Non-steroid receptor-mediated antiproliferative activity of styrylpyrone derivative in human breast cancer cell lines

Azimahtol Hawariah Lope Pihie, Johnson Stanslas, Laily Bin Din

    Research output: Contribution to journalArticle

    67 Citations (Scopus)

    Abstract

    The antiproliferative activity of a strylpyrone derivative (SPD) plant extract, was studied in three different human breast cancer cell lines in culture, and was compared with tamoxifen. The number of living cells was evaluated by Methylene Blue staining technique. SPD showed strong antiproliferative activity in estrogen receptor (ER) and progestin receptor (PgR) positive MCF-7 CELLS (EC50 = 6.30 x 10-7 M and receptor-negative MDA-MB-231 (EC50 = 5.62 x 10-7 M), but it partially inhibited the high progestin receptor positive T47D cells (EC50 = 1.58 x 10-6 M). Whereas tamoxifen, a non-steroidal antiestrogen exhibited strong inhibition on MCF-7 CELLS (EC50 = 1.41 x 10-6 M) and partial inhibition on T47D cells (EC50 = 2.5 x 10 -6 M), but did not affect the MDA-MB-231 cells in the concentration range 0.1 nM-1 μM (EC50 = 5.01 μM). At the same concentration range SPD and tamoxifen did not inhibit the proliferation of normal human liver cell line CCL 13 and normal bovine kidney MDBK; whereas adriamycin, a common chemotherapy drug for the treatment of advance cancer, caused 95% inhibition at 10-6 M. Competitive binding studies showed SPD had no ability to inhibit the binding of [3H]estradiol and [3H]progesterone to ER and PgR, respectively but, tamoxifen exhibited affinity for ER. Therefore, it can be concluded that the antiproliferative activity of SPD was selective towards breast cancer cell lines and not mediated by ER or PgR.

    Original languageEnglish
    Pages (from-to)1739-1743
    Number of pages5
    JournalAnticancer Research
    Volume18
    Issue number3 A
    Publication statusPublished - May 1998

    Fingerprint

    Progesterone Receptors
    Tamoxifen
    Estrogen Receptors
    Breast Neoplasms
    Cell Line
    Competitive Binding
    Estrogen Receptor Modulators
    Methylene Blue
    Plant Extracts
    Doxorubicin
    Progesterone
    Estradiol
    Cell Count
    Staining and Labeling
    Kidney
    Drug Therapy
    Liver
    Pharmaceutical Preparations
    Neoplasms
    Therapeutics

    Keywords

    • Antiproliferative activity
    • Human breast cancer cell lines
    • Styrylpyrone derivative

    ASJC Scopus subject areas

    • Cancer Research
    • Oncology

    Cite this

    Non-steroid receptor-mediated antiproliferative activity of styrylpyrone derivative in human breast cancer cell lines. / Pihie, Azimahtol Hawariah Lope; Stanslas, Johnson; Din, Laily Bin.

    In: Anticancer Research, Vol. 18, No. 3 A, 05.1998, p. 1739-1743.

    Research output: Contribution to journalArticle

    Pihie, Azimahtol Hawariah Lope ; Stanslas, Johnson ; Din, Laily Bin. / Non-steroid receptor-mediated antiproliferative activity of styrylpyrone derivative in human breast cancer cell lines. In: Anticancer Research. 1998 ; Vol. 18, No. 3 A. pp. 1739-1743.
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