从多花山竹子叶中分离得到的蛋白酪氨酸磷酸酶 1B（PTP1B）抑制剂成分。

Protein tyrosine phosphatase 1B (PTP1B)-inhibiting constituents from the leaves of Syzygium polyanthum.

机构信息

Division of Natural Products Chemistry, Institute of Natural Medicine, University of Toyama, Toyama, Japan.

出版信息

Planta Med. 2012 Aug;78(12):1378-81. doi: 10.1055/s-0032-1315000. Epub 2012 Jul 4.

Abstract

A methanol extract of the leaves of Syzygium polyanthum (Wight) Walp. afforded four new acylbenzene derivatives (1-4) together with seven known compounds (5-11). The structures of 1-11 were elucidated by extensive spectroscopic methods and comparison with the literature data. The new compounds 1-3 and a known compound, campest-4-en-3-one (10), exhibited a significant protein tyrosine phosphatase 1B inhibitory activity with IC₅₀ values of 13.1 ± 0.1, 5.77 ± 0.15, 4.01 ± 0.26, and 10.4 ± 0.5 µM, respectively. The inhibitory potency of the new compounds 2 and 3 was comparable to that of a positive control RK-682 (IC₅₀, 5.51 ± 0.04 µM).

摘要

从 Syzygium polyanthum (Wight) Walp. 的叶子甲醇提取物中分离得到四个新的酰基苯衍生物（1-4）以及七个已知化合物（5-11）。通过广泛的光谱方法和与文献数据的比较，确定了 1-11 的结构。新化合物 1-3 和一个已知化合物，菜油甾-4-烯-3-酮（10），表现出显著的蛋白酪氨酸磷酸酶 1B 抑制活性，其 IC₅₀ 值分别为 13.1 ± 0.1、5.77 ± 0.15、4.01 ± 0.26 和 10.4 ± 0.5 µM。新化合物 2 和 3 的抑制活性与阳性对照 RK-682（IC₅₀，5.51 ± 0.04 µM）相当。