Wu Shufen, Dong Changyan, Zhang Meihui, Cheng Yi, Cao Xiaobo, Yang Benxu, Li Chao, Peng Xin
State Key Laboratory of Food Nutrition and Safety, College of Food Science and Engineering, Tianjin University of Science and Technology, Tianjin 300457, China.
Tianjin Lida Food Technology Co., Ltd., Tianjin 300393, China.
Foods. 2024 May 17;13(10):1573. doi: 10.3390/foods13101573.
Red yeast rice dietary supplements have been proven to ameliorate hyperglycemia, but the mechanism was unclear. In this work, ankaflavin (AK) and monascin (MS), as typical pigments derived from red yeast rice, were found to exert noteworthy inhibitory ability against α-glucosidase, with an IC of 126.5 ± 2.5 and 302.6 ± 2.5 μM, respectively, compared with acarbose (IC = 341.3 ± 13.6 μM). They also exhibited mixed-type inhibition of α-glucosidase in vitro and caused fluorescence quenching through the static-quenching process. Molecular-docking studies indicated that AK and MS bind to amino acid residues outside the catalytic center, which induces structural changes in the enzyme, thus influencing its catalytic activity. The anti-glycation ability of -fermented products was evaluated, and they exhibited a high inhibition rate of 87.1% in fluorescent advanced glycation end-product formation at a concentration of 0.2 mg mL, while aminoguanidine showed a rate of 75.7% at the same concentration. These results will be significant in broadening the application scope of pigments, especially AK and MS, in treating type 2 diabetes.
红曲米膳食补充剂已被证明可改善高血糖，但机制尚不清楚。在这项研究中，发现红曲米中的典型色素安卡黄素（AK）和红曲素（MS）对α-葡萄糖苷酶具有显著的抑制能力，其IC50分别为126.5±2.5和302.6±2.5μM，而阿卡波糖的IC50为341.3±13.6μM。它们在体外对α-葡萄糖苷酶还表现出混合型抑制作用，并通过静态猝灭过程导致荧光猝灭。分子对接研究表明，AK和MS与催化中心外的氨基酸残基结合，从而诱导酶的结构变化，进而影响其催化活性。对发酵产物的抗糖基化能力进行了评估，在浓度为0.2mg/mL时，它们对荧光晚期糖基化终产物形成的抑制率高达87.1%，而在相同浓度下氨基胍的抑制率为75.7%。这些结果对于拓宽色素尤其是AK和MS在治疗2型糖尿病方面的应用范围具有重要意义。
