Lorber A, Jackson W H, Simon T M
Scand J Rheumatol. 1981;10(2):129-37. doi: 10.3109/03009748109095285.
Auranofin (AF) differs significantly from gold sodium thiomalate (GST) in formulation, i.e., aurous gold is stabilized by dual sulfur and phosphorus ligands, has hydrophobic rather than hydrophilic characteristics, and lacks ionic charge. These attributes facilitate: oral absorption of AF, plasma membrane penetration, increase in intracellular lymphocyte gold concentration and perhaps thereby influence lymphocyte function. AF therapy was observed to affect primarily T rather than B lymphocyte function in 16 RA subjects receiving 6 mg of AF per day for an average of 45 weeks (range 20-74 weeks) compared with GST-treated RA subjects. Lymphocytes from AF-treated subjects manifested prompt and sharp declines in mitogen-induced lymphoproliferative response (LPR); suppressed response to skin testing with dinitrochlorobenzene (DNCB); and blebbing of lymphocyte membranes as shown by scanning electron microscopy. Suppression of LPR with AF was approximately 60% after the first week and 80% after 20 weeks of therapy, contrasting with 0% and 30% for the respective intervals in GST-treated subjects. DNCB skin testing of AF patients, indicated 11 of 14, failed to respond, whereas all GST patients responded. Local or systemic fungal, bacterial and/or opportunistic infections were not encountered. The effect of AF on B cell effector function, e.g., suppression of immunoglobulins and rheumatoid factor titer, was less marked when contrasted with GST therapy in RA subjects, as previously reported.
金诺芬（AF）在制剂方面与硫代苹果酸金钠（GST）有显著差异，即一价金通过双硫和磷配体得以稳定，具有疏水而非亲水特性，且不带离子电荷。这些特性有助于：AF的口服吸收、质膜穿透、细胞内淋巴细胞金浓度增加，进而可能影响淋巴细胞功能。在16名类风湿关节炎（RA）患者中，观察到AF治疗主要影响T淋巴细胞功能而非B淋巴细胞功能，这些患者平均45周（范围20 - 74周）每天服用6毫克AF，与接受GST治疗的RA患者相比。来自接受AF治疗患者的淋巴细胞在有丝分裂原诱导的淋巴细胞增殖反应（LPR）中迅速且显著下降；对二硝基氯苯（DNCB）皮肤试验的反应受到抑制；扫描电子显微镜显示淋巴细胞膜出现泡状改变。AF治疗第一周后对LPR的抑制约为60%，治疗20周后为80%，而在接受GST治疗的患者中，相应时间段分别为0%和30%。对AF患者进行DNCB皮肤试验，14例中有11例无反应，而所有GST患者均有反应。未出现局部或全身性真菌、细菌和/或机会性感染。如先前报道，与RA患者中GST治疗相比，AF对B细胞效应功能的影响，例如对免疫球蛋白和类风湿因子滴度的抑制作用不那么明显。
