tcsc5717 Nigericin (sodium salt)

Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H⁺, K⁺, and Pb²⁺ ionophore.

In Vitro: Nigericin (0.1 µM) decreases inhibits proliferation and clonogenicity of H460 lung cancer cells in a dose dependent manner. Nigericin inhibits migration and invasion of H460 lung cancer cells^[1]. Nigericin (0.1-10 nM) has apparently a dual effect on cell volume, that is a shrinking effect at lower Nigericin concentrations and a swelling effect at higher concentrations. Nigericin (0.1-1 nM) significantly decreases cytosolic pH (pHi), and slightly increases the pHi at 5 and 10 nM^[2]. Nigericin exhibits higher toxicity on S18 cells than S26 cells, with IC₅₀ of 2.03±0.55 μM and 4.77±2.35 μM, respectively. Nigericin can selectively kill cancer stem cells in NPC in vitro. Nigericin dramatically reduces the migration ability of S18 and HONE-1 cells^[3]. Nigericin exhibits gteat toxicity for the HT29 and SW116 cell line with IC₅₀ of 12.92±0.25 μmol and 15.86±0.18 μmol. Nigericin also shows a decreased ability to form colonies under anchorage-independent conditions in a standard soft agar assay^[4].

In Vivo: Ngericin (4 mg/kg, i.p.) significantly reduces tumor growth and acts synergistically with the chemotherapeutic agent DDP, as shown by the tumor volumes. Nigericin markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partially restores CSC content and metastatic ability of NPC cells under Nigericin treatment. The downregulation of Bmi-1 may be involved in the inhibitory effect of Nigericin on CSCs in NPC^[3].