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从[具体来源]中生物导向分离抗生物膜和抗菌孕烷糖苷:消除多重耐药病原体

Bioguided Isolation of Antibiofilm and Antibacterial Pregnane Glycosides from : Disarming Multidrug-Resistant Pathogens.

作者信息

El-Shiekh Riham A, Hassan Mariam, Hashem Rasha A, Abdel-Sattar Essam

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, El-Kasr El-Aini Street, Cairo 11562, Egypt.

Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, El-Kasr El-Aini Street, Cairo 11562, Egypt.

出版信息

Antibiotics (Basel). 2021 Jul 3;10(7):811. doi: 10.3390/antibiotics10070811.

Abstract

Methicillin-resistant (MRSA) and multidrug-resistant (MDRAB) present a serious challenge because of their capability to cause biofilm resistance to commonly used antibiotics producing chronic infections and hindering the process of wound healing. In the current study, we investigated the antibacterial activity of extracts (MeOH, and its fractions CHCl and -butanol) against multidrug-resistant MRSA USA300 and AB5057. In vitro, the MeOH extract and both fractions of significantly inhibited biofilm formation and disrupted previously established biofilm by MRSA and MDRAB at all the tested concentrations (0.625, 0.313, and 0.156 mg/mL). In vivo, extracts successfully decreased bacterial loads in MRSA-infected skin lesions in mice. Four pregnane glycosides and one flavone glycoside were isolated from the bioactive -butanol fraction. The isolated compounds (-) were tested for their biofilm inhibition and biofilm detachment activities. The results revealed that was the most active compound (IC = 0.139 mmole), while was the least active (IC = 0.818 mmole). These results support the potential use of extracts or their isolated compounds for hindering the biofilm attachment and the virulence of MRSA and MDRAB and their application as a topical antimicrobial preparation for MRSA skin infections.

摘要

耐甲氧西林(MRSA)和多重耐药(MDRAB)因其能够形成生物膜,对常用抗生素产生耐药性,导致慢性感染并阻碍伤口愈合进程,从而带来了严峻挑战。在本研究中,我们调查了提取物(甲醇提取物及其氯仿和正丁醇馏分)对多重耐药的MRSA USA300和AB5057的抗菌活性。在体外,甲醇提取物及其两个馏分在所有测试浓度(0.625、0.313和0.156毫克/毫升)下均能显著抑制MRSA和MDRAB生物膜的形成,并破坏先前已形成的生物膜。在体内,提取物成功降低了小鼠MRSA感染皮肤损伤处的细菌载量。从具有生物活性的正丁醇馏分中分离出了四种孕烷糖苷和一种黄酮糖苷。对分离出的化合物进行了生物膜抑制和生物膜脱离活性测试。结果显示,[具体化合物名称1]是活性最强的化合物(IC50 = 0.139毫摩尔),而[具体化合物名称2]活性最弱(IC50 = 0.818毫摩尔)。这些结果支持了[提取物名称]提取物或其分离出的化合物在阻碍MRSA和MDRAB生物膜附着及毒力方面的潜在用途,以及它们作为MRSA皮肤感染局部抗菌制剂的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/066c/8300726/7494516c5daa/antibiotics-10-00811-g001.jpg

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