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制霉菌素

制霉菌素用途

Nystatin是一种对酵母和支原体有效的多烯抗真菌抗生素。

制霉菌素作用

有特殊气味及引湿性菌谱及抗菌机理与两性霉素B相似，主要用于皮肤粘膜、口腔、阴道的白色念珠菌感染.

制霉菌素名称

[ CAS 号 ]:
1400-61-9

[ 中文名 ]:
制霉菌素

[ 英文名 ]:
Nystatin

[中文别名 ]:

[英文别名 ]:

biofanal
9,11,13,15-Octadecatetraenoic acid
stamycin
MFCD00036240
nystatin A1
Nystex
nilstat
nystatin A2
nystan
MORONAL

制霉菌素生物活性

[ 描述 ]:

Nystatin是一种对酵母和支原体有效的多烯抗真菌抗生素。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 真菌

研究领域 >> 感染

[体外研究]

制霉菌素导致所有六种念珠菌属物种的颊上皮细胞粘附显着降低[1]。制霉菌素是一种抗生素,可增加质膜对小的单价离子(包括氯离子)的渗透性。制霉菌素增加顶端氯离子渗透性,使得跨上皮细胞氯离子转运受到穿过气管上皮细胞基底外侧膜的转运的限制,这主要反映了协同转运蛋白的活性。制霉菌素(400单位/ mL)使跨上皮36Cl通量的基础水平增加约1.5倍并且消除了该通量的UTP刺激。制霉菌素处理也消除了可饱和的基底外侧[3H]布美他尼结合的UTP刺激,这是这些细胞中功能性Na-K-Cl协同转运蛋白的量度;异戊二烯醇对结合的刺激仅通过制霉菌素治疗轻度抑制[2]。制霉菌素通过主要转换为网格蛋白介导的途径内皮抑素内化,显着增强内皮细胞对内皮抑素的摄取。制霉菌素增强的内皮抑素内化也增加了其对内皮细胞管形成和迁移的抑制作用[3]。

[体内研究]

制霉菌素与内皮抑素联合使用可选择性地增强肿瘤血管和肿瘤组织中的内皮抑素摄取和生物分布,但不能在荷瘤小鼠的正常组织中增强,最终导致内皮抑素在体内的抗血管生成和抗肿瘤效力提高[3]。脂质体制霉菌素,剂量低至2毫克/千克体重/天,与无治疗,生理盐水或无盐治疗相比,在50天时间点以统计学显着方式保护中性粒细胞减少症小鼠免受曲霉菌诱导的死亡。空脂质体组[4]。

[参考文献]

[1]. Ellepola AN, et al. Adhesion of oral Candida species to human buccal epithelial cells following brief exposure to nystatin. Oral Microbiol Immunol. 1999 Dec;14(6):358-63.

[2]. Haas M, et al. Na-K-Cl cotransport in nystatin-treated tracheal cells: regulation by isoproterenol, apical UTP, and [Cl]i. Am J Physiol. 1994 May;266(5 Pt 1):C1440-52.

[3]. Chen Y, et al. Cholesterol sequestration by nystatin enhances the uptake and activity of endostatin in endothelium via regulating distinct endocytic pathways. Blood. 2011 Jun 9;117(23):6392-403

[4]. Wallace TL, et al. Activity of liposomal nystatin against disseminated Aspergillus fumigatus infection in neutropenic mice. Antimicrob Agents Chemother. 1997 Oct;41(10):2238-43

[相关活性小分子]

制霉菌素物理化学性质

[ 密度 ]:
0.9±0.1 g/cm3

[ 沸点 ]:
400.2±14.0 °C at 760 mmHg

[ 熔点 ]:
>155°C (dec.)

[ 分子式 ]:
C₄₇H₇₅NO₁₇

[ 分子量 ]:
276.414

[ 闪点 ]:
297.0±15.2 °C

[ 精确质量 ]:
276.208923

[ PSA ]:
327.45000

[ LogP ]:
6.14

[ 外观性状 ]:
黄色悬浮物

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.504

[ 储存条件 ]:
-20°C，易燃物区域

制霉菌素MSDS

详细MSDS(安全技术说明书)

制霉菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RF5950000

CHEMICAL NAME :: Nystatin

CAS REGISTRY NUMBER :: 1400-61-9

LAST UPDATED :: 199512

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C46-H83-N-O18

MOLECULAR WEIGHT :: 938.30

WISWESSER LINE NOTATION :: T-38-VO D&V GU IU MU OU QU SUTJ C1 D1 EQ F1 WQ A&VQ B&Q F&Q G&Q J&Q L&Q N&Q UO- BT6OTJ CQ DZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 gm/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 - rat

DOSE/DURATION :: 24305 ug/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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8 gm/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 :: 4400 ug/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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 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 :: 3 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 :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 180 mg/kg/90D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 33,306,1977 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - M1053 No. of Facilities: 28 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 8736 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M1053 No. of Facilities: 372 (estimated) No. of Industries: 1 No. of Occupations: 10 No. of Employees: 25202 (estimated) No. of Female Employees: 22859 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X9349 No. of Facilities: 3 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 2199 (estimated) No. of Female Employees: 2176 (estimated)

制霉菌素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
F, C

[ 风险声明 (欧洲) ]:
R11

[ 安全声明 (欧洲) ]:
S22-S24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
RF5950000

[ 海关编码 ]:
2942000000

制霉菌素海关

[ 海关编码 ]: 2942000000

制霉菌素文献

Compounded preparations with nystatin for oral and oromucosal administration.

Acta Pol. Pharm. 70(4) , 759-62, (2013)

Therapy of oral, esophageal and gastrointestinal candidiasis is still a common problem that can be solved by an administration of antimycotics. Major disadvantage of registered commercial antifungal m...

[Clinical factors associated with invasive pulmonary aspergillosis in patients with chronic pneumopathies and respiratory isolation of Aspergillus spp].

Med. Clin. (Barc.) 139(15) , 668-71, (2012)

To determine clinical variables to distinguish invasive pulmonary aspergillosis (IPA) from colonization in patients with chronic pneumopathies with positive culture of Aspergillus spp. in respiratory ...

Topical steroids for chronic wounds displaying abnormal inflammation.

Ann. R. Coll. Surg. Engl. 95(4) , 291-6, (2013)

Chronic, non-healing wounds are often characterised by an excessive, and detrimental, inflammatory response. We review our experience of using a combined topical steroid, antibiotic and antifungal pre...

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