Sang Yazhou, Hu Yue, Zhang Yueyue, Chen Luyi, Lu Yutian, Gao Lin, Lu Yunyun, Cao Xuan, Zhang Yaqiong, Chen Guofu
Department of General Surgery, Affiliated Wenling First People's Hospital, Taizhou University, Taizhou, 318000, Zhejiang, China; School of Basic Medicine, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, Hubei, China.
Department of General Surgery, Affiliated Wenling First People's Hospital, Taizhou University, Taizhou, 318000, Zhejiang, China; Department of Basic Medicine, School of Medicine, Taizhou University, Taizhou, 318000, Zhejiang, China.
J Ethnopharmacol. 2025 Feb 10;338(Pt 2):119071. doi: 10.1016/j.jep.2024.119071. Epub 2024 Nov 9.
Tripterygium wilfordii Hook. f. (TW) is extensively utilized in clinical practice for its effective anti-inflammatory and anti-cancer properties.
This study aims to elucidate the processes of TW in combating prostate cancer through a comprehensive strategy that integrates network pharmacology, molecular docking and molecular biology validation.
A drug-target network and protein-protein interaction network were constructed established to predict the potential targets of TW for prostate cancer treatment. The interaction between active components and targets was confirmed using molecular docking. Moreover, prostate cancer cells were used to examine the anti-tumor effects of active ingredients in vitro. The xenograft animal model was constructed to evaluate the anti-tumor effect of triptonoterpene in vivo.
Twenty-nine active components interact with 226 corresponding targets, and 112 disease targets specifically related with prostate cancer were identified. The primary targets (AKT1, TP53, RELA) were chosen, and kaempferol, triptolide, and triptonoterpene exhibited probable binding affinity with these targets, respectively. Triptonoterpene was subsequently confirmed to inhibit the growth of prostate cancer cells and induce apoptosis in vitro and in vivo.
Overall, this study demonstrated that TW may serve as a viable therapeutic agent for prostate cancer. Triptonoterpene is a specific inhibitor of p-AKT1 and p65, making it an attractive contender for prostate cancer therapy.
雷公藤（Tripterygium wilfordii Hook. f.，TW）因其有效的抗炎和抗癌特性而在临床实践中被广泛应用。
本研究旨在通过整合网络药理学、分子对接和分子生物学验证的综合策略，阐明雷公藤治疗前列腺癌的作用机制。
构建药物-靶点网络和蛋白质-蛋白质相互作用网络，以预测雷公藤治疗前列腺癌的潜在靶点。通过分子对接确认活性成分与靶点之间的相互作用。此外，利用前列腺癌细胞在体外检测活性成分的抗肿瘤作用。构建异种移植动物模型以评估雷公藤红素在体内的抗肿瘤作用。
29种活性成分与226个相应靶点相互作用，鉴定出112个与前列腺癌特异性相关的疾病靶点。选择主要靶点（AKT1、TP53、RELA），山奈酚、雷公藤甲素和雷公藤红素分别与这些靶点表现出可能的结合亲和力。随后证实雷公藤红素在体外和体内均能抑制前列腺癌细胞的生长并诱导其凋亡。
总体而言，本研究表明雷公藤可能是一种可行的前列腺癌治疗药物。雷公藤红素是p-AKT1和p65的特异性抑制剂，使其成为前列腺癌治疗的一个有吸引力的候选药物。
