RT info:eu-repo/semantics/article
T1 Withanolide-Type Steroids from Physalis nicandroides Inhibit HIV Transcription
A1 Taddeo, Vito A.
A1 Núñez, Marvin J.
A1 Beltrán, Manuela
A1 Castillo, Ulises G.
A1 Menjívar, Jenny
A1 Jiménez Díaz, Ignacio Antonio
A1 Alcamí, José
A1 Bedoya, Luis M.
A1 López Bazzocchi, Isabel
AB The aim of the present study is to report theisolation, structural elucidation, and antiviral evaluation of fournew withanolide-type steroids, named nicansteroidins A−D (1−4), together with nine related known compounds (5−13) isolatedfrom the aerial parts of Physalis nicandroides. Their structures wereestablished based on an extensive spectroscopic analysis, including1D and 2D NMR techniques. Outstandingly, nicansteroidins Aand B possess an unusual side chain with an exocyclic double bondon the δ-lactone system, whereas nicansteroidins C and D have anuncommon cycloperoxide functionality in ring A as distinctstructural motifs. Their biological evaluation as inhibitors ofhuman immunodeficiency virus type 1 replication revealed that two compounds from this series, 7 and 13, displayed stronginhibition of HIV-1 replication with IC50 values lower than 2 μM. Moreover, cellular mechanism experiments showed that the maintarget of these compounds in the HIV replication cycle is viral transcription. This study is the first report of withanolide-type steroidsas HIV inhibitors and provides insight into their potential as candidates for further preclinical studies.
YR 2021
FD 2021
LK http://riull.ull.es/xmlui/handle/915/35934
UL http://riull.ull.es/xmlui/handle/915/35934
LA en
DS Repositorio institucional de la Universidad de La Laguna
RD 20-dic-2024