New structural analogues of curcumin exhibit potent growth suppressive activity in human colorectal carcinoma cells View Full Text


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Article Info

DATE

2009-03-30

AUTHORS

Ling Cen, Brian Hutzen, Sarah Ball, Stephanie DeAngelis, Chun-Liang Chen, James R Fuchs, Chenglong Li, Pui-Kai Li, Jiayuh Lin

ABSTRACT

BackgroundColorectal carcinoma is one of the major causes of morbidity and mortality in the Western World. Novel therapeutic approaches are needed for colorectal carcinoma. Curcumin, the active component and yellow pigment of turmeric, has been reported to have several anti-cancer activities including anti-proliferation, anti-invasion, and anti-angiogenesis. Clinical trials have suggested that curcumin may serve as a potential preventive or therapeutic agent for colorectal cancer.MethodsWe compared the inhibitory effects of curcumin and novel structural analogues, GO-Y030, FLLL-11, and FLLL-12, in three independent human colorectal cancer cell lines, SW480, HT-29, and HCT116. MTT cell viability assay was used to examine the cell viability/proliferation and western blots were used to determine the level of PARP cleavages. Half-Maximal inhibitory concentrations (IC50) were calculated using Sigma Plot 9.0 software.ResultsCurcumin inhibited cell viability in all three of the human colorectal cancer cell lines studied with IC50 values ranging between 10.26 μM and 13.31 μM. GO-Y030, FLLL-11, and FLLL-12 were more potent than curcumin in the inhibition of cell viability in these three human colorectal cancer cell lines with IC50 values ranging between 0.51 μM and 4.48 μM. In addition, FLLL-11 and FLLL-12 exhibit low toxicity to WI-38 normal human lung fibroblasts with an IC-50 value greater than 1,000 μM. GO-Y030, FLLL-11, and FLLL-12 are also more potent than curcumin in the induction of apoptosis, as evidenced by cleaved PARP and cleaved caspase-3 in all three human colorectal cancer cell lines studied.ConclusionThe results indicate that the three curcumin analogues studied exhibit more potent inhibitory activity than curcumin in human colorectal cancer cells. Thus, they may have translational potential as chemopreventive or therapeutic agents for colorectal carcinoma. More... »

PAGES

99

References to SciGraph publications

  • 2007. HIGHLY ACTIVE ANTICANCER CURCUMIN ANALOGUES in THE MOLECULAR TARGETS AND THERAPEUTIC USES OF CURCUMIN IN HEALTH AND DISEASE
  • 2007. CURCUMIN AND AUTOIMMUNE DISEASE in THE MOLECULAR TARGETS AND THERAPEUTIC USES OF CURCUMIN IN HEALTH AND DISEASE
  • 2007. CLINICAL STUDIES WITH CURCUMIN in THE MOLECULAR TARGETS AND THERAPEUTIC USES OF CURCUMIN IN HEALTH AND DISEASE
  • 2008-03-07. Curcumin: From ancient medicine to current clinical trials in CELLULAR AND MOLECULAR LIFE SCIENCES
  • 2004-03. Curcumin, A Multi-Functional Chemopreventive Agent, Blocks Growth of Colon Cancer Cells by Targeting β-Catenin-Mediated Transactivation and Cell–Cell Adhesion Pathways in JOURNAL OF MOLECULAR HISTOLOGY
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    http://scigraph.springernature.com/pub.10.1186/1471-2407-9-99

    DOI

    http://dx.doi.org/10.1186/1471-2407-9-99

    DIMENSIONS

    https://app.dimensions.ai/details/publication/pub.1022360492

    PUBMED

    https://www.ncbi.nlm.nih.gov/pubmed/19331692


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    40 PARP cleavage
    41 ResultsCurcumin
    42 SW480
    43 Western blot
    44 Western world
    45 active components
    46 activity
    47 addition
    48 agents
    49 analogues
    50 anti-cancer activity
    51 apoptosis
    52 approach
    53 blot
    54 cancer
    55 cancer cell lines
    56 cancer cells
    57 carcinoma
    58 carcinoma cells
    59 caspase-3
    60 cause
    61 cell lines
    62 cell viability
    63 cell viability/proliferation
    64 cells
    65 cleavage
    66 clinical trials
    67 colorectal cancer
    68 colorectal cancer cell lines
    69 colorectal cancer cells
    70 colorectal carcinoma
    71 colorectal carcinoma cells
    72 components
    73 concentration
    74 curcumin
    75 curcumin analogues
    76 effect
    77 exhibit
    78 exhibit low toxicity
    79 growth-suppressive activity
    80 half maximal inhibitory concentration
    81 human colorectal cancer cell lines
    82 human colorectal cancer cells
    83 human colorectal carcinoma cells
    84 human lung
    85 induction
    86 induction of apoptosis
    87 inhibition
    88 inhibitory activity
    89 inhibitory concentration
    90 inhibitory effect
    91 levels
    92 lines
    93 low toxicity
    94 lung
    95 major cause
    96 morbidity
    97 mortality
    98 new structural analogs
    99 normal human lung
    100 novel structural analogues
    101 novel therapeutic approaches
    102 pigments
    103 potent growth suppressive activity
    104 potent inhibitory activity
    105 potential
    106 proliferation
    107 results
    108 software
    109 structural analogues
    110 suppressive activity
    111 therapeutic agents
    112 therapeutic approaches
    113 toxicity
    114 translational potential
    115 trials
    116 turmeric
    117 values
    118 viability
    119 viability/proliferation
    120 world
    121 yellow pigment
    122 μM
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