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Bioorg Chem ; 103: 104227, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32891004

RESUMO

Rheumatoid Arthritis is a chronic, inflammatory, and systemic autoimmune disease, it affects elders worldwide. Herbal medicines have been used for the treatment of various ailments from ancient times. Betelvine (Piper betle L.) leaves have long been used in Asian countries as a medicine to relieve pain and some metabolic diseases. The present study of methanolic extract of phytochemical analysis confirms the presence of alkaloids, tannins, terpenoids, saponins, steroids, total flavonoids and total phenols. GC-MS analysis of MeOH extract of Piper betle (PBME) revealed the presence of 40 bioactive compounds. In vitro antioxidant and anti-inflammatory assays showed greater inhibitory effect. The anti-arthritic effects of PBME at 250 and 500 mg/kg concentration showed recovery from joint damage in in vivo rat model. Among the 40 GC-MS derived bioactives, 4-Allyl-1,2-Diacetoxybenzene exhibited the higher interactions with minimized binding energy to the RA targets of MMP 1 (-6.4 kcal/mol), TGF-ß (-6.9 kcal/mol), IL-1ß (-5.9 kcal/mol). Further, the effect of PBME extract against RA molecular disease targets (IL-1ß, MMP1 and TGF- ß) were studied using Real-time PCR. These results substantiate that P. betle leaves could be a source of therapeutics for the treatment of rheumatoid arthritis.


Assuntos
Antirreumáticos/uso terapêutico , Artrite Experimental/tratamento farmacológico , Piper betle/química , Extratos Vegetais/uso terapêutico , Animais , Antirreumáticos/isolamento & purificação , Antirreumáticos/farmacocinética , Artrite Experimental/induzido quimicamente , Artrite Experimental/patologia , Feminino , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacocinética , Sequestradores de Radicais Livres/uso terapêutico , Adjuvante de Freund , Articulações/patologia , Simulação de Acoplamento Molecular , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacocinética , Folhas de Planta/química , Ratos Wistar
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