Antitumor and antimicrobial activities of lipid A-subunit analogue GLA-27.

Activities for enhancing nonspecific host resistance against microbial infections and growth inhibition against tumors by a lipid A-subunit analogue GLA-27 were investigated. GLA-27, a 4-O-phosphono-D-glucosamine derivative with 2-N-3-tetradecanoyloxytetradecanoyl and 3-O-tetradecanoyl group, inhibited significantly the growth of solid-type tumors RL male 1 lymphoma and Meth A fibrosarcoma. In the case of RL male 1 lymphoma, 2.5 micrograms of GLA-27 was needed to exhibit the activity, while for Meth A fibrosarcoma, 250 micrograms of GLA-27 was needed. On the other hand, tail lesions induced by intravenous inoculation with vaccinia virus were effectively suppressed in mice injected with 1 microgram of GLA-27 1 day before the viral injection. The antiviral activity of GLA-27 was 100 times higher than that of MDP by ED50. GLA-27 also showed nonspecific protective activity against Pseudomonas aeruginosa infection at a dose of 30 micrograms/mouse, although the activity was far less than that induced by lipid A. GLA-27 did not exhibit toxic activities such as pyrogenicity and Shwartzman reaction.
AuthorsM Nakatsuka, Y Kumazawa, S Ikeda, A Yamamoto, C Nishimura, J Y Homma, M Kiso, A Hasegawa
JournalJournal of clinical & laboratory immunology (J Clin Lab Immunol) Vol. 26 Issue 1 Pg. 43-7 (May 1988) ISSN: 0141-2760 [Print] ITALY
PMID3184160 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Adjuvants, Immunologic
  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Antiviral Agents
  • Lipid A
  • GLA 27
  • Adjuvants, Immunologic
  • Animals
  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Antiviral Agents
  • Drug Evaluation, Preclinical
  • Lipid A (analogs & derivatives, pharmacology)
  • Male
  • Mice
  • Mice, Inbred Strains
  • Neoplasms, Experimental (drug therapy)
  • Pseudomonas Infections (drug therapy)
  • Vaccinia (drug therapy)

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