Advances of Pharmacological Action Research of Natural Medicine Artemisinin and Its Derivatives_CHINESE JOURNAL OF BASES AND CLINICS IN GENERAL SURGERY

Authors：

DING Huanxin , LI Jingfeng , CHEN Xuming , LI Li

The Second Department of Hepatobiliaropancreatic Surgery, The Affiliated Ganmei Hospital of Kunming Medical College and The First People’s Hospital of Kunming City, Kunming 650011, China;

Corresponding author：

Keywords：

Artemisinin; Artemisinin derivatives; Pharmacological action; Anti-tumor; Immune mechanism

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Objective To investigate the pharmacological effects and mechanisms of natural medicine artemisinin and its derivatives.
Methods The pertinent domestic and overseas literatures of recent years were reviewed and summarized. Results Artemisinin and its derivatives have unique structure, high efficiency with low toxicity. The pharmacological effects include anti-malaria, anti-tumor, immune function regulation, anti-bacterial, anti-fetation, anti-fibrosis, heat-clearing and detoxicating, etc.
Conclusion Artemisinin and its derivatives play pharmacological effects in different ways, and have a good foreground in the application.

Citation： DING Huanxin,LI Jingfeng,CHEN Xuming,LI Li. Advances of Pharmacological Action Research of Natural Medicine Artemisinin and Its Derivatives. CHINESE JOURNAL OF BASES AND CLINICS IN GENERAL SURGERY, 2010, 17(5): 519-521. doi: Copy

1.	李子颖, 李士雨, 齐向娟. 青蒿素提取技术研究进展 [J]．中药研究与信息, 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.	郑全芳, 杨志刚, 孙红祥. 青蒿素及其衍生物药理作用研究进展 [J]. 中国兽药杂志, 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.	茹炜炜, 梁幼生. 青蒿素类药物抗寄生虫作用研究进展 [J]. 中国血吸虫病防治杂志, 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.	董海鹰, 王知非, 宋维华, 等. 青蒿素诱导K562细胞凋亡研究 [J]. 中国肿瘤, 2003; 12(8)： 473-475.
22.	王勤, 吴理茂, 赵一, 等. 青蒿琥酯抗肿瘤作用的机制研究 [J]. 药学学报, 2002; 37(6)： 477-478.
23.	周晋, 孟然, 李丽敏, 等. 青蒿素对人白血病细胞株和原代细胞的影响 [J]. 中华内科杂志, 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.	徐丽敏, 陈学荣, 屠呦呦. 双氢青蒿素对狼疮性BXSB小鼠的作用 [J]. 中国中西医结合皮肤性病学杂志, 2002; 1(1)：19-20.
30.	蒋江红. 青蒿琥酯的药理研究纂要 [J]. 中医药学刊, 2003; 21(9)： 1502-1503.
31.	徐继红, 章元沛. 二氢青蒿素与青蒿琥酯的抗孕作用 [J]. 药学学报, 1996; 31(9): 657-661.
32.	娄小娥, 周慧君. 青蒿琥酯对大鼠孕酮、雌二醇和蜕膜组织的影响 [J]. 药学学报, 2001; 36(4): 254-257.
33.	曹治东, 石崇荣, 黄崇本. 青蒿素对体外瘢痕成纤维细胞的生物学影响 [J]. 重庆医学, 2003; 32(5): 521-523.
34.	郑红艳. 青蒿素母液体外抗真菌试验 [J]. 四川畜牧兽医, 2001; 28(5): 33-34.
35.	卢岚. 冬虫夏草和青蒿素抑制狼疮性肾炎复发的研究 [J]. 中国中西医结合杂志, 2002; 22(3): 169-171.
36.	刘云海, 杜光. 青蒿素等中药化学成分抗内毒素研究现状 [J]. 医药导报, 2001; 20(8): 525-526.

1. 李子颖, 李士雨, 齐向娟. 青蒿素提取技术研究进展 [J]．中药研究与信息, 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. 郑全芳, 杨志刚, 孙红祥. 青蒿素及其衍生物药理作用研究进展 [J]. 中国兽药杂志, 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. 茹炜炜, 梁幼生. 青蒿素类药物抗寄生虫作用研究进展 [J]. 中国血吸虫病防治杂志, 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. 董海鹰, 王知非, 宋维华, 等. 青蒿素诱导K562细胞凋亡研究 [J]. 中国肿瘤, 2003; 12(8)： 473-475.
22. 王勤, 吴理茂, 赵一, 等. 青蒿琥酯抗肿瘤作用的机制研究 [J]. 药学学报, 2002; 37(6)： 477-478.
23. 周晋, 孟然, 李丽敏, 等. 青蒿素对人白血病细胞株和原代细胞的影响 [J]. 中华内科杂志, 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. 徐丽敏, 陈学荣, 屠呦呦. 双氢青蒿素对狼疮性BXSB小鼠的作用 [J]. 中国中西医结合皮肤性病学杂志, 2002; 1(1)：19-20.
30. 蒋江红. 青蒿琥酯的药理研究纂要 [J]. 中医药学刊, 2003; 21(9)： 1502-1503.
31. 徐继红, 章元沛. 二氢青蒿素与青蒿琥酯的抗孕作用 [J]. 药学学报, 1996; 31(9): 657-661.
32. 娄小娥, 周慧君. 青蒿琥酯对大鼠孕酮、雌二醇和蜕膜组织的影响 [J]. 药学学报, 2001; 36(4): 254-257.
33. 曹治东, 石崇荣, 黄崇本. 青蒿素对体外瘢痕成纤维细胞的生物学影响 [J]. 重庆医学, 2003; 32(5): 521-523.
34. 郑红艳. 青蒿素母液体外抗真菌试验 [J]. 四川畜牧兽医, 2001; 28(5): 33-34.
35. 卢岚. 冬虫夏草和青蒿素抑制狼疮性肾炎复发的研究 [J]. 中国中西医结合杂志, 2002; 22(3): 169-171.
36. 刘云海, 杜光. 青蒿素等中药化学成分抗内毒素研究现状 [J]. 医药导报, 2001; 20(8): 525-526.

CHINESE JOURNAL OF BASES AND CLINICS IN GENERAL SURGERY

Advances of Pharmacological Action Research of Natural Medicine Artemisinin and Its Derivatives

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