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1.
Drug Res (Stuttg) ; 73(9): 506-512, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37935202

RESUMO

Osteoarthritis is a common chronic degenerative disease, of which the essence is the degenerative changes of bone and joint cartilage, involving damage in multiple structures such as bone, synovium and joints. In the mechanism of arthritis inflammation is closely related, and therefore the exploration to inhibit inflammatory mediators is crucial for the clinical prevention and treatment of osteoarthritis. Inotodiol is a lanostane triterpenoid isolated from Inonotus obliquus, which had been extensively reported to be an anti-inflammatory agent, but its effect on arthritis remains unknown. In this study, we firstly demonstrated that inotodiol significantly reduced IL-1ß-induced chondrocyte injury and inhibited the release of inflammatory factors. At the same time, experiments in vivo showed that inotodiol could effectively improve the symptoms of joint injury in mice and reduce the area of cartilage destruction, indicating that inotodiol may be a potential therapeutic drug for osteoarthritis.


Assuntos
Lanosterol , Osteoartrite , Camundongos , Animais , Lanosterol/farmacologia , Lanosterol/uso terapêutico , Osteoartrite/tratamento farmacológico , Inflamação/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico
2.
J Org Chem ; 87(15): 10173-10184, 2022 08 05.
Artigo em Inglês | MEDLINE | ID: mdl-35877650

RESUMO

An efficient palladium-catalyzed oxidative nonclassical Heck reaction of arylhydrazines with allylic alcohols via C-N bond cleavage has been successfully developed. This method provides a series of ß-arylated carbonyl compounds with broad functional group tolerance under base-free, simple, and mild open air reaction conditions. In the reaction, arylhydrazines with the smaller molecular weight of the leaving group were employed as the "green" arylation reagent, which released N2 and water as the byproducts under air. Mechanistic studies suggested that an aryl radical process and Pd-H complex migration reinsertion were involved. Moreover, the synthesis of the antiarrhythmic drug propafenone was completed with this transformation as the key step.


Assuntos
Estresse Oxidativo , Paládio , Catálise , Estrutura Molecular , Oxirredução , Paládio/química
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