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绵枣儿鳞茎乙酸乙酯提取物对脂氧合酶和透明质酸酶活性的抑制作用。

Inhibitory effects of the ethyl acetate extract from bulbs of Scilla scilloides on lipoxygenase and hyaluronidase activities.

作者信息

Nishida Youichirou, Sugahara Shintaro, Wada Kensuke, Toyohisa Daiki, Tanaka Toshiharu, Ono Masateru, Yasuda Shin

机构信息

Department of Bioscience, School of Agriculture, Tokai University , Kawayo, Minamiaso, Aso, Kumamoto , Japan and.

出版信息

Pharm Biol. 2014 Oct;52(10):1351-7. doi: 10.3109/13880209.2014.891140. Epub 2014 Jul 15.

Abstract

CONTEXT

Scilla scilloides Druce (Liliaceae) is a folk medicine to treat dermal inflammation; however, the medicinal properties of this plant have not been completely established.

OBJECTIVE

The current study investigates the potent anti-inflammatory effects of S. scilloides bulbs for its traditional usage using lipoxygenase and hyaluronidase as the inflammation model. To gain insight into the active constituents, nine homoisoflavones (1-9) were subsequently tested.

MATERIALS AND METHODS

Lipoxygenase and hyaluronidase inhibition of ethyl acetate extract from the bulbs of this plant within 2000 µg/mL or homoisoflavones within 1000 µM were determined by colorimetric methods. RAW264.7 cells were incubated with 10 or 50 µM homoisoflavones plus lipopolysaccharide (LPS) for 24 h. The culture media were collected and analyzed for determination of the nitric oxide (NO) level by the colorimetric Griess method to measure the extent of inflammation.

RESULTS

The extract exhibited inhibitory effects on lipoxygenase and hyaluronidase activities with IC50 values 31.5 and 169 µg/mL, respectively. Among the nine homoisoflavones tested, four (1 and 3-5) resulted in 79.3-97.9% higher lipoxygenase inhibition than 6.7-32.7% of the others at 500 µM. Calculated IC50 values indicated 5 as the compound responsible for strong lipoxygenase inhibition with 15.8 µM as the IC50 value. In the hyaluronidase assay, all homoisoflavones tested at 1000 µM demonstrated 16.2-58.0% inhibition. Incubating the cells in the presence of all nine homoisoflavones tested at 50 µM significantly suppressed the NO production, downward to 1.5-66.0%, in the LPS-activated macrophage cells as a model.

DISCUSSION AND CONCLUSION

These results may indicate a potential role of S. scilloides for anti-inflammatory purposes.

摘要

背景

绵枣儿(百合科)是一种用于治疗皮肤炎症的民间药物;然而,这种植物的药用特性尚未完全明确。

目的

本研究以脂氧合酶和透明质酸酶为炎症模型,探究绵枣儿鳞茎因其传统用途所具有的强效抗炎作用。为深入了解其活性成分,随后对9种高异黄酮(1 - 9)进行了测试。

材料与方法

采用比色法测定该植物鳞茎乙酸乙酯提取物在2000μg/mL以内或高异黄酮在1000μM以内对脂氧合酶和透明质酸酶的抑制作用。将RAW264.7细胞与10或50μM高异黄酮加脂多糖(LPS)孵育24小时。收集培养基,采用比色Griess法分析测定一氧化氮(NO)水平,以衡量炎症程度。

结果

该提取物对脂氧合酶和透明质酸酶活性具有抑制作用,IC50值分别为31.5和169μg/mL。在测试的9种高异黄酮中,4种(1和3 - 5)在500μM时对脂氧合酶的抑制率比其他几种高79.3 - 97.9%,而其他几种的抑制率为6.7 - 32.7%。计算得出的IC50值表明化合物5是导致强效脂氧合酶抑制作用的物质,其IC50值为15.8μM。在透明质酸酶测定中,所有测试的高异黄酮在1000μM时的抑制率为16.2 - 58.0%。以LPS激活的巨噬细胞为模型,在50μM下测试的所有9种高异黄酮存在时孵育细胞,可显著抑制NO生成,抑制率降至1.5 - 66.0%。

讨论与结论

这些结果可能表明绵枣儿在抗炎方面具有潜在作用。

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