Synthesis and anti-inflammatory activity of curcumin succinate prodrugs
10.16438/j.0513-4870.2018-0882
- VernacularTitle:姜黄素琥珀酸酯前药的合成及其抗炎活性评价
- Author:
Cheng NIU
1
;
Dong-ge WANG
1
;
Tian-hong ZHANG
2
;
Hong-liang WEN
1
Author Information
1. School of Chemistry and Chemical Engineering, Beijing Institution of Technology, Beijing 102488, China
2. Institute of Pharmacology and Toxicology, Academy of Military Medical Science, Beijing 100850, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
curcumin;
succinate;
prodrug;
anti-inflammatory
- From:
Acta Pharmaceutica Sinica
2018;53(12):2085-2092
- CountryChina
- Language:Chinese
-
Abstract:
Curcumin, a polyphenolic compound from the plant Curcuma longa L., has shown a wide-spectrum of anti-inflammatory and antitumor activities. Despite the promising biological effects of curcumin, its poor solubility has restricted its use in the management of human ailments. To improve its water-solubility, curcumin succinate prodrugs were designed and synthesized and their aqueous solubility, stability, metabolism in rats and anti-inflammatory activity were evaluated (experiments had been approved by the ethics committee and carried out in accordance with the relevant guidelines and regulations; rats were provided by Beijing courtyard experimental animal center of Academy of Military Medical Sciences). The results showed that curcumin succinate prodrugs are very soluble in water and more stable than curcumin in water and in phosphate buffer solution. They released curcumin rapidly and quantitatively after intravenous administration. In phlogogen-induced paw edema in rats, curcumin succinate prodrugs showed anti-inflammatory activity as potent as dexamethasone.
