Kim, Ji-Young Kim, Tai Young Son, So-Ri Kim, Suyeon Yellena Kwon, Jaeyoung Kwon, Hak Cheol Lee, C. Justin Jang, Dae Sik 2024-01-26T01:42:02Z 2024-01-26T01:42:02Z 2024-01-25 2024-01 https://pubs.kist.re.kr/handle/201004/148474 Triterpenoidal saponins have been reported to be able to restrain SARS-CoV-2 infection. To isolate antiviral compounds against SARS-CoV-2 from the leaves of Aster koraiensis, we conducted multiple steps of column chromatography. We isolated six triperpenoidal saponins from A. koraiensis leaves, including three unreported saponins. Their chemical structures were determined using HR-MS and NMR data analyses. Subsequently, we tested the isolates to assess their ability to impede the entry of the SARS-CoV-2 pseudovirus (pSARS-CoV-2) into ACE2+ H1299 cells and found that five of the six isolates displayed antiviral activity with an IC50 value below 10 μM. Notably, one unreported saponin, astersaponin J (1), blocks pSARS-CoV-2 in ACE2+ and ACE2/TMPRSS2+ cells with similar IC50 values (2.92 and 2.96 μM, respectively), without any significant toxic effect. Furthermore, our cell-to-cell fusion and SARS-CoV-2 Spike-ACE2 binding assays revealed that astersaponin J inhibits membrane fusion, thereby blocking both entry pathways of SARS-CoV-2 while leaving the interaction between the SARS-CoV-2 Spike and ACE2 unaffected. Overall, this study expands the list of antiviral saponins by introducing previously undescribed triterpenoidal saponins isolated from the leaves of A. koraiensis, thereby corroborating the potency of triterpenoid saponins in impeding SARS-CoV-2 infection. English MDPI AG Triterpenoidal Saponins from the Leaves of Aster koraiensis Offer Inhibitory Activities against SARS-CoV-2 Article 10.3390/plants13020303 1 Plants, v.13, no.2 Plants 13 2 Y scie scopus 001152747200001 Plant Sciences Plant Sciences Article GYMNASTER-KORAIENSIS SPIKE PROTEIN POLYACETYLENE Aster koraiensis leaves compositae triterpenoidal saponins SARS-CoV-2