Triptolide (PG490) belongs to the tricyclic diterpenoid group of natural products and is an inhibitor of NF-κB activation. Triptolide exhibits immunosuppressive, anti-rheumatic, anti-inflammatory, anti-proliferative and anti-tumor activities.

MDM2-p53:47-73 nM (IC50)

METHODS: Neuroblastoma cells BE(2)-C were treated with Triptolide (5-100 nM) for 24 h. Cell viability was measured using the CCK-8 Assay.
RESULTS: A concentration-dependent response to Triptolide was observed in BE(2)-C cells. At 50 nM Triptolide, cell viability was significantly reduced to 50%. [1]
METHODS: Breast cancer cells MCF-7 were treated with Triptolide (10-50 nmol/L) for 24 h, and the expression levels of target proteins were detected using Western Blot.
RESULTS: Triptolide decreased the messenger RNA and protein levels of ERα in MCF-7 cells in a dose-dependent manner. [2]

METHODS: To assay antitumor activity in vivo, Triptolide (0.4 mg/kg) was administered by gavage to BALB/c-nu+/nu+ mice harboring the breast cancer tumor MCF-7 once daily for three weeks.
RESULTS: Triptolide inhibited the growth of MCF-7 cell xenografts in a mouse model. [2]
METHODS: To investigate the effects on ulcerative colitis (UC), Triptolide (0.1-0.4 mg/kg) was administered orally to DSS-induced UC mice once daily for seven days.
RESULTS: Triptolide has anti-inflammatory and therapeutic effects on UC mice. [3]

Triptolide is dissolved in DMSO (1 mg/mL) and stored, and then diluted with RPMI 1640 medium before use[3]. The viability of differentiated PC12 cells treated with different concentrations of Triptolide. After differentiated PC12 cells are cultured on 96-well plates with RPMI 1640 medium for stabilization, differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) for 24 hours. The concentrations in this study are chosen. Then cell viability is determined by the MTT assay. Each condition and experiment is repeated three times[3].