硬脂酸红霉素

硬脂酸红霉素用途

硬脂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。硬脂酸红霉素结合细菌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]。硬脂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]。

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硬脂酸红霉素名称

[ CAS 号 ]:
643-22-1

[ 中文名 ]:
硬脂酸红霉素

[ 英文名 ]:
Erythromycin stearate

[中文别名 ]:

硬酯酸红霉素

[英文别名 ]:

EINECS 211-396-1
MFCD00084690
Erythromycin stearate

硬脂酸红霉素生物活性

[ 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]

硬脂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]。硬脂酸红霉素(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]

硬脂酸红霉素(胃插管；0.1-50 mg/kg；30-120天)可减少肿瘤生长,并延长小鼠从5 mg/kg剂量开始的存活时间[3]。硬脂酸红霉素(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]。硬脂酸红霉素(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月龄)[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：皮下单次注射结果：减少梗死体积和水肿体积,改善神经功能缺损。

[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]. K Hamada, et al. Antitumor Effect of Erythromycin in Mice. Chemotherapy

[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.

硬脂酸红霉素物理化学性质

[ 密度 ]:
1.112g/cm3

[ 熔点 ]:
77-79ºC

[ 分子式 ]:
C₅₅H₁₀₃NO₁₅

[ 分子量 ]:
1004.377

[ 闪点 ]:
523.101ºC

[ 精确质量 ]:
1003.717102

[ PSA ]:
231.21000

[ LogP ]:
8.11810

[ 外观性状 ]:
细白色粉末

[ 折射率 ]:
1.518

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stable. Combustible. Incompatible with acids, strong oxidizing agents.

[ 水溶解性 ]:
ethanol: soluble50mg/mL, clear to very slightly hazy, colorless

硬脂酸红霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KF5785000

CHEMICAL NAME :: Erythromycin, stearate (salt)

CAS REGISTRY NUMBER :: 643-22-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C37-H67-N-O13.C18-H36-O2

MOLECULAR WEIGHT :: 1018.59

WISWESSER LINE NOTATION :: T-14-VO GVTJ C2 DQ D EQ F H JQ J L N KO- BT6OTJ CQ DN1&1 F& MO- FT6OTJ B CQ DO1 D &622

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of endocrine pancreas Gastrointestinal - nausea or vomiting Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 34,93,1996

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3112 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,211,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2500 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,211,1990

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 413 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,211,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 13037 mg/kg/14D-C

TOXIC EFFECTS :: Behavioral - food intake (animal) Gastrointestinal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: NTPTR* National Toxicology Program Technical Report Series. (Research Triangle Park, NC 27709) No.206- Volume(issue)/page/year: NTP-TR-338,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 71 gm/kg/14D-C

TOXIC EFFECTS :: Behavioral - food intake (animal) Gastrointestinal - other changes Related to Chronic Data - death

REFERENCE :: NTPTR* National Toxicology Program Technical Report Series. (Research Triangle Park, NC 27709) No.206- Volume(issue)/page/year: NTP-TR-338,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - M0726 No. of Facilities: 592 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 1977 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M0726 No. of Facilities: 78 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1108 (estimated) No. of Female Employees: 615 (estimated)

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硬脂酸红霉素安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H317-H334

[ 警示性声明 ]:
P261-P280-P284-P304 + P340-P342 + P311

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R42/43

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
2

[ RTECS号 ]:
KF5785000

[ 海关编码 ]:
2942000000

硬脂酸红霉素海关

[ 海关编码 ]: 2942000000

硬脂酸红霉素文献

Antibiotics for ureaplasma in the vagina in pregnancy.

Cochrane Database Syst. Rev. (9) , CD003767, (2011)

Preterm birth is a significant perinatal problem contributing to perinatal morbidity and mortality. Heavy vaginal ureaplasma colonisation is suspected of playing a role in preterm birth and preterm ru...

Cholestasis and liver cell damage due to hypersensitivity to erythromycin stearate--recurrence following therapy with erythromycin succinate.

Wien. Klin. Wochenschr. 111(2) , 76-7, (1999)

Erythromycin is a frequently used antibiotic in patients with atypical respiratory infection and/or an allergy to penicillin. We report the case of a young woman who developed severe cholestasis and j...

Efficacy and tolerance of roxithromycin in comparison with erythromycin stearate in patients with lower respiratory tract infections.

Scand. J. Infect. Dis. 24(2) , 219-25, (1992)

The efficacy and tolerance of roxithromycin 150 mg b.i.d. were compared with those of erythromycin stearate 500 mg b.i.d. in patients with lower respiratory tract infections. Out of 86 patients recrui...

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