关键词: honokiol inhibition mechanism inhibitor nature product α-glucosidase

来  源:   DOI:10.3389/fphar.2024.1425832   PDF(Pubmed)

Abstract:
Honokiol, a naturally occurring compound from Magnolia obovata Thunb., has many biological activities, but its anti-α-glucosidase activity is still unclear. Therefore, we determined its inhibitory effects against α-glucosidase. Activity assays showed that honokiol was a reversible mixed-type inhibitor of α-glucosidase, and its IC50 value was 317.11 ± 12.86 μM. Fluorescence results indicated that the binding of honokiol to α-glucosidase caused a reduction in α-glucosidase activity. 3D fluorescence and CD spectra results indicated that the binding of honokiol to α-glucosidase caused conformational change in α-glucosidase. Docking simulated the detailed interactions between honokiol and α-glucosidase, including hydrogen and hydrophobic bonds. All findings showed that honokiol could be used as a natural inhibitor to develop α-glucosidase agents.
摘要:
和厚朴酚,一种来自白玉兰的天然化合物。,有许多生物活性,但其抗α-葡萄糖苷酶活性尚不清楚。因此,我们确定了其对α-葡萄糖苷酶的抑制作用。活性测定表明和厚朴酚是α-葡萄糖苷酶的可逆混合型抑制剂,IC50值为317.11±12.86μM。荧光结果表明和厚朴酚与α-葡萄糖苷酶的结合导致α-葡萄糖苷酶活性降低。3D荧光和CD光谱结果表明,和厚朴酚与α-葡萄糖苷酶的结合引起了α-葡萄糖苷酶的构象变化。对接模拟了和厚朴酚与α-葡萄糖苷酶之间的详细相互作用,包括氢键和疏水键。所有发现表明和厚朴酚可以作为天然抑制剂来开发α-葡萄糖苷酶试剂。
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