Department of Agro-environmental Sciences, Faculty of Agriculture, Kyushu University, Fukuoka 812-8581, Japan.
Phytomedicine. 2011 Sep 15;18(12):1053-5. doi: 10.1016/j.phymed.2011.03.011. Epub 2011 May 18.
α-Glucosidase inhibitor has considerable potential as a diabetes mellitus type 2 drug because it prevents the digestion of carbohydrates. The search for the constituents reducing α-glucosidase activity led to the finding of active compounds in the fruiting body of Ganoderma lucidum. The CHCl(3) extract of the fruiting body of G. lucidum was found to show inhibitory activity on α-glucosidase in vitro. The neutral fraction, with an IC(50) of 88.7 μg/ml, had stronger inhibition than a positive control, acarbose, with an IC(50) of 336.7 μg/ml (521.5 μM). The neutral fraction was subjected to silica gel column chromatography and repeated p-HPLC to provide an active compound, (3β,24E)-lanosta-7,9(11),24-trien-3,26-diol (ganoderol B). It was found to have high α-glucosidase inhibition, with an IC(50) of 48.5 μg/ml (119.8 μM).
α-葡萄糖苷酶抑制剂作为 2 型糖尿病药物具有很大的潜力，因为它可以阻止碳水化合物的消化。寻找降低 α-葡萄糖苷酶活性的成分导致在灵芝的子实体中发现了具有活性的化合物。灵芝子实体的 CHCl(3)提取物在体外显示出对 α-葡萄糖苷酶的抑制活性。中性部分的 IC(50)为 88.7μg/ml，比阳性对照阿卡波糖（IC(50)为 336.7μg/ml，即 521.5μM）的抑制作用更强。中性部分经硅胶柱色谱和重复 p-HPLC 处理，得到一种活性化合物，（3β,24E）-羊毛甾烷-7,9(11),24-三烯-3,26-二醇（灵芝醇 B）。发现它对 α-葡萄糖苷酶具有很高的抑制活性，IC(50)为 48.5μg/ml（119.8μM）。
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