Shuai Ge, Xiangjun Wang, Yajing Hou, Yuexin Lv, Cheng Wang, Huaizhen He

Eur J Pharmacol . 2021 Jan 23;896:173897. doi: 10.1016/j.ejphar.2021.173897. Online ahead of print.

The spread of the coronavirus SARS-CoV-2 has continuously threatened our global health since the end of 2019. There is an urgent need for effective drugs and vaccines to fight the COVID-19; however, this may take longer than expected. One of the feasible strategies to combat this situation is to repurpose existing drugs, shorten the development time, and fight this virus outbreak.

It has been shown that histamine H1 receptor antagonists (H1-antihistamines) have broad-spectrum antiviral effects.

This study’s objective was to screen potential drugs among histamine H1 receptors that may have the capacity to inhibit the infection by the SARS-CoV-2 virus.

Five FDA-approved H1-antihistamines were found to have bioaffinity to angiotensin-converting enzyme 2 (ACE2), based on the model of ACE2 overexpressing HEK293T cell membrane chromatography.

Afterward, the interaction between these drugs and ACE2 was determined by frontal analysis and surface plasmon resonance (SPR), which also consistently demonstrated that these hits bind to ACE2 at micromolar levels of affinity.

A pseudovirus assay has helped identify that doxepin could inhibit SARS-CoV-2 spike pseudovirus from entering the ACE2-expressing cell, reducing the infection rate to 25,8%.

Doxepin may be a viable drug candidate for clinical trials to fight COVID-19. It is now recommended to compare these results with in vivo results and provide evidence for clinical trials’ final attempt. (215 words)

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