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编 号：F760486
分子式：C13H14N2O3
分子量：246.26
分子式：C13H14N2O3
分子量：246.26
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CAS No: 81307-24-6
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生物活性：
Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct.
体内研究：
Antibiotic DC 81 (0-10 mg/kg, i.p., at day 4, 7, 10, 13 after tumor cell injection) decreases the tumor burden in tumor-bearing mice, but the Antibiotic DC 81 at 10 mg/kg impairs cardiac muscle enzyme and liver function significantly.Animal Model:Female C57BL/6 mice (8-12 weeks old, B16 cells were injected into the tail veins of mice)
Dosage:0.1, 1, 10 mg/kg
Administration:i.p., at day 4, 7, 10, 13 after tumor cell injection
Result:Substantially decreased the tumor burden by 20% at 1 mg/kg. DC-81 at 10 mg/kg induced an 8-10-fold increase of GPT and a 6-8-fold increase in CPK, which indicated severe impaired liver function and muscle damage. Did not impair significant renal function as demonstrated by serum creatinine.
体外研究：
Antibiotic DC 81 shows cytotoxicity against human melanoma cell lines B16, A375, A2058, and RPMI7951, with IC50 values of 4.4 μM, 18.5 μM, 31.0 μM, and 41.5 μM, respectively.Antibiotic DC 81 exhibits its biological activity by covalently binding to the N2 of guanine in the minor groove of DNA, via the electrophilic carbinolamine functionality at N10-C11.Antibiotic DC 81 (4 μM, 24 h) induces mitochondria dependent apoptosis.
Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct.
体内研究：
Antibiotic DC 81 (0-10 mg/kg, i.p., at day 4, 7, 10, 13 after tumor cell injection) decreases the tumor burden in tumor-bearing mice, but the Antibiotic DC 81 at 10 mg/kg impairs cardiac muscle enzyme and liver function significantly.Animal Model:Female C57BL/6 mice (8-12 weeks old, B16 cells were injected into the tail veins of mice)
Dosage:0.1, 1, 10 mg/kg
Administration:i.p., at day 4, 7, 10, 13 after tumor cell injection
Result:Substantially decreased the tumor burden by 20% at 1 mg/kg. DC-81 at 10 mg/kg induced an 8-10-fold increase of GPT and a 6-8-fold increase in CPK, which indicated severe impaired liver function and muscle damage. Did not impair significant renal function as demonstrated by serum creatinine.
体外研究：
Antibiotic DC 81 shows cytotoxicity against human melanoma cell lines B16, A375, A2058, and RPMI7951, with IC50 values of 4.4 μM, 18.5 μM, 31.0 μM, and 41.5 μM, respectively.Antibiotic DC 81 exhibits its biological activity by covalently binding to the N2 of guanine in the minor groove of DNA, via the electrophilic carbinolamine functionality at N10-C11.Antibiotic DC 81 (4 μM, 24 h) induces mitochondria dependent apoptosis.
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