RESUMEN
We investigated whether Hyuganatsu orange (Citrus tamurana Hort. ex Tanaka) contains water and acetic-acid soluble substances that increase bone mineral density (BMD) in ovariectomized rats. In in vivo study, femoral BMD can significantly increased. In in vitro study, tartrate-resistant acid phosphatase (TRAP) positive cells significantly decreased. We speculate that Hyuganatsu orange contains biologically active substances other than hesperidin that increase BMD.
Asunto(s)
Densidad Ósea/efectos de los fármacos , Citrus sinensis/química , Extractos Vegetales/uso terapéutico , Ácido Acético , Fosfatasa Ácida , Animales , Femenino , Fémur , Isoenzimas , Ovariectomía , Extractos Vegetales/farmacología , Ratas , Solubilidad , Fosfatasa Ácida Tartratorresistente , AguaRESUMEN
In this study, we analyzed the CYP3A inhibitory components of star fruit Averrhoa carambola L., using liquid chromatography-mass spectrometry (LC-MS). The stereoisomer of procyanidin B1 and B2 and/or the trimer consisting of catechin and/or epicatechin were suggested to be potent inhibitory components.
Asunto(s)
Inhibidores Enzimáticos del Citocromo P-450 , Magnoliopsida/química , Extractos Vegetales/farmacología , Biflavonoides/aislamiento & purificación , Biflavonoides/farmacología , Catequina/aislamiento & purificación , Catequina/farmacología , Cromatografía Liquida , Citocromo P-450 CYP3A , Frutas , Humanos , Técnicas In Vitro , Espectrometría de Masas , Microsomas Hepáticos/enzimología , Microsomas Hepáticos/metabolismo , Extractos Vegetales/química , Proantocianidinas/aislamiento & purificación , Proantocianidinas/farmacología , EstereoisomerismoRESUMEN
There is limited information on the effect of fruits on human cytochrome P450 (CYP) 2C9 activity. The objective of this study was to determine the effect of fruit juice on CYP2C9-mediated drug metabolism. Nine citrus fruits and eight tropical fruits were chosen. We investigated effects of the fruits on diclofenac 4'-hydroxylation and tolbutamide hydroxylation by human liver microsomes. Among the fruits, pineapple juice showed potent inhibition of CYP2C9 activity. The addition of 25 microl (5.0% v/v) of pineapple juice resulted in almost complete inhibition. Next we examined the inhibitory effect of bromelain, a cysteine protease in pineapple. Bromelain also strongly inhibited CYP2C9 activity. In addition, E-64, a cysteine protease inhibitor, almost entirely blocked inhibition by pineapple juice and bromelain. Thus we found that pineapple juice was a potent inhibitor of CYP2C9, and that the inhibitory effect might be due to the bromelain contained in pineapple.
Asunto(s)
Hidrocarburo de Aril Hidroxilasas/antagonistas & inhibidores , Bebidas , Frutas , Hidrocarburo de Aril Hidroxilasas/metabolismo , Bromelaínas/farmacología , Citocromo P-450 CYP2C9 , Microsomas Hepáticos/enzimología , Inhibidores de Proteasas/farmacología , UltrafiltraciónRESUMEN
The present study was conducted to identify cytochrome P450 3A (CYP3A) inhibitory components of Hyuganatsu, Citrus tamurana Hort., by investigating the effects on midazolam 1'-hydroxylase activity of human liver microsomes. As a consequence, limonin and nomilin were identified as CYP3A inhibitors from the endocarp of Hyuganatsu.