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1.
Nat Prod Res ; 32(4): 468-472, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28385073

RESUMO

The present investigation aimed to evaluate the activity of the essential oil of Mentha arvensis L. on exogenously induced bronchoconstriction in experimental animals. The anti-asthmatic effect of M. arvensis essential oil (MAEO) was studied using histamine aerosol-induced bronchoconstriction in guinea pigs and ovalbumin (OVA) sensitised albino mice. Treatment with M. arvensis oil significantly (p < 0.001) increased the time of preconvulsive dyspnoea in histamine-induced guinea pigs. Oral treatment of MAEO significantly (p < 0.001) decreased absolute eosinophil count, serum level of IgE and the number of eosinophils, neutrophils in BALF. Histopathological examination of lungs showed that essential oil rescinded bronchial asthma. The present investigation provides evidence that MAEO relaxes bronchial smooth muscles and suppressed immunological response to OVA.


Assuntos
Asma/tratamento farmacológico , Broncoconstrição/efeitos dos fármacos , Mentha/química , Óleos Voláteis/farmacologia , Animais , Asma/induzido quimicamente , Asma/patologia , Modelos Animais de Doenças , Dispneia/tratamento farmacológico , Eosinófilos/efeitos dos fármacos , Feminino , Cobaias , Histamina/efeitos adversos , Imunoglobulina E/sangue , Pulmão/efeitos dos fármacos , Pulmão/patologia , Camundongos , Neutrófilos/efeitos dos fármacos , Ovalbumina/efeitos adversos , Ovalbumina/imunologia
2.
Indian J Pharmacol ; 49(1): 55-59, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28458423

RESUMO

OBJECTIVE: Angelica glauca Edgew (Apiaceae) is used in traditional medicine for treatment of several diseases including bronchial asthma. The present investigation was aimed to evaluate broncho-relaxant activity of A. glauca essential oil in histamine and ovalbumin (OVA)-induced broncho constriction in experimental animals. MATERIALS AND METHODS: Airway was induced using histamine aerosol in guinea pigs (n = 24) and OVA aerosol in albino mice (n = 24). The number of inflammatory cells, namely, absolute eosinophils count in blood, total immunoglobulin E (IgE) in serum, eosinophils, and neutrophils in bronchoalveolar lavage fluid (BALF) and histopathological examination of lung tissues were investigated in A. glauca oil and dexamethasone-treated groups. A. glauca oil 200 µL/kg was given orally, and dexamethasone 2 mg/kg was given intraperitoneal. Both the treatments were repeated daily for 7 days. Results were analyzed by one-way ANOVA, and P ≤ 0.05 was considered statistically significant. RESULTS: Treatment with A. glauca essential oil significantly (P < 0.001) increased the time of preconvulsive dyspnea in histamine-induced guinea pigs. Oral treatment of A. glauca oil significantly (P < 0.001) decreased absolute blood eosinophil count (from 325 ± 3.69 to 200 ± 3.05 cells/mm3), serum level of IgE (from 6.10 ± 0.05 to 0.70 ± 0.08 IU/L), and the number of eosinophils (from 11.0% ±1.41% to 3.0% ±0.51%), neutrophils (from 13.0% ±1.12% to 5.0% ±1.39%) in BALF. Histopathological changes observed in lungs of untreated group were marked suppressed by treatment with A. glauca oil. CONCLUSION: The essential oil of A. glauca has bronchorelaxation in both histamine and OVA-induced bronchoconstriction in animals. The traditional use of A. glauca against asthma could be attributed to its bronchodilator property as observed in the present study.


Assuntos
Angelica/química , Broncoconstrição/efeitos dos fármacos , Broncodilatadores/farmacologia , Óleos Voláteis/farmacologia , Administração Oral , Animais , Asma/tratamento farmacológico , Asma/imunologia , Líquido da Lavagem Broncoalveolar , Broncoconstrição/imunologia , Broncodilatadores/administração & dosagem , Broncodilatadores/isolamento & purificação , Dexametasona/farmacologia , Modelos Animais de Doenças , Eosinófilos/efeitos dos fármacos , Eosinófilos/metabolismo , Feminino , Cobaias , Histamina/imunologia , Imunoglobulina E/sangue , Camundongos , Neutrófilos/efeitos dos fármacos , Neutrófilos/metabolismo , Óleos Voláteis/administração & dosagem , Óleos Voláteis/isolamento & purificação , Ovalbumina/imunologia
3.
Eur J Med Chem ; 69: 316-22, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24056147

RESUMO

The present article describes the synthesis of dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-one (2a-h) under microwave irradiation. The product was obtained in excellent yield (74-94%) in a shorter reaction time (2 min). These molecules (2a, b) further reacted with various substituted 4-bromomethylcoumarins (3a-f) to yield a new series of coumarin substituted dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-ones (4a-h). The structure of all the synthesized compounds were confirmed by spectral studies and screened for their in vitro antibacterial activity against three Gram-positive bacteria viz., Staphylococcus aureus, Enterococcus faecalis, Streptococcus mutans and three Gram-negative bacteria viz., Escherichia coli, Klebsiella pneumonia, Pseudomonas aeruginosa and antifungal activity against Candida albicans, Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus, Fusarium oxysporum, Penicillium chrysogenum and anticancer activity against Dalton's Ascitic Lymphoma (DAL) cell line. In general, all the compounds possessed better antifungal properties than antibacterial properties. The coumarin substituted dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-one (4g) (R = i-Pr, R1 = 6-Cl) was found to be the most potent cytotoxic compound (88%) against Dalton's Ascitic Lymphoma cell line at the concentration of 100 µg/mL.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos/farmacologia , Bactérias/efeitos dos fármacos , Benzimidazóis/farmacologia , Cumarínicos/química , Fungos/efeitos dos fármacos , Micro-Ondas , Pirimidinonas/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Benzimidazóis/síntese química , Benzimidazóis/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Testes de Sensibilidade Microbiana , Modelos Moleculares , Estrutura Molecular , Pirimidinonas/síntese química , Pirimidinonas/química
4.
Eur J Med Chem ; 45(3): 1151-7, 2010 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-20047777

RESUMO

A series of new and novel coumarin-6-sulfonamides with a free C4-azidomethyl group have been synthesized as antimicrobials in three steps starting from 7-methyl-4-bromomethylcoumarin 1. The reaction of 1 with chlorosulfonic acid was found to yield the corresponding 6-sulfonylchloride 2, which when treated with sodium azide led to intermediate 3. The title sulfonamides 5a-y were obtained from the reaction of 3 with various aromatic amines 4 in refluxing benzene. The chemical structures of the compounds were elucidated by IR, NMR and LC-MS spectral data. All the synthesized compounds have been screened for their in vitro anti-bacterial and anti-fungal activities. Some of the compounds have been found to be active against both bacterial species at a concentration of 1 microg/mL.


Assuntos
Antibacterianos , Antifúngicos , Azidas , Bactérias/efeitos dos fármacos , Cumarínicos , Fungos/efeitos dos fármacos , Sulfonamidas , Antibacterianos/síntese química , Antibacterianos/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Azidas/síntese química , Azidas/farmacologia , Cumarínicos/síntese química , Cumarínicos/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Sulfonamidas/síntese química , Sulfonamidas/farmacologia
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