Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues
In an effort to decrease the toxicity of camptothecin (CPT) and improve selectivity for hepatoma and colon cancer cells, bile acid groups were introduced into the CPT 20 or 10 positions, resulting in the preparation of sixteen novel CPT-bile acid analogues. The compounds in which a bile acid group w...
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| Format: | Article |
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MDPI AG
2014-03-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/19/3/3761 |
| _version_ | 1818023094168584192 |
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| author | Xingnuo Li Tengfei Zhao Dongping Cheng Chu Chu Shengqiang Tong Jizong Yan Qing-Yong Li |
| author_facet | Xingnuo Li Tengfei Zhao Dongping Cheng Chu Chu Shengqiang Tong Jizong Yan Qing-Yong Li |
| author_sort | Xingnuo Li |
| collection | DOAJ |
| description | In an effort to decrease the toxicity of camptothecin (CPT) and improve selectivity for hepatoma and colon cancer cells, bile acid groups were introduced into the CPT 20 or 10 positions, resulting in the preparation of sixteen novel CPT-bile acid analogues. The compounds in which a bile acid group was introduced at the 20-hydroxyl group of CPT showed better cytotoxic selectivity for human hepatoma and colon cancer cells than for human breast cancer cells. Fluorescence microscopy analysis demonstrated that one compound (E2) entered human hepatoma cells more effectively than it did human breast cancer cells. Compound G4 exhibited the best anti-tumour activity in vivo. These results suggested that introduction of a bile acid group at the 20-position of CPT could decrease toxicity in vivo and improve selectivity for hepatoma cells. |
| first_indexed | 2024-12-10T03:38:51Z |
| format | Article |
| id | doaj.art-d26610ac904a4067a00de57c92ea7fa4 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-10T03:38:51Z |
| publishDate | 2014-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-d26610ac904a4067a00de57c92ea7fa42022-12-22T02:03:37ZengMDPI AGMolecules1420-30492014-03-011933761377610.3390/molecules19033761molecules19033761Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin AnaloguesXingnuo Li0Tengfei Zhao1Dongping Cheng2Chu Chu3Shengqiang Tong4Jizong Yan5Qing-Yong Li6College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, ChinaKey Laboratory of Forest Plant Ecology (Northeast Forestry University), Ministry of Education, 332# No. 26 Hexing Road, Harbin 150040, ChinaCollege of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, ChinaIn an effort to decrease the toxicity of camptothecin (CPT) and improve selectivity for hepatoma and colon cancer cells, bile acid groups were introduced into the CPT 20 or 10 positions, resulting in the preparation of sixteen novel CPT-bile acid analogues. The compounds in which a bile acid group was introduced at the 20-hydroxyl group of CPT showed better cytotoxic selectivity for human hepatoma and colon cancer cells than for human breast cancer cells. Fluorescence microscopy analysis demonstrated that one compound (E2) entered human hepatoma cells more effectively than it did human breast cancer cells. Compound G4 exhibited the best anti-tumour activity in vivo. These results suggested that introduction of a bile acid group at the 20-position of CPT could decrease toxicity in vivo and improve selectivity for hepatoma cells.http://www.mdpi.com/1420-3049/19/3/3761camptothecinbile acidsanti-tumour activityhepatoma cells |
| spellingShingle | Xingnuo Li Tengfei Zhao Dongping Cheng Chu Chu Shengqiang Tong Jizong Yan Qing-Yong Li Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues Molecules camptothecin bile acids anti-tumour activity hepatoma cells |
| title | Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues |
| title_full | Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues |
| title_fullStr | Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues |
| title_full_unstemmed | Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues |
| title_short | Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues |
| title_sort | synthesis and biological activity of some bile acid based camptothecin analogues |
| topic | camptothecin bile acids anti-tumour activity hepatoma cells |
| url | http://www.mdpi.com/1420-3049/19/3/3761 |
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