Editor-in-Chief İlkay Küçükgüzel Associate Editor Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Marmara Pharmaceutical Journal 2014 , Vol 18 , Issue 2
Kamptotesin
Merve KURTAN1, Sezin KURTOGLU2, Gulay MELIKOGLU2
1Acıbadem Fulya Hastanesi Eczanesi, 34349-Fulya, Beşiktaş, İstanbul
2İstanbul Üniversitesi, Eczacılık Fakültesi, Farmakognozi Anabilim Dalı, 34116-Beyazıt, İstanbul
DOI : 10.12991/mpj.2014186125 Camptothecin, a monoterpene indole alkaloid, first isolated from the Chinese tree Camptotheca acuminata Decaisne in 1957. Camptothecin has been found not only in C. acuminata (Nyssaceae) but also in several other plant species belonging to various plant families, i.e., Icacinaceae, Rubiaceae, Loganiaceae and Apocynaceae. This study provides a detailed evaluation of distribution of camptothecin and its related compounds. Camptothecin, a well-known anti-tumor alkaloid, possesses inhibitory activity against DNA topoisomerase I. Due to the extremely poor solubility of camptothecin in water, clinical trials were initiated using its water-soluble sodium salt. The clinical development of camptothecin was discontinued because of its severe adverse effects and its low efficiency. In this study, physical and chemical characteristics, mechanism of action, biological activities and biosynthesis of camptothecin are analysed. A series derivative of camptothecin have been developed that increase solubility, lactone stability and bioavailability to varying levels. Two semi-synthetic camptothecin analogues are presently approved for use in the clinic as antitumor agents and several others are in clinical trials. In this review, a systematic evaluation of novel and important analogues of camptothecin are performed and their current structure–activity profile are investigated. Keywords : Camptothecin, Camptotheca acuminata, antitumor
Marmara University