Valinomycin

Valinomycin是一种具有钾选择性离子活性的环沉积肽抗生素。它可以作为解偶联剂来诱导去极化。.

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货号: ajci18138
CAS: 2001-95-8
别名: 缬氨霉素,NSC 122023
分子式: C54H90N6O18
分子量: 1111.32
纯度: >98%
溶解度: DMF: 30 mg/ml,DMSO: 5 mg/ml,Ethanol: 10 mg/ml
储存: Store at -20°C,protect from light
库存: 现货

Background

Valinomycin is a dodecadepsipeptide antibiotic, which is obtained from several Streptomyces strains. Valinomycin functions as a potassium-specific transporter and promotes the movement of K+ through lipid membranes. Excessive K+ efflux is an ionic mechanism underlying apoptosis.It can be used as uncoupling agent to induce depolarization[1-3].

Valinomycin(1-100μM;12-24 h) treated CHO cells underwent an apoptotic event due to potassium efflux[4]. Valinomycin (2 nM) induced energy-dependent mitochondrial swelling, cytochrome c release, cytosolic NADH/cytochrome c oxidation and apoptosis[5]. Neurite formation and membrane changes of mouse neuroblastoma cells induced by valinomycin(100 μM)^[6].

Incorporation of valinomycin into multilamellar liposomes composed of dimyristoyl phosphatidyl choline:cholesterol:phosphatidyl serine (10:4:1 M ratio) results in a profound reduction in toxicity with maintainence of antitumor efficacy in mice, the LD50 for liposome incorporated valinomycin (MVL-VM) is in excess of 50 mg/kg[7].

参考文献:
[1]. Varma S, Sabo D, ,et,al. K+/Na+ selectivity in K channels and valinomycin: over-coordination versus cavity-size constraints. J Mol Biol. 2008 Feb 8;376(1):13-22. doi: 10.1016/j.jmb.2007.11.059. Epub 2007 Nov 28. PMID: 18155244; PMCID: PMC2390915.
[2]. Daniele RP, Holian SK. A potassium ionophore (valinomycin) inhibits lymphocyte proliferation by its effects on the cell membrane. Proc Natl Acad Sci U S A. 1976 Oct;73(10):3599-602. doi: 10.1073/pnas.73.10.3599. PMID: 1068473; PMCID: PMC431165.
[3]. Berezin SK. Valinomycin as a Classical Anionophore: Mechanism and Ion Selectivity. J Membr Biol. 2015 Aug;248(4):713-26. doi: 10.1007/s00232-015-9784-y. Epub 2015 Mar 4. PMID: 25736817.
[4]. Abdalah R, Wei L, ,et,al. Valinomycin-induced apoptosis in Chinese hamster ovary cells. Neurosci Lett. 2006 Sep 11;405(1-2):68-73. doi: 10.1016/j.neulet.2006.06.055. Epub 2006 Jul 20. PMID: 16857314.
[5]. Lofrumento DD, La Piana G, ,et,al. Valinomycin induced energy-dependent mitochondrial swelling, cytochrome c release, cytosolic NADH/cytochrome c oxidation and apoptosis. Apoptosis. 2011 Oct;16(10):1004-13. doi: 10.1007/s10495-011-0628-7. PMID: 21739274.
[6]. Koike T. Neurite formation and membrane changes of mouse neurobalstoma cells induced by valinomycin. Biochim Biophys Acta. 1978 Jun 2;509(3):429-39. doi: 10.1016/0005-2736(78)90237-7. PMID: 656419.
[7]. Daoud SS, Juliano RL. Reduced toxicity and enhanced antitumor effects in mice of the ionophoric drug valinomycin when incorporated in liposomes. Cancer Res. 1986 Nov;46(11):5518-23. PMID: 3756900.

缬霉素Valinomycin是一种十二肽抗生素,从几种链霉菌菌株中获得。Valinomycin作为钾特异性转运体,促进钾离子通过脂质膜的运动。过量的K+外排是细胞凋亡的离子机制。它可以作为解偶联剂来诱导去极化[1-3]。

Valinomycin (1-100μM;12-24 h)处理的CHO细胞由于钾外排而发生凋亡事件[4]。Valinomycin (2 nM)诱导能量依赖性线粒体肿胀、细胞色素C释放、胞浆NADH/细胞色素c氧化和细胞凋亡[5]。Valinomycin (100 μM)诱导小鼠神经母细胞瘤细胞的神经突形成和膜的改变[6]。

将Valinomycin掺入由二肉豆醇磷脂酰胆碱:胆固醇:磷脂酰丝氨酸(10:4:1)组成的多层脂质体中,可显著降低小鼠的毒性并保持抗肿瘤功效,掺入缬霉素脂质体的LD50超过50 mg/kg[7]。

Protocol

Cell experiment^[1]:
Cell lines	CHO cells
Preparation method	Valinomycin is added into the culture medium.
Reaction Conditions	1-100μM;12-24 h
Applications	100 μM valinomycin caused 77% and 86% cell death at 12 h and 24 h, respectively.
参考文献: [1]. Abdalah R, Wei L,et,al. Valinomycin-induced apoptosis in Chinese hamster ovary cells. Neurosci Lett. 2006 Sep 11;405(1-2):68-73. doi: 10.1016/j.neulet.2006.06.055. Epub 2006 Jul 20. PMID: 16857314.