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高、低分子量盐酸壳聚糖、羧甲基壳聚糖、壳寡糖和N-乙酰-D-葡糖胺对白色念珠菌、克柔念珠菌和光滑念珠菌的抗真菌作用。

Antifungal effect of high- and low-molecular-weight chitosan hydrochloride, carboxymethyl chitosan, chitosan oligosaccharide and N-acetyl-D-glucosamine against Candida albicans, Candida krusei and Candida glabrata.

作者信息

Seyfarth F, Schliemann S, Elsner P, Hipler U-C

机构信息

Department of Dermatology and Dermatological Allergology, Friedrich-Schiller University Hospital Jena, Jena, Germany.

出版信息

Int J Pharm. 2008 Apr 2;353(1-2):139-48. doi: 10.1016/j.ijpharm.2007.11.029. Epub 2007 Nov 23.

Abstract

OBJECTIVES

Generally, chitosan is a water-insoluble polyaminosaccharide with antimicrobial activity. The antifungal activity of water-soluble low- and high-molecular-weight chitosan hydrochloride, carboxymethyl chitosan, chitosan oligosaccharide and N-acetyl-d-glucosamine against Candida albicans, Candida krusei and Candida glabrata was investigated.

METHODS

Solutions of the tested substances in different concentrations (1, 0.5, 0.25, 0.1, 0.05, 0.025, 0.01, 0.005, and 0.0025%) were prepared and the influence on C. albicans DSM 11225, C. krusei ATCC 6258 and C. glabrata DSM 11226 was investigated. Yeasts (3 x 10(5) cells/mL) were incubated with Sabouraud liquid medium at 30 degrees C. Measurements were done with a microplate nephelometer (NEPHELOstar Galaxy, BMG LABTECH Ltd.) for 24 h. High values of light scattering correlate with strong cultural growth. Results were shown as growth curves and histograms displaying 24 h end points. These were compared with control by Mann-Whitney test. Furthermore, MIC(50%), MIC(80%) and Spearman correlation coefficients were calculated.

RESULTS

C. albicans and C. krusei were the most sensitive species. C. glabrata was also inhibited, whereas 1% of tested substances could not prevent its growth completely. However, only both chitosan hydrochlorides showed a definite antifungal effect with high correlation between inhibition and test concentration. Carboxymethyl chitosan, chitosan oligosaccharide and N-acetyl-D-glucosamine showed only a weak or no antifungal activity, respectively.

CONCLUSIONS

Antifungal activity decreases with declining molecular mass (chitosan oligosaccharide and N-acetyl-D-glucosamine) and increasing masking of the protonated amino groups with functional groups (carboxymethyl chitosan).

摘要

目的

一般来说,壳聚糖是一种具有抗菌活性的水不溶性聚氨基糖。研究了水溶性低分子量和高分子量壳聚糖盐酸盐、羧甲基壳聚糖、壳寡糖和N-乙酰-D-葡萄糖胺对白色念珠菌、克柔念珠菌和光滑念珠菌的抗真菌活性。

方法

制备不同浓度(1%、0.5%、0.25%、0.1%、0.05%、0.025%、0.01%、0.005%和0.0025%)的受试物质溶液,并研究其对白色念珠菌DSM 11225、克柔念珠菌ATCC 6258和光滑念珠菌DSM 11226的影响。将酵母(3×10⁵个细胞/mL)与沙氏液体培养基在30℃下孵育。使用微孔板散射仪(NEPHELOstar Galaxy,BMG LABTECH Ltd.)进行24小时测量。高散射光值与旺盛的培养生长相关。结果以生长曲线和显示24小时终点的直方图表示。通过曼-惠特尼检验与对照组进行比较。此外,计算了MIC(50%)、MIC(80%)和斯皮尔曼相关系数。

结果

白色念珠菌和克柔念珠菌是最敏感的菌种。光滑念珠菌也受到抑制,而1%的受试物质不能完全阻止其生长。然而,只有两种壳聚糖盐酸盐显示出明确的抗真菌作用,抑制作用与测试浓度之间具有高度相关性。羧甲基壳聚糖、壳寡糖和N-乙酰-D-葡萄糖胺分别仅显示出微弱的抗真菌活性或无抗真菌活性。

结论

抗真菌活性随着分子量的降低(壳寡糖和N-乙酰-D-葡萄糖胺)以及质子化氨基被官能团(羧甲基壳聚糖)的掩蔽增加而降低。

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