天然产物的生物转化

本文按反应类型综述了近五年来天然产物生物转化的研究进展,并对生物技术干预下的生物转化作了简要介绍.     

Plant-Cell Culture: Natural Products and Industrial Application

Abstract

Reporter gene assay is an invaluable tool for both biomedical and pharmaceutical researches to monitor cellular events associated with gene expression, regulation and signal transduction. On the basis of the alternations in reporter gene activities mediated by attaching response elements to these reporter genes, one sensitive, reliable and convenient assay can be provided to efficiently report the activation of particular messenger cascades and their effects on gene expression and regulations inside cells or living subjects. In this review, we introduce the current status of several commonly used reporter genes such as chloramphenicol acetyltransferase (CAT), alkaline phos-phatase (AP), β-galactosidase (β-gal), luciferases, green fuorescent protein (GFP), and β-lactamase. Their applications in monitoring gene expression and regulations in vitro and in vivo will be summarized. With the development of advanced technology in gene expression and optical imaging modalities, reporter genes will become increasingly important in real-time detection of the gene expression at the single-cell level. This synergy will make it possible to understand the molecular basis of diseases, track the effectiveness of pharmaceuticals, monitor the response to therapies and evaluate the development process of new drugs.     

植物内生真菌抗肿瘤活性代谢产物研究进展

癌症已成为全球头号杀手,迫切需要从自然界寻找更新、更有效的抗肿瘤药物。植物内生真菌是指生活在宿主植物体内,不会对宿主植物组织引起明显病害症状的一类真菌。众多研究表明,植物内生真菌在寻找抗肿瘤药物中起着至关重要的作用。随着植物内生真菌研究的深入,从植物内生真菌中寻找新的抗肿瘤活性成分已成为研究的热点。大量的抗肿瘤活性成分从植物内生真菌中分离出来,并表现出良好的抗肿瘤活性。目前,植物内生真菌抗肿瘤活性代谢产物主要有紫杉醇、喜树碱、长春新碱,鬼臼毒素等等,本文主要对近年来植物内生真菌抗肿瘤活性成分的研究进展进行了综述。     

天然产物抗病毒活性成分的研究进展

按照化学成分结构类型的不同,将近五年来具有抗病毒活性的天然产物研究近况做一综述,旨为以天然产物为研究对象,大力开展开发抗病毒药物提供依据。     

塞克肽类(Sactipeptide)天然产物的研究进展

塞克肽是一类重要的核糖体肽天然产物,具有多种生物活性,它们的共同特征是存在由半胱氨酸巯基与受体氨基的α-碳原子连接的分子内硫醚键.本篇综述总结了近年来塞克肽的发现、活性、生物合成、作用机制等多方面的工作,详细讨论了由SAM自由基酶介导的硫醚键形成机制.     

Marine Natural Products: The Important Resource of Biological Insecticide

Due to the unique environmental conditions and vast territory, marine habitat breeds more abundant biological resources than terrestrial environment. Massive marine biological species provide valuable resources for obtaining a large number of natural products with diverse structure and excellent activity. In recent years, new breakthroughs have been made in the application of marine natural products in drug development. In addition, the use of marine natural products to develop insecticides and other pesticide products has also been widely concerned. Targeting marine plants, animals, and microorganisms, we have collected information on marine natural products with insecticidal activity for nearly decade, including alkaloids, terpenes, flavonoids and phenols fatty acids, peptides, and proteins, et al. In addition, some active crude extracts are also included. This review describes the insecticidal activities of marine natural products and their broad applications for future research in agriculture and health.     

Evaluation of Natural Products for Algicidal Properties

A procedure for the screening of antialgal substances has been described and evaluated with specific reference to microbial products. Data on the extracellular materials of 545 actinomycete and fungal isolates showed a wide distribution of agents having algicidal activities. Of these culture filtrates, 20.4% apparently had selective antagonistic effects against particular algal groups. A more comprehensive examination revealed that metabolic products from two actinomycete cultures exhibited properties that warrant further studies on their chemical and physiological characteristics.     

The Natural Products and Extracts: Anti-Triple-Negative Breast Cancer in Vitro

Triple-negative breast cancer (TNBC) makes up 15 % to 20 % of all breast cancer (BC) cases, and represents one of the most challenging malignancies to treat. For many years, chemotherapy has been the main treatment option for TNBC. Natural products isolated from marine organisms and terrestrial organisms with great structural diversity and high biochemical specificity form a compound library for the assessment and discovery of new drugs. In this review, we mainly focused on natural compounds and extracts (from marine and terrestrial environments) with strong anti-TNBC activities (IC₅₀<100 μM) and their possible mechanisms reported in the past six years (2015–2021).     

天然多羟基化合物在酶催化下的选择性酯化

综述了近十几年来几种天然多羟基化合物包括皂草苷类、黄酮苷类、生物碱类、甾醇类、倍半萜(烯)化合物、熊果苷和槐糖脂在脂肪酶和枯草杆菌蛋白酶催化下的选择性酯化。     

天然产物在新药开发中的应用--HMG-CoA还原酶抑制剂新药的发现对天然产物研究与开发的启示

自1973年发现第一个作用于HMG-CoA还原酶的化合物mevastatin以来,多个具有HMG-CoA还原酶抑制活性的抗高血脂新药被开发成功,并成为治疗高血脂症的首选药物。在此简单介绍该类新药的发现与开发过程,并就天然产物的研究与开发提出一点个人见解。     

天然产物的C-糖基化研究进展

自然界中的天然产物在其结构上存在各种修饰,C-糖基化为其中一种比较稀少的修饰方式.C-C糖苷键的形成由C-糖基转移酶负责催化.含C-糖基的化合物多数来自微生物,但高等植物也会有少量积累.综述了近些年来在天然产物C-糖基化方面的研究工作,并对其在药物开发方面的潜力进行了展望.     

Natural Products in High Throughput Screening: Automated High-Quality Sample Preparation

At present, compound libraries from combinatorial chemistry are the major source for high throughput screening (HTS) programs in drug discovery. On the other hand, nature has been proven to be an outstanding source for new and innovative drugs. Secondary metabolites from plants, animals, and microorganisms show a striking structural diversity that supplements chemically synthesized compounds or libraries in drug discovery programs. Unfortunately, extracts from natural sources are usually complex mixtures of compounds, often generated in time-consuming and, for the most part, manual processes. Because quality and quantity of the provided samples play a pivotal role in the success of HTS programs, this poses serious problems. In order to make samples of natural origin competitive with synthetic compound libraries, we devised a novel, automated sample preparation procedure based on solid-phase extraction (SPE). By making use of modified Zymark (Hopkinton, MA) RapidTrace? SPE workstations, we developed an easy-to-handle and effective fractionation method that generates high-quality samples from natural origin, fulfilling the requirements for an integration in high throughput drug discovery programs.