Division of Urology, Department of Surgery, Chi Mei Medical Center, No.21, Taikang, Liuying Dist., Tainan City 73657, Taiwan.
Molecules. 2012 May 25;17(6):6277-89. doi: 10.3390/molecules17066277.
Cantharidin, an active component in mylabris, is used in traditional Chinese medicine (TCM) to treat scabies and hepatoma, but accompanied by hemorrhagic cystitis. Evidence shows that cantharidin induces human bladder carcinoma cell death through COX-2 overexpression in vitro. In TCM, Scutellaria baicalensis is usually used to cure mylabris-induced hematuria. This work was undertaken to determine the mechanisms of cantharidin-induced rat hemorrhagic cystitis and explore the uroprotective effect of S. baicalensis. In vitro results showed cantharidin could induce cytotoxicity through prostaglandin (PG)E₂ overproduction of T24 cells. Boiling-water extract of S. baicalensis (SB-WE) could significantly inhibit PGE₂ production and COX-2 expression in lipo-polysaccharide-induced RAW 264.7 cells, indicating obvious anti-inflammatory abilities. In vivo results indicated that cantharidin caused rat hemorrhagic cystitis with hematuria via c-Fos and COX-2 overexpression. SB-WE was given orally to cantharidin-treated rats, whereby hematuria level, elevated PGE₂ and COX-2 protein overexpression were significantly and dose-dependently inhibited by SB-WE. The anti-inflammatory components of SB-WE are baicalin and wogonin, whose contents were 200.95 ± 2.00 and 31.93 ± 0.26 μg/mg, respectively. In conclusion, cantharidin induces rat cystitis through c-Fos and COX-2 over-expression and S. baicalensis can prevent the resulting hematuria because of its anti-inflammatory effects.
斑蝥素是芫青科昆虫南方大斑蝥或黄黑小斑蝥的干燥体，在传统中药（TCM）中用于治疗疥疮和肝癌，但伴有出血性膀胱炎。有证据表明，斑蝥素通过体外 COX-2 的过表达诱导人膀胱癌细胞死亡。在 TCM 中，黄芩通常用于治疗斑蝥素引起的血尿。本工作旨在确定斑蝥素诱导大鼠出血性膀胱炎的机制，并探讨黄芩的尿保护作用。体外结果表明，斑蝥素可通过 T24 细胞前列腺素（PG）E₂的过产生诱导细胞毒性。黄芩的沸水提取物（SB-WE）可显著抑制脂多糖诱导的 RAW 264.7 细胞中 PGE₂的产生和 COX-2 的表达，表明具有明显的抗炎能力。体内结果表明，斑蝥素通过 c-Fos 和 COX-2 的过表达导致大鼠出血性膀胱炎和血尿。将 SB-WE 口服给予斑蝥素处理的大鼠，SB-WE 可显著抑制血尿水平、升高的 PGE₂和 COX-2 蛋白过表达，且呈剂量依赖性。SB-WE 的抗炎成分是黄芩苷和汉黄芩素，其含量分别为 200.95±2.00 和 31.93±0.26μg/mg。总之，斑蝥素通过 c-Fos 和 COX-2 的过表达诱导大鼠膀胱炎，黄芩具有抗炎作用，可预防由此引起的血尿。
