RESUMO
Pueraria thomsonii has long been used in traditional Chinese medicine. Isoflavonoids are the principle pharmacologically active components, which are primarily observed as glycosyl-conjugates and accumulate in P. thomsonii roots. However, the molecular mechanisms underlying the glycosylation processes in (iso)flavonoid biosynthesis have not been thoroughly elucidated. In the current study, an O-glucosyltransferase (PtUGT8) was identified in the medicinal plant P. thomsonii from RNA-seq database. Biochemical assays of the recombinant PtUGT8 showed that it was able to glycosylate chalcone (isoliquiritigenin) at the 4-OH position and glycosylate isoflavones (daidzein, formononetin, and genistein) at the 7-OH or 4'-OH position, exhibiting no enzyme activity to flavonones (liquiritigenin and narigenin) in vitro. The identification of PtUGT8 may provide a useful enzyme catalyst for efficient biotransformation of isoflavones and other natural products for food or pharmacological applications.
Assuntos
Clonagem Molecular , Genisteína , Glucosiltransferases/metabolismo , Isoflavonas/farmacologia , Pueraria/químicaRESUMO
OBJECTIVE:To investigate the effect of Cyslosorus acuminatus flavonone glycoside (CAF) on kidney epitheli-al-mesenchymal transition(EMT)in rats with diabetic kidney disease(DKD). METHODS:Rats were randomly divided into nor-mal group(normal saline),model group(normal saline),positive group [rosiglitazone,0.4 mg/(kg·d)],CAF high-dose and low-dose groups [12.5,25 mg/(kg·d)],10 in each group. Except for normal group,other groups were intraperitoneally injected strepto-zotocin(60 mg/kg)+high fat diet to induce DKD,and intragastrically administrated related medicines in 13-16 weeks. After the ex-perimental period,fasting blood glucose level and serum creatinine(Scr),blood urea nitrogen(BUN)contents of rats were detect-ed,collagen deposition and basement membrane thickening in kidney tissue were observed. Immunohistochemistry was used to de-tect α-smooth muscle actin(α-SMA),fibronectin,epithelial cadherin(E-cadherin)expressions in kidney tissue,and Western blot was used to determine the glycogen synthase kinase 3β(GSK-3β),phosphorylated GSK-3β(p-GSK-3β),β-catenin expressions in kidney tissue. RESULTS:Compared with normal group,fasting blood glucose level,Scr and BUN contents in model group were significantly increased (P<0.01);kidney tissue showed obvious collagen deposition and basement membrane thickening;theα-SMA,fibronectin,β-catenin expression levels and GSK-3β phosphorylation degree in kidney tissue were significantly increased (P<0.01),while E-cadherin expression levels was significantly decreased(P<0.01). Compared with model group,fasting blood glucose level,Scr and BUN contents in each administration group were significantly reduced(P<0.05 or P<0.01);collagen depo-sition and basement membrane thickening in kidney tissue were significantly improved;the α-SMA,fibronectin,and β-catenin ex-pression levels and GSK-3β phosphorylation degree in kidney tissue were significantly decreased (P<0.05 or P<0.01),while E-cadherin expression levels in positive group and CAF high-dose group were significantly increased(P<0.01). CONCLUSIONS:CAF can inhibit the kidney EMT of rats with DKD,the molecular mechanism may be associated with downregulating β-catenin ex-pression and inhibiting GSK-3βphosphorylation inactivation.
RESUMO
Citri Reticulatae Pericarpium is a common Chinese materia medica, with extensive distribution, abundant resource, and high medicinal value. Epidemiologic studies showed that Citrus flavonoid intake can relieve the symptom of cardiovascular and cerebrovascular disease. Numerous in vitro and in vivo studies have found that Citri Reticulatae Pericarpium and its composition were good to treat cardiovascular and cerebrovascular disease, including hypolipidemic, anti-fatty liver, anti-thrombusis, anti-atherosclerosis, cardio-cerebral-vascular protection, and anti-oxidant and anti-inflammatory effects closely related to the above. Evidence obtained from these studies indicates that Citri Reticulatae Pericarpium has the potential in the prevention and treatment of cardiovascular and cerebrovascular disease.
RESUMO
Object A systematic study on the chemical constituents of Citrus changshan huyou Y B Chang was carried out in order to reveal the active components for their further development Methods By repeated silica gel chromatographic separation and spectral analysis the structures were determined Results Six compounds of the flavonoids were obtained and identified They were hesperidin (hysperetin 7 O rutonoside) (Ⅰ); naringenin (Ⅱ); nobiletin (3′, 4′, 5, 6, 7, 8 hexamethoxyflavone) (Ⅲ); tangertin (4′, 5, 6, 7, 8 pentamethoxyflavone) (Ⅳ); 5 hydroxy 3′, 4′, 6, 7, 8 pentamethoxyflavone (Ⅴ); 5 hydroxy 3′, 4′, 6, 7, 8 haxamethoxyflavone (Ⅵ) Conclusion The above six compounds were obtained from this plant for the first time