Abstract
Baicalein is the main active compound of Scutellaria baicalensis Georgi, a medicinal herb with multiple pharmacological activities, including the broad anti-virus effects. In this paper, the preclinical study of baicalein on the treatment of COVID-19 was performed. Results showed that baicalein inhibited cell damage induced by SARS-CoV-2 and improved the morphology of Vero E6 cells at a concentration of 0.1 μM and above. The effective concentration could be reached after oral administration of 200 mg/kg crystal form β of baicalein in rats. Furthermore, baicalein significantly inhibited the body weight loss, the replication of the virus, and relieved the lesions of lung tissue in hACE2 transgenic mice infected with SARS-CoV-2. In LPS-induced acute lung injury of mice, baicalein improved the respiratory function, inhibited inflammatory cell infiltration in the lung, and decreased the levels of IL-1β and TNF-α in serum. In conclusion, oral administration of crystal form β of baicalein could reach its effective concentration against SARS-CoV-2. Baicalein could inhibit SARS-CoV-2-induced injury both in vitro and in vivo. Therefore, baicalein might be a promising therapeutic drug for the treatment of COVID-19.
【저자키워드】 severe acute respiratory syndrome coronavirus 2, Coronavirus disease 2019, main protease, Bronchoalveolar lavage fluid, dengue virus, Human immunodeficiency virus, Human angiotensin-converting enzyme 2, Cytopathic effect, peak expiratory flow, COVID-19coronavirus disease 2019, SARS-CoV-2severe acute respiratory syndrome coronavirus 2, HIVhuman immunodeficiency virus, DENVdengue virus, MOImultiplicity of infection, multiplicity of infection, ANOVAanalysis of variance, analysis of variance, LLOQLower Limit of Quantitation, Lower Limit of Quantitation, BALFbronchoalveolar lavage fluid, Cavgaverage steady-state plasma concentration, average steady-state plasma concentration, CC50half-cytotoxic concentration, half-cytotoxic concentration, Cmaxpeak plasma concentration, peak plasma concentration, CPEcytopathic effect, EC50half-maximal effective concentrations, half-maximal effective concentrations, EEPend-expiratory pause, end-expiratory pause, hACE2human angiotensin-converting enzyme 2, H & EHematoxylin and eosin, Hematoxylin and eosin, JEVJapanese encephalitis virus, Japanese encephalitis virus, Mpromain protease, PEFpeak expiratory flow, Penhenhanced pause, enhanced pause, SIselection index, selection index, ZIKVZika virus, Zika virus, 【초록키워드】 COVID-19, Treatment, SARS-CoV-2, Respiratory function, lung, in vitro, virus, acute lung injury, hACE2, Scutellaria baicalensis, Replication, serum, mice, morphology, Vero E6 cell, in vivo, TNF-α, IL-1β, administration, Concentration, Injury, baicalein, lesion, activities, transgenic mice, lung tissue, Body weight loss, cell damage, inflammatory cell infiltration, pharmacological, Effects, effective, Result, significantly, inhibit, inhibited, was performed, reached, infected with SARS-CoV-2, therapeutic drug, 【제목키워드】 COVID-19, Treatment, in vitro, in vivo, baicalein, therapeutic effect,