RESUMO
Natural helicid (4-formylphenyl-O-ß-d-allopyranoside), a main active constituent from seeds of the Chinese herb Helicia nilagirica, has been reported to exert a sedative, analgesic and hypnotic effect, and is used clinically to treat neurasthenic syndrome, vascular headaches and trigeminal neuralgia. In the current study, mechanical allodynia tests, electroencephalograms, electromyogram recordings and c-Fos expression in neuropathic pain-like model mice of partial sciatic nerve ligation were used to investigate the effect of helicid on neuropathic pain and co-morbid insomnia. Our results showed that helicid at a dose of 100, 200 or 400 mg kg-1 could increase the mechanical threshold by 2.5-, 2.8- and 3.1-fold for 3 h after administration, respectively. Helicid at 200 and 400 mg kg-1 given at 07:00 hours increased the amount of non-rapid eye movement sleep in a 3-h period by 1.27- and 1.35-fold in partial sciatic nerve ligated mice. However, helicid (400 mg kg-1 ) given at 21:00 hours did not change the sleep pattern in normal mice. Immunohistochemical study showed that helicid (400 mg kg-1 ) administration could reverse the increase of c-Fos expression in the neurons of the rostral anterior cingulate cortex and tuberomammillary nucleus, and the decrease of c-Fos expression in the ventrolateral preoptic area caused by partial sciatic nerve ligation. These results indicate that helicid is an effective agent for both neuropathic pain and sleep disturbances in partial sciatic nerve ligated mice.
Assuntos
Benzaldeídos/uso terapêutico , Neuralgia/complicações , Neuralgia/tratamento farmacológico , Distúrbios do Início e da Manutenção do Sono/etiologia , Distúrbios do Início e da Manutenção do Sono/prevenção & controle , Analgésicos/administração & dosagem , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Benzaldeídos/administração & dosagem , Benzaldeídos/farmacologia , Modelos Animais de Doenças , Eletroencefalografia , Eletromiografia , Genes fos/genética , Giro do Cíngulo/efeitos dos fármacos , Giro do Cíngulo/metabolismo , Hiperalgesia/diagnóstico , Hipnóticos e Sedativos/administração & dosagem , Hipnóticos e Sedativos/farmacologia , Hipnóticos e Sedativos/uso terapêutico , Região Hipotalâmica Lateral/efeitos dos fármacos , Região Hipotalâmica Lateral/metabolismo , Ligadura , Masculino , Camundongos , Área Pré-Óptica/efeitos dos fármacos , Área Pré-Óptica/metabolismo , Nervo Isquiático , Sono/efeitos dos fármacos , Sono/fisiologiaRESUMO
A new phenylpropanoid allopyranoside (1) and a new indolinone alkaloid (2) were isolated from the rhizomes of Actaea dahurica (syn. Cimicifuga dahurica). The structures of those two compounds were deduced as cimicifugaside F (1) and 3E,11E-(3-methyl-2-butenylidene acid)-2-indolinone-1-O-ß-d-glucopyranoside (2) by detailed analysis of their MS, 1D and 2D NMR data and comparison with literatures. Additionally, the isolates were evaluated for their inhibitory effects on the production of NO by LPS-stimulated RAW 264.7 macrophages.
Assuntos
Actaea , Alcaloides , Antineoplásicos , Cimicifuga , Actaea/química , Alcaloides/análise , Antineoplásicos/análise , Cimicifuga/química , Estrutura Molecular , Rizoma/químicaRESUMO
Seven new glycosides (1-7) and seventeen known analogues (8-24) were isolated from the leaves of Datura metel L. The structures of these compounds were all elucidated by detailed spectroscopic analyses and comparison with literature values. All isolates were evaluated for cytotoxicity against Hela, MGC-803, Ishikawa cell lines and compounds 6, 7, 14-17 and 24 exhibited different degrees of antiproliferative effects.