海绵中抗HIV活性成分的研究进展

从海洋生物资源中寻找具有抗HIV活性的天然产物是新药研究开发的重要途径之一。海绵分布广泛,容易采集,并含有丰富的天然活性产物。本文综述来源于海绵中的炔类、甾醇类、萜类、生物碱、环缩酚肽、类脂等抗HIV活性的天然产物。     

天然产物抗血小板聚集作用的研究进展

目的综述近年来天然产物抗血小板聚集作用的最新研究进展。方法重点查阅61篇近期国内外天然产物抗血小板聚集的文献,对具有抗血小板聚集活性的天然产物进行总结和分析。结果总结得出114个天然产物单体成分并分析其在抗血小板聚集作用中发展前景,为研究和开发新型高效低毒的血小板聚集抑制剂提供理论基础。结论多种天然产物在抗血小板聚集作用方面具有良好开发前景,应对其进行更为深入的机制及构效关系研究从而筛选出新型血小板聚集抑制剂。     

抗心肌纤维化天然产物的研究进展

心肌纤维化是一种常见的临床疾患，可导致心源性猝死、心律失常和心力衰竭等疾病，研发有效的治疗药物显得尤为重要。近年来大量研究表明，天然产物在预防和治疗心肌纤维化方面有巨大潜力。本文归纳和总结了抗心肌纤维化天然产物的研究进展，为探寻抗心肌纤维化的活性先导物以及天然产物的深入研究和开发提供参考。     

抗分枝杆菌植物天然产物研究进展

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。     

海洋天然产物治疗心血管疾病作用机制的研究进展

海洋中复杂的生存条件造就了海洋天然产物区别于陆地天然产物的独特结构和多样的生理活性。从海洋生物中提取的活性物质大多具有良好的抗炎、抗肿瘤、免疫调节和治疗心血管疾病等作用。心血管疾病又称循环系统疾病,在我国的患病率和死亡率不断增加,成为城乡居民致死和致残的首要原因。就近年来海洋天然产物在治疗心血管疾病方面抗血栓形成、改善心功能、抗高血压的作用机制研究进展进行综述。     

海洋真菌来源的抗植物病原菌活性天然产物

近年来,海洋真菌来源的天然产物因其化学结构新颖和活性显著而受到广泛关注,其中许多代谢产物对植物病原菌具有较强的抗菌性。本文综述了从2002年-2018年5月间报道的33个新的抗植物病原菌活性天然产物的来源、结构及其生物活性。     

具有降尿酸或抗痛风活性的天然产物研究进展

目前临床上使用的抗痛风小分子药物在降低血清尿酸水平方面有明显的治疗效果,但其具有严重的过敏反应和肝肾损害等不良反应。许多天然产物具有广泛的降尿酸或抗痛风活性,且安全性高,已成为抗痛风新药发现的重要方向。本文综述了具有降尿酸或抗痛风药理作用的天然产物及其机制研究,以期为药物研发提供参考。     

抗艾滋病海洋天然产物的研究进展

本文综述了具有抗艾滋病活性的海洋天然产物及其作用机制,对海洋抗艾滋病物质今后的发展作了展望,为进一步研究提供了较为详细的参考资料.     

海洋药物——二十一世纪中国药学研究的新热点

海洋是生命之源 ,海洋生物活性物质主要包括生物信息物质、各类活性成分、海生毒素、生物功能材料等 ,研究海洋生物活性物质是海药研究的主导方向。近年来 ,国际上出现大量涉及药学、食品、功能食品、化妆品、酶制剂、生物工具药方面的海洋天然产物专利产品 ,发现一大批高效的抗菌、抗病毒、抗炎、抗肿瘤、镇痛、防治心脑血管疾病的海洋生物活性物质 ,多数化合物具有新药开发潜力。但与来源于陆生植物的 1 5万多种天然产物相比 ,海洋天然产物至今才 1万多种 ,从资源研究上看 ,目前用于研究的海洋生物仅几千种 ,表明海洋生物具有巨大潜力等待…     

抗炎天然产物活性成分研究进展

炎症是具有血管系统的活体组织对各种损伤因子的刺激所发生的防御反应,在人体许多重大疾病的发生发展过程中起着极其重要的作用。临床上应用的抗炎药物主要有非甾体类抗炎药、甾体类抗炎药和中草药。由于现有的化学合成抗炎药物具有明显的不良反应,近年来人们越来越重视从天然产物中寻找、开发抗炎药物。以往的综述主要侧重于天然药物的抗炎机制,而对于天然药物中抗炎活性成分的总结却少有报道,笔者对近年来报道的具有抗炎作用的天然药物活性成分的研究进行综述,以期对进一步开发高效安全的抗炎药物提供参考。     

Study of anti-fertility effect of lemon seeds (Citrus limonum) in female albino mice

Among the citrus species, Citrus-limonum is native of North West region of India. The petroleum ether, alcoholic and aqueous extracts of Citrus-limonum (lemon) seeds were investigated for anti-fertility effect in female albino mice. The extracts were administered orally for 7 days after insemination (i.e. post-ovulatory test). The control group received 4% gum acacia. The animals were examined for implantation sites on 10th day of pregnancy and the number of pups delivered at term for each group was recorded. The alcoholic extract showed significant anti-fertility effect as compared to petroleum ether and aqueous extracts. The alcoholic extract was subjected for fractionation and the fractions were again tested for their anti-fertility effect. The fraction of ethyl-acetate (12-25 fractions) showed most encouraging anti-fertility activity. In second part of the study, the alcoholic extract and its ethyl-acetate fraction (12-25 fractions) were subjected to evaluation of their mechanism of action and it was found that their principal mode of action is as an anti-zygotic agent. Withdrawal of the test drug, resulted in complete restoration of fertility. Thus the ethyl-acetate fraction (12-25 fractions) of alcoholic extract of lemon seeds exerted reversible anti-fertility effect in female mice by virtue of its anti-zygotic action.     

The role of pharmacognosy in modern medicine and pharmacy

This review details the contribution to modern medicine and pharmacy made by natural products and drugs derived from natural products, with an emphasis on essential medicines and new introductions to the market. Areas covered include recent advances in the development of drugs derived from marine organisms, microbes, terrestrial animals, and vascular plants, and current issues regarding botanical medicines. The role of natural products in drug discovery and development is evaluated, particularly with regard to their value as sources of drug leads with "drug-like" properties. A rationale for the success of natural products research in providing new drugs and drug prototypes is presented, drawing on lines of evidence from chemical informatics and chemical ecology. Several innovative strategies for natural products drug discovery and evaluation of botanical medicines are also reviewed.     

Misassigned natural products and their revised structures

Natural products are a major pipeline for drug development and are responsible for more than 50 % of drugs on the market. NMR is a fundamental and powerful tool for the structure determination of natural products. It is essential to provide unambiguous chemical structure information on natural products in drug development research, including the structure–activity relationship, derivatization and pharmacokinetic/pharmacodynamic studies. Advancement of NMR instruments has made it possible to deal with nanomole-scale natural products for structure elucidation, but misinterpretation of NMR spectra still occurs. We review 21 natural products with revised chemical structures and the methods used for those revisions.     

Fishing for drugs from nature: zebrafish as a technology platform for natural product discovery

Emerging challenges within the current drug discovery paradigm are prompting renewed interest in natural products as a source of novel, bioactive small molecules. With the recent validation of zebrafish as a biomedically relevant model for functional genomics and in vivo drug discovery, the zebrafish bioassay-guided identification of natural products may be an attractive strategy to generate new lead compounds in a number of indication areas. Here, we review recent natural product research using zebrafish and evaluate the potential of this vertebrate model as a discovery platform for the systematic identification of bioactive natural products.     

The modification of natural products for medical use

Drug innovation is characterized by painstaking molecular-level syntheses and modifications as the basic components of research and development. Similarly, natural products are chemically tailored and modified based upon their structural and biological properties. To some extent, the modification of natural products is quite different from de novo structure-based drug discovery. This review describes the general strategies and principles for the modification of natural products to drugs, as illustrated by several successful medicines that originated from natural products.     

天然产物促进药物发现（英文）

Natural products or natural product derived drugs comprised 32% of small molecule approved drugs between 1981 and 2010.In the same period of time,16% of small molecule approved drugs were synthetic or natural mimics based on the study of pharmacophores related to natural products.Indisputably,natural products provide diverse structural diversity and intricate carboskeletal frameworks.As it is believed that nature has evolved optimized biologically active compounds-the secondary metabolites-to ensure survival of the species that produce them,natural products are perceived by some to be more′drug-like′than totally synthetic compounds.As such,natural products may provide us with the′best′lead compounds yet for drug discovery,giving rise to natural product inspired drug design.This talk will provide an overview of some of my research in this area.Specifically,I will outline the challenges and some of the lessons learnt in this quest to develop natural products as leads to potential drugs.     

6个小分子海洋药物的全合成方法

骨架新颖、活性独特的海洋天然产物是药物先导化合物的重要来源,但由于海洋样品采集困难、一些高活性天然产物在海洋生物体中含量低微,往往难以获取足够量的化合物进行后续药物的深入研究,成为海洋小分子药物研究的瓶颈之一。现代有机合成尤其是海洋天然产物全合成的迅猛发展,为获取复杂小分子海洋活性天然产物提供了一个重要手段。探究复杂小分子海洋天然产物合成的新策略和新方法,建立高效、高选择性的规模化制备技术,是国际海洋药物研究的热点。本文就6个上市的小分子海洋药物的全合成研究作一概述,重点阐述有机合成对于成药分子规模化制备的途径。     

Current strategies for drug discovery through natural products

Importance to the field: Natural products are the most consistently successful source of drug leads, both historically and currently. Despite this, the use of natural products in industrial drug discovery has fallen out of favour. Natural products are likely to continue to be sources of new commercially viable drug leads because the chemical novelty associated with natural products is higher than that of any other source: this is particularly important when searching for lead molecules against newly discovered targets for which there are no known small molecule leads. Areas to be covered: Current drug discovery strategies involving natural products are described in three sections: developments from traditionally used medicines, random testing of natural compounds on biological assays and use of virtual screening techniques with structures of natural products. What the reader will gain: The reader will gain an insight into the potential for natural products in current drug discovery paradigms, particularly in the value of using natural products in virtual screening approaches. Take home message: Drug discovery would be enriched if fuller use was made of the chemistry of natural products.     

Nature's bounty – drug discovery from the sea

With ～ 40 years of research completed after the development of self-contained underwater breathing apparatus, drug discovery opportunities in the sea are still too numerous to count. Since the FDA approval of the direct-from-the-sea calcium channel blocker ziconotide, marine natural products have been validated as a source for new medicines. However, the demand for natural products is extremely high due to the development of high-throughput assays and this bottleneck has created the need for an intense focus on increasing the rate of isolating and elucidating the structures of new bioactive secondary metabolites. In addition to highlighting the drug discovery potential of the marine environment, this review discusses several of the pressing needs to increase the rate of drug discovery in marine natural products, and describes some of the work and new technologies that are contributing in this regard.     

Recent developments in antibacterial drug discovery: microbe-derived natural products – from collection to the clinic

The pharmaceutical industry has historically relied on nature to provide compounds for antibacterial drug discovery. In recent years, several pharmaceutical companies have scaled back their efforts in natural product research. Nevertheless, the screening of natural products for antibacterial activity continues to provide excellent sources of biologically and chemically informative leads for new drugs. New technologies in high-throughput cultivation, genetic approaches to biodiversity and discovery of relatively untapped sources of natural products are expanding the ability to find novel, potent and highly selective antibacterial structures. Advances in purification, dereplication and structure elucidation, combined with the ability to chemically or biologically derivatise hits, aim to make the timeline for natural product-derived drug discovery similar or shorter than that expected for small synthetic molecules. This review addresses the strengths and shortcomings of technologies focused on microbe-derived natural products for antibacterial drug discovery and stresses the need for commitment to these approaches in order to achieve the goal of delivering safe, efficacious and high-quality medicines in the long run.