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从 C.H. Wright(紫葳科)果实中化合物的胆碱酯酶、α-葡萄糖苷酶、酪氨酸酶和脲酶抑制活性。

Cholinesterase, α-glucosidase, tyrosinase and urease inhibitory activities of compounds from fruits of C.H. Wright (Violaceae).

机构信息

Department of Organic Chemistry, Faculty of Science, The University of Yaounde I, Yaounde, Cameroon.

Department of Chemical Engineering, School of Chemical Engineering and Mineral Industries, University of Ngaoundere, Ngaoundere, Cameroon.

出版信息

Nat Prod Res. 2023 Nov-Dec;37(24):4169-4180. doi: 10.1080/14786419.2023.2176491. Epub 2023 Feb 9.

DOI:10.1080/14786419.2023.2176491
PMID:36757210
Abstract

From fruits, 3-Nor-4β-friedelan-24-ol () and 3-decyl-6,7,8-trimethoxy-2H,5H-furo[4,3,2-de]isochromene-2,5-dione (), new derivatives alongside, 28-hydroxyfriedelan-3-one (), friedelin (), 3,3',4,4',5'-pentamethylcoruleoellagic acid (), hexamethylcoruleoellagic acid (), 3',4,4',5,5'-pentamethylcoruleoellagic acid (), and fatty compounds were isolated and characterized using HRESIMS, EIMS, 1D and 2D NMR. enzyme inhibition of compounds and were evaluated on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glucosidase, urease and tyrosinase. Against AChE and BChE, the phenolic compounds and had good activity probably due to the phenolic nature and methoxy substituents. Compounds and exhibited good α-glucosidase inhibition especially compound whose IC = 42.45 ± 0.46 µg/mL was close that of acarbose (IC = 20.52 ± 0.84 µg/mL) standard drug. Urease and tyrosinase were appreciably inhibited by the compounds. Overall results of enzyme inhibitory assays indicate fruits and its constituents as potential remedy for enzymatic disorders.

摘要

从果实中分离得到了 3-Nor-4β-friedelan-24-ol()和 3-癸基-6,7,8-三甲氧基-2H,5H-furo[4,3,2-de]isochromene-2,5-二酮(),以及一些新的衍生物,如 28-羟基friedelan-3-one()、friedelin()、3,3',4,4',5'-五甲基鞣花酸()、hexamethylcoruleoellagic acid()、3',4,4',5,5'-五甲基鞣花酸()和脂肪酸化合物。利用 HRESIMS、EIMS、1D 和 2D NMR 对这些化合物进行了分离和表征。对化合物和进行了乙酰胆碱酯酶(AChE)、丁酰胆碱酯酶(BChE)、α-葡萄糖苷酶、脲酶和酪氨酸酶的抑制活性评价。对于 AChE 和 BChE,酚类化合物和具有较好的活性,这可能是由于其酚类性质和甲氧基取代基。化合物和对 α-葡萄糖苷酶具有较好的抑制活性,特别是化合物的 IC = 42.45 ± 0.46 μM,接近于阿卡波糖(IC = 20.52 ± 0.84 μM)的标准药物。化合物对脲酶和酪氨酸酶也有明显的抑制作用。酶抑制试验的总体结果表明,果实及其成分可能是治疗酶失调的潜在药物。

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