Drug Discov Ther. 2022;16(6):273-279. (DOI: 10.5582/ddt.2022.01087)

Screening for microbial potentiators of neutral lipid degradation in CHO-K1 cells

Nur EAA, Kobayashi K, Ohte S, Tomoda H, Ohshiro T


A cell-based assay was conducted to screen microbial culture broths for potentiators of neutral lipid degradation in Chinese Hamster Ovary K1 cells. A total of 5,363 microbial cultures from fungi and actinomycetes were screened in this assay. Brefeldin A (1) from fungal cultures was found to promote the degradation of triacylglycerol (TG) with an EC50 of 2.6 μM. Beauveriolides I (2), III (3), beauverolides A (4), B (5), and K (6) from fungal cultures showed potentiating effect on cholesteryl ester (CE) degradation with EC50s ranging from 0.02 to 0.13 μM. Among these compounds, 2 and 6 exhibited the strongest activities (EC50, 0.02 μM). From actinomycete cultures, oxohygrolidin (7) (EC50 for TG and CE, > 1.7 and 0.8 μM, respectively) and hygrolidin (8) (EC50 for TG and CE, 0.08 and 0.004 μM, respectively) promoted degradation of CE more preferably than TG.

KEYWORDS: Neutral lipid degradation, screening, microbial potentiator, brefeldin A, beauveriolide, hygrolidin

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