• 약학회지
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• 제44권2호
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• pp.149-154
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• 2000

Flavin mononucleotide (1,4-butanediamine) Pt(II) complex (7FMN) was synthesized and screened anticancer activity [J. Pharm. Soc. Korea 43(6),762-770 (1999)]. 7FMN have good water solubility and moderate anticancer activiy In this paper cell-cycle specificity and nephrotoxicity were studied. Interaction of DNA with cisplatin and synthesized 7FMN was analyzed by flow cytometry and showed G2 arrest in L1210 cell line. It means that cell-cycle on L1210 was inhibit in S phase by cisplatin and 7FMN. In order to biochemically analyze nephrotoxicity of cisplatin and 7FMN, after injecting each agent intraperitoneally, blood was exsanguinated after 6 hours, 1 day, 3 days and 7 days, respectively. Then, serum was separated from the blood. The serum level of BUN, creatinine and uric acid in cisplatin and 7FMN administated mice (25~35 g, ICR strain, a dose each 8,12 and 16 times of the $IC_{50}$/ value, cisplatin; 7 times) were determined by autochemistry analyzer. In cisplatinadministered mice group, BUN level was elevated than normal control group at 3rd day and repaired at 7th day. In 7FMN administrated group was not elevated. Creatinine and uric acid level were no difference with the normal control group. Therefore synthesized 7FMN is less toxic than cisplatin in nephrotoxiciaty.

• 약학회지
• /
• 제43권6호
• /
• pp.762-770
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• 1999

A series of vitamin-containing Pt(II) complexes of the type [Pt (FMN) (L)] (FMN=flavin mononucleotide, L=ethylenediamine, 1,3-propanediamine, 1,4-bu-tanediamine) was synthesizd and characterized by IR, electronic absorption, elemental analysis and FAB=Mass. The coordination sites of FMN to Pt(II) ions were determined to be N(5) and O(6) with resultant chelate ring formation. Theses compounds have much better water solubility (30-35 mg/ml) than cisplatin (1 mg/ml). The anticancer activity of this vitamin-containing Pt(II) series was investigated by MTT assay against mouse and human leukemia cell lines in vitro. Among these compounds, FMN (1,4-butanediamine) Pt(II) having seven-membered ring structure as amine ligand showed moderate anticancer activity.