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The development of VIP-ellipticine conjugates

  1. Author:
    Moody, T. W.
    Czerwinski, G.
    Tarasova, N. I.
    Moody, D. L.
    Michejda, C. J.

  2. Author Address

    NCI, Off Director, CCR, Dept Hlth & Human Serv, Bethesda, MD 20892 USA. NCI, Adv Biosci Labs, Macromol Struct Lab, Mol Aspects Drug Design Sect, Ft Detrick, MD 21702 USA Moody, TW, NCI, Off Director, CCR, Dept Hlth & Human Serv, Bldg 31,Room 3A34,31 Ctr Dr, Bethesda, MD 20892 USA
    1. Year: 2004
    2. Date: DEC 15
  2. Journal: Regulatory Peptides
    1. 123
    2. 1-3
    3. Pages: 187-192
  4. Type of Article: Article
  1. Abstract:

    The mechanism by which vasoactive intestinal peptide (VIP)-ellipticine (E) conjugates are cytotoxic for human lung cancer cells was investigated. VIP-alanyl-leucyl-alanyl-leucyl-alanine (ALALA)-E and VIP-leucyl-alanyl-leucyl-alanine (LALA)-E inhibited I-125-VIP binding to NCI-H1299 cells with an IC50 values of 0.5 and 0.1 muM, respectively. VIP-ALALA-E and VIP-LALA-E caused elevation of cAMP in NCI-H1299 cells with ED50 values of 0.7 and 0.1 muM. Radiolabeled VIP-LALA-E was internalized at 37degreesC and delivered the cytotoxic E into NCI-H1299 cells. VIP-LALA-E inhibited the growth of NCI-H1299 cells in vitro. Three days after the addition of VIP LALA-E to NCI-HI299 cells, cell viability decreased based on trypan blue exclusion and reduced 3 H-thymidine uptake. These results suggest that VIP-E conjugates are internalized in lung cancer cells as a result of VPAC(1) receptor-mediated endocytosis. (C) 2004 Elsevier B.V. All rights reserved

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External Sources

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  2. DOI: 10.1016/j.regpep.2004.03.021
  3. View record in Web of Science®
  4. WOS: 000225154400027

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