Gd-Complex of a Rosmarinic Acid Conjugate as an Anti-Inflammatory Theranostic Agent via Reactive Oxygen Species Scavenging

Antioxidants

Bokyung Sung¹  Seonghwan Hwang¹  Yongmin Chang¹  Hee-Kyung Kim²  Yeoun-Hee Kim³ 

[1] Department of Medical & Biological Engineering, Kyungpook National University, Daegu 41944, Korea;Laboratory Animal Center, Daegu-Gyeongbuk Medical Innovation Foundation, Dong-gu, Daegu 41061, Korea;Mirae BioPharm. Co., 124, Sagimakgol-ro, Jungwon-gu, Gyeonggi-do 13207, Korea;

关键词: rosmarinic acid;    Gd-chelate;    anti-inflammatory effects;    antioxidants;    theranostic agent;   

DOI  :  10.3390/antiox9080744

来源: DOAJ

【 摘 要 】

Rosmarinic acid (RosA), an important polyphenol, is known for its antioxidant and anti-inflammatory activities. However, its application in theranostics has been rarely reported. Therefore, a new single-molecule anti-inflammatory theranostic compound containing RosA would be of great interest. A gadolinium (Gd) complex of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid (DO3A) and RosA (Gd(DO3A-RosA)(H₂O)) was synthesized and examined for use as a single-molecule theranostic agent. Its kinetic stability is comparable to that of clinically used macrocyclic magnetic resonance imaging contrast agents. In addition, its relaxivity is higher than that of structurally analogous Gd-BT-DO3A. This agent was evaluated for inflammatory targeting magnetic resonance contrast and showed strong and prolonged enhancement of imaging in inflamed tissues of mice. The theranostic agent also possesses antioxidant and anti-inflammatory activities, as evidenced by reactive oxygen species scavenging, superoxide dismutase activity, and inflammatory factors. The novel RosA-conjugated Gd complex is a promising theranostic agent for the imaging of inflamed tissues, as well as for the treatment of inflammation and oxidative stress.

【 授权许可】

Unknown