木犀草素简介：

木犀草素，多以糖苷的形式存在于多种植物中，这些植物以全叶青兰、辣椒、野菊花、金银花、紫苏含量较高。木犀草素具有镇咳和祛痰作用。据 研究，呼吸道症状咳嗽、咳痰、喘息，均与气道慢性炎症有关。如支气管哮喘、慢性阻塞性肺疾病、慢性咽炎、变应性鼻炎等引起咳嗽、咳痰、喘息，均被认为与局部的炎症浸润有关，炎症的存在，使得气道的免疫应答混乱，患者常出现气道反应性增高。治疗的手段首先应该消除气道的慢性炎症浸润。目前常用糖皮质激素，以消除气道炎症。但糖皮质激素的副作用较多，不宜长期应用。研究表明，木犀草素抑制巨噬细胞磷酸化，抑制转录因子NF-kB的活性，能够抑制脂多糖(LPS)诱导的巨噬细胞产生细胞因子IL-6，TNF-a。后两种细胞因子在炎症机制中扮演非常重要的角色，是反映炎症程度的敏感指标。木犀草素还能提高IFN-γ，降低特异性Ig-E，减少嗜酸性粒细胞的浸润。另外，木犀草素除了抗炎、抗过敏作用以外，还具有抑制PDE、抗SARS、HIV病毒特性，其原因为抑制SARS病毒前S蛋白的活性，从而阻止其进入宿主细胞。用于治疗COPD、支气管哮喘、以及慢性咽炎、变应性鼻炎等引起的慢性咳嗽。

木犀草素检测标准

木犀草素检测（面积归一法）

色谱条件

色 谱 柱：（ODS）C18 (250MM*4.6MM.孔径5μm)

流    速：1.0ml/min。

检测波长：270nm

流 动 相：乙腈:水:磷酸（40:60:0.2）

 

样品溶液配制

称取约含10mg左右木犀草素样品，加入50ml容量瓶中，先加入适量甲醇，超声充分溶解后定容至刻度线，然后混匀备用。

吸取样品溶液20u1，注入色谱仪进样阀，测定。

 

木犀草素检测(外标法)

色谱条件

色 谱 柱：（ODS）C18(250MM*4.6MM.孔径5μm)

流    速：1.0ml/min。

检测波长：270nm

流 动 相：乙腈:水:磷酸（40:60:0.2）

对照品溶液配制

称取10mg左右木犀草素标品，加入50ml容量瓶中，先加入适量甲醇，充分溶解后定容至刻度线，然后混匀备用。

样品溶液配制

称取约含10mg左右木犀草素样品，加入50ml容量瓶中，先加入适量甲醇，充分溶解后定容至刻度线，然后混匀备用。

测定法

分别吸取对照品和样品溶液200u1，注入色谱仪进样阀（满定量环进样，重现性好），按照外标法计算样品含量。

计算公式（因为都是定容到50ml容量瓶中，所以公式可以简化至如下）

 

                                样品峰面积×标品称样量×标品含量（%）

样品含量（%）= ------------------------------------------------------------

                                     标品峰面积×样品称样量

木犀草素HPLC图谱

参考文献：

1.López-Lázaro M. Distribution and biological activities of the flavonoid luteolin. Mini Rev Med Chem. 2009;9(1):31–59.

2.Lin Y, Shi R, Wang X, et al. Luteolin, a flavonoid with potential for cancer prevention and therapy. Curr Cancer Drug Targets. 2008;8(7):634–46.

3.Rao PS. Luteolin induces apoptosis in multidrug resistant cancer cells without affecting the drug transporter function: involvement of cell line-specific apoptotic mechanisms. Int J Cancer. 2012;130(11):2703–14.

4.Dajas F, Rivera-Megret F, Blasina F, et al. Neuroprotection by flavonoids. Braz J Med Biol Res. 2003;36:1612–20.

5.Wang J, He Y, Zhang W, et al. Advances in studies on pharmacological effects of luteolin. Chin Bull Life Sci. 2013;25(6):560–5.

6.Han W, Xing Y, Kang T. Advances in studies on biological activities of Luteolin. Yunnan J Tradit Chin Med Matera Med. 2010;31(4):60–2.

7.Ulubelen A, Miski M, Neuman P, et al. Flavonoids of Salvia tomentosa (Labiatae). J Nat Prod. 1979;42(4):261–3.

8.Zhao G, Qin GW, Wang J, et al. Functional activation of monoamine transporters by luteolin and apigenin isolated from the fruit of Perilla frutescens (L.) Britt. Neurochem Int. 2010;56(1):168–76.

9.Separation of a Mixture of Luteolin-7-rutinoside and Luteolin-7-neohesperidoside Isolated from Ligustrum vulgare L.
Simple and rapid TLC and column chromatographic methods have been established for separation of luteolin-7-rutinoside and luteolin- 7-neohesperidoside on polyamide. A flavonoid...Ligustrum vulgare L. HPLC analysi...

Pavel Mučaji, Milan Nagy, Tibor Liptaj… in JPC – Journal of Planar Chromatography – M… (2009)

10.7-O-Methilether luteolin
Natural Compounds (2013)

11.Isoorientin (Luteolin-6-C-β-glucopyranoside)
Natural Compounds (2013)

12.Luteolin and luteolin-7-O-glucoside from dandelion flower suppress iNOS and COX-2 in RAW264.7 cells
Both reactive oxygen- and nitrogen-derived reactive species play important roles in physiological and pathophysiological conditions. Flavones, luteolin and luteolin-7-O-glucoside along with a rich...Taraxacum off...

Chun Hu, David D. Kitts in Molecular and Cellular Biochemistry (2004)

13.Erratum to: Anti-inflammatory effects of luteolin and luteoloside from Taraxacum coreanum in RAW264.7 macrophage cells
Ah Young Lee, Sullim Lee, Hyun Young Kim, Sanghyun Lee… in Applied Biological Chemistry (2016)

14.Erratum to: Palmitoylethanolamide and luteolin ameliorate development of arthritis caused by injection of collagen type II in mice
Daniela Impellizzeri, Emanuela Esposito, Rosanna Di Paola… in Arthritis Research & Therapy (2016)

15.Quercimeritrin and luteolin 7-glucoside in some species of Dipsacaceae
G. N. Zemtsova, V. A. Bandyukova in Chemistry of Natural Compounds (1968)

16.Cinaroside (Luteolin-7-O-glucoside)
Natural Compounds (2013)
17.Dynamics of the accumulation of luteolin 7-glucoside in the leaves ofSalix acutifolia
V. L. Shelyuto, A. A. Kir'yanov, L. P. Smirnova… in Chemistry of Natural Compounds (1986)

18.Anti-tumor activities of luteolin and silibinin in glioblastoma cells: overexpression of miR-7-1-3p augmented luteolin and silibinin to inhibit autophagy and induce apoptosis in glioblastoma in vivo Glioblastoma is the deadliest brain tumor in humans. High systemic toxicity of conventional chemotherapies prompted the search for natural compounds for controlling glioblastoma. The natural flavonoids luteolin (...Mrinmay Chakrabarti, Swapan K. Ray in Apoptosis (2016)

19.Cynaroside and luteolin from Campanula persicifolia and C. rotundifolia
L. S. Teslov, S. V. Teslov in Chemistry of Natural Compounds (1972)

20.Erratum to: Luteolin triggers global changes in the microglial transcriptome leading to a unique anti-inflammatory and neuroprotective phenotype
Correction to Dirscherl K, Karlstetter M, Ebert S, Kraus D, Hlawatsch J, Walczak Y, Moehle C, Fuchshofer R, Langmann T. Luteolin triggers global changes in the microglial transcriptome...J Neuroinflammation 2010,...

Konstantin Dirscherl, Marcus Karlstetter, Stefanie Ebert… in Journal of Neuroinflammation (2012)

21.Erratum to: A new co-ultramicronized composite including palmitoylethanolamide and luteolin to prevent neuroinflammation in spinal cord injury
Irene Paterniti, Daniela Impellizzeri, Rosanna Di Paola… in Journal of Neuroinflammation (2016)

22.Luteolin-7,3′-O-diglucoside
Natural Compounds (2013)

23.Luteolin-5-O-glucoside
Natural Compounds (2013)

24.Immunomodulatory responses of peripheral blood mononuclear cells from multiple sclerosis patients upon in vitro incubation with the flavonoid luteolin: additive effects of IFN-β
The study is aimed to determine the role of luteolin (3',4',5,7-tetrahydroxyflavone), ... -1 was assessed in the culture supernatants. Luteolin reduced, in a dose-dependent manner, ... released by PBMCs in the cu...

Zohara Ster