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拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展

蒋琰 盛春泉 董国强

蒋琰, 盛春泉, 董国强. 拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004
引用本文: 蒋琰, 盛春泉, 董国强. 拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004
JIANG Yan, SHENG Chunquan, DONG Guoqiang. Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004
Citation: JIANG Yan, SHENG Chunquan, DONG Guoqiang. Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004

拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.004

Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors

  • 摘要: 拓扑异构酶(topoisomerases,Tops)是参与调节细胞内DNA复制、转录、重组和修复等过程的必需酶。Tops分为TopⅠ和TopⅡ,两者通过DNA切断和连接,维持DNA正常拓扑结构和代谢过程。由于Tops在DNA代谢过程的重要作用,干扰Tops的催化活性或者诱导产生Tops介导的DNA损伤已经成为抗肿瘤治疗的重要策略。Tops已经成为最重要的抗肿瘤靶点之一。综述近年来Tops双重抑制剂的研究进展。
  • [1] Wall ME, Wani MC, Cook CE, et al. Plant antitumor agents Ⅰ. The isolation and structure of camptothecin, a noveⅠ alkaloidal leukemia and tumor inhibitor from camptotheca acuminata1,2[J]. J Am Chem Soc, 1966, 88(16): 3888-3890.
    [2] Hsiang YH, Hertzberg R, Hecht S, et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase Ⅰ[J]. J Biol Chem, 1985, 260(27): 14873-14878.
    [3] Dallavalle S, Gattinoni S, Mazzini S, et al. Synthesis and cytotoxic activity of a new series of topoisomerase Ⅰ inhibitors[J]. Bioorg Med Chem Lett, 2008, 18(4): 1484-1489.
    [4] Kruczynski A, Barret JM, Van Hille B, et al. Decreased nucleotide excision repair activity and alterations of topoisomerase Ⅱ alpha are associated with the in vivo resistance of a P388 leukemia subline to F11782, a novel catalytic inhibitor of topoisomerases Ⅰ and Ⅱ[J]. Clin Cancer Res, 2004, 10(9): 3156(3168.
    [5] Kluza J, Mazinghien R, Irwin H, et al. Relationships between DNA strand breakage and apoptotic progression upon treatment of HL(60 leukemia cells with tafluposide or etoposide[J]. Anticancer Drugs, 2006, 17(2): 155(164.
    [6] Mucci(LoRusso P, Polin L, Bissery MC, et al. Activity of batracylin (NSC-320846) against solid tumors of mice[J]. Invest New Drugs, 1989, 7(4): 295-306.
    [7] Plowman J, Paull KD, Atassi G, et al. Preclinical antitumor activity of batracylin (NSC 320846)[J]. Invest New Drugs, 1988, 6(3): 147-153.
    [8] Rao VA, Agama K, Holbeck S, et al. Batracylin (NSC 320846), a dual inhibitor of DNA topoisomerases Ⅰ and Ⅱ induces histone gamma-H2AX as a biomarker of DNA damage[J]. Cancer Res, 2007, 67(20): 9971-9979.
    [9] Lewis LJ, Mistry P,Charlton PA,et al. Mode of action of the novel phenazine anticancer agents XR11576 and XR5944. Anticancer Drugs 2007, 18, 139-48.
    [10] de Jonge MJ, Kaye S, Verweij J, et al. Phase I and pharmacokinetic study of XR11576, an oral topoisomerase Ⅰ and Ⅱ inhibitor, administered on days 1-5 of a 3-weekly cycle in patients with advanced solid tumours[J]. Br J Cancer, 2004, 91(8): 1459-1465.
    [11] Verborg W, Thomas H, Bissett D, et al. First-into-man phase Ⅰ and pharmacokinetic study of XR5944.14, a novel agent with a unique mechanism of action[J]. Br J Cancer, 2007, 97(7): 844-850.
    [12] Montaner B, Castillo-Avila W, Martinell M, et al. DNA interaction and dual topoisomerase Ⅰ and Ⅱ inhibition properties of the anti-tumor drug prodigiosin[J]. Toxicol Sci, 2005, 85(2): 870-879.
    [13] Montaner B, Navarro S, Pique M, et al. Prodigiosin from the supernatant of Serratia marcescens induces apoptosis in haematopoietic cancer cell lines[J]. Br J Pharmacol, 2000, 131(3): 585-593.
    [14] Montaner B, Perez-Tomas R. Prodigiosin-induced apoptosis in human colon cancer cells[J]. Life Sci, 2001, 68(17): 2025-2036.
    [15] Lin JK. Molecular targets of curcumin[J]. Adv Exp Med Biol, 2007, 595: 227-243.
    [16] Lopez-Lazaro M, Willmore E, Jobson A, et al. Curcumin induces high levels of topoisomerase Ⅰ-and Ⅱ-DNA complexes in K562 leukemia cells[J]. J Nat Prod, 2007, 70(12): 1884-1888.
    [17] Dhandapani KM, Mahesh VB,Brann DW. Curcumin suppresses growth and chemoresistance of human glioblastoma cells via AP-Ⅰ and NF kappaB transcription factors[J]. J Neurochem, 2007, 102(2): 522-538.
    [18] Chih LL,Jen KL. Curcumin: a potential cancer chemopreventive agent through suppressing NF-κB signaling[J]. J Cancer Mol, 2008, 4(1): 11-16.
    [19] Choi JY, Seo CS, Zheng MS, et al. Topoisomerase Ⅰ and Ⅱ inhibitory constituents from the bark of Tilia amurensis[J]. Arch Pharm Res, 2008, 31(11): 1413-1418.
    [20] Ishiyama D, Kanai Y, Senda H, et al. Novel human topoisomerase Ⅰ inhibitors, topopyrones A, B, C and D. Ⅱ. Structure elucidation[J]. J Antibiot (Tokyo), 2000, 53(9): 873-878.
    [21] Kanai Y,Ishiyama D,Senda H,et al. Novel human topoisomerase Ⅰ inhibitors, topopyrones A, B, C and D. Ⅰ. Producing strain, fermentation, isolation, physico-chemical properties and biological activity. J Antibiot (Tokyo) 2000, 53, 863-72.
    [22] Khan QA, Elban MA; Hecht SM. The topopyrones poison human DNA topoisomerases Ⅰ and Ⅱ[J]. J Am Chem Soc, 2008, 130(39): 12888-12889.
    [23] Hecht SM, Khan QA, Maini R, et al. Topopyrones: Dual topoisomerase inhibitors. Patent PCT/US2009/050081, 2010.
    [24] López-Lázaro M, Willmore E,Austin CA. The dietary flavonoids myricetin and fisetin act as dual inhibitors of DNA topoisomerases Ⅰ and Ⅱ in cells[J]. Mutat Res, 2010, 696:41-47.
    [25] Demarquay D, Huchet M, Coulomb H, et al. BN80927: A novel homocamptothecin that inhibits proliferation of human tumor cells in vitro and in vivo[J]. Cancer Res, 2004, 64:4942-4949.
    [26] Lavergne O, Demarquay D, Bailly C, et al. Topoisomerase Ⅰ-mediated antiproliferative activity of enantiomerically pure fluorinated homocamptothecins[J]. J Med Chem, 2000, 43(11): 2285-2289.
    [27] Taniguchi K, Kohno K, Kawanami K, et al. Drug-induced down-regulation of topoisomerase Ⅰ in human epidermoid cancer cells resistant to saintopin and camptothecins[J]. Cancer Res, 1996, 56(10): 2348-2354.
    [28] Basnet A, Thapa P, Karki R, et al. 2,4,6-Trisubstituted pyridines: synthesis, topoisomerase Ⅰ and Ⅱ inhibitory activity, cytotoxicity, and structure-activity relationship[J]. Bioorg Med Chem, 2007, 15(13): 4351-4359.
    [29] Dalla Via L, Magno SM, Gia O, et al. Benzothiopyranoindole-based antiproliferative agents: synthesis, cytotoxicity, nucleic acids interaction, and topoisomerases inhibition properties[J]. J Med Chem, 2009, 52(17): 5429-5441.
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  • 收稿日期:  2013-10-15
  • 修回日期:  2014-02-19

拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.004

摘要: 拓扑异构酶(topoisomerases,Tops)是参与调节细胞内DNA复制、转录、重组和修复等过程的必需酶。Tops分为TopⅠ和TopⅡ,两者通过DNA切断和连接,维持DNA正常拓扑结构和代谢过程。由于Tops在DNA代谢过程的重要作用,干扰Tops的催化活性或者诱导产生Tops介导的DNA损伤已经成为抗肿瘤治疗的重要策略。Tops已经成为最重要的抗肿瘤靶点之一。综述近年来Tops双重抑制剂的研究进展。

English Abstract

蒋琰, 盛春泉, 董国强. 拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004
引用本文: 蒋琰, 盛春泉, 董国强. 拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004
JIANG Yan, SHENG Chunquan, DONG Guoqiang. Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004
Citation: JIANG Yan, SHENG Chunquan, DONG Guoqiang. Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004
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