Loppnow H, Brade L, Brade H, Rietschel E T, Kusumoto S, Shiba T, Flad H D
Eur J Immunol. 1986 Oct;16(10):1263-7. doi: 10.1002/eji.1830161013.
Lipopolysaccharides (LPS) are well known inducers of interleukin 1 (IL 1). Here we show that synthetic heptaacyl Salmonella minnesota (compound 516) and synthetic E. coli type (compound 506) lipid A, as well as monodephospho part structures thereof, are able to induce IL 1 production in human mononuclear cells. The 4'-monodephospho part structure (compound 505) was found to be the most active IL 1 inducer as compared to compound 506 and the 1-monodephospho part structure (compound 504). Synthetic lipid A precursor Ia, lacking nonhydroxylated fatty acids (compound 406), and its 1- or 4'-monodephospho part structures (compounds 404 and 405) did not induce IL 1 production. IL 2 is not produced during stimulation with the synthetic compounds. IL 1 activity was partially heat labile and could be inhibited by a rabbit antiserum against human leukocytic pyrogen. These results show that the lipid A component of LPS is active in inducing IL 1 and that the presence of 3-acyloxyacyl residues is necessary for IL 1 induction.
脂多糖（LPS）是众所周知的白细胞介素1（IL - 1）诱导剂。在此我们表明，合成的七酰基明尼苏达沙门氏菌（化合物516）和合成的大肠杆菌型（化合物506）脂多糖A，以及它们的单去磷酸化部分结构，能够在人单核细胞中诱导IL - 1的产生。与化合物506和1 - 单去磷酸化部分结构（化合物504）相比，发现4' - 单去磷酸化部分结构（化合物505）是最活跃的IL - 1诱导剂。缺乏非羟基化脂肪酸的合成脂多糖A前体Ia（化合物406）及其1 - 或4' - 单去磷酸化部分结构（化合物404和405）不诱导IL - 1的产生。在用合成化合物刺激过程中不产生IL - 2。IL - 1活性部分对热不稳定，并且可以被抗人白细胞热原的兔抗血清抑制。这些结果表明，LPS的脂多糖A成分在诱导IL - 1方面具有活性，并且3 - 酰氧基酰基残基的存在对于IL - 1的诱导是必要的。
