Drug discovery leading to robust and viable lead candidates’ remains a challenging scientific task, which is the transition from a screening hit to a drug candidate, requires expertise and experience. Natural product...Drug discovery leading to robust and viable lead candidates’ remains a challenging scientific task, which is the transition from a screening hit to a drug candidate, requires expertise and experience. Natural products and their derivatives have been recognized for many years as a source of therapeutic agents and of structural diversity. However, in addition to their chemical structure diversity and their biodiversity, the development of new technologies has revolutionized the screening of natural products in discovering new drugs. Applying these technologies compensates for the inherent limitations of natural products and offers a unique opportunity to re-establish natural products as a major source for drug discovery. The present article attempts to describe the utilization of compounds derived from natural resources as drug candidates, with a focus on the success of these resources in the process of finding and discovering new and effective drug compounds, an approach commonly referred to as “natural product drug discovery”.展开更多
A potential strategy for drug lead identification and in-active natural products re-discovery is elaborated.Starting from fifteen structurally diverse natural products,a focused library featured by Michael acceptors i...A potential strategy for drug lead identification and in-active natural products re-discovery is elaborated.Starting from fifteen structurally diverse natural products,a focused library featured by Michael acceptors is constructed with IBX mediated oxidation.Biological assay on five tumor cell lines indicates that four Michael acceptors,8a,11a,12a,14a,are with improved cytotoxicity(3-10 folds more potent than the parent compounds),which merit further investigations.Further thiol-sensitive assay of the active hit 8a revealed that it was an irreversible Michael acceptor.The results suggest that the strategy is not only effective and relatively high discovery rate(28%),but also resource saving.展开更多
The 2022 Nobel Prize in Chemistry was awarded to American scientists Carolyn Bertozzi,K.Barry Sharpless,and Danish scientist Morten P.Merdahl for their contributions to the development of click chemistry and bioorthog...The 2022 Nobel Prize in Chemistry was awarded to American scientists Carolyn Bertozzi,K.Barry Sharpless,and Danish scientist Morten P.Merdahl for their contributions to the development of click chemistry and bioorthogonal chemistry.展开更多
我国医院信息化建设目前正逐步向数字化医院的方向发展,通过信息化建设,医院的管理者可以更多、更全面的掌握信息,使管理更加有效。本文主要介绍了射频标签(Radio Frequency Identification,RFID)技术在医院精细化管理中的作用;提出了...我国医院信息化建设目前正逐步向数字化医院的方向发展,通过信息化建设,医院的管理者可以更多、更全面的掌握信息,使管理更加有效。本文主要介绍了射频标签(Radio Frequency Identification,RFID)技术在医院精细化管理中的作用;提出了医院医疗设备精细化管理中存在的问题,研究并分析了RFID定位算法,通过实验平台测量并量化分析了射频读写器接收信号强度(Received Signal Strength Indication,RSSI)与距离以及读写器矢状面夹角之间的关系;最后,结合国内外使用RFID技术在医院管理研究进展,分析了RFID技术在定位、识别、药品防伪管理、新生儿防盗、医疗设备消毒溯源管理以及库房管理中的具体应用。展开更多
文摘Drug discovery leading to robust and viable lead candidates’ remains a challenging scientific task, which is the transition from a screening hit to a drug candidate, requires expertise and experience. Natural products and their derivatives have been recognized for many years as a source of therapeutic agents and of structural diversity. However, in addition to their chemical structure diversity and their biodiversity, the development of new technologies has revolutionized the screening of natural products in discovering new drugs. Applying these technologies compensates for the inherent limitations of natural products and offers a unique opportunity to re-establish natural products as a major source for drug discovery. The present article attempts to describe the utilization of compounds derived from natural resources as drug candidates, with a focus on the success of these resources in the process of finding and discovering new and effective drug compounds, an approach commonly referred to as “natural product drug discovery”.
基金We thanked the National Natural Science Foundation of China(No.90813004,U0932602,20802083 and 973 Program No.2009CB522303 and No.2011CB915503)the State Key Laboratory of Phytochemistry and Plant Resources in West China(P2010-ZZ18)for financial support.
文摘A potential strategy for drug lead identification and in-active natural products re-discovery is elaborated.Starting from fifteen structurally diverse natural products,a focused library featured by Michael acceptors is constructed with IBX mediated oxidation.Biological assay on five tumor cell lines indicates that four Michael acceptors,8a,11a,12a,14a,are with improved cytotoxicity(3-10 folds more potent than the parent compounds),which merit further investigations.Further thiol-sensitive assay of the active hit 8a revealed that it was an irreversible Michael acceptor.The results suggest that the strategy is not only effective and relatively high discovery rate(28%),but also resource saving.
基金supported by the Natural Science Foundation of Xinjiang Uygur Autonomous Region(No.2022D01D38)the National Natural Science Foundation of China(Nos.82173681,21977116,82104004,81973223)+1 种基金the Open Project of State Key Laboratory of Natural Medicines(No.SKLNMZZ202213)the State Key Laboratory of Pathogenesis,Prevention and Treatment of High Incidence Diseases in Central Asia Fund(No.SKL-HIDCA-2021-1).
文摘The 2022 Nobel Prize in Chemistry was awarded to American scientists Carolyn Bertozzi,K.Barry Sharpless,and Danish scientist Morten P.Merdahl for their contributions to the development of click chemistry and bioorthogonal chemistry.
文摘我国医院信息化建设目前正逐步向数字化医院的方向发展,通过信息化建设,医院的管理者可以更多、更全面的掌握信息,使管理更加有效。本文主要介绍了射频标签(Radio Frequency Identification,RFID)技术在医院精细化管理中的作用;提出了医院医疗设备精细化管理中存在的问题,研究并分析了RFID定位算法,通过实验平台测量并量化分析了射频读写器接收信号强度(Received Signal Strength Indication,RSSI)与距离以及读写器矢状面夹角之间的关系;最后,结合国内外使用RFID技术在医院管理研究进展,分析了RFID技术在定位、识别、药品防伪管理、新生儿防盗、医疗设备消毒溯源管理以及库房管理中的具体应用。
