Unit Toxicology and Pharmacology, Herbal Medicine Research Center, Institute for Medical Research, Kuala Lumpur, Malaysia.
J Ethnopharmacol. 2011 Jan 27;133(2):647-53. doi: 10.1016/j.jep.2010.10.055. Epub 2010 Oct 29.
Orthosiphon stamineus, Benth, also known as Misai Kucing in Malaysia and Java tea in Indonesia, is traditionally used in Southeastern Asia to treat kidney dysfunctions, diabetes, gout and several other illnesses. Recent studies of Orthosiphon stamineus pharmacological profile have revealed antioxidant properties and other potentially useful biological activities thereby lending some scientific support to its use in folk medicine. So far the genotoxicity of Orthosiphon stamineus extracts has not been evaluated. In this study the genotoxic potential of Orthosiphon stamineus aqueous extract was investigated by the Salmonella/microsome mutation assay and the mouse bone marrow micronucleus test.
Chemical composition of Orthosiphon stamineus aqueous extract was analyzed by High Performance Liquid Chromatography-Diode Array Detector (HPLC-DAD). The Salmonella/microsome assay (TA97a, TA98, TA100 and TA1535; plate incorporation method) was performed in the presence or in the absence of extrinsic metabolic activation (S9 mixture). In the mouse micronucleus assay, Orthosiphon stamineus extract was administered by gavage (0, 500, 2000 and 4000 mg/kg body weight/day for 3 days) to male and female Swiss Webster mice (N=6 per dose per sex) and bone marrow cells were harvested 24 h after the last dose. Ethoxy-resorufin-O-dealkylase (EROD) and benzyloxy-resorufin-O-dealkylase (BROD) activities were determined in mouse liver microsomes.
The chemical analysis revealed that the Orthosiphon stamineus extract contained flavonoids (sinensetin, eupatorin), caffeic acid, and rosmarinic acid (44.00±1.879 μg/mg), the latter seemed to be one of its major constituent. Tested at doses up to 5000 μg/plate, the Orthosiphon stamineus extract was not toxic to Salmonella tester strains and did not increase the number of revertant colonies over the background incidence. In the mouse bone marrow assay, the extract did not alter the polychromatic:normochromatic erythrocytes (PCE:NCE) ratio, nor did it increase the incidence of micronucleated polychromatic erythrocytes (MNPEs). No overt toxicity and no change of CYP1A (EROD) and 2B9/10 (BROD) activities were noted.
Based on the aforementioned findings, it is concluded that the use of Orthosiphon stamineus in the traditional medicine poses no genotoxic risk.
在东南亚，苦荬菜（Orthosiphon stamineus，Benth），又名马来西亚的猫须草和印度尼西亚的爪哇茶，传统上被用于治疗肾脏功能障碍、糖尿病、痛风和其他几种疾病。最近对苦荬菜的药理学研究揭示了其抗氧化特性和其他潜在的有用生物活性，从而为其在民间医学中的应用提供了一些科学依据。到目前为止，苦荬菜提取物的遗传毒性尚未得到评估。在这项研究中，通过沙门氏菌/微粒体突变试验和小鼠骨髓微核试验研究了苦荬菜水提物的遗传毒性潜力。
采用高效液相色谱-二极管阵列检测器（HPLC-DAD）分析苦荬菜水提物的化学成分。在存在或不存在外源性代谢激活（S9 混合物）的情况下，进行沙门氏菌/微粒体试验（TA97a、TA98、TA100 和 TA1535；平板掺入法）。在小鼠微核试验中，雄性和雌性瑞士韦伯斯特小鼠（每组 6 只）经灌胃给予苦荬菜提取物（500、2000 和 4000mg/kg 体重/天，连续 3 天），并在最后一次给药后 24 小时采集骨髓细胞。测定小鼠肝微粒体中的乙氧基-Resorufin-O-脱烷基酶（EROD）和苄氧基-Resorufin-O-脱烷基酶（BROD）活性。
化学分析表明，苦荬菜提取物含有黄酮类化合物（橙皮素、芹黄素）、咖啡酸和迷迭香酸（44.00±1.879μg/mg），后者似乎是其主要成分之一。在高达 5000μg/平板的剂量下，苦荬菜提取物对沙门氏菌测试菌株没有毒性，也没有增加回复突变菌落的数量超过背景发生率。在小鼠骨髓试验中，提取物没有改变多色性/正常红细胞（PCE/NCE）的比值，也没有增加微核多色性红细胞（MNPEs）的发生率。未观察到明显毒性，也未观察到 CYP1A（EROD）和 2B9/10（BROD）活性的改变。
基于上述发现，可以得出结论，在传统医学中使用苦荬菜不会带来遗传毒性风险。
