Ionomycin calcium salt is a narrow spectrum antibiotic being active against Gram-positive bacteria, which produced by the bacterium Streptomyces conglobatus[1]. Ionomycin calcium salt promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC)[2].
In vitro, treatment with 2 µM Ionomycin in LCLC 103H cells results in an instantaneous increase in intracellular Ca2+ concentration from 50 to 180 nM. And in Ionomycin-treated cultures, there is obvious DNA fragmentation and PARP cleavage to an 85-kDa fragment, and necrosis could be detected in ~1-5% of the Ionomycin treated cells[2]. In ras oncogene expressing cells, Ionomycin leads to a dose dependent increase of intracellular calcium activity. At 100 nmol/l ionomycin intracellular calcium is increased from 114 ± 17 nmol/l to 342 ± 24 nmol/l, a value within the range of intracellular calcium concentrations following application of bradykinin[3].
In vivo efficacy test, treatment with 1 µm ionomycin for 6 h, ubiquitination of ENaC-β was robustly enhanced in cells overexpressing wild-type Nedd4-2a[4].
References:
[1] Liu WC, et al. Ionomycin, a new polyether antibiotic. J Antibiot (Tokyo). 1978 Sep;31(9):815-9.
[2] Chatila T, et al. Mechanisms of T cell activation by the calcium ionophore ionomycin. J Immunol. 1989 Aug 15;143(4):1283-9.
[3] WÖll E, et al. The role of calcium in cell shrinkage and intracellular alkalinization by bradykinin in Ha-ras oncogene expressing cells. FEBS Lett. 1993 May 17;322(3):261-5.
[4] Wang J, et al. Calcium activates Nedd4 E3 ubiquitin ligases by releasing the C2 domain-mediated auto-inhibition. J Biol Chem. 2010 Apr 16;285(16):12279-88.
Ionomycin calcium salt是一种窄谱抗生素,对革兰氏阳性菌具有活性,由丛生链霉菌(Streptomyces conglobatus)产生[1]。Ionomycin calcium salt可促进细胞凋亡。Ionomycin calcium salt还能诱导激活蛋白激酶 C (PKC)[2]。
在体外,用 2 µM Ionomycin calcium sal处理 LCLC 103H 细胞,细胞内 Ca2+ 浓度会瞬间从 50 nM 增至 180 nM。在经Ionomycin calcium sal处理的培养物中,会出现明显的 DNA 断裂和 PARP 分裂,形成 85 kDa 的片段,在约 1-5% 经Ionomycin calcium sal处理的细胞中可检测到坏死[2]。在表达ras癌基因的细胞中,Ionomycin calcium sal会导致细胞内钙活性的剂量依赖性增加。当Ionomycin calcium sal浓度为 100 nmol/l 时,细胞内钙的浓度从 114 ± 17 nmol/l 增至 342 ± 24 nmol/l,这一数值在使用缓激肽后细胞内钙浓度的范围内[3]。
在体内药效试验中,用 1 µm Ionomycin calcium sal处理 6 小时后,在过表达野生型 Nedd4-2a 的细胞中,ENaC-β 的泛素化显著增强[4]。