title: Isocorydine derivatives and their anticancer activities.
abstract: In order to improve the anticancer activity of isocorydine (ICD), ten isocorydine derivatives were prepared through chemical structure modifications, and their in vitro and in vivo activities were experimentally investigated. 8-Amino-isocorydine (8) and 6a,7-dihydrogen-isocorydione (10) could inhibit the growth of human lung (A549), gastric (SGC7901) and liver (HepG2) cancer cell lines in vitro. Isocorydione (2) could inhibit the tumor growth of murine sarcoma S180-bearing mice, and 8-acetamino-isocorydine (11), a pro-drug of 8-amino-isocorydine (8), which is instable in water solution at room temperature, had a good inhibitory effect on murine hepatoma H22-induced tumors. The results suggested that the isocorydine structural modifications at C-8 could significantly improve the biological activity of this alkaloid, indicating its suitability as a lead compound in the development of an effective anticancer agent.
authors.affiliation: Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou 730000, China. zhongmei@licp.cas.cn.
authors.forename: Mei
authors.initials: M
authors.lastname: Zhong
authors.affiliation: Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou 730000, China. liuyanjuan09@163.com.
authors.forename: Yanjuan
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou 730000, China. liujx@licp.cas.cn.
authors.forename: Junxi
authors.initials: J
authors.lastname: Liu
authors.affiliation: Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou 730000, China. didl@licp.cas.cn.
authors.forename: Duolong
authors.initials: D
authors.lastname: Di
authors.affiliation: Gansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China. xmr1991@126.com.
authors.forename: Mengrou
authors.initials: M
authors.lastname: Xu
authors.affiliation: Gansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China. yangmegan2011@hotmail.com.
authors.forename: Yaya
authors.initials: Y
authors.lastname: Yang
authors.affiliation: Gansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China. liwg@lzu.edu.cn.
authors.forename: Wenguang
authors.initials: W
authors.lastname: Li
authors.affiliation: Gansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China. chenyl2013@licp.cas.cn.
authors.forename: Yali
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Institute of Biology, Gansu Academy of Sciences, Lanzhou 730000, China. Liujinx0168@163.com.
authors.forename: Jinxia
authors.initials: J
authors.lastname: Liu
mesh_terms: D000470:Alkaloids / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry*; D001060:Aporphines / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects*; D056945:Hep G2 Cells; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology
chemical_list: D000470:Alkaloids; D000972:Antineoplastic Agents, Phytogenic; D001060:Aporphines; C030168:isocorydine