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Oridonin, a diterpenoid isolated from Rabdo-sia rubescens (Hemsl.) Hara, has been proved to possess remarkable anticancer activity, in addition to its potential in antiinflammation and antibacteria. The purpose of this article is to review current progress in oridonin conceed about a relationship between the chemical structure/modifications and its anticancer activity and to discuss the molecular mechanisms underlying its anticancer activity, such as suppression of tumor proliferation and induction of tumor cell death, and the cell signal transduction in anticancer activity of oridonin.