Biochemical Pharmacology 2005-03-15

Involvement of SULT1A3 in elevated sulfation of 4-hydroxypropranolol in Hep G2 cells pretreated with beta-naphthoflavone.

Junko Miyano, Shigeo Yamamoto, Nobumitsu Hanioka, Shizuo Narimatsu, Tsutomu Ishikawa, Kenichiro Ogura, Tadashi Watabe, Masuhiro Nishimura, Nobuhiko Ueda, Shinsaku Naito

文献索引：Biochem. Pharmacol. 69(6) , 941-50, (2005)

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摘要

Pretreatment of Hep G2 cells with beta-naphthoflavone (BNF 1-25microM) significantly increased cytosolic sulfation activities of 4-hydroxypropranolol (4-OH-PL) racemate. The profile was similar to those of sulfations towards dopamine and triiodothyronine in the same cytosolic fractions. Kinetic studies of 4-OH-PL sulfation in Hep G2 cytosolic fractions revealed that V(max) values increased but apparent K(m) values remained unchanged following the BNF pretreatment. Among five recombinant human SULT isoforms (SULT1A1, -1A3, -1B1, -1E1 and -2A1) examined, only SULT2A1 did not show 4-OH-PL sulfation activities under the conditions used. SULT1A3 and -1E1 exhibited an enantioselectivity of 4-OH-R-PL sulfation>4-OH-S-PL sulfation, which agreed with that of BNF-pretreated Hep G2 cells as well as of nontreated cells, whereas SULT1A1 and -1B1 showed a reversed enantioselectivity (R