Nerolidol-beta-cyclodextrin inclusion complex enhances anti-inflammatory activity in arthritis model and improves gastric protection
| Autor: | Ricardo Neves Marreto, Adriano Antunes de Souza Araújo, Ricardo Luiz Cavalcanti de Albuquerque Júnior, Lucindo José Quintans Júnior, Luiz André Santos Silva, Bruno dos Santos Lima, Eloísa Portugal Barros Silva Soares de Souza, Marcelo Duarte Cavalcanti, Saravanan Shanmugan, Flavio Machado de Souza Carvalho, Marcelo Vinicius Lins Dantas Gomes, Cláudio Moreira de Lima |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Drug Male medicine.drug_class media_common.quotation_subject Indomethacin Anti-Inflammatory Agents Arthritis Inflammation Pharmacology 030226 pharmacology & pharmacy General Biochemistry Genetics and Molecular Biology Anti-inflammatory Cell Line 03 medical and health sciences chemistry.chemical_compound Mice 0302 clinical medicine medicine Animals Stomach Ulcer General Pharmacology Toxicology and Pharmaceutics Cytotoxicity Nerolidol media_common business.industry Plant Extracts Zymosan Stomach beta-Cyclodextrins General Medicine medicine.disease Anti-Ulcer Agents Arthritis Experimental 030104 developmental biology chemistry Gastric Mucosa Rheumatoid arthritis medicine.symptom business Sesquiterpenes |
| Zdroj: | Life sciences. 265 |
| ISSN: | 1879-0631 |
| Popis: | Rheumatoid arthritis is an autoimmune inflammatory disease with progressive degradation of cartilage and joints. Additionally, gastric ulcer affects many patients who make prolonged use of non-steroidal anti-inflammatory drugs widely used in the symptomatic treatment of rheumatoid arthritis. Nerolidol, a natural sesquiterpene, has several biological activities including anti-inflammatory and antiulcerogenic action. This study aims to develop and characterize a nerolidol s-cyclodextrin inclusion complex and to evaluate its activity in an experimental arthritis model. Inclusion complex was prepared by the lyophilization method and characterized by NMR, term analysis, XRD and SEM. Neutrophil migration assays and histopathological analysis were performed on zymosan-induced arthritis model using Swiss mice. And the gastroprotective effect was evaluated in two models of gastric ulcers: induced by ethanol and indomethacin. Inclusion complex showed no cytotoxicity and free nerolidol at a dose of 100 mg/kg (p.o.) in the arthritis model reduced neutrophil migration in 56% in relation to vehicle, and this inhibition was more expressive in the inclusion complex (67%) at the same dose. Histopathological analysis of the joint tissue confirmed the reduction of inflammatory signs. In the ethanol-induced gastric ulcer model, free nerolidol reduced the relative ulcer area more expressively (4.64%) than the inclusion complex (21.3%). However, in the indomethacin induction model, the inclusion complex showed better results in gastric protection compared to free nerolidol. The action of nerolidol complexed in beta-cyclodextrin in reducing arthritis inflammation combined with its gastroprotective action make it a potential new drug. |
| Databáze: | OpenAIRE |
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