Browsing by Author "Chen, Bin"
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Item Inhibition of CYP3A4 and CYP2C9 by podophyllotoxin: Implication for clinical drug–drug interactions.(2011-12) Song, Jin-Hui; Sun, Dong-Xue; Chen, Bin; Ji, Dai-Hong; Pu, Jie; Jie, Xu; Tian, Feng-De; Guo, LinPodophyllotoxin (PPT) and its derivatives exert significant anti-cancer activities, and one derivative etoposide is often utilized to treat various cancers in the clinic. The aim of the present study is to investigate the inhibitory effects of PPT on major cytochrome P450 (CYP) isoforms in human livers. Inhibition of CYP3A4, CYP2C9, CYP2C8, CYP2D6, CYP2E1 and CYP2A6 by PPT was investigated in the human liver microsomal system. Time-dependent inhibition of CYP3A4 by PPT was also evaluated. The results showed that PPT strongly exhibited inhibitory effects on CYP3A4 and CYP2C9 in a concentration-dependent manner. Half inhibition concentration (IC50) was 1.1±0.3 and 4.6±0.3 μM for CYP3A4 and CYP2C9, respectively. Inhibition kinetic analysis showed that PPT exhibited competitive inhibition towards CYP3A4 and CYP2C9 with Ki of 1.6 and 2.0 μM, respectively. Additionally, PPT exerted time-dependent inhibition towards CYP3A4 and the kinetic parameters were 4.4±2.1 μM and 0.06±0.01 min–1 for KI and kinact, respectively. Our experimental data indicate that potential drug–drug interaction (DDI) might exist when PPT is co-administered with the substrates which mainly undergo CYP3A4- or CYP2C9-mediated metabolism.Item Intraspecific hybridization of Anopheles minimus (Diptera: Culicidae) species A and C in Thailand.(2002-03-16) Choochote, Wej; Rongsriyam, Yupha; Leemingsawat, Somjai; Jitpakdi, Atchariya; Komalamisra, Narumon; Surathin, Kamhaeng; Somboon, Pradya; Chen, Bin; Wongkamchai, Sirijit; Jariyapan, Narissara; Tippawangkosol, Pongsri; Pitasawat, Benjawan; Riyong, DoungratHybridization tests of laboratory-raised, isolines of Anopheles minimus, species A and C were conducted by induced copulation. The three isolines were established based on three morphological variants of wild-caught, fully engorged females and two distinct types of metaphase chromosomes. They were An. minimus species A: V form (X1,Y1), M form (X2,Y1); species C: P form (X3,Y2). The results of reciprocal and back crosses indicated that the two morphologically variant forms of species A were genetically compatible, providing viable progeny and completely synaptic salivary gland polytene chromosomes, whereas they were genetically incompatible with species C and/or the P form. Hybrid progeny was only obtained from both forms of species A females x species C males, but asynaptic salivary gland polytene chromosomes on 3L and partial development of ovarian follicles in females were seen. Back crosses of F1 hybrid males with parental species A females provided viable progeny, while back crosses of F1 hybrid females with parental species C males provided progeny of low viability and adult males with abnormal spermatozoa, suggesting the partial reproductive isolation of An. minimus species A and C.Item Proteomic analysis of cervical cancer cells treated with suberonylanilide hydroxamic acid.(2008-12-31) He, Jianxiong; Huang, Canhua; Tong, Aiping; Chen, Bin; Zeng, Zhi; Zhang, Peng; Wang, Chunting; Wei, YuquanSuberonylanilide hydroxamic acid (SAHA)is an orally administered histone deacetylase inhibitor (HDACI) that has shown significant antitumour activity in a variety of tumour cells.To identify proteins involved in its antitumour activity,we utilized a proteomic approach to reveal protein expression changes in the human cervical cancer cell line HeLa following SAHA treatment.Protein expression profiles were analysed by 2-dimensional polyacrylamide gel electrophoresis (2-DE) and protein identification was performed on a MALDI-Q-TOF MS/MS instrument.As a result,a total of nine differentially expressed proteins were visualized by 2-DE and Coomassie brilliant blue (CBB) staining.Further,all the changed proteins were positively identified via mass spectrometry (MS)/MS analysis. Of these,PGAM1 was significantly downregulated in HeLa cells after treatment with SAHA. Moreover,PGAM1 has been proven to be downregulated in another cervical cancer cell line (CaSki) by western blot analysis.Together,using proteomic tools,we identified several differentially expressed proteins that underwent SAHA-induced apoptosis. These changed proteins may provide some clues to a better understanding of the molecular mechanisms underlying SAHA-induced apoptosis in cervical cancer.