Structural Characterization and Bioactivity Evaluation of an Acidic Proteoglycan Extract from Ganoderma Lucidum Fruiting Bodies for PTP1B Inhibition and Anti-Diabetes
Structural Characterization and Bioactivity Evaluation of an Acidic Proteoglycan Extract from Ganoderma Lucidum Fruiting Bodies for PTP1B Inhibition and Anti-Diabetes
复制标题
灵芝子实体酸性蛋白多糖提取物抑制 PTP1B 和抗糖尿病的结构表征和生物活性评价
DOI：
10.1002/bip.22426
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发表时间：
2014-06-01
期刊：
影响因子：
2.9
通讯作者：
Zhou, Ping
中科院分区：
文献类型：
--
作者：
Pan, Deng;Wang, Linqiang;Zhou, Ping
对一种水溶性的PTP 1B抑制剂FYGL-a进行了结构分析和生物活性评价。FYGL-a是已报道的来自灵芝子实体的抗高血糖提取物的成分。组成分析表明FYGL-a是一个100.2 kDa的酸性蛋白多糖，由85 +/- 2%的杂多糖链组成，其中鼠李糖、半乳糖、葡萄糖和葡萄糖醛酸残基的摩尔比为1.0：3.7：3.9：2.0，并且FYGL-a的15 +/- 2%的蛋白部分通过苏氨酸残基以O-键型共价结合到多糖链上。通过高碘酸氧化、Smith降解、甲基化分析、H-1和C-13 1D NMR和2D NMR（HSQC、HMBC、NOESY、COSY和TOCSY）系统地表征了FYGL-a的完整序列。FYGL-a的化学结构确定如下，其可能在PTP 1B的竞争性抑制和降血糖作用中发挥特殊作用。
A water-soluble PTP1B inhibitor, named FYGL-a, was fractionated for structure investigation and bioactivity evaluation. FYGL-a is an ingredient of a reported antihyperglycemia extract from Ganoderma Lucidum fruiting bodies. Composition analysis indicated that FYGL-a was a 100.2 kDa acidic proteoglycan, consisting of 85 +/- 2% heteropolysaccharide chain with rhamnose, galactose, glucose, and glucuronic acid residues in a mole ratio of 1.0:3.7:3.9:2.0, and the 15 +/- 2% protein moiety of FYGL-a was covalently bonded to the polysaccharide chain in O-linkage type via threonine residues. The complete sequence of FYGL-a was characterized systematically by periodate oxidation, Smith degradation, methylation analysis, H-1 & C-13 1D NMR, and 2D NMR (HSQC, HMBC, NOESY, COSY, & TOCSY). The chemical structure of FYGL-a was determined as following, which may play special role in the competitive inhibition of PTP1B and antihyperglycemia potency.