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Cerulenin

CAS No. : 17397-89-6

MCE 国际站：Cerulenin

产品活性：Cerulenin 是一种有效的，广泛使用的天然脂肪酸合成酶 (FASN) 抑制剂。Cerulenin 是由真菌 Cephalosporium caeruleus 产生的。Cerulenin 抑制拓扑异构酶I催化活性并增强 SN-38 诱导的细胞凋亡。Cerulenin 具有抗真菌和抗肿瘤活性。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection  |  Apoptosis

作用靶点：Fatty Acid Synthase (FASN)  |  Fungal  |  Apoptosis  |  Antibiotic

结构分类：抗生素  |  疾病研究  |  抗真菌  |  抗生素  |  疾病研究  |  抗癌  |  抗生素  |  其他类  |  抗生素  |  哺乳动物细胞培养  |  结构分类

In Vitro: Cerulenin covalently binds to the catalytic site of FAS and disrupts the condensation reaction of acetyl-COA and malonyl-COA, inhibiting the biosynthesis of fatty acids and sterols in yeast. The Flavonoids quercetin and trans-Chalcone are effective against T. rubrum, with MICs of 125 and 7.5 μg/mL for the wild-type strain (MYA3108) and of 63 and 1.9 μg/mL for the ABC transporter mutant strain (ΔTruMDR2), respectively. The MICs of the Fluconazole and Cerulenin controls are 63 and 125 μg/mL for the wild-type strain and 30 and 15 μg/mL for the mutant strain, respectively. To explore the underlying mechanism of Steroidogenic acute regulatory protein (StAR)’s protective effect on endothelial dysfunction model, the inhibitor of fatty acid synthase and HMG-CoA reductase, Cerulenin (5 μg/mL) and Lovastatin, are used before palmitic acid (PA) added. The mRNA expression of IL-1β, TNFα, VCAM-1 and IL-6 are reduced while NO production is recovered with inhibitor treatment.

In Vivo: Cerulenin treatment of ob/ob mice has obvious effects on body weight. With 2 days of treatment, body weight in treated mice is decreased compared to a 5.7% weight gain in the controls. With prolonged (7 days) treatment, no body weight loss is observed, but body weight gain is slowed. In all groups, 60 mg/kg of Cerulenin is more effective than 30 mg/kg in inhibiting weight gain. If given daily or every other day, ATP content are increased 58.1% and 61.5% respectively by 7-day treatment of 60 mg/kg Cerulenin. Significant ATP elevation is also observed with only 2 days of treatment with 60 mg/kg Cerulenin. In contrast, 30 mg/kg Cerulenin, given either 2 or 7 days, does not show any significant effect on cellular ATP content.

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