title: Research on the in vitro anticancer activity and in vivo tissue distribution of Amoitone B nanocrystals.
abstract: Amoitone B, a natural agonist to Nur77, is a promising anticancer drug. However, its application is seriously restricted due to the water-insolubility and short biological half-life. Amoitone B nanocrystals (AmB-NC) were formulated by microfluidization method to overcome the above obstacles. This study aims to evaluate the cytotoxicity and tissue distribution of AmB-NC. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay revealed the improved in vitro antitumor activity of AmB-NC against stomach, colon, liver and lung cancer cells compared with Amoitone B solution. Meanwhile, observation of morphological changes, cell cycle and apoptosis examination using flow cytometry exhibited that AmB-NC could induce G1 cycle arrest and markedly enhance the apoptosis of human gastric cancer BGC-823 cell line. Tissue distribution study demonstrated that AmB-NC had a higher distribution in liver and lung, which was helpful for relevant cancer treatment. In conclusion, AmB-NC could be a potential delivery system for treatment of human cancer.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Leilei
authors.initials: L
authors.lastname: Hao
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Luan
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China. Electronic address: zhangdianrui2006@163.com.
authors.forename: Dianrui
authors.initials: D
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Caiyun
authors.initials: C
authors.lastname: Li
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Hejian
authors.initials: H
authors.lastname: Guo
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Lisi
authors.initials: L
authors.lastname: Qi
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Xinquan
authors.initials: X
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Li
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100083, PR China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D061605:Administration, Intravenous; D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D019540:Area Under Curve; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D048430:Cell Shape / Q000187:drug effects; D005434:Flow Cytometry; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D010648:Phenylacetates / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D014018:Tissue Distribution / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D010648:Phenylacetates; C576231:n-amyl 2-(3,5-dihydroxy-2-(1-nonanoyl)phenyl)acetate
keywords: Amoitone B; Cytotoxicity; Flow cytometry; Nanocrystals; Tissue distribution