• 昆明市第一人民醫(yī)院暨昆明醫(yī)學院附屬甘美醫(yī)院肝膽胰腺外二科（昆明 650011）;

目的 探討天然藥物青蒿素及其衍生物的藥理作用及機理。
方法 復習近年來國內、外相關文獻并進行綜述。
結果 青蒿素及其衍生物結構獨特、高效低毒，除具有抗瘧疾作用外，亦被證明具有抗腫瘤、調節(jié)免疫功能、抗菌、抗孕、抗纖維化、清熱解毒等藥理作用。
結論 青蒿素及其衍生物通過不同的途徑發(fā)揮藥理作用，具有較好的應用前景。

引用本文： 丁煥新,李鏡鋒,陳旭明,李立. 天然藥物青蒿素及其衍生物的作用機理研究進展. 中國普外基礎與臨床雜志, 2010, 17(5): 519-521. doi: 復制

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1. 李子穎, 李士雨, 齊向娟. 青蒿素提取技術研究進展 [J]． 中藥研究與信息, 2002; 4(2): 17-21.
2. Lee S. Artemisinin, promising lead natural product for various drug developments [J]. Mini Rev Med Chem, 2007; 7(4): 411-422.
3. Dhingra V, Vishweshwar Rao K, Lakshmi Narasu M. Current status of artemisinin and its derivatives as antimalarial drugs [J]. Life Sci, 2000; 66(4): 279-300.
4. 鄭全芳, 楊志剛, 孫紅祥. 青蒿素及其衍生物藥理作用研究進展 [J]. 中國獸藥雜志, 2006; 40(1)： 40-44.
5. Efferth T. Molecular pharmacology and pharmacogenomics of artemisinin and its derivatives in cancer cells [J]. Curr Drug Targets, 2006; 7(4): 407-421.
6. 茹煒煒, 梁幼生. 青蒿素類藥物抗寄生蟲作用研究進展 [J]. 中國血吸蟲病防治雜志, 2006; 18(1)： 78-80.
7. Lai H, Singh NP. Oral artemisinin prevents and delays the development of 7,12-dimethylbenz[a]anthracene (DMBA)-induced breast cancer in the rat [J]. Cancer Lett, 2006; 231(1): 43-48.
8. Anfosso L, Efferth T, Albini A, et al. Microarray expression profiles of angiogenesis-related genes predict tumor cell response to artemisinins [J]. Pharmacogenomics J, 2006; 6(4): 269-278.
9. Fujita T, Felix K, Pinkaew D, et al. Human fortilin is a molecular target of dihydroartemisinin [J].　FEBS Lett, 2008; 582(7): 1055-1060.
10. Berger TG, Dieckmann D, Efferth T, et al. Artesunate in the treatment of metastatic uveal melanoma-irst experiences [J]. Oncol Rep, 2005; 14(6): 1599-1603.
11. Yamachika E, Habte T, Oda D. Artemisinin: an alternative treatment for oral squamous cell carcinoma [J]. Anticancer Res, 2004; 24(4): 2153-2160.
12. Huang XJ, Ma ZQ, Zhang WP, et al. Dihydroartemisinin exerts cytotoxic effects and inhibits hypoxia inducible factor-1alpha activation in C6 glioma cells [J]. J Pharm Pharmacol, 2007; 59(6): 849-856.
13. Mu D, Chen W, Yu B, et al. Calcium and survivin are involved in the induction of apoptosis by dihydroartemisinin in human lung cancer SPC-A-1 cells [J]. Methods Find Exp Clin Pharmacol, 2007; 29(1): 33-38.
14. Mu D, Zhang W, Chu D, et al. The role of calcium, P38 MAPK in dihydroartemisinin-induced apoptosis of lung cancer PC-14 cells [J]. Cancer Chemother Pharmacol, 2008; 61(4): 639-645.
15. Li LN, Zhang HD, Yuan SJ, et al. Artesunate attenuates the growth of human colorectal carcinoma and inhibits hyperactive Wnt/beta-catenin pathway [J]. Int J Cancer, 2007; 121(6): 1360-1365.
16. Lee J, Zhou HJ, Wu XH. Dihydroartemisinin downregulates vascular endothelial growth factor expression and induces apoptosis in chronic myeloid leukemia K562 cells [J]. Cancer Chemother Pharmacol, 2006; 57(2): 213-220.
17. Hou J, Wang D, Zhang R, et al. Experimental therapy of hepatoma with artemisinin and its derivatives: in vitro and in vivo activity, chemosensitization, and mechanisms of action [J]. Clin Cancer Res, 2008; 14(17): 5519-5530.
18. Zhou HJ, Wang Z, Li A. Dihydroartemisinin induces apoptosis in human leukemia cells HL60 via downregulation of transferrin receptor expression [J]. Anticancer Drugs, 2008; 19(3): 247-255.
19. Nakase I, Lai H, Singh NP, et al. Anticancer properties of artemisinin derivatives and their targeted delivery by transferrin conjugation [J]. Int J Pharm, 2008; 354(1-2): 28-33.
20. Li LN, Zhang HD, Yuan SJ, et al. Differential sensitivity of colorectal cancer cell lines to artesunate is associated with expression of beta-catenin and E-cadherin [J]. Eur J Pharmacol, 2008; 588(1): 1-8.
21. 董海鷹, 王知非, 宋維華, 等. 青蒿素誘導K562細胞凋亡研究 [J]. 中國腫瘤, 2003; 12(8)： 473-475.
22. 王勤, 吳理茂, 趙一, 等. 青蒿琥酯抗腫瘤作用的機制研究 [J]. 藥學學報, 2002; 37(6)： 477-478.
23. 周晉, 孟然, 李麗敏, 等. 青蒿素對人白血病細胞株和原代細胞的影響 [J]. 中華內科雜志, 2003; 42(10)： 713-714.
24. Chen HH, Zhou HJ, Wu GD, et al. Inhibitory effects of artesunate on angiogenesis and on expressions of vascular endothelial growth factor and VEGF receptor KDR/flk-1 [J]. Pharmacology, 2004; 71(1): 1-9.
25. Efferth T. Willmar Schwabe Award 2006: antiplasmodial and antitumor activity of artemisinin-from bench to bedside [J]. Planta Med, 2007; 73(4): 299-309.
26. Yang ZS, Zhou WL, Sui Y, et al. Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(beta or alpha)-Dihydroartemisininoxy] phen(ox)yl aliphatic acids and esters [J]. J Med Chem, 2005; 48(14): 4608-4617.
27. Yang ZS, Wang JX, Zhou Y, et al. Synthesis and immunosuppressive activity of new artemisinin derivatives. Part 2: 2-[12(beta or alpha)-dihydroartemisinoxymethyl(or 1′-ethyl)] phenoxyl propionic acids and esters [J]. Bioorg Med Chem, 2006; 14(23): 8043-8049.
28. Zhou WL, Wu JM, Wu QL, et al. A novel artemisinin derivative, 3-(12-beta-artemisininoxy) phenoxyl succinic acid (SM735), mediates immunosuppressive effects in vitro and in vivo [J]. Acta Pharmacol Sin, 2005; 26(11): 1352-1358.
29. 徐麗敏, 陳學榮, 屠呦呦. 雙氫青蒿素對狼瘡性BXSB小鼠的作用 [J]. 中國中西醫(yī)結合皮膚性病學雜志, 2002; 1(1)：19-20.
30. 蔣江紅. 青蒿琥酯的藥理研究纂要 [J]. 中醫(yī)藥學刊, 2003; 21(9)： 1502-1503.
31. 徐繼紅, 章元沛. 二氫青蒿素與青蒿琥酯的抗孕作用 [J]. 藥學學報, 1996; 31(9): 657-661.
32. 婁小娥, 周慧君. 青蒿琥酯對大鼠孕酮、雌二醇和蛻膜組織的影響 [J]. 藥學學報, 2001; 36(4): 254-257.
33. 曹治東, 石崇榮, 黃崇本. 青蒿素對體外瘢痕成纖維細胞的生物學影響 [J]. 重慶醫(yī)學, 2003; 32(5): 521-523.
34. 鄭紅艷. 青蒿素母液體外抗真菌試驗 [J]. 四川畜牧獸醫(yī), 2001; 28(5): 33-34.
35. 盧嵐. 冬蟲夏草和青蒿素抑制狼瘡性腎炎復發(fā)的研究 [J]. 中國中西醫(yī)結合雜志, 2002; 22(3): 169-171.
36. 劉云海, 杜光. 青蒿素等中藥化學成分抗內毒素研究現(xiàn)狀 [J]. 醫(yī)藥導報, 2001; 20(8): 525-526.
  1. 1. 李子穎, 李士雨, 齊向娟. 青蒿素提取技術研究進展 [J]． 中藥研究與信息, 2002; 4(2): 17-21.
  2. 2. Lee S. Artemisinin, promising lead natural product for various drug developments [J]. Mini Rev Med Chem, 2007; 7(4): 411-422.
  3. 3. Dhingra V, Vishweshwar Rao K, Lakshmi Narasu M. Current status of artemisinin and its derivatives as antimalarial drugs [J]. Life Sci, 2000; 66(4): 279-300.
  4. 4. 鄭全芳, 楊志剛, 孫紅祥. 青蒿素及其衍生物藥理作用研究進展 [J]. 中國獸藥雜志, 2006; 40(1)： 40-44.
  5. 5. Efferth T. Molecular pharmacology and pharmacogenomics of artemisinin and its derivatives in cancer cells [J]. Curr Drug Targets, 2006; 7(4): 407-421.
  6. 6. 茹煒煒, 梁幼生. 青蒿素類藥物抗寄生蟲作用研究進展 [J]. 中國血吸蟲病防治雜志, 2006; 18(1)： 78-80.
  7. 7. Lai H, Singh NP. Oral artemisinin prevents and delays the development of 7,12-dimethylbenz[a]anthracene (DMBA)-induced breast cancer in the rat [J]. Cancer Lett, 2006; 231(1): 43-48.
  8. 8. Anfosso L, Efferth T, Albini A, et al. Microarray expression profiles of angiogenesis-related genes predict tumor cell response to artemisinins [J]. Pharmacogenomics J, 2006; 6(4): 269-278.
  9. 9. Fujita T, Felix K, Pinkaew D, et al. Human fortilin is a molecular target of dihydroartemisinin [J].　FEBS Lett, 2008; 582(7): 1055-1060.
  10. 10. Berger TG, Dieckmann D, Efferth T, et al. Artesunate in the treatment of metastatic uveal melanoma-irst experiences [J]. Oncol Rep, 2005; 14(6): 1599-1603.
  11. 11. Yamachika E, Habte T, Oda D. Artemisinin: an alternative treatment for oral squamous cell carcinoma [J]. Anticancer Res, 2004; 24(4): 2153-2160.
  12. 12. Huang XJ, Ma ZQ, Zhang WP, et al. Dihydroartemisinin exerts cytotoxic effects and inhibits hypoxia inducible factor-1alpha activation in C6 glioma cells [J]. J Pharm Pharmacol, 2007; 59(6): 849-856.
  13. 13. Mu D, Chen W, Yu B, et al. Calcium and survivin are involved in the induction of apoptosis by dihydroartemisinin in human lung cancer SPC-A-1 cells [J]. Methods Find Exp Clin Pharmacol, 2007; 29(1): 33-38.
  14. 14. Mu D, Zhang W, Chu D, et al. The role of calcium, P38 MAPK in dihydroartemisinin-induced apoptosis of lung cancer PC-14 cells [J]. Cancer Chemother Pharmacol, 2008; 61(4): 639-645.
  15. 15. Li LN, Zhang HD, Yuan SJ, et al. Artesunate attenuates the growth of human colorectal carcinoma and inhibits hyperactive Wnt/beta-catenin pathway [J]. Int J Cancer, 2007; 121(6): 1360-1365.
  16. 16. Lee J, Zhou HJ, Wu XH. Dihydroartemisinin downregulates vascular endothelial growth factor expression and induces apoptosis in chronic myeloid leukemia K562 cells [J]. Cancer Chemother Pharmacol, 2006; 57(2): 213-220.
  17. 17. Hou J, Wang D, Zhang R, et al. Experimental therapy of hepatoma with artemisinin and its derivatives: in vitro and in vivo activity, chemosensitization, and mechanisms of action [J]. Clin Cancer Res, 2008; 14(17): 5519-5530.
  18. 18. Zhou HJ, Wang Z, Li A. Dihydroartemisinin induces apoptosis in human leukemia cells HL60 via downregulation of transferrin receptor expression [J]. Anticancer Drugs, 2008; 19(3): 247-255.
  19. 19. Nakase I, Lai H, Singh NP, et al. Anticancer properties of artemisinin derivatives and their targeted delivery by transferrin conjugation [J]. Int J Pharm, 2008; 354(1-2): 28-33.
  20. 20. Li LN, Zhang HD, Yuan SJ, et al. Differential sensitivity of colorectal cancer cell lines to artesunate is associated with expression of beta-catenin and E-cadherin [J]. Eur J Pharmacol, 2008; 588(1): 1-8.
  21. 21. 董海鷹, 王知非, 宋維華, 等. 青蒿素誘導K562細胞凋亡研究 [J]. 中國腫瘤, 2003; 12(8)： 473-475.
  22. 22. 王勤, 吳理茂, 趙一, 等. 青蒿琥酯抗腫瘤作用的機制研究 [J]. 藥學學報, 2002; 37(6)： 477-478.
  23. 23. 周晉, 孟然, 李麗敏, 等. 青蒿素對人白血病細胞株和原代細胞的影響 [J]. 中華內科雜志, 2003; 42(10)： 713-714.
  24. 24. Chen HH, Zhou HJ, Wu GD, et al. Inhibitory effects of artesunate on angiogenesis and on expressions of vascular endothelial growth factor and VEGF receptor KDR/flk-1 [J]. Pharmacology, 2004; 71(1): 1-9.
  25. 25. Efferth T. Willmar Schwabe Award 2006: antiplasmodial and antitumor activity of artemisinin-from bench to bedside [J]. Planta Med, 2007; 73(4): 299-309.
  26. 26. Yang ZS, Zhou WL, Sui Y, et al. Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(beta or alpha)-Dihydroartemisininoxy] phen(ox)yl aliphatic acids and esters [J]. J Med Chem, 2005; 48(14): 4608-4617.
  27. 27. Yang ZS, Wang JX, Zhou Y, et al. Synthesis and immunosuppressive activity of new artemisinin derivatives. Part 2: 2-[12(beta or alpha)-dihydroartemisinoxymethyl(or 1′-ethyl)] phenoxyl propionic acids and esters [J]. Bioorg Med Chem, 2006; 14(23): 8043-8049.
  28. 28. Zhou WL, Wu JM, Wu QL, et al. A novel artemisinin derivative, 3-(12-beta-artemisininoxy) phenoxyl succinic acid (SM735), mediates immunosuppressive effects in vitro and in vivo [J]. Acta Pharmacol Sin, 2005; 26(11): 1352-1358.
  29. 29. 徐麗敏, 陳學榮, 屠呦呦. 雙氫青蒿素對狼瘡性BXSB小鼠的作用 [J]. 中國中西醫(yī)結合皮膚性病學雜志, 2002; 1(1)：19-20.
  30. 30. 蔣江紅. 青蒿琥酯的藥理研究纂要 [J]. 中醫(yī)藥學刊, 2003; 21(9)： 1502-1503.
  31. 31. 徐繼紅, 章元沛. 二氫青蒿素與青蒿琥酯的抗孕作用 [J]. 藥學學報, 1996; 31(9): 657-661.
  32. 32. 婁小娥, 周慧君. 青蒿琥酯對大鼠孕酮、雌二醇和蛻膜組織的影響 [J]. 藥學學報, 2001; 36(4): 254-257.
  33. 33. 曹治東, 石崇榮, 黃崇本. 青蒿素對體外瘢痕成纖維細胞的生物學影響 [J]. 重慶醫(yī)學, 2003; 32(5): 521-523.
  34. 34. 鄭紅艷. 青蒿素母液體外抗真菌試驗 [J]. 四川畜牧獸醫(yī), 2001; 28(5): 33-34.
  35. 35. 盧嵐. 冬蟲夏草和青蒿素抑制狼瘡性腎炎復發(fā)的研究 [J]. 中國中西醫(yī)結合雜志, 2002; 22(3): 169-171.
  36. 36. 劉云海, 杜光. 青蒿素等中藥化學成分抗內毒素研究現(xiàn)狀 [J]. 醫(yī)藥導報, 2001; 20(8): 525-526.