37293-17-7

• 常用中文名：bleomycin A6
• 常用英文名：bleomycin A6
• CAS号：37293-17-7
• 分子式：C₆₀H₉₆N₂₀O₂₁S₂
• 分子量：1497.66000
• 相关类别： 信号通路 细胞凋亡 细胞凋亡
• 发布时间：2017-02-25 21:15:47
• 更新时间：2024-01-16 16:42:31
• 博安霉素是一种具有抗肿瘤活性的抗生素,可诱导细胞衰老和凋亡[1][2][3]。

名称

• 英文名: bleomycin A6
• 英文别名: Zhengguangmycin A6; Pingyangmycin A6; N1-[3-[[4-[(3-Aminopropyl)amino]butyl]amino]propyl]bleomycinamide

物化性质

• 密度: 1.53g/cm3
• 分子式: C₆₀H₉₆N₂₀O₂₁S₂
• 分子量: 1497.66000
• 精确质量: 1496.65000
• PSA: 733.63000

生物活性

• 描述: 博安霉素是一种具有抗肿瘤活性的抗生素,可诱导细胞衰老和凋亡[1][2][3]。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
• 体外研究: 博安霉素(50-125μg/mL,0.5-36小时)可诱导Eca-109细胞凋亡并阻断细胞周期处于G2/M期[2]。博安霉素(6.7µg/mL,24小时)诱导细胞衰老[3]。细胞存活率测定[3]细胞系：人肺成纤维细胞系IMR90,小鼠原代成骨细胞(OBs)浓度：6.7µg/mL,孵育时间：24小时结果：与对照组的30%相比,IMR90细胞和OBs中SA-βgal染色细胞的阳性率分别为90%和95%。RT-PCR[3]细胞系：小鼠原代成骨细胞(OBs)浓度：6.7µg/mL孵育时间：24小时结果：衰老相关分泌表型(SASP)因子IL-6表达增加达6倍。
• 体内研究: 博安霉素(BAM)(i.p.,10或15 mg/kg,每周两次,5周)可有效抑制含有HT-29、Hce-8693或CT-26细胞的BALB/c裸鼠的肿瘤生长[1]。动物模型：具有HT-29或Hce-8693细胞的BALB/c裸鼠[1]剂量：10或15mg/kg给药：腹腔注射；一周两次5周结果：在HT-29模型小鼠中,10 mg/kg和15 mg/kg显著抑制肿瘤生长,分别为89%和92%,在Hce-8693模型小鼠中也分别抑制了90%和92%的肿瘤生长。动物模型：具有CT-26细胞的BALB/c裸鼠[1]剂量：10mg/kg给药：肌肉注射；每第二天；10倍结果：皮下肿瘤生长抑制88%,盲肠肿瘤生长抑制99%。
• 参考文献:

  [1]. Y C Deng, et al. Activity of boanmycin against colorectal cancer. World J Gastroenterol. 2001 Feb;7(1):93-7.

  [2]. Hao Tang, et al. Effect of boanmycin on apoptosis and cell cycle of human esophageal cancer(Eca-109) cells]. Ai Zheng. 2002 Aug;21(8):855-9.

  [3]. Peng Chen, et al. The chemotherapeutic drug boanmycin induces cell senescence and senescence-associated secretory phenotype factors, thus acquiring the potential to remodel the tumor microenvironment. Anticancer Drugs. 2016 Feb;27(2):84-8.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : EC5991325 CHEMICAL NAME : Bleomycinamide, N(sup 1)-(3-((4-((3-aminopropyl)amino)butyl)amino)propyl)- CAS REGISTRY NUMBER : 37293-17-7 LAST UPDATED : 199607 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C60-H96-N20-O21-S2 MOLECULAR WEIGHT : 1497.88 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 102 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ZKZAEY Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics. (Zhongguo Kangshengsu Zazhi Bianjibu, 9 Shanbanqiaolu, Chenqdu, 610051 Peop. Rep. China) V.13- 1988- Volume(issue)/page/year: 15,453,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 80330 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ZKZAEY Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics. (Zhongguo Kangshengsu Zazhi Bianjibu, 9 Shanbanqiaolu, Chenqdu, 610051 Peop. Rep. China) V.13- 1988- Volume(issue)/page/year: 15,453,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 97780 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ZKZAEY Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics. (Zhongguo Kangshengsu Zazhi Bianjibu, 9 Shanbanqiaolu, Chenqdu, 610051 Peop. Rep. China) V.13- 1988- Volume(issue)/page/year: 15,453,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 70530 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ZKZAEY Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics. (Zhongguo Kangshengsu Zazhi Bianjibu, 9 Shanbanqiaolu, Chenqdu, 610051 Peop. Rep. China) V.13- 1988- Volume(issue)/page/year: 15,453,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 24500 ug/kg/7W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death REFERENCE : ZKZAEY Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics. (Zhongguo Kangshengsu Zazhi Bianjibu, 9 Shanbanqiaolu, Chenqdu, 610051 Peop. Rep. China) V.13- 1988- Volume(issue)/page/year: 15,453,1990