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黑种草籽油及其衍生的百里醌可抑制白细胞中类花生酸的生成以及膜脂质过氧化。

Fixed oil of Nigella sativa and derived thymoquinone inhibit eicosanoid generation in leukocytes and membrane lipid peroxidation.

作者信息

Houghton P J, Zarka R, de las Heras B, Hoult J R

机构信息

Department of Pharmacy, King's College London, U.K.

出版信息

Planta Med. 1995 Feb;61(1):33-6. doi: 10.1055/s-2006-957994.

Abstract

Samples of the expressed fixed oil from different sources of Nigella sativa seeds were examined by thin-layer and gas chromatography for content of fixed oils and thymoquinone, and these substances were tested as possible inhibitors of eicosanoid generation and membrane lipid peroxidation. The crude fixed oil and pure thymoquinone both inhibited the cyclooxygenase and 5-lipoxygenase pathways of arachidonate metabolism in rat peritoneal leukocytes stimulated with calcium ionophore A23187, as shown by dose-dependent inhibition of thromboxane B2 and leukotriene B4, respectively. Thymoquinone was very potent, with approximate IC50 values against 5-lipoxygenase and cyclo-oxygenase of < 1 microgram/ml and 3.5 micrograms/ml, respectively. Both substances also inhibited non-enzymatic peroxidation in ox brain phospholipid liposomes, but thymoquinone was about ten times more potent. However, the inhibition of eicosanoid generation and lipid peroxidation by the fixed oil of N. sativa is greater than is expected from its content of thymoquinone (ca. 0.2% w/v), and it is possible that other components such as the unusual C20:2 unsaturated fatty acids may contribute also to its anti-eicosanoid and antioxidant activity. These pharmacological properties of the oil support the traditional use of N. sativa and its derived products as a treatment for rheumatism and related inflammatory diseases.

摘要

对来自不同来源的黑种草籽所提取的固定油样本进行了薄层色谱和气相色谱分析,以测定固定油和百里醌的含量,并对这些物质作为类花生酸生成和膜脂质过氧化的潜在抑制剂进行了测试。粗制固定油和纯百里醌均抑制了用钙离子载体A23187刺激的大鼠腹膜白细胞中花生四烯酸代谢的环氧化酶和5-脂氧合酶途径,分别表现为对血栓素B2和白三烯B4的剂量依赖性抑制。百里醌的活性很强,对5-脂氧合酶和环氧化酶的半数抑制浓度(IC50)值分别约为<1微克/毫升和3.5微克/毫升。这两种物质还抑制了牛脑磷脂脂质体中的非酶促过氧化反应,但百里醌的效力约强十倍。然而,黑种草籽固定油对类花生酸生成和脂质过氧化的抑制作用大于根据其百里醌含量(约0.2%w/v)所预期的效果,并且其他成分如不寻常的C20:2不饱和脂肪酸也可能对其抗类花生酸和抗氧化活性有贡献。该油的这些药理特性支持了黑种草及其衍生产品作为治疗风湿病和相关炎症性疾病的传统用途。

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