植物中萘醌类化合物及其衍生物的抗微生物作用的研究进展

萘醌类化合物广泛存在于传统药用植物中。紫草素、胡桃醌、指甲花醌、白花丹素等是从传统药用植物中提取的萘醌类化合物。实验研究显示,这些萘醌类化合物及其衍生物具有广泛的抗细菌、抗真菌、抗病毒、抗寄生虫等病原微生物活性。现将其研究进展作一综述。     

近年抗生素（微生物药物）研究开发进展

主要介绍近两年微生物来源的药物,包括抗细菌、抗真菌、抗结核菌、抗病毒等抗感染药物、抗肿瘤、以及微生物来源的具有各种生理活性的物质,同时包括传统概念的合成、半合成抗菌药.     

植物中抗感染成分的研究进展

植物为了保护自身免受外界的侵袭,特别是微生物的侵袭,作为一种防御机制,产生了抗菌物质。近年来,国内外医药界工作者经过研究发现大量植物药,并分离得到许多活性成分。经初步统计,已经证实具有抗细菌活性的有128种,抗真菌的有27种,抗病毒的有12种[1]。其中有的既有抗菌作用,又有抗霉菌和抗病毒作用。这些活性成分,具有多种结构类型,现综述如下。1生物碱类1．1小檗碱（berberin）：为毛莨科植物黄连（Coptischinesis）根茎中提取的一种主要生物碱,可由黄连、黄柏或三棵针提取,也可人工合成。小檗碱对细菌只有弱的抑菌作用,但…     

含哌嗪类抗微生物药物研究进展

含哌嗪类化合物在抗微生物药物方面的研究开发较为活跃.本文结合国内外文献简述了在抗疟、抗菌、抗结核、抗真菌、抗病毒等方面已经上市及正在进行临床试验的含哌嗪类抗微生物药物,着重强调了含哌嗪的抗微生物药物及其构效关系的研发近况.随着研究的深入,有望成功地开发出更多具有克服多药耐药性的高效低毒哌嗪类抗微生物药物.     

小檗碱的抗病原生物作用研究进展

小檗碱又名黄连素,具有非常广泛的药理活性,但其准确的作用靶点至今不清.本文主要综述其抗病毒作用、抗细菌作用、抗真菌作用及其作用的构效关系和分子机制,对揭示生命现象的本质,发现新药靶点具有重要意义,也为小檗碱的结构优化改造和应用研究提供新的线索.     

小檗红碱药理作用及其结构修饰研究进展

天然来源的小檗红碱具有多种药理活性,对于其药物活性及结构修饰多有报道.本文围绕小檗红碱抗癌、抗炎、抗神经系统疾病、抗心血管疾病、抗真菌、抗糖尿病方面进行综述.同时对其结构修饰也作概述,为小檗红碱合理开发利用提供参考.     

糖类缩氨基硫脲衍生物及其过渡金属配合物的合成和生物活性的研究

缩氨基硫脲衍生物及其金属配合物具有抗肿瘤、抗病毒、抗真菌及抗细菌活性。但这类化合物却很少应用于临床,原因之一是其水溶性很小。因此,我们设计在这类化合物中引入了一个或多个亲水性基团。本研究合成了9种糖类缩氨基硫脲衍生物及它们的5种过渡金属配合物。其中,1种糖衍生物及其     

含三唑的抗微生物药物研究进展

含三唑的化合物是目前抗微生物药物研究开发中的热点领域之一。本文结合国内外文献简述了在抗菌、抗真菌、抗结核、抗病毒方面已经上市及正在进行临床试验的含三唑的药物,着重强调了含三唑的抗微生物药物及其构效关系的研发近况。随着研究的进一步发展,有望成功地开发出更多具有显著生物学活性的新药。     

特邀主编点评

<正>抗生素是指由微生物（包括细菌、真菌、放线菌属）或高等动植物在生活过程中所产生的具有抗病原体或其他活性的一类物质。按照化学结构,抗生素分为β-内酰胺类、氨基糖苷类、四环素类、氯霉素类、大环内酯类、林可霉素类等。按照用途,抗生素分为抗细菌抗生素、抗真菌抗生素、抗肿瘤抗生素、抗病毒抗生素、畜用抗生素、农用抗生素及其他微生物药物等。     

近年抗感染药物研究进展

本文综述了近年来抗感染药物包括抗细菌、抗真菌与抗病毒药物的研究进展,并概述了临床研究中的若干新化合物.     

New 6-nitroquinolones: synthesis and antimicrobial activities

Pursuing our searches on quinolonecarboxylic acids we used a simple three-step one pot procedure to synthesize novel 1,7-disubstituted-6-nitroquinolones. The new derivatives were tested against Mycobacterium tuberculosis and Mycobacterium avium complex (MAC) as well as against both gram-positive and gram-negative bacteria. In vitro assays showed some derivatives were endowed with good inhibiting activities against tested mycobacteria. Some derivatives were also found more potent than ciprofloxacin and ofloxacin (used as reference drugs) against gram-positive bacteria.     

Snake venom: kill and cure

Snake venom is a natural biological resource that contains several components, which are not only responsible for death but also have a potential therapeutic activity. The use of snake venom for medicinal purposes dates back to ancient times, now many drugs and clinical diagnostic kits have derived from components of snake venom. The scientists can extract, purify and identify new components of venom that may serve as starting point for structure–function relationship studies leading to design new medications. This review will highlight the activities of snake venoms and their components against cancer, microbes, parasitic infections and platelet aggregation.     

高喜树碱类抗肿瘤药物研究进展

在近年来研究的拓扑异构酶抑制剂中,高喜树碱类化合物是对喜树碱类化合物结构改造非常成功的衍生物,其活性等较喜树碱类强。本文主要就高喜树碱类在肿瘤治疗中的优越性及研究进展进行简要综述。     

4-substituted 1,5-diarylpyrazole,analogues of celecoxib: synthesis and preliminary evaluation of biological properties

A number of 5-aryl-1-[4-(methylsulfonyl)-phenyl]-1H-pyrazoles and 4-(5-aryl-1H-pyrazol-1-yl)benzenesulfonamides 3, 4, 5, 6, analogues of the COX-2 selective inhibitor celecoxib (celebrex), were synthesized. In order to verify the effects on the biological properties of certain substituents put on position 4 of the pyrazole nucleus, some of these compounds were screened in vivo for their anti-inflammatory and analgesic activities. Moreover, sodium salts of carboxylic acids 4 were tested in vitro for their platelet anti-aggregating properties. The results of these preliminary biological assays showed that new derivatives are not endowed with improved anti-inflammatory and analgesic properties, in comparison with celecoxib. In addition, docking studies were carried out on the most significative compounds to evaluate their interaction mode at the active site of both COX-1 and COX-2. Some remarks about the SAR of this class of COX-inhibitors are drown out.     

氟喹诺酮类药物对大鼠肝外组织药物代谢酶的影响

目的:探讨氟喹诺酮类药物(FQs)对大鼠肺、脑、肾、小肠中细胞色素P450(CYP)含量、氨基比林N- 脱甲基酶(AMND)、红霉素N-脱甲基酶(ERND)活性的影响。方法:体外实验中环丙沙星、妥苏沙星和司帕沙星的药物终浓度均为1 mmol·L-1;体内实验按1 mmol·kg-1剂量灌胃,qd×7。制备大鼠肺、脑、肾、小肠S9,分光光度法测定CYP含量、AMND及ERND活性变化。结果:大鼠肺、肾组织CYP含量低;3种药物可不同程度地抑制各组织AMND活性(P<0．05)。肾和小肠中可测到ERND活性,而肺、脑中未测到;给药后肾、小肠 ERND活性有降低趋势,但大多无显著差异。结论:FQs对肝外组织CYP含量无显著影响,对AMND活性有抑制作用,对ERND有抑制趋势。     

Synthesis,Antifolate and Anticancer Activities of N5‐Substituted 8,10‐Dideazatetrahydrofolate Analogues

Based on our previous work, seven N⁵‐substituted 8,10‐dideazatetrahydrofolate analogues and one 8‐deazatetrahydrofolate analogue were designed and synthesized as human dihydrofolate reductase (hDHFR) inhibitors. All compounds were assayed versus DHFR and five different cancer cell lines. The biological assay indicated that replacing N¹⁰ with carbon would significantly increase inhibitory activities against DHFR and cytotoxicities against cancer cell lines. Compound 19a with 4‐amino and N⁵‐formyl showed great antitumour activities against HL‐60, Bel‐7402 and BGC823 which were much better than MTX.     

Novel pharmaceutical options for treating fibromyalgia

Fibromyalgia is a chronic disorder whose symptoms have a devastating effect on patients’ lives as they limit their ability to engage in everyday working and social activities, and make it difficult to maintain normal relationships with family, friends and employers. None of the currently available drugs are fully effective against the whole spectrum of symptoms of pain, fatigue, sleep disturbances and depression, but increasing efforts by the pharmaceutical industry have led to the introduction of new investigational drugs and new formulations of older drugs, as well as studies of the possibility of applying drugs currently used for other diseases. The aim of this review is to summarise the data relating to the new therapeutic options that have become available over the last few years.     

新型核苷膦酸酯类化合物的合成及其抗乙肝病毒活性研究

目的设计合成新型核苷膦酸酯类化合物,并进行体外抗乙肝病毒活性评价。方法以不同取代的硫酚与2-氨基-9-[2-[二(2,2,2-三氟乙氧基)膦酰甲氧基]乙基]-6-氯嘌呤进行烃化反应合成目标化合物,化合物结构经1H-NMR和FAB-MS谱确证。采用HepG2.2215细胞进行体外抗乙肝病毒活性评价。结果与结论设计合成了9个核苷膦酸酯类新化合物,这些化合物均有一定的抗乙肝病毒活性。化合物4a、4b的活性强于拉米夫定、阿德福韦酯。苯环上取代基的类型显著影响核苷膦酸酯类化合物抗乙肝病毒活性。     

Synthesis and antifungal properties of N-[(1,1'-biphenyl)-4-ylmethyl]-1H-imidazol-1-amine derivatives

In the course of a study on 1H-imidazol-1-amine derivatives as antifungal agents, we found that N-[(1,1'-biphenyl)-4-ylmethyl]-N-[(2,4-dichlorophenyl)methyl]-1H-imidazol-1-amine (1a) exhibited promising activities. In order to explore more in detail the structure-activity relationship of this new class of antifungal agents, we report now the synthesis and the biological activity of new analogues (1b-k) of compound 1a. The synthesis was performed using N-[(1,1'-biphenyl)-4-ylmethyl]-1H-imidazol-1-amine as starting material which was reacted with the proper arylmethyl halide. Most of the newly synthesized imidazolamines exhibited both fungal growth inhibition activity and cellular selectivity.     

Recent cancer drug development with xanthone structures

Objectives Xanthones are simple three‐membered ring compounds that are mainly found as secondary metabolites in higher plants and microorganisms. Xanthones have very diverse biological profiles, including antihypertensive, antioxidative, antithrombotic and anticancer activity, depending on their diverse structures, which are modified by substituents on the ring system. Although several reviews have already been published on xanthone compounds, few of them have focused on the anticancer activity of xanthone derivatives. In this review we briefly summarize natural and synthetic xanthone compounds which have potential as anticancer drugs. Key findings The interesting structural scaffold and pharmacological importance of xanthone derivatives have led many scientists to isolate or synthesize these compounds as novel drug candidates. In the past, extensive research has been conducted to obtain xanthone derivatives from natural resources as well as through synthetic chemistry. Xanthones interact with various pharmacological targets based on the different substituents on the core ring. The anticancer activities of xanthones are also dramatically altered by the ring substituents and their positions. Summary The biological activities of synthetic xanthone derivatives depend on the various substituents and their position. Study of the biological mechanism of action of xanthone analogues, however, has not been conducted extensively compared to the diversity of xanthone compounds. Elucidation of the exact biological target of xanthone compounds will provide better opportunities for these compounds to be developed as potent anticancer drugs. At the same time, modification of natural xanthone derivatives aimed at specific targets is capable of expanding the biological spectrum of xanthone compounds.