天然产物中抗真菌成分研究进展

自然界中存在很多高活性的抗真菌天然成分，特别是在樟科和百合科植物中，多数为萜类或酮类结构。综述了近年来国内外关于天然抗真菌活性成分的研究进展。     

抗真菌天然活性成分研究进展

目的：综述近年来抗真菌天然活性成分研究的进展。方法：查阅国内外的相关文献，并进行分类归纳和总结。结果：近年来研究的抗真菌天然活性成分主要有黄烷类、酮类、皂苷类、肽类、萜类和醛类化合物。结论：关于抗真菌天然活性成分的研究较多，也取得了一定的进展，但仍缺乏系统性，尤其没有进一步的开发应用。     

几种植物抗真菌活性成分的研究近况

报道了８种植物抗真菌活性成分的研究近况,为该类植物用于抗真菌研究及寻找活笥更强的抗真菌化合物提供科学依据。     

“十二五”国家重点图书出版规划项目《植物药活性成分大辞典》（上、中、下册）

植物中的活性成分是植物药发挥疗效的物质基础,植物活性成分研究是阐释植物药的生物活性、临床疗效和毒性的必要手段,也是新药发现和创制的可行途径,更是中药药效物质基础研究、质量控制以及配伍合理性及作用规律研究的前提和基础。近些年来,随着国际上植物化学以及天然药物化学学科的迅速发展,大量的植物活性成分被研究和报道,形成大量、丰富的植物活性成分研究的信息源。但是,     

中药协同抗真菌药物抗念珠菌的研究进展

侵袭性念珠菌感染已成为备受关注的公共卫生问题,而现行治疗念珠菌感染的药物有限,联合用药是一种实用有效的新药开发策略。从天然植物（尤其是药用植物）中提取的化合物及其衍生物与传统的抗真菌剂联合使用对杀灭念珠菌具有显著的协同作用。归纳了念珠菌对传统抗真菌药物的耐药情况,并总结了中药协同传统抗真菌药物的抑菌活性和抑菌机制,以期为抗念珠菌新型治疗策略的研究提供参考依据。     

建立植物活性成分数据库—为新药研究服务、为中药现代化服务

自古以来 ,植物药是人类防治疾病的主要天然药物。植物中的活性成分是植物产生疗效的物质基础。回顾药物的发展史和现代药物的生产 ,可以看到世界上通过植物来源的药物约占全部药物的 1 /3;全世界 3/4人口的医药保健依靠植物 ;美国 1 /3处方药来自植物。近 50年来 ,我国新化学实体的发现大多来源于植物。世界上自从长春花碱、青蒿素、紫杉醇等植物活性成分的开发成功 ,为植物新药研究展示了光明的前景。当前从植物中寻找新的活性分子或先导化合物已成为世界大制药公司竞争的新目标。进入二十一世纪 ,我国创新药物研究和中药现代化研究都将面…     

芦荟属植物提取物及其主要成分的抗真菌活性[英]／Ali M I A…∥Phytother Res．-1999，13（5）．-401～407

已知芦荟属植物具有医疗价值，作者研究了芦荟属植物不同提取物的抗真菌活性，分离出活性成分，并通过色谱法鉴定了不同提取物及部位的化学成分。     

天然镇痛活性成分研究进展

天然镇痛活性成分一直是药物研发的热点之一。随着对海洋生物、微生物研究的深入和扩展,发现了许多结构新颖,活性独特的新型天然镇痛活性成分。本文综合了国外文献报道,按结构类型对新发现的天然镇痛活性成分进行分类,综述其研究现状。     

埃及芳香植物的抗菌活性

本文报告了40种挥发油和32种挥发油成分抗菌和抗真菌活性的筛选工作。实验所研究的植物材料均采自埃及的Assiut 地区.挥发油样品是从新鲜植物经水蒸汽蒸馏     

抗真菌中药的研究进展

近年来,由于广谱抗生素、激素、化疗和免疫抑制剂的普遍应用,真菌感染的发病率日益增加.但目前临床上应用的西药抗真菌药物,均存在着疗效差、毒性大等缺点.寻找广谱、高效、低毒的抗真菌新药已成为药物研究的热点.特别是从植物中寻找抗真菌药物,已成为公认的重要研究方向.我国科学家经过几十年的探索,发现了许多中药具有抗真菌作用,分离得到了多种有效化学成分,对这些成分的作用机理作出了初步研究,这些工作为开发抗真菌新药和中药用于临床抗真菌,奠定了坚实基础.     

Natural products – antifungal agents derived from plants

A new spectrum of human fungal infections is increasing due to increased cancer, AIDS, and immunocompromised patients. The increased use of antifungal agents also resulted in the development of resistance to the present drugs. It makes necessary to discover new classes of antifungal compounds to cure fungal infections. Plants are rich source of bioactive secondary metabolites of wide variety such as tannins, terpenoids, saponins, alkaloids, flavonoids, and other compounds, reported to have in vitro antifungal properties. Since the plant kingdom provides a useful source of lead compounds of novel structure, a wide-scale investigation of species from the tropics has been considered. Therefore, the research on natural products and compounds derived from natural products has accelerated in recent years due to their importance in drug discovery. A series of molecules with antifungal activity against different strains of fungus have been found in plants, which are of great importance to humans. These molecules may be used directly or considered as a precursor for developing better molecules. This review attempts to summarize the current status of important antifungal compounds from plants.     

Inhibition of human CYP19 by azoles used as antifungal agents and aromatase inhibitors, using a new LC-MS/MS method for the analysis of estradiol product formation

Azoles are used as fungicides in agriculture or antifungal drugs in medicine. Their therapeutic activity is based on the inhibition of fungal lanosterol-14alpha-demethylase (CYP51). Azoles are also used for the treatment of estrogen-dependent diseases, e.g. in breast cancer therapy. Inhibition of CYP19 (aromatase) is the working principle for tumor therapy, but is an unwanted side effect of azoles used as fungicides or antifungal drugs. The inhibition of recombinant human CYP19 by 21 azoles in use for the three different purposes was investigated using the natural substrate testosterone. Estradiol product formation was measured by a newly developed and fully validated analytical method based on liquid chromatography-tandem mass spectrometry utilizing photospray ionization (APPI). Potency of enzyme inhibition was expressed in terms of IC50 concentrations. The two cytostatic drugs fadrozole and letrozole were the most potent inhibitors. However, azoles used as fungicides, e.g. prochloraz, or as antifungal drugs, e.g. bifonazole, were almost as potent inhibitors of aromatase as the drugs used in tumor therapy. Comparison of plasma concentrations that may be reached in antifungal therapy do not allow for large safety factors for bifonazole and miconazole. The IC50 values were compared to data obtained with other substrates, such as the pseudo-substrate dibenzylfluorescein (DBF). A high correlation was found, indicating that the fluorescence assay with DBF can well be used for potency ranking and screening of chemicals for aromatase inhibition. The data for antifungal drugs show that side effects on steroid hormone synthesis in humans due to inhibition of aromatase should be considered.     

有机硫类抗真菌药物的研究进展

抗真菌药物(antifungal drugs)是一种用于治疗真菌感染的有效药物。近年来,天然抗真菌化合物的筛选和合成抗真菌药物的结构修饰促进了有机硫类抗真菌药物迅速发展。文中对天然有机硫类抗真菌化合物的研究进展进行了综述,同时从氮唑类、硫脲类和丙烯胺类以及硫色酮类等3类化合物的结构修饰方面综述了目前合成有机硫类抗真菌药物的研究进展。     

我院4年皮肤病用药情况分析

目的 :了解皮肤病治疗药物的使用现状和发展趋势 ,以引导临床合理用药和皮肤科国产新药的开发。方法 :对本院1996年～1999年间的用药品种、金额和来源进行归类统计分析和比较。结果与结论 :进口、合资的抗变态反应药占该类药品金额82 %～88 % ,提示应加强国产药物的研究。抗微生物药呈逐年上升趋势。天然药种类偏少 ,有广阔的开发前景。外用皮质激素、抗变态反应药和抗真菌药仍是皮肤病的主要用药     

抗分枝杆菌植物天然产物研究进展

摘要：由分枝杆菌引起的感染是人类健康的巨大威胁。目前,多种结核分枝杆菌和非结核分枝杆菌对临床抗分枝杆菌药 物具有较高的耐药性。中药治疗分枝杆菌感染具有悠久历史。例如,中药材狼毒已应用于抗结核分枝杆菌的治疗。非中药来源 的植物中,也蕴含丰富的抗分枝杆菌成分。这些植物来源的天然产物具有较好的结构多样性,是开发抗分枝杆菌药物的潜在来 源。本文综述了近年来在中药和其他非中药来源植物中发现的,具有良好抗分枝杆菌活性的化合物或提取物,并介绍了它们的 作用机制。这些活性植物天然产物为新抗分枝杆菌药物的发现提供了化合物库。同时,这些植物天然产物结构与现有抗分枝杆 菌药物具有显著的差别,研究其作用机制,也可发现新的抗分枝杆菌靶标。     

Heterocyclic Coenzyme A - independent transacylase inhibitors

The efforts of scientists to optimise the performance of existing antifungal drugs has resulted in their continued commercial success and also in renewed efforts of drug design within the pharmaceutical industry. Modification of existing compounds and the discovery and synthesis of new antifungal compounds in an attempt to produce efficacious drugs for the treatment of a range of human mycoses has led to a substantial increase in the number of patent applications in this area over the past decade. Recent filings include a range of process and application issues for both natural and semi-synthetic derivatives and a large proportion of patents describe compounds that target fungal enzymes and cell structural components. New leading compounds which appear to show good biological activity as both immunosuppressive and antifungal agents arise mainly from the macrolide class. These and other fermentation and synthetic compounds look promising; further development of many compounds is likely.     

Discovery and characterization of ß-1,6-glucan inhibitors

Importance of the field: The increasing number of patient populations at high risk of opportunistic infections has highlighted the need for the improvement in antifungal treatments. Due to the limited number of currently available antifungal drugs and the concerns for possible prevalence of resistant strains, drugs with a new mechanism of action are most desirable. Areas covered in this review: Although the cell wall is considered to be one of the ideal targets for antifungal drugs, insufficient information on the enzymes involved in its construction has restricted the discovery of new inhibitors. This review introduces the recent discovery of the inhibitors of β-1,6-glucan, one of the essential components of the yeast cell wall. What the reader will gain: The readers will gain the strategy to obtain the β-1,6-glucan synthesis inhibitors, their mechanisms of actions, and antifungal activities in vitro as well as in vivo. Take home message: The β-1,6-glucan inhibitors are considered to be promising candidates for new antifungal drugs which could give valuable options in a clinical setting, although their usage may be limited because of their fungistatic action and limited spectrum. Additionally, they can be useful tools in the study on β-1,6-glucan synthesis and the virulence of Candida species.     

Introduction of "clinical pharmacognosy"--integration between pharmacognosy and clinical pharmacy

In Japanese hospitals or pharmacies, crude drugs and natural products are used as the components of kampo medicine and dietary supplements. Clinical pharmacy can provide information such as the efficacy, adverse action, or interactions of crude drugs or natural products as well as chemical drugs. However, it is very difficult for a clinical pharmacist without a knowledge of pharmacognosy to offer full information, because crude drugs and natural products have very different pharmaceutical characteristics from chemical drugs containing a single compound. Drug information provided by such a pharmacist is sometimes ridiculous and may be misleading by suggesting the unusefulness of crude drugs. Therefore, in order to use crude drugs and kampo medicine effectively and safely, it is necessary to integrate the clinical pharmacy and pharmacognosy as "clinical pharmacognosy". Clinical pharmacognosy would also be capable of handling kampo medicine, a Japanese traditional medicine. Since basic pharmacognosy is a modern pharmaceutical science, pharmacognosists are limited in their understanding of a kampo formula and its clinical usefulness solely with a knowledge of that field. I suggest here that clinical pharmacognosy would better adopt the knowledge of traditional Chinese medicine that includes a theory of traditional pharmacology of the crude drugs used in kampo medicine.     

2010—2012年南京地区34家医院抗真菌药物使用分析

目的通过对南京地区34家医院2010—2012年抗真菌药物使用情况的分析,评价近年来抗真菌药物治疗情况。方法采用金额和用药频度（DDDs）分析及排序法进行药物利用分析。结果①抗真菌药物占抗菌药物的总金额呈逐年增加趋势,其中2011年增长率最高为10．8％。②抗真菌药物金额构成比最大的是深部真菌感染用药,尤其是三唑类药物,年均增长率为10．5％。③抗真菌药物通用名金额排序中三唑类药物排在前列,伏立康唑排名从2010年的第3位上升到2012年的第1位。④抗真菌药物DDDs排序中,深部真菌感染用药氟康唑和伊曲康唑排在前列,浅表部真菌感染用药特比萘芬排名也居前。结论2010—2012年南京地区34家医院使用抗真菌药物结构相对合理,用药金额增长较为显著,深部真菌感染用药趋于选用三唑类,浅表真菌感染趋于使用特比萘芬。     

2008—2010年南京地区抗真菌药应用分析

目的:分析2008—2010年南京地区抗真菌药使用现状及发展趋势。方法:采用金额和用药频度(DDDs)排序法,对南京地区31家入网医院的抗真菌药数据进行汇总并排序分析。结果:3年来,南京地区抗真菌药用药总金额逐年增加,三唑类代表药氟康唑、伊曲康唑和伏立康唑稳居用药金额排序前3位。抗真菌药市场以进口药为主。抗深部真菌药中三唑类的氟康唑和伊曲康唑,以及抗浅部真菌药中的特比萘芬和制霉菌素居DDDs排序前列。结论:2008—2010年南京地区抗真菌药用药金额呈增长趋势,临床疗效和是否为医保药品影响该类药物使用率。