Structure-activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity

Teh Soek Sin; Ee Gwendoline Cheng Lian; Mah Siau Hui; Ahmad Zuraini

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Structure-activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity

机译：墨索亚墨鱼，花墨索亚花和充血墨索亚次生代谢产物抗胆碱酯酶活性的构效关系研究

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Our search for potential anti-acetylcholinesterase (AChE) inhibitors for treatment of Alzheimer's disease has led to the discovery of two bioactive compounds, alpha-mangostin (11) and congestiflorone acetate (13). This discovery was achieved from a preliminary screening of the anti-AChE activity on the extracts of three Mesua species namely M. ferrea, M. beccariana and M. congestiflora using Ellman's method. The pure metabolites, 1-12 which were isolated from the Mesua species, along with a synthetic derivative, compound 13 were then evaluated for their activities in order to identify the compounds that correspond to the enzyme inhibitory activities. Compounds 11 and 13 were found to give significant anti-AChE activities with IC50 values of 17.51 and 20.25 A mu M.

机译：我们寻找用于治疗阿尔茨海默氏病的潜在抗乙酰胆碱酯酶（AChE）抑制剂的结果导致发现了两种生物活性化合物，α-Mangostin（11）和乙酸充填酮（13）。该发现是通过使用Ellman方法初步筛选了三种Mesua物种（M. ferrea，M。beccariana和M. congestiflora）提取物的抗AChE活性而实现的。然后，从梅苏亚物种中分离出的纯代谢产物1-12与合成衍生物化合物13的活性进行了评估，以鉴定出与酶抑制活性相对应的化合物。发现化合物11和13具有明显的抗AChE活性，IC50值为17.51和20.25 AμM。

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《Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents》 |2016年第5期|共5页
作者
Teh Soek Sin; Ee Gwendoline Cheng Lian; Mah Siau Hui; Ahmad Zuraini;
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正文语种 eng
中图分类药学;
关键词
Anti-acetylcholinesterase; Mesua ferrea; Mesua beccariana; Mesua congestiflora; alpha-mangostin; Congestiflorone acetate;

机译：抗乙酰胆碱酯酶;Fers墨苏阿;bescaria mesua;充血Mesua充血;α-芒果;充血醋酸琼脂;

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1. Structure-activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity [J] . Teh Soek Sin, Ee Gwendoline Cheng Lian, Mah Siau Hui, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2016,第5期

机译：墨索亚墨鱼，花墨索亚花和充血墨索亚次生代谢产物抗胆碱酯酶活性的构效关系研究
2. Cytotoxicity and Structure-Activity Relationships of Xanthone Derivatives from Mesua beccariana, Mesua ferrea and Mesua congestiflora towards Nine Human Cancer Cell Lines [J] . Molecules . 2013,第2期

机译：墨克苏墨鱼，铁豆墨鱼和洋生花墨鱼的X吨酮衍生物对九种人类癌细胞系的细胞毒性和结构活性关系
3. In Vitro Cytotoxic, Antioxidant, and Antimicrobial Activities of Mesua beccariana (BailL) Knstenn., Mesua ferrea Linn., and Mesua congestiflora Extracts [J] . Soek Sin Teh, Gwendoline Cheng Lian Ee, Siau Hui Mah, BioMed research international . 2013,第Pta20期

机译：墨克苏木（BailL）Knstenn。，铁杉木薯和红花木薯的体外细胞毒性，抗氧化和抗菌活性
4. Development of Microwave System for Extraction of Essential Oils from Mesua ferrea L. leaves and Jasminum sambac flowers [C] . Rudy Nurdin, Nurshahidah Osman, Kaida Khalid, International RF and Microwave Conference . 2006

机译：MESUA Ferrea L.叶片和Jasminum Sambac Flowers提取微波系统的微波系统
5. A structure-activity approach to drug action in pharmacology: (A) Structure-activity relationships involved in DT-diaphorase (NQO1) mediated reduction kinetics and mode of action of anticancer bioreductive benzoquinone alkylating agents. (B) Structural characteristics of novel NMDA receptor antagonists required for renal tubule organic cation secretion . [D] . Fourie, Jeanne. 2004

机译：一种在药理学中用于药物作用的结构活性方法：（A）DT-黄递酶（NQO1）介导的抗癌生物还原苯醌烷基化剂的还原动力学和作用方式的结构活性关系。（B）肾小管有机阳离子分泌所需的新型NMDA受体拮抗剂的结构特征。
6. Cytotoxicity and Structure-Activity Relationships of Xanthone Derivatives from Mesua beccariana Mesua ferrea and Mesua congestiflora towards Nine Human Cancer Cell Lines [O] . Soek Sin Teh, Gwendoline Cheng Lian Ee, Siau Hui Mah, 2013

机译：墨克索墨鱼铁豆墨鱼和花粉墨鱼的X吨酮衍生物对9种人类癌细胞系的细胞毒性和结构活性关系
7. Cytotoxicity and Structure-Activity Relationships of Xanthone Derivatives from Mesua beccariana, Mesua ferrea and Mesua congestiflora towards Nine Human Cancer Cell Lines [O] . Zuraini Ahmad, Yang Mooi Lim, Gwendoline Cheng Lian Ee, 2013

机译：墨克索墨鱼，铁豆墨鱼和红花墨鱼的X吨酮衍生物对九种人类癌细胞系的细胞毒性和构效关系

Structure-activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity

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