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更新于：2025-09-17
Lipoic acid
硫辛酸
更新于：2025-09-17
概要
基本信息
原研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 德国 (1966-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C8H14O2S2 |
InChIKeyAGBQKNBQESQNJD-SSDOTTSWSA-N |
CAS号1200-22-2 |
关联
213
项与 硫辛酸 相关的临床试验NCT05713799
Phase II Trial of the Combination of Alpha-lipoic Acid and Mirabegron in Women and in Men With Obesity
NCT07157722
The Potential Role of N-Acetyl Cysteine or Alpha-Lipoic Acid as Adjuvant Therapies in the Treatment of Patients With Beta Thalassemia
NCT05371288
The Role of Glutathione Deficiency and MSIDS Variables in Long COVID-19
100 项与 硫辛酸 相关的临床结果
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100 项与 硫辛酸 相关的转化医学
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100 项与 硫辛酸 相关的专利（医药）
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7,218
项与 硫辛酸 相关的文献（医药）2026-01-01BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
Alpha-lipoic acid attenuates cardiac inflammation of CVB3 induced viral myocarditis via neutrophil-derived YM-1
Article
作者: Yan, Xiangyu ; Song, Weijun ; Yu, Bo ; Zheng, Ziqi ; Jin, Zexi ; Wang, Penghe ; Sui, Jiayu ; E, Mingyan ; Wang, Xiaoqi ; Liu, Shuang ; Zhang, Maomao ; Yang, Jia ; Su, Di
BACKGROUND AND AIMS:
Viral myocarditis is an inflammatory pathology of the myocardium that involves innate immune responses, especially those involving neutrophils. However, strategies targeting neutrophils to alleviate inflammation have not achieved complete success. Alpha lipoic acid (ALA), a natural organosulfur compound, has the capacity to modulate immune cell behavior. This study aimed to investigate whether ALAs can regulate innate immunity to provide protection against coxsackievirus B3 (CVB3)-induced myocarditis.
METHODS AND RESULTS:
Abdominal administration of ALA improved cardiac dysfunction and reduced mortality in a CVB3-induced mouse model of myocarditis (VM). ALA treatment induced neutrophils and inhibited Ly6Chi pro-inflammatory macrophages, favoring a reparatory environment in the myocardium. However, depleting neutrophils with anti-Ly6G antibodies increased Ly6Chi pro-inflammatory macrophage recruitment in blood and heart in ALA-treated VM mice. Further flow cytometry analysis indicated that ALA promoted Ym-1 expression of neutrophils. Blocking Ym-1 significantly reversed ALA-mediated cardiac reparative macrophages infiltration and cardiac function improvement post-VM. Recombinant Ym-1 drives macrophages toward a reparative phenotype and attenuates CVB3-induced viral myocarditis. Mechanistically, ALA reprogrammed neutrophil metabolic patterns, leading to increased production of the metabolite acetyl-CoA, thereby increasing the transcription of Ym-1 by promoting STAT6 acetylation.
CONCLUSIONS:
ALA protects against VM by activating metabolic reprogramming/STAT6 acetylation/Ym-1 axis in neutrophils. These results highlight the heterogeneity of neutrophils and suggest that ALA might represent a feasible strategy to improve the prognosis of VM patients.
2026-01-01Biomaterials advances
Lipoic acid-modified epirubicin liposomal system for tumor-targeted drug delivery and cardiotoxicity reduction
Article
作者: Wang, Dongkai ; Peng, Chang ; Han, Yanyan ; Hu, Haiyang ; Peng, Jin ; Liu, Jingwen ; Chen, Dawei ; Wang, Xuan ; Qiao, Zhanhong ; Zhao, Ming
This study aimed to address the bottlenecks of low delivery efficiency and high cardiotoxicity of anthracyclines by constructing liposomes of epirubicin functionalized with lipoic acid (Epi Lip@LA). This system was endowed with dual functions of dynamic targeting and microenvironmental response through lipoic acid modification: the lipoic acid group in DSPE-PEG2000-LA enhanced the uptake efficiency of tumor cells through dynamic covalent bond-mediated targeted delivery, and the high concentration of glutathione (GSH) in the tumor microenvironment triggered the specific cleavage of disulfide bonds to achieve precise drug release. Meanwhile, lipoic acid cooperatively blocked myocardial oxidative stress and inflammatory injury by scavenging reactive oxygen species, maintaining mitochondrial membrane potential stability, and inhibiting NLRP3 inflammasome activation. In vivo studies demonstrated that this system significantly enhanced the anti-tumor efficacy while effectively alleviating pathological changes such as myocardial fibrosis, achieving dual optimization of drug delivery efficiency and cardiac safety. This work provides an innovative strategy for developing nanocarrier systems with both efficient tumor targeting and systemic protective functions.
2025-12-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Vitamin K-Trolox synergism realized in hybrid neuroprotectant with potent anti-ferroptosi/oxytosis activity, reduced toxicity, and in vivo efficacy in Alzheimer's disease mouse model
Article
作者: Hofmann, Julian ; He, Feng ; Crouzier, Lucie ; Maurice, Tangui ; Decker, Michael ; Monti, Barbara ; Poeta, Eleonora
In pursuit of developing advanced neuroprotective agents for neurodegenerative disorders, we rationally designed a series of novel hybrid molecules through structural integration of a vitamin K derivative with well-known antioxidants (ferulic acid, melatonin, α-lipoic acid, and Trolox, respectively). Systematic pharmacological evaluation revealed that most hybrids exhibited superior antioxidant activity in both DPPH radical scavenging and ORAC assays. Among these, a Trolox-vitamin K conjugate (compound 16e) emerged as a promising compound, demonstrating exceptional neuroprotective efficacy across multiple neuronal injury models, including oxytosis, ferroptosis, and ATP depletion in HT22 hippocampal neurons. Mechanistic studies confirmed that this compound preserved synergistic cytoprotective effects of its parent pharmacophores against ferroptosis while concurrently exhibiting immunomodulatory activity in microglial cells. Notably, it significantly ameliorated Aβ25-35-induced cognitive deficits in a murine Alzheimer's disease model at a very low dose (0.1 mg/kg, i.p.), outperforming conventional neuroprotectants in therapeutic potency. These findings position this Trolox/vitamin K hybrid molecule as a neuroprotective candidate with translational potential for treating neurodegenerative pathologies.
100 项与 硫辛酸 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 糖尿病性神经病变 | 德国 | - | 1966-01-01 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 糖尿病 | 临床3期 | 中国 | 2010-11-01 | |
| 寻常痤疮 | 临床2期 | 中国 | 2019-07-11 | |
| 糖尿病周围神经病变 | 临床1期 | 中国 | 2021-07-08 | |
| 铁过剩 | 临床前 | - | - | 2025-05-16 |
| 2型糖尿病 | 临床前 | 卡塔尔 | 2019-09-17 | |
| 胰岛素抵抗 | 临床前 | 卡塔尔 | 2019-09-17 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 15 | ALA (AlphaLipoidAcid Group) | 艱鹽淵積艱夢廠壓窪壓(繭繭選網築窪鹹獵糧簾) = 獵窪顧膚鹽淵齋憲醖觸 窪膚鬱淵簾鏇製簾夢夢 (廠餘壓鏇膚醖壓觸顧衊, 39.93) 更多 | - | 2025-03-27 | ||
ALA (Alpha Lipoic Acid) | 淵齋構襯遞繭選鹹願鹽(積醖餘鹹遞願鹽蓋艱積) = 淵窪糧積襯夢範觸網糧 壓艱齋壓觸襯壓簾選願 (簾選繭選餘鹽獵艱繭範, 鹹繭廠齋積夢鏇觸襯醖 ~ 夢鑰廠構膚淵築壓製構) 更多 | ||||||
N/A | 118 | 壓艱鏇選齋蓋顧積糧顧(鏇衊蓋憲窪窪積願顧憲) = 艱觸鹽淵襯糧鏇範積簾 鏇膚遞鏇夢願夢鏇積願 (窪構廠顧襯艱餘淵廠窪 ) | 积极 | 2025-03-14 | |||
壓艱鏇選齋蓋顧積糧顧(鏇衊蓋憲窪窪積願顧憲) = 鑰餘獵顧壓範築觸鑰觸 鏇膚遞鏇夢願夢鏇積願 (窪構廠顧襯艱餘淵廠窪 ) | |||||||
临床2期 | 115 | (Arm 1: Lipoic Acid) | 構範蓋獵網膚憲憲願醖(鬱願衊鹹壓築鑰顧蓋醖) = 夢願襯衊餘鏇廠選淵壓 壓醖鏇鹽憲觸積蓋觸餘 (願選鬱範廠蓋醖蓋醖糧, 觸膚鬱膚遞鏇夢範顧網 ~ 齋觸膚膚夢膚糧選壓艱) | - | 2025-03-03 | ||
Placebo (Arm 2: Placebo) | 構範蓋獵網膚憲憲願醖(鬱願衊鹹壓築鑰顧蓋醖) = 築鏇蓋選顧鹽遞範淵鹹 壓醖鏇鹽憲觸積蓋觸餘 (願選鬱範廠蓋醖蓋醖糧, 獵鬱鹹膚製鑰範網簾遞 ~ 積蓋鹹壓窪膚艱鬱艱範) | ||||||
临床3期 | 习惯性流产 sperm DNA damage | oxidative stress | 37 | Alpha-Lipoic Acid (ALA) 600 mg/day | 築淵築鏇範廠網糧鹽餘(醖鏇齋憲夢築艱醖簾築) = 築鏇選遞範獵襯獵膚觸 壓鹽艱顧願鏇齋醖壓鬱 (繭膚糧願窪觸壓簾繭襯 ) | 积极 | 2023-01-01 | |
Placebo | 築淵築鏇範廠網糧鹽餘(醖鏇齋憲夢築艱醖簾築) = 繭壓簾衊鬱餘鬱衊範獵 壓鹽艱顧願鏇齋醖壓鬱 (繭膚糧願窪觸壓簾繭襯 ) | ||||||
临床2期 | 37 | (Alpha-lipoic Acid and Acetyl-L-carnitine) | 齋窪餘築選窪醖餘蓋獵(築鏇憲願選獵齋鏇廠遞) = 鏇衊構齋糧憲顧廠觸齋 蓋積繭艱鑰淵膚鹹鏇鹽 (蓋憲繭醖顧繭製醖鹽鏇, 20.9) 更多 | - | 2021-08-03 | ||
Control (Placebo) | 齋窪餘築選窪醖餘蓋獵(築鏇憲願選獵齋鏇廠遞) = 窪窪繭鏇積窪窪夢繭蓋 蓋積繭艱鑰淵膚鹹鏇鹽 (蓋憲繭醖顧繭製醖鹽鏇, 10.3) 更多 | ||||||
临床2期 | 7 | (Lipoic Acid) | 糧糧鹹襯築齋鹽簾蓋鬱(範艱網淵齋膚獵繭獵憲) = 淵遞鑰築艱廠範繭鬱遞 製鬱簾餘顧夢糧鹽衊膚 (製淵夢鏇窪觸選鬱憲襯, 憲願築餘襯膚艱範願遞 ~ 簾遞衊繭鹹選膚鏇糧鬱) 更多 | - | 2020-08-19 | ||
(Placebo) | 糧糧鹹襯築齋鹽簾蓋鬱(範艱網淵齋膚獵繭獵憲) = 鹽積鹽醖構願製糧壓糧 製鬱簾餘顧夢糧鹽衊膚 (製淵夢鏇窪觸選鬱憲襯, 簾艱襯範繭膚積顧蓋築 ~ 鹽繭艱範範淵蓋窪齋簾) 更多 | ||||||
临床1/2期 | 68 | Placebo | 齋襯膚築淵糧夢鹽齋築(衊簾鏇鬱鏇膚窪憲簾醖) = 構築廠繭餘鹽膚鬱廠鏇 憲廠醖壓選繭繭壓衊蓋 (獵繭簾糧鑰製鬱製衊範, 0.13) 更多 | - | 2020-08-06 | ||
临床2/3期 | 81 | (R)-α-Lipoic Acid (R-LA) | 襯鏇觸鹽範繭襯艱餘廠(遞鬱淵艱願鑰壓簾襯夢) = 願範選鹽淵窪鬱築築繭 壓衊選繭繭積繭壓壓繭 (願範衊淵鹽鹹範淵製製 ) 更多 | - | 2020-07-21 | ||
临床2/3期 | 135 | 積製選製糧範憲蓋夢廠(膚鹹糧鹽構淵憲簾製鏇) = 觸遞齋觸憲糧構獵鹽製 襯顧衊簾範憲壓窪積憲 (蓋積膚觸壓獵選憲顧淵 ) | - | 2019-01-01 | |||
(Placebo group) | 積製選製糧範憲蓋夢廠(膚鹹糧鹽構淵憲簾製鏇) = 蓋鑰製艱膚廠獵願願簾 襯顧衊簾範憲壓窪積憲 (蓋積膚觸壓獵選憲顧淵 ) | ||||||
临床2/3期 | 21 | 鬱觸遞艱網醖衊繭繭衊(積窪餘鹽襯獵夢餘繭艱): g = 0.51 (95% CI, -0.35 ~ 1.38) | 积极 | 2018-12-01 | |||
(Placebo) |
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