Work

Vernonia amygdalina aqueous leaf extract modulates metformin pharmacokinetics, inhibits CYP3A4 and CYP2C9 enzymes in streptozotocin-induced diabetic rats

Year: 2024

Type: article

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. 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 0-t ), maximum plasma concentration (C max ), time to reach C max (T max ), half-life (t 1/2 ), 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. Results The combined treatment altered the pharmacokinetic parameters of metformin. The T max increased from 90±0.18 min to 180±0.13 min and the C max, increased from 0.91±0.32 μg/mL to 2.153±0.28 μg/mL. Additionally, the AUC (0-t) increased from 118.25±1.37 μg min mL −1 to 301.006±1.96 μg min mL −1 and the t 1/2 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. Conclusions The alteration of pharmacokinetic parameters by the extract suggests potential herb-drug interactions.

Source: Journal of Complementary and Integrative Medicine

DOI: 10.1515/jcim-2024-0217

Authors: Gabriel Akyirem Akowuah, Bassel Al Sabbagh, Vijayaraj Kumar Palanirajan, Yik-ling Chew, Jin Han Chin, Mariam Ahmad

Institutions: Monash University Malaysia, UCSI University, Mahsa University, Universiti Sains Malaysia

Language: English

Topic: Pharmacogenetics and Drug Metabolism

Subfield: Pharmacology

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $2,489