乳糖酸阿奇霉素

更新时间:2024-01-02 13:38:25

乳糖酸阿奇霉素结构式
乳糖酸阿奇霉素结构式
品牌特惠专场
常用名 乳糖酸阿奇霉素 英文名 n-2,10-dion(1:1)
CAS号 3847-29-8 分子量 1092.223
密度 0.9083 (rough estimate) 沸点 818.4ºC at 760mmHg
分子式 C49H89NO25 熔点 145-150°
MSDS N/A 闪点 448.8ºC

 乳糖酸阿奇霉素用途


乳酸红霉素是一种由放线菌红霉素链霉菌产生的大环内酯类抗生素,具有广谱抗菌活性。乳糖酸红霉素结合细菌50S核糖体亚基,通过阻断转肽和/或易位反应抑制RNA依赖性蛋白质合成,而不影响核酸的合成[1][2]。乳糖酸红霉素在不同的研究领域也表现出抗肿瘤和神经保护作用[3][4]。

 乳糖酸阿奇霉素名称

中文名 乳糖酸红霉素
英文名 erythromycin lactobionate (200 mg)
中文别名 糖酸罗红霉素 | 红霉素乳糖醛酸
英文别名 更多

 乳糖酸阿奇霉素生物活性

描述 乳酸红霉素是一种由放线菌红霉素链霉菌产生的大环内酯类抗生素,具有广谱抗菌活性。乳糖酸红霉素结合细菌50S核糖体亚基,通过阻断转肽和/或易位反应抑制RNA依赖性蛋白质合成,而不影响核酸的合成[1][2]。乳糖酸红霉素在不同的研究领域也表现出抗肿瘤和神经保护作用[3][4]。
相关类别
靶点

Bacterial; RNA-dependent protein synthesis[1]

体外研究 乳糖酸红霉素抑制恶性疟原虫的生长,IC50和IC90值分别为58.2μM和104.0μM[1]。乳糖酸红霉素(10μM,100μM;24小时,72小时)具有抗氧化和抗炎作用,抑制4-HNE(p<0.01)和8-OHdG(p<1.01)的积累,显著降低Iba-1(p<2.01)及TNF-α(p<3.01)表达[4]。细胞存活率测定[4]细胞系:胚胎原代皮质神经元(来自17日龄Sprague-Dawley大鼠的大脑皮质)浓度:10,100μM孵育时间:24,72小时结果:在3小时缺氧-葡萄糖剥夺(OGD)后,提高了体外培养的神经元细胞的存活率。
体内研究 乳糖酸红霉素(胃插管;0.1-50 mg/kg;30-120天)可降低肿瘤生长,并延长小鼠的存活时间,剂量为5 mg/kg[3]。乳糖酸红霉素(胃插管;5 mg/kg)即使在接种后120天也能保护小鼠的存活,但50 mg/kg剂量可将荷瘤小鼠的平均存活时间缩短4-5天[3]。乳糖酸红霉素(i.h.单次注射;50 mg/kg)对大鼠脑缺血再灌注损伤模型具有保护作用[4]。动物模型:具有EAC细胞的雌性ddY小鼠(6周龄)或具有P388细胞的CDF小鼠(6周龄)[3]剂量:0.1mg/kg;0.5mg/kg;10mg/kg;30mg/kg;50mg/kg给药:胃插管;30-120天结果:从5mg/kg剂量开始,降低肿瘤生长并延长小鼠的平均生存时间,然而,50mg/kg剂量缩短了荷瘤小鼠的MST。动物模型:雄性Sprague-Dawley大鼠(8周龄,250-300 g)[4]剂量:50 mg/kg给药:
参考文献

[1]. Gribble MJ, et al. Erythromycin. Med Clin North Am. 1982 Jan;66(1):79-89.

[2]. Nakornchai S, et al. Activity of azithromycin or erythromycin in combination with antimalarial drugs against multidrug-resistant Plasmodium falciparum in vitro. Acta Trop. 2006 Dec;100(3):185-91. Epub 2006 Nov 28.

[3]. Hamada K, et al. Antitumor effect of erythromycin in mice. Chemotherapy. 1995 Jan-Feb. 41(1):59-69.

[4]. Katayama Y, et al. Neuroprotective effects of erythromycin on cerebral ischemia reperfusion-injury and cell viability after oxygen-glucose deprivation in cultured neuronal cells. Brain Res. 2014 Nov 7. 1588:159-67.

 乳糖酸阿奇霉素物理化学性质

密度 0.9083 (rough estimate)
沸点 818.4ºC at 760mmHg
熔点 145-150°
分子式 C49H89NO25
分子量 1092.223
闪点 448.8ºC
精确质量 1091.572388
PSA 411.51000
外观性状 白色至米白色固体
折射率 1.5300 (estimate)
储存条件 20°C
水溶解性 Soluble in water, freely soluble in anhydrous ethanol and in methanol, very slightly soluble in acetone and in methylene chloride.

 乳糖酸阿奇霉素毒性和生态

 乳糖酸阿奇霉素安全信息

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

 乳糖酸阿奇霉素合成线路

~98%

乳糖酸阿奇霉素结构式

乳糖酸阿奇霉素

3847-29-8

文献:Liu, Li Patent: EP2301945 A1, 2011 ; Location in patent: Page/Page column 9-10 ;

 乳糖酸阿奇霉素上下游产品

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 乳糖酸阿奇霉素英文别名

decane-2,10-dione (1:1)
Erythrocin lactobionate
(2R,3R,4R,5R)-2,3,5,6-Tetrahydroxy-4-{[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy}hexanoic acid - (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-{[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy}-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione (1:1) (non-preferred name)
ERYTHROMYCIN LACTOBIONATE USP(CRM STANDARD)
lactobionic acid,compd. with erythromycin
Azithromycin lactobionate
(2R,3R,4R,5R)-2,3,5,6-Tetrahydroxy-4-{[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy}hexanoic acid - (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-{[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy}-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione (1:1)
Erythromycin,lactobionate (1:1) (salt)
4-O-b-D-Galactopyranosyl-D-gluconic Acid compd. with Erythromycin (1:1)
Erythomycin lactobionate
lactobionicacid,compd.witherythromycin(1:1)
tradécane-2,10-dione (1:1)
decane-2,10-dione (1:1) (non-preferred name)
Erythromycin,compd. with lactobionic acid (7CI)
acide (2R,3R,4R,5R)-2,3,5,6-tétrahydroxy-4-{[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxyméthyl)tétrahydro-2H-pyran-2-yl]oxy}hexanoïque - (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-{[(2S,3R,4S,6R)-4-(diméthylamino)-3-hydroxy-6-méthyltétrahydro-2H-pyran-2-yl]oxy}-14-éthyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-méthoxy-4,6-diméthyltétrahydro-2H-pyran-2-yl]oxy}-3,5,7,9,11,13-hexaméthyloxacyclotétradécane-2,10-dione (1:1)
n-2,10-dion(1:1)
erythromycin lactobionate
(2R,3R,4R,5R)-2,3,5,6-Tetrahydroxy-4-{[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy}hexansäure--(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-{[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy}-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2,10-dion(1:1)
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