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.     

海洋天然产物研究与新药开发

近年来海洋天然产物越来越引起科学家们的关注。在浩瀚的海洋中存在着大量超乎人们想象的化学结构新颖、生物活性多样、作用机制独特的次生代谢产物。海洋天然产物已成为发现重要先导药物的主要源泉。本文主要探讨近年来发现的重要的海洋天然活性产物以及在新药开发中所起的作用。     

Eudistomin类海洋生物碱的研究进展

海洋是一个巨大的天然产物宝库。海洋生物不同于陆地生物 ,它们生活在高盐、高压、缺氧和缺少光照的特殊环境中 ,在其生长和代谢过程中 ,产生并积累了大量具有特殊化学结构和独特生理活性的物质。海洋天然产物是寻找新药的重要资源。从上世纪 6 0年代起 ,世界各国便开始了海洋生物活性物质的研究。从海洋植物、动物、真菌和微生物中分离得到了大量结构各异的天然产物 ,它们的主要生物活性表现在抗肿瘤、抗菌、抗病毒和抗心脑血管病等方面。在过去的几十年间 ,大约 6 0 0 0多种海洋天然产物被发现 ,其中有重要生物活性并已申请专利的新化合物…     

海洋天然产物对抗阿尔茨海默症的研究进展

阿尔茨海默症（AD）是老年人群发病率最高的神经退行性疾病,在老龄人口日益增多的现代社会引发严重经济和社会问题。但目前尚无治疗AD特效药物,现有药物仅能减轻AD症状,无法对因治疗。海洋生物数量庞大,能产生大量结构独特的天然产物,部分化合物具有神经保护作用,可能用于AD治疗。尤其是藻类来源的甘露寡糖二酸GV971已完成抗AD临床III期实验,是近十年最接近成功的抗AD药物,这一海洋来源的“中国新药”可能为全球AD患者提供新的希望。本文分类综述了从不同海洋生物,包括动物、植物及其他生物中提取的具有抗AD潜力的海洋天然产物的作用机理,以期为抗AD海洋天然药物开发提供参考。     

生物活性的海洋天然产物

开发源自海洋的生物活性化合物作为医药决不是什么新的想法.中国人利用海藻治疗许多严重的疾病至少已有千余年的历史了,但是在西方系统地、科学地寻找这样的海洋天然产物,或称为源自海洋的药物,大概是由耶鲁大学Bergmann在五十年代开始的.作者从1974年起致力于海洋机体的抗微生物活性物质分布的考察,随后又开展了抗肿瘤和抗病毒活性物质的研究.现在已有许多学者开创了源自海洋机体的心肌调节活性、抗炎症活性以及免疫调节活性的物质研究.     

海洋天然抗肿瘤活性产物的临床研究现状

海洋特殊的生态系统是天然抗肿瘤活性物质的重要来源之一,许多源于海洋生物的抗肿瘤活性化合物已经进入临床研究阶段。简要介绍海洋天然抗肿瘤活性产物的作用机制,综述新近发现的海洋天然抗肿瘤活性化合物的最新临床研究进展。     

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。     

海洋天然产物Avarol及其衍生物的药理活性研究进展

自贪婪倔海绵Dysidea avara中分离的海洋天然产物avarol及其衍生物avarone具有多种药理活性。其抗肿瘤活性极为显著且治疗效果与环磷酰胺、柔红霉素及氨甲蝶呤相似；抗HIV活性与AZT相似；而醛糖还原酶抑制活性与sorbinil接近。鉴于avarol及avarone的抗HIV活性，又具有免疫调节及毒性低的特点，可望开发为新型的治疗艾滋病药物。     

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。     

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。     

海洋抗癌活性物质最新研究概况

分类简要概述近年来源自海洋生物抗肿瘤药物的最新研究与开发,其中包括肽类、大环内酯类、生物碱类、萜类、多聚乙酰类、多烯醚类等。海洋抗癌活性物质在海洋天然产物研究中占据重要地位,大多具有新结构和新作用机制,其中许多化合物作为抗癌药物已进入临床前及临床研究阶段。     

Drug discovery from natural sources

Organic compounds from terrestrial and marine organisms have extensive past and present use in the treatment of many diseases and serve as compounds of interest both in their natural form and as templates for synthetic modification. Over 20 new drugs launched on the market between 2000 and 2005, originating from terrestrial plants, terrestrial microorganisms, marine organisms, and terrestrial vertebrates and invertebrates, are described. These approved substances, representative of very wide chemical diversity, together with several other natural products or their analogs undergoing clinical trials, continue to demonstrate the importance of compounds from natural sources in modern drug discovery efforts.     

Potential matrix metalloproteinase inhibitors from edible marine algae: A review

Matrix metalloproteinases are endopeptidases which belong to the group of metalloproteinases that contribute for the extra-cellular matrix degradation, and several tissue remodeling processes. An imbalance in the regulation of these endopeptidases eventually leads to several severe pathological complications like cancers, cardiac, cartilage, and neurological related diseases. Hence inhibitory substances of metalloproteinases (MMPIs) could prove beneficial in the management of above specified pathological conditions. The available synthetic MMPIs that have been reported until now have few shortcomings and thus many of them could not make to the final clinical trials. Hence a growing interest among researchers on screening of MMPIs from different natural resources is evident and especially natural products from marine origin. As there has been an unparalleled contribution of several biologically active compounds from marine resources that have shown profound applications in nutraceuticals, cosmeceuticals, and pharmaceuticals, we have attempted to discuss the various MMPIs from edible sea-weeds.     

Marine bacteria and fungi as promising source for new antibiotics

Natural products and derivatives thereof are of considerable importance in the discovery of new pharmaceuticals, for example, for the treatment of cancer, diabetes, inflammation diseases, and infection diseases caused by bacteria, fungi, viruses, or parasites. The great biodiversity of marine microorganisms is reflected in their huge chemical diversity, which provides a rich source of biologically active compounds. An increasing interest in marine microorganisms as promising producers of new compounds with potential medical applications has raised increasing interest in the sustainable exploration of marine microbial resources for the discovery of new antibiotics, which is highlighted. The bottlenecks in the development of drugs using the large marine natural product pipeline are also discussed.     

海洋天然活性物质心血管药理作用的研究进展

从30多年来国内外学者在海洋生物天然活性物质的研究中，对具心血管药理作用的活性产物作系统、概括的报道。从1968年以来获得的55种海洋生物活性物质，对每一种天然产物分别概括其来源、化学成分，并重点阐述其心血管方面的药理作用。系统报道这些海洋天然活性物质的研究成果及进展，对进一步开展海洋心血管药物的研发提供参考。     

Chemistry and biology of new marine alkaloids from the indole and annelated indole series

Chemistry and biology of marine natural products from the indole and annelated indole series have become an attractive research field for development of new pharmacological lead substances. In the past years some of the isolated natural organic compounds were synthesized by chemists and evaluated with great enthusiasm to find new lead natural compounds against different diseases. In this review the latest results for new compounds including isolation, biological evaluation, synthetic pathways and some retrosynthetic analyses are summarized.     

藻类生物活性物质在化妆品中的应用

随着化妆品行业的迅猛发展以及人们对美的追求,天然温和、绿色安全的环境友好型化妆品已经成为广大消费者的诉求.消费者更青睐于以天然产物为基础的化妆品,而不是合成化学品.随着天然产物化学和海洋生物资源技术的迅速发展,藻类(包括大型藻和微藻)生物活性物质已得到了广泛的应用.许多研究已经证明藻类活性物质具有保湿补水、抗氧化、抗衰...     

海洋放线菌次级代谢产物及其抗菌、抗病毒、抗肿瘤活性研究进展

放线菌是发现大量药用天然产物的资源宝库,在微生物新药研究中占据着十分重要的地位。海洋放线菌生活环境特殊造就了其不同于陆地微生物独特的代谢途径,具有产生多种生物活性物质的潜力,是天然药用活性先导化合物的重要来源。从不同海洋生境来源放线菌的次级代谢产物中寻找生物活性物质已成为近年来的研究热点。目前已经分离到许多结构新颖、活性显著的化合物,为新药的研究提供了丰富的物质基础。本文主要对近3年（2015～2017）不同海洋生境来源且具有明显抗菌、抗病毒、抗肿瘤生物活性的放线菌次级代谢产物进行综述。     

Recent advances in the synthesis of marine polycyclic ether natural products

For more than twenty years, chemists and biologists have been fascinated by the highly complex molecular architectures and the diverse and potent biological activities of marine polycyclic ether natural products. Given the scarce availability of these intriguing substances from natural sources, total chemical synthesis is the only way to obtain sufficient quantities for biological investigation. This review describes recent synthetic advances in the field of marine polycyclic ether natural products and their successful implementation in total synthesis endeavors.     

The use of marine-derived bioactive compounds as potential hepatoprotective agents

The marine environment may be explored as a rich source for novel drugs. A number of marine-derived compounds have been isolated and identified, and their therapeutic effects and pharmacological profiles are characterized. In the present review, we highlight the recent studies using marine compounds as potential hepatoprotective agents for the treatment of liver fibrotic diseases and discuss the proposed mechanisms of their activities. In addition, we discuss the significance of similar studies in Oman, where the rich marine life provides a potential for the isolation of novel natural, bioactive products that display therapeutic effects on liver diseases.