Robinson D R, McGuire M B, Bastian D, Kantrowitz F, Levine L
Prostaglandins Med. 1978 Dec;1(6):461-77. doi: 10.1016/0161-4630(78)90117-9.
The effect of anti-inflammatory drugs on prostaglandin production by rheumatoid synovial tissue has been investigated. Synovial explants were maintained in tissue culture for periods up to six days and PGE2 concentrations in culture were determined by radioimmunoassay. The more potent nonsteroidal inhibitors of PGE2 production and their IC50 (micrometer) values were indomethacin 0.005, flufenamic acid 0.2, flurbiprofen 0.6, ibuprofen 2.0 , naproxen 6.0, phenylbutazone 10.0, and aspirin 20.0. Drugs with weak or insignificant effects were hydroxychloroquin, acetaminophen, azathioprine, chloroquin, penicillamine, gold Na thiomalate, and Na salicylate. Glucocorticoids were potent inhibitors; dexamethasone 0.003, prednisolone 0.01, hydrocortisone 0.03; while mineralocorticoids deoxycorticosterone and aldosterone were inactive at 1.0 micrometer. There is a reasonably good correlation between the IC50 concentrations of the nonsteroidal inhibitors and their peak free plasma concentration achieved during therapy in man. Inhibition of prostaglandin synthesis may contribute to the effects of many but not all anti-inflammatory drugs.
已对抗炎药物对类风湿性滑膜组织产生前列腺素的作用进行了研究。将滑膜外植体在组织培养中维持长达6天，并通过放射免疫测定法测定培养物中的PGE2浓度。PGE2产生的更有效的非甾体类抑制剂及其IC50（微米）值分别为：消炎痛0.005、氟灭酸0.2、氟比洛芬0.6、布洛芬2.0、萘普生6.0、保泰松10.0和阿司匹林20.0。作用微弱或不显著的药物有羟基氯喹、对乙酰氨基酚、硫唑嘌呤、氯喹、青霉胺、硫代苹果酸金钠和水杨酸钠。糖皮质激素是有效的抑制剂；地塞米松0.003、泼尼松龙0.01、氢化可的松0.03；而盐皮质激素脱氧皮质酮和醛固酮在1.0微米时无活性。非甾体类抑制剂的IC50浓度与其在人体治疗期间达到的游离血浆峰值浓度之间存在相当良好的相关性。前列腺素合成的抑制可能有助于许多但并非所有抗炎药物的作用。
