title: Self-assembling bisphosphonates into nanofibers to enhance their inhibitory capacity on bone resorption.
abstract: Osteoporosis (OP) is an important aging-related disease and the effective prevention/treatment of this disease remains challenging. Considering the acidic microenvironment of bone resorption lacunae, herein, we rationally designed two pamidronate (Pami)-derivative and alendronate (Alen)-derivative hydrogelators and which self-assemble into nanofibers to form supramolecular hydrogels under acidic conditions. Cell viability assay, osteoclastogenesis, osteoclastic gene expression, and in vitro bone resorption results indicated that both and have better inhibitory effects on osteoclastic formation and bone resorption than Pami and Alen, respectively. We anticipate that our new drugs and could "smartly" self-assemble and locally concentrate the drugs at bone resorption lacunae in vivo and subsequently prevent/treat osteoporosis more efficiently.
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Department of Chemistry, University of Science and Technology of China, 96 Jinzhai Road, Hefei, Anhui 230026, China. gliang@ustc.edu.cn and Institute of Nuclear Physics and Chemistry, Chinese Academy of Engineering Physics, 64 Mianshan Road, Mianyang, Sichuan 621900, China.
authors.forename: Anming
authors.initials: A
authors.lastname: Tang
authors.affiliation: Department of Orthopaedics, Shaoxing People's Hospital, Shaoxing, Zhejiang 312000, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Qian
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Department of Chemistry, University of Science and Technology of China, 96 Jinzhai Road, Hefei, Anhui 230026, China. gliang@ustc.edu.cn.
authors.forename: Shuang
authors.initials: S
authors.lastname: Liu
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Department of Chemistry, University of Science and Technology of China, 96 Jinzhai Road, Hefei, Anhui 230026, China. gliang@ustc.edu.cn and Institute of Nuclear Physics and Chemistry, Chinese Academy of Engineering Physics, 64 Mianshan Road, Mianyang, Sichuan 621900, China.
authors.forename: Weijuan
authors.initials: W
authors.lastname: Wang
authors.affiliation: Department of Chemistry, Brandeis University, 415 South St, Waltham, MA 02454, USA.
authors.forename: Bing
authors.initials: B
authors.lastname: Xu
authors.affiliation: Shanghai Key Laboratory of Orthopedic Implants, Department of Orthopedic Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, 639 Zhizaoju Road, Shanghai 200011, China. dr_qinan@163.com.
authors.forename: An
authors.initials: A
authors.lastname: Qin
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Department of Chemistry, University of Science and Technology of China, 96 Jinzhai Road, Hefei, Anhui 230026, China. gliang@ustc.edu.cn.
authors.forename: Gaolin
authors.initials: G
authors.lastname: Liang
mesh_terms: D019386:Alendronate; D001862:Bone Resorption; D002478:Cells, Cultured; D004164:Diphosphonates / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D020100:Hydrogels; D057139:Nanofibers / Q000737:chemistry*; D010010:Osteoclasts / Q000187:drug effects*
chemical_list: D004164:Diphosphonates; D020100:Hydrogels; D019386:Alendronate