nargenicin A1

Nargenicin is a macrolide antibiotic that selectively inhibits the growth of S. aureus, methicilin resistant S. aureus (MRSA), and M. luteus (MICs = 0.6, 0.3, and 2.5 μg/ml, respectively) over a panel of 11 Gram-positive and Gram-negative bacteria (MICs = >80 μg/ml). It dose-dependently inhibits S. aureus DnaE in the presence of DNase I-activated DNA and E. coli DnaE when used at concentrations of 0.00001-0.1 and 0.01-100 μg/mL, respectively. In murine BV-2 microglial cells, nargenicin (1 μM) inhibits cytokine expression and nitric oxide production induced by LPS. Nargenicin (200 μM), when used in combination with 1,25-dihydroxyvitamin D₃ or all-trans retinoic acid , reduces cell proliferation by 37-47% and increases cell differentiation by 82-85% in HL-60 human myeloid leukemia cells. In vivo, nargenicin (50 mg/kg, p.o.) reduces the number of colony-forming units (CFUs) in infected kidneys by 100,000-fold in a murine model of S. aureus infection.

Nargenicin A1 is an antibiotic with a broad efficacy.

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[1] JAE KYUNG SOHNG. Production, isolation and biological activity of nargenicin from Nocardia sp. CS682[J]. Archives of Pharmacal Research, 2008, 31 10: 1339-1345. DOI: 10.1007/s12272-001-2115-0
[2] RONALD E PAINTER. Elucidation of DnaE as the Antibacterial Target of the Natural Product, Nargenicin.[J]. Chemistry & biology, 2015, 22 10: 1362-1373. DOI: 10.1016/j.chembiol.2015.08.015
[3] JIN CHEOL YOO. Nargenicin attenuates lipopolysaccharide-induced inflammatory responses in BV-2 cells.[J]. Neuroreport, 2009, 20 11: 1007-1012. DOI: 10.1097/wnr.0b013e32832d2239
[4] SEUNG HYUN KIM  Tae S K  Jin Cheol Yoo. Nargenicin enhances 1,25-dihydroxyvitamin D3- and all-trans retinoic acid-induced leukemia cell differentiation via PKCβI/MAPK pathways[J]. Biochemical pharmacology, 2009, 77 11: Pages 1694-1701. DOI: 10.1016/j.bcp.2009.03.004