Department of Pharmacology and Key Lab of Basic Pharmacology of Guizhou, Zunyi Medical College, Zunyi 563003.
Exp Biol Med (Maywood). 2011 Feb;236(2):233-9. doi: 10.1258/ebm.2010.010247.
Realgar (As(4)S(4)) and cinnabar (HgS) are frequently included in traditional Chinese medicines and Indian Ayurvedic medicines. Both As and Hg are well known for toxic effects, and their safety is of concern. The aim of this study was to compare chronic nephrotoxicity of An-Gong-Niu-Huang Wan (AGNH), realgar and cinnabar with common arsenicals and mercurials. Mice were orally administrated with AGNH (3 g/kg, 6-fold of clinical dose), cinnabar (0.3 g/kg, amount in AGNH) and realgar (0.3 g/kg, amount in AGNH), HgCl(2) (0.118 mmol/kg, 1/10 of cinnabar), MeHg (0.012 mmol/kg, 1/100 of cinnabar), NaAsO(2) (As(3+) 0.028 mmol/kg, 1/100 of realgar) or Na(2)HAsO(4) (As(5+) 0.056 mmol/kg, 1/50 of realgar), daily for six weeks, and nephrotoxicity was examined. Animal body weights were decreased by MeHg and HgCl(2). Blood urea nitrogen and creatinine levels were elevated by MeHg. Renal pathology was severe in the MeHg and HgCl(2) groups, moderate in the arsenite, arsenate and realgar groups and mild in the cinnabar and AGNH groups. Renal Hg accumulation in the MeHg and HgCl(2) groups was 50-200 folds higher than the cinnabar group. Expressions of metallothionein-1 and heme oxygenase-1, biomarkers for metal toxicity, were increased 2-5 folds by arsenite, arsenate, MeHg and HgCl(2), but not by realgar, cinnabar and AGNH. The chemokine and glutathione-S transferase-α4, markers for inflammation, were also increased by MeHg and HgCl(2). Expressions of cell adhesion gene S100a9 and E-cadherin were altered by HgCl(2), arsenite and realgar. Taken together, chemical forms of mercury and arsenic are major determinants in their disposition and toxicity.
雄黄(As(4)S(4)) 和朱砂(HgS)经常被包含在中药和印度阿育吠陀药物中。砷 (As) 和汞 (Hg) 都以毒性作用而闻名,它们的安全性令人担忧。本研究旨在比较安宫牛黄丸 (AGNH)、雄黄和朱砂与常见的砷剂和汞剂的慢性肾毒性。小鼠经口给予 AGNH(3 g/kg,临床剂量的 6 倍)、朱砂(0.3 g/kg,AGNH 中的量)和雄黄(0.3 g/kg,AGNH 中的量)、HgCl(2)(0.118 mmol/kg,朱砂的 1/10)、MeHg(0.012 mmol/kg,朱砂的 1/100)、NaAsO(2)(As(3+) 0.028 mmol/kg,雄黄的 1/100)或 Na(2)HAsO(4)(As(5+) 0.056 mmol/kg,雄黄的 1/50),每天一次,共 6 周,检查肾毒性。MeHg 和 HgCl(2) 导致动物体重减轻。MeHg 使血尿素氮和肌酐水平升高。MeHg 和 HgCl(2) 组的肾脏病理严重,亚砷酸盐、砷酸盐和雄黄组的肾脏病理中度,朱砂和 AGNH 组的肾脏病理轻度。MeHg 和 HgCl(2) 组的肾汞积累量比朱砂组高 50-200 倍。金属毒性生物标志物金属硫蛋白-1 和血红素加氧酶-1 的表达在亚砷酸盐、砷酸盐、MeHg 和 HgCl(2) 作用下增加了 2-5 倍,但在雄黄、朱砂和 AGNH 作用下没有增加。趋化因子和谷胱甘肽-S-转移酶-α4,炎症标志物,也被 MeHg 和 HgCl(2) 增加。HgCl(2)、亚砷酸盐和雄黄改变了细胞黏附基因 S100a9 和 E-钙黏蛋白的表达。综上所述,汞和砷的化学形式是决定其分布和毒性的主要因素。