10-hydroxy-Camptothecin is an inhibitor of topoisomerase I originally isolated from the Chinese tree C. acuminata. 10-Hydroxycamptothecin is a member of the camptothecin family that demonstrates less toxicity than its parent compound. (S)-10-hydroxy-Camptothecin has strong anti-tumor activity against a wide range of experimental tumors including L1210 leukemia cells (IC50 = 1.15 μM). In vitro treatment of human HepG2 cells with 5-20 μM (S)-10-hydroxy-camptothecin results in cell cycle arrest at the G2/M phase.
|Cell lines||MDA-231, and BT-20 cells|
|Preparation method||Exposing cells to various concentrations of 10-Hydroxycamptothecin for 72 hours. Monitoring cell growth by the standard MTT assay.|
|Concentrations||Dissolved in DMSO, final concentrations ~50 μM|
|Incubation time||72 hours|
|Animal models||BALB/c-nu mice transplanted subcutaneously with Colo 205 cells|
|Formulation||Dissolved in propylene glycol|
|Administration||Orally once per two days|
|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.
[Studies on the effects of cucurbit (n = 7) uril on the physicohemical properties and anticancer activity of 10-hydroxycamptothecin].
Lü Y, et al. Guang Pu Xue Yu Guang Pu Fen Xi. 2014 Jun;34(6):1610-4. PMID: 25358173.
Anticancer effects of low-dose 10-hydroxycamptothecin in human colon cancer.
Ping YH, et al. Oncol Rep. 2006 May;15(5):1273-9. PMID: 16596197.
DNA topoisomerase I as a site of action for 10-hydroxycamptothecin in human promyelocytic leukemia cells.
Ling YH, et al. Cancer Biochem Biophys. 1990 Jan;11(1):23-30. PMID: 2159843.
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