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CC BY 4.0 · Pharmaceutical Fronts 2023; 05(02): e77-e83
DOI: 10.1055/s-0043-1768691
Original Article

In Vivo Antihyperuricemic Activities of 3,4,5-Tri-O-caffeoylquinic acid, 4,4',6'-Trihydroxy-2'-Methoxychalcone, and Caffeic Acid from the Aerial Parts of Gnaphalium Affine

An Jia‡   #
1   Department of Pharmacy, Medical School, Huanghe Science and Technology College, Zhengzhou, People's Republic of China
,
Fei Liu‡   #
2   State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China
3   Marine Sugar Engineering Drug R & D Lab., Marine Biomedical Research Institute of Qingdao, Qingdao, People's Republic of China
,
Si-Yang Fan
1   Department of Pharmacy, Medical School, Huanghe Science and Technology College, Zhengzhou, People's Republic of China
2   State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China
› Author Affiliations Funding This work was supported by the National Natural Science Foundation of China (Grant No. 81603279) and the Natural Science Foundation of Shanghai (Grant No. 15ZR1440100).
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Abstract

The extract of Gnaphalium affine has been reported to have antihyperuricemic and renal protective effects in vivo. The plant could alleviate acute hyperuricemia by inhibiting the activity of xanthine oxidase (XOD). 3,4,5-Tri-O-caffeoylquinic acid (3,4,5-triCQA), 4,4',6'-trihydroxy-2'-methoxychalcone (Chal), and caffeic acid (CA) were identified as the main ingredients of the plant attributed to the potential to retard XOD activity. However, whether the compounds were the effective ingredient of the plant exerting antihyperuricemic activity remained largely unknown. In this study, an experimental mouse model of hyperuricemia was induced by potassium oxonate and hypoxanthine, and orally administered with 3,4,5-triCQA (10 and 20 mg/kg/d), Chal (20 and 40 mg/kg/d), and CA (40 and 80 mg/kg/d) for 6 consecutive days, respectively. Then, serum urate levels and liver XOD activities were assessed. The liver- or kidney-to body weight ratio was calculated. Allopurinol (AP, 50 mg/kg/d) and benzbromarone (BBR, 10 mg/kg/d) were used as controls. Our data showed that there were 52.7 to 81.0% inhibitions in XOD activities in mice treated with 3,4,5-TriCQA (10 and 20 mg/kg/d), Chal (20 and 40 mg/kg/d), and CA (80 mg/kg/d), and 38.8 to 72.5% reduction in uric acid levels in mice treated with 3,4,5-TriCQA (20 mg/kg/d), Chal (20 and 40 mg/kg/d), and CA (40 and 80 mg/kg/d). A larger kidney-to-body weight ratio was observed in hyperuricemic mice and further enhanced by AP treatment. However, the increasing trend was significantly reversed by additional treatment of 3,4,5-triCQA (10 and 20 mg/kg/d) and CA (40 mg/kg/d). Given the above fundings, 3,4,5-triCQA, Chal, and CA may be the key component responsible for the in vivo activities of G. affine for urate-lowering therapy and even promising agents for the treatment of hyperuricemia.

Keywords

Gnaphalium affine - 3,4,5-tri-O-caffeoylquinic acid - 4,4',6'-trihydroxy-2'-methoxychalcone - caffeic acid - antihyperuricemia

Ethics Statement

The use of animals in the study was approved by the Animal Ethical Committee of the Shanghai Institute of Pharmaceutical Industry, which conformed to the National Institutes of Health Guidelines on Laboratory Research and Guide for the Care and Use of Laboratory Animals.


# These authors contributed equally to this work.




Publication History

Received: 08 December 2022

Accepted: 14 April 2023

Article published online:
24 May 2023

© 2023. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting unrestricted use, distribution, and reproduction so long as the original work is properly cited. (https://creativecommons.org/licenses/by/4.0/)

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