海洋天然产物的检测筛选

海洋天然产物在人类医学上的应用或更确切地说其潜在的用途已引起人们广泛关注.80年代以来对来源于海洋的药物筛选无论在工业或学术上均引起人们极大兴趣.涌现了一类专业公司——海洋药学公司,完全致力于源于海洋的药物筛选研究.     

天然药物化学教学改革与实践

天然药物化学是运用现代科学理论与方法研究天然药物中化学成分的一门学科。其研究内容包括各类天然药物的化学成分（主要是生理活性成分或药效部分）的结构特点、物理化学性质、提取分离方法以及主要类型化学成分的结构鉴定等［1、2］,是药学专业开设的一门重要专业必修课,其研究对象包括植物、动物及微生物,近年来,海洋生物的研究也发展迅速。由于天然产物大多化学结构复杂、理化性质多样、结构鉴定繁琐,是师生公认的药学专业最难课程之一。为适应教育现代化及教学改革要求,培养具有创新能力的人才,作者通过借鉴同行的先进教学经验［3~7］,结合自身的教学体会,对本校药学专业的天然药物化学理论课程进行改革,现报道如下。     

《天然药物化学》课程教学改革的探讨

天然药物化学是运用现代科学理论和技术方法研究天然产物中化学成分的一门学科,是高等医药院校药学类专业的一门必修课,在整个药学教育体系中具有十分重要的作用和地位。随着我国药学事业的飞速发展以及中药现代化的实施,《天然药物化学》课程显得更加重要。为了使学生更好的掌握这门课程,达到药学专业的培养目标,这要求我们教师必须更新教育观念,不断更新教学内容,改进教学方法和思路,尽可能的增加信息量,提高《天然药物化学》的教学质量。在几年的教学改革实践中,我们收到了较好的教学效果,在这里仅做一些探讨。     

棘皮动物天然产物的研究进展

海洋中存在大量具特殊化学结构且有独特生理活性和功能的物质,是开发新型药物和功能食品的巨大天然产物宝库.棘皮动物是海洋药物和功能食品研究的一大重点,本文分海星纲、海参纲和海胆纲三个部分对其天然产物的研究进展加以综述,并对其发展前景做进一步的分析与展望.     

《中国天然药物》杂志2020年征订启事

《中国天然药物》(Chinese Journal of Natural Medicines,CJNM)是由中国药科大学与中国药学会共同主办、科学出版社出版的国家级药学学术期刊,刊物以报道来自天然产物活性化合物的发现与研究,其药效与药理作用机制为重点,内容包括中药与天然药物的分离鉴定/活性筛选、药理学机制研究、生化与微生物药学、药物分析与药代动力学、天然药物资源等,是具有我国独特优势的中药、草药、海洋药物、微生物药物、生化药物、民族药物进行国际交流的重要窗口。     

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。     

海洋拟诺卡菌来源的天然产物

海洋拟诺卡菌由于其独特的代谢功能，成为海洋放线菌次级代谢产物的重要来源。根据2010-2013年初的海洋放线菌天然产物的统计表明，对拟诺卡菌的研究仅次于链霉菌。本文综述了从2001年的第一个海洋来源的拟诺卡菌天然产物至2018年6月17年间报道的65个海洋拟诺卡菌天然产物的微生物来源、结构及其生物活性。其结构包括吡喃酮类、二酮哌嗪类、多肽类等，其中吡喃酮类化合物是主要类型，占海洋拟诺卡菌天然产物总数的46%；而29%的海洋拟诺卡菌天然产物表现出抑菌、细胞毒、抗炎等生物活性。     

海洋卤化天然产物研究进展

卤化天然产物是一类常见的次级代谢产物,在医药研发领域占有重要地位。卤素的存在通常可以增强化合物的生物活性。海洋是卤化天然产物的主要来源。这些卤化物由海绵、海藻、珊瑚、真菌和细菌等生物产生。文章按照化合物中卤素原子的不同综述了近十年（2012年-2022年3月）181个海洋来源卤化天然产物及其抗菌、抗抗肿瘤和抗污等生物活性的研究进展。     

天然产物化学研究现状

近年来随着科学技术的飞速发展以及人们对自然资源的开发,利用不断广泛和深入,天然产物化学的研究引起了世界各地药学家,化学家和制药企业的高度重视,每年发表的腾天然产物化学研究的报道成千上万,在有限的篇幅内综括天然产物化学的研究进展几乎是不可能的。本篇主要以近年来国内外天然产物研究取得的成果为例,概述了天然产物化学在选题和研究方向,样品的搜集和筛选,资源保护,分离分析技术,结构鉴定,生物合成,活性评价等     

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。     

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.     

抗肿瘤天然药物的研究概况

目的介绍近年来一些抗肿瘤天然药物的研究概况。方法综合最新国内外文献报道,总结抗肿瘤天然药物的研究近况。结果一些抗肿瘤天然药物及其衍生物的研究取得很大进展。结论从天然活性产物中寻找开发抗肿瘤新药具有重要意义。     

Natural Products as a Resource for New Drugs

Natural products have served as a major source of drugs for centuries, and about half of the pharmaceuticals in use today are derived from natural products. The aim of this review is to provide an overview of the continuing central role of natural products in the discovery and development of new pharmaceuticals. In this context, selected examples of important natural product-derived drugs are cited, focusing on some of the most recent introductions to the clinical setting, and a brief overview of some of the important recent developments and remaining challenges in the process of discovering and developing bioactive natural products is provided. Interest in natural products research is strong and can be attributed to several factors, including unmet therapeutic needs, the remarkable diversity of both chemical structures and biological activities of naturally occurring secondary metabolites, the utility of bioactive natural products as biochemical and molecular probes, the development of novel and sensitive techniques to detect biologically active natural products, improved techniques to isolate, purify, and structurally characterize these active constituents, and advances in solving the demand for supply of complex natural products. Opportunities for multidisciplinary research that joins the forces of natural products chemistry, molecular and cellular biology, synthetic and analytical chemistry, biochemistry, and pharmacology to exploit the vast diversity of chemical structures and biological activities of natural products are discussed.     

Cheminformatics analysis of natural products and indication distribution prediction

As a valuable resource for drug discovery, natural products remain largely unexplored. The cheminformatics analysis of natural product databases could help us know better about natural products, providing valuable information in drug design. In this study, we collected an in-home natural product library consisting of more than 220 000 molecules. The results showed that natural products were distributed more diversely than synthetic compounds and approved drugs in chemical space, and natural products still possessed better scaffold diversity. Besides, natural product scaffolds had more potential in some specific indications, such as antiarthritic, antihypertensive, antiallergic and analgesic. However, the utilization rate of natural product scaffolds is relatively low, especially in terms of potential indications. Therefore, we recommend the greater use of natural products while designing lead libraries.     

Nucleoside natural products and related analogs with potential therapeutic properties as antibacterial and antiviral agents

Nucleoside natural products possess a variety of interesting biological activities, including antibacterial, antiviral and antitumor properties, and are therefore expected to be potential candidates for developing drugs. Complex nucleoside natural products exhibiting antibacterial activity by specific inhibition of bacterial cell wall peptidoglycan biosynthesis are described. In addition to the class of antibacterial nucleoside natural products, the newest members of nucleoside natural products exhibiting interesting antiviral activity are briefly described. In spite of promising properties, no nucleoside natural products and their analogs are presently used in the clinic. A global structure–activity relationship of these classes of nucleoside natural products clearly indicates that it is very important to: i) modulate the cell entry ability; and ii) simplify hydrophilic core structures in order to reduce the size of molecules and stabilize the chemically labile structure.     

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.     

Update on natural product--drug interactions.

The interactions of natural products with drugs are discussed. Interactions between natural products and drugs are based on the same pharmacokinetic and pharmacodynamic principles as drug-drug interactions. Clinically important interactions appear to involve effects on drug metabolism via cytochrome P-450 isoenzymes, impairment of hepatic or renal function, and other possible mechanisms. Natural products that have been reported to interact with drugs in humans include coenzyme Q10, dong quai, ephedra, Ginkgo biloba, ginseng, glucosamine sulfate, ipriflavone, melatonin, and St. John's wort. In many cases, more research is needed to confirm these interactions and to determine whether other natural products may also interact with drugs. To effectively counsel patients about interactions involving natural products, pharmacists should be familiar with the most commonly used products and have access to information on more obscure products. In view of the less than stringent provisions of the Dietary Supplement Health and Education Act, pharmacists should consult reliable, independent sources of information on natural products rather than rely on literature provided by manufacturers. Pharmacists should recommend only those products that are manufactured to high quality-control standards. Natural products can interact with drugs and with other natural products by the same mechanisms as drugs.     

Antineoplastic agents from natural sources: achievements and future directions

The influence of natural products upon anticancer drug discovery and design cannot be overestimated. Approximately 60% of all drugs now in clinical trials for the multiplicity of cancers are either natural products, compounds derived from natural products, contain pharmacophores derived from active natural products or are 'old drugs in new clothes', where (modified) natural products are attached to targeting systems. This review covers those materials that the authors are aware of as being in clinical trials through early 2000 and demonstrates how, even today, in the presence of massive numbers of agents from combinatorial libraries, the compounds produced by 'Mother Nature' are still in the forefront of cancer chemotherapeutics as sources of active chemotypes.     

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.     

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.