Hidayatullah Arief, Widiastuti Diana, Putra Wira Eka, Rifa'i Muhaimin, Heikal Muhammad Fikri
Democratic Governance and Poverty Reduction Unit, United Nations Development Programme, Eijkman-RSCM Building, Jl. Diponegoro 69, 10430 Jakarta, Indonesia.
Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Pakuan, Jl. Pakuan, RT.02/RW.06, 16129 Tegallega, Bogor, West Java, Indonesia.
Trop Life Sci Res. 2025 Mar;36(1):1-24. doi: 10.21315/tlsr2025.36.1.1. Epub 2025 Mar 30.
Infection of keratinocytes by high-risk human papillomavirus (HPV) strains, notably HPV16, is responsible for the onset of cervical cancer. The E6 protein serves as a pivotal oncoprotein implicated in the progression of cancer. We utilised a virtual screening method to identify bioactive compounds in a variety of commonly used medicinal plants in Indonesia. All the top five compounds bind to a single binding site on the E6 major hydrophobic groove, which corresponds to the binding site for the E6AP and IRF3's LxxLL motifs. They are expected to function as competitive inhibitors, inhibiting the development of the E6-E6AP and E6-IRF3 complexes, which limit p53 degradation and therefore cell proliferation, thus preserving the innate immune response to HPV16 infection. Asarinin and thiazolo[3,2-a]benzimidazole-3(2H)-one,2-(2-fluorobenzylideno)-7,8-dimethyl were predicted to be the most effective compounds in this research owing to their strong affinity for and persistent interactions with the E6 major hydrophobic groove, particularly in comparison to pharmacological controls.
高危型人乳头瘤病毒(HPV)毒株,尤其是HPV16感染角质形成细胞,是宫颈癌发病的原因。E6蛋白是一种关键的癌蛋白,与癌症进展有关。我们利用虚拟筛选方法,在印度尼西亚多种常用药用植物中鉴定生物活性化合物。所有排名前五的化合物都结合到E6主要疏水凹槽上的单个结合位点,该位点对应于E6相关蛋白(E6AP)和干扰素调节因子3(IRF3)的LxxLL基序的结合位点。它们有望作为竞争性抑制剂,抑制E6-E6AP和E6-IRF3复合物的形成,这些复合物限制了p53的降解,从而限制了细胞增殖,从而保留对HPV16感染的先天免疫反应。由于与E6主要疏水凹槽具有很强的亲和力和持续的相互作用,尤其是与药理对照相比,细辛脂素和噻唑并[3,2-a]苯并咪唑-3(2H)-酮,2-(2-氟亚苄基)-7,8-二甲基预计是本研究中最有效的化合物。