1 Department of Molecular Medicine, University of Malaya , Kuala Lumpur, Malaysia .
OMICS. 2013 Nov;17(11):560-7. doi: 10.1089/omi.2013.0056. Epub 2013 Sep 17.
Dengue virus infects millions of people worldwide, and there is no vaccine or anti-dengue therapeutic available. Antimicrobial peptides have been shown to possess effective antiviral activity against various viruses. One of the main limitations of developing these peptides as potent antiviral drugs is the high cost of production. In this study, high yield production of biologically active plectasin peptide was inexpensively achieved by producing tandem plectasin peptides as inclusion bodies in E. coli. Antiviral activity of the recombinant peptide towards dengue serotype-2 NS2B-NS3 protease (DENV2 NS2B-NS3pro) was assessed as a target to inhibit dengue virus replication in Vero cells. Single units of recombinant plectasin were collected after applying consecutive steps of refolding, cleaving by Factor Xa, and nickel column purification to obtain recombinant proteins of high purity. The maximal nontoxic dose (MNTD) of the recombinant peptide against Vero cells was 20 μM (100 μg/mL). The reaction velocity of DENV2 NS2B-NS3pro decreased significantly after increasing concentrations of recombinant plectasin were applied to the reaction mixture. Plectasin peptide noncompetitively inhibited DENV2 NS2B-NS3pro at Ki value of 5.03 ± 0.98 μM. The percentage of viral inhibition was more than 80% at the MNTD value of plectasin. In this study, biologically active recombinant plectasin which was able to inhibit dengue protease and viral replication in Vero cells was successfully produced in E. coli in a time- and cost- effective method. These findings are potentially important in the development of potent therapeutics against dengue infection.
登革热病毒感染了全球数百万人,目前尚无可用的疫苗或抗登革热疗法。抗菌肽已被证明对多种病毒具有有效的抗病毒活性。将这些肽开发为有效的抗病毒药物的主要限制之一是生产成本高。在这项研究中,通过在大肠杆菌中产生包涵体来廉价地实现生物活性的 plectasin 肽的高产。评估了重组肽对登革热血清型 2 NS2B-NS3 蛋白酶(DENV2 NS2B-NS3pro)的抗病毒活性,作为抑制登革病毒在 Vero 细胞中复制的靶标。通过应用连续的复性、Factor Xa 切割和镍柱纯化步骤,收集单个单位的重组 plectasin,以获得高纯度的重组蛋白。重组肽对 Vero 细胞的最大无毒剂量(MNTD)为 20μM(100μg/mL)。当向反应混合物中加入更高浓度的重组 plectasin 时,DENV2 NS2B-NS3pro 的反应速度明显下降。plectasin 肽以 Ki 值 5.03±0.98μM 非竞争性地抑制 DENV2 NS2B-NS3pro。在 MNTD 值下,病毒抑制率超过 80%。在这项研究中,成功地在大肠杆菌中以时间和成本有效的方式生产出能够抑制登革热蛋白酶和 Vero 细胞中病毒复制的生物活性重组 plectasin。这些发现对于开发针对登革热感染的有效治疗方法具有重要意义。