Camptothecin

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Camptothecin
Systematic (IUPAC) name
4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]
quinoline-3,14-(4H,12H)-dione
Identifiers
CAS number 7689-03-4
ATC code ?
PubChem 2538
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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Routes ?

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Overview

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.(2)Template:Fix/category[citation needed] A close analogue, 9-methoxycamptothecin, is also present in the same source.

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.

Related medications

Since Camptothecin manifested a severe life threatening adverse reaction in the form of cystitis (Inflammation of the urinary bladder and ureters) concerted efforts over years by many research institutions, academic as well as industrial, resulted in chemically related analogues with less toxicity and enhanced therapeutic potency.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.

References

  1. 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. 

2.Alkaloids of mappia foetida, Govindachari and viswanathan, Phytochemistry, 11,3529-3531(1972)

External links



fi:Kamptotesiini



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