Sucipto Teguh H, Martak Fahimah
Dengue Study Group, Institute of Tropical Disease, Universitas Airlangga, Jl. Mulyorejo, Surabaya, East Java.
Department of Chemistry, Faculty of Science, Institut Teknologi Sepuluh Nopember, Jl. Raya ITS, Surabaya, East Java, Indonesia.
Infect Dis Rep. 2020 Jul 7;12(Suppl 1):8744. doi: 10.4081/idr.2020.8744.
Dengue fever and dengue hemorrhagic fever are transmitted to humans by the and mosquitoes, with an observed 30-fold increase in global incidence the last 50 years. Despite the tremendous efforts invested anti-dengue virus research, no clinically approved vaccine or antiviral chemotherapeutics are available for humans, and disease treatment is limited to supportive care. Over the years there has been a continuous interest in the chemistry of metal complexes with biological activity, including platinum complexes with antitumor activity and silver complexes with antimicrobial action. Aim of the project was to investigate [Cu(2,4,5-triphenyl-1imidazole) (HO)].Cl as antiviral compound that was further tested for inhibitory effect on the replication of dengue virus type 2 (DENV-2) in Vero cell. DENV-2 were infected in Vero cells and replication of virus was measured by Viral ToxGlo with selectivity index value (SI) and determined as the ratio of cytotoxic concentration 50 (CC) to inhibitory concentration 50 (IC) for compound. The standard curve between concentration of compound (μg/mL) and %viability of cells was analyzed by logarithmic correlation regression with regression equation. For infection rates, t-test was used to examine the statistical significances among the concentrations of compound. P<0.05 was considered to be significant. The maximum inhibitory concentration (IC) of [Cu(2,4,5- triphenyl-1-imidazole) (HO)].Cl against DENV-2 was 98.62 μg/mL. The cytotoxic concentration (CC) of compound against Vero cells was 300.36μg/mL. The SI values for [Cu(2,4,5-triphenyl-1-imidazole) (HO)].Cl 1.86.Based on selectivity index values, [Cu(2,4,5-triphenyl-1-imidazole) (HO)].Cl can inhibit the growth of DENV- 2 and has low toxicity values for Vero cells.
登革热和登革出血热通过伊蚊和埃及伊蚊传播给人类,在过去50年中全球发病率增长了30倍。尽管在抗登革病毒研究方面投入了巨大努力,但目前尚无临床批准的用于人类的疫苗或抗病毒化学疗法,疾病治疗仅限于支持性护理。多年来,人们一直对具有生物活性的金属配合物的化学性质感兴趣,包括具有抗肿瘤活性的铂配合物和具有抗菌作用的银配合物。该项目的目的是研究[Cu(2,4,5-三苯基-1-咪唑)(HO)].Cl作为抗病毒化合物,并进一步测试其对2型登革病毒(DENV-2)在Vero细胞中复制的抑制作用。DENV-2在Vero细胞中感染,病毒复制通过Viral ToxGlo测定,具有选择性指数值(SI),并确定为化合物细胞毒性浓度50(CC)与抑制浓度50(IC)的比值。通过对数相关回归和回归方程分析化合物浓度(μg/mL)与细胞活力百分比之间的标准曲线。对于感染率,使用t检验来检查化合物浓度之间的统计学意义。P<0.05被认为具有显著性。[Cu(2,4,5-三苯基-1-咪唑)(HO)].Cl对DENV-2的最大抑制浓度(IC)为98.62μg/mL。该化合物对Vero细胞的细胞毒性浓度(CC)为300.36μg/mL。[Cu(2,4,5-三苯基-1-咪唑)(HO)].Cl的SI值为1.86。基于选择性指数值,[Cu(2,4,5-三苯基-1-咪唑)(HO)].Cl可以抑制DENV-2生长,并且对Vero细胞具有低毒性值。