Table 1.

Effect of saccharolactone on various UGT activities measured using pooled human liver microsomes (pHLMs) and recombinant UGTs. A substrate concentration of 4 mM was used for the 5-HT assay, 200 μM for the trifluoperazine, 1 mM for codeine, 500 μM for AZT, 5 mM for salicylic acid, and 100 μM for the estradiol assay.

	Saccharolactone Concentration (mM)
	0	1	2	5	10	20
5-HT glucuronidation
pHLM	100±3	104±8	93±5	86±4a	87±4a	63±5a
UGT1A6 (insect)	100±2			88±7		96±0
UGT1A6 (HEK293)	100±4			91±6		90±7
Trifluoperazine glucuronidation
pHLM	100±5	98±5	101±9	95±3	93±4	97±5
UGT1A4	100±10			90±4		82±5a
Codeine glucuronidation
pHLM	100±2	98±7	97±4	91±2a	95±5	88±8
UGT2B4	100±11			91±4		88±2
UGT2B7	100±9.04			90±7		90±3
AZT glucuronidation
pHLM	100±11	96±2	98±2	94±2	94±3	94±1
UGT2B7	100±3			102±2		102±8
Salicylic Acid glucuronidation
pHLM	100±8	101±5	111±5	83±3a	90±1	85±9a
UGT1A9	100±13			96±7		99±7
Estradiol-3 glucuronidation
pHLM	100±18	68±5	84±1	76±9a	67±5a	67±7a
UGT1A1	100±12			92±2		87±5
UGT1A3	100±25			92±18		97±10
Estradiol-17 glucuronidation
pHLM	100±17	71±4a	81±8	78±7a	68±2	66±6a
UGT1A3	100±12			90±14		98±10
UGT2B7	100±7			97±2		87±7a

Data are presented as mean±s.d. % of the control activity (measured at 0 mM), n=3.

^aP<0.05 points versus control activity by unpaired t-test.