Liang Kai, Pan Xinwei, Chen Yumei, Huang Shaode
Department of Pharmacy, Guangxi Medical University Cancer Hospital, No. 71 Hedi Road, Qingxiu District, Guangxi, Nanning, People's Republic of China.
Maternal and Child Health Hospital of Guangxi Zhuang Autonomous Region, Nanning, People's Republic of China.
Naunyn Schmiedebergs Arch Pharmacol. 2023 Jun;396(6):1205-1210. doi: 10.1007/s00210-023-02393-w. Epub 2023 Jan 24.
Ovarian cancer is a gynecological malignancy characterized with increasing death rate in the world. It is clinically reported that chemotherapy against ovarian cancer is still found with poor curative effect and potential side effect. Plumbagin is an emerging anti-cancer compound. Although some experimental findings of plumbagin anti-ovarian cancer activity are described, the pharmacological targets should be further explored. In this study, we aimed to investigate the underlying pharmacological activities and targets of plumbagin against ovarian cancer in vitro. As results, in silico docking analysis suggested plumbagin potently treating ovarian cancer through regulating pharmacological targets, including octamer-binding transcription factor 4 (OCT4) and Kruppel-like factor 4 (KLF4). The preliminary experimental data showed that plumbagin treatment inhibited cell growth and induced apoptosis in cancer cells. In addition, decreased mRNA expressions of intracellular OCT4, PCNA, and elevated KLF4 mRNA activation were detected in plumbagin-treated cancer cells. Furthermore, immunostaining determination showed reduced OCT4-positive cells and increased KLF4-positive cells were observed following plumbagin treatments. To sum up, our current findings have preliminarily showed the anti-ovarian cancer benefits of plumbagin, and the pharmacological targets may be identified as KLF4 and OCT4 pathway. Thus, we conclude that plumbagin may be a bioactive compound for ovarian cancer treatment.
卵巢癌是一种妇科恶性肿瘤,其死亡率在全球呈上升趋势。临床报告显示,针对卵巢癌的化疗疗效仍较差且存在潜在副作用。白花丹醌是一种新兴的抗癌化合物。尽管已有一些关于白花丹醌抗卵巢癌活性的实验结果描述,但仍需进一步探索其药理学靶点。在本研究中,我们旨在体外研究白花丹醌抗卵巢癌的潜在药理活性和靶点。结果表明,计算机对接分析提示白花丹醌可通过调节包括八聚体结合转录因子4(OCT4)和 Kruppel样因子4(KLF4)在内的药理学靶点有效治疗卵巢癌。初步实验数据显示,白花丹醌处理可抑制癌细胞生长并诱导其凋亡。此外,在白花丹醌处理的癌细胞中检测到细胞内OCT4、PCNA的mRNA表达降低,而KLF4 mRNA激活升高。此外,免疫染色测定显示,白花丹醌处理后,OCT4阳性细胞减少,KLF4阳性细胞增加。综上所述,我们目前的研究结果初步显示了白花丹醌对卵巢癌的有益作用,其药理学靶点可能为KLF4和OCT4通路。因此,我们得出结论,白花丹醌可能是一种用于治疗卵巢癌的生物活性化合物。