Camptothecin
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Camptothecin
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| Systematic (IUPAC) name | |
| 4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b] quinoline-3,14-(4H,12H)-dione |
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| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C20H16N2O4 |
| Mol. mass | 348.352 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Camptothecin is a plant secondary metabolite used as an anti-cancer drug that damages DNA, leading to the destruction of the cell.
It comes from Camptotheca acuminata, a deciduous tree found in southern China. Stem woods of Nothopodytes foetida (previously known as Mappia foetida) found in the western ghats of India are an even better source of camptothecin.[citation needed] A close analogue, 9-methoxycamptothecin, is also present in the same source.
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[edit] Mechanism of action
Camptothecin affects the activity of the enzyme topoisomerase I, whose normal action is to cleave, unwind, and religate DNA. [1]
When camptothecin binds to topoisomerase I, it will be able to cleave but not to religate DNA. Thereby, camptothecin causes single strand breaks in DNA.
[edit] Related medications
Topotecan (trade name Hycamtin) and irinotecan {trade name Camptosar, also known as CPT-11) are camptothecin derivatives marketed as anti-cancer drugs by GlaxoSmithKline and Pfizer, respectively. Topotecan is indicated for small cell lung cancer after failure of first-line chemotherapy and metastatic carcinoma of the ovary following failure of initial or subsequent chemotherapy. Irinotecan is indicated for colorectal cancers and is usually taken with other drugs in chemotherapy.
[edit] References
- ^ Capranico G, Ferri F, Fogli M, Russo A, Lotito L, Baranello L (2007). "The effects of camptothecin on RNA polymerase II transcription: Roles of DNA topoisomerase I". Biochimie. PMID 17336444.
[edit] External links
- Camptothecin Project From the Stehlin Foundation for Cancer Research
- Pfizer Oncology From Pfizer Oncology
- GlaxoSmithKline From GlaxoSmithKline
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