Ecdysones from Zoanthus spp. with inhibitory activity against dengue virus 2

Abstract

Bioassay-guided fractionation of an ethanolic extract of Zoanthus spp. collected in Taiwan has resulted in the isolation of one new ecdysone, zoanthone A (1), along with thirteen known compounds (2-14). The structures of these compounds were determined by spectroscopic methods, especially 2D NMR analyses. The in vitro antiviral activities of all isolated ecdysones (1-14) against dengue virus type 2 (DENV-2) were evaluated using DENV infectious system. New compound (1) exhibited potent antiviral activity (EC50=19.61 ± 2.46 μM) with a selectivity index (CC50/EC50) value of 36.7. The structure-activity relationships of isolated ecdysones against DENV-2 were concluded. Molecular docking information of 3 and NS5 polymerase was performed either.

Potential Antivirals: Natural Products Targeting Replication Enzymes of Dengue and Chikungunya Viruses

“…This is an important approach since inhibition of these enzymes can disrupt the virus life cycle. Most of the studies herein described were conducted in vitro using enzymatic assays [ 8 , 47 , 48 , 49 , 50 , 51 , 52 ] or viral strain/replicon on cells evaluating replication, inhibition and/or protein expression [ 49 , 51 , 52 , 53 , 54 , 56 , 68 , 69 , 70 , 71 ]. Three studies were conducted utilizing the in silico docking approach [ 57 , 58 , 72 ].…”

“…Ecdysone 42 was found to be active against all DENV serotypes, with the following EC 50 values: DENV-1 (15.70 ± 2.36 μM), DENV-3 (9.48 ± 0.24 μM) and DENV-4 (12.15 ± 1.22 μM) with a high CC 50 (the 50% cytotoxic concentration). After analyses of both the structure-activity relationship and molecular docking, the authors proposed that ecdysone 42 impairs DENV RNA replication by blocking the viral polymerase channel [ 54 ].…”

Anti-Dengue Virus Constituents from Formosan Zoanthid Palythoa mutuki

“…Due to the anti-dengue virus activities of some ecdysteroids ( 5 – 8 ) that were revealed previously [9], the other five compounds ( 1 – 4 , and 9 ) were selected to evaluate their anti-dengue virus 2 (DENV-2) activities and cytotoxicity. As a result, palythone A ( 1 ) and 24- epi -makisterone ( 4 ) demonstrated weak anti-DENV-2 activities (Table 2).…”

“…Recently, our research group has studied anti-dengue virus ecdysteroids from Formosan zoanthid Zoanthus spp. [9]. In our continuous screening for bioactive marine natural products, the ethanolic extract of P. mutuki showed strong anti-dengue virus activity.…”

Potential Antivirals: Natural Products Targeting Replication Enzymes of Dengue and Chikungunya Viruses

“…Ecdysone 42 was found to be active against all DENV serotypes, with the following EC50 values: DENV-1 (15.70 ± 2.36 µM), DENV-3 (9.48 ± 0.24 µM), and DENV-4 (12.15 ± 1.22 µM). After analyzes of both the structure-activity relationship and molecular docking, the authors proposed that ecdysone 42 impairs DENV RNA replication by blocking the viral polymerase channel [54]. β-Carbolines are widespread plant and animal alkaloids that possess important biological activities [55].…”