General

Scientific Names: Artemisia argyi Lévl. et Van.

Common Names: Ai, Ai Ye, Ai Hao.

BOTANICAL:

来 源： 为双子叶植物药菊科植物艾Artemisia argyi Lévl. et Van的干燥叶。

植物形态 : 多年生草本，高0.5～1.2m。茎直立，被白色细软毛，上部分枝。叶互生，中下部叶片广阔，3～5深裂或羽状深裂，裂片椭圆形或椭圆状披针形，边缘有不规则的锯齿，上面散生白色腺点，疏生毡毛，下面密生白色毡毛。头状花序钟形，长3～4mm，直径2～2.5mm，几无柄；总苞片4～5层，密被白色绵毛，边缘膜质，外层披针形；雌花长约1mm； 两性花结实，长约2mm，紫褐色。瘦果椭圆形，无毛。花期7～10月。

生药材鉴定:干燥的叶片，多皱缩破碎，有短柄。叶片略呈羽状分裂，裂片边缘有不规则的粗锯齿。上面灰绿色，生有软毛，下面密生灰白色绒毛。质柔软，气清香，味微苦辛。以下面灰白色、绒毛多、香气浓郁者为佳。

Pharmacology

化学成分: 艾含挥发油，成分是水芹烯(Phellandrene)、毕澄茄烯(Cadinene)、侧柏醇(Thujyl　 alcohol)等。野艾的石油醚抽提物中含侧柏酮、豆甾醇、β-谷甾醇、 α-香树脂醇(α -Amyrin)及其乙酸酯、α-及β-蒎烯、羊齿烯醇(Fernenol)。又含多炔化合物去氢母菊酯(Dehy-dromatricaria　ester)和十四碳-8，10，12-三炔-6-烯-3-酮等。野艾所含挥发油的成分以1，8-桉叶素(Cineole)为主，其余为α-及β-蒎烯、侧柏酮等。叶尚含廿四醇、 β-谷甾醇、ι-甲基肌醇(ι-Quebrachitol)和ι-肌醇(ι-Inositol)。根及茎含一种类似菊粉(Inulin)的多糖称蒿淀粉(Artemose)。根含多种多炔化合物，其中有廿-碳-1，11， 13-三烯-15，17，19-三炔，十四碳-8， 10，12-三炔-6-烯-3-酮和十二碳-6，8，10-三炔- 4-烯-3-酮。小枝还含有催产素(Oxytocin)样作用的物质。此外，野艾比其他植物含碘较多，也较易从土壤中吸收钡。野艾变种小野艾Artemisia　vulgaris　L.　Var.　 IndicaMaxim.的挥发油含多量1，8-桉叶素(占50%以上)，其他有α-侧柏酮、倍半萜烯醇及其酯。风干叶含矿物质10.13%，脂肪2.59%，蛋白质25.85%，以及维生素A、B1、B2、 C等。同属植物A.　Feddei　Lev.　Et　Van.的挥发油含艾醇A(Yomogi　alcohol　A)。多种艾属植物中还分出一种倍半萜烯内酯名日登内酯(Ridentin)。全草含挥发油0.2 %-0.33%，油中含侧柏酮(thujone)、侧柏醇(thujyl alcohol,3-thujanol)、杜松烯(cadinene),尚含β-谷甾醇、豆甾醇、α-、β-香树酯、无羁萜、柑橘素、槲皮素与4个桉烷衍生物，其中2个为桉烷内酯化合物(eudesmanolides)。另据报道艾叶油中分得桉油精(cineol)、萜品烯醇-4(terpineol-4)、蒿醇(artemisia　 alcohol)、樟脑、龙脑、芳樟脑(linalool)、β-石竹烯(β-caryophyllene)、α-水芹烯(α-phelandrene)、莰烯(camphene)、α-雪松烯(α-cedrene)、反式香苇醇(trans- carveol)、乙醇龙脑酯、榄香醇(elemol)、异龙脑、α-萜品烯(α-terpineol)及香芹酮(carvone)。挥发油经气质联用分析鉴定了34个成分，其中苧烯含量最高，其次为香叶烯、乙酸龙脑酯、β-蒎烯、龙脑、桧烯等。

Efficacy

In Vitro:

Chen T, et al., Dihydroartemisinin Induces Apoptosis and Sensitizes Human Ovarian Cancer Cells to Carboplatin Therapy. J Cell Mol Med . 2008 May 2.

Badireenath Konkimalla V, et al., Effect of artemisinins and other endoperoxides on nitric oxide-related signaling pathway in RAW 264.7 mouse macrophage cells. Nitric Oxide . 2008 Apr 22.

Li LN, Zhang HD, et al., Differential sensitivity of colorectal cancer cell lines to artesunate is associated with expression of beta-catenin and E-cadherin. Eur J Pharmacol . 2008 Jun 24; 588 ( 1 ): 1-8 . Epub 2008 Apr 3.

Zhang ZY, Yu SQ, et al., [Artesunate combined with vinorelbine plus cisplatin in treatment of advanced non-small cell lung cancer: a randomized controlled trial] Zhong Xi Yi Jie He Xue Bao . 2008 Feb; 6 ( 2 ): 134-8 .

Kelter G, Steinbach D, et al., Role of transferrin receptor and the ABC transporters ABCB6 and ABCB7 for resistance and differentiation of tumor cells towards artesunate. PLoS ONE . 2007 Aug 29; 2 ( 8 ): e798 .

Efferth T, et al., Artesunate induces ROS-mediated apoptosis in doxorubicin-resistant T leukemia cells. PLoS ONE . 2007 Aug 1; 2 ( 1 ): e693 .

Jiao Y, et al., Dihydroartemisinin is an inhibitor of ovarian cancer cell growth. Acta Pharmacol Sin . 2007 Jul; 28 ( 7 ): 1045-56 .

Zhao HJ, et al., Artesunate inhibits angiogenesis and downregulates vascular endothelial growth factor expression in chronic myeloid leukemia K562 cells. Vascul Pharmacol . 2007 Aug-Sep; 47 ( 2-3 ): 131-8 .

Li LN, et al., Artesunate attenuates the growth of human colorectal carcinoma and inhibits hyperactive Wnt/beta-catenin pathway. Int J Cancer . 2007 Sep 15; 121 ( 6 ): 1360-5 .

Efferth T. Willmar Schwabe Award 2006: antiplasmodial and antitumor activity of artemisinin--from bench to bedside. Planta Med . 2007 Apr; 73 ( 4 ): 299-309 . Epub 2007 Mar 12. Review.

Nam W, et al., Effects of artemisinin and its derivatives on growth inhibition and apoptosis of oral cancer cells. Head Neck . 2007 Apr; 29 ( 4 ): 335-40 .

Paik IH, et al., Second generation, orally active, antimalarial, artemisinin-derived trioxane dimers with high stability, efficacy, and anticancer activity. J Med Chem . 2006 May 4; 49 ( 9 ): 2731-4 .

Anfosso L, et al., Microarray expression profiles of angiogenesis-related genes predict tumor cell response to artemisinins. Pharmacogenomics J . 2006 Jul-Aug; 6 ( 4 ): 269-78 . Epub 2006 Jan 24.

Efferth T. Molecular pharmacology and pharmacogenomics of artemisinin and its derivatives in cancer cells. Curr Drug Targets . 2006 Apr; 7 ( 4 ): 407-21 .

Lai H, et al., Oral artemisinin prevents and delays the development of 7,12-dimethylbenz[a]anthracene (DMBA)-induced breast cancer in the rat. Cancer Lett . 2006 Jan 8; 231 ( 1 ): 43-8 .

Disbrow GL, et al., Dihydroartemisinin is cytotoxic to papillomavirus-expressing epithelial cells in vitro and in vivo. Cancer Res . 2005 Dec 1; 65 ( 23 ): 10854-61 .

Singh NP, et al., Synergistic cytotoxicity of artemisinin and sodium butyrate on human cancer cells. Anticancer Res . 2005 Nov-Dec; 25 ( 6B ): 4325-31 .

Lai H, et al., Targeted treatment of cancer with artemisinin and artemisinin-tagged iron-carrying compounds. Expert Opin Ther Targets . 2005 Oct; 9 ( 5 ): 995-1007 . Review.

Efferth T. Mechanistic perspectives for 1,2,4-trioxanes in anti-cancer therapy. Drug Resist Updat . 2005 Feb-Apr; 8 ( 1-2 ): 85-97 . Review.

Efferth T, et al., Glutathione-related enzymes contribute to resistance of tumor cells and low toxicity in normal organs to artesunate. In Vivo . 2005 Jan-Feb; 19 ( 1 ): 225-32 .

Lai H, et al., Effects of artemisinin-tagged holotransferrin on cancer cells. Life Sci . 2005 Jan 28; 76 ( 11 ): 1267-79 . Epub 2004 Nov 23.

Efferth T, et al., Enhancement of cytotoxicity of artemisinins toward cancer cells by ferrous iron. Free Radic Biol Med . 2004 Oct 1; 37 ( 7 ): 998-1009 .

Singh NP, et al., Artemisinin induces apoptosis in human cancer cells. Anticancer Res . 2004 Jul-Aug; 24 ( 4 ): 2277-80 .

Efferth T, et al., Combination treatment of glioblastoma multiforme cell lines with the anti-malarial artesunate and the epidermal growth factor receptor tyrosine kinase inhibitor OSI-774. Biochem Pharmacol . 2004 May 1; 67 ( 9 ): 1689-700 .

Posner GH, et al., Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacy. J Med Chem . 2003 Mar 13; 46 ( 6 ): 1060-5 .

In Vivo:

Badireenath Konkimalla V, et al., Effect of artemisinins and other endoperoxides on nitric oxide-related signaling pathway in RAW 264.7 mouse macrophage cells. Nitric Oxide . 2008 Apr 22.

Lai H, et al., Oral artemisinin prevents and delays the development of 7,12-dimethylbenz[a]anthracene (DMBA)-induced breast cancer in the rat. Cancer Lett . 2006 Jan 8; 231 ( 1 ): 43-8 .

Disbrow GL, et al., Dihydroartemisinin is cytotoxic to papillomavirus-expressing epithelial cells in vitro and in vivo. Cancer Res . 2005 Dec 1; 65 ( 23 ): 10854-61 .

Efferth T et al., Glutathione-related enzymes contribute to resistance of tumor cells and low toxicity in normal organs to artesunate. In Vivo . 2005 Jan-Feb; 19 ( 1 ): 225-32 .

Dell'Eva R, et al., Inhibition of angiogenesis in vivo and growth of Kaposi's sarcoma xenograft tumors by the anti-malarial artesunate. Biochem Pharmacol . 2004 Dec 15; 68 ( 12 ): 2359-66 .

Clinical:

Efferth T, et al., From traditional Chinese medicine to rational cancer therapy. Trends Mol Med . 2007 Aug; 13 ( 8 ): 353-61 . Epub 2007 Jul 17. Review

Paik IH, et al., Second generation, orally active, antimalarial, artemisinin-derived trioxane dimers with high stability, efficacy, and anticancer activity. J Med Chem . 2006 May 4; 49 ( 9 ): 2731-4 .

Berger TG, et al., Artesunate in the treatment of metastatic uveal melanoma--first experiences. Oncol Rep . 2005 Dec; 14 ( 6 ): 1599-603 .

Lai H, et al., Targeted treatment of cancer with artemisinin and artemisinin-tagged iron-carrying compounds. Expert Opin Ther Targets . 2005 Oct; 9 ( 5 ): 995-1007 . Review.

Efferth T. Mechanistic perspectives for 1,2,4-trioxanes in anti-cancer therapy. Drug Resist Updat . 2005 Feb-Apr; 8 ( 1-2 ): 85-97 . Review.

Efferth T, et al., Combination treatment of glioblastoma multiforme cell lines with the anti-malarial artesunate and the epidermal growth factor receptor tyrosine kinase inhibitor OSI-774. Biochem Pharmacol . 2004 May 1; 67 ( 9 ): 1689-700 .

Posner GH, et al., Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacy. J Med Chem . 2003 Mar 13; 46 ( 6 ): 1060-5 .

Wang Q, et al., [Experimental studies of antitumor effect of artesunate on liver cancer] Zhongguo Zhong Yao Za Zhi . 2001 Oct; 26 ( 10 ): 707-8, 720 . Chinese.

Safety

用药忌宜： 阴虚血热者慎用。《纲目》：“苦酒、香附为之使。”《本草备要》：“血热为病者禁用。”《本经逢原》：“阴虚火旺，血燥生热，及宿有失血病者为禁。”