During the search for secondary metabolites with antiproliferative activity, six new lanostane triterpenoids, tyrosamic acids A-F (1-6) together with ten known compounds (7-16), were isolated from the fruiting body of Tyromyces sambuceus. Their structures were elucidated using MS analyses, extensive 2D-heteronuclear NMR data interpretation and the structure of 3 was further confirmed by single-crystal X-ray data analyses. All lanostane triterpenoids (1-16) possesses a carboxy group at C-20 position and their strength of antiproliferative activity was affected by the presence or absence of a hydroxy group at C-15 position and at the side chain. Four of the compounds (1, 6, 10, 14) showed antiproliferative activities against human cancer cell lines with IC₅₀ values of 16.8-48.3 µM (HL-60).
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ACS Omega
December 2024
Department of Organic and Inorganic Chemistry, Science Center, Federal University of Ceará, Fortaleza, CE 60455-760, Brazil.
One of the most investigated molecular targets for anticancer therapy is the proto-oncogene , which is amplified and thus overexpressed in many types of cancer. Due to its structural characteristics, developing inhibitors for the target has proven to be challenging. In this study, the anti-MYC potential of lanostane-type triterpenes was investigated for the first time, using computational approaches that involved ensemble docking, prediction of structural properties and pharmacokinetic parameters, molecular dynamics (MD), and binding energy calculation using the molecular mechanics-generalized born surface area (MM-GBSA) method.
View Article and Find Full Text PDFMar Drugs
December 2024
G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Sciences, Pr. 100-letya Vladivostoka 159, 690022 Vladivostok, Russia.
Five new non-holostane di- and trisulfated triterpene pentaosides, conicospermiumosides A-1 (), A-2 (), A-3 (), A-1 (), and A-2 () were isolated from the Far Eastern sea cucumber Levin et Stepanov (Cucumariidae, Dendrochirotida). Twelve known glycosides found earlier in other species were also obtained and identified. The structures of new compounds were established on the basis of extensive analysis of the 1D and 2D NMR spectra, as well as by the HR-ESI-MS data.
View Article and Find Full Text PDFFitoterapia
January 2025
National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency (NSTDA), 111 Thailand Science Park, Phahonyothin Road, Klong Luang, Pathumthani 12120, Thailand. Electronic address:
Background: (), which possesses various biological effects, has been widely used as traditional medicine and functional food in Asian countries, especially China. In consideration of its various biological effects on human healthcare, . was usually used in combination with other drugs.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
December 2024
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing, 100191, China.
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