Department of Traditional Chinese Medicine, the First Affiliated Hospital of Liaoning Medical University, Jinzhou 121000, China.
J Ethnopharmacol. 2013 Jul 9;148(2):682-90. doi: 10.1016/j.jep.2013.05.029. Epub 2013 May 21.
The heartwood of Caesalpinia sappan L. (Leguminosae), a widely used Chinese medicine in folk, has been used for the treatment of traumatic injury, stasis pain, amenorrhea, dysmenorrheal, as well as stabbing pain in the chest, abdomen and so on. Protosappanin B and brazilin, as the major bioactive homoisoflavones of Sappan Lignum, are used as the marker components for the quality control of the herb in China Pharmacopoeia.
To establish a sensitive LC/MS/MS method for investigating the pharmacokinetic properties of protosappanin B and brazilin in rats after oral administration of Sappan Lignum extract, and compare their pharmacokinetics difference between normal and streptozotocin-treated rats.
A rapid, selective and sensitive LC/MS/MS method was developed and validated for the simultaneous quantification of protosappanin B and brazilin in rat plasma. Normal and streptozotocin-treated rats were orally administered with the Sappan Lignum extract at the same dose of 2.83 g extract/kg body weight (equivalent to 35.56 mg/kg of protosappanin B and 52.25 mg/kg of brazilin), respectively.
After oral administration of Sappan Lignum extract, a remarkable increase (p<0.05) in the value of AUC0-24h, AUC0-∞, Cmax and T1/2 associated with protosappanin B and brazilin was observed in the streptozotocin-treated group. Compared with the normal rats, elimination of both compounds in the streptozotocin-treated rats was slower.
The established method was successfully applied to compare the pharmacokinetic behaviors of protosappanin B and brazilin in rat plasma after oral administration of Sappan Lignum extract between normal and streptozotocin-treated groups; the results might suggest the accumulation of both compounds in diabetic pathologic states and the adverse reaction should be considered when it was used.
苏木（豆科）的心材，一种民间广泛应用的中药，已被用于治疗创伤、瘀痛、闭经、痛经、以及胸痛、腹痛等刺痛。原苏木素 B 和巴西红，作为苏木属植物的主要生物活性异黄酮，被用作中国药典中该草药的质量控制的标记成分。
建立一种灵敏的 LC/MS/MS 方法，用于研究口服苏木提取物后原苏木素 B 和巴西红在大鼠体内的药代动力学特性，并比较正常和链脲佐菌素处理的大鼠之间的药代动力学差异。
建立并验证了一种快速、选择性和灵敏的 LC/MS/MS 方法，用于同时定量大鼠血浆中的原苏木素 B 和巴西红。正常和链脲佐菌素处理的大鼠分别以 2.83 克提取物/公斤体重（相当于 35.56 毫克/公斤原苏木素 B 和 52.25 毫克/公斤巴西红）的相同剂量口服给予苏木提取物。
口服苏木提取物后，链脲佐菌素处理组原苏木素 B 和巴西红的 AUC0-24h、AUC0-∞、Cmax 和 T1/2 值显著增加（p<0.05）。与正常大鼠相比，链脲佐菌素处理大鼠体内两种化合物的消除速度较慢。
该方法成功地应用于比较正常和链脲佐菌素处理组大鼠口服苏木提取物后原苏木素 B 和巴西红在大鼠血浆中的药代动力学行为；结果可能表明两种化合物在糖尿病病理状态下的积累，当使用时应考虑不良反应。
