Abstract

Tilia amurensis Rupr. (Tiliaceae) is commonly known as bee tree and it has been used to treat various diseases as a Korean traditional medicine since ancient times. On the search for biologically active compounds from T. amurensis, a bioassay-guided fractionation and chemical investigation of its MeOH extract resulted in the isolation and identification of four flavan-3-ols, including a new flavan-3-ol dimer, tiliabisflavan A (1). The isolated compounds were evaluated for their antiproliferative activities against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines and their inhibitory effects on NO production in a lipopolysaccharide (LPS)-activated BV2 cell line. Compound 1 exhibited the strongest cytotoxicity against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines (IC50 (1): 13.37, 14.61, 5.68, and 11.03µM, respectively). In addition, compound 1 significantly inhibited NO levels with an IC50 value of 4.96 µM, which is more effective than N G-monomethyl-L-arginine (NMMA), a well-known NO synthase inhibitor.

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