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