Cytotoxic and antitumour activity of scopadulcic acid from Scoparia dulcis L.

Scopadulcic acid B is a diterpenoid recently isolated from Scoparia dulcis L. This compound showed greater cytotoxicity against cell lines derived from tumour tissues with a 50% inhibitory concentration (IC50) of 0.068–0.076 μg/mL, compared with cell lines from normal tissues with an IC50 of 0.097–0.245 μg/mL. The in vivo antitumour activity of scopadulcic acid B was determined using mice inoculated with Ehrlich ascites tumour cells. Oral administration of the compound at doses of 25 or 100 mg/kg/day prolonged the median survival time of the animals. However, when administered intraperitoneally to mice at doses of 25, 50 or 100 mg/kg/day, scopadulcic acid B increased the survival rate by 12.5%, 12.5% and 25%, respectively, without weight change over the treatment period.

[1]  Y. Tezuka,et al.  Scopadulcic acid B, a new tetracyclic diterpenoid from Scoparia dulcis L. Its structure, H+, K(+)-adenosine triphosphatase inhibitory activity and pharmacokinetic behaviour in rats. , 1990, Chemical & pharmaceutical bulletin.

[2]  H. Ochiai,et al.  In vitro and in vivo antiviral activity of scopadulcic acid B from Scoparia dulcis, Scrophulariaceae, against herpes simplex virus type 1. , 1988, Antiviral research.

[3]  Toshimitsu Hayashi,et al.  Scopadulcic acid-A and -B, new diterpenoids with a novel skeleton, from a Paraguayan crude drug “typychá kuratũ” (scoparia dulcis L.) , 1987 .

[4]  Y. Nishiyama,et al.  Characterization of an aphidicolin-resistant mutant of herpes simplex virus type 2 which induces an altered viral DNA polymerase. , 1984, Virology.

[5]  S. Yoshida,et al.  Effects of DNA polymerase inhibitors on replicative and repair DNA synthesis in ultraviolet-irradiated HeLa cells. , 1982, International journal of radiation biology and related studies in physics, chemistry, and medicine.

[6]  S. Spadari,et al.  Mechanism of inhibition of herpes simplex virus and vaccinia virus DNA polymerases by aphidicolin, a highly specific inhibitor of DNA replication in eucaryotes , 1980, Journal of virology.

[7]  R. Diasio,et al.  Metabolism and biological activity of 5'-deoxy-5-fluorouridine, a novel fluoropyrimidine. , 1980, Cancer research.

[8]  S. Spadari,et al.  Effect of aphidicolin on viral and human DNA polymerases. , 1979, Biochemical and biophysical research communications.

[9]  T. Taguchi,et al.  Aphidicolin prevents mitotic cell division by interfering with the activity of DNA polymerase-α , 1978, Nature.

[10]  T. Taguchi,et al.  Aphidicolin: a specific inhibitor of DNA polymerases in the cytosol of rat liver. , 1978, Biochemical and biophysical research communications.

[11]  G. Henle,et al.  The establishment of strains of human cells in tissue culture. , 1957, Journal of immunology.

[12]  J. Fogh,et al.  Continuous Cultivation of Epithelial Cell Strain (FL) from Human Amniotic Membrane.∗ , 1957, Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine.

[13]  T. Puck,et al.  Clonal growth of mammalian cells in vitro; growth characteristics of colonies from single HeLa cells with and without a feeder layer. , 1956 .

[14]  H. Toolan,et al.  Culture characteristics of four permanent lines of human cancer cells. , 1955, Cancer research.

[15]  Chang Rs Continuous subcultivation of epithelial-like cells from normal human tissues. , 1954 .