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肉桂(锡兰肉桂和中国肉桂)提取物的抗炎活性——鉴定反式肉桂醛和邻甲氧基肉桂醛为最具活性的生物活性化合物。

Anti-inflammatory activity of cinnamon (C. zeylanicum and C. cassia) extracts - identification of E-cinnamaldehyde and o-methoxy cinnamaldehyde as the most potent bioactive compounds.

作者信息

Gunawardena Dhanushka, Karunaweera Niloo, Lee Samiuela, van Der Kooy Frank, Harman David G, Raju Ritesh, Bennett Louise, Gyengesi Erika, Sucher Nikolaus J, Münch Gerald

机构信息

School of Medicine, University of Western Sydney, Locked Bag 1797, Penrith, NSW 2751, Australia.

出版信息

Food Funct. 2015 Mar;6(3):910-9. doi: 10.1039/c4fo00680a.

Abstract

Chronic inflammation is a contributing factor in many age-related diseases. In a previous study, we have shown that Sri Lankan cinnamon (C. zeylanicum) was one of the most potent anti-inflammatory foods out of 115 foods tested. However, knowledge about the exact nature of the anti-inflammatory compounds and their distribution in the two major cinnamon species used for human consumption is limited. The aim of this investigation was to determine the anti-inflammatory activity of C. zeylanicum and C. cassia and elucidate their main phytochemical compounds. When extracts were tested in LPS and IFN-γ activated RAW 264.7 macrophages, most of the anti-inflammatory activity, measured by down-regulation of nitric oxide and TNF-α production, was observed in the organic extracts. The most abundant compounds in these extracts were E-cinnamaldehyde and o-methoxycinnamaldehyde. The highest concentration of E-cinnamaldehyde was found in the DCM extract of C. zeylanicum or C. cassia (31 and 34 mg g(-1) of cinnamon, respectively). When these and other constituents were tested for their anti-inflammatory activity in RAW 264.7 and J774A.1 macrophages, the most potent compounds were E-cinnamaldehyde and o-methoxycinnamaldehyde, which exhibited IC₅₀ values for NO with RAW 264.7 cells of 55 ± 9 μM (7.3 ± 1.2 μg mL(-1)) and 35 ± 9 μM (5.7 ± 1.5 μg mL(-1)), respectively; and IC₅₀ values for TNF-α of 63 ± 9 μM (8.3 ± 1.2 μg mL(-1)) and 78 ± 16 μM (12.6 ± 2.6 μg mL(-1)), respectively. If therapeutic concentrations can be achieved in target tissues, cinnamon and its components may be useful in the treatment of age-related inflammatory conditions.

摘要

慢性炎症是许多与年龄相关疾病的一个促成因素。在之前的一项研究中,我们已经表明,在测试的115种食物中,斯里兰卡肉桂(锡兰肉桂)是最有效的抗炎食物之一。然而,关于抗炎化合物的确切性质及其在用于人类食用的两种主要肉桂品种中的分布的知识是有限的。本研究的目的是确定锡兰肉桂和桂皮的抗炎活性,并阐明其主要植物化学化合物。当提取物在脂多糖(LPS)和干扰素-γ(IFN-γ)激活的RAW 264.7巨噬细胞中进行测试时,通过一氧化氮和肿瘤坏死因子-α(TNF-α)产生的下调来衡量的大部分抗炎活性在有机提取物中被观察到。这些提取物中最丰富的化合物是反式肉桂醛和邻甲氧基肉桂醛。在锡兰肉桂或桂皮的二氯甲烷(DCM)提取物中发现反式肉桂醛的最高浓度(分别为每克肉桂31毫克和34毫克)。当这些及其他成分在RAW 264.7和J774A.1巨噬细胞中测试其抗炎活性时,最有效的化合物是反式肉桂醛和邻甲氧基肉桂醛,它们对RAW 264.7细胞中一氧化氮的半数抑制浓度(IC₅₀)值分别为55±9微摩尔(7.3±1.2微克/毫升)和35±9微摩尔(5.7±1.5微克/毫升);对TNF-α的IC₅₀值分别为63±9微摩尔(8.3±1.2微克/毫升)和78±16微摩尔(12.6±2.6微克/毫升)。如果能在靶组织中达到治疗浓度,肉桂及其成分可能有助于治疗与年龄相关的炎症性疾病。

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