Isolation and Identification of Triterpenoids from Rosa laevigata var. leiocapus and Evaluation of Their Anti-SARS-COV-2 Activity

Abstract:

To understand the triterpenoids from Rosa laevigata var. leiocapus and their SARS-CoV-2 inhibitory activities, 15 compounds were isolated from the 95% EtOH extract by using chromatographic separation techniques, such as silica gel, Sephadex LH-20 and pre-HPLC. On the basis of spectral data, their structures were identified as laevigaterpene A (1), 2α, 23-dihydroxy oleanolic acid (2), 1β-hydroxyeuscaphic acid (3), 3β-(p-hydroxytranscin-namoyloxy)olean-12-en-28-oic acid (4), 3β-trans-p-coumaroyloxy-2α-hydroxy oleanolic acid (5), 2α, 3α-dihydroxyo-lean-12-en-28-oic acid (6), pomolic acid (7), lup-3β-ol-28-carboxylate (8), 2α, 3α, 19α, 23-tetrahydroxyurs-12-en-28-oic acid (9), acetyl-11α-methoxy-β-boswellic acid (10), arjunic acid (11), 2α, 3α, 19α-trihydroxy-28-norurs-12-ene (12), euscaphic acid (13), 2α, 19α-dihydroxy-3-oxo-12-ursen-28-oic acid (14), and oleanolic acid (15). Compounds 1-15 were obtained from this species at first time. Moreover, compounds4,10 and 12 were isolated from Rosa at first time. Compounds 8 and15 exhibited strong inhibitory effects on SARS-CoV-2 M^pro, with IC₅₀ of (6.74±0.33) and (5.19±0.25) μmol/L, respectively, showing potential anti-SARS-CoV-2 activity.