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Phytotherapy research : PTR, v.26 no.5, 2012년, pp.692 - 696
Seven lignans, previously isolated from Pycnanthus angolensis or obtained by derivatization, namely the dibenzylbutane‐type lignans threo‐4,4’‐dihydroxy‐3‐methoxylignan (1), 4’‐hydroxy‐3,3’,4‐trimethoxylignan (2), (−)‐dihydroguaiaretic acid (3), 3,3’,4,4’‐tetramethoxylignan (4), 4,4’‐diacetyl‐3,3’‐dimethoxylignan (5), heliobuphthalmin (6) and the butyrolactone lignan hinokinin (7), were evaluted for their ability as apoptosis inducers in human hepatoma HuH‐7 cells. Cell viability assays, morphological evaluation of apoptosis and enzymatic analyses of caspase activity in HuH‐7 cells were carried out. Using the lactate dehydrogenase lactate dehydrogenase (LDH) assay, it was demonstrated that the lignans (1–7) tested significantly reduced viability of HuH‐7 cells. Morphologic evaluation of HuH‐7 cells using Hoechst staining and fluorescence microscopy revealed that lignans 1–7 were strong inducers of apoptosis. In fact, HuH‐7 cells developed morphological changes of apoptosis, including chromatin condensation, nuclear fragmentation and formation of apoptotic bodies. However, lignans 2 and 7 were the most promising compounds in this study, inducing 2.4‐ and 2.5‐fold increases in apoptotic cells as compared to controls. Caspase‐3‐like activity assays confirmed the morphologic data. Copyright © 2011 John Wiley & Sons, Ltd.
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