中文名：缬氨霉素

国际站：Valinomycin | 缬氨霉素

AS：2001-95-8

品牌：MedChemExpress (MCE)

存储条件：Powder: -80°C, 2 years; -20°C, 1 year.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：Valinomycin (NSC 122023) 是一种环缩肽类抗生素，可作为钾选择性离子载体。 Valinomycin (NSC 122023) 通过作用于细胞膜抑制淋巴细胞增殖，并诱导 CHO 细胞凋亡^[1]。 Valinomycin 诱导 PINK1 激活，导致 Parkin Ser65 磷酸化^[2]。

体外：Lipo-Valinomycin (1-100 μM, 24 h) 剂量依赖性地抑制 HepG2 的细胞活性[2]。 Lipo-Valinomycin (15 μM, 12 h) 破坏线粒体膜电位并诱导 HepG2 的细胞凋亡 (23%)[2]。 1.19 Valinomycin 生物活性[1] Bioactivity Target Efficacy Antibacterial Streptococcus pyogenes MIC 0.02 µg/mL Clostridium sporogenes MIC 8 µg/mL Enterococcus faecalis MIC 0.39–0.78 µg/disk Streptococcus pneumoniae MIC 0.39–0.78 µg/disk Micrococcus luteus MIC 25–50 µg/disk Antifungal Candida albicans MIC 0.39–0.78 µg/disk Cryptococcus neoformans MIC 50–100 µg/disk Phytophthora capsici IC50 15.9 µg/mL Botrytis cinerea MIC 4 µg/mL Magnaporthe grisea MIC 4 µg/mL Candida albicans MIC 32 µg/mL Colletotrichum gloeosporioides MIC 256 µg/mL Rhizoctonia solani MIC 256 µg/mL Penicillium verrucosum IC50 0.005 ng/mL Antiviral SARS-CoV EC50 0.85 µM PRRSV IC50 24 nM RSV IC50 0.0015 µM MERS-CoV IC50 84 nM HCoV-OC43 EC50 4.43 µM HCoV-NL63 EC50 1.89 µM MHV-A59 EC50 6.78 µM LACV IC50 588 nM RVFV MP-12 IC50 41 nM HRV2 IC50 610 nM CVB3 IC50 971 nM ZIKV IC50 78 nM KEYV IC50 156 nM HCoV-229E IC50 67 nM LASV EC50 0.61 µM LCMV EC50 0.15 µM Antitumor Human ovarian tumor cells CaOV-3 IC50 0.1 nM Murine P388 leukemia cancer cells GI50 0.019 µg/mL Human ovary OVCAR-3 tumor cells GI50 0.19 ng/mL Brain SF-295 tumor cells GI50 0.35 ng/mL Renal A-498 carcinoma cells GI50 1.9 ng/mL Lung NCI-H460 cancer cells GI50 0.21 ng/mL Colon KM20L2 carcinoma cells GI50 0.27 ng/mL Melanoma SK-MEL-5 cancer cells GI50 0.26 ng/mL Rat C6 glioma cells IC50 0.4 µM Human A2780 ovarian carcinoma cells IC50 2.18 µM Human MCF-7 breast carcinoma cells IC50 1.77 µM Human HepG2 hepatocellular carcinoma cells IC50 0.0008 µM Human U251 glioma cells IC50 7.6 nM MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Lipo-Valinomycin (1-40 μg/g, 静脉注射, 每二天, 16 d) 抑制裸鼠内的 HepG2 肿瘤生长[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: nude mice with HepG2[2] Dosage: 1, 2, 5, 10, 20, 40 μg/g Administration: Intravenous injection (i.v.), every two days for 16 d Result: Exerted remarkable inhibition effect on tumor growth and no weight loss during the therapeutic period. Caused destructive tumor necrosis as most of the tumor cells were in apoptotic status.

参考文献：

[1]. Daniele RP, et al. 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.

[2]. Tosteson DC, et al. The effect of valinomycin on potassium and sodium permeability of HK and LK sheep red cells. J Gen Physiol. 1967 Dec;50(11):2513-25.

[3]. Abdalah R, et al. Valinomycin-induced apoptosis in Chinese hamster ovary cells. Neurosci Lett. 2006 Sep 11;405(1-2):68-73.

[4]. Kondapalli C, et al. PINK1 is activated by mitochondrial membrane potential depolarization and stimulates Parkin E3 ligase activity by phosphorylating Serine 65. Open Biol. 2012 May;2(5):120080.

[5]. Huang S, et al. The Nonribosomal Peptide Valinomycin: From Discovery to Bioactivity and Biosynthesis. Microorganisms. 2021，9(4):780.

[6]. Zhang QW, et al. RETRACTED: Liposomal valinomycin mediated cellular K+ leak promoting apoptosis of liver cancer cells. J Control Release. 2021，337:317-328.