西洋參萃取物CVT-E002 對C57BL/6J 鼷鼠肝藥物代謝之影響

Effects of CVT-E002, a Proprietary Extract from the North American Ginseng (Panax quinquefolium) on Hepatic Drug-Metabolizing Enzymes in C57BL/6J Mice

CVT-E002 是一具專利之西洋參 （Panax quinquefolium ） 萃取物，具有調節免疫功能之作用。細胞色素 P450 （CYP）， UDP-葡萄糖醛酸轉移　（ UGT），及 glutathione 硫 -轉移　為重要之藥物代謝　，藥物代謝　之調控影響是產生藥物交互作用之重要因素。為評估 CVT-E002 因影響藥物代謝　而產生藥物交互作用之可能性，因而研究 CVT-E002 對鼷鼠 C57BL/6J 肝 CYP， UGT及 GST 之影響，結果顯示以 5 克 /公斤 /天 CVT-E002 連續處理鼠 3 天後，對鼠肝微粒體 CYP 及細胞色素b5 含量無影響，對 NADPH-CYP 還原　活性亦無影響。這處理不影響鼠肝微粒體 CYP氧化代謝 7-ethoxyresorufin ， 7-methoxyresorufin ， benzo（a）pyrene ， 7-ethoxycoumarin ， benzphetamine， N-nitrosodimethylamine， erythromycin 及 nifedipine 等的活性。 CVT-E002 對鼠肝微粒體 UGT 及細胞質液 GST 活性無影響。這些結果顯示 CVT-E002 在此處理劑量與時程，對鼠肝 CYP， UGT，及 GST 活性均無影響， CVT-E002 與其他藥物因影響藥物代謝，而發生交互作用之機會可能相對較低。CVT-E002, a proprietary extract from North American ginseng (Panax quinquefolium ) showed immunomodulating activity. Cytochrome P450 (CYP), UDP-glucuronosyl transferase (UGT), and glutathione S-transferase (GST) are important drug-metabolizing enzymes. Modulation of drugmetabolizing enzymes is a main cause of drug interactions. To assess the possible metabolism-based drug interaction of CVT-E002, effects of CVT-E002 on hepatic CYP, UGT, and GST were studied in C57BL/6J mice. Treatment of mice with 5g/kg/day CVT-E002 for three days had no effects on liver microsomal CYP and cytochrome b5 contents and NADPH-CYP reductase activity. CVT-E002 had no effect on microsomal CYP catalytic activities of the oxidations of 7-ethoxyresorufin, 7-methoxyresorufin, benzo(a)pyrene, 7-ethoxycoumarin, benzphetamine, N-nitrosodimethylamine, erythromycin, and nifedipine in mouse liver. Hepatic microsomal UGT and cytosolic GST activities were not affected by CVT-E002-treatment. These results suggested that CVT-E002 had no effects on hepatic CYP, UGT, and GST activities in mice under this treatment regimen. There might be low potential of incidence of metabolism-based drug interaction by CVT-E002.