Journal ArticleDOI
Analgesic and anti-inflammatory activities evaluation of (-)-O-acetyl, (-)-O-methyl, (-)-O-dimethylethylamine cubebin and their preparation from (-)-cubebin.
Gustavo H. B. Souza,AA Da Silva Filho,V. A. de Souza,A. C. Pereira,V. de A. Royo,Mla Silva,R. S. da Silva,Paulo Marcos Donate,José Carlos Tavares Carvalho,Jairo Kenupp Bastos +9 more
TLDR
The results showed that the acetylation and amination of cubebin were efficient in enhancing its analgesic activity, as well as its anti-inflammatory activity.Abstract:
The anti-inflammatory and antinociceptive effects of the acetylated (2), methylated (3) and aminated (4) derivatives of cubebin (1), obtained by its reaction with acetic anhydride, methyl iodide and dimethylethylamine chloride, respectively, were investigated, using different animal models. The compound (2) was the most effective anti-inflammatory one in the carrageenin-induced paw edema in rats and was the only one which showed dose-response correlation for this assay with r = 0.993 and Y = 64.58x + 0.22. Besides, compounds (2) and (4) were more effective than cubebin in inhibiting acetic acid-induced writhing in mice, producing dose-response correlation with doses of 10, 20 and 30 mg/kg, respectively. Regarding the hot plate and the cell migration tests in rats, none of the four tested compounds showed activity. Overall, the results showed that the acetylation and amination of cubebin were efficient in enhancing its analgesic activity, as well as its anti-inflammatory activity.read more
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Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.
Vanessa A. Souza,Rosangela da Silva,Ana C. Pereira,Vanessa de Andrade Royo,Juliana Saraiva,Marisa Montanheiro,Gustavo Henrique Bianco de Souza,Ademar A. da Silva Filho,Marcella D. Grando,Paulo Marcos Donate,Jairo Kenupp Bastos,Sérgio de Albuquerque,Márcio Luis Andrade e Silva +12 more
TL;DR: Five (-)-cubebin derivative compounds, (-)-O-acetyl cubebin (3), (-)-N,N-dimethylaminoethyl-cub Pastebin (5), (--hinokinin (6) and (-)-6,6'-dinitrohinokin in (7), previously synthesised by the research group, were evaluated on in vitro assay against free amastigote forms of Trypanosoma cruzi.
Journal ArticleDOI
In vitro and in vivo activity of lignan lactones derivatives against Trypanosoma cruzi
Juliana Saraiva,Celeste Vega,Mirian Rolon,Rosangela da Silva,Márcio Luis Andrade e Silva,Paulo Marcos Donate,Jairo Kenupp Bastos,Alicia Gómez-Barrio,Sérgio de Albuquerque +8 more
TL;DR: In vivo assays showed significant reduction of parasitaemia after administration of five in mice infected, and compounds 5, 6 and 2 showed higher trypanocidal activity against epimastigote forms of T. cruzi.
Journal ArticleDOI
In vitro antileishmanial and antimalarial activities of tetrahydrofuran lignans isolated from Nectandra megapotamica (Lauraceae).
Ademar A. da Silva Filho,Eveline S. Costa,Wilson Roberto Cunha,Márcio Luis Andrade e Silva,N. P. Dhammika Nanayakkara,Jairo Kenupp Bastos +5 more
TL;DR: In order to compare the effect on the parasites with toxicity to mammalian cells, the cytotoxic activity of the isolated compounds were evaluated against the Vero cells, showing that all evaluated tetrahydrofuran lignans exhibited no cytotoxicity at the maximum dose tested.
Journal ArticleDOI
Schistosomicidal and trypanocidal structure–activity relationships for (±)-licarin A and its (−)- and (+)-enantiomers
A. C. Pereira,Lizandra Guidi Magalhães,UO Gonçalves,Priscilla P. Luz,Ana C. G. Moraes,Vanderlei Rodrigues,P.M. da Matta Guedes,AA Da Silva Filho,Wilson Roberto Cunha,Jairo Kenupp Bastos,Npd Nanayakkara,Márcio Luis Andrade e Silva +11 more
TL;DR: Results suggest that (±)-licarin A and (-)-enantiomer A are promising compounds that could be used for the development of schistosomicidal and trypanocidal agents.
Journal ArticleDOI
Evaluation of analgesic and anti-inflammatory activities of Nectandra megapotamica (Lauraceae) in mice and rats.
Ademar A. da Silva Filho,Márcio Luis Andrade e Silva,José Carlos Tavares Carvalho,Jairo Kenupp Bastos +3 more
TL;DR: It was suggested that the analgesic effects obtained for EBCA could be due mainly to the presence of its major compound, α‐asarone (1), which showed activity in the abdominal constriction test and the anti‐inflammatory assay.
References
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Carrageenin-Induced Edema in Hind Paw of the Rat as an Assay for Antiinflammatory Drugs
TL;DR: The potency ratios obtained for aspirin, phenylbutazone and hydrocortisone are fairly close to the ratios of their respective daily doses in the treatment of rheumatic disease.
Book
The practice of medicinal chemistry
TL;DR: Section 1 - General Aspects of Medicinal Chemistry Section 2 - Lead Compound Discovery Strategies Section 3 - Primary Exploration of Structure-Activity Relationships Section 4 - Substituents and Functions: Qualitative and Quantitative aspects of structure- activity Relationships.
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The evaluation of the analgesic action of pethidine hydrochloride (demerol)
G. Woolfe,A. D. Macdonald +1 more
TL;DR: A new method for the evaluation of analgesics has been described and pethidine hydrochloride has been found to possess one fifth to one sixth of the analgesic activity of morphine hydrochlorides against mild pain stimuli, but to be ineffective against severe pain.
Journal ArticleDOI
Macrocortin: a polypeptide causing the anti-phospholipase effect of glucocorticoids
TL;DR: It is reported that Macrocortin derived from rat peritoneal leukocytes is an intracellular polypeptide whose release and synthesis are stimulated by steroids.