echanisms of antihyperuricemic effect of Phyllanthus niruri and its lignan onstituents ikneswaran Murugaiyah (original) (raw)
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Tropical Journal of Pharmaceutical Research, 2015
Purpose: To evaluate the in-vitro inhibition of xanthine oxidase (purified from bovine milk) by extracts of Lycium arabicum, as well as it is in vivo hypouricemic and renal protective effects. Methods: Four extracts of Lycium arabicum, methanol (CrE), chloroform (ChE), ethyl acetate (EaE) and aqueous (AqE) extracts, were screened for their total phenolics and potential inhibitory effects on purified bovine milk xanthine oxidase (XO) activity by measuring the formation of uric acid or superoxide radical. The mode of inhibition was investigated and compared with the standard drugs, allopurinol, quercitin and catechin. To evaluate their hypouricemic effect, the extracts were administered to potassium oxonate-induced hyperuricemic mice at a dose of 50 mg/kg body weight. Results: The results showed that EaE had the highest content of phenolic compounds and was the most potent inhibitor of uric acid formation (IC50 = 0.017 ± 0.001 mg/mL) and formation of superoxide (IC50 = 0.035 ± 0.001 mg/ml). Lineweaver-Burk analysis showed that CrE and EaE inhibited XO competitively, whereas the inhibitory activities exerted by ChE and AqE were of a mixed type. Intraperetoneal injection of L. arabicum extracts (50 mg/kg) elicited hypouricemic actions in hyperuricemic mice. Hyperuricemic mice presented a serum uric acid concentration of 4.71 ± 0.29 mg/L but this was reduced to 1.78 ± 0.11 mg/L by EaE, which was the most potent hyporuricemic extract. Conclusion: L. arabicum fractions have a strong inhibitory effect on xanthine oxidase and and also have a significantly lowering effect on serum and liver creatinine and urea levels in hyperuricemic mice.
Pharmacia
Hyperuricemia is a risk factor for gout and other cardiovascular diseases. One of the therapies used is Allopurinol. Unfortunately, it has unwanted side effects. These conditions made researchers continue to seek and develop alternative treatments from natural products. One of which is from plants of the Phyllanthus genus. One of their contents was polyphenols, especially flavonoids. It is an alternative treatment for hyperuricemia because of its minimal side effects. The flavonoids in this genus were reported to have xanthine oxidase inhibitory: quercetin, kaempferol, rutin, apigenin, luteolin, myricetin, catechin, epicatechin, and epigallocatechin with IC50 values from 0.44 M to > 100μM. The presence of π-π interactions between planar rings A and C on flavones with phe 1009 and phe 914 and the addition of hydroxyl groups on flavonoid compounds plays a crucial role in inhibiting xanthine oxidase.
Pakistan journal of scientific and industrial research, 2021
The Phyllanthus niruri is traditionally used for curing of kidney disorders and urinary stones in Malaysia. Hence the current work was aimed to evaluate the effect of different solvents extract (n- hexane, ethyl acetate, methanol and water) of P. niruri for in vitro anti-urolithiatic properties in terms of inhibition activity on CaOx by using the rate of CaOx aggregation assay and dissolution of calcium oxalate (CaOx) crystal by using titrimetry method. Cystone was used as positive control. The effects of cystone on slope of nucleation and aggregation as well as growth of CaOx were evaluated spectrophotometrically. The highest yield percentage of P.niruri was occupied by methanol (5.74 %). The maximum inhibition against aggregation of CaOx crystals was also occupied by methanol (66.67 % ± 1.61) and was comprised with alkaloid, steroid, terpenoid and tannin. Dissolution effect on calcium oxalate crystals indicates that the aqueous extracts of P. niruri was found to be more effective ...
Molecules
Toona sinensis leaf is used as a seasonal vegetable in Korea. A 70% ethanol extract of these leaves exhibited potent xanthine oxidase (XO) inhibition, with a 50% inhibitory concentration (IC50) of 78.4 µM. To investigate the compounds responsible for this effect, bioassay-guided purification led to the isolation of five constituents, identified as quercetin-3-O-rutinoside, quercetin-3-O-β-d-glucopyranoside, 1,2,3,4,6-penta-O-galloyl-β-d-glucopyranose (compound 3), quercetin-3-O-α-l-rhamnopyranoside, and kaempferol-3-O-α-l-rhamnopyranoside. Compound 3 showed the most potent inhibition of XO, with an IC50 of 2.8 µM. This was similar to that of allopurinol (IC50 = 2.3 µM), which is used clinically to treat hyperuricemia. Kinetic analyses found that compound 3 was a reversible noncompetitive XO inhibitor. In vivo, the T. sinensis leaf extract (300 mg/kg), or compound 3 (40 mg/kg), significantly decreased serum uric acid levels in rats with potassium oxonate-induced hyperuricemia. Furthe...
Potravinarstvo Slovak Journal of Food Sciences
Uric acid is the final product of purine metabolism and is categorized as hyperuricemia when it reaches >6.0 mg.dL-1 for women and >7.0 mg.dL-1 for men. The chayote leaves (Sechium edule) contain a high amount of flavonoid and might be used as an alternative to reduce hyperuricemia. The purpose of this study is to analyze the effect of chayote leaves (Sechium edule)’s flavonoid fraction on the level of uric acid and the activity of xanthine oxidase (XO) in Sprague Dawley Rats. The flavonoid fraction (FF) was obtained by extracting the chayote leaves, fractionating with n-hexane, hydrolyzing with HCl, and finally re-fractionating with ethyl acetate. Thirty male Sprague Dawley rats were induced for hyperuricemia by potassium oxonate and broth block for 21 days, and the interventions were given orally for 14 days. The rats were divided randomly into five groups: normal control (K-), hyperuricemia control (K+), hyperuricemia with FF dose 50 mg.200g-1 body weight (P1), hyperuricemi...
Phyllanthus amarus is a medicinal plant with immense benefits. Several experimental investigations have explored and establish its phytochemical constituents. This study was carried out to evaluate the antioxidant potentials and inhibitory effects of the hydro-alcoholic extract of the leaves on two major enzymes involved in the hydrolysis of extracellular ATP- Nucleoside triphosphate diphosphohydrolase (NTPDases) and 5?-nucleotidase in rat tissues using in-vitro models. The extract shows a dose dependent scavenging abilities against free radicals such as 2,2 diphenyl-2-picrylhydrazyl (DPPH), hydrogen peroxide (H2O2), hydroxyl radical, superoxide radical, and nitric oxide(NO) radicals. The ferric reducing power, Vitamin C content and total phenol content also increases as the concentration increases. The extract of Phyllanthus amarus showed significant inhibition (P< 0.05) of NTPDase and 5?-nucleotidase enzymes in rat tissues with increasing concentrations. Research has shown that targeting these purinergic enzymes could be a novel target for cancer immunotherapy and have been projected to be valuable tools in clinical therapeutics such as in the treatment of chronic pain, immune system diseases and cancer, as they would prolong the physiological effects of extracellular nucleotides or simultaneously administered nucleotide analogues. The hydro- alcoholic extract of Phyllanthus amarus with its high radical scavenging ability and inhibitory effects on the purinergic enzymes could be explored in the treatment of chronic pain, cancer and immune system related diseases.
International Journal of Pharmacy and Pharmaceutical Sciences, 2015
Objective: The objective of this research was to evaluate the xanthine oxidase (XO) inhibitory activity and the ability to reduce serum uric acid levels of 70% ethanol extracts of Anredera cordifolia (ACE) and Sonchus arvensis (SAE) leaves, and its combinations. Methods: Inhibitory activity of XO was determined by measuring uric acid formation by UV spectrophotometry. Moreover, the antihyperuricemic assay conducted in vivo in male Wistar rats was induced by high-purine diet and potassium oxonate (PO). The reduction of serum uric acid levels after extracts administration was observed and compared to allopurinol. Results: The IC50 results of ACE, SAE, and the combination of both with a ratio of 1:1 were obtained 635.25 ppm, 1345.93 ppm, and 846.32 ppm, respectively. The IC50 Conclusion: ACE and SAE had xanthine oxidase inhibitory and antihyperuricemic activities, and its combination provided an additive effect. The results were suggested that the extracts may have a considerable potential for developing as antihyperuricemia agent. of allopurinol as reference was 0.88 ppm. Hence, XO inhibitory activity of the combination extracts was additive. Results of antihyperuricemic assay showed that uric acid levels of the group of allopurinol, ACE, SAE, and the combination of both extracts were significantly lower compared to the positive control group at 120 and 150 minutes after PO induction (p<0.05). Combination extracts provide an additive effect in lowering serum uric acid levels.
The pharmacological potential of Phyllanthus niruri
Introduction Phyllanthus niruri is a traditional shrub of the genus Phyllan-thaceae with long-standing Ayurvedic, Chinese and Malay ethnomedical records. Preliminary studies from cell and animal model have provided valuable scientific evidence for its use. Aim This review aims to summarize selected scientific evidence on the pharmacological properties of P. niruri over the past 35 years while identifying potential areas of further development of this herb as an economical adjunct. Methods The review covers literature pertaining to the evidence base therapeutic potential of P. niruri spanning from 1980 to 2015 available on PubMed. Results Evidence suggests that the extracts of P. niruri possess hepatoprotective, antiviral, antibacterial, hypolipidaemic, hypoglycaemic, analgesic, anti-inflamma-tory, cardioprotective, anti-urolithiatic and antihyperuricaemic properties due its novel bioactive compounds. Conclusion Scientific evidence suggests that there is strong pharmacological potential in developing P. niruri as a drug to be used in liver disorders and in antiviral therapy. Despites this, large-scale heterogeneity in study protocol and unstandardized reporting standards limit the ability for valuable comparison and may mask the ability to replicate these studies. Thus interpretation of findings should be performed with caution and further studies should be performed in line with best practices. More cheminformatics, toxicological and mechanistic studies would aid the progress to clinical trial studies.
Asian Journal of Pharmaceutical and Clinical Research
Objective: Hyperuricemia (high uric acid levels) prevalence increased year by year. This study was aimed to elaborate the in vitro xanthine oxidase (XO) inhibitory activity and in vivo lowering hyperuricemic effect of Uncaria gambir (Hunter) Roxb) (gambir), Caesalpinia sappan L. (secang) and the combined extract of secang and gambir (formulae extract [FE]).Methods: Gambir and secang extracts were prepared by maceration with ethanol and FE was the proportioned combination of these two extracts. XO inhibitory activity was determined by measuring the formation of uric acid in the xanthine/XO system in vitro using allopurinol as a positive control at 100 ug/mL. Antioxidant activity was by 1,1-diphenyl-2-picrylhydrazyl radical reducing methods. The in vivo experiments were conducted in the oxonate-induced hyperuricemia rat model, in which FE was gavaged p.o. at the arrange dose of 75, 150, and 300 mg/kg bw for 2 weeks. Polyphenol content was measured using Folin–Ciocalteu reagent spectr...
Xylopia aethiopica fruit extract lowers uric acid levels in wistar albino rats
The effect of aqueous fruit extract of Xylopia aethiopica on bile, serum and fecal uric acid levels as well as bile secretion and cholesterol (LDL, VLDL, HDL and triglycerides) were studied in wistar albino rats. Thirty (30) wistar albino rats were divided into three groups of ten (10) rats each after an acclimatization period of seven (7) days. The control group received normal rat chow and water freely. The two test group's ii and iii received daily oral administration of 100mg/kg b.w and 200mg/kg b.w/day respectively of the fruit extract for 28 days, water and standard feed given ad libitum. At the end of the experimental period, bile, serum and feces from the three groups were analyzed for bilirubin and uric acid. Bile flow rate (ml/h) was significantly (p<0.05) lower in the test groups when compared with control. Total and unconjugated bile bilirubin in group ii were significantly (p<0.001) lower than control, while total, conjugated and unconjugated bile bilirubin in group iii was significantly (p<0.001) higher when compared with control. In the serum, total, conjugated and unconjugated biliribin was significantly (p<0.05, 0.001) higher in the group iii when compared with the control. Serum and fecal uric acid levels in the test groups were significantly (p<0.001) lower than in their control. The plasma cholesterol, LDL, HDL and triglycerides were significantly decreased in group i while the extract significant increased plasma triglyceride, VLDL but increased plasma LDL and HDL. It appears that low and high doses of aqueous fruit extract of Xylopia aethiopica caused the lowering of uric acid levels in serum and feces, and this might be a panacea to arthritis and gout , atherosclerosis, coronary heart diseases and other cardiovascular related disorders.