Institute of Biology, Fen-Edebiyat Fakültesi, Adnan Menderes Universitesi, Aydin, Turkey.
Phytomedicine. 2010 Jan;17(1):55-62. doi: 10.1016/j.phymed.2009.06.001. Epub 2009 Jul 2.
Within the genus Scutellaria various species are used in different folk medicines throughout Asia. Traditional Chinese Medicine (TCM) uses S. baicalensis (Labiatae) to treat various inflammatory conditions. The root shows strong anticancer properties in vitro and was suggested for clinical trials against multiple myeloma. Further, S. barbata was successfully tested against metastatic breast cancer in a phase I/II trial. Therefore, we investigated the anti-cancer properties of S. orientalis L. ssp. carica Edmondson, an endemic subspecies from the traditional medicinal plant S. orientalis L. in Turkey, which is used to promote wound healing and to stop haemorrhage.
Freeze-dried plant material was extracted with petroleum ether, dichloromethane, ethyl acetate, and methanol and the bioactivity of these extracts was analysed by proliferation assay, cell death determination, and by investigating protein expression profiles specific for cell cycle arrest and apoptosis.
The strongest anti-leukemic activity was shown by the methanol extract, which contained apigenin, baicalein, chrysin, luteolin and wogonin, with an IpC50 of 43 microg/ml (corresponding to 1.3mg/ml of dried plant material) which correlated with cyclin D1- and Cdc25A suppression and p21 induction. At 132 microg/ml (=4 mg/ml of the drug) this extract caused genotoxic stress indicated by substantial phosphorylation of the core histone H2AX (gamma-H2AX) followed by activation of caspase 3 and signature-type cleavage of PARP resulting in a 55% apoptosis rate after 48 hours of treatment.
Here, we report for the first time that S. orientalis L. ssp. carica Edmondson exhibited potent anti-leukaemic properties likely through the anti-proliferative effect of baicalein and the genotoxic property of wogonin.
在黄芩属中，不同种被用于亚洲各地的不同民间药物。传统中药（TCM）使用黄芩（唇形科）来治疗各种炎症。其根在体外显示出强烈的抗癌特性，并被建议用于多发性骨髓瘤的临床试验。此外，黄芩在 I/II 期临床试验中成功地用于转移性乳腺癌的治疗。因此，我们研究了来自土耳其传统药用植物黄芩的特有亚种东方黄芩 L. ssp. carica Edmondson 的抗癌特性，该亚种用于促进伤口愈合和止血。
冻干植物材料用石油醚、二氯甲烷、乙酸乙酯和甲醇提取，并通过增殖测定、细胞死亡测定以及研究细胞周期停滞和细胞凋亡特异性的蛋白质表达谱来分析这些提取物的生物活性。
甲醇提取物显示出最强的抗白血病活性，其中含有芹菜素、黄芩素、白杨素、木樨草素和汉黄芩素，IC50 为 43μg/ml（相当于 1.3mg/ml 干植物材料），与细胞周期蛋白 D1 和 Cdc25A 的抑制以及 p21 的诱导相关。在 132μg/ml（相当于 4mg/ml 的药物）时，该提取物引起明显的核心组蛋白 H2AX（γ-H2AX）磷酸化，随后激活 caspase 3，并导致 PARP 的特征性切割，从而导致 48 小时处理后的细胞凋亡率达到 55%，这表明存在遗传毒性应激。
我们首次报道东方黄芩 L. ssp. carica Edmondson 表现出强大的抗白血病特性，可能是通过黄芩素的抗增殖作用和汉黄芩素的遗传毒性作用。
