Abstract
AbstractPeripheral CB1R blockers without crossing the blood–brain barrier (BBB) have demonstrated therapeutic benefits in metabolic syndromes, including obesity. Among them is Alisol G, a tetracyclic triterpene from Alismatis rhizoma (zexie), which can effectively reduce the weight of obese mice. Results from CP55940-induced [35S] GTPγS cannabinoid-type 1 receptor (CB1R) binding assay show an IC50 of 34.8 μmol/L for Alisol G, implicating its role as a CB1R antagonist. The purpose of our study is to assess whether Alisol G could serve as a peripheral CB1R antagonist for obesity treatment. In this study, we build a simple, reliable, and sensitive method to detect the concentration of Alisol G in rat tissue by ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). The results showed that Alisol G was mainly distributed in intestinal midgut, mucosa and small intestine, with little brain exposure. We suggested that intestine may be the main acting sites of Alisol G. Through comparison of brain and blood concentrations of Alisol G, our data showed that Alisol G cannot penetrate the BBB easily. In conclusion, Alisol G may represent a peripheral CB1R antagonist for the further treatment of obesity.
Highlights
Alismatis rhizoma is documented in the oldest materia medica book, “Shennong’s Classic of Materia Medica,” and has been used as a Chinese herbal medicine for hypolipemic, anti-inflammation, and antiatherosclerotic benefits for thousands of years
Alisol G has a significant effect on weight loss and hypoglycemic effects in obese mice induced by high-fat diet[1]; whether Alisol G serves as a peripheral cannabinoid-type 1 receptor (CB1R) antagonist to exert antiobesity effect remains largely unknown
Alisol G and I.S. were found to show a higher response in the positive-ion mode
Summary
Alismatis rhizoma (zexie) is documented in the oldest materia medica book, “Shennong’s Classic of Materia Medica,” and has been used as a Chinese herbal medicine for hypolipemic, anti-inflammation, and antiatherosclerotic benefits for thousands of years. Alisol G is a triterpenoid from Alismatis rhizoma. Our previous studies showed that Alisol G significantly inhibited body weight gain, while improved glucose and lipid metabolism of obese mice.[1] Evidence suggested that the blockade of the cannabinoid-type 1 receptor (CB1R) is one of the promising strategies for the treatment of. Alisol G has a significant effect on weight loss and hypoglycemic effects in obese mice induced by high-fat diet[1]; whether Alisol G serves as a peripheral CB1R antagonist to exert antiobesity effect remains largely unknown
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