Du Zhongliang, Jiao Yukun, Shi Lianting
Department of Pharmacy, Weifang Yidu Central Hospital, Qingzhou, Shandong, China (mainland).
Med Sci Monit. 2016 Oct 31;22:4107-4113. doi: 10.12659/msm.897626.
BACKGROUND This study aimed to analyze the relationship of UGT2B7 and UGT1A4 polymorphisms with metabolism of valproic acid (VPA) and lamotrigine (LTG) in epileptic children. MATERIAL AND METHODS We administered VPA (102) and LTG (102) to 204 children with epilepsy. Blood samples were collected before the morning dose. Serum concentration of LTG was measured by high-performance liquid chromatography (HPLC). Serum VPA concentration was tested by fluorescence polarization immunoassay. UGT2B7 A268G, C802T, and G211T polymorphisms, as well as UGT1A4 L48V polymorphism, were assayed by direct automated DNA sequencing after PCR. Evaluation of efficacy was conducted using the Engel method. RESULTS The adjusted serum concentration of VPA was 4.26 μg/mL per mg/kg and LTG was 1.56 μg/mL per mg/kg. Multiple linear regression analysis revealed that VPA or LTG adjusted concentration showed a good linear relation with sex and age. UGT2B7 A268G and C802T polymorphisms were demonstrated to affect the serum concentration of VPA (F=3.147, P=0.047; F=22.754, P=0.000). UGT1A4 L48V polymorphism was not related with the serum concentration of LTG (F=5.328, P=0.006). In the efficacy analysis, we found that C802T polymorphism exerted strong effects on efficacy of VPA (χ²=9.265, P=0.010). L48V polymorphism also showed effects on efficacy of LTG (χ²=17.397, P=0.001). CONCLUSIONS UGT2B7, UGT1A4 polymorphisms play crucial roles in metabolism of VPA and LTG.
背景 本研究旨在分析UGT2B7和UGT1A4基因多态性与癫痫患儿丙戊酸(VPA)和拉莫三嗪(LTG)代谢的关系。
材料与方法 我们对204例癫痫患儿给予VPA(102例)和LTG(102例)。在早晨给药前采集血样。采用高效液相色谱法(HPLC)测定血清LTG浓度。采用荧光偏振免疫分析法检测血清VPA浓度。PCR后通过直接自动DNA测序法检测UGT2B7 A268G、C802T和G211T基因多态性以及UGT1A4 L48V基因多态性。采用恩格尔方法进行疗效评估。
结果 VPA的校正血清浓度为每毫克/千克4.26微克/毫升,LTG为每毫克/千克1.56微克/毫升。多元线性回归分析显示,VPA或LTG的校正浓度与性别和年龄呈良好的线性关系。UGT2B7 A268G和C802T基因多态性被证明会影响VPA的血清浓度(F = 3.147,P = 0.047;F = 22.754,P = 0.000)。UGT1A4 L48V基因多态性与LTG的血清浓度无关(F = 5.328,P = 0.006)。在疗效分析中,我们发现C802T基因多态性对VPA的疗效有显著影响(χ² = 9.265,P = 0.010)。L48V基因多态性也对LTG的疗效有影响(χ² = 17.397,P = 0.001)。
结论 UGT2B7、UGT1A4基因多态性在VPA和LTG的代谢中起关键作用。