Antiviral activity of fluorinated compounds against DNA- and RNA-containing viruses

K. Naumenko, Polina A. Zaremba, S. Zagorodnya, Yurii Shermolovych
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Abstract

Viral infections occupy an important in human as one of the most common and poorly controlled infections. At present, Influenza A virus (IAV) and Epstein-Barr virus (EBV) cause different infections, thereby imposing a huge toll on both human health and the economy worldwide. Therefore, screening new effective drugs is an urgent and important problem. Our study aimed to determine cytotoxicity and antiviral effect of fluorinated compounds against the Influenza A virus and Epstein-Barr virus. The cytotoxicity was studied in two cell lines by MTT assay. The cytotoxicity of the compounds the rate was 41 – 990 μg/ml in the B95-8 cell culture, which produces EBV, and 200 – 478 μg/ml in MDCK cells. Compounds 10S-47 and 10S-49 were able to inhibit reproduction of IAV with EC 50 of 38 μg/ml and 50 μg/ml, respectively. It was shown that fluorinated compounds showed low effectiveness against the Epstein-Barr virus, and inhibited the reproduction of the virus at 20% in the concentration range of 1 – 100 μg/ml. Also, we studied the potency of compound 10S-47 to make an apoptosis induction because it exhibited a significant cytotoxic effect on the growth of transformed cells. It was established that for compound 10S-47 at 40 mg/ml, the percentage of apoptotic cells exceeded the control and was 10%. The cytotoxicity of compounds was determined by MTT-method, CC 50 were in the range 41 – 990 µg/ml. The antiviral activity of the compounds was determined by RT-PCR. It was shown that only 10S-48 and 10S-49 compounds inhibit EBV reproduction, percentage of inhibition of synthesis of viral DNA was in range from 1 to 7. This data do not allow us to assign this class of compounds to promising anti-EBV agents.
含氟化合物对含DNA和rna病毒的抗病毒活性
病毒感染是人类最常见和控制最差的感染之一,在人类中占有重要地位。目前,甲型流感病毒(IAV)和eb病毒(EBV)引起不同的感染,从而对人类健康和全球经济造成巨大损失。因此,筛选新的有效药物是一个迫切而重要的问题。本研究旨在确定氟化化合物对甲型流感病毒和eb病毒的细胞毒性和抗病毒作用。用MTT法对两株细胞株进行了细胞毒性研究。对产生EBV的B95-8细胞的细胞毒性为41 ~ 990 μg/ml,对MDCK细胞的细胞毒性为200 ~ 478 μg/ml。化合物10S-47和10S-49抑制IAV的繁殖,ec50分别为38 μg/ml和50 μg/ml。结果表明,在1 ~ 100 μg/ml浓度范围内,含氟化合物对Epstein-Barr病毒的抑制率为20%,对Epstein-Barr病毒的抑制率较低。此外,我们还研究了化合物10S-47诱导凋亡的效力,因为它对转化细胞的生长表现出明显的细胞毒性作用。结果表明,当浓度为40 mg/ml时,化合物10S-47的凋亡细胞比例超过对照,为10%。mtt法测定化合物的细胞毒性,cc50在41 ~ 990µg/ml范围内。采用RT-PCR检测化合物的抗病毒活性。结果表明,只有10S-48和10S-49化合物能抑制EBV的繁殖,抑制病毒DNA合成的百分比在1 ~ 7之间。这些数据不允许我们将这类化合物分配给有希望的抗ebv药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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