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Editorial [Hot topic: Natural Products (Guest Editors: Wei-Shuo Fang and Junzeng Zhang)]

机译:社论[热门话题:天然产品(来宾编辑:方伟硕和张俊增)

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Natural products have been used for thousands of years in human history for prevention and treatment of diseases, or for maintaining general wellness. Bioactive natural products are also the important sources of many current therapeutic agents, either in original forms or derivatives made from the natural lead compounds. During the past decades, new tools and strategies such as the combinatorial chemistry, high-throughput screening and computer-aided drug design have been introduced into drug discovery and development process and this certainly helps accelerating the pre-clinical studies in pharmaceutical industry. On the other hand, however, pharmaceutical industry is still in great need of the unique chemical diversity and biological relevancy observed in the natural products, resulting from millions of years' evolution.nnThe chemical diversity of natural products comes from the biodiversity of organisms on earth. As such, the topics for these two themed issues on bioactive natural products (issues 16 and 17) would reflect this type of diversity and cover natural products from microbes to higher plants and from marine to terrestrial environment. As a continuation to issue 16, we are delighted to offer the CTMC readers another five reviews as follows.nnFor the microbe-derived natural products, Zhan provided overview on the recent progress in biosynthesis research of bioactive aromatic polyketides from microorganisms with a focus on new enzymes or methods used in building the novel polyketide biosynthetic machinery.nnNatural products and herbal remedies for treatment of allergic inflammation, such as allergic rhinitis are reviewed by Kulka with discussions on their molecular mechanisms. This unique pharmacological perspective of bioactive natural products emphasizes the importance of biological activity - novel chemical structure is exciting, but new therapeutical applications are equally valuable.nnBioactive natural products are important lead for drug discovery, and many therapeutic agents actually come from the chemical derivation and synthesis based on the natural leads. Dai provided in-depth coverage on a chemo-enzymatic transformation of taxanes, and the reversal activity towards multidrug resistance (MDR) tumor cells. These works demonstrate a powerful approach for natural products-based lead compound discovery by combining biotransformation with chemical conversion in structure diversification of natural products. In the review by Chen, the synthesis as well as biological activity of nordihydroguaiaretic acid and its derivatives, which have been extensively explored for their potential uses in the treatment of cancers, diabetes, viral, bacterial infections, and inflammation, are comprehensively documented. In closing this issue, Chang et al. reviewed the synthesis and biological activity of Wuweizisu C and analogues, lignans from a popular Chinese medicinal herb, illustrating this successful drug discovery strategy of combining ethnopharmacological knowledge and modern medicinal chemistry technology.nnFinally, we would like to thank Dr. Allen B. Reitz, for the invitation to be the Guest Editor of this special issue. We wish to offer our sincere appreciation to all the contributors for their dedication and hard work.
机译:天然产物已在人类历史上用于预防和治疗疾病或维持总体健康已有数千年的历史。具有生物活性的天然产物还是许多当前治疗剂的重要来源,无论是原始形式还是由天然铅化合物制成的衍生物。在过去的几十年中,新的工具和策略(例如组合化学,高通量筛选和计算机辅助药物设计)已被引入到药物发现和开发过程中,这无疑有助于加速制药业的临床前研究。但是另一方面,由于数百万年的发展,制药行业仍然非常需要天然产物中观察到的独特化学多样性和生物学相关性.nn天然产物的化学多样性来自地球上生物的生物多样性。这样,有关生物活性天然产物(第16和第17期)的这两个主题问题的主题将反映这种类型的多样性,并涵盖从微生物到高等植物以及从海洋到陆地环境的天然产物。作为第16期的继续,我们很高兴为CTMC读者提供以下五条评论:nn对于微生物衍生的天然产物,詹提供了微生物在生物活性芳香族聚酮化合物的生物合成研究方面的最新进展的概述,重点是新的库尔卡(Kulka)对天然产物和用于治疗过敏性炎症(如过敏性鼻炎)的草药进行了评论,并讨论了它们的分子机制。生物活性天然产物的这种独特的药理学观点强调了生物活性的重要性-新颖的化学结构令人兴奋,但新的治疗应用同样有价值.nn生物活性天然产物是药物发现的重要线索,许多治疗剂实际上来自于化学衍生和基于天然铅的合成。 Dai对紫杉烷类化合物的化学酶转化以及对多药耐药性(MDR)肿瘤细胞的逆转活性进行了深入报道。这些工作通过将生物转化与化学转化相结合,在天然产物的结构多样化中展示了一种基于天然产物的先导化合物发现的有效方法。在Chen的评论中,已全面记录了正二氢愈创木酸及其衍生物的合成及其生物学活性,这些化合物已被广泛地探讨其在治疗癌症,糖尿病,病毒,细菌感染和炎症中的潜在用途。在结束这个问题时,Chang等人。最后回顾了来自中药材的无味子素C及其类似物木脂素的合成和生物活性,阐明了将民族药理学知识与现代药物化学技术相结合的成功的药物发现策略。最后,我们要感谢Allen B. Reitz博士,邀请成为本期特刊的特邀编辑。我们衷心感谢所有贡献者的奉献和辛勤工作。

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