Lorber A, Jackson W H, Simon T M
J Rheumatol Suppl. 1982 Jul-Aug;8:37-45.
Auranofin (AF) differs significantly from gold sodium thiomalate (GSTM) in formulation, i.e., aurous gold is stabilized by dual sulfur and phosphorus ligands, hydrophobic rather than hydrophilic characteristics, and lack of 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 treated subjects recorded prompt and sharp declines in mitogen-induced lymphoproliferative response (LMR) greater than 80%; suppressed response to skin testing with dinitrochlorobenezene (DNCB) in 11 of 14 subjects; and blebbing of lymphocyte membranes by scanning electron microscopy. In contrast, lymphocytes from a matched group of GSTM treated subjects recorded later onset and less suppression of LMR; normal response to DNCB skin testing; and did not manifest membrane blebbing. Accordingly, the therapeutic action of AF on immune response was observed in the 16 subjects receiving 6 mg/d of an average of 45 weeks to effect primarily cell mediated rather than humoral immune response when compared with a matched group of GSTM treated patients.
金诺芬(AF)在制剂方面与硫代苹果酸金钠(GSTM)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;并可能由此影响淋巴细胞功能。接受AF治疗的受试者有丝分裂原诱导的淋巴细胞增殖反应(LMR)迅速且急剧下降超过80%;14名受试者中有11名对二硝基氯苯(DNCB)皮肤试验的反应受到抑制;通过扫描电子显微镜观察到淋巴细胞膜出现泡状突起。相比之下,一组接受GSTM治疗的匹配受试者的淋巴细胞LMR出现较晚且抑制程度较小;对DNCB皮肤试验反应正常;且未出现膜泡状突起。因此,在16名平均接受45周每日6毫克AF治疗的受试者中观察到AF对免疫反应的治疗作用,与一组接受GSTM治疗的匹配患者相比,主要影响细胞介导免疫反应而非体液免疫反应。