Development of inhibitors against lipase and α-glucosidase from derivatives of monascus pigment
Development of inhibitors against lipase and α-glucosidase from derivatives of monascus pigment
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DOI：
10.1111/j.1574-6968.2007.00917.x
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发表时间：
2007-11-01
影响因子：
2.1
通讯作者：
Shin, Chul Soo
中科院分区：
文献类型：
--
作者：
Kim, Jong Hoon;Kim, Hyun Jung;Shin, Chul Soo
通过添加非天然氨基酸，在红曲发酵过程中产生了新的红曲色素衍生物，并测试了衍生物对饮食相关脂肪酶和α-葡萄糖苷酶的抑制活性。青霉胺 (H-Pen)、环己基丙氨酸 (H-Cha)、丁基甘氨酸 (L-t-Bg) 和正亮氨酸 (H-Nle) 的衍生物对脂肪酶表现出相对较高的抑制活性。 H-Pen衍生物表现出最高的抑制活性，IC50（50％抑制）值为24.0μM。四种衍生物均表现出对脂肪酶的非竞争性抑制模式。 H-Pen衍生物的抑制常数(K-i)估计为20.7μM。H-Pen衍生物还表现出相对较高的α-葡萄糖苷酶抑制活性，IC50值为50.9μM。H-Pen衍生物对α-葡萄糖苷酶的抑制模式似乎是混合型的。抑制常数K-i和K-i'估计分别为25.9和98.9μM。
New derivatives of monascus pigment were produced during Monascus fermentation by the addition of unnatural amino acids, and the inhibitory activities of the derivatives against diet-related lipase and alpha-glucosidase were tested. Derivatives with penicillamine (H-Pen), cyclohexylalanine (H-Cha), butylglycine (L-t-Bg), and norleucine (H-Nle) showed relatively high inhibitory activities against lipase. The H-Pen derivative exhibited the highest inhibitory activity, with an IC50 (50% inhibition) value of 24.0 mu M. The four derivatives all showed noncompetitive inhibition patterns against lipase. The inhibition constant (K-i) of the H-Pen derivative was estimated to be 20.7 mu M. The H-Pen derivative also exhibited a relatively high inhibitory activity against alpha-glucosidase, with an IC50 value of 50.9 mu M. The inhibition pattern of the H-Pen derivative against alpha-glucosidase appeared to be of a mixed type. The inhibition constants K-i and K-i' were estimated to be 25.9, and 98.9 mu M, respectively.