海洋抗病毒活性的小分子化合物研究概况

海洋是具有生物活性多样性的天然产物宝库,近年来从海藻、海绵、海鞘、珊瑚、海洋微生物等多种海洋生物中陆续发现了大量的具有抗病毒活性的新次生代谢产物,结构类型包括了萜类、甾体、生物碱、肽类、大环内酯和脂肪酸衍生物等,许多化合物的结构十分特异。本文对来自海洋具有抗病毒活性的小分子化合物进行了综述,为抗病毒药物的研发提供可借鉴的先导化合物。     

海洋真菌活性代谢产物研究进展

海洋真菌由于其资源优势和新颖的代谢产物,成为海洋天然活性物质的研究热点。按照萜类、生物碱、甾体、醌类、香豆素、肽类和抗生素等主要成分类型对近5年来海洋真菌的生物活性代谢产物国内外研究简况加以综述。     

天然产物中抗HIV生物碱类化合物的研究进展

近年来,从天然产物中寻找高效低毒的先导化合物已成筛选抗HIV药物的重要研究方向。生物碱类化合物作为一类重要的天然产物,数量众多,结构类型复杂,其中有多种抑制和阻断HIV感染的有效成分,通过实验室研究工作和临床用药观察,有望从中获得抗HIV的有效药物。以生物碱类化合物的化学结构为基础,将生物碱类化合物分为异喹啉类、喹啉类、大环类、哌啶类、莨菪烷类、吲哚类、咔唑类、海洋多环胍类、萜类、manzamine型生物碱等10类,对其抗HIV活性进行综述。     

珊瑚及其共生菌来源的生物碱类物质的研究进展

珊瑚及其共生菌能产生大量结构新颖功能多样的生物碱,是药物先导化合物的重要来源之一。生物碱是一类重要的天然药物,临床广泛用于镇痛、抗菌和抗肿瘤等。本文综述海洋生物碱的开发现状及近五年珊瑚来源的生物碱类物质。     

海鞘微生物来源活性次级代谢产物研究进展

海鞘作为海洋药物的重要源泉,从中分离的8%的活性化合物被认为源自其共附生微生物。近年来,海鞘微生物来源次级代谢产物因其新颖的化学结构和显著活性而逐渐受到关注,在海洋药物研发中具有广阔的前景。本文综述了1994~2022年初报道的150个新的海鞘微生物天然产物的来源、化学结构及其生物活性,结构类型主要包括聚酮类、生物碱类、萜类和肽类等,并展望了海鞘微生物天然产物的发展方向。     

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。     

海洋来源Neolamellarin A类似物的神经保护活性

目的 生物碱是自然界中普遍存在的一类含氮的碱性有机化合物,其中海洋生物碱因具有广泛的生物活性而受到极大关注。Neolamellarin A是一种来源于海洋动物海绵并具有新颖吡咯类骨架的生物碱。作者认为人们对Neolamellarin A类生物碱的生物活性的认识有限,希望可以通过更多的活性研究对其加以全面的开发。方法 采用细胞毒活性检测（MTT法）及神经细胞保护模型对五中新颖Neolamellarin A的3,4二芳基取代全甲基化类似物进行检测。结果 发现该类3,4二芳基取代全甲基化的Neolamellarin A类似物较弱的细胞毒活性和突出的神经保护活性。结论 实验结果扩展了该类Neolamellarin A类似物潜在的应用方向并丰富了海洋生物碱的生物功能。     

活性天然醛类化合物药理活性研究进展

天然醛类化合物种类繁多,主要包括萜类、苯丙素类、皂苷类以及生物碱等。目前已发现多种结构独特天然醛类化合物具有明显的抗肿瘤,抗炎,抑菌以及神经系统活性等,本文对这些天然醛类化合物的结构和药理活性进行综述,以期为今后该类化合物的开发利用提供参考。     

天然生物碱及衍生物抗肿瘤机制研究进展

生物碱是存在于中草药中的主要抗肿瘤活性成分之一,近年来天然生物碱及衍生物的抗肿瘤机制研究取得了较大进展。特别是在缺氧诱导因子-1、端粒酶、拓扑异构酶等作用靶点上取得的新进展,该文主要就这3个靶点进行综述。     

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。     

新药研究与开发的发展动态概述

从基础研究到制药企业开发全方位视角,对近期新药研发的发展与动态进行综述,并对今后药物研发进行了展望。源于天然植物的药物开发历史悠久且富有生命力;利用生物技术从动物毒液组分进行新药研究正在取得成效;化学合成药物仍是新药开发重要途径,但周期长、成本高;利用已有药物再开发获得新用途是快捷新药开发的一个方向。     

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.     

来源于海洋链霉菌属的宜他霉素

如今,医院（HA）相关型和社区（CA）相关型的耐甲氧西林金黄色葡萄球菌（MRSA）的大量出现使人们不顾一切地去寻找有效的新型抗生素。然而,陆地资源的减少,使人们将目光转向了有待开发的海洋资源。在浩瀚的海洋中存在着大量令人激动、活性独特、结构新颖的次级代谢产物,它们已成为发现重要先导药物和新的生物作用机制的主要源泉。本文将综述来源于海洋链霉菌属放线菌CNS-575且具有很强抗MRSA活性的宜他霉素,主要从其来源、化学性质、结构、活性以及未来开发价值进行论述。     

天然产物抗氧化活性成分研究进展

天然产物抗氧化剂在自然界有广泛的分布,研究表明多糖、黄酮、多酚、生物碱、皂苷、维生素等天然产物均能有效清除自由基以保护机体健康。随着人们回归自然思潮的兴起及安全意识的提高,天然抗氧化剂因其高效、低毒更是倍受关注。从天然产物中寻找新的清除体内自由基的抗氧化剂已成为现代医药、保健行业发展的必然趋势。综述了天然产物抗氧化活性成分的研究进展,以期为天然产物抗氧化活性的研究和发展提供参考。     

The future of natural products as a source of new antibiotics

One reason for the current crisis in antibiotic development is the low return on investment, which is intrinsic to anti-infective drug development. Despite this, smaller pharmaceutical companies are attempting to address the medical need for new antibiotics. Natural products have played a major role in antibiotic drug discovery since 1941 when penicillin was introduced to the market, and currently natural products are again the most important source for promising drug candidates. This review discusses novel methods and technologies that will increase the success rate for identifying novel antibiotics from natural sources.     

Biosynthetic engineering of natural products for lead optimization and development

It is now possible to rapidly and rationally modify, at a genetic level, the machinery responsible for natural product biosynthesis. This provides the opportunity to design new structures and to optimize natural product lead compounds in a way that would be extremely difficult through synthetic chemistry means alone. The technology can also be used to overcome limitations of compound supply, which might otherwise preclude natural products from progressing into clinical trials. Described herein are some recent examples which highlight how biosynthetic engineering has been applied to drug discovery and development, and which attempt, in particular, to demonstrate how the technology functions most effectively when combined with synthetic organic and medicinal chemistry.     

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.     

Self-assembled small molecule natural product gel for drug delivery: a breakthrough in new application of small molecule natural products

Natural products, as a gift of nature to humanity, have long been used as drugs or pharmacological actives to help people cure various diseases. Yet we still know comparatively little about their ability to be materials. In recent years, some small molecule natural products isolated from traditional Chinese medicines have been found to have new features, namely, self-assembly to form gels (i.e., natural product gels, NPG). However, the application development of these natural products is seriously lacking, which greatly weakens their practical value and delays the maturity of the field. Here, a series of self-assembled triterpenoid natural products are used as materials (gel scaffolds) to construct drug delivery systems. Surprisingly, these NPG not only exhibit the excellent self-healing, controlled gelation, good safety and sustained release, but also achieve synergistic treatment of tumors through bioactive natural products. Compared with non-bioactive gel scaffolds, NPG scaffolds show great advantages in tumor therapy, including optimal tumor inhibition, preferable health, better body recovery, stronger immune function, less toxic side effects and longer survival. The successful construction of NPG scaffolds not only takes full advantage of the self-assembled natural products, but also takes an important step in the development of new applications for natural products.     

苜蓿素生物活性研究进展

苜蓿素为天然黄酮类化合物，广泛存在许多天然可食性植物中，其生物活性主要有抗炎、抗氧化应激、抗过敏、抗肿瘤、抑制微生物生长（巨细胞病毒、利什曼虫和胃肠道线虫）、降血糖和降血脂等作用，且安全性好，可成为新药开发的方向。本文综述近些年国内外文献，对苜蓿素的生物学活性及其作用机制的研究现状作一总结，为新药开发提供理论依据。     

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。