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Euphorbia factor L1 (EFL1,  1 ) is a natural tri-ester of 6,17-epoxylathyrol with cancer multidrug resistance (MDR) reversal activity. Several EFL1 derivatives ( 2 – 9 ) were prepared by chemical and microbial transformations and their ability to inhibit P-glycoprotein (P-gp) activity was estimated. Six de-acylated derivatives ( 2 – 7 ) were obtained through base-hydrolysis of  1 , and the base-catalysed hydrolysis  via  KOH and NaOH yielded different hydrolysed products of  1 . Two biotransformed products ( 8 – 9 ) were directly obtained  via  microbial transformation of  1 , and  8  was also formed by microbial conversion of the hydrolysed product  3 . The P-gp modulation of  1 – 9  was assessed by a zebrafish model. The substrate  1  and its biotransformed product  9  as the tri-esters of lathyranes possessed the highest P-gp inhibitory activity with IC 50  values of 34.97 and 15.50 µM, respectively, through down-regulating P-gp expression at the protein level rather than at MDR1 mRNA level.

Microbial and chemical transformations of euphorbia factor L1 and the P-glycoprotein inhibitory activity in zebrafishes