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Vernonia amygdalina aqueous leaf extract modulates metformin pharmacokinetics, inhibits CYP3A4 and CYP2C9 enzymes in streptozotocin-induced diabetic rats.
- Source :
-
Journal of complementary & integrative medicine [J Complement Integr Med] 2024 Dec 24. Date of Electronic Publication: 2024 Dec 24. - Publication Year :
- 2024
- Publisher :
- Ahead of Print
-
Abstract
- Objectives: Vernonia amygdalina Del. leaves are used in traditional Southeast Asia and Africa medicinal practices. Metformin is used for diabetes management. This study investigated the effect of a single dose of aqueous leaf extract of V. amygdalina on metformin pharmacokinetics in diabetic rats.<br />Methods: Diabetic rats were randomly assigned to four groups, with six rats in each group. Group 1 was administered distilled water. Group 2 was administered V. amygdalina aqueous leaf extract alone. Group 3 was administered metformin alone. Group 4 was co-administered V. amygdalina extract plus metformin. Blood was collected at predetermined intervals, and plasma metformin levels were measured with liquid chromatography. The area under the curve (AUC <subscript>0-t</subscript> ), maximum plasma concentration (C <subscript>max</subscript> ), time to reach C <subscript>max</subscript> (T <subscript>max</subscript> ), half-life (t <subscript>1/2</subscript> ), and clearance (CL), were calculated based on noncompartment analysis. The effect of the extract on CYP2C9, CYP3A4, and UGT activities was determined using a Fluorometric Screening Kit.<br />Results: The combined treatment altered the pharmacokinetic parameters of metformin. The T <subscript>max</subscript> increased from 90±0.18 min to 180±0.13 min and the C <subscript>max,</subscript> increased from 0.91±0.32 μg/mL to 2.153±0.28 μg/mL. Additionally, the AUC <subscript>(0-t)</subscript> increased from 118.25±1.37 μg min mL <superscript>-1</superscript> to 301.006±1.96 μg min mL <superscript>-1</superscript> and the t <subscript>1/2</subscript> increased from 34.69±0.61 min to 101.321±0.55 min. However, the CL rate was decreased. The extract inhibited CYP3A4 and CYP2C9 enzyme activities.<br />Conclusions: The alteration of pharmacokinetic parameters by the extract suggests potential herb-drug interactions.<br /> (© 2024 the author(s), published by De Gruyter, Berlin/Boston.)
Details
- Language :
- English
- ISSN :
- 1553-3840
- Database :
- MEDLINE
- Journal :
- Journal of complementary & integrative medicine
- Publication Type :
- Academic Journal
- Accession number :
- 39710889
- Full Text :
- https://doi.org/10.1515/jcim-2024-0217