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新生霉素

新生霉素用途

新生霉素是一种有效的口服抗生素。新生霉素也是DNA回转酶抑制剂和热休克蛋白90(Hsp90)拮抗剂。新生霉素具有研究高度β-内酰胺耐药肺炎球菌感染的潜力。新生霉素具有抗正氧病毒活性[1][2][3][4][6]。

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新生霉素名称

[ CAS 号 ]:
303-81-1

[ 中文名 ]:
新生霉素

[ 英文名 ]:
Novobiocin

[英文别名 ]:

Notonesomycin
Novobiocin

新生霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> HSP

研究领域 >> 感染

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

信号通路 >> 细胞周期/DNA损伤 >> HSP

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

HSP90

[体外研究]

新生霉素(1mM)竞争性地抑制ATP与回转酶B的结合,以干扰核苷酸结合,并干扰共伴侣Hsc70和p23与Hsp90的结合[1]。新生霉素(200µM；24小时)抑制顺式DDP和BCNU诱导的DNA链间交联的修复率,并相应降低人类多形性胶质母细胞瘤细胞的克隆形成存活率[2]。新生霉素(0.3 mM；48小时)通过诱导K562、HL60和Mutz-2中约三至五倍的凋亡细胞,诱导caspase-3/7酶依赖性凋亡测定[5]。

[体内研究]

新生霉素(25、50、100、200 mg/kg；皮下注射；感染后1、5、24和48小时注射4次)在感染耐阿莫西林肺炎链球菌的小鼠中显示出抗感染活性[3]。动物模型：30g成年雌性瑞士小鼠(由青霉素敏感菌株(AR33118)诱导的脓毒症)[3]剂量：25、50、100、200mg/kg给药：皮下注射。；在感染后1、5、24和48小时给予结果：在感染耐阿莫西林肺炎链球菌的小鼠中显示抗感染活性。

[参考文献]

[1]. Marcu MG, et al. The heat shock protein 90 antagonist novobiocin interacts with a previously unrecognized ATP-binding domain in the carboxyl terminus of the chaperone. J Biol Chem. 2000 Nov 24;275(47):37181-6.

[2]. Ali-Osman F, et al. Topoisomerase II inhibition and altered kinetics of formation and repair of nitrosourea and cisplatin-induced DNA interstrand cross-links and cytotoxicity in human glioblastoma cells. Cancer Res. 1993 Dec 1;53(23):5663-8.

[3]. Rodríguez-Cerrato V, et al. Comparative efficacy of novobiocin and amoxicillin in experimental sepsis caused by beta-lactam-susceptible and highly resistant pneumococci. Int J Antimicrob Agents. 2010 Jun;35(6):544-9.

[4]. Eder JP, et al. A phase I clinical trial of novobiocin, a modulator of alkylating agent cytotoxicity. Cancer Res. 1991 Jan 15;51(2):510-3.

[5]. Bhatia S, et al. Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response.Blood. 2018 Jul 19;132(3):307-320.

[6]. Smee DF. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24.

[7]. Smee DF. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24.

新生霉素物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
848.2±65.0 °C at 760 mmHg

[ 熔点 ]:
170-172°C (lit.)

[ 分子式 ]:
C₃₁H₃₆N₂O₁₁

[ 分子量 ]:
612.624

[ 闪点 ]:
466.8±34.3 °C

[ 精确质量 ]:
612.231934

[ PSA ]:
200.01000

[ LogP ]:
2.37

[ 蒸汽压 ]:
0.0±3.3 mmHg at 25°C

[ 折射率 ]:
1.640

[ 储存条件 ]:
室温

新生霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CU9080000

CHEMICAL NAME :: Benzamide, N-(7-((3-O-(aminocarbonyl)-6-deoxy-5-C-methyl-4-O-met hyl-beta-L-lyxo- hexopyranosyl)oxy)-4-hydroxy-8-methyl-2-oxo-2H-1-benz opyran-3-yl)-4-hydrox y- 3-(3-methyl-2-butenyl)-

CAS REGISTRY NUMBER :: 303-81-1

LAST UPDATED :: 199410

DATA ITEMS CITED :: 20

MOLECULAR FORMULA :: C31-H36-N2-O11

MOLECULAR WEIGHT :: 612.69

WISWESSER LINE NOTATION :: T66 BOVJ DMVR DQ C2UY1&1& EQ J1 IO- FT6OTJ B1 B1 CV1 DOVZ EQ &-NA-

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human

DOSE/DURATION :: 171 mg/kg/12D-C

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - conjunctive irritation Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 262 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 407 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 200 mg/L

REFERENCE :: CHROAU Chromosoma. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1939- Volume(issue)/page/year: 85,603,1982

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新生霉素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H317

[ 警示性声明 ]:
P280-P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

新生霉素

新生霉素用途

新生霉素名称

新生霉素生物活性

新生霉素物理化学性质

新生霉素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

新生霉素安全信息

新生霉素上下游产品

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