bleomycin A6

bleomycin A6用途

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]。

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bleomycin A6名称

[ CAS 号 ]:
37293-17-7

[ 英文名 ]:
bleomycin A6

[英文别名 ]:

Zhengguangmycin A6
Pingyangmycin A6

bleomycin A6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.

bleomycin A6物理化学性质

[ 密度 ]:
1.53g/cm3

[ 分子式 ]:
C₆₀H₉₆N₂₀O₂₁S₂

[ 分子量 ]:
1497.66000

[ 精确质量 ]:
1496.65000

[ PSA ]:
733.63000

bleomycin A6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