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香叶醇的抗念珠菌活性涉及细胞膜完整性和功能的破坏。

Anti-Candida activity of geraniol involves disruption of cell membrane integrity and function.

作者信息

Sharma Y, Khan L A, Manzoor N

机构信息

Medical Mycology Lab, Department of Biosciences, Jamia Millia Islamia, 110025 New Delhi, India.

College of Applied Medical Sciences, Taibah University, 30001 Al-Madinah Al-Munawarah, Saudi Arabia; Medical Mycology Lab, Department of Biosciences, Jamia Millia Islamia, 110025 New Delhi, India.

出版信息

J Mycol Med. 2016 Sep;26(3):244-54. doi: 10.1016/j.mycmed.2016.04.004. Epub 2016 Aug 20.

Abstract

Candidiasis is a major problem in immunocompromised patients. Candida, an opportunistic fungal pathogen, is a major health concern today as conventional drugs are highly toxic with undesirable side effects. Their fungistatic nature is responsible for drug resistance in continuously evolving strains. Geraniol, an acyclic monoterpene alcohol, is a component of several plant essential oils. In the present study, an attempt has been made to understand the antifungal activity of geraniol at the cell membrane level in three Candida species. With an MIC of 30-130μg/mL, this natural compound was fungicidal at concentrations 2×MIC. There was complete suppression of fungal growth at MIC values (growth curves) and encouragingly geraniol is non-toxic even at the concentrations approaching 5×MIC (hemolysis assay). Exposed cells showed altered morphology, wherein the cells appeared either broken or shrivelled up (SEM studies). Significant reduction was seen in ergosterol levels at sub-MIC and glucose-induced H(+) efflux at concentrations>MIC values. Our results suggest that geraniol disrupts cell membrane integrity by interfering with ergosterol biosynthesis and inhibiting the very crucial PM-ATPase. It may hence be used in the management and treatment of both superficial and invasive candidiasis but further studies are required to elaborate its mode of action.

摘要

念珠菌病是免疫功能低下患者面临的一个主要问题。念珠菌是一种机会性真菌病原体,由于传统药物具有高毒性和不良副作用,它已成为当今主要的健康问题。其抑菌特性导致不断进化的菌株产生耐药性。香叶醇是一种无环单萜醇,是几种植物精油的成分。在本研究中,已尝试在细胞膜水平上了解香叶醇对三种念珠菌的抗真菌活性。这种天然化合物的最低抑菌浓度(MIC)为30 - 130μg/mL,在2×MIC浓度下具有杀菌作用。在MIC值时真菌生长完全受到抑制(生长曲线),令人鼓舞的是,即使在接近5×MIC的浓度下香叶醇也无毒(溶血试验)。暴露的细胞显示出形态改变,细胞呈现出破裂或皱缩的状态(扫描电子显微镜研究)。在亚MIC浓度下麦角固醇水平显著降低,在浓度>MIC值时葡萄糖诱导的H(+)外流也显著降低。我们的结果表明,香叶醇通过干扰麦角固醇生物合成和抑制非常关键的质膜ATP酶来破坏细胞膜完整性。因此,它可用于浅表性和侵袭性念珠菌病的管理和治疗,但需要进一步研究来详细阐述其作用方式。

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