Triptolide is a diterpene triepoxide isolated for the first time from the medicinal plant Tripterygium wilfordii, exhibiting immunosuppressive, anti-inflammatory, anti-proliferative, and antitumor effects. It acts as an inhibitor of NF-κB activation, where NF-κB is a family of transcription factor protein complexes[1]. Triptolide possesses broad-spectrum anticancer activity, inhibiting the development of colon cancer, breast cancer, renal cell carcinoma, and cervical cancer[2].
In vitro, triptolide (50 nM, 72 h) significantly inhibits the proliferation of ovarian cancer cells SKOV3 and A2780. Triptolide (15 nM, 48h) significantly inhibits cell migration and blocks the invasive capability of cells[2]. Triptolide (50-200 nmol/L) incubated with PANC-1 and MiaPaCa-2 cells significantly reduces cell viability without affecting the viability of normal pancreatic ductal cells[3]. The IC50 value of triptolide on RSF cell viability is 74.3 nM, and its IC50 value on RSF cell proliferation is 20.4 nM[4]. Triptolide (0-150 nM) significantly inhibits the viability of HK1, FaDu, and C666-1 cells in a dose- and time-dependent manner[5].
In vivo, treatment with triptolide (1 mg/kg/d, p.o.) for three weeks in nude mice reduced the number of metastatic nodules by approximately 80%[2]. Triptolide (0.2 mg/kg/d) administered to mice with transplanted pancreatic tumors for 60 days reduced pancreatic cancer growth and significantly decreased local tumor spread[3].
References:
[1] Zhang W, et al. Triptolide Combined with Radiotherapy for the Treatment of Nasopharyngeal Carcinoma via NF-κB-Related Mechanism. Int J Mol Sci. 2016 Dec 19;17(12).
[2] Zhao H, Yang Z, Wang X, et al. Triptolide inhibits ovarian cancer cell invasion by repression of matrix metalloproteinase 7 and 19 and upregulation of E-cadherin[J]. Experimental & molecular medicine, 2012, 44(11): 633-641.
[3] Phillips P A , Dudeja V , Mccarroll J A ,et al.Triptolide Induces Pancreatic Cancer Cell Death via Inhibition of Heat Shock Protein 70[J].Cancer Research, 2007, 67(19):9407.
[4] Kusunoki N, Yamazaki R, Kitasato H, Beppu M, Aoki H, Kawai S: Triptolide, an active compound identified in a traditional Chinese herb, induces apoptosis of rheumatoid synovial fibroblasts. BMC Pharmacol 2004, 4:2.
[5] Cai J, et al. Natural product triptolide induces GSDME-mediated pyroptosis in head and neck cancer through suppressing mitochondrial hexokinase-ΙΙ. J Exp Clin Cancer Res. 2021;40(1):190. Published 2021 Jun 9.
雷公藤甲素(Triptolide)是一种二萜三环氧化物,首次从药用植物雷公藤 (Tripterygium wilfordii) 中分离出来,具有免疫抑制,抗炎,抗增殖和抗肿瘤作用。雷公藤甲素是 NF-κB 活化的抑制剂,NF-κB是转录因子蛋白复合物家族[1]。雷公藤甲素具有广谱抗癌活性,它可以抑制结肠癌、乳腺癌、肾细胞癌和宫颈癌的发生过程[2]。
在体外,雷公藤甲素(50 nM,72 h)显著抑制卵巢癌细胞SKOV 3和A2780的增殖。雷公藤甲素(15 nM,48h)显著抑制细胞迁移,还可阻断细胞的侵袭能力[2]。雷公藤甲素(50-200 nmol/L)与PANC-1 和 MiaPaCa-2 细胞一起孵育,显着降低细胞活力,但对正常胰腺导管细胞活力没有影响[3]。雷公藤甲素对RSF细胞活力的IC50值为74.3 nM,雷公藤甲素对RSF细胞增殖的IC50值为20.4nM[4]。雷公藤甲素(0-150 nM)以剂量和时间依赖性方式显著抑制HK 1、FaDu、C666-1细胞的活力[5]。
在体内,雷公藤甲素(1 mg/kg/d,p.o.)处理三周的裸鼠中,转移结节的数量减少了约 80%[2]。雷公藤甲素(0.2 mg/kg/d)对移植胰腺肿瘤的小鼠治疗60天可减少胰腺癌的生长,并显着减少局部肿瘤扩散[3]。