Potent in vitro and in vivo antimicrobial activity of semisynthetic amphiphilic γ-mangostin derivative LS02 against Gram-positive bacteria with destructive effect on bacterial membrane.,Biochimica et Biophysica Acta (BBA) - Biomembranes

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Potent in vitro and in vivo antimicrobial activity of semisynthetic amphiphilic γ-mangostin derivative LS02 against Gram-positive bacteria with destructive effect on bacterial membrane.
Biochimica et Biophysica Acta (BBA) - Biomembranes ( IF 2.8 ) Pub Date : 2020-05-11 , DOI: 10.1016/j.bbamem.2020.183353
Shuimu Lin ₁ , Chunjie Zhu ₁ , Hongxia Li ₁ , Yongzhi Chen ₁ , Shouping Liu ₁

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Semisynthetic γ-mangostin derivative LS02 is a novel cationic amphiphilic peptidomimetic antimicrobial agent containing a hydrophobic scaffold and three hydrophilic and positively charged residues of arginine. LS02 showed low in vitro toxicity, potent activities against Gram-positive bacteria including MRSA (MIC = 1.56-6.25 μg/mL) and avoidance of drug resistance. The mode of action studies indicated that LS02 killed bacteria by disrupting bacterial cell membranes. LS02 not only exhibited good water solubility, low hemolytic activity and cell cytotoxicity, but also displayed excellent in vitro and in vivo antibacterial activity, indicating its great potential of being a lead compound as a novel membrane-active antibacterial agent capable of combating bacterial resistance.

中文翻译：

半合成的两亲性γ-Mangostin衍生物LS02对革兰氏阳性细菌具有强大的体外和体内抗菌活性，对细菌膜具有破坏性作用。

半合成γ-芒果素衍生物LS02是一种新型的阳离子两亲拟肽抗微生物剂，包含疏水性支架和三个精氨酸的亲水性和带正电荷的残基。LS02显示出低的体外毒性，对包括MRSA（MIC = 1.56-6.25μg/ mL）在内的革兰氏阳性细菌有效的活性，并且避免了耐药性。作用方式研究表明，LS02通过破坏细菌细胞膜杀死细菌。LS02不仅表现出良好的水溶性，低溶血活性和细胞毒性，而且还表现出优异的体外和体内抗菌活性，表明其作为潜在化合物作为新型抗细菌耐药性的膜活性抗菌剂的巨大潜力。

更新日期：2020-05-11

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