木犀草素簡介：

木犀草素，多以糖苷的形式存在於多種植物中，這些植物以全葉青蘭、辣椒、野菊花、金銀花、紫甦含量較高。木犀草素具有鎮咳和祛痰作用。據 研究，呼吸道症狀咳嗽、咳痰、喘息，均與氣道慢性炎症有關。如支氣管哮喘、慢性阻塞性肺疾病、慢性咽炎、變應性鼻炎等引起咳嗽、咳痰、喘息，均被認為與局部的炎症浸潤有關，炎症的存在，使得氣道的免疫應答混亂，患者常出現氣道反應性增高。治療的手段首先應該消除氣道的慢性炎症浸潤。目前常用糖皮質激素，以消除氣道炎症。但糖皮質激素的副作用較多，不宜長期應用。研究表明，木犀草素抑制巨噬細胞磷酸化，抑制轉錄因子NF-kB的活性，能夠抑制脂多糖(LPS)誘導的巨噬細胞產生細胞因子IL-6，TNF-a。后兩種細胞因子在炎症機制中扮演非常重要的角色，是反映炎症程度的敏感指標。木犀草素還能提高IFN-γ，降低特異性Ig-E，減少嗜酸性粒細胞的浸潤。另外，木犀草素除了抗炎、抗過敏作用以外，還具有抑制PDE、抗SARS、HIV病毒特性，其原因為抑制SARS病毒前S蛋白的活性，從而阻止其進入宿主細胞。用於治療COPD、支氣管哮喘、以及慢性咽炎、變應性鼻炎等引起的慢性咳嗽。

木犀草素檢測標準

木犀草素檢測（面積歸一法）

色譜條件

色 譜 柱：（ODS）C18 (250MM*4.6MM.孔徑5μm)

流    速：1.0ml/min。

檢測波長：270nm

流 動 相：乙腈:水:磷酸（40:60:0.2）

 

樣品溶液配製

稱取約含10mg左右木犀草素樣品，加入50ml容量瓶中，先加入適量甲醇，超聲充分溶解后定容至刻度線，然後混勻備用。

吸取樣品溶液20u1，注入色譜儀進樣閥，測定。

 

木犀草素檢測(外標法)

色譜條件

色 譜 柱：（ODS）C18(250MM*4.6MM.孔徑5μm)

流    速：1.0ml/min。

檢測波長：270nm

流 動 相：乙腈:水:磷酸（40:60:0.2）

對照品溶液配製

稱取10mg左右木犀草素標品，加入50ml容量瓶中，先加入適量甲醇，充分溶解后定容至刻度線，然後混勻備用。

樣品溶液配製

稱取約含10mg左右木犀草素樣品，加入50ml容量瓶中，先加入適量甲醇，充分溶解后定容至刻度線，然後混勻備用。

測定法

分別吸取對照品和樣品溶液200u1，注入色譜儀進樣閥（滿定量環進樣，重現性好），按照外標法計算樣品含量。

計算公式（因為都是定容到50ml容量瓶中，所以公式可以簡化至如下）

 

                                樣品峰面積×標品稱樣量×標品含量（%）

樣品含量（%）= ------------------------------------------------------------

                                     標品峰面積×樣品稱樣量

木犀草素HPLC圖譜

參考文獻：

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 Sternberg, Kailash Chadha, Alicia Lieberman… in Journal of Neuroinflammation (2009)

25.A study of the antioxidant and membranotropic activities of luteolin using different model systems
Luteolin, a water-insoluble 3′,4′,5 ... of the best-studied representatives of bioflavonoids. Luteolin is an essential food component for humans ... the antioxidant (free-radical scavenging) properties of luteolin

A. M. Popov, A. N. Osipov, E. A. Korepanova, O. N. Krivoshapko… in Biophysics (2016)

26.Inhibitory effects of luteolin isolated fromixeris sonchifolia hance on the proliferation of hepg2 human hepatocellular carcinoma cells
We investigated the anti-proliferative effects of luteolin and apigenin, isolated fromIxeris sonchifolia...Hance, on HepG2 human hepatocellular carcinoma cells. In MTT assay luteolin showed more efficient anti-pr...

Yee Su Bog, Lee Jung Hwa, Chung Hae Young, Im Kwang Sik… in Archives of Pharmacal Research (2003)

27.Evaluation of Luteolin in the Prevention of N-nitrosodiethylamine-induced Hepatocellular Carcinoma Using Animal Model System
Hepatocellular carcinoma (HCC) is one of the commonest tumors worldwide. The treatment of HCC is vital for disease diagnosis and prognosis, as the liver is the most important organ controlling metabolic functions...

K. Balamurugan, J. Karthikeyan in Indian Journal of Clinical Biochemistry (2012)