School of Pharmacy and Health Sciences, International Medical University, No. 126, Jalan 19/155B, 57000 Bukit Jalil, Kuala Lumpur, Malaysia.
J Ethnopharmacol. 2009 Dec 10;126(3):406-14. doi: 10.1016/j.jep.2009.09.025. Epub 2009 Sep 22.
Euphorbia hirta (E. hirta) is a weed commonly found in tropical countries and has been used traditionally for asthma, bronchitis and conjunctivitis. However, one of the constituents in this plant, quercetin, was previously reported to be mutagenic. This work aimed to determine the level of quercetin in the aqueous and methanol plant extracts and to investigate the mutagenic effects of quercetin and the extracts in the Ames test utilising the mutant Salmonella typhimurium TA98 and TA100 strains. The antimutagenic activity of Euphorbia hirta aqueous and methanol extracts was also studied in Salmonella typhimurium TA98. HPLC analyses showed that quercetin and rutin, a glycosidic form of quercetin, were present in the acid-hydrolysed methanol extract and non-hydrolysed methanol extract respectively. The quercetin concentration was negligible in both non-hydrolysed and acid-hydrolysed aqueous extracts. The total phenolic contents in Euphorbia hirta were determined to be 268 and 93 mg gallic acid equivalent (GAE) per gram of aqueous and methanol extracts, respectively. Quercetin (25 microg/mL) was found to be strongly mutagenic in Salmonella typhimurium TA98 in the absence and presence of S-9 metabolic activation. However, both the aqueous and methanol extracts did not demonstrate any mutagenic properties when tested with Salmonella typhimurium TA98 and TA100 strains at concentrations up to 100 microg/mL in the absence and presence of S-9 metabolic activation. In the absence of S-9 metabolic activation, both the extracts were unable to inhibit the mutagenicity of the known mutagen, 2-nitrofluorene, in Salmonella typhimurium TA98. On the other hand, the aqueous extracts at 100 microg/mL and methanol extracts at 10 and 100 microg/mL exhibited strong antimutagenic activity against the mutagenicity of 2-aminoanthracene, a known mutagen, in the presence of S-9 metabolic activating enzymes. The results indicated that these extracts could modulate the xenobiotic metabolising enzymes in the liver at the higher concentrations.
飞扬草(E. hirta)是一种常见于热带国家的杂草,传统上用于治疗哮喘、支气管炎和结膜炎。然而,该植物的一种成分槲皮素以前曾被报道具有致突变性。本工作旨在测定水提和甲醇提植物提取物中槲皮素的含量,并利用突变型鼠伤寒沙门氏菌 TA98 和 TA100 菌株,在 Ames 试验中研究槲皮素和提取物的致突变作用。还研究了飞扬草水提和甲醇提提取物在鼠伤寒沙门氏菌 TA98 中的抗突变活性。HPLC 分析表明,酸水解甲醇提取物和非水解甲醇提取物中分别存在槲皮素和槲皮素的糖苷形式芦丁。非水解和酸水解水提物中槲皮素的浓度可忽略不计。飞扬草中的总酚含量分别为水提物和甲醇提物每克含 268 和 93 毫克没食子酸当量(GAE)。在缺乏和存在 S-9 代谢激活的情况下,25μg/mL 的槲皮素在鼠伤寒沙门氏菌 TA98 中表现出很强的致突变性。然而,在缺乏和存在 S-9 代谢激活的情况下,水提物和甲醇提物在 100μg/mL 及以下浓度时,用鼠伤寒沙门氏菌 TA98 和 TA100 菌株检测均未显示出任何致突变特性。在缺乏 S-9 代谢激活的情况下,两种提取物均不能抑制已知致突变剂 2-硝基芴在鼠伤寒沙门氏菌 TA98 中的致突变性。另一方面,在存在 S-9 代谢激活酶的情况下,水提物在 100μg/mL 时和甲醇提物在 10μg/mL 和 100μg/mL 时对 2-氨基蒽的致突变性表现出很强的抗突变活性,2-氨基蒽是一种已知的致突变剂。结果表明,这些提取物在较高浓度下可以调节肝脏中的异生物质代谢酶。