Whitehouse M W, Rainsford K D, Taylor R M, Vernon-Roberts B
Department of Pathology, University of Adelaide, South Australia.
Agents Actions. 1990 Aug;31(1-2):47-58. doi: 10.1007/BF02003221.
Zinc repletion by parental administration of zinc monoglycerolate (ZMG) or certain other lipophilic zinc complexes, suppressed the development of adjuvant-induced polyarthritis in rats. While ZMG was effective when given parenterally over various limited time schedules (immunosuppressant, therapeutic, singledose), it was not effective given orally. The complex showed no acute anti-inflammatory activity in the carrageenan paw oedema assay and little gastric-intestinal or other organ toxicity. When injected s.c. it caused very much less local irritation than most zinc salts. Being lubrous, ZMG could be applied as the dry powder for rubbing into the skin and by this route was found to have anti-arthritic activity. 65Zn was shown to be absorbed and excreted in the faeces (biliary excretion) after applying 65Zn-ZMG dermally to shaved dorsal skin of rats. ZMG showed consistent anti-arthritic activity in rats under conditions in which 2 gold drugs (aurothiomalate, Auranofin) exhibited variable effects, depending on the strain of rat. The role of zinc and its availability in chronic inflammation are discussed on the basis of these studies.
通过肠胃外给予甘油单锌(ZMG)或某些其他亲脂性锌络合物来补充锌,可抑制大鼠佐剂诱导的多关节炎的发展。虽然ZMG在不同的有限时间给药方案(免疫抑制剂、治疗性、单剂量)下肠胃外给药时有效,但口服时无效。该络合物在角叉菜胶足爪水肿试验中未显示出急性抗炎活性,且几乎没有胃肠道或其他器官毒性。皮下注射时,它引起的局部刺激比大多数锌盐小得多。由于ZMG具有润滑性,可作为干粉用于擦入皮肤,经此途径发现其具有抗关节炎活性。在大鼠剃毛的背部皮肤经皮应用65Zn-ZMG后,65Zn显示在粪便中被吸收并排泄(胆汁排泄)。在两种金制剂(硫代苹果酸金钠、金诺芬)根据大鼠品系表现出不同效果的条件下,ZMG在大鼠中显示出一致的抗关节炎活性。基于这些研究,讨论了锌及其有效性在慢性炎症中的作用。