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编 号：F285317
分子式：C27H29NO11
分子量：543.52
分子式：C27H29NO11
分子量：543.52
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CAS No: 23214-92-8
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生物活性：
Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
体内研究：
Doxorubicin (4-8 mg/kg) 在PC3 异种抑移植裸鼠中会延迟肿瘤的生长，降低小鼠中 c-FLIP 水平的表达。Doxorubicin (腹腔注射; 单剂量 (10 mg/kg) /一天一次连续 10 天 (1 mg/kg) /一周一次连续5周 (2 mg/kg)) 在 Sprague-Dawley 大鼠中具有心脏毒性，但是与一次性给药 10 mg/kg 相比，通过多次在几天或几周累计给药 10 mg/kg 的方式可以提高大鼠的存活率。Doxorubicin (4%- 20%; Intrastriatal 注射; 单剂量) 在 Sprague-Dawley 大鼠中具有神经毒性。Doxorubicin 在酸性条件下可以通过 PH-敏感键偶联在金纳米颗粒 (Au NPs) 上面，从而能通过血脑屏障，最大的吸收波长为528 nm。Animal Model:Athymic male nude mice model of xenografts of PC3 prostate carcinoma cells
Dosage:2 mg/kg, 4 mg/kg, 8 mg/kg
Administration:ntraperitoneal injection (i.p.); Single dose .After injected PC3 cells (4 × 106) subcutaneously into the flank of mice.
Result:A dose of 2 mg/ kg did not affect tumor growth while higher dosages (4 mg/kg, 8 mg/kg) delayed tumor growth initially.
Animal Model:Male Sprague-Dawley rats model
Dosage:10 mg/kg (schedule 1), 1 mg/kg (schedule 2), 2 mg/kg (schedule 3)
Administration:Intraperitoneal injection (i.p.) ; Single dose (schedule 1).Intraperitoneal injection (i.p.); Once daily for 10 days (schedule 2).Intraperitoneal injection (i.p.); Once per week, for 5 weeks(schedule 3).
Result:In schedule 1, caused 30% of the rats to die at the end of week 2 and 80% by day 28.In schedule 2 , caused 55% of the rats to die at the end of week 13 and 80% by day 107.In schedule 3, caused 42% of the rats to die at the end of week 13 and 80% by day 98.
Animal Model: Male Sprague-Dawley rats
Dosage:1%, 2%, 4%, 5%, 6%, 10%, 20%
Administration:Intrastriatal injection; Single dose
Result:In doses of 4, 5, 6, 10 or 20% caused obvious loss of ipsilateral SNc and VTA neuronsz and doses of 1 or 2% failed to produce obvious neuron loss.
体外研究：
Doxorubicin (Hydroxydaunorubicin) 和辛伐他汀 (HY-17502) 在最高测试浓度 (分别为2 μM和10 μM) 联合使用可杀死 97% 的 Hela 细胞。Doxorubicin 可以标记神经元细胞，且罗丹明滤袋下呈鲜红色，在儿茶酚胺滤袋下呈淡红橙色。Doxorubicin (5 μM; 10-30 分钟) 在 B16-F10 黑色素瘤细胞系 CRL-6475 细胞中能以时间依赖方式在细胞中积累，且可以通过绿色或红色荧光来进行检测 (绿色荧光的检测灵敏度更高), 最大激发波长 (λex) 和最大发射波长为 (λem) 分别为 470 nm 和 560 nm.
Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
体内研究：
Doxorubicin (4-8 mg/kg) 在PC3 异种抑移植裸鼠中会延迟肿瘤的生长，降低小鼠中 c-FLIP 水平的表达。Doxorubicin (腹腔注射; 单剂量 (10 mg/kg) /一天一次连续 10 天 (1 mg/kg) /一周一次连续5周 (2 mg/kg)) 在 Sprague-Dawley 大鼠中具有心脏毒性，但是与一次性给药 10 mg/kg 相比，通过多次在几天或几周累计给药 10 mg/kg 的方式可以提高大鼠的存活率。Doxorubicin (4%- 20%; Intrastriatal 注射; 单剂量) 在 Sprague-Dawley 大鼠中具有神经毒性。Doxorubicin 在酸性条件下可以通过 PH-敏感键偶联在金纳米颗粒 (Au NPs) 上面，从而能通过血脑屏障，最大的吸收波长为528 nm。Animal Model:Athymic male nude mice model of xenografts of PC3 prostate carcinoma cells
Dosage:2 mg/kg, 4 mg/kg, 8 mg/kg
Administration:ntraperitoneal injection (i.p.); Single dose .After injected PC3 cells (4 × 106) subcutaneously into the flank of mice.
Result:A dose of 2 mg/ kg did not affect tumor growth while higher dosages (4 mg/kg, 8 mg/kg) delayed tumor growth initially.
Animal Model:Male Sprague-Dawley rats model
Dosage:10 mg/kg (schedule 1), 1 mg/kg (schedule 2), 2 mg/kg (schedule 3)
Administration:Intraperitoneal injection (i.p.) ; Single dose (schedule 1).Intraperitoneal injection (i.p.); Once daily for 10 days (schedule 2).Intraperitoneal injection (i.p.); Once per week, for 5 weeks(schedule 3).
Result:In schedule 1, caused 30% of the rats to die at the end of week 2 and 80% by day 28.In schedule 2 , caused 55% of the rats to die at the end of week 13 and 80% by day 107.In schedule 3, caused 42% of the rats to die at the end of week 13 and 80% by day 98.
Animal Model: Male Sprague-Dawley rats
Dosage:1%, 2%, 4%, 5%, 6%, 10%, 20%
Administration:Intrastriatal injection; Single dose
Result:In doses of 4, 5, 6, 10 or 20% caused obvious loss of ipsilateral SNc and VTA neuronsz and doses of 1 or 2% failed to produce obvious neuron loss.
体外研究：
Doxorubicin (Hydroxydaunorubicin) 和辛伐他汀 (HY-17502) 在最高测试浓度 (分别为2 μM和10 μM) 联合使用可杀死 97% 的 Hela 细胞。Doxorubicin 可以标记神经元细胞，且罗丹明滤袋下呈鲜红色，在儿茶酚胺滤袋下呈淡红橙色。Doxorubicin (5 μM; 10-30 分钟) 在 B16-F10 黑色素瘤细胞系 CRL-6475 细胞中能以时间依赖方式在细胞中积累，且可以通过绿色或红色荧光来进行检测 (绿色荧光的检测灵敏度更高), 最大激发波长 (λex) 和最大发射波长为 (λem) 分别为 470 nm 和 560 nm.
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