抗真菌药物的分类及研究进展概述

目的综述抗真菌药物的分类及研究新进展。方法综合和分析国内外有关文献报道。结果总结各类型抗真菌药物的作用机制及耐药机制;从脂质体药物的开发、三哇类药物的构效关系、作用于真菌细胞壁的药物等几方面最新的研究成果,探讨抗真菌药物的发展方向。结论多项研究表明抗真菌药物的联合应用。可产生协同作用和相加作用,并减少真菌耐药的发生。     

抗真菌药物作用机制及真菌耐药机制的研究进展

抗真菌药物的作用靶位包括真菌细胞壁、细胞膜、蛋白质合成和核酸合成.依据作用靶位分别阐述了抗真菌药物的作用机制.目前临床常用的抗真菌药物有唑类、多烯类、烯丙胺类、5-氟胞嘧啶和芬净类,从分子层面上分别介绍了真菌对以上药物的耐药机制.     

植物体内的抗真菌成分

本文介绍近年来从植物中提取的具有抗真菌活性的化合物及其对某些真菌的抑制活性强度。     

抗真菌药物与其他药物的相互作用及机制

自咪唑类抗真菌药临床应用以来 ,尤其是酮康唑问世以来 ,研究人员发现通过作用于真菌细胞膜合成可影响细胞色素Ｐ450 的一些酶 ,尤其是其中的 3Ａ4酶 ,可与其他有类似作用的药物发生相互作用 ,二药合用 ,有时可降低抗真菌药的药效 ,有时可提高其药效 ;或反过来被抗真菌药提高或降低其原来的药效。为了对抗真菌药与其他药物间的相互作用及其机制有更进一步认识 ,减少其不良反应 ,现作一综述。1　抗真菌药与其他药物间的作用机制1 .1　作用机制　已知人类细胞色素Ｐ450 酶中已发现 1 7～ 2 0种单体酶 ,其中第 3族中的酶与药物间有密切关系 ,特别是 3Ａ4酶。根据生物化学、免疫化学和酶的特性及其序列的相似性 ,已发现 1 8种人类细胞色素Ｐ450 ,而其中细胞色素Ｐ450 之 3Ａ4及2Ｃ8～2Ｃ1 0 是成人肝中主要的酶 ,因此 ,不涉及这 2种酶的抗真菌药物就很少引起人类肝酶的改变[1 ] 。作用于真菌细胞膜合成途径中的细胞色素Ｐ450 中任何成分的咪唑类及三氮唑类药物 ,易与同样有作用于此成分的药物如华法林、苯妥英钠、地高辛、三唑仑、美乐地辛、氯氮、环孢素、利福平、异烟肼、安替比林、西沙必利、Ｈ1 ...     

天然植物成分抗真菌研究新进展

查阅近年来有关天然植物成分抗真菌研究的国内外文献,并对其进行分析、归纳和总结,综述了天然植物成分抗真菌研究的新进展。天然植物以提取物和活性成分的形式发挥抗真菌作用,或作为抗真菌药物的增效剂和增敏剂,与抗真菌药物联合应用。研究的深入为筛选天然植物抗真菌活性成分和先导化合物提供了有利条件。     

唑类抗真菌药物耐药机制

真菌对人类生命危害很大。近几十年来广泛应用广谱抗生素、激素、免疫抑制药、抗肿瘤药物等加剧了真菌病的蔓延。深部真菌感染已成为癌症病人、爱滋(AIDS)病人及免疫缺陷病人等死亡因素之一。念珠菌是人类主要的致病菌之一,而口咽部念珠菌症在AIDS病人中最为普遍。在血液感染的     

抗真菌药物的系统分类、耐药机制及新药研发进展

由于癌症放化疗、器官移植等患者人数的增加以及广谱抗菌药物的广泛使用，白念珠菌、新型隐球菌等深部真菌感染病例急剧增加，严重威胁人类健康。目前治疗真菌感染的药物按作用靶点可分为7类，但是耐药性严重、抗菌谱窄、不良反应多等问题限制了其临床应用，开发安全、有效的抗真菌新药成为一个亟待解决的难题。本文从抗真菌药物的分类、耐药机制和新药的研发3个方面进行综述，以期为抗真菌药物的进一步研发提供参考。     

抗真菌药物研究进展

综述近年来抗真菌药物的研究进展,包括抗真菌抗生素与合成抗真菌药.还概述了开发中的新药.     

微生物来源的新抗真菌物质研究进展

本文综述了近几年发现的一些微生物来源的新抗真菌物质,如大环内酯类、蛋白质和肽类、糖类、抗真菌因子和植物内生菌.     

真菌对临床抗真菌药物的耐药机制

真菌感染,尤其是深部真菌感染的发病率近年来呈上升趋势,抗真菌药物的大量使用引起了真菌耐药曰益严重,严重影响了抗真菌药物治疗的效果,也增加了危重患者的病死率,因此对真菌耐药机制的研究十分必要.本文依据常用抗真菌药物的药物种类,分别总结论述了近年来真菌耐药机制研究的新进展.     

Antibacterial and Antifungal Activities of Nine Medicinal Plants from Zaire

Abstract

Zairean medicinal plants were extracted and screened for in vitro antibacterial and antifungal activities. Of nine plants investigated, extracts of six plants (Alchornea cordifolia, Bridelia ferruginea, Eucalyptus citriodora, Hymenocardia acida, Maprounea africana and Sida rhombifolia) demonstrated a marked antibacterial activity against the microorganisms Klebsiella pneumoniae, Staphylococcus aureus and Streptococcus mutans; and extracts of four plants (A. cordifolia, E. citriodora, M. africana and S. rhombifolia) exhibited significant antifungal activity against Aspergillus niger, Candida albicans and Microsporum gypseum. Extracts from A. cordifolia and M. africana were the most active with a MIC value of 62.5 μg/ml. Fractionation of the crude methanol extracts revealed that the bactericidal and fungicidal constituents of the active plants were mainly distributed in their ethyl acetate and aqueous fractions. These results may provide a basis for the isolation of compounds of biological interest from these medicinal plants.     

Antibacterial and Antifungal Potential of some Arid Zone Plants

Sequential extracts of some medicinally important arid zone plants of Rajasthan, viz. Lepidagathis trinervis Nees., Polycarpea corymbosa Lam. and Sericostoma pauciflorum Stocks. ex Wight. were tested against six bacterial (Gram +ve and Gram -ve) and five fungal strains using agar well diffusion method. Ethyl acetate extract of L. trinervis showed maximum activity against Bacillus subtilis, Enterobactor aerogenes, Pseudomonas aeruginosa, Aspergillus flavus and Trichophyton rubrum (inhibition zone 16.00±0.81, 13.33±0.66, 14.33±1.85, 14.30±0.34 and 23.00±0.00 mm) at varied minimum inhibitory concentrations of 82, 20, 41, 41 and 20 μg/ml, respectively.     

Antibacterial,Antifungal, and Cytotoxic Activities of 11 Solanaceae Plants from Colombian Biodiversity

Abstract

The hexane, dichloromethane, and methanol extracts of 11 Solanaceae plants collected in Regional Natural Park Ucumarí (RNPU) Colombia were evaluated for their antibacterial and antifungal activities through the agar-well diffusion method and for cytotoxic activity by the brine shrimp lethality assay. In general, the methanol plant extracts were more bioactive in the three different tests performed in this work. Under conditions and concentrations of the plant extracts evaluated in this research, the cytotoxic activities against brine shrimp Artemia salina. (Leach) larvae were the strongest compared with the antibacterial or the antifungal activities. The strongest cytotoxic activities were observed with the methanol extracts from Browallia speciosa. Hook (LC₅₀ 0.01 mg/ml) and Deprea glabra. (Standl.) A.T. Hunziker (LC₅₀ 0.01 mg/ml). The three extracts from Solanum deflexiflorum. Bitter (MIC 0.31 mg/ml) and the dichloromethane extract from Solanum leucocarpun. Dunal (MIC 0.31 mg/ml) were more bioactive against the Gram-positive bacteria Bacillus subtilis.. The methanol extract from Lycianthes synanthera. (Send.) Bitter exhibited good antimycotic activities against Candida albicans. and Fusarium solani. both with a MIC of 0.62 mg/ml.     

糖苷酶序列分类法和作用机理的研究进展

糖苷酶作为维持生物体基本功能的重要酶类之一，在生物催化和转化领域具有广泛的应用价值。文章介绍了一种能显示酶的结构和机理特征的糖苷酶分类法——序列分类法。它能更好的反映酶的结构特征，显示酶与酶之间的进化关系，为获得机理相关信息提供方便。同时又从糖苷酶作用的一般催化机理（包括保持型和倒置型糖苷酶）、各类糖苷酶的活性位点的结构特点、糖苷酶机理的研究方法3方面对糖苷酶作一介绍。     

真菌耐药机制及新药研究动态

本文通过归纳目前临床常用和正在研发中的抗真菌药物的作用机制,进而综述了真菌对不同作用机制药物而产生的不同耐药机制,认为真菌高度耐药是多种机制共同作用的结果.克服相应耐药性来创制新药难度很大,可通过研究发现新活性物质和新靶点,以减少耐药性的发生.介绍了近年发现的几个微生物来源新抗真菌活性物质,研究发现的新抗真菌靶点,并阐述了合理的用药方案.     

微生物来源的免疫抑制剂及其作用机制

微生物来源的免疫抑制剂的作用机制包括三个方面,即抑制淋巴细胞内的信号转导,抑制抗原的处理和呈递,抑制DNA的合成。本文对此类免疫抑制剂的作用机制进行了综述,并介绍了几个根据作用机制从微生物产物中筛选免疫抑制剂的筛选体系。     

Antibacterial and Antifungal Activities of Volatile Oils from Zanthoxylum Rhoifolium. Leaves

Abstract

The volatile oil extracted from Zanthoxylum rhoifolium. Lam (Rutaceae) leaves was tested to verify its antimicrobial activity efficacy against six types of different high-virulent Gram-negative bacteria isolated from clinical material and against three different types of fungi (two yeast and a filamentous one). Some results were different from those observed in the literature, and these differences might have occurred due to seasonal, geographic, or nutritional variations of the plants. Nevertheless, the volatile oil was found to be very efficient against Salmonella enteritidis. and Shigella sonnei., bacteria responsible for diarrhea and for a huge number of deaths. Regarding the fungi, a great capacity of the volatile oil in inhibiting the growth of Aspergillus flavus. was found, although it does not affect Candida tropicalis. and Candida guilliermondii. growth.