Abstract
Schisantherin A is an active ingredient originating from Schisandra chinensis (Turcz.) which has hepatoprotective and anti-oxidation activities. In this study, in vitro metabolisms investigated on rat liver microsomes (RLMs) and in vivo metabolisms explored on male Sprague Dawley rats of Schisantherin A were tested, respectively. The metabolites of Schisantherin A were identified using ultra-high-performance liquid chromatography coupled with hybrid triple quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS). Based on the method, 60 metabolites were successfully identified and structurally characterized including 48 phase-I and 12 phase-II metabolites. Among the metabolites, 45 metabolites were reported for the first time. Moreover, 56 and eight metabolites were detected in urine and bile and 19 metabolites were identified in rats’ plasma. It demonstrated that hepatic and extra-hepatic metabolic pathways were both involved in Schisantherin A biotransformation in rats. Five in vitro metabolites were structurally characterized for the first time. The results indicated that the metabolic pathways mainly include oxidation, reduction, methylation, and conjugation with glucuronide, taurine, glucose, and glutathione groups. This study provides a practical strategy for rapidly screening and identifying metabolites, and the results provide basic data for future pharmacological and toxicology studies of Schisantherin A and other lignin ingredients.
Highlights
The traditional Chinese medicine Schisandra chinensis, and its dried mature fruits (Turcz.) Baill or Schisandra sphenanthera Rehd et Wils, belong to a type of herbal ingredient, and has been used for thousands of years [1,2]
In vitro and in vivo metabolic profiles were investigated by UPLC-Q-TOF-MS/MS
Five in vitro metabolisms were concentrated in phase-I, it was suggested that the metabolism pathway in vivo is more complicated than that of in vitro
Summary
The traditional Chinese medicine Schisandra chinensis (commonly named as WuWeiZi in Chinese), and its dried mature fruits (Turcz.) Baill or Schisandra sphenanthera Rehd et Wils, belong to a type of herbal ingredient, and has been used for thousands of years [1,2]. Modern pharmacological and clinical studies have shown that Schisandra chinensis possesses hepatoprotective effects, anti-oxidant, anti-tumor, anti-human immunodeficiency virus (HIV), antiviral activity, and antagonistic activity towards platelet-activating factors [7,8,9,10,11]. Schisantherin A (the structure is shown in Figure 1) is a lignans compound of the highest concentration in Schisandra chinensis [12,13,14], and has the effects of protecting the liver, anti-oxidant, anti-tumor, etc. The metabolism of Schisantherin A has been reported, it has only detected a few metabolites [21,22]. Metabolite identification is a part of drug discovery and development, and metabolism in vivo plays an important role in explaining and predicting efficacy and toxicity [23]
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