Antiviral and immunomodulating activities of chemically synthesized lipid A-subunit analogues GLA-27 and GLA-60

Autor: Chiaki Nishimura, Mitsunobu Nakatsuka, Makoto Kiso, Akira Hasegawa, J. Yuzuru Homma, S. Ikeda
Rok vydání: 1988
Předmět:
Zdroj: Antiviral research. 9(1-2)
ISSN: 0166-3542
Popis: Biological and antiviral activities of chemically synthesized lipid A-subunit analogues, GLA-27 and GLA-60, were investigated with respect to defense mechanisms such as macrophage and natural killer (NK) cell activation and interferon (IFN)-indluding activity. GLA-27, a 4-O- phosphono - D - glucosamine derivative carrying 3-O-tetradecanoyl (C14) and 2-N-3-tetradecanoyloxytetradecanoyl (C14-O-(C14)) group, and GLA-60, a similar analogue carrying 3-O-linked C14-O-(C14) and 3-N-linked 3-hydroxytetradecanoyl (C14-OH) groups, strongly inhibited the formation of pox tail lesions and the growth of vaccinia virus at the tail lesion sites in infected mice. The antiviral activity of GLA-60 was about 1000-fold higher than that of muramyldipeptide (MDP), a representative immunomodulator. GLA-27 and GLA-60 had stronger immunomodulating activity than MDP in macrophage activation, NK cell activation and IFN-inducing activity, although it was weaker than natural lipid A. Toxic manifestations such as pyrogenicity, local Shwartzman reaction and lethality were far less pronounced for GLA-27 and GLA-60 than for natural lipid A.
Databáze: OpenAIRE