Institute for Medicinal Plant Research "Dr Josif Pančić", Belgrade, Serbia.
Planta Med. 2012 Mar;78(5):415-27. doi: 10.1055/s-0031-1298172. Epub 2012 Jan 24.
Sideritis scardica Griseb. (ironwort, mountain tea), an endemic plant of the Balkan Peninsula, has been used in traditional medicine in the treatment of gastrointestinal complaints, inflammation, and rheumatic disorders. This study aimed to evaluate its gastroprotective and anti-inflammatory activities. Besides, continuously increasing interest in assessing the role of the plant active constituents preventing the risk of cancer was a reason to make a detailed examination of the investigated ethanol, diethyl ether, ethyl acetate, and N-butanol extracts regarding cytotoxicity. Oral administration of the investigated extracts caused a dose-dependent anti-inflammatory effect in a model of carrageenan-induced rat paw edema. Gastroprotective activity of the extracts was investigated using an ethanol-induced acute stress ulcer in rats. The cytotoxic activity of plant extracts was assessed on PBMC, B16, and HL-60 cells and compared to the cytotoxicity of phenolic compounds identified in extracts. Apoptotic and necrotic cell death were analyzed by double staining with fluoresceinisothiocyanate (FITC)-conjugated annexin V and PI. The developed HPLC method enabled qualitative fingerprint analysis of phenolic compounds in the investigated extracts. Compared to the effect of the positive control, the anti-inflammatory drug indomethacine (4 mg/kg), which produced a 50 % decrease in inflammation, diethyl ether and N-butanol extracts exhibited about the same effect in doses of 200 and 100 mg/kg (53.6 and 48.7 %; 48.4 and 49.9 %, respectively). All investigated extracts produced dose-dependent gastroprotective activity with the efficacy comparable to that of the reference drug ranitidine. The diethyl ether extract showed significant dose-dependent cytotoxicity on B16 cells and HL-60 cells, decreasing cell growth to 51.3 % and 77.5 % of control, respectively, when used at 100 µg/mL. It seems that phenolic compounds (apigenin, luteolin, and their corresponding glycosides) are responsible for the diethyl ether extract cytotoxic effect. It also appears that induction of oxidative stress might be involved in its cytotoxicity, since B16 and HL-60 cells increased their ROS production in response to treatment with diethyl ether extract. Neither of the tested extracts nor any phenolic compounds showed significant cytotoxic effect to human PBMC. These results demonstrated the potent anti-inflammatory and gastroprotective activities, as well as the promising cytotoxicity.
铁线莲属植物 Scardica（铁线莲，高山茶）是巴尔干半岛的特有植物，在传统医学中用于治疗胃肠道不适、炎症和风湿性疾病。本研究旨在评估其胃保护和抗炎活性。此外，人们对评估植物活性成分预防癌症风险的作用的兴趣不断增加，这也是对所研究的乙醇、二乙醚、乙酸乙酯和正丁醇提取物进行详细检查的原因。在角叉菜胶诱导的大鼠爪肿胀模型中，口服给予所研究的提取物可产生剂量依赖性抗炎作用。使用乙醇诱导的大鼠急性应激性溃疡研究了提取物的胃保护活性。用 PBMC、B16 和 HL-60 细胞评估植物提取物的细胞毒性，并将其与提取物中鉴定的酚类化合物的细胞毒性进行比较。通过用异硫氰酸荧光素（FITC）缀合的 annexin V 和 PI 双重染色分析细胞凋亡和坏死。开发的 HPLC 方法能够对所研究的提取物中酚类化合物进行定性指纹分析。与阳性对照抗炎药物吲哚美辛（4 mg/kg）相比，产生 50%的炎症减少，二乙醚和正丁醇提取物在 200 和 100 mg/kg 剂量下表现出相似的效果（分别为 53.6%和 48.7%；48.4%和 49.9%）。所有研究的提取物均表现出剂量依赖性的胃保护活性，其疗效与参考药物雷尼替丁相当。二乙醚提取物对 B16 细胞和 HL-60 细胞表现出显著的剂量依赖性细胞毒性，当以 100 µg/mL 使用时，细胞生长分别降至对照的 51.3%和 77.5%。似乎酚类化合物（芹菜素、木犀草素及其相应的糖苷）负责二乙醚提取物的细胞毒性。似乎诱导氧化应激也参与了其细胞毒性，因为 B16 和 HL-60 细胞在响应二乙醚提取物处理时增加了其 ROS 的产生。所测试的提取物或任何酚类化合物对人 PBMC 均无明显的细胞毒性作用。这些结果表明具有强大的抗炎和胃保护活性，以及有希望的细胞毒性。
