Wogonin (Vogonin) is a cell-permeable and orally available flavonoid that displays anti-inflammatory and anticancer properties.

Wogonin inhibits PMA-induced COX-2 gene expression by inhibiting c-Jun expression and AP-1 activation in A549 cells[1]. Wogonin is an inhibitor of cyclin-dependent kinase 9 (CDK9) and block phosphorylation of the carboxy-terminal domain of RNA polymerase II at Ser. Thus, it reduces RNA synthesis and subsequently rapid downregulation of the short-lived anti-apoptotic protein myeloid cell leukemia 1 (Mcl-1) resulting in apoptosis induction in cancer cells. Wogonin directly binds to CDK9, presumably to the ATP-binding pocketa and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity. Wogonin preferentially inhibits CDK9 in malignant compared with normal lymphocytes. Wogonin is a also potent anti-oxidant capable to scavenge ?O2? [2]. Wogonin significantly inhibits the translocation of NFATc1 from the cytoplasm to the nucleus and its transcriptional activation activity. It also significantly inhibits osteoclast differentiation and decreases the transcription of osteoclast?associated immunoglobulin?like receptor, tartrate?resistant acid phosphatase and calcitonin receptor[4]. Wogonin Inhibits N-acetyltransferase Activity[5].

Wogonin suppresses growth of human cancer xenografts in vivo. At doses lethal to tumor cells, wogonin shows no or little toxicity for normal cells and had also no obvious toxicity in animals[2]. Wogonin could induce apoptosis in murine sarcoma S180 thereby inhibiting the tumor growth both in vitro and in vivo[3]. An intraperitoneal injection of 200 mg/kg Wogonin could completely inhibit leukemia and CEM cells[4].

A549 cells are culture in 24-well plate (1.2×105 cells/well) 1 day before wogonin treatment. DMSO or wogonin is added into A549 cells 1 h before PMA stimulation, and cells are incubated for another 6 h. Cells are collected by trypsin treatment and cell numbers are counted by using a hemocytometer and trypan blue exclusion method.(Only for Reference)