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肉桂酸衍生物作为潜在的基质金属蛋白酶-9抑制剂:分子对接和动力学模拟

Cinnamic acid derivatives as potential matrix metalloproteinase-9 inhibitors: molecular docking and dynamics simulations.

作者信息

Malekipour Mohammad Hossein, Shirani Farzaneh, Moradi Shadi, Taherkhani Amir

机构信息

Dental Students Research Center, School of Dentistry, Isfahan University of Medical Sciences, Isfahan 8174673461, Iran.

Dental Research Center, Dental Research Institute, Department of Operative Dentistry, School of Dentistry, Isfahan University of Medical Sciences, Isfahan 8174673461, Iran.

出版信息

Genomics Inform. 2023 Mar;21(1):e9. doi: 10.5808/gi.22077. Epub 2023 Mar 31.

Abstract

Matrix metalloproteinase-9 (MMP-9) is a zinc and calcium-dependent proteolytic enzyme involved in extracellular matrix degradation. Overexpression of MMP-9 has been confirmed in several disorders, including cancers, Alzheimer's disease, autoimmune diseases, cardiovascular diseases, and dental caries. Therefore, MMP-9 inhibition is recommended as a therapeutic strategy for combating various diseases. Cinnamic acid derivatives have shown therapeutic effects in different cancers, Alzheimer's disease, cardiovascular diseases, and dental caries. A computational drug discovery approach was performed to evaluate the binding affinity of selected cinnamic acid derivatives to the MMP-9 active site. The stability of docked poses for top-ranked compounds was also examined. Twelve herbal cinnamic acid derivatives were tested for possible MMP-9 inhibition using the AutoDock 4.0 tool. The stability of the docked poses for the most potent MMP-9 inhibitors was assessed by molecular dynamics (MD) in 10 nanosecond simulations. Interactions between the best MMP-9 inhibitors in this study and residues incorporated in the MMP-9 active site were studied before and after MD simulations. Cynarin, chlorogenic acid, and rosmarinic acid revealed a considerable binding affinity to the MMP-9 catalytic domain (ΔGbinding < -10 kcal/ mol). The inhibition constant value for cynarin and chlorogenic acid were calculated at the picomolar scale and assigned as the most potent MMP-9 inhibitor from the cinnamic acid derivatives. The root-mean-square deviations for cynarin and chlorogenic acid were below 2 Å in the 10 ns simulation. Cynarin, chlorogenic acid, and rosmarinic acid might be considered drug candidates for MMP-9 inhibition.

摘要

基质金属蛋白酶-9(MMP-9)是一种锌和钙依赖性蛋白水解酶,参与细胞外基质的降解。MMP-9的过表达已在多种疾病中得到证实,包括癌症、阿尔茨海默病、自身免疫性疾病、心血管疾病和龋齿。因此,推荐抑制MMP-9作为对抗各种疾病的治疗策略。肉桂酸衍生物已在不同的癌症、阿尔茨海默病、心血管疾病和龋齿中显示出治疗效果。采用计算机辅助药物发现方法评估所选肉桂酸衍生物与MMP-9活性位点的结合亲和力。还检查了排名靠前的化合物对接构象的稳定性。使用AutoDock 4.0工具测试了12种草药肉桂酸衍生物对MMP-9的抑制可能性。通过10纳秒模拟中的分子动力学(MD)评估了最有效的MMP-9抑制剂对接构象的稳定性。在MD模拟前后,研究了本研究中最佳MMP-9抑制剂与MMP-9活性位点中所含残基之间的相互作用。绿原酸、咖啡酸和迷迭香酸对MMP-9催化结构域显示出相当大的结合亲和力(ΔG结合<-10千卡/摩尔)。绿原酸和咖啡酸的抑制常数值在皮摩尔范围内计算,并被指定为肉桂酸衍生物中最有效的MMP-9抑制剂。在10纳秒模拟中,绿原酸和咖啡酸的均方根偏差低于2埃。绿原酸、咖啡酸和迷迭香酸可能被视为抑制MMP-9的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c85b/10085732/070ffecf707d/gi-22077f1.jpg

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