Abstract

BackgroundThe medicinal plant Siegesbeckia orientalis L. has been commonly used for the treatment of acute arthritis, rheumatism, and gout in Vietnam. However, pharmacological research of this plant associated with gout has not been reported. Anti-hyperuricemic and anti-inflammatory effects were evaluated and observed for the crude ethanol extract (CEE) of S. orientalis. Retention of these biological properties was found in a n-butanol-soluble fraction (BuOH fr.) of the extract, and therefore further biological and chemical investigations were undertaken on the BuOH fr. to support the medical relevance of this plant.MethodsThe aerial part of S. orientalis was obtained in the mountainous region of Vietnam. The crude ethanol extract (CEE) and its BuOH fr. were prepared from the plant materials. Anti-hyperuricemic activities of the CEE and BuOH fr. were tested in vivo using the model oxonate-induced hyperuricemia rats through determination of serum uric acid levels and inhibitory effects on xanthine oxidase (XO) in the rat liver. Anti-inflammatory activities of the BuOH fr. were also evaluated in vivo using carrageenan-induced paw edema and urate-induced synovitis in rats. Active components of the BuOH fr. were characterized by comparison of HPLC retention time (tR) and spectroscopic data (UV, 1H–NMR) with those of reference compounds.ResultsThe CEE of S. orientalis displayed anti-hyperuricemic activity, and the BuOH fr. was found to be the most active portion of the extract. Further in vivo studies on this fraction showed 31.4% decrease of serum uric acid levels, 32.7% inhibition of xanthine oxidase (XO), 30.4% reduction of paw edema volume, symptomatic relief in urate-induced synovitis and significant analgesic effect at the dose of 120 mg/kg, as compared to the corresponding values of the control groups. Chemical analysis of the BuOH fr. revealed high phenolic content, identified as caffeic acid analogues and flavonones.ConclusionsThis study suggested that anti-hyperuricemic and anti-inflammatory mechanism of S. orientalis is related to XO inhibitory effect of the phenolic components. Our findings support the use of this plant as the treatment of gout and other inflammatory diseases.

Highlights

  • The medicinal plant Siegesbeckia orientalis L. has been commonly used for the treatment of acute arthritis, rheumatism, and gout in Vietnam

  • Taking into consideration both anti-inflammatory and xanthine oxidase (XO) inhibitory effects, we focused on flavonoids and other phenolic compounds which are extensively studied and well-known antioxidants as potential phytochemical agents for treating diseases mediated by free radicals, including inflammation and gout [19, 20]

  • Effect of crude ethanol extract (CEE) on serum uric acid levels in rats The CEE at 300, 600, and 1200 mg/kg were orally administered for 5 days on oxonate-induced hyperuricemia rats, and serum uric acid levels were measured by the phosphotungstic acid method

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Summary

Introduction

The medicinal plant Siegesbeckia orientalis L. has been commonly used for the treatment of acute arthritis, rheumatism, and gout in Vietnam. Anti-hyperuricemic and anti-inflammatory effects were evaluated and observed for the crude ethanol extract (CEE) of S. orientalis. Retention of these biological properties was found in a n-butanol-soluble fraction (BuOH fr.) of the extract, and further biological and chemical investigations were undertaken on the BuOH fr. Being known as a Vietnamese indigenous medicine “hy-thiem”, this plant has been applied in a series of traditional remedies for the treatment of acute arthritis, rheumatism, inflammation, and especially gout and pain [1, 3, 4]. Given that inflammatory response is a key step in the onset of gout symptoms [10], anti-inflammatory effects were thought to be responsible for traditional utilization of S. orientalis as a part of symptomatic treatment of this disorder

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