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Various proteinase inhibitors decrease prolactin and growth hormone release by anterior pituitary cells.

G Rappay, G B Makara, S Bajusz

    Life Sciences
    |February 11, 1985
    PubMed
    Summary
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    Certain tripeptide aldehydes, particularly those with lysine, significantly inhibit prolactin (PRL) and growth hormone (GH) release from rat pituitary cells. Boc-DPhe-Phe-lysinal showed the strongest inhibition of PRL release.

    Area of Science:

    • Endocrinology
    • Molecular Pharmacology

    Background:

    • Prolactin (PRL) and growth hormone (GH) are key pituitary hormones.
    • Understanding the regulation of PRL and GH release is crucial for endocrine research.

    Purpose of the Study:

    • To investigate the inhibitory effects of various proteinase inhibitors on rat anterior pituitary cell hormone release.
    • To identify specific inhibitors that can modulate prolactin and growth hormone secretion.

    Main Methods:

    • Cultured rat anterior pituitary cells were used to assess hormone release.
    • A panel of proteinase inhibitors, including microbial and synthetic tripeptide aldehydes, were tested.

    Main Results:

    • Microbial inhibitors (chymostatin, elastatinal, leupeptin) showed minimal to moderate effects on PRL and GH release.

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  • Tripeptide aldehydes, especially those with a C-terminal lysine, significantly inhibited PRL and, to a lesser extent, GH release.
  • Boc-DPhe-Phe-lysinal was the most potent inhibitor, reducing PRL release by over 50% at 10(-4) M.

    • Conclusions:

    • Specific tripeptide aldehydes represent potent inhibitors of prolactin and growth hormone release.
    • Further research is needed to elucidate the precise mechanism and site of action for these tripeptide aldehyde inhibitors.