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两种杯[4]芳烃衍生物对人冠状病毒 229E 的抗菌性能。

Antiseptic properties of two calix[4]arenes derivatives on the human coronavirus 229E.

机构信息

GEVSM, SRSMC, UMR, Nancy-University, CNRS, France.

出版信息

Antiviral Res. 2010 Dec;88(3):343-6. doi: 10.1016/j.antiviral.2010.09.009. Epub 2010 Sep 18.

Abstract

Facing the lack in specific antiviral treatment, it is necessary to develop new means of prevention. In the case of the Coronaviridae this family is now recognized as including potent human pathogens causing upper and lower respiratory tract infections as well as nosocomial ones. Within the purpose of developing new antiseptics molecules, the antiseptic virucidal activity of two calix[4]arene derivatives, the tetra-para-sulfonato-calix[4]arene (C[4]S) and the 1,3-bis(bithiazolyl)-tetra-para-sulfonato-calix[4]arene (C[4]S-BTZ) were evaluated toward the human coronavirus 229E (HCoV 229E). Comparing these results with some obtained previously with chlorhexidine and hexamidine, (i) these two calixarenes did not show any cytotoxicity contrary to chlorhexidine and hexamidine, (ii) C[4]S showed as did hexamidine, a very weak activity against HCoV 229E, and (iii) the C[4]S-BTZ showed a stronger activity than chlorhexidine, i.e. 2.7 and 1.4log₁₀ reduction in viral titer after 5min of contact with 10⁻³mol L⁻¹ solutions of C[4]S-BTZ and chlorhexidine, respectively. Thus, the C[4]S-BTZ appeared as a promising virucidal (antiseptic) molecule.

摘要

面对缺乏特异性抗病毒治疗的情况,有必要开发新的预防手段。在冠状病毒科,该家族现在被认为包括引起上呼吸道和下呼吸道感染以及医院获得性感染的强效人类病原体。为了开发新的防腐剂分子,评估了两种杯[4]芳烃衍生物,即四对磺酸钠杯[4]芳烃(C[4]S)和 1,3-双(双噻唑基)-四对磺酸钠杯[4]芳烃(C[4]S-BTZ)对人类冠状病毒 229E(HCoV 229E)的防腐病毒活性。将这些结果与先前用洗必泰(chlorhexidine)和己脒定(hexamidine)获得的一些结果进行比较,(i)这两种杯芳烃与洗必泰和己脒定相反,没有显示出任何细胞毒性,(ii)C[4]S 表现出与己脒定相似的非常弱的抗 HCoV 229E 活性,和(iii)C[4]S-BTZ 的活性比洗必泰强,即与 10⁻³mol L⁻¹的 C[4]S-BTZ 和洗必泰溶液接触 5 分钟后,病毒滴度分别降低了 2.7 和 1.4log₁₀。因此,C[4]S-BTZ 似乎是一种有前途的病毒杀灭(防腐剂)分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8731/7114180/30d5339398fb/gr1.jpg

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