In vitro antifungal activity of hydroxychavicol isolated from Piper betle L
In vitro antifungal activity of hydroxychavicol isolated from Piper betle L
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DOI：
10.1186/1476-0711-9-7
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发表时间：
2010-01-01
影响因子：
5.7
通讯作者：
Khan, Inshad A.
中科院分区：
文献类型：
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作者：
Ali, Intzar;Khan, Farrah G.;Khan, Inshad A.
背景：羟基胡椒酚，分离自胡椒叶水提取物的氯仿提取物，对124株真菌进行了抗真菌活性测定。方法：采用微量肉汤稀释法测定羟基胡椒酚的最低抑菌浓度（MIC）和最低杀菌浓度（MFC）。时间杀灭曲线研究，后抗真菌效果和突变预防浓度分别确定对念珠菌属和曲霉属。还测试了羟基胡椒酚抑制和减少白色念珠菌生物膜形成的潜力。通过碘化丙啶摄取量测定膜通透性。羟基胡椒酚对具有临床意义的真菌种类表现出抑制作用，对酵母菌的MIC范围为15.62至500 μ g/ml，对曲霉菌的MIC范围为125至500 μ g/ml，对于皮肤癣菌，7.81至62.5 μ g/ml，其中发现MFC与MIC相似或比MIC大两倍。羟基胡椒酚还表现出在4 x MIC下对念珠菌属物种的6.25至8.70 h的延长后抗真菌作用，并在2 x至8 x MIC浓度下抑制测试的真菌物种的突变体的出现。此外，它还能抑制C.白念珠菌和减少预形成的生物膜。C. albicans细胞暴露于hydroxychavicol，从而表明膜破坏可能是hydroxychavicol.Conclusions的作用模式：该化合物表现出的抗真菌活性保证其作为一种抗真菌剂，特别是用于治疗局部感染，以及漱口水对口腔念珠菌感染。
Background: Hydroxychavicol, isolated from the chloroform extraction of the aqueous leaf extract of Piper betle L., (Piperaceae) was investigated for its antifungal activity against 124 strains of selected fungi. The leaves of this plant have been long in use tropical countries for the preparation of traditional herbal remedies.Methods: The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of hydroxychavicol were determined by using broth microdilution method following CLSI guidelines. Time kill curve studies, post-antifungal effects and mutation prevention concentrations were determined against Candida species and Aspergillus species "respectively". Hydroxychavicol was also tested for its potential to inhibit and reduce the formation of Candida albicans biofilms. The membrane permeability was measured by the uptake of propidium iodide.Results: Hydroxychavicol exhibited inhibitory effect on fungal species of clinical significance, with the MICs ranging from 15.62 to 500 mu g/ml for yeasts, 125 to 500 mu g/ml for Aspergillus species, and 7.81 to 62.5 mu g/ml for dermatophytes where as the MFCs were found to be similar or two fold greater than the MICs. There was concentration-dependent killing of Candida albicans and Candida glabrata up to 8 x MIC. Hydroxychavicol also exhibited an extended post antifungal effect of 6.25 to 8.70 h at 4 x MIC for Candida species and suppressed the emergence of mutants of the fungal species tested at 2 x to 8 x MIC concentration. Furthermore, it also inhibited the growth of biofilm generated by C. albicans and reduced the preformed biofilms. There was increased uptake of propidium iodide by C. albicans cells when exposed to hydroxychavicol thus indicating that the membrane disruption could be the probable mode of action of hydroxychavicol.Conclusions: The antifungal activity exhibited by this compound warrants its use as an antifungal agent particularly for treating topical infections, as well as gargle mouthwash against oral Candida infections.