In vitro metabolism in Sprague-Dawley rat liver microsomes of forsythoside A in different compositions of Shuang-Huang-Lian |
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Authors: | Zhou Wei Di Liu-qing Shan Jin-jun Bi Xiao-lin Chen Le-tian Wang Ling-chong Cai Bao-chang |
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Affiliation: | aCollege of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, PR China |
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Abstract: | Shuang–Huang–Lian (SHL), a traditional Chinese formula containing Lonicerae japonicae flos (LJF), Scutellariae radix (SR) and Forsythiae fructus (FF), is commonly used to treat acute upper respiratory tract infection, acute bronchitis and light pneumonia. Forsythoside A is one of the main active ingredients in Forsythiae fructus, a key herb in SHL. In the present study, effects of different compositions in SHL on the in vitro metabolism in Sprague–Dawley rat liver microsomes of forsythoside A were investigated. The observations from Sprague–Dawley rat liver microsomes in the presence of β-NADPH or UDPGA that forsythoside A may be the substrates of CYP3A4, CYP2C9, CYP1A2, UGT1A6, UGT1A3, UGT1A1 and UGT1A9; Chlorogenic acid may be the substrates of CYP3A4, CYP2C9, CYP1A2, CYP2C19, UGT1A6, UGT1A3 and UGT1A1; Baicalin may be the substrates of CYP3A4, CYP2C19, CYP1A2, UGT1A9, UGT1A1 and UGT1A3; Baicalein may be the substrates of CYP3A4, CYP2E1 and UGT1A6. It was also found that the residue of forsythoside A in SHL, FF + LJF and FF + SR was greatly increased compared with that in FF in Sprague–Dawley rat liver microsomes in the presence of β-NADPH or UDPGA, which indicated that the metabolism of forsythoside A in SHL may be influenced by chlorogenic acid in LJF acting on the CYP3A4, CYP2C9, CYP1A2, UGT1A6, UGT1A3 and UGT1A1; baicalin in SR acting on the CYP3A4, CYP1A2, UGT1A9, UGT1A1 and UGT1A3; baicalein acting on the CYP3A4 and UGT1A6 respectively. |
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Keywords: | Abbreviations: SHL, Shuang&ndash Huang&ndash Lian, a traditional Chinese formula LJF, Lonicerae japonicae flos SR, Scutellariae radix FF, Forsythiae fructus FTA, Forsythoside A CHA, Chlorogenic acid BC, Baicalin BAI, Baicalein Cmax, The maximum plasma concentration RLM, Rat liver microsome AUC, The area under the concentration&ndash time curves Vmax, The maximum reaction rate Km, The kinetic constant CLintin vitro, In vitro internal clearance |
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