<p>Lycopene occurs as multiple geometrical isomers, whereas most studies on its cancer-related effects have focused on the all-<i>E</i>-isomer or on preparations with an undefined isomer composition. In this study, the antiproliferative activities of all-<i>E</i>-isomer-rich lycopene preparation (<i>E</i>-LYC) and <i>Z</i>-isomer-rich lycopene preparation (<i>Z</i>-LYC) were compared using a panel of 102 human cancer cell lines under identical experimental conditions. <i>Z</i>-LYC showed a broader antiproliferative profile than <i>E</i>-LYC, with IC<sub>50</sub> values within the tested concentration range (3.16–31,600 nM) in 91 and 16 cell lines, respectively. Tissue sensitivity analysis indicated that lymphoid malignancies and leukemia were relatively sensitive to <i>Z</i>-LYC, with additional sensitivity observed in bone, soft tissue, ovarian, and testicular germ cell tumors. Phenotypic similarity analysis further showed broader correlations for <i>Z</i>-LYC than <i>E</i>-LYC with reference anticancer agents, suggesting a more distinct biological response profile at the cellular level. Preliminary molecular docking simulations also suggested that lycopene <i>Z</i>-isomers may interact more favorably than the all-<i>E</i>-isomer with selected cancer-related proteins. These findings indicate that lycopene <i>Z</i>-isomers exhibit broader antiproliferative activity than the all-<i>E</i>-isomer in this in vitro screening platform and warrant further mechanistic and in vivo studies.</p>

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Screening of the antiproliferative activity of lycopene isomers in a panel of human cancer cell lines: Lycopene Z-isomers exhibit greater activity than the all-E-isomer

  • Masaki Honda,
  • Kako Matsumoto,
  • Asih Gayatri,
  • Mitsuya Ito,
  • Kazumi Sawada,
  • Kento Nakamura

摘要

Lycopene occurs as multiple geometrical isomers, whereas most studies on its cancer-related effects have focused on the all-E-isomer or on preparations with an undefined isomer composition. In this study, the antiproliferative activities of all-E-isomer-rich lycopene preparation (E-LYC) and Z-isomer-rich lycopene preparation (Z-LYC) were compared using a panel of 102 human cancer cell lines under identical experimental conditions. Z-LYC showed a broader antiproliferative profile than E-LYC, with IC50 values within the tested concentration range (3.16–31,600 nM) in 91 and 16 cell lines, respectively. Tissue sensitivity analysis indicated that lymphoid malignancies and leukemia were relatively sensitive to Z-LYC, with additional sensitivity observed in bone, soft tissue, ovarian, and testicular germ cell tumors. Phenotypic similarity analysis further showed broader correlations for Z-LYC than E-LYC with reference anticancer agents, suggesting a more distinct biological response profile at the cellular level. Preliminary molecular docking simulations also suggested that lycopene Z-isomers may interact more favorably than the all-E-isomer with selected cancer-related proteins. These findings indicate that lycopene Z-isomers exhibit broader antiproliferative activity than the all-E-isomer in this in vitro screening platform and warrant further mechanistic and in vivo studies.