Comparison of the Metabolism of Baicalin in Rats Orally Administered with Radix scutellariae Extract and Shuang-Huang-Lian Extract

Abstract

Shuang-Huang-Lian (SHL) is a traditional Chinese formula containing Flos lonicerae, Radix scutellariae (RS) and Fructus forsythiae, and is commonly used for treating acute upper respiratory tract infection, acute bronchitis and light pneumonia. The aim of the present study is to compare the metabolites of baicalin in rats when orally administered with SHL and Radix scutellariae, and try to explore the principle of SHL compatibility. By using LC-MSⁿ and HPLC-DAD, the metabolites of baicalin were analyzed from bile, urine and feces of rats dosed with SHL and RS. Our results showed significant difference of baicalin metabolism between RS and SHL. However, baicalein was found to be the main metabolites of baicalin in intestinal tract after oral administration of RS and SHL, glucuronide, glucoside and methylated products were also found in rat urine after administration of either RS or SHL. Meanwhile, several sulphates were found in rat urine after RS administration, but not found after SHL. Among the metabolites of the SHL, potentially there existed a isomerized baicalin and methylated product: 5,7-dihydroxy-6-methoxyisoflavone-7-O-β-glucopyranuronoside, but without unidentified metabolite M3. Baicalein-6-O-β-glucopyranuronoside-7-O-β-glucopyranuronoside and baicalein-6-O-β-glucose-7-O-β-glucopyranuronoside were first reported by this study. The major metabolites of baicalin of RS and SHL in rat bile were the same, including baicalin-6-O-β-glucopyranuronoside-7-O-β-glucopyranuronoside, baicalin-6-β-glucopyranuronoside and 6-O-methyl-baicalin-7-O-β-glucopyranuronoside. Moreover, baicalein-6-O-β-glucose-7-O-β-glucopyranuronoside was also first found in rat bile by this study. Although baicalin-6-O-sulfate-7-O-β-glucopyranuronoside was found in rat bile after RS administration, no sulphated products were found after oral administration of SHL. These differences of baicalin metabolism between RS and SHL indicated that compatibility of medicines could result in the differences of metabolites.