Anti-inflammatory and anticancer compounds isolated from Ventilago madraspatana Gaertn., Rubia cordifolia Linn. and Lantana camara Linn.
Anti-inflammatory and anticancer compounds isolated from Ventilago madraspatana Gaertn., Rubia cordifolia Linn. and Lantana camara Linn.
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DOI：
10.1111/j.2042-7158.2010.01151.x
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发表时间：
2010-09-01
影响因子：
3.3
通讯作者：
Hazra, Banasri
中科院分区：
文献类型：
--
作者：
Ghosh, Subhalakshmi;Sarma, Madhushree Das;Hazra, Banasri
目的目的是从三种药用植物中寻找抗炎和抗癌化合物，即： Ventilago madraspatana Gaertn., Rubia cordifolia Linn.方法在LPS/IFN-γ激活的小鼠腹腔巨噬细胞培养物上测定所选植物提取物的NO中心点清除潜力，并通过蛋白质印迹分析评估iNOS和COX-2的表达。生物测定指导下的分级分离产生了四种化合物：来自 V. madraspatana 的大黄素甲醚和大黄素、来自 R. cordifolia 的 1-羟基四氢醌和来自 L. camara 的齐墩果酸。通过角叉菜胶诱导的大鼠爪水肿模型测试了这些化合物的抗炎活性。然后对它们进行了针对小鼠肿瘤（艾氏腹水癌）和三种人类癌细胞系（即 A375（恶性皮肤黑色素瘤）、Hep2（表皮样喉癌）和 U937（淋巴瘤））的测试。 主要发现所有四种化合物通过抑制 iNOS 蛋白，剂量依赖性地抑制 NO 中心点，而不影响巨噬细胞活力。大黄素甲醚和大黄素在 40 mg/kg 剂量下可使水肿体积减少 65-68%，这验证了它们的体内抗炎作用。 1-羟基四氢醌和齐墩果酸对 A375 细胞表现出有希望的细胞毒性。 结论 通过深入了解四种成分的抗炎和抗癌潜力，对这些传统药用植物的民族医学报告已经合理化，这些成分被认为是设计新型治疗剂的潜在候选者。
ObjectivesThe aim was to search for anti-inflammatory and anticancer compounds from three medicinal plants, viz. Ventilago madraspatana Gaertn., Rubia cordifolia Linn. and Lantana camara Linn.MethodsThe NO center dot scavenging potential of selected plant extracts was determined on LPS/IFN-gamma activated murine peritoneal macrophage cultures, and iNOS and COX-2 expression was evaluated by Western blot analysis. Bio-assay guided fractionation yielded four compounds: physcion and emodin from V. madraspatana, 1-hydroxytectoquinone from R. cordifolia, and oleanonic acid from L. camara. The anti-inflammatory activity of these compounds was tested through the carrageenan-induced rat-paw oedema model. They were then tested against a murine tumour (Ehrlich ascites carcinoma), and three human cancer cell lines, namely A375 (malignant skin melanoma), Hep2 (epidermoid laryngeal carcinoma) and U937 (lymphoma).Key findingsAll four compounds dose dependently inhibited NO center dot through suppression of iNOS protein without affecting macrophage viability. Physcion and emodin caused 65-68% reduction of oedema volume at 40 mg/kg, which validated their in-vivo anti-inflammatory effect. 1-hydroxytectoquinone and oleanonic acid exhibited promising cytotoxicity against A375 cells.ConclusionsEthnomedical reports on these traditional medicinal plants have been rationalised through an insight into the anti-inflammatory as well as anticancer potential of four constituents, characterised to be prospective candidates for designing novel therapeutic agents.