Inasse Cherfi, Nasma Mahboub, Salah Eddine Laouini, Bachir Khezzani, Abderrhmane Bouafia, Youcef Ben Aissa, Abir Benaissa, Saravanan Muthupandhian, Farid Menaa
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引用次数: 0
Abstract
Introduction: This study investigates the protective effect of orally administered Artemisia campestris leaf extract against carbimazole (CMZ)-induced hypothyroidism in albino rats, aiming to evaluate its therapeutic potential as an alternative or adjunct treatment for hypothyroidism, a global endocrine disorder characterized by low free thyroxine (FT4) and high thyroid-stimulating hormone (TSH) levels.
Materials and methods: Aqueous A. campestris leaf extract was administered to albino rats with CMZ-induced hypothyroidism. Ultra-performance liquid chromatography (UPLC) identified key phytocompounds. Biochemical assays assessed in-vitro antioxidant and anti-inflammatory activities, and serum FT4 and TSH levels were measured in test (CMZ + extract) and control groups (untreated, CMZ, CMZ + Levothyroxine (LT4)). Histological studies examined thyroid tissue changes. Molecular Docking Simulation (MDS) and ADMET analysis evaluated phytocompound interactions with thyroid peroxidase (TPO) and their in-silico efficacy.
Results: A. campestris exhibited strong antioxidant and anti-inflammatory properties. Key phytocompounds (β-Sitosterol, Arteannuin B, 2,3-Butanediol) showed high binding affinity with TPO and favorable ADMET profiles, with 2,3-Butanediol indicating a novel role in thyroid hormone modulation. After 60 days, the test group showed marked recovery of thyroid function, with TSH reduced (approximately) 73% from 5.2 ± 0.6 ng/mL (CMZ group) to 1.4 ± 0.2 ng/mL and FT4 increased (approximately) 39% from 0.44 ± 0.05 ng/dL to 1.12 ± 0.08 ng/dL, comparable to the LT4 group.
Discussion: The study demonstrates that A. campestris phytocompounds effectively counteract CMZ-induced hypothyroidism, likely due to their antioxidant, anti-inflammatory, and thyroid hormone-modulating properties. The high TPO binding affinity and favorable ADMET profiles suggest potential for drug development, with 2,3-Butanediol as a novel therapeutic candidate.
Conclusion: A. campestris leaf extract offers significant therapeutic potential as an alternative or adjunct therapy for hypothyroidism, fully reversing CMZ-induced effects in rats, comparable to standard LT4 treatment, highlighting its promise for further exploration in endocrine disorder management.
期刊介绍:
Aims & Scope
Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry. The journal also publishes reviews on recent patents. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.