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Synthesis of New Artemisinin Derivatives and Preliminary Evaluation of Their Antitumor Activities

Author: MengLiLi
Tutor: KuangYongQing
School: Hunan University
Course: Medicinal Chemistry
Keywords: Artemisinin derivatives Docosahexaenoic acid Solanesol Isosorbide mononitrate Aspirin Ibuprofen Antitumor Polyethylene glycol monomethyl ether - polylactic acid Micelle
CLC: R730.5
Type: Master's thesis
Year: 2009
Downloads: 309
Quote: 0
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Abstract


Efficient antimalarial artemisinin and its derivatives, is one of the most effective drugs for the treatment of malaria. Recent studies show that a variety of biological activity of artemisinin and its derivatives have anti-tumor, anti-parasitic disease and immunosuppression. Especially in the anti-tumor, has a broad spectrum of anti-tumor drug side effects, can reverse multidrug resistance and cross-resistance phenomenon does not exist with traditional chemotherapy drugs, has become a hot research field of anticancer drugs. Antitumor mechanism, mainly because the tumor cells Fe 2 ion content is higher than normal cells, and the Fe 2 ion catalytic artemisinin peroxide bridge fracture generating free radicals, and thus damage the cells of the biological macromolecules. This paper carried out the work in three areas: 1. With NaBH 4 (the KBH 4 ) reduction of artemisinin to dihydroartemisinin, polyunsaturated fatty acids on tumor cells special targeting select docosahexaenoic acid ester as targeting drug carrier the DCC method dihydroartemisinin with 22 carbon acid into the sixth. The same prepared the oleic the dihydroartemisinin ester, for control. MTT assay investigated conjugates of human Burkitt lymphoma cell lines CA46, human T-lymphoblastic leukemia the cells the strains Molt4 and mouse lymphoma cells in vitro P388 inhibition of proliferation activity, results showed the dihydroartemisinin ester of docosahexaenoic acid activity superior to artemisinin and Dihydroartemisinin. Succinic anhydride as acylating agent the acylation Dihydroartemisinin get artesunate drugs put together the principle design, synthesis pieced together from a variety of new artemisinin-based drugs. Solanesol NO donor anti-tumor activity, taking into account the DCC method solanesol 5 - the isosorbide hydroxy and artesunate side chain carboxyl to ester; view of some tumor cells in the inner ring oxygenation enzyme 2 expression levels higher than normal cells, non-steroidal anti-inflammatory drugs inhibit the cyclooxygenase activity, aspirin and ibuprofen dihydroartemisinin into ester with DCC method and acid chloride method to give with multiple anti-tumor mechanisms the new artemisinin Flatten drugs. MTT assay expedition put together material on human Burkitt lymphoma cell line CA46 human T lymphocyte leukemia the cell lines Molt4 and mouse lymphoma cells P388 in vitro growth inhibitory activity, results showed that in addition to ibuprofen of dihydroartemisinin ester of outside, the rest of the inhibitory effect than the control group. 3 Synthesis of polyethylene glycol monomethyl ether - the amphoteric block copolymer of polylactic acid and copolymer blank micelles prepared by dialysis method, artemether the micelles and artemisinin copolymer micelles investigated raw material feeding ratio and dialysis conditions and other factors, the initial micelle core - shell structure and rod-shaped structure, provide clues for the development of the Artemisia annua drugs new formulations.

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