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从 Polyscias fulva Hiern(伞形科)茎皮的二氯甲烷-甲醇(1:1 v/v)提取物的体外和体内抗皮肤真菌活性。

In vitro and in vivo antidermatophytic activity of the dichloromethane-methanol (1:1 v/v) extract from the stem bark of Polyscias fulva Hiern (Araliaceae).

机构信息

Laboratory of Microbiology and Antimicrobial Substances, Faculty of Science, University of Dschang, P,O, Box 67, Dschang, Cameroon.

出版信息

BMC Complement Altern Med. 2013 May 6;13:95. doi: 10.1186/1472-6882-13-95.

Abstract

BACKGROUND

During the last decades, the number of people suffering from dermatophytoses has seriously increased, mainly due to the development of resistant strains of microorganisms to a range of formally efficient antibiotics. Polyscias fulva, a medium size tree which grows in the West Region of Cameroon is traditionally used for local application against dermatoses and orally against venereal infections. The dichloromethane-methanol (1:1 v/v) extract from the stem bark of Polyscias fulva was evaluated for its in vitro and in vivo antifungal activities.

METHODS

The plant extract was prepared by maceration of its stem bark powder in CH(2)Cl(2)-MeOH (1:1 v/v). The extract obtained was successively partitioned in hexane, ethyl acetate and n-butanol. Phytochemical screening was performed using standard methods. In vitro antidermatophytic activity was assayed by the well diffusion and broth microdilution methods. The degree of dermal irritation of the crude extract was determined in guinea pigs using the occluded dermal irritation test method. The in vivo antidermatophytic activity of the extract-oil formulation (1.25, 2.5 and 5% w/w concentrations) was evaluated using Trichophyton mentagrophytes-induced dermatophytosis in a guinea pigs model.

RESULTS

Phytochemical screening indicated that, the crude extract, ethyl acetate, n-butanol and residue fractions contain in general saponins, tannins, alkaloids, anthraquinones and phenols while the hexane fraction contains only alkaloids. The ethyl-acetate, n-butanol and residue fractions displayed higher antifungal activities (MIC = 0.125-0.5 mg.mL(-1)) against eight dermatophytes as compared to the crude extract (MIC = 0.5-1 mg.mL(-1)). This latter appeared to have slight perceptible erythema effects on guinea pigs as the primary irritation index (PII) was calculated to be 0.54. In vivo, the antidermatophytic activities of the extract-oil formulations were dose-dependent. Griseofulvin-oil 5% at 0.01 g/kg and formulated extract-oil (5%) at 0.1 g/kg eradicated the microbial infection after thirteen and fourteen days of daily treatment respectively.

CONCLUSIONS

The results of preclinical in vitro and in vivo evaluations indicate that the extract-oil formulation at 5% may constitute an alternative means to alleviate fungal infections caused by dermatophytes.

摘要

背景

在过去的几十年中,患有皮肤真菌病的人数严重增加,主要是由于微生物对一系列有效抗生素的耐药菌株的发展。在喀麦隆西部地区生长的中等大小的树 Polyscias fulva,传统上用于局部治疗皮肤病和口服治疗性病。从 Polyscias fulva 的茎皮中用二氯甲烷-甲醇(1:1v/v)提取的提取物评估了其体外和体内抗真菌活性。

方法

通过将其茎皮粉在 CH(2)Cl(2)-MeOH(1:1v/v)中浸渍来制备植物提取物。所得提取物依次在正己烷、乙酸乙酯和正丁醇中进行分配。使用标准方法进行植物化学筛选。通过平板扩散和肉汤微量稀释法测定体外抗皮肤真菌活性。通过封闭性皮肤刺激试验方法在豚鼠中确定粗提取物的皮肤刺激性程度。使用豚鼠模型中的 Trichophyton mentagrophytes 诱导的皮肤真菌病评估提取物-油制剂(1.25、2.5 和 5%w/w 浓度)的体内抗皮肤真菌活性。

结果

植物化学筛选表明,粗提取物、乙酸乙酯、正丁醇和残渣部分通常含有皂苷、单宁、生物碱、蒽醌和酚类,而正己烷部分仅含有生物碱。与粗提取物(MIC=0.5-1mg.mL(-1))相比,乙酸乙酯、正丁醇和残渣部分对八种皮肤真菌具有更高的抗真菌活性(MIC=0.125-0.5mg.mL(-1))。后者似乎对豚鼠有轻微的可察觉的红斑作用,因为初级刺激指数(PII)计算为 0.54。在体内,提取物-油制剂的抗皮肤真菌活性呈剂量依赖性。灰黄霉素-油 5%(0.01g/kg)和配方提取物-油(5%)(0.1g/kg)在每日治疗 13 和 14 天后分别消除了微生物感染。

结论

临床前体外和体内评价的结果表明,5%的提取物-油制剂可能是减轻由皮肤真菌引起的真菌感染的替代手段。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2ad/3658906/89111037fafd/1472-6882-13-95-1.jpg

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