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粉防己碱衍生物作为有前景的抗菌剂。

Tetrandrine Derivatives as Promising Antibacterial Agents.

作者信息

Calvillo-Páez Viviana I, Plascencia-Jatomea Maribel, Ochoa-Terán Adrián, Del-Toro-Sánchez Carmen L, González-Vega Ricardo I, González-Martínez Sandra M, Ochoa Lara Karen

机构信息

Centro de Graduados e Investigación en Química, Tecnológico Nacional de México, Campus Tijuana, CP 22444 Tijuana, B.C., México.

Departamento de Investigación y Posgrado en Alimentos, Universidad de Sonora, Rosales y Encinas s/n, Col. Centro, CP 83000 Hermosillo, Sonora, México.

出版信息

ACS Omega. 2023 Jul 26;8(31):28156-28164. doi: 10.1021/acsomega.3c01368. eCollection 2023 Aug 8.

DOI:10.1021/acsomega.3c01368
PMID:37576675
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10413380/
Abstract

This work reports on the antibacterial activity of two tetrandrine derivatives, with acridine () and anthracene () units, against Gram-positive and Gram-negative bacteria of clinical importance by the broth microdilution method as well as their antioxidant activity against ABTS and DPPH radicals. Unlike natural tetrandrine, its derivatives inhibited bacterial growth, showing selectivity against with notable activity of (MIC = 0.035 μg/mL); this compound also has good activity against the ABTS radical (IC = 4.59 μg/mL). Cell membrane integrity studies and reactive oxygen species (ROS) detection by fluorescent stains helped to understand possible mechanisms related to antibacterial activity, while electrophoretic mobility assays showed that the derivatives can bind to bacterial DNA plasmid. The results indicate that can induce a general state of oxidative stress in and , while induces an oxidative response in . Complementary electrochemical studies were included.

摘要

这项工作报道了两种具有吖啶()和蒽()单元的粉防己碱衍生物通过肉汤微量稀释法对具有临床重要性的革兰氏阳性菌和革兰氏阴性菌的抗菌活性,以及它们对ABTS和DPPH自由基的抗氧化活性。与天然粉防己碱不同,其衍生物抑制细菌生长,对显示出选择性,具有显著活性(MIC = 0.035μg/mL);该化合物对ABTS自由基也具有良好活性(IC = 4.59μg/mL)。通过荧光染色进行的细胞膜完整性研究和活性氧(ROS)检测有助于了解与抗菌活性相关的可能机制,而电泳迁移率测定表明这些衍生物可以与细菌DNA质粒结合。结果表明,可在和中诱导氧化应激的一般状态,而在中诱导氧化反应。还包括补充性的电化学研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/49c5cebd65c7/ao3c01368_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/7c45a3d7cac3/ao3c01368_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/ec36df9b1102/ao3c01368_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/ea6130656b45/ao3c01368_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/49c5cebd65c7/ao3c01368_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/7c45a3d7cac3/ao3c01368_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/ec36df9b1102/ao3c01368_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/ea6130656b45/ao3c01368_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c6e/10413380/49c5cebd65c7/ao3c01368_0004.jpg

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