An anticancer nucleoside
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Kinetin riboside is a purine derivative and nucleoside with anticancer activity.1 It induces the production of reactive oxygen species (ROS), cellular ATP depletion, and apoptosis in HepG2 cells. Kinetin riboside (10 ?M) reduces cyclin D1 and cyclin D2 levels, as well as induces cell cycle arrest at the G1 phase and apoptosis in patient-derived multiple myeloma cells.2 In vivo, kinetin riboside (85 mg/kg) reduces tumor growth in OCI-My5 and RPMI-8226 myeloma mouse xenograft models.
1.Orlicka-P?ocka, M., Gurda-Wozna, D., Fedoruk-Wyszomirska, A., et al.Circumventing the Crabtree effect: Forcing oxidative phosphorylation (OXPHOS) via galactose medium increases sensitivity of HepG2 cells to the purine derivative kinetin ribosideApoptosis25(11-12)835-852(2020) 2.Tiedemann, R.E., Mao, X., Shi, C.-X., et al.Identification of kinetin riboside as a repressor of CCND1 and CCND2 with preclinical antimyeloma activityJ. Clin. Invest.118(5)1750-1764(2008)
Cell experiment: | HeLa and mouse melanoma B16F-10 cells are treated with 5, 10, 20 μM kinetin riboside for 48 h. 15 μL of MTT solution (5 mg/mL) is added to each well and cells are maintained for 4 h at 37°C. Hundred microlitres of solubilizing solution is then added. After an overnight incubation at room temperature, absorbance at 490 nm is measured[2]. |
Animal experiment: | Mice: Male C57BL/6 mice are injected B16 F-10 cells. After 5 days for tumor growth, kinetin riboside (10, 20, 40 mg/kg) is injected to tumor mass directly. Drug injection is performed once a 3 days for three times. After third injection of drug, mice are kept for 3 days with no injection and tumor mass is removed from each mouse and weighed[2]. |
参考文献: [1]. Rajabi M, et al. Antiproliferative activity of kinetin riboside on HCT-15 colon cancer cell line. Nucleosides Nucleotides Nucleic Acids. 2012;31(6):474-81. |
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