锦葵根中的抗菌、抗脲酶和抗增殖abru醌类

Pub Date : 2022-05-04 DOI:10.1080/22311866.2022.2069154
E. Okoro, M. S. Ahmad, Rukesh Maharjan, Majid Khan, Z. A. Sherwani, Zaheer Ul-Haq, Samuel E. Ugheighele, O. Erukainure, O. Osoniyi, F. Onajobi, M. Iqbal Choudhary
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引用次数: 1

摘要

摘要:通过对豆科植物Abrus precatorius Linn甲醇可溶性组分的植物化学研究,分离得到4个abruquinones (abruquinones M、A、E和B),并利用1D、2D NMR和HRESI-MS对化合物结构进行了鉴定。结果表明,腐竹提取物的抗菌和抗脲酶活性显著(p < 0.05)。进一步的治疗性评价表明,abruquinones M、A、E和B通过诱导多药耐药金黄色葡萄球菌(MIC值为20 ~ 30 μg/mL)(µM)的形态损伤并伴随膜分割,显著抑制其生长(p < 0.05),显示出抗菌活性。Abruquinones A和B表现出显著(p < 0.05)的脲酶抑制活性(IC50值分别为35.2和37.7 μM),通过π-正值相互作用与脲酶活性位点侧链紧密结合,对AU565和MDA-MB231乳腺癌细胞具有细胞毒性(IC50值分别为23.13和9.05 μM)。这些发现表明,从牛蒡根中提取的abruquinones(异黄酮)可能是抗菌、抗脲酶和抗癌药物开发的进一步机制研究的可行候选人。图形抽象
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Antibacteria, Antiurease, and Antiproliferative Abruquinones from Abrus precatorius Roots
Abstract Phytochemical studies of methanol soluble fractions of Abrus precatorius Linn (Fabaceae) led to the isolation of four abruquinones (abruquinones M, A, E, and B). Structures of the compounds were elucidated using spectroscopic analyses - 1D, 2D NMR, HRESI-MS. Evaluation of the therapeutic effects of A. precatorius fractions showed significant (p < 0.05) antibacterial and antiurease activities. Further therapeutic evaluation of the compounds showed that abruquinones M, A, E, and B demonstrated antibacterial activities by inhibiting significantly (p < 0.05) the growth of multidrug resistant S. aureus (MIC values ranged from 20 - 30 μg/mL) (µM) via induction of morphological damages with concomitant membrane segmentation. Abruquinones A and B showed significant (p < 0.05) urease inhibiting activity (IC50 values 35.2 and 37.7 µM, respectively), docked tightly to the side chains of urease enzyme active site via π-cation interactions, as well as showed cytotoxicity against AU565 and MDA-MB231 breast cancer cells (IC50 values 23.13 and 9.05 μM, respectively). These findings suggest abruquinones (isoflavanquinones) from A. precatorius roots as viable candidates for further mechanistic studies on possible antibacterial, antiurease, and anticancer drug development. GRAPHICAL ABSTRACT
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