Name: Camptothecin
Active ingredients: Camptothecin
Test method:HPLC
Formula : C 20 H 16 N 2 O 4
Mol. mass : 348.352 g/mol
CAS.No:7689-3-4
Appearance:White to off-white powder
Introduction:
Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase 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 . It was isolated from the bark and stem of Camptotheca acuminata (Camptotheca, Happy tree), a tree native to China used as a cancer treatment in Traditional Chinese Medicine .CPT showed remarkable anticancer activity in preliminary clinical trials but also low solubility and (high) adverse drug reaction . Because of these disadvantages synthetic and medicinal chemists have developed numerous syntheses of Camptothecin [2] [3] [4] and various derivatives to increase the benefits of the chemical , with good results. Two CPT analogues have been approved and are used in cancer chemotherapy [5] today, topotecan and irinotecan .
Functions:
1. 10-Hydroxy camptothecin and its derivatives are unique in their ability to inhibit DNA Topoisomerase I, by stabilizing a covalent reaction intermediate termed the cleavable complex which ultimately causes tumor cell death.
2.In clinical 10-Hydroxy camptothecin is widely believed that camptothecin analogs exhibited remarkable anti-tumour and antileukaemia activity. Topoisomerase is a basilic enzyme in the process of DNA replication, it is responsible for the winding / unwinding of the supercoiled DNA composing the chromosomes. If the chromosomes cannot be unwound, transcription of DNA message cannot occur and the protein cannot be synthesized, it ultimately causes cell death.
Pharmacology:anti-cancer, anti-virus, immune inhibition, anti early pregnancy, changes in skin epidermal keratinization process