Department of Microbiology, Faculty of Medicine, Khon Kaen University, Khon Kaen 40002, Thailand.
HPV & EBV and Carcinogenesis Research (HEC) Group, Khon Kaen University, Khon Kaen 40002, Thailand.
Int J Mol Sci. 2021 Jun 24;22(13):6806. doi: 10.3390/ijms22136806.
Regardless of the prophylactic vaccine accessibility, persistent infections of high-risk human papillomaviruses (hr-HPVs), recognized as an etiology of cervical cancers, continues to represent a major health problem for the world population. An overexpression of viral early protein 6 (E6) is linked to carcinogenesis. E6 induces anti-apoptosis by degrading tumor suppressor proteins p53 (p53) via E6-E6-associated protein (E6AP)-mediated polyubiquitination. Thus, the restoration of apoptosis by interfering with the E6 function has been proposed as a selective medicinal strategy. This study aimed to determine the activities of andrographolide (Androg) on the disturbance of E6-mediated p53 degradation in cervical cancer cell lines using a proteomic approach. These results demonstrated that Androg could restore the intracellular p53 level, leading to apoptosis-induced cell death in HPV16-positive cervical cancer cell lines, SiHa and CaSki. Mechanistically, the anti-tumor activity of Androg essentially relied on the reduction in host cell proteins, which are associated with ubiquitin-mediated proteolysis pathways, particularly HERC4 and SMURF2. They are gradually suppressed in Androg-treated HPV16-positive cervical cancer cells. Collectively, the restoration of p53 in HPV16-positive cervical cancer cells might be achieved by disruption of E3 ubiquitin ligase activity by Androg, which could be an alternative treatment for HPV-associated epithelial lesions.
尽管预防性疫苗具有可及性,但高危型人乳头瘤病毒(hr-HPV)的持续感染仍然是全球人口的一个主要健康问题,这些病毒被认为是宫颈癌的病因。病毒早期蛋白 6(E6)的过表达与致癌作用有关。E6 通过 E6-E6 相关蛋白(E6AP)介导的多泛素化降解肿瘤抑制蛋白 p53(p53),诱导细胞抗凋亡。因此,通过干扰 E6 功能恢复细胞凋亡已被提议作为一种选择性的药物治疗策略。本研究旨在采用蛋白质组学方法确定穿心莲内酯(Androg)对宫颈癌细胞系中 E6 介导的 p53 降解干扰的作用。这些结果表明,Androg 可以恢复细胞内 p53 水平,导致 HPV16 阳性宫颈癌细胞系 SiHa 和 CaSki 发生凋亡诱导的细胞死亡。从机制上讲,Androg 的抗肿瘤活性主要依赖于宿主细胞蛋白的减少,这些蛋白与泛素介导的蛋白水解途径有关,特别是 HERC4 和 SMURF2。在 Androg 处理的 HPV16 阳性宫颈癌细胞中,它们逐渐受到抑制。总之,通过 Androg 破坏 E3 泛素连接酶活性,可能在 HPV16 阳性宫颈癌细胞中恢复 p53,这可能是 HPV 相关上皮病变的一种替代治疗方法。