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1.
Fitoterapia ; 151: 104867, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-33621655

RESUMEN

Salvia castanea (Family Labiatae), a perennial fragrant herb with castaneous flowers, is mainly distributed in areas with an altitude of 2500-3750 m. The roots of this plant were used as a tea drink by local residents to strengthen physical health. The aim of present study was to acquire secondary metabolites of the ethanol extract obtained from the whole plant of S. castanea and to evaluate their potential anti-Alzheimer's disease. Six new sesquiterpene lactones, salcastanins A-F (1-6), together with three known guaiane-type sesquiterpenoids nubiol (7), nubdienolide (8), and nubenolide (9), were separated from the whole plant of S. castanea. The structures of these compounds were determined by HRESIMS and NMR experiments. The absolute configurations of 1-6 were ascertained by electronic circular dichroism (ECD) experiments. The humanized Caenorhabditis elegans AD pathological model was used to evaluate anti-Alzheimer's disease (AD) activities of 1-9. The results showed the compounds 1-3 and 7 significantly delayed AD-like symptoms of worm paralysis phenotype, which could be used as novel anti-AD candidates.


Asunto(s)
Enfermedad de Alzheimer/tratamiento farmacológico , Extractos Vegetales/química , Salvia/química , Sesquiterpenos/farmacología , Animales , Caenorhabditis elegans/efectos de los fármacos , China , Modelos Animales de Enfermedad , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Sesquiterpenos/aislamiento & purificación
2.
Fitoterapia ; 142: 104536, 2020 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32145310

RESUMEN

Commiphoins A-C (1-3), three new cadinane-type sesquiterpenes, together with two known cadinane-type sesquiterpenes (4 and 5) were isolated from the resinous exudates of Commiphora myrrha. Their structures and relative configurations were established on the basis of comprehensive spectroscopic methods, including HRESIMS, 1D and 2D NMR analyses. Compounds 1 and 3-5 were screened for anti-Alzheimer's disease (AD) activities using the AD pathological model in Caenorhabditis elegans. The results showed that they all had significant anti-AD activities.


Asunto(s)
Enfermedad de Alzheimer/tratamiento farmacológico , Commiphora/química , Sesquiterpenos Policíclicos/aislamiento & purificación , Animales , Animales Modificados Genéticamente , Caenorhabditis elegans , Evaluación Preclínica de Medicamentos , Sesquiterpenos Policíclicos/química , Sesquiterpenos Policíclicos/uso terapéutico , Resinas de Plantas/química
3.
Pak J Pharm Sci ; 32(3): 997-1003, 2019 May.
Artículo en Inglés | MEDLINE | ID: mdl-31278712

RESUMEN

The aim of this study was to investigate the antiepileptic effects of duloxetine in the maximal electroshock test and convulsions induced by four compounds: Pentylenetetrazole, 3-mercaptopropionic acid, thiosemicarbazide, and bicuculline. Duloxetine exhibited moderate anticonvulsive activity with an ED50 (median effective dose) of 48.21 mg/kg in the maximal electroshock test in mice. The anticonvulsive action of duloxetine was also confirmed in chemical-induced seizure tests, where this drug decreased tonic convulsions. Single administration of duloxetine (6.25-25 mg/kg) significantly increased the anticonvulsant effects of valproate, carbamazepine, and oxcarbazepine in the maximal electroshock test. Furthermore, pretreatment with thiosemicarbazide (an inhibitor of GABA synthesis enzyme) significantly increased the ED50 of duloxetine, suggesting the GABAergic system may contribute to the anticonvulsive action of duloxetine. These results support the use of duloxetine in the treatment of coexisting depression and epilepsy.


Asunto(s)
Anticonvulsivantes/farmacología , Clorhidrato de Duloxetina/farmacología , Epilepsia/tratamiento farmacológico , Ácido 3-Mercaptopropiónico/farmacología , Animales , Anticonvulsivantes/administración & dosificación , Anticonvulsivantes/efectos adversos , Antidepresivos/farmacología , Carbamazepina/farmacología , Depresión/tratamiento farmacológico , Evaluación Preclínica de Medicamentos/métodos , Sinergismo Farmacológico , Clorhidrato de Duloxetina/administración & dosificación , Clorhidrato de Duloxetina/efectos adversos , Electrochoque/efectos adversos , Fenclonina/farmacología , GABAérgicos/farmacología , Masculino , Ratones , Síndromes de Neurotoxicidad/etiología , Oxcarbazepina/farmacología , Convulsiones/inducido químicamente , Convulsiones/tratamiento farmacológico , Semicarbacidas/farmacología , Ácido Valproico/farmacología
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