School of Pharmacy, China Medical University, Taichung 40402, Taiwan, R.O.C.
Department of Medical Laboratory Science and Biotechnology, China Medical University, Taichung 40402, Taiwan, R.O.C.
Int J Mol Med. 2019 May;43(5):2024-2032. doi: 10.3892/ijmm.2019.4113. Epub 2019 Feb 27.
In a previous study from our group, a novel compound, namely CW‑33 (ethyl 2‑(3',5'‑dimethylanilino)‑4‑oxo‑4,5‑dihydrofuran‑3‑carboxylate) was identified that exhibited antiviral activity for Japanese encephalitis virus (JEV). The viral NS2B‑NS3 serine protease serves an important role in cytoplasmic cleavage events that occur during viral polyprotein maturation. The inhibition of viral RNA and protein syntheses was responsible for the antiviral activities of the novel furanonaphthoquinone derivatives that were discovered for the prevention of JEV infection. Consequently, the present study examined the molecular docking simulation of JEV protease with compound CW‑33 and its analogues, and developed quantitative structure‑activity relationship (QSAR) models to assess the potential antiviral activities of these compounds with regard to JEV. Molecular docking simulation indicated the potential ligand‑protein interactions associated with the antiviral activities of these compounds. According to the results of the QSAR models, the secondary amine group was an important moiety required for compound bioactivity, which enabled the formation of hydrogen bonding with the residue Glu155. Furthermore, the aromatic ring mapping of the phenyl moiety of each compound was predicted to form a π‑cation interaction with residue Arg76, whereas the hydrophobic feature represented by the ethyl moiety exhibited hydrophobic contacts with residue Glu74. Finally, the hydrophobic substituents in the meta‑position of the phenyl ring further contributed to the efficacy of the antiviral activity. These results unravel the structural characteristics that are required for binding of CW‑33 to the JEV protease and can be used for potential therapeutic and drug development purposes for JEV.
在我们小组的一项先前研究中,发现了一种新型化合物,即 CW-33(乙基 2-(3',5'-二甲基苯胺基)-4-氧代-4,5-二氢呋喃-3-羧酸酯),该化合物对乙型脑炎病毒(JEV)具有抗病毒活性。病毒 NS2B-NS3 丝氨酸蛋白酶在病毒多蛋白成熟过程中发生的细胞质切割事件中起重要作用。新型呋喃萘醌衍生物的抗病毒活性归因于抑制病毒 RNA 和蛋白质合成,这些衍生物可用于预防 JEV 感染。因此,本研究对 JEV 蛋白酶与化合物 CW-33 及其类似物进行了分子对接模拟,并建立了定量构效关系(QSAR)模型,以评估这些化合物预防 JEV 的潜在抗病毒活性。分子对接模拟表明了与这些化合物抗病毒活性相关的潜在配体-蛋白相互作用。根据 QSAR 模型的结果,仲胺基团是化合物生物活性所必需的重要部分,它能够与残基 Glu155 形成氢键。此外,每个化合物苯环上的芳基部分被预测与残基 Arg76 形成π-阳离子相互作用,而由乙基部分代表的疏水性特征与残基 Glu74 表现出疏水性接触。最后,苯环间位的疏水性取代基进一步增强了抗病毒活性的功效。这些结果揭示了 CW-33 与 JEV 蛋白酶结合所需的结构特征,可用于 JEV 的潜在治疗和药物开发目的。