Dooley T P, Haldeman-Cahill R, Joiner J, Wilborn T W
IntegriDerm, Inc., 2130 Memorial Parkway, South West, Huntsville, Alabama, 35801, USA.
Biochem Biophys Res Commun. 2000 Oct 14;277(1):236-45. doi: 10.1006/bbrc.2000.3643.
The bioavailability of drugs administered topically or orally depends on their metabolism by epithelial enzymes such as the cytosolic sulfotransferases (SULT). Reverse transcriptase-polymerase chain reaction (RT-PCR) methods were established to detect expression of 8 SULT genes and 4 arylsulfatase (ARS) genes in human tissues of epithelial origin and in cultures of normal and transformed (cancer) cells. The results indicate: (i) SULT 1A1, 1A3, ARSC, and ARSD genes are ubiquitously expressed; (ii) expression is frequently similar between cell lines and corresponding tissues; (iii) SULT gene expression in normal cultured cells is generally comparable to the expression in associated transformed (cancer) cell lines; (iv) SULT 1A1 promoter usage is mainly tissue specific; however, both promoters are frequently used in SULT 1A3 expression; and (v) the expression profile of SULT 1A1, 1A3, 1E1, and 2B1a/b suggests that one or more of these isoforms may be involved in the cutaneous sulfoconjugation of minoxidil and cholesterol.
局部或口服给药药物的生物利用度取决于它们被上皮酶（如胞质磺基转移酶，SULT）代谢的情况。建立了逆转录聚合酶链反应（RT-PCR）方法来检测8种SULT基因和4种芳基硫酸酯酶（ARS）基因在人上皮组织以及正常和转化（癌）细胞培养物中的表达。结果表明：（i）SULT 1A1、1A3、ARSC和ARSD基因普遍表达；（ii）细胞系与相应组织之间的表达通常相似；（iii）正常培养细胞中的SULT基因表达通常与相关转化（癌）细胞系中的表达相当；（iv）SULT 1A1启动子的使用主要具有组织特异性；然而，两种启动子在SULT 1A3表达中均经常被使用；以及（v）SULT 1A1、1A3、1E1和2B1a/b的表达谱表明这些同工型中的一种或多种可能参与了米诺地尔和胆固醇的皮肤硫酸化结合。
