Keogh R W, Bundick R V, Cunnington P G, Jenkins S N, Blackham A, Orr T S
Agents Actions. 1981 Jul;11(4):361-72. doi: 10.1007/BF01982472.
A tricyclic chromone, proxicromil (sodium 6,7,8,9-tetrahydro-5-hydroxy-4-oxo-10-propyl-naphtho (2,3-b) pyran-2-carboxylate), has been tested for activity against certain immunological and inflammatory reactions. When given parenterally it suppressed the development of delayed hypersensitivity reactions in sensitized mice and guinea-pigs but did not affect the rejection of skin allografts in mice. The compound had no activity against certain in vitro correlates of delayed hypersensitivity reactions (lymphocyte transformation and lymphokine activity), but did have an inhibitory effect on lymphokine (MIF) productions at 10(-4) M but not at 10(-5) M. Proxicromil was also found to be active in non-immunologically mediated models of inflammation and in models having an immunological component which are known to be sensitive to non-steroidal anti-inflammatory drugs (adjuvant arthritis, reversed passive Arthus reaction). The activity of this compound was enhanced when administered in arachis oil when compared to its activity in saline. Proxicromil has not direct activity on the development of immune responsiveness but appear to suppress the expression of delayed hypersensitivity and immune complex mediated hypersensitivity reactions by virtue and its anti-inflammatory properties. This activity is not associated with inhibition of cyclo-oxygenase.
一种三环色酮,丙氧苯柳胺(6,7,8,9-四氢-5-羟基-4-氧代-10-丙基萘并[2,3-b]吡喃-2-羧酸钠),已针对某些免疫和炎症反应进行了活性测试。经肠胃外给药时,它可抑制致敏小鼠和豚鼠中迟发型超敏反应的发展,但不影响小鼠同种异体皮肤移植的排斥反应。该化合物对迟发型超敏反应的某些体外相关指标(淋巴细胞转化和淋巴因子活性)无活性,但在10(-4)M时对淋巴因子(MIF)的产生有抑制作用,而在10(-5)M时则无此作用。还发现丙氧苯柳胺在非免疫介导的炎症模型以及具有免疫成分且已知对非甾体抗炎药敏感的模型(佐剂性关节炎、反向被动阿瑟斯反应)中具有活性。与在盐水中的活性相比,该化合物在花生油中给药时活性增强。丙氧苯柳胺对免疫反应性的发展没有直接活性,但似乎凭借其抗炎特性抑制迟发型超敏反应和免疫复合物介导的超敏反应的表达。这种活性与环氧化酶的抑制无关。