Pyoluteorin

Pyoluteorin is an antibiotic that inhibits Oomycete fungi, including the plant pathogen Pythium ultimum, and suppresses plant diseases caused by this fungus[1]. Pyoluteorin induces human triple-negative breast cancer MDA-MB-231 cells apoptosis in vitro. Pyoluteorin can be used for the research of human triple-negative breast cancer[2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Fungal

Pyoluteorin is an antifungal compound composed of a bichlorinated pyrrole linked to a resorcinol moiety, were identified within a 24-kb genomic region of Pseudomonas fluorescens Pf-5[1]. Pyoluteorin has significant cytotoxicity towards MCF-7 (IC50=1.84 μM). Pyoluteorin also displays significantly selective cytotoxicity against BT474, HCC1954, MAD-MB-468, MDA-MB-231, and MCF-10A cells with IC50s of 9.75±0.16, 0.94±0.01, 3.89±0.08, 0.97±0.01, and 57.01±0.76 μM, respectively[2]. Pyoluteorin (0.1-10 μM; for 24 hours) induces change of apoptosis-related protein expressions. Pyoluteorin-induced cell apoptosis in MDA-MB-231 is related to Bcl-2 family proteins and caspase cascade[2]. Pyoluteorin (0.1-10 μM; for 24 h) induces cell cycle arrest and apoptosis in human triple-negative breast cancer cells MDA-MB-231[2]. Cell Proliferation Assay[2] Cell Line: Human triple-negative breast cancer cell MDA-MB-231 Concentration: 0, 0.032, 0.16, 0.8, 4, 20, 100 μM Incubation Time: 24, 48, 72 hours Result: Inhibited cells proliferation in a dose- and time-dependent manner. Western Blot Analysis[2] Cell Line: MDA-MB-231 cells Concentration: 0.1, 0.3, 1, 3, 10 μM Incubation Time: 24 hours Result: The levels of the anti-apoptotic proteins Bcl-2, Bcl-XL and PARP were obviously decreased while the pro-apoptotic proteins BAX and caspase 3 were increased in a dose-dependent manner.

[1]. B Nowak-Thompson, et al. Characterization of the pyoluteorin biosynthetic gene cluster of Pseudomonas fluorescens Pf-5. J Bacteriol. 1999 Apr;181(7):2166-74.

[2]. Ting Ding, et al. Pyoluteorin induces cell cycle arrest and apoptosis in human triple-negative breast cancer cells MDA-MB-231. J Pharm Pharmacol. 2020 Jul;72(7):969-978.

DATA ITEMS CITED :

2

MOLECULAR FORMULA :

C11-H7-Cl2-N-O3

MOLECULAR WEIGHT :

272.09

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

125 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 5,48,1981

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

45 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 5,48,1981