脱氨基基酸盐通过调节Akt/GSK3β和MuRF-1通路来减轻德克萨米他诱导的骨肌肉缩
Hengzhe Jin1, Hyoung Sig Seo2, Jinyoung Shin3
1Department of Physiology, School of Medicine, Konkuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul, 05029, South Korea.
European journal of pharmacology
|January 12, 2025
概括
来自Andrographis paniculata的脱水andrographolide酸盐 (DAS) 和andrographolide (AD) 显示出对肌肉缩的潜在作用. 在临床前模型中,DAS在改善肌肉功能和质量方面表现出卓越的疗效.
科学领域:
- 药理学 药理学 是一个学科.
- 肌肉生物学 肌肉生物学
- 自然产品 自然产品
背景情况:
- 安德罗格拉菲斯·帕尼库拉塔 (AGPA) 具有多样化的生物活动.
- AGPA的关键成分andrographolide (AD) 和 dehydroandrographolide succinate (DAS) 对骨肌肉缩的影响尚不清楚.
- 肌肉缩是一个重要的健康问题,治疗选择有限.
研究的目的:
- 调查AD和DAS在缓解骨肌肉缩方面的疗效.
- 阐明它们作用的潜在分子机制.
- 评估DAS作为肌肉缩的潜在治疗剂.
主要方法:
- 在体内使用德克萨米他 (DEX) 诱导的小鼠肌肉缩的研究.
- 在体外研究使用DEX处理的C2C12神经管.
- 评估肌肉力量,跑步表现,肌肉质量和肌管特征.
- 对Akt/GSK3β酸化和MuRF-1表达的分析.
主要成果:
- 在小鼠中,DAS和AD都改善了握力和肌肉质量.
- DAS显著提高了跑步速度和耐力,表现优于AD.
- 在体外,DAS和AD增加了ATP的产生和肌管直径.
- 这两种化合物都调节了Akt/GSK3β和MuRF-1通路.
结论:
- DAS和AD通过激活Akt/GSK3β通路并抑制MuRF-1,有效地减轻骨肌肉缩.
- DAS表现出比AD更大的抗缩作用.
- DAS是预防肌肉缩的有希望的治疗候选者.
相关概念视频
Skeletal Muscle Relaxants: Adverse Effects
333
Skeletal muscle relaxants are widely used for muscle paralysis and relieving pain following any muscle injury or stiffness. However, depending on the drug type, they can have adverse effects that range from mild to severe. Usually, nondepolarizing neuromuscular blockers have minimal side effects. For example, drugs like d-tubocurarine, cisatracurium, and rocuronium cause hypotension, whereas drugs like baclofen, when stopped abruptly, can lead to the recurrence of spastic conditions.
Unlike...
Unlike...
333
Myasthenia Gravis: Overview and Treatment
1.2K
Myasthenia gravis is a neuromuscular transmission disorder characterized by weakness and increased fatigability of skeletal muscles. It is an autoimmune disease affecting approximately one in 2000 people, where antibodies against the α1 subunit of nicotinic acetylcholine receptors are produced.
These antibodies interfere with the function of the nicotinic receptors in three ways: by binding to the receptor and disrupting acetylcholine binding; by causing cross-linking of receptors which...
These antibodies interfere with the function of the nicotinic receptors in three ways: by binding to the receptor and disrupting acetylcholine binding; by causing cross-linking of receptors which...
1.2K
Satellite Stem Cells and Muscular Dystrophy
1.9K
Satellite stem cells or myosatellite cells are quiescent stem cells that Alexander Mauro first identified in 1961. These cells are located between the sarcolemma, the plasma membrane of muscle fibers, and the basal lamina, the connective tissue sheath covering it. These mononucleated cells are activated in response to muscle injury, can transform into myoblasts, and may form or repair muscle fibers. Myosatellite cells can provide additional myonuclei for muscle regeneration or return to a...
1.9K
Directly Acting Muscle Relaxants: Dantrolene and Botulinum Toxin
653
Directly acting muscle relaxants like dantrolene and botulinum toxin (BoNT) have distinct mechanisms and applications. Dantrolene, a hydantoin derivative, acts on the ryanodine receptor (RYR1) in skeletal muscle cells. RYR1 are calcium channels present at the sarcoplasmic reticulum membrane. In response to excitation, they release calcium ions from the sarcoplasmic reticulum to the cytosol. Calcium promotes actin-myosin-mediated contraction of muscles.
The binding of dantrolene to the RYR1...
The binding of dantrolene to the RYR1...
653


