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- Title
Bioavailability Assessment of an Extract of Artemisia dracunculus L with Antidiabetic Activities In Vitro and In Vivo.
- Authors
Ribnicky, David M.; Poulev, Alexander; Kuhn, Peter E.; Logendra, Sithes; Zuberi, Aamir; Cefalu, William T.; Raskin, Ilya
- Abstract
Despite the widespread use of botanicals for treatment and prevention of disease, including Type 2 diabetes, there is a paucity of data regarding the plasma bioavailability of active compounds from plant extracts. An extract of Artemisia dracunculus was shown to decrease hyperglycemia and improve insulin sensitivity in animal models for type 2 diabetes. In vitro studies, employing bioactivity guided fractionation of the extract, resulted in the purification of 6 compounds that were suggested to be responsible for the activities observed in vivo. To evaluate the plasma appearance of active metabolites, C57BL/6J mice were gavaged with 500 mg extract per kg body weight, after 4 h of food restriction. Blood plasma samples (200 uL) were obtained at specified times (2, 4, 6, 8 and 2411) after ingestion. The samples were treated with β glucuronidase and sulfatase, which release chemically bound forms of flavonoids and related compounds for purposes of detection, and partitioned with hexane to selectively remove fatty acids and lipids that interfere with the analysis. A sensitive LC-MS/MS assay was developed to detect and quantitatively estimate the compounds in the plasma. The masses of the active compounds in the blood of treated mice (i.e. sakuranetin, MW 286) were detected by electrospray LC-MS but were not detectable by electron impact LC-MS. Abundance of the ions was then used to determine the time course for appearance of the components of the extract in the blood plasma. The maximal concentration for most of the compounds occurred at 4-6 h after treatment. In addition, measurements of the compounds in the blood was used to evaluate the effectiveness of Self Emulsifying Drug Delivery Systems (SEDDS) that are known to enhance the solubility and availability of poorly soluble drug compounds. The SEDDS did increase the concentrations of the active compounds in the blood relative to the control treatments. Conclusion: sensitive LC-MS methods can be used to assess the bioavailability of pharmacologically active components of botanical preparations.
- Subjects
TYPE 2 diabetes treatment; FRENCH tarragon; THERAPEUTIC use of plant extracts; HYPOGLYCEMIC agents; BIOAVAILABILITY
- Publication
Diabetes, 2007, Vol 56, pA559
- ISSN
0012-1797
- Publication type
Article