| Objective: Hyperuricemia is a metabolic disease caused by purine metabolism disorder,and hyperuricemia is also the biochemical basis of gout.In order to understand the effect of the extract of Malus hupehensis tea on hyperuricemia and to guide the drinking of Malus hupehensis tea better,this paper studies the effect of the extract of Malus hupehensis tea on xanthine oxidase in vitro,the influence on hyperuricemia rats and gout rats.Methods: 1.The inhibitory effects of flavonoids such as tea water extract,alcohol extract and root glucoside of Begonia,triterpenoids such as oleanol and ursolic acid on xanthine oxidase were determined by the method of uric acid generation in vitro.The inhibition mechanism and type of xanthine oxidase were determined.The combined inhibition of two monomers of root skin glycoside and root skin element on xanthine oxidase was determined.2.Hyperuricemia model was established by gavage of 300 mg / kg potassium oxyzinate and 15 g / kg yeast extract.Methods: 72 SD rats were randomly divided into blank group,model group,allopurinol group,low-,medium-,and high-dose groups of Malus hupehensis tea water extract,low-,medium-,and high-dose phloridzin groups,and low-,medium-,and high-dose trihydroxyphloridzin groups,with 6 rats in each group.One hour after modeling,rats in each experimental group were given corresponding samples by gavage,and rats in blank group and model group were given equal volume of normal saline by gavage.Once a day for 14 consecutive days.One hour after the last injection,rats were anesthetized with10% chloral hydrate.Blood was collected from abdominal aorta,serum,liver,kidney and small intestine were taken.The levels of serum uric acid,plasma creatinine and urea nitrogen,XOD activity in liver,GLUT9 and ABCG2 protein and m RNA expression in kidney and small intestine were measured.3.The model of acute gouty arthritis was established by Coderre method.Methods: fifty four SD rats were randomly divided into blank group,model group,colchicine group,low-,medium-,and high-dose groups of Malus hupehensis tea water extract,and low-,medium-,and high-dose phloridzin groups,with 6 rats in each group.The initial circumference of the right ankle joint was measured 12 days after administration.The back of rats in each group was fixed,the right hind leg joint hair was removed and disinfected.At the end of anesthesia,No.6 injection needle was used to insert the medial tibial tendon from 45 directions of the posterior side of the calf joint.The control group was injected with 25 mg / ml sodium urate solution 200 mg / ml μ 50.The blank group was given the same amount of normal saline.The circumference of the same part of the right ankle joint was measured 1 hour before modeling and 24 and 48 hours after modeling,and the swelling index was calculated.The content of uric acid in the joint tissue was measured.Serum samples were taken to determine IL-1 in serum β level.Results:1.The results showed that the extracts of Malus hupehensis tea water,root cortex glycosides,root dermatosin and trihydroxy root glycosides of Malus hupehensis tea alcohol extract had XOD inhibitory activities.IC50 was 1379,22.24,355.2,123.4 and 2.02 μ g/ml,respectively.However,oleanolic acid and ursolic acid did not detect the XOD inhibitory activity in vitro.The inhibition mechanism of root glucosides,root dermatosin and trihydroxy root glucosides on XOD was reversible.The inhibition type of phlegtin on XOD is the mixed inhibition in reversible inhibition.The inhibition type of root skin hormone on XOD was competitive reversible inhibition.The inhibition type of trihydroxy root glucoside on XOD was anti competition inhibition.The combined use of root skin glycoside and root skin hormone had a good inhibitory effect on XOD,and the combined inhibition rate was(73.75 ±2.18)%.2.The hyperuricemia model was successfully reproduced.In the model group,serum uric acid,liver XOD activity,plasma creatinine and urea nitrogen water were significantly increased,and the expression levels of GLUT9 protein and GLUT9 m RNA that promote uric acid reabsorption were significantly increased,while the expression levels of ABCG2 protein and ABCG2 m RNA that promote uric acid excretion were significantly decreased.The water extract of Malus hupehensis tea,phloridzin and trihydroxyphloridzin can reduce serum uric acid.Compared with the model group,the levels of serum uric acid,liver XOD activity,plasma creatinine and urea nitrogen were significantly decreased after administration of phloridzin and trihydroxyphloridzin.Moreover,it significantly reduced the expression of GLUT9 protein in kidney and intestine,and reduced the reabsorption of uric acid by GLUT9 protein.The results showed that the extract of Malus hupehensis tea and phloridzin significantly increased the expression of ABCG2 protein in kidney and intestine,and increased the excretion of uric acid.The expressions of GLUT9 and ABCG2 in intestine were significantly decreased in phloridzin group,while the expressions of GLUT9 and ABCG2 in kidney were increased in high-dose phloridzin group.3.The gouty arthritis model was successfully reproduced.The swelling degree of ankle joint,serum IL-1 β level and uric acid level of ankle joint in model group were significantly increased.After administration of high dose of Malus hupehensis tea extract and phloridzin,the paw swelling of rats was significantly reduced.The results showed that the levels of serum IL-1 β were significantly decreased by low-dose and middle dose of Malus hupehensis tea extract and low-dose phloridzin,and the levels of uric acid in ankle joint were significantly decreased by phloridzin and low-dose and middle dose of Malus hupehensis tea extract.Conclusion: The aqueous extract of Malus hupehensis tea and its main components phloridzin and trihydroxyphloridzin have the effect of reducing uric acid.Its mechanism is related to inhibition of XOD activity and reduction of uric acid production;It can inhibit the protein expression of GLUT9 in kidney and small intestine,promote the protein expression of ABCG2,reduce uric acid reabsorption and increase uric acid excretion.It has a positive effect on regulating uric acid metabolism.Malus hupehensis tea extract and its main component phloridzin can reduce the uric acid in the joints of gouty arthritis rats,which is beneficial to the treatment of gouty arthritis,but has no significant effect on the alleviation of gouty arthritis in rats.The anti-inflammatory effect of water extract from Malus hupehensis and phloridzin was lower in high dose than in medium and low dose.It shows that the traditional application of Malus hupehensis tea is small and scientific. |
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