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1.
Zhonghua Nan Ke Xue ; 18(7): 583-9, 2012 Jul.
Artigo em Zh | MEDLINE | ID: mdl-22994041

RESUMO

OBJECTIVE: To compare the expression of nuclear matrix proteins (NMPs) in benign prostatic hyperplasia (BPH) epithelial cell line BPH-1 versus those in androgen-dependent human prostate cancer cell line LNCap and androgen-independent prostate cancer cell line PC-3. METHODS: We isolated NMPs from the BPH-1, LNCap and PC-3 cell lines by 2-dimensional electrophoresis (2-DE), analyzed the differentially expressed proteins by matrix-assisted laser desorption / ionization time of flight mass spectrometry (MALDI-TOF-MS), and identified them by peptide mass fingerprint and database searching. RESULTS: We successfully obtained well-resolved reproducible 2-DE patterns of NMPs in human prostate cancer cell lines, identified 12 differentially expressed NMPs including enzymes, regulatory proteins, RNA-binding protein and various other factors, 3 up-regulated and 9 down-regulated in prostate cancer cell lines. CONCLUSION: There are obvious differences in the expressions of NMPs between human prostate cancer cell lines and benign prostatic hyperplasia epithelial cell line.


Assuntos
Proteínas Associadas à Matriz Nuclear/metabolismo , Hiperplasia Prostática/metabolismo , Neoplasias da Próstata/metabolismo , Proteoma/análise , Linhagem Celular , Linhagem Celular Tumoral , Eletroforese em Gel Bidimensional , Humanos , Masculino , Proteômica , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz
2.
Steroids ; 159: 108649, 2020 07.
Artigo em Inglês | MEDLINE | ID: mdl-32389717

RESUMO

Mifepristone is one of potent anti-progesterone agents, which binds to progesterone receptors and glucocorticoid receptors. Until now, there are a lot of research focusing on enhancing the solubility and oral bioavailability of Mifepristone. However, poor solubility and oral bioavailability has some undesirable consequences. In this work, Mifepristone in form D was discovered for the first time and characterized by PXRD, TGA, DSC, FT-IR, SEM and SS NMR. Form D was a metastable crystal type which manifested favorable stability under ambient conditions. Form D had better dissolution characteristic compared with commercial Mifepristone in 0.5% SDS solution. In addition, Mifepristone in form D exhibited a 1.43-fold higher peak plasma concentration (Cmax) and 1.46-fold higher area under the curve (AUC) in rats. The work in this paper is a complement to the present understanding of drug polymorphism on the in vitro and in vivo behavior, and establishes the ground work for future development of Mifepristone in form D as a promising drug for the market.


Assuntos
Antagonistas de Hormônios/química , Antagonistas de Hormônios/farmacocinética , Mifepristona/química , Mifepristona/farmacocinética , Administração Oral , Animais , Disponibilidade Biológica , Feminino , Antagonistas de Hormônios/administração & dosagem , Mifepristona/administração & dosagem , Conformação Molecular , Ratos , Ratos Sprague-Dawley , Solubilidade
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