Triptolide是从雷公藤根中提取的一种二萜类三环氧化物，它是NF-Κb活化的抑制剂，具有免疫抑制，抗炎，抗增殖和抗肿瘤作用。

Triptolide is a diterpenes trioxide, immunosuppressive agent extracted from the Chinese herb Tripterygium wilfordii.

在小鼠体内,Triptolide可抑制B16F10细胞转移到脾脏和肺中.在小鼠模型中,Triptolide具有体内外抗多囊性肾病的作用.LD50（小鼠）: 0.83 mg/kg,i.v.Triptolide与环孢素A对动物模型中移植物的存活具有协同促进作用,且协同抑制同种异体骨髓移植伴随的移植物抗宿主病.且经抑制c-IAP2和c-IAP1的诱导作用,它可造成肿瘤细胞的细胞凋亡,同时部分增强TNF-α)诱导的细胞凋亡.Triptolide处理14-21天抑制由B16黑色素瘤、MDA-435乳腺癌、TSU膀胱癌及MGC80-3胃癌形成的异种移植物的生长,这表明TPL有广谱抗肿瘤作用,对野生型和突变体p53均具有效.

Triptolide可抑制胃癌,乳腺癌和白血病细胞系HL-60细胞活性。在肿瘤细胞中,Triptolide通过阻断NF-κB激活并增加肿瘤细胞对TNF-α诱导的程序性细胞死亡的敏感性,从而诱导细胞凋亡。在嘌呤盒/核因子和NF-κB介导的转录激活水平,Triptolide可抑制激活T细胞中的IL-2表达。Triptolide在(2–10ng/ml)可抑制肿瘤细胞增殖与集落形成。

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].

38748-32-2

C20H24O6

360.406

雷公藤甲素;PG490;NSC 163062

DMSO:7.2 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years