Integrative Biology Journals

Natural Products and Bioprospecting ›› 2018, Vol. 8 ›› Issue (4): 303-319.DOI: 10.1007/s13659-018-0162-1

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Antitumor Research on Artemisinin and Its Bioactive Derivatives

Yunqin Zhang1,2, Guowei Xu1,2, Shuqun Zhang1, Dong Wang1, P. Saravana Prabha1, Zhili Zuo1,3   

  1. 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;
    2 University of the Chinese Academy of Sciences, Beijing 100049, China;
    3 Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming 650201, Yunnan, China
  • Received:2018-01-09 Revised:2018-03-27 Online:2018-08-28 Published:2018-08-24
  • Contact: Zhili Zuo,zuozhili@mail.kib.ac.cn
  • Supported by:
    This work was financially supported by CAS "Light of West China" Program ([2014]91 to Z.Z.), the Basic Research Plan of Yunnan Provincial Science and Technology Department (grant number 2014FA042), CAS Strategic biological resources service network (ZSTH-021),and the Strategic Priority Research Program of the Chinese Academy of Sciences,Grant No. XDA12030206.

Antitumor Research on Artemisinin and Its Bioactive Derivatives

Yunqin Zhang1,2, Guowei Xu1,2, Shuqun Zhang1, Dong Wang1, P. Saravana Prabha1, Zhili Zuo1,3   

  1. 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;
    2 University of the Chinese Academy of Sciences, Beijing 100049, China;
    3 Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming 650201, Yunnan, China
  • 通讯作者: Zhili Zuo,zuozhili@mail.kib.ac.cn
  • 基金资助:
    This work was financially supported by CAS "Light of West China" Program ([2014]91 to Z.Z.), the Basic Research Plan of Yunnan Provincial Science and Technology Department (grant number 2014FA042), CAS Strategic biological resources service network (ZSTH-021),and the Strategic Priority Research Program of the Chinese Academy of Sciences,Grant No. XDA12030206.

Abstract: Cancer is the leading cause of human death which seriously threatens human life. The antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer properties. Simultaneously, a variety of target-selective artemisinin-related compounds with high efficiency have been discovered. Many researches indicated that artemisininrelated compounds have cytotoxic effects against a variety of cancer cells through pleiotropic effects, including inhibiting the proliferation of tumor cells, promoting apoptosis, inducing cell cycle arrest, disrupting cancer invasion and metastasis, preventing angiogenesis, mediating the tumor-related signaling pathways, and regulating tumor microenvironment. More importantly, artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in cancer patients. Therefore, we concentrated on the new advances and development of artemisinin and its derivatives as potential antitumor agents in recent 5 years. It is our hope that this review could be helpful for further exploration of novel artemisinin-related antitumor agents.

Key words: Artemisinin, Artemisinin derivatives, Antitumor, Activity, Mechanism

摘要: Cancer is the leading cause of human death which seriously threatens human life. The antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer properties. Simultaneously, a variety of target-selective artemisinin-related compounds with high efficiency have been discovered. Many researches indicated that artemisininrelated compounds have cytotoxic effects against a variety of cancer cells through pleiotropic effects, including inhibiting the proliferation of tumor cells, promoting apoptosis, inducing cell cycle arrest, disrupting cancer invasion and metastasis, preventing angiogenesis, mediating the tumor-related signaling pathways, and regulating tumor microenvironment. More importantly, artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in cancer patients. Therefore, we concentrated on the new advances and development of artemisinin and its derivatives as potential antitumor agents in recent 5 years. It is our hope that this review could be helpful for further exploration of novel artemisinin-related antitumor agents.

关键词: Artemisinin, Artemisinin derivatives, Antitumor, Activity, Mechanism