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  • Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoiso- merase I (topo I).
  • It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs.
  • Camptothecin was isolated from the bark and stem of Camptotheca acuminata (Camptotheca, Happy tree), a tree native to China.
  • CPT showed remarkable anticancer activity in preliminary clinical trials but also low solubility and (high) adverse drug
    reaction.
  • Camptothecins (CPT) are one of the most important alkaloids of the 21st century because of their clinical applications
    against cancer and HIV-I.
  • Camptothecin, a pentacyclic quinoline alkaloid, has been discovered through an extensive screening by the U.S. National Cancer Institute. This compound exhibits an antitumor activity due to its inhibitory action to DNA topoisomerase I.
  • Camptothecin-11 destroys the cancerous cells and prevents the further division of these cells, they also induce the self-destruction of these cancerous cells, this mode of cancer treatment is cell specific and destroys only those affected cancerous cells.
  • CPT has a unique penta- cyclic ring structure which gives itself and its derivatives the necessary antitumour activity and such spatial configuration cannot be synthesized artificially.
  • CPT inhibits the replica-tion of Human Immuno Deficiency Virus (HIV) in vitro and is also shown to be effective in the complete remission of lung, breast, uterine and cervical cancer. The molecular and cytotoxic effects of camptothecin on  Plasmodium falciparum proven that it is an interesting target for new anti-malarial drug development.
  • Camptothecin affects the activity of the enzyme topoisomerase I, whose normal action is to cleave, unwind, and religate DNA. When  camptothe- cin binds to topoiso- merase I, it will be able to cleave but not to religate DNA. Thereby, camptothecin causes single strand breaks in DNA.
  • Camptothecins are among the most recently approved anticancer agents with two derivatives approved by the FDA: Camptosar (Irinotecan hydrochloride; CPT-11) for advanced colo-rectal carcinomas and Hycamtin(Topotecan) for ovarian cancers. Both drugs are water-soluble derivatives of the parent natural alkaloid camptothecin.
  • Camptothecin (CPT) has recently attracted increasing attention as a promising anticancer agent for a variety of tumors. But the clinical application is largely hampered by its extreme water insolubility and unpredictable side effect. It is essential to establish an efficient and safe protocol for the admi-nistration of CPT versus melanoma.
  • Camptothecins are an important and fast growing class of anti-cancer drugs. However, like taxanes, their full benefit is limited by poor solubility and significant toxicity.
  • At present, semisynthetic water-soluble camptothe- cin analogs, topotecan and irinotecan, are prescribed as clinical antitumor drugs through out the world. The worldwide market size of irinotecan / topotecan in 2003 was estimated at about US$1 billion. Worldwide sales for camptothecins exceeded $725.0 million in 2004.

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