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提取物及次生代谢产物对脂肪酸合酶、α-葡萄糖苷酶和黄嘌呤氧化酶的多靶点作用。

Multi-target action of extract and secondary metabolites against fatty acid synthase, α-glucosidase, and xanthine oxidase.

作者信息

Abdul-Rahman Azza M, Elwekeel Ahlam, Alruhaimi Reem S, Kamel Emadeldin M, Bin-Ammar Albandari, Mahmoud Ayman M, Moawad Abeer S, Zaki Mohamed A

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Beni-Suef University, 62514, Beni-Suef, Egypt.

Department of Biology, College of Science, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia.

出版信息

Saudi Pharm J. 2023 Oct;31(10):101762. doi: 10.1016/j.jsps.2023.101762. Epub 2023 Aug 25.

Abstract

is a traditional herbal medicine that showed beneficial health effects and bioactivities. Four compounds have been isolated from the plant leaves and were elucidated as lupeol, betulin, podocarpusflavone A, and amentoflavone. The inhibitory activities of extract and isolated metabolites against fatty acid synthase (FAS), α-glucosidase, and xanthine oxidase (XO) were investigated . The affinity of the compounds toward the studied enzymes was investigated . The plant extract inhibited FAS, α-glucosidase, and XO with IC values of 26.34, 67.88, and 33.05 µg/mL, respectively. Among the isolated metabolites, betulin exhibited the most inhibitory activity against α-glucosidase and XO with IC values of 38.96 and 30.94 µg/mL, respectively. Podocarpusflavone A and betulin were the most potent inhibitors of FAS with IC values of 24.08 and 27.96 µg/mL, respectively. Computational studies corroborated these results highlighting the interactions between metabolites and the enzymes. In conclusion, and its constituents possess the potential to modulate enzymes involved in metabolism and oxidative stress.

摘要

是一种具有有益健康作用和生物活性的传统草药。已从该植物叶子中分离出四种化合物,分别鉴定为羽扇豆醇、桦木醇、罗汉松黄酮A和穗花杉双黄酮。研究了该提取物和分离出的代谢产物对脂肪酸合酶(FAS)、α-葡萄糖苷酶和黄嘌呤氧化酶(XO)的抑制活性。研究了这些化合物对所研究酶的亲和力。该植物提取物对FAS、α-葡萄糖苷酶和XO的抑制常数(IC)值分别为26.34、67.88和33.05μg/mL。在分离出的代谢产物中,桦木醇对α-葡萄糖苷酶和XO表现出最强的抑制活性,其IC值分别为38.96和30.94μg/mL。罗汉松黄酮A和桦木醇是FAS最有效的抑制剂,其IC值分别为24.08和27.96μg/mL。计算研究证实了这些结果,突出了代谢产物与酶之间的相互作用。总之,该草药及其成分具有调节参与代谢和氧化应激的酶的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/683a/10494472/efbc612b316a/gr1.jpg

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