Lignans from the Twigs of and Their Bioactivities.

Molecules

State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Published: January 2019

, an important medicinal plant, is widely used as a traditional Chinese medicine and spice. Using cytotoxicity-guided fractionation, nine new lignans ⁻ and ten known analogues ⁻ were obtained from the EtOH extract of the twigs of . Their structures were assigned by extensive 1D- and 2D-NMR experiments, and the absolute configurations were resolved by specific rotation and a combination of experimental and theoretically calculated electronic circular dichroism (ECD) spectra. In the cytotoxicity assay, 7',9-epoxylignans with feruloyl or cinnamoyl groups (compounds ⁻, and ) were selectively cytotoxic against NCI-H1650 cell line, while the dibenzylbutyrolactone lignans ⁻ exerted cytotoxicities against HCT-116 and A2780 cell lines. The results highlighted the structure-activity relationship importance of a feruloyl or a cinnamoyl moiety at C-9' or/and C-7 ketone in 7',9-epoxylignans. Furthermore, compound was moderate active toward protein tyrosine phosphatase 1B (PTP1B) with an IC value of 13.5 μM, and compounds ⁻, and displayed inhibitory activity against LPS-induced NO production in RAW264.7 macrophages, with IC values of 46.8, 50.1, 58.6, 47.5, and 66.5 μM, respectively.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359749PMC
http://dx.doi.org/10.3390/molecules24020306DOI Listing

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