Nystatin

Nystatin is a polyene antifungal antibiotic effective against yeast and mycoplasma.

Signaling Pathways >> Anti-infection >> Fungal

Research Areas >> Infection

Nystatin results in a significant reduction in buccal epithelial cell adhesion of all six Candida species[1]. Nystatin is an antibiotic that increases the permeability of plasma membranes to small monovalent ions, including chloridion. Nystatin increases apical chloridion permeability to the point where transepithelial chloridion transport is limited by transport across the basolateral membrane of tracheal epithelial cells, which reflects primarily the activity of the cotransporter. Nystatin (400 units/mL) increases the basal level of transepithelial 36Cl flux approximately 1.5-fold and eliminates UTP stimulation of this flux. Nystatin treatment also abolishes UTP stimulation of saturable, basolateral [3H]bumetanide binding, a measure of functioning Na-K-Cl cotransporters in these cells; isoproterenol stimulation of binding is only mildly inhibited by nystatin treatment[2]. Nystatin significantly enhances endostatin uptake by endothelial cells through switching endostatin internalization predominantly to the clathrin-mediated pathway. Nystatin-enhanced internalization of endostatin also increases its inhibitory effects on endothelial cell tube formation and migration[3].

Nystatin combined with endostatin selectively enhances endostatin uptake and biodistribution in tumor blood vessels and tumor tissues but not in normal tissues of tumor-bearing mice, ultimately resulting in elevated antiangiogenic and antitumor efficacies of endostatin in vivo[3]. Liposomal Nystatin, at doses as low as 2 mg/kg of body weight/day, protects neutropenic mice against Aspergillus-induced death in a statistically significant manner at the 50-day time point compared to either the no-treatment, the saline, or the empty-liposome group[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

Cycloheximide | Hygromycin B | Cancidas | 5-Flucytosine | Posaconazole | Terbinafine | Ciclopirox | Isavuconazole | Anidulafungin | Clotrimazole | Clioquinol | Miconazole Nitrate | Pimaricin | Ascomycin | Econazole (nitrate)

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)