Botanical inhibitors of SARS-CoV-2 viral entry: a phylogenetic perspective

• Published in: Scientific reports Vol. 13; no. 1; pp. 1244 - 12
• Main Authors: Risener, Caitlin J., Woo, Sunmin, Samarakoon, Tharanga, Caputo, Marco, Edwards, Emily, Klepzig, Kier, Applequist, Wendy, Zandi, Keivan, Goh, Shu Ling, Downs-Bowen, Jessica A., Schinazi, Raymond F., Quave, Cassandra L.
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 23-01-2023; Nature Publishing Group; Nature Portfolio
• Subjects: 631/326/22/1295; 631/449/2667; ACE2; Angiotensin-converting enzyme 2; Animals; Antiviral activity; Antiviral Agents; Aquatic plants; Biological Products; Cardiac glycosides; Coronaviruses; COVID-19; Cytotoxicity; Dietary supplements; Flowers; Flowers & plants; Glycosides; Humanities and Social Sciences; Humans; Mammals; multidisciplinary; Natural products; Pandemics; Phylogeny; Plant Extracts; Protein Binding; Rhizomes; SARS-CoV-2; Science; Science (multidisciplinary); Severe acute respiratory syndrome coronavirus 2; Spike protein; Virus Internalization
• ISSN: 2045-2322; 2045-2322
• DOI: 10.1038/s41598-023-28303-x

Throughout the SARS-CoV-2 pandemic, the use of botanical dietary supplements in the United States has increased, yet their safety and efficacy against COVID-19 remains underexplored. The Quave Natural Product Library is a phylogenetically diverse collection of botanical and fungal natural product extracts including popular supplement ingredients. Evaluation of 1867 extracts and 18 compounds for virus spike protein binding to host cell ACE2 receptors in a SARS-CoV-2 pseudotyped virus system identified 310 extracts derived from 188 species across 76 families (3 fungi, 73 plants) that exhibited ≥ 50% viral entry inhibition activity at 20 µg/mL. Extracts exhibiting mammalian cytotoxicity > 15% and those containing cardiotoxic cardiac glycosides were eliminated. Three extracts were selected for further testing against four pseudotyped variants and infectious SARS-CoV-2 and were then further chemically characterized, revealing the potent (EC
50
 < 5 µg/mL) antiviral activity of
Solidago altissima
L. (Asteraceae) flowers and
Pteridium aquilinum
(L.) Kuhn (Dennstaedtiaceae) rhizomes.