In vitro antifungal activity of naphthoquinone derivatives

In vitro antifungal activity of naphthoquinone derivatives
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DOI:
10.1248/bpb.25.669
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发表时间:
2002-05-01
影响因子:
2
通讯作者:
Yoshizaki, F
Yoshizaki, F
中科院分区:
医学4区
文献类型:
--
作者:
Sasaki, K;Abe, H;Yoshizaki, F

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研究了紫草根中萘醌类化合物对几种常见真菌的体外抑菌活性。当测试这些化合物对真菌的生物活性时,记录了广泛的敏感性。紫草素对酵母样真菌的抑制作用强于氟康唑:对克柔念珠菌的抑制作用为4倍(最小抑菌浓度(MIC):4 μ g/ml),对酿酒酵母的抑制作用为2倍(MIC:4 μ g/ml),尽管它对C.光滑的脱氧紫草素对C. krusei(MIC; 4 μ g/ml)和3倍(MIC; 2 μ g/ml)对S.啤酒。乙酰紫草素和β-羟基异戊酰紫草素对除C. krusei与标准相比。针对丝状真菌皮肤丝孢酵母,发现所有萘醌具有一系列活性,效力低于标准品。这一结果为紫草的临床应用提供了合理的依据,并显示了其作为具有抗真菌活性的抗炎药在药物治疗中应用的可能性。
In vitro antifungal activities of naphtoquinone-derivatives, which are constituents of Shikon, roots of Lithospermum erythrorhizon, were investigated against several fungal pathogens. When the biological activity of these compounds was tested against fungi, a wide range of sensitivity was recorded. Shikonin was found to have a stronger than fluconazole against yeast-like fungi: four-fold against Candida krusei (minimal inhibitory concentration (MIC); 4 mug/ml) and two-fold (MIC; 4 mug/ml) against Saccharomyces cerevisiae, though it showed the same potency as fluconazole against C. glabrata. Deoxyshikonin also exhibited four-fold stronger activity against C. krusei (MIC; 4 mug/ml) and three-fold (MIC; 2 mug/ml) stronger against S. cerevisiae. Acetylshikonin and beta-hydroxyisovaleryl shikonin showed lower activities against all fungal pathogens except for C. krusei compared with the standard. Against the filamentous fungus, Trichosporon cutaneum, all naphthoquinones were found to have a range of activity with lower potency than standard. This result provides a rational basis for the clinical use of shikon and shows the possibility of its use in medicinal treatment as an anti-inflammatory agent with antifungal activity.