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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
Published on: June 26, 2018
Coumarin derivatives from Ferula kuhistanica and their biological activities
Khushang Ashurov1, Sodik Numonov2, Deng Zang3
1State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization and The Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China; University of the Chinese Academy of Sciences, Beijing 100039, China.
Abstract:
Twenty-five sesquiterpene coumarins, including twelve previously undescribed ones, were isolated from the roots of Ferula kuhistanica Korovin. Their structures were established through comprehensive spectroscopic analysis, NMR, HRESIMS, quantum 13C NMR DP4+ analysis, ECD calculations, and single-crystal X-ray diffraction analysis. This study systematically evaluated the melanogenesis, tyrosinase, anti-inflammatory, and cytotoxic activities of isolates. Kuhistanin B (1) significantly, promoted melanin synthesis (157.8% ± 1.8%) and increased tyrosinase activity (147.9% ± 10.5%) at 50 μM in B16F10 cells. An MTT assay confirmed no significant cytotoxicity at this concentration (cell viability = 100.0% ± 1.6%). In the anti-inflammatory assay, ethyl galbanate (17) and kopeolin (19) showed good activity with IC50 values of 7.1 ± 0.9 and 9.4 ± 3.1 μM. Isosamarcandin (14) and kopeolin (19) exhibited good cytotoxicity against HT-29 cells with IC50 values of 9.82 ± 0.51 and 7.64 ± 0.41 μM, respectively.