OBJECTIVETo investigate the effect of ginsenoside-Rg3 on lung metastasis of ribonuclease inhibitor (RI) gene-transfected mouse B16 melanoma.METHODSC57BL/6 mice were iv injected with parental or RI-transfected B16 melanoma cells. Lung metastasis was assessed by the number of surface tumor nodules. Mice were divided into 6 groups. Group I, II and III of mice were given parental, mock-transfected and RI-transfected B16 melanoma cells, respectively while in group IV, V and VI, Rg3 (1.5 mg/kg, iv q.o.d. x 10) was given to mice bearing parental, mock-transfected and RI-transfected B16 melanoma, respectively. Micovessel density (MVD) of the lung metastatic tumor was assessed by immunohistochemical staining of factor VIII-R expression.RESULTSThe number of tumor nodules was significantly decreased in mice injected with RI-transfected B16 melanoma (Gp III, compared to Gp I and II). Rg3 treatment per se could also decrease the number of lung tumor nodules but to a lesser extent (Gp IV and V compared to Gp III). However, Rg3 synergized with RI transfection resulting in most significant inhibition of lung metastasis (Gp VI). Mice in Gp I and II died within 26 days of the experiment, whereas all the mice in Gp VI were alive during the observation period of one and one half month. MVD was significantly decreased in the lung tumor nodules in mice injected with RI-transfected B16 melanoma. It was further decreased when additional Rg3 was given (Gp VI).CONCLUSIONTransfection of ribonuclease inhibitor gene significantly reduces the metastatic potential of B16 melanoma. Ginsenoside-Rg3 has a synergistic effect.

International Journal of Molecular Sciences

Identification of Ribonuclease Inhibitors for the Control of Pathogenic Bacteria

Article

作者: Fishwick, Colin W. G. ; Simmons, Katie J. ; McDowall, Kenneth J. ; Matos, Rute G. ; Arraiano, Cecília M.

Bacteria are known to be constantly adapting to become resistant to antibiotics. Currently, efficient antibacterial compounds are still available; however, it is only a matter of time until these compounds also become inefficient. Ribonucleases are the enzymes responsible for the maturation and degradation of RNA molecules, and many of them are essential for microbial survival. Members of the PNPase and RNase II families of exoribonucleases have been implicated in virulence in many pathogens and, as such, are valid targets for the development of new antibacterials. In this paper, we describe the use of virtual high-throughput screening (vHTS) to identify chemical compounds predicted to bind to the active sites within the known structures of RNase II and PNPase from Escherichia coli. The subsequent in vitro screening identified compounds that inhibited the activity of these exoribonucleases, with some also affecting cell viability, thereby providing proof of principle for utilizing the known structures of these enzymes in the pursuit of new antibacterials.

100 项与 Ribonuclease H function inhibitor(Université De Lille) 相关的药物交易

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