Department of Biomedical Sciences, College of Veterinary Medicine, King Faisal University, Al-Ahsa, Saudi Arabia.
Department of Pharmacology, Faculty of Veterinary Medicine, Kafrelsheikh University, Kafrelsheikh, Egypt.
J Med Virol. 2020 Sep;92(9):1665-1670. doi: 10.1002/jmv.25928. Epub 2020 May 8.
The Middle East respiratory syndrome coronavirus (MERS-CoV) is an emerging virus that causes infection with a potentially fatal outcome. Dendrimers are highly branched molecules that can be added to antiviral preparations to improve their delivery, as well as their intrinsic antiviral activity. Studies on identifying anti-MERS-CoV agents are few. Three types of polyanionic dendrimers comprising the terminal groups sodium carboxylate (generations 1.5, 2.5, 3.5, and 4.5), hydroxyl (generations 2, 3, 4, and 5), and succinamic acid (generations 2, 3, 4, and 5) and polycationic dendrimers containing primary amine (generations 2, 3, 4, and 5) were used to assess their antiviral activity with the MERS-CoV plaque inhibition assay. The hydroxyl polyanionic set showed a 17.36% to 29.75% decrease in MERS-CoV plaque formation. The most potent inhibition of MERS-CoV plaque formation was seen by G(1.5)-16COONa (40.5% inhibition), followed by G(5)-128SA (39.77% inhibition). In contrast, the cationic dendrimers were cytotoxic to Vero cells. Polyanionic dendrimers can be added to antiviral preparations to improve the delivery of antivirals, as well as the intrinsic antiviral activity.
中东呼吸综合征冠状病毒（MERS-CoV）是一种新兴病毒，可导致感染，具有潜在致命后果。树枝状大分子是高度分支的分子，可以添加到抗病毒制剂中，以改善其递送以及内在的抗病毒活性。鉴定抗 MERS-CoV 药物的研究很少。使用了三种类型的带负电荷的树枝状大分子，其末端基团为羧酸钠（1.5 代、2.5 代、3.5 代和 4.5 代）、羟基（2 代、3 代、4 代和 5 代）和琥珀酸（2 代、3 代、4 代和 5 代）以及带正电荷的树枝状大分子，其中包含伯胺（2 代、3 代、4 代和 5 代），以评估它们在 MERS-CoV 蚀斑抑制测定中的抗病毒活性。羟基带负电荷的树枝状大分子使 MERS-CoV 蚀斑形成减少了 17.36％至 29.75％。对 MERS-CoV 蚀斑形成的抑制作用最强的是 G(1.5)-16COONa（抑制率为 40.5％），其次是 G(5)-128SA（抑制率为 39.77％）。相比之下，阳离子树枝状大分子对 Vero 细胞具有细胞毒性。带负电荷的树枝状大分子可以添加到抗病毒制剂中，以改善抗病毒药物的递送，以及内在的抗病毒活性。
