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A non-antibiotic erythromycin derivative improves muscle endurance by regulating endogenous anti-fatigue protein orosomucoid in mice.
Feng, Jiayi; Wan, Jingjing; Guo, Pengyue; Sun, Yang; Chen, Fei; Chen, Yi; Sun, Qingyan; Zhang, Weidong; Liu, Xia.
Afiliación
  • Feng J; School of Pharmacy, Second Military Medical University, Shanghai, China.
  • Wan J; School of Pharmacy, Second Military Medical University, Shanghai, China.
  • Guo P; School of Pharmacy, Second Military Medical University, Shanghai, China.
  • Sun Y; School of Pharmacy, Second Military Medical University, Shanghai, China.
  • Chen F; School of Pharmacy, Second Military Medical University, Shanghai, China.
  • Chen Y; School of Pharmacy, Second Military Medical University, Shanghai, China.
  • Sun Q; China Institute of Pharmaceutical Industry, Shanghai, China.
  • Zhang W; School of Pharmacy, Second Military Medical University, Shanghai, China.
  • Liu X; Key Lab of Chinese Medicine Resources Conservation, State Administration of Traditional Chinese Medicine of the People's Republic of China, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, China.
Clin Exp Pharmacol Physiol ; 51(7): e13873, 2024 Jul.
Article en En | MEDLINE | ID: mdl-38815994
ABSTRACT
At present, there are no official approved drugs for improving muscle endurance. Our previous research found acute phase protein orosomucoid (ORM) is an endogenous anti-fatigue protein, and macrolides antibiotics erythromycin can elevate ORM level to increase muscle bioenergetics and endurance parameters. Here, we further designed, synthesized and screened a new erythromycin derivative named HMS-01, which lost its antibacterial activity in vitro and in vivo. Data showed that HMS-01 could time- and dose-dependently prolong mice forced-swimming time and running time, and improve fatigue index in isolated soleus muscle. Moreover, HMS-01 treatment could increase the glycogen content, mitochondria number and function in liver and skeletal muscle, as well as ORM level in these tissues and sera. In Orm-deficient mice, the anti-fatigue and glycogen-elevation activity of HMS-01 disappeared. Therefore, HMS-01 might act as a promising small molecule drug targeting ORM to enhance muscle endurance.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Resistencia Física / Orosomucoide / Eritromicina / Músculo Esquelético / Fatiga Muscular / Glucógeno Límite: Animals Idioma: En Revista: Clin Exp Pharmacol Physiol Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Australia
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Resistencia Física / Orosomucoide / Eritromicina / Músculo Esquelético / Fatiga Muscular / Glucógeno Límite: Animals Idioma: En Revista: Clin Exp Pharmacol Physiol Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Australia