Novobiocin (sodium)

国际站：Novobiocin (sodium)

中文名：新生霉素钠

CAS：1476-53-5

品牌：MedChemExpress (MCE)

存储条件：4°C, sealed storage, away from moisture

生物活性：Novobiocin (Albamycin) sodium 是一种有效的口服活性抗生素。 Novobiocin sodium 还是一种DNA 促旋酶 抑制剂和热休克蛋白 90 (Hsp90) 拮抗剂。 Novobiocin sodium 具有研究高度 β-内酰胺耐药性肺炎球菌感染的潜力。 Novobiocin sodium 具有抗正痘病毒活性^[1][2][3][4]。 IC50 和目标：IC50：700 μM (HSP90)。

体外：Novobiocin sodium (1 mM) 竞争性抑制 ATP 与促旋酶 B 的结合，从而干扰核苷酸结合并干扰辅助伴侣 Hsc70 和 p23 与 Hsp90 的结合^[1]。Novobiocin sodium （200 µM；24 小时）抑制顺式 DDP 和 BCNU 诱导的 DNA 链间交联的修复速率，并相应降低人多形性胶质母细胞瘤细胞的克隆形成存活率^[2] .新生霉素钠（0.3 mM；48 小时）诱导 caspase-3/7 酶依赖性细胞凋亡测定，在 K562、HL60、Mutz-2 中诱导大约三到五倍的凋亡细胞^{[ 5]}.

体内：Novobiocin sodium (25, 50, 100, 200 mg/kg; sc; 4 times at 1, 5, 24 and 48 h after infection) 在感染阿莫西林耐药 肺炎链球菌^[3]。

参考文献：[1]. 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.[2]. 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.[3]. 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.[4]. 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.[5]. 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.[6]. Smee DF. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24.