、多花山姜和八角茴香，在 25μg/mL 时表现出≥70%的抑制活性。水提物中，白花丹（IC50，2.26μg/mL）和千层塔（IC50，2.05μg/mL），以及甲醇提取物中，肉桂（IC50，2.47μg/mL）、石榴（IC50，2.40μg/mL）和多花山姜（IC50，1.03μg/mL）的抑制活性较强，与阳性对照 RK-682（IC50，2.05μg/mL）相当。然后评估了肉桂和八角茴香成分对 PTP1B 的抑制活性。5'-羟基-5-羟甲基-4″,5″-亚甲二氧基-1,2,3,4-二苯并-1,3,5-环庚三烯（2；IC50，29.7μM）和反式肉桂醛（5；IC50，57.6μM）是肉桂的活性成分，而环羊毛甾烯-5-醇-8-酮（21；IC50，27.7μM）、山奈酚-3,4'-二甲醚（32；IC50，17.5μM）和（S）-6-姜辣素（33；IC50，28.1μM）是八角茴香的活性成分。这些结果表明，这些药用植物可能通过抑制 PTP1B 来治疗和/或预防 II 型糖尿病和/或肥胖症。
