Unveiling the Healing Power of Artemisia campestris: A Breakthrough in Hypothyroidism Treatment Through In Vitro, In Vivo, and In Silico Insights.

IF 3.2 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
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.

揭示青蒿的治疗能力:通过体外,体内和计算机洞察治疗甲状腺功能减退症的突破。
摘要:本研究研究了口服青蒿叶提取物对卡马唑(carbimazole, CMZ)诱导的白化大鼠甲状腺功能减退的保护作用,旨在评估其作为替代或辅助治疗甲减的治疗潜力。甲减是一种以游离甲状腺素(FT4)低和促甲状腺激素(TSH)水平高为特征的全球性内分泌疾病。材料与方法:将野樟叶水提液给予cmz诱导的白化大鼠甲状腺功能减退。超高效液相色谱法(UPLC)鉴定了关键的植物化合物。生化试验评估了体外抗氧化和抗炎活性,并测定了试验组(CMZ +提取物)和对照组(未处理组,CMZ, CMZ +左旋甲状腺素(LT4))血清FT4和TSH水平。组织学检查甲状腺组织的变化。分子对接模拟(MDS)和ADMET分析评估了植物化合物与甲状腺过氧化物酶(TPO)的相互作用及其在硅中的功效。结果:野樟具有较强的抗氧化和抗炎作用。关键的植物化合物(β-谷甾醇、青蒿素B、2,3-丁二醇)与TPO具有较高的结合亲和力和良好的ADMET谱,其中2,3-丁二醇在甲状腺激素调节中具有新的作用。60天后,试验组甲状腺功能明显恢复,TSH从5.2±0.6 ng/mL (CMZ组)降低(约)73%至1.4±0.2 ng/mL, FT4从0.44±0.05 ng/dL增加(约)39%至1.12±0.08 ng/dL,与LT4组相当。讨论:研究表明,campestris植物化合物有效地对抗cmz诱导的甲状腺功能减退,可能是由于它们的抗氧化、抗炎和甲状腺激素调节特性。高TPO结合亲和力和良好的ADMET谱表明,2,3-丁二醇具有开发药物的潜力,是一种新的治疗候选药物。结论:野樟叶提取物作为甲状腺功能减退症的替代或辅助治疗具有显著的治疗潜力,可完全逆转cmz诱导的大鼠甲状腺功能减退,与标准LT4治疗相当,在内分泌失调治疗方面有进一步探索的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Current medicinal chemistry
Current medicinal chemistry 医学-生化与分子生物学
CiteScore
8.60
自引率
2.40%
发文量
468
审稿时长
3 months
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.
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