Department of Biotechnology, Daegu University, Kyoungsan, Kyoungbook 712-714, Republic of Korea.
N Biotechnol. 2010 Sep 30;27(4):419-23. doi: 10.1016/j.nbt.2010.04.002. Epub 2010 Apr 10.
Microbial conversion of unsaturated fatty acids often leads to special changes in their product structures and in biological potential. In our continuous effort to screen natural products for their antimicrobial and enzyme inhibitor activities, we found that 10-hydroxy-8(E)-octadecenoic acid (HOD) exhibited strong anti-alpha-glucosidase (EC 3.2.1.20) activity. HOD is an intermediate in the bioconversion of oleic acid to 7,10-dihydroxy-8(E)-octadecenoic acid (DOD) by a bacterial isolate, Pseudomonas aeruginosa (PR3). Diabetes mellitus is the most serious, chronic metabolic disorder characterized by defect in insulin secretion and action, which can lead to damage blood vessels and nerves. We analyzed the inhibitory activity of HOD and the commercially available antidiabetic remedy, acarbose. We found that HOD exhibited a better inhibition (IC(50) 0.07+/-0.12) on alpha-glucosidase as compared to acarbose (IC(50) 0.42+/-0.1). HOD showed competitive inhibition against yeast alpha-glucosidase. Our study is the first report on anti-alpha-glucosidase activity of HOD and could be helpful to develop medicinal preparation or functional food for diabetes and related symptoms.
不饱和脂肪酸的微生物转化通常会导致其产物结构和生物潜力的特殊变化。在我们不断筛选具有抗菌和酶抑制剂活性的天然产物的过程中，我们发现 10-羟基-8(E)-十八烯酸 (HOD) 表现出很强的抗α-葡萄糖苷酶 (EC 3.2.1.20) 活性。HOD 是一种细菌分离株铜绿假单胞菌 (PR3) 将油酸生物转化为 7,10-二羟基-8(E)-十八烯酸 (DOD) 的中间产物。糖尿病是一种最严重的慢性代谢紊乱，其特征是胰岛素分泌和作用缺陷，可导致血管和神经损伤。我们分析了 HOD 和市售抗糖尿病药物阿卡波糖的抑制活性。我们发现 HOD 对α-葡萄糖苷酶的抑制作用（IC50 为 0.07+/-0.12）优于阿卡波糖（IC50 为 0.42+/-0.1）。HOD 对酵母α-葡萄糖苷酶表现出竞争性抑制作用。我们的研究首次报道了 HOD 的抗α-葡萄糖苷酶活性，这可能有助于开发用于糖尿病和相关症状的药物制剂或功能性食品。
