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对印度尼西亚可食用植物进行生物活性成分筛选,并从印度尼西亚多花蒲桃叶片中发现一种新型蛋白酪氨酸磷酸酶1B抑制性酰基苯衍生物。

Screening of Indonesian Edible Plants for Bioactive Constituents and a New Protein Tyrosine Phosphatase 1B Inhibitory Acylbenzene Derivative from Leaves of Indonesian Syzygium polyanthum.

作者信息

Kapojos Magie Melanie, Abdjul Delfly Booby, Yamazaki Hiroyuki, Yagi Akiho, Uchida Ryuji

机构信息

Faculty of Nursing, University of Pembangunan Indonesia.

Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University.

出版信息

Chem Pharm Bull (Tokyo). 2020;68(9):903-906. doi: 10.1248/cpb.c20-00457.

DOI:10.1248/cpb.c20-00457
PMID:32879232
Abstract

Bioassay screening using Indonesian plants, such as traditional foods (vegetables, spices, and tea) and folk medicinal herbs, identified eight protein tyrosine phosphatase (PTP) 1B inhibitory and two antibacterial plants. The leaves of Syzygium polyanthum (Wight) Walp. were examined in more detail to define PTP1B inhibitory components, resulting in the isolation of a new active acylbenzene (1) along with four related congeners of 1 (2-5) and four oleanane triterpenes (6-9). The structure of 1 was elucidated as 12-oxo-12-(2,3,5-trihydroxy-4-methylphenyl)dodecanoic acid based on its spectroscopic data. The acylbenzenes 1 and 3-5 inhibited PTP1B activity with IC values ranging between 9.5 and 14 µM, whereas the triterpenes 7-9 also suppressed this activity with IC values of 3.3-5.7 µM.

摘要

利用印度尼西亚的植物进行生物测定筛选,如传统食物(蔬菜、香料和茶)以及民间草药,鉴定出了8种蛋白酪氨酸磷酸酶(PTP)1B抑制剂植物和2种抗菌植物。对多花蒲桃(Syzygium polyanthum (Wight) Walp.)的叶子进行了更详细的研究,以确定PTP1B抑制成分,结果分离出一种新的活性酰基苯(1)以及1的四种相关同系物(2 - 5)和四种齐墩果烷三萜(6 - 9)。根据其光谱数据,1的结构被确认为12 - 氧代 - 12 -(2,3,5 - 三羟基 - 4 - 甲基苯基)十二烷酸。酰基苯1和3 - 5抑制PTP1B活性,IC值在9.5至14 μM之间,而三萜7 - 9也抑制该活性,IC值为3.3 - 5.7 μM。

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