制霉菌素

Nystatin是一种对酵母和支原体有效的多烯抗真菌抗生素。

信号通路 >> 抗感染 >> 真菌

研究领域 >> 感染

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]。

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]。

[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

放线菌酮 | 潮霉素B | 醋酸卡泊芬净 | 5-氟胞嘧啶 | 泊沙康唑 | 特比萘芬 | 环吡酮胺 | 艾沙康唑 | 阿尼芬净 | 克霉唑 | 5-氯-8-羟基-7-碘喹啉 | 硝酸咪康唑 | 纳他霉素 | 长川霉素 | 硝酸益康唑

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)