乳糖酸阿奇霉素

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

[ CAS 号 ]:
3847-29-8

[ 中文名 ]:
乳糖酸红霉素

[ 英文名 ]:
n-2,10-dion(1:1)

[中文别名 ]:

[英文别名 ]:

decane-2,10-dione (1:1)
Erythrocin lactobionate
ERYTHROMYCIN LACTOBIONATE USP(CRM STANDARD)
lactobionic acid,compd. with erythromycin
Azithromycin lactobionate
Erythromycin,lactobionate (1:1) (salt)
Erythomycin lactobionate
lactobionicacid,compd.witherythromycin(1:1)
tradécane-2,10-dione (1:1)
decane-2,10-dione (1:1) (non-preferred name)

乳糖酸阿奇霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

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 >> 抗感染 >> 细菌

[ 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

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OD7320000

CAS REGISTRY NUMBER :: 3847-29-8

LAST UPDATED :: 199712

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C37-H67-N-O13.C12-H22-O12

MOLECULAR WEIGHT :: 1092.39

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 61 mg/kg/1D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Ear) - tinnitus Sense Organs and Special Senses (Ear) - changes in vestibular functions

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 60 mg/kg/1D-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate increase, without fall in BP

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 240 mg/kg/4D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Ear) - change in acuity

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 735 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 50 gm/kg/6W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

MUTATION DATA

TYPE OF TEST :: Gene conversion and mitotic recombination

TEST SYSTEM :: Yeast - Saccharomyces cerevisiae

DOSE/DURATION :: 1 gm/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 12,357,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3884 No. of Facilities: 98 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 3317 (estimated) No. of Female Employees: 1523 (estimated)

乳糖酸阿奇霉素

乳糖酸阿奇霉素用途

乳糖酸阿奇霉素名称

乳糖酸阿奇霉素生物活性

乳糖酸阿奇霉素物理化学性质

乳糖酸阿奇霉素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

乳糖酸阿奇霉素安全信息

乳糖酸阿奇霉素合成路线

详细合成路线

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