Isocorydine Derivatives and Their Anticancer Activities
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 inhib...
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doaj-23e976d3ebce4101bc0ccd8436da85122020-11-24T23:59:39ZengMDPI AGMolecules1420-30492014-08-01198120991211510.3390/molecules190812099molecules190812099Isocorydine Derivatives and Their Anticancer ActivitiesMei Zhong0Yanjuan Liu1Junxi Liu2Duolong Di3Mengrou Xu4Yaya Yang5Wenguang Li6Yali Chen7Jinxia Liu8Key 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, ChinaKey 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, ChinaKey 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, ChinaKey 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, ChinaGansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, ChinaGansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, ChinaGansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, ChinaGansu Key Laboratory of Preclinical Study for New Drugs, Institute of Pharmacology, School of Basic Medical Science, Lanzhou University, Lanzhou 730000, ChinaInstitute of Biology, Gansu Academy of Sciences, Lanzhou 730000, ChinaIn 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.http://www.mdpi.com/1420-3049/19/8/12099aporphine alkaloidsisocorydinesynthesisanticancer activity |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Mei Zhong Yanjuan Liu Junxi Liu Duolong Di Mengrou Xu Yaya Yang Wenguang Li Yali Chen Jinxia Liu |
spellingShingle |
Mei Zhong Yanjuan Liu Junxi Liu Duolong Di Mengrou Xu Yaya Yang Wenguang Li Yali Chen Jinxia Liu Isocorydine Derivatives and Their Anticancer Activities Molecules aporphine alkaloids isocorydine synthesis anticancer activity |
author_facet |
Mei Zhong Yanjuan Liu Junxi Liu Duolong Di Mengrou Xu Yaya Yang Wenguang Li Yali Chen Jinxia Liu |
author_sort |
Mei Zhong |
title |
Isocorydine Derivatives and Their Anticancer Activities |
title_short |
Isocorydine Derivatives and Their Anticancer Activities |
title_full |
Isocorydine Derivatives and Their Anticancer Activities |
title_fullStr |
Isocorydine Derivatives and Their Anticancer Activities |
title_full_unstemmed |
Isocorydine Derivatives and Their Anticancer Activities |
title_sort |
isocorydine derivatives and their anticancer activities |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2014-08-01 |
description |
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. |
topic |
aporphine alkaloids isocorydine synthesis anticancer activity |
url |
http://www.mdpi.com/1420-3049/19/8/12099 |
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