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Interactions of Flavone and Steroid from A. subintegra as Potential Inhibitors for Porcine Pancreatic Lipase.
Current Computer-Aided Drug Design ( IF 1.7 ) Pub Date : 2020-11-30 , DOI: 10.2174/1573409915666191015112320
Mastura Ibrahim 1 , Saripah Salbiah Syed Abdul Azziz 1 , Chee Fah Wong 2 , Yuhanis Mhd Bakri 1 , Fauziah Abdullah 3
Affiliation  

Background: Obesity is one serious health condition that contributes to various chronic diseases. The inhibition of pancreatic lipase is a promising treatment for obesity.

Objective: The present study was designed to investigate anti-porcine pancreatic lipase effect of isolated compounds from Aquilaria subintegra and its mechanism.

Methods: Compounds were isolated with serial column chromatography and their structure were identified using spectroscopic methods. Isolated compounds were tested for anti-lipase potential activity using colorimetric assay. The prediction of energy binding between isolated compounds and enzyme was described using YASARA software.

Results: Four compounds were successfully isolated from the bark of A. subintegra, namely, 5- hydroxy-7,4’-dimethoxyflavone, luteolin-7,3’,4’-trimethyl ether, 5,3’-dihydroxy-7,4’-dimethoxyflavone and β-sitosterol. The results indicated that all compounds displayed promising pancreatic lipase inhibitory activity ranging between of 6% to 53% inhibition. Compound 5-hydroxy-7,4’- dimethoxyflavone was a competitive inhibitor and decreases the enzyme catalysis. Meanwhile, β- sitosterol was a non- competitive inhibitor since the latter was bind allosterically toward enzyme.

Conclusion: This finding is significant for further investigation of bioactive compounds from A. subintegra on animal study.



中文翻译:

来自 A. subintegra 的黄酮和类固醇作为猪胰腺脂肪酶的潜在抑制剂的相互作用。

背景:肥胖是一种严重的健康状况,会导致各种慢性疾病。胰脂肪酶的抑制是治疗肥胖症的一种有前途的治疗方法。

目的:本研究旨在探讨沉香分离物的抗猪胰脂肪酶作用及其机制。

方法:采用系列柱色谱法分离化合物,并采用光谱法对其结构进行鉴定。使用比色法测试分离的化合物的抗脂肪酶潜在活性。使用 YASARA 软件描述了分离化合物和酶之间能量结合的预测。

结果:从A. subintegra树皮中成功分离出4种化合物,即5-羟基-7,4'-二甲氧基黄酮、木犀草素-7,3',4'-三甲醚、5,3'-二羟基-7、 4'-二甲氧基黄酮和β-谷甾醇。结果表明,所有化合物都显示出有希望的胰脂肪酶抑制活性,抑制范围在 6% 至 53% 之间。化合物 5-羟基-7,4'-二甲氧基黄酮是一种竞争性抑制剂,可降低酶的催化作用。同时,β-谷甾醇是一种非竞争性抑制剂,因为后者与酶变构结合。

结论:这一发现对于在动物研究中进一步研究来自 A. subintegra 的生物活性化合物具有重要意义。

更新日期:2021-01-19
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