Chemical constituents from the leaves of Anisopus mannii and the melanogenesis inhibitory activities / 中国药科大学学报

@#The phytochemical studies on the leaves of Anisopus mannii led to the isolation of seven compounds by silica gel, ODS, DIAION HP-20, Sephadex LH-20 colunmn chromatographer, their structures were elucidated on the basis of the spectroscopic analyses(NMR, HRMS)and the comparisons with the literatures as 3β-acetoxylup-20(29)-ene(1), 1-acetoxy-2-isopropyl-1-tridecene(2), rutin(3), 3, 6′-diferuloylsucrose(4), 3-O-β-D-glucopyranosyl-3-β-hydroxyolean-12-en-28-oic acid 28-O-［α-L-rhamnopyra- nosyl-(1→2)-β-D-glucopyranosyl］ ester(5), conduritol A(6), hoyacarnoside I(7). Meanwhile, the isolated compounds were evaluated for their inhibitory activities against melanogensis in B16 melanoma cells, as the results, all compounds exhibited melanogenesis-inhibitory activity and compound 5 showed a strongest activity(Melanin content: (27. 4±3. 5)%, Cell Viability: (54. 9±5. 6)% with a concentration of 30 μmol/L)which could be further developed.

Total phenolic contents and bioactivities of defatted Vitellaria paradoxa kernels from different origin / 中国药科大学学报

@#Total phenolic contents, antioxidant, cytotoxic and Epstein-Barr virus early antigen(EBV-EA)inhibitory activities of twenty-six methanol extracts from defatted Vitellaria paradoxa kernel at different sites were investigated. Furthermore, the correlation between total phenolic contents and bioactivities was discussed. The total phenolic contents were determined spectrometrically and antioxidant activities were evaluated by 1, 1-diphenyl-2-picrylhydrazyl(DPPH), 2, 2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid(ABTS)radical scavenging activity and ferric-reducing antioxidant power(FRAP)methods. The cytotoxic activities against human leukemia HL60 cells, lung cancer A549 cells and breast cancer SK-BR-3 cells were assessed by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl-2H-tetrazolium bromide(MTT)assay and the inhibitory effect on EBV-EA was assayed by the indirect immunofluorescence technique. Results showed that the total phenolic contents of twenty-six methanol extracts were different(25. 8 - 265. 7 mg GAE/g DW). In addition, some of the extracts had potent antioxidant activities(DPPH: IC50 3. 4 - 54. 9 μg/mL, ABTS: 1. 11- 4. 09 mmol TE/g, FRAP: 1. 24 - 1. 93 mmol TE/g), toxicities against one or more of HL60, A549 and SK-BR-3 cells(IC50 25. 1- 95. 5 μg/mL)and inhibitory effect on EBV-EA(85. 8%- 94. 9% at 100 μg/mL). A significant correlation was observed between total phenolic contents and antioxidant activities(r=0. 750-0. 837, P< 0. 01).

Effects of Suppressor of Cytokine Signaling-1 Silencing on the Proliferation and Interferon Gamma Susceptibility of Human Pancreatic Cancer Cells / 天津医药

Objective To detect the changes of cell proliferation and IFN-γsusceptibility of human pancreatic can-cer cells after suppressor of cytokine signaling-1 (SOCS1) gene silencing, and to explore the SOCS1 as the target of anti-tu-mor therapy through enhancing the function of IFN-γ. Methods Western blot assay, PCR and real-time PCR were used to verify the down regulation of SOCS1 in human pancreatic cancer cell (PANC1) after transfection;subsequently, PANC1 was stimulated with IFN-γ. Western blot assay was also used to detect the expression of signal transducers and activators of tran-scription (STAT)1 and phosphorylation STAT(pSTAT)1;and the change of IFN-γsusceptibility was detected by MTT assay. Real-time PCR was used to detect the mRNA of interferon regulatory factor-1(IRF-1). Flow cytometry was used to detect the cell cycle. Results The expression levels of SOCS1 mRNA and protein were significantly decreased in small hairpin SCOS1 (shSOCS1) transfected PANC1 cells. After the silence of SOCS1, the expression levels of IRF-1 and pSTAT1 in-creased significantly (P<0.05), and the median inhibitory concentration(IC50)of IFN-γfor PANC1 cells decreased signifi-cantly (P<0.01). The cell count of shSOCS1 cells dropped significantly compared with that of control group after the SOCS1 silencing for 72 hours (P<0.05). The cell cycle arrest was promoted at the G0/G1 phase, but the percentage of cells in S phase and G2/M decreased compared to that of control groups (P<0.05). Conclusion After the inhibition of SOCS1 gene expression, the proliferation ability of human pancreatic cancer cell line PANC1 decreased, and the sensitivity of PANC1 cells to IFN-γwas enhanced.