Linnaeus（天使之钟）果实中分离得到的桉叶烷型三萜的强效 -葡萄糖苷酶和 -分泌酶抑制作用。
Potent -Glucosidase and -Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Linnaeus (Angel's Trumpet) Fruits.
机构信息
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah, P.O. Box 42, Saudi Arabia.
Department of Chemistry, University of Swabi, Swabi-Anbar-, 23430 KPK, Pakistan.
出版信息
Biomed Res Int. 2020 Aug 25;2020:8530165. doi: 10.1155/2020/8530165. eCollection 2020.
This study deals with -glucosidase and -secretase inhibitory screening of extract/fractions and isolated daturaolone (), namely, 3-oxo-6--hydroxy--amyrin (daturaolone) from chloroform fraction of L. Among entire fractions, the chloroform soluble fraction showed excellent activity against -glucosidase with % inhibition 90.8 with IC160.2 ± 1.85 g and daturaolone () with 98.7% inhibition with IC840.4 ± 1.74 M, respectively. Similarly, extract and daturaolone () also exhibited significant activity against the -secretase enzyme (BACE1) with % activities 88.27 and 95.19 and with IC values 304.21 ± 2.98 g and 260.70 ± 1.87 M, respectively, as compared to the standard inhibitor (Ans670, Sta671, Val672)-amyloid-/A4 precursor protein 770 fragments 662-675) with % activity 94.21 and IC value 289.24 ± 1.60 M. This finding encourages and opens a new window for further detail phytochemical investigation on . in order to isolate novel compounds with promising enzyme inhibitory potential.
本研究涉及-葡萄糖苷酶和-分泌酶抑制剂的筛选，从 L 的氯仿部分分离得到的提取物/馏分和分离得到的颠茄酮（），即 3-氧代-6--羟基--羽扇豆醇（颠茄酮）。在整个馏分中，氯仿可溶部分对-葡萄糖苷酶表现出极好的活性，抑制率为 90.8%，IC160.2±1.85μg；颠茄酮（）对-分泌酶（BACE1）的抑制活性分别为 98.7%，IC840.4±1.74μM。同样，提取物和颠茄酮（）对 - 分泌酶（BACE1）也表现出显著的活性，抑制率分别为 88.27%和 95.19%，IC 值分别为 304.21±2.98μg 和 260.70±1.87μM，而标准抑制剂（Ans670、Sta671、Val672）-淀粉样蛋白/A4 前体蛋白 770 片段 662-675 的抑制率为 94.21%，IC 值为 289.24±1.60μM。这一发现为进一步深入研究 提供了鼓励和新的契机，以分离具有潜在酶抑制活性的新型化合物。
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