RESUMO
Cocktail recipes containing Psoralea corylifolia seeds (PCS) are used to empirically treat Parkinson disease. A PCS isolate Delta(3),2-hydroxybakuchiol (BU) can inhibit dopamine uptake in dopamine transporter (DAT) transfected Chinese hamster ovary (CHO) cells, and dopamine reuptake blockade may provide an alternative approach for ameliorating parkinsonism. Here, we assessed the potential dopaminergic neuroprotective, and antiparkinsonian-like activity of BU. BU sample size was increased by using a scale-up extraction paradigm. Pharmacologically, BU significantly protected SK-N-SH cells from 1-methyl-4-phenylpyridinium (MPP(+)) insult, produced striking inhibitory actions on dopamine/norepinephrine uptake and WIN35,428 binding in synaptosomes on in vivo administration, and significantly preventing poor performance on rotarod and dopaminergic loss in substantia nigra in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mice. BU acts by protecting dopaminergic neurons from MPP(+) injury and preventing against MPTP-induced behavioral and histological lesions in the Parkinson's disease (PD) model, possibly by inhibiting monoamine transporters. These findings suggest that BU could be meaningful in PD treatment.
Assuntos
Antiparkinsonianos/farmacologia , Dopaminérgicos/farmacologia , Fármacos Neuroprotetores/farmacologia , Fenóis/farmacologia , Psoralea/química , 1-Metil-4-Fenil-1,2,3,6-Tetra-Hidropiridina/farmacologia , 1-Metil-4-fenilpiridínio/farmacologia , Animais , Antiparkinsonianos/química , Antiparkinsonianos/isolamento & purificação , Células CHO , Linhagem Celular , Cocaína/análogos & derivados , Cocaína/metabolismo , Cricetinae , Cricetulus , Dopamina/metabolismo , Dopaminérgicos/química , Dopaminérgicos/isolamento & purificação , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Norepinefrina/metabolismo , Doença de Parkinson/tratamento farmacológico , Fenóis/química , Fenóis/isolamento & purificação , Ratos , Ratos Sprague-Dawley , Sinaptossomos/efeitos dos fármacos , Sinaptossomos/metabolismo , Tirosina 3-Mono-Oxigenase/metabolismoRESUMO
Three new diterpenoids, eriocalyxins C-E (1-3), were isolated from Isodon eriocalyx. Their structures were elucidated as 6beta-hydroxy-15beta-acetoxy-3alpha,20-epoxy-16beta, 17-epoxy-ent-kaur-1,7-dione (1), 1alpha,7beta-dihydroxy-6beta, 15beta-diacetoxy-7,20-epoxy-ent-kaur-16-ene (2), and 15beta-acetoxy-1,6-dioxo-6,7-seco-ent-kaur-2,16-dien-7,20-olide (3), respectively, by means of spectroscopic methods, including one- and two-dimensional NMR techniques.
RESUMO
Two new diterpenoids, pierisformoside A (1) and pierisformosin D (2), and two known diterpenoids, asebotoxins VIII (3) and V (4), were isolated from leaves of Pieris formosa. Their structures were elucidated on the basis of spectral analysis, including 1H-1H COSY, 13C-1H COSY, HMBC, and NOESY experiments.
