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伊拉克种植的芸香科植物中的抗耐甲氧西林金黄色葡萄球菌成分,以及两种最具活性的化合物查勒平辛和6-羟基芦丁3',7-二甲醚的研究。

Anti-MRSA Constituents from (Rutaceae) Grown in Iraq, and Studies on Two of Most Active Compounds, Chalepensin and 6-Hydroxy-rutin 3',7-Dimethyl ether.

作者信息

Al-Majmaie Shaymaa, Nahar Lutfun, Rahman M Mukhlesur, Nath Sushmita, Saha Priyanka, Talukdar Anupam Das, Sharples George P, Sarker Satyajit D

机构信息

Centre for Natural Products Discovery, School of Pharmacy and Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, Liverpool L3 3AF, UK.

Laboratory of Growth Regulators, Institute of Experimental Botany ASCR & Palacký University, Šlechtitelů 27, 78371 Olomouc, Czech Republic.

出版信息

Molecules. 2021 Feb 19;26(4):1114. doi: 10.3390/molecules26041114.

Abstract

L. (Rutaceae), a perennial herb with wild and cultivated habitats, is well known for its traditional uses as an anti-inflammatory, analgesic, antipyretic agent, and in the treatment of rheumatism, nerve diseases, neuralgia, dropsy, convulsions and mental disorders. The antimicrobial activities of the crude extracts from the fruits, leaves, stem and roots of were initially evaluated against two Gram-positive and two Gram-negative bacterial strains and a strain of the fungus . Phytochemical investigation afforded 19 compounds, including alkaloids, coumarins, flavonoid glycosides, a cinnamic acid derivative and a long-chain alkane. These compounds were tested against a panel of methicillin-resistant (MRSA) strains, i.e., ATCC 25923, SA-1199B, XU212, MRSA-274819 and EMRSA-15. The MIC values of the active compounds, chalepin (), chalepensin (), rutamarin (), rutin 3'-methyl ether (), rutin 7,4'-dimethyl ether (), 6-hydroxy-rutin 3',7-dimethyl ether () and arborinine () were in the range of 32-128 µg/mL against the tested MRSA strains. Compounds and were the most active compounds from , and were active against four out of six tested MRSA strains, and studies were performed on these compounds. The anti-MRSA activity of compound was comparable to that of the positive control norfloxacin (MICs 32 vs 16 μg/mL, respectively) against the MRSA strain XU212, which is a Kuwaiti hospital isolate that possesses the TetK tetracycline efflux pump. This is the first report on the anti-MRSA property of compounds isolated from and relevant studies on the most active compounds.

摘要

L.(芸香科)是一种多年生草本植物,有野生和人工栽培两种生长环境,因其传统上用作抗炎、止痛、退热剂以及用于治疗风湿病、神经疾病、神经痛、水肿、惊厥和精神障碍而闻名。最初评估了从其果实、叶子、茎和根中提取的粗提物对两种革兰氏阳性菌、两种革兰氏阴性菌菌株以及一种真菌菌株的抗菌活性。植物化学研究得到了19种化合物,包括生物碱、香豆素、黄酮苷、一种肉桂酸衍生物和一种长链烷烃。对这些化合物针对一组耐甲氧西林金黄色葡萄球菌(MRSA)菌株进行了测试,即ATCC 25923、SA - 1199B、XU212、MRSA - 274819和EMRSA - 15。活性化合物chalepin()、chalepensin()、rutamarin()、芦丁3'-甲醚()、芦丁7,4'-二甲醚()、6 - 羟基芦丁3',7 - 二甲醚()和arborinine()对测试的MRSA菌株的最低抑菌浓度(MIC)值在32 - 128μg/mL范围内。化合物和是中最具活性的化合物,对六种测试的MRSA菌株中的四种有活性,并对这些化合物进行了研究。化合物对MRSA菌株XU212的抗MRSA活性与阳性对照诺氟沙星相当(MIC分别为32μg/mL和16μg/mL),XU212是科威特一家医院分离出的具有TetK四环素外排泵的菌株。这是关于从分离出的化合物的抗MRSA特性以及对最具活性化合物的相关研究的首次报道。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c867/7923287/a10ea82026de/molecules-26-01114-g001.jpg

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