Nakatomi I, Nakamura K, Furukawa K, Koda A
Int J Immunopharmacol. 1987;9(2):243-53. doi: 10.1016/0192-0561(87)90099-3.
A newly synthesized anti-allergic agent, cis-1-methyl-4-isohexylcyclohexane carboxylic acid (IG-10), has the capacity to inhibit the effector phase of delayed hypersensitivity reactions. In the present paper, the effect of IG-10 was studied on the generation of superoxide anion (O2) from macrophages, on macrophage chemotaxis, and on the activity of lymphokines such as skin reactive factor (SRF), macrophage migration inhibitory factor (MIF) and monocyte/macrophage chemotactic factor (MCF) in guinea pigs. Oral administration of IG-10 (50-200 mg/kg) inhibited SRF-induced skin erythema in a dose-dependent manner. In vitro, this agent (10(-7) -10(-5) g/ml) did not inhibit the generation of O2- from macrophages. The agent (10(-7) -10(-6) g/ml) significantly inhibited the activity of MIF and this inhibition was not due to the facilitation of normal migration. For macrophage chemotaxis, IG-10 (10(-8) -10(-6) g/ml) significantly inhibited MCF-induced chemotaxis. The agent also depressed the macrophage chemotaxis induced by N-formyl-methionyl-leucyl-phenylalanine but not the chemotaxis induced by E. coli culture filtrate. The inhibitory action of IG-10 on MCF activity was not influenced by antiglucocorticoid agents such as 17 alpha-methyltestosterone and androstenedione which reverse significantly the inhibitory action of glucocorticoids. The inhibitory action of IG-10 was relatively dependent on exogenous Ca2+ and Mg2+, and was antagonized by dbc-GMP.
一种新合成的抗过敏剂，顺式-1-甲基-4-异己基环己烷羧酸（IG-10），具有抑制迟发型超敏反应效应阶段的能力。在本文中，研究了IG-10对豚鼠巨噬细胞超氧阴离子（O₂）生成、巨噬细胞趋化性以及皮肤反应因子（SRF）、巨噬细胞移动抑制因子（MIF）和单核细胞/巨噬细胞趋化因子（MCF）等淋巴因子活性的影响。口服IG-10（50 - 200 mg/kg）以剂量依赖方式抑制SRF诱导的皮肤红斑。在体外，该药剂（10⁻⁷ - 10⁻⁵ g/ml）不抑制巨噬细胞O₂⁻的生成。该药剂（10⁻⁷ - 10⁻⁶ g/ml）显著抑制MIF的活性，且这种抑制并非由于促进正常移动所致。对于巨噬细胞趋化性，IG-10（10⁻⁸ - 10⁻⁶ g/ml）显著抑制MCF诱导的趋化性。该药剂还抑制了N-甲酰甲硫氨酰亮氨酰苯丙氨酸诱导的巨噬细胞趋化性，但不抑制大肠杆菌培养滤液诱导的趋化性。IG-10对MCF活性的抑制作用不受抗糖皮质激素如17α-甲基睾酮和雄烯二酮的影响，这些抗糖皮质激素可显著逆转糖皮质激素的抑制作用。IG-10的抑制作用相对依赖于外源性Ca²⁺和Mg²⁺，并被二丁酰环磷腺苷（dbc-GMP）拮抗。
