College of Pharmacy, Chungbuk National University, Cheongju, North Chungcheong 28160, Republic of Korea.
College of Pharmacy, Keimyung University, Daegu 704‑701, Republic of Korea.
Int J Mol Med. 2017 Nov;40(5):1566-1572. doi: 10.3892/ijmm.2017.3122. Epub 2017 Sep 6.
Triptolide, an active component extracted from the medicinal plant Tripterygium wilfordii Hook F., has been used to treat various diseases, including lupus, cancer, rheumatoid arthritis and nephritic syndrome. The present study investigated the effects of triptolide on multiple myeloma using western blotting and an electrophoretic mobility shift assay. Triptolide was found to suppress the inducible and constitutive activation of signal transducer and activator of transcription 3 (STAT3), which is closely associated with inflammation and tumorigenesis. Triptolide also inhibited the DNA binding of STAT3. This correlated with the downregulation of Src kinase and Janus kinase 1 and 2, and with the upregulation of protein tyrosine phosphatase non‑receptor type 6 (also known as SHP‑1). In addition, triptolide downregulated the expression of the STAT3‑regulated antiapoptotic (Bcl‑xL and myeloid cell leukemia‑1), proliferative (cyclin D1), and angiogenic (vascular endothelial growth factor) genes, suggesting that triptolide can induce apoptosis of tumor cells. These results suggest that triptolide may be a potential therapeutic anticancer agent for the prevention and treatment of multiple myeloma; thus further in‑depth investigations into its efficacy and toxicity are warranted.
雷公藤红素是从药用植物雷公藤（Tripterygium wilfordii Hook F.）中提取的一种活性成分，已被用于治疗多种疾病，包括狼疮、癌症、类风湿关节炎和肾病综合征。本研究采用 Western blot 和电泳迁移率变动分析研究了雷公藤红素对多发性骨髓瘤的作用。研究发现，雷公藤红素可抑制信号转导和转录激活因子 3（STAT3）的诱导性和组成性激活，而 STAT3 与炎症和肿瘤发生密切相关。雷公藤红素还抑制 STAT3 的 DNA 结合。这与 Src 激酶和 Janus 激酶 1 和 2 的下调以及蛋白酪氨酸磷酸酶非受体型 6（也称为 SHP-1）的上调相关。此外，雷公藤红素下调了 STAT3 调节的抗凋亡（Bcl-xL 和髓样细胞白血病-1）、增殖（细胞周期蛋白 D1）和血管生成（血管内皮生长因子）基因的表达，提示雷公藤红素可诱导肿瘤细胞凋亡。这些结果表明，雷公藤红素可能是预防和治疗多发性骨髓瘤的一种潜在的治疗性抗癌药物；因此，有必要进一步深入研究其疗效和毒性。
