TABLE 2

Optimal alamethicin concentration for activation of β-estradiol (UGT1A1) and trifluoperazine (UGT1A4) glucuronidation in human liver microsomes

	Alamethicin Concentration^{^a}					β-Estradiol-3-glucuronide				Trifluoperazine N-Glucuronide
	μg/ml	μg/mg HLM protein				μM				μM
HLM conc., mg/ml	0.01–0.5	0.01	0.05	0.2	0.5	0.01	0.05	0.2	0.5	0.01	0.05	0.2	0.5
	0	0	0	0	0	0.20	0.79	2.6	3.5	0.28	1.3	3.4	4.8
	1.0	100	20	5.0	2.0	0.17	0.77	2.2	3.3	0.29	1.4	3.5	4.8
	1.71	171	34.2	8.55	3.42	0.18	0.79	2.3	3.3	0.28	1.4	3.5	4.6
	2.92	292	58.4	14.6	5.84	0.19	0.88	2.2	3.4	0.31	1.5	3.5	4.7
	5.0	500	100	25	10	0.28	1.3	3.4	4.1	0.44	2.2	4.6	5.5
	8.55	855	171	42.8	17.1	0.32	1.5	3.4	4.6	0.52	2.6	5.2	6.4
	14.6	1460	292	73	29.2	0.32	1.4	3.7	4.7	0.51	2.6	5.2	6.6
	25	2500	500	125	50	0.27	1.2	3.3	4.5	0.47	2.5	5.3	6.8

↵a HLM were incubated without and with alamethicin at a constant concentration ranging 1 to 25 μg/ml at 4 HLM protein concentrations ranging 0.01 to 0.5 mg/ml, as described under Materials and Methods. Based on the HLM concentration in incubation, the corresponding alamethicin concentration expressed as μg/mg HLM protein ranges 100 to 2500 μg/mg for 0.01 mg/ml HLM and 2 to 50 μg/mg for 0.5 mg/ml HLM.