Lipoxamycin hemisulfate 是一种抗真菌抗生素，也是一种有效的丝氨酸棕榈酰转移酶 (serine palmitoyltransferase) 抑制剂，IC50 为 21 nM。
Lipoxamycin hemisulfate is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM[1][2].
Lipoxamycin has antifungal activity against a panel of humanpathogenic fungi with better potency against some of the Candida species (MIC values, 0.25-16 µg/mL). Cryptococcus neoformans is the most sensitive organism, followed by various species of Candida. Other filamentous fungi are sensitive to the Lipoxamycin in disk diffusion assays[1].Lipoxamycin has a long alkyl chain and an amino-containing polar head group. Lipoxamycin is on the same order of potency as the sphingofungins and also have potent activity against the mammalianenzyme[1].
Lipoxamycin is highly toxic in mice when applied subeutaneously or topically. Toxicity may be mechanism based, since studies with a Chinese hamster ovary cell mutant have shown that the serine palmitoyltransferase is an essential enzymein mammalian cells[1].
[1]. S M Mandala, et al. Inhibition of Serine Palmitoyl-Transferase Activity by Lipoxamycin. J Antibiot (Tokyo). 1994 Mar;47(3):376-9. [2]. H A Whaley. The Structure of Lipoxamycin, a Novel Antifungal Antibiotic. J Am Chem Soc. 1971 Jul 28;93(15):3767-9.
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