Camptothecin is a DNA topoisomerase I inhibitor. Camptothecin inhibits topo I by blocking the rejoining step of the cleavage/religation reaction of topo-I, resulting in accumulation of a covalent reaction intermediate, the cleavable complex. Camptothecin induces extensive single strand DNA breaks in reactions containing purified mammalian DNA topoisomerase I. DNA breakage in vitro is immediate and reversible. Camptothecin showed remarkable anticancer activity in preliminary clinical trials.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Mechanism of action of camptothecin.
Liu LF, et al. Ann N Y Acad Sci. 2000;922:1-10. PMID: 11193884.
Camptothecin derivatives induce regression of human ovarian carcinomas grown in nude mice and distinguish between non-tumorigenic and tumorigenic cells in vitro.
Pantazis P, et al. Int J Cancer. 1993 Mar 12;53(5):863-71. PMID: 8449612.
Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I.
Hsiang YH, et al. J Biol Chem. 1985 Nov 25;260(27):14873-8. PMID: 2997227.
|Related Topoisomerase Products|
Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL).
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.
Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
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