Uses
21-Hydroxyoligomycin A is an oligomycin antibiotic coisolated with nemadectins.
Uses
21-Hydroxyoligomycin A is a rare member of the oligomycin class isolated as a co-metabolite of nemadectin, hence its original naming as nemadectin omega. Only limited literature references to this metabolite are available. However, in-house testing suggests that 21-hydroxyoligomycin has a more selective action against mammalian tumour cell lines than oligomycin A, exhibiting only weak antifungal and nematocidal activity.
Biological Activity
21-hydroxy oligomycin a is an antibiotic which was first isolated from s. cyaneogriseus ssp.noncyanogenus [1]. 21-hydroxy oligomycin a functions as μm inhibitor of the multidrug efflux pump p-gp, and low nm inhibitors of k-ras pm localization [1].cancer cell viability screening confirmed that 21-hydroxy oligomycin a was cytotoxic to human colorectal carcinoma cells (ic50 > 3 μm), and was inhibitor of the abc transporter efflux pump p-glyco-protein (p-gp). significantly, 21-hydroxy oligomycin a was exceptionally potent inhibitor of k-ras pm localisation with emax of 0.67–0.75 and an ic50 of 1.5–14 nm [1]. 21-hydroxy oligomycin a was inhibitor of k-ras pm localisation in mdck cell with an ic50 of 4.82 ± 0.70 nm. 21-hydroxy oligomycin a was moderately cytotoxic towards both sw620 and sw620 ad300 cells with the ic50 of 14.4 ± 0.6 and 11.8 ± 3.1 μm, respectively. in the flow cytometry assay, 21-hydroxy oligomycin a (20 μm) increased intracellular calcein fluorescence significantly when compared with the negative control [1].
References
[1] salim a a, tan l, huang x c, et al. oligomycins as inhibitors of k-ras plasma membrane localisation[j]. organic & biomolecular chemistry, 2016, 14(2): 711-715.
