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Full-Text Articles in Pharmaceutics and Drug Design

Induction Of Apoptosis In Human Breast Cancer Cells Via Caspase Pathway By Vernodalin Isolated From Centratherum Anthelminticum(L.) Seeds, Kok Hoong Leong Feb 2013

Induction Of Apoptosis In Human Breast Cancer Cells Via Caspase Pathway By Vernodalin Isolated From Centratherum Anthelminticum(L.) Seeds, Kok Hoong Leong

Kok Hoong Leong

In this study, we showed that CACF inhibited growth of MCF-7 human breast cancer cells. CACF induced apoptosis in MCF-7 cells as marked by cell size shrinkage, deformed cytoskeletal structure and DNA fragmentation. To identify the cytotoxic compound, CACF was subjected to bioassay-guided fractionation which yielded 6 fractions. CACF fraction A and B (CACF-A, -B) demonstrated highest activity among all the fractions. Further HPLC isolation, NMR and LC-MS analysis of CACF-A led to identification of vernodalin as the cytotoxic agent in CACF-A, and -B. 12,13-dihydroxyoleic acid, another major compound in CACF-C fraction was isolated for the first time from Centratherum …


Identification And Characterization Of Kava-Derived Compounds Mediating Tnf-Α Suppression, Michael P. Pollastri, Adrian Whitty, Jamie Cassidy Merrill, Trent D. Ashton, Salomon Amar Jan 2012

Identification And Characterization Of Kava-Derived Compounds Mediating Tnf-Α Suppression, Michael P. Pollastri, Adrian Whitty, Jamie Cassidy Merrill, Trent D. Ashton, Salomon Amar

Michael Pollastri

There is a substantial unmet need for new classes of drugs that block TNF-α-mediated inflammation, and particularly for small molecule agents that can be taken orally. We have screened a library of natural products against an assay measuring TNF-α secretion in lipopolysaccharide (LPS)-stimulated THP-1 cells, seeking compounds capable of interfering with the TNF-α inducing transcription factor Lipopolysaccharide Induced TNF Alpha Factor (LITAF). Among the active compounds were several produced by the kava plant (Piper mysticum), extracts of which have previously been linked to a range of therapeutic effects. When tested in vivo, a representative of these compounds, kavain, was found …