title: A Glycyrrhetinic Acid-Modified Curcumin Supramolecular Hydrogel for liver tumor targeting therapy.
abstract: Curcumin (Cur), a phenolic anti-oxidant compound obtained from Curcuma longa plant, possesses a variety of therapeutic properties. However, it is suffered from its low water solubility and low bioavailability property, which seriously restricts its clinical application. In this study, we developed a glycyrrhetinic acid (GA) modified curcumin supramolecular pro-gelator (GA-Cur) and a control compound Nap-Cur by replacing GA with the naphthylacetic acid (Nap). Both compounds showed good water solubility and could form supramolecular gels by disulfide bond reduction triggered by glutathione (GSH) in vitro. Both formed gels could sustainedly release Cur in buffer solutions. We also investigated the cytotoxicity of pro-gelators to HepG2 cells by a MTT assay and determined the cellular uptake behaviours of them by fluorescence microscopy and LC-MS. Due to the over expression of GA receptor in liver cancer cells, our pro-gelator of GA-Cur showed an enhanced cellular uptake and better inhibition capacity to liver tumor cells than Nap-Cur. Therefore, the GA-Cur could significantly inhibit HepG2 cell growth. Our study provides a novel nanomaterial for liver tumor chemotherapy.
authors.affiliation: Cardiology Department of Panyu Central Hospital, Guangzhou, China; Cardiovascular Disease Institute of Panyu District, Guangzhou, Guangdong 511400, P. R. China.
authors.forename: Guoqin
authors.initials: G
authors.lastname: Chen
authors.affiliation: Guangzhou University of Chinese Medicine, Guangzhou, Guangdong 510006, Cardiology Department of Panyu Central Hospital, Guangzhou, Guangdong 511400, P. R. China.
authors.forename: Jinliang
authors.initials: J
authors.lastname: Li
authors.affiliation: Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China.
authors.forename: Yanbin
authors.initials: Y
authors.lastname: Cai
authors.affiliation: Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China.
authors.forename: Jie
authors.initials: J
authors.lastname: Zhan
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, Nankai University, Tianjin 300071, P. R. China.
authors.forename: Jie
authors.initials: J
authors.lastname: Gao
authors.affiliation: Cardiology Department of Panyu Central Hospital, Guangzhou, China; Cardiovascular Disease Institute of Panyu District, Guangzhou, Guangdong 511400, P. R. China.
authors.forename: Mingcai
authors.initials: M
authors.lastname: Song
authors.affiliation: Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Shi
authors.affiliation: Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China.
authors.forename: Zhimou
authors.initials: Z
authors.lastname: Yang
mesh_terms: D003474:Curcumin / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D006034:Glycyrrhetinic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D020100:Hydrogels / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology
chemical_list: D020100:Hydrogels; D003474:Curcumin; D006034:Glycyrrhetinic Acid