Baicalein alleviates hyperuricemia by promoting uric acid excretion and inhibiting xanthine oxidase

Chen, Yanyu; Zhao, Zean; Li, Yongmei; Yang, Yang; Lü, Li; Yu, Jiang; Lin, Cuiting; Cao, Ying; Zhou, Pingzheng; Tian, Yuanxin; Wu, Ting; Pang, Jianxin

doi:10.1016/j.phymed.2020.153374

Cited by 77 publications

(51 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Another flavonoid, baicalein (compound 4) ( Figure 2 ), was shown by Chen et al [ 41 ] to noncompetitively inhibit URAT1 in a dose-dependent manner with IC 50 of 31.6 μ M. In vivo animal studies have demonstrated that 200 mg/kg baicalein can significantly lower urate levels in PO-induced hyperuricemia mice by elevating urate excretion. Docking analysis and site mutation indicate that baicalein interacts with Ser35 and Phe241 of URAT1.…”

Section: Resultsmentioning

confidence: 99%

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Chen

You

Wang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Human urate anion transporter 1 (hURAT1) is responsible for the reabsorption of uric acid in the proximal renal tubules and is a promising therapeutic target for treating hyperuricemia. To mitigate the side effects of URAT1-targeted clinical agents such as benzbromarone, there is significant interest in discovering new URAT1 inhibitors and developing technology that can evaluate URAT1 inhibition. This review summarizes the methods for assay of URAT1 inhibition and the progress on the discovery of natural and synthetic URAT1 inhibitors in the past five years.

show abstract

Section: Resultsmentioning

confidence: 99%

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Chen

You

Wang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

show abstract

“…Additionally, we demonstrated that DMLE could decrease serum UA levels in PO-induced hyperuricemic mice by inhibiting hepatic XOD activity. Inhibiting XOD activity in the liver reduces UA production and enhances UA excretion [43,44]. DMLE-70 at all doses did not exhibit potent hypouricemic effects in serum compared with PC, but inhibiting hepatic XOD activity was significantly effective with DMEE-200 compared with the PC (Table 6), although the amount of uric acid excreted in urine was decreased compared with PC.…”

Section: Discussionmentioning

confidence: 97%

Antihyperuricemic Effect of Dendropanax morbifera Leaf Extract in Rodent Models

Lee

Kim

Han

et al. 2021

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Dendropanax morbifera is a well-known traditional medicine used in China and Korea to treat intestinal disorders, urosis, diuresis, and chronic glomerulonephritis. Hyperuricemia is a metabolic disorder characterized by a high uric acid level in serum due to an imbalance between uric acid production and excretion and causes gout. Recently, the prevalence of hyperuricemia worldwide has been continuously increasing. Xanthine oxidase (XOD) inhibitors (allopurinol (ALP) and febuxostat) and uricosuric agents (benzbromarone and probenecid) are used to treat hyperuricemia clinically. However, because these drugs are poorly tolerated and cause side effects, such as kidney diseases, hepatotoxicity, gastrointestinal symptoms, and hypersensitivity syndrome, only a limited number of drugs are available. We investigated the antihyperuricemic effects of Dendropanax morbifera leaf ethanol extract (DMLE) and its underlying mechanisms of action through in vitro and in vivo studies. We evaluated uric acid levels in serum and urine, and xanthine oxidase (XOD) inhibition activity in the serum and liver tissue of a hyperuricemic rat model of potassium oxonate (PO)-induced hyperuricemic rats. In vitro study, XOD-inhibitory activity was the lowest among the test substances at the IC50 of ALP. However, the IC50 of DMLE-70 was significantly low compared with that of other DMLEs ( p < 0.05 ). In PO-induced hyperuricemic rats, uric acid (UA) levels in serum and urine were significantly reduced in all DMLE-70 and allopurinol-treated (ALT) groups than in the PC group ( p < 0.05 ). UA levels in urine were lower than those in serum in all DME groups. In PO-induced hyperuricemic rats, DMEE-200 reduced UA concentration in serum and increased UA excretion in the urine. These findings suggest that DMLE exerts antihyperuricemic and uricosuric effects on promoting UA excretion by enhanced secretion and inhibition of UA reabsorption in the kidneys. Thus, DMLE may be a potential treatment for hyperuricemia and gout.

show abstract

“…Following hypertension, hyperlipidemia, and hyperglycemia, hyperuricemia has become one of the most common metabolic diseases, [ 1 ] which is primarily caused by excessive elevation of serum uric acid (UA) owing to “underexcretion” or “renal overload” of the urate. [ 2 , 3 , 4 ] Hyperuricemia is the most crucial risk factor for the occurrence of gout triggered by the deposition of monosodium urate crystals around the joints derived from the supersaturation of urate in the blood.…”

Section: Introductionmentioning

confidence: 99%

Noninvasive and Individual‐Centered Monitoring of Uric Acid for Precaution of Hyperuricemia via Optical Supramolecular Sensing

Zhang

Chai

et al. 2022

Advanced Science

View full text Add to dashboard Cite

Characterized by an excessively increased uric acid (UA) level in serum, hyperuricemia induces gout and also poses a great threat to renal and cardiovascular systems. It is urgent and meaningful to perform early warning by noninvasive diagnosis, thus conducing to blockage of disease aggravation. Here, guanidinocalix[5]arene (GC5A) is successfully identified from the self-built macrocyclic library to specifically monitor UA from urine by the indicator displacement assay. UA is strongly bound to GC5A at micromolar-level, while simultaneously excluding fluorescein (Fl) from the GC5A•Fl complex in the "switch-on" mode. This method successfully differentiates patients with hyperuricemia from volunteers except for those with kidney dysfunction and targets a volunteer at high risk of hyperuricemia. In order to meet the trend from hospital-centered to individual-centered testing, visual detection of UA is studied through a smartphone equipped with a color-scanning feature, whose adaptability and feasibility are demonstrated in sensing UA from authentic urine, leading to a promising method in family-centered healthcare style. A high-throughput and visual detection method is provided here for alarming hyperuricemic by noninvasive diagnosis.

show abstract

Baicalein alleviates hyperuricemia by promoting uric acid excretion and inhibiting xanthine oxidase

Cited by 77 publications

References 27 publications

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Antihyperuricemic Effect of Dendropanax morbifera Leaf Extract in Rodent Models

Noninvasive and Individual‐Centered Monitoring of Uric Acid for Precaution of Hyperuricemia via Optical Supramolecular Sensing

Contact Info

Product

Resources

About