Cholinesterase inhibitory triterpenoids from the bark of Garcinia hombroniana

被引:41
|
作者
Jamila, Nargis [1 ]
Khairuddean, Melati [1 ]
Yeong, Khaw Kooi [2 ]
Osman, Hasnah [1 ]
Murugaiyah, Vikneswaran [2 ]
机构
[1] Univ Sains Malaysia, Sch Chem Sci, George Town 11800, Malaysia
[2] Univ Sains Malaysia, Sch Pharmaceut Sci, George Town 11800, Malaysia
关键词
2 beta-hydroxy-3 alpha-O-caffeoyltaraxar-14-en-28-oic acid; acetylcholinesterase; butyrylcholinesterase; molecular docking; triterpenoids; ALZHEIMERS-DISEASE; ACETYLCHOLINESTERASE; CONSTITUENTS; ANTIOXIDANT; FRIEDOLANOSTANES; XANTHONES; EXTRACT; TWIGS; ANTICHOLINESTERASE; BENZOPHENONES;
D O I
10.3109/14756366.2014.895720
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Context: Garcinia hombroniana Pierre, known as manggis hutan in Malaysia is a rich source of xanthones and benzophenones. Objectives: This study was aimed to isolate and characterize potential cholinesterase inhibitors from the extracts of G. hombroniana bark and investigate their interactions with the enzymes. Materials and methods: The dichloromethane extract afforded five triterpenoids which were characterized by NMR and mass spectral techniques. Cholinesterase inhibitory assay and molecular docking were performed to get insight of the inhibitory activity and molecular interactions of the compounds. The compounds were also tested for their antioxidant capacity. Results: The isolated triterpenoids were identified as: 2 beta-hydroxy-3 alpha-O-caffeoyltaraxar-14-en-28-oic acid (1), taraxerol (2), taraxerone (3), betulin (4) and betulinic acid (5). Compound 1 was the most active dual inhibitor of both AChE and BChE. Compound 1 also showed good antioxidant activities. Conclusion: Compound 1 had dual and moderate inhibitory activity on AChE and BChE worthy for further investigations.
引用
收藏
页码:133 / 139
页数:7
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