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2-氨基壬烷-6-甲氧基四氢萘盐酸盐体外抗氟康唑耐药白念珠菌活性研究 被引量:3

Study on in vitro antifungal activity of 10b against fluconazole-resistant Candida albicans
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摘要 目的:考察2-氨基壬烷-6-甲氧基四氢萘盐酸盐(10b)对氟康唑耐药白念珠菌的体外抗菌活性。方法:采用美国临床和实验室标准协会(CLSI)推荐的微量液基稀释法考察10b对20株氟康唑耐药白念珠菌的抗菌活性。通过琼脂纸片扩散实验、时间生长曲线实验和MFC值测定,比较10b与酮康唑对氟康唑耐药白念珠菌SC5314R的体外抗真菌活性。通过罗丹明6G外排试验初步探讨10b可能的作用机制。结果:10b对氟康唑耐药白念珠菌的抗菌活性强于酮康唑,其作用机制可能与抑制药物流出泵外排功能有关。结论:10b化学结构新颖,对氟康唑耐药白念珠菌体外抗菌活性强大,值得深入探讨和研究。 OBJECTIVE To investigate 2-Amino-nonyl-6-methoxyl-tetralin muriate (10 b) in vitro activity against flucon azole-resistant Candida albicans. METHODS The antifungal activities of 10 b against 20 fluconazole-resistant Candida albi- cans strains were assayed by microbroth dilution in 96-well plates according to methods of the Clinical and Laboratory Standards Institute (CLSI). The sensitivity to fluconazole-resistant Candida albicans strain SC5314R of 10 b with ketoconazole was corn pared by plotting the time-growth curves and determining the values of MFC. In addition, the potential mechanism of 10 b a- gainst flueonazole-resistant Candida albicans strains was investigated by Rhodamine 6G efflusion test. RESULTS 10b had a stronger antifungal activity to fluconazole-resistant Candida albicans strains than ketoconazole did. Its potential mechanism maybe related to the inhibition of the function of muhidrug efflux pump. CONCLUSION 10b possessed a novel chemical struc ture and powerful antifungal activity against fluconazole-resistant Candida albicans strains which deserve further investigating.
出处 《中国医院药学杂志》 CAS CSCD 北大核心 2014年第9期720-724,共5页 Chinese Journal of Hospital Pharmacy
关键词 2-氨基壬烷-6-甲氧基四氢萘盐酸盐 氟康唑耐药白念珠菌 抗真菌活性 体外 10b fluconazole-resistant Candida albicans antifungal activities in vitro
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参考文献13

  • 1Sheng CQ, Zhu J, Zhang WN, et al. 3D-QSAR and molecular docking studies on benzothiazole derivative as Candida albicans N-myristoyltransferase inhibitors[J]. EurJ Med Chem,2007, 42 : 477-486.
  • 2Sheng CQ, Zhang WN, Ji HT,et al. Structure based optimi-zation of azole antifungal agents by CoMFA, CoMSIA, and molecular docking[J]. J Med Chem 2006, 49: 2512-2525.
  • 3Ji H, Zhang WN, Zhang M, et al. Structure based de novo design, synthesis, and biological evaluation of nomazole inhib- itors specific for lanosterol 14r-demethylase of fungi[J]. J Med Chem,2003, 46: 474-485.
  • 4ZhuJ, Lu JG, Zhou YJ, etal. Design, synthesis, and anti fungal activities in vitro of novel tetrahydroisoquinoline com- pounds based on the structure of lanosterol 14a-demethylase (CYP51) of fungi[J]. Bioorg Med Chem Let, 2006, 16 (20) : 5285-5289.
  • 5梁蓉梅,曹永兵,周有骏,汪涛,卢嘉,姚斌,姜远英.20种四氢萘类抗真菌化合物体外抑菌活性测定[J].第二军医大学学报,2007,28(3):286-293. 被引量:2
  • 6Yao B, Ji HT, Cao YB, et al. Synthesis and antifungal activi ties of novel 2-aminotetralin derivatives [J]. J Med Chem, 2007, 50: 5293-5300.
  • 7Clinical and Laboratory Standards Institute (CLSI). Reference method for broth dilution antifungal susceptibility testing of yeasts. Approved standard M27 A2. Wayne, Pa; 2002.
  • 8Benjamin JP, Beth AS, Rana AH, et al. Evaluation of am photericin B interpretive break points for Candida bloodstream isolates by correlation with therapeutic outcome[J]. Antimi- crob Agents Chemother,2(106, 50(4) : 1287-1292.
  • 9Hope WW, Tabernero L, Denning DW, et al. Molecular mechanisms of primary resistance to flucytosine in Cand da al bicans [J]. Antimicr Agents Chemother, 2004,48 : 4377-4386.
  • 10Yeaman MR, Yount NY. Mechanisms of antimicrobial pep- tideaction and resistance [J]. Pharmacol Rev, 2003,55: 27- 55.

二级参考文献7

  • 1Monk B C,Niimi K,Lin S,et al.Surface-active fungicidal Dpeptide inhibitors of the plasma membrane proton pump that block azole resistance[J].Antimicrob Agents Chemother,2005,49:57-70.
  • 2Mukhopadhyay K,Prasad T,Saini P,et al.Membrane sphingolipid-ergosterol interactions are important determinants of multidrug resistance in Candida albicans[J].Antimicrob Agents Chemother,2004,48:1778-1787.
  • 3MacPherson S,Akache B,Weber S,et al.Candida albicans zinc cluster protein Upc2 confers resistance to antifungal drugs and is an activator of ergosterol biosynthetic genes[J].Antimicrob Agents Chemother,2005,49:1745-1752.
  • 4Lambrechts S,Aalders M,Van Marle J.Mechanistic study of the photodynamic inactivation of Candida albicans by a cationic porphyrin[J].Antimicrob Agents Chemother,2005,49:2026-2034.
  • 5Fukuoka T,Johnston DA,Winslow CA,et al.Genetic basis for differential activities of fluconazole and voriconazole against Candida krusei[J].Antimicrob Agents Chemother,2003,47:1213-1219.
  • 6Perea S,Gonzalez G,Annette W,et al.In vitro activities of terbinafine in combination with fluconazole,itraconazole,voriconazole,and posaconazole against clinical isolates of Candida glabrata with decreased susceptibility to azole[J].J Clin Microbiol,2002,40:1831-1833.
  • 7唐珊熙,刘锡光.人微生物学及微生物学检验[M].北京:人民卫生出版社,2001:464-476.

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同被引文献41

  • 1饶小平,宋湛谦,高宏.含氟脱氢枞胺Schiff碱的合成及抑菌活性[J].林产化学与工业,2007,27(2):97-99. 被引量:15
  • 2Vandeputte P, Ferrari S, Coste AT. Antifungal resistance and new strategies to control fungal infections [ J ]. Int J Microbiol, 2012 : 1-26.
  • 3Khodavandi A, Alizadeh F, Vandan VA, et al. Possible mechanisms of the antifungal activity of fluconazole in combination with terbinafine against Candida albicans [ J]. Pharm Biol,2014,52(12) :1505-1509.
  • 4Chen LM, Xu YH, Zhou CL, et al. Overexpression of CDR1 and CDR2 genes plays an important role in flucon- azole resistance in Candida albicans with G487T and T916C mutations[J]. J Int Med Res,2010,38(2):536- 545.
  • 5Cannon RD, Lamping E, Holmes AR,et al. Efflux-medi- ated antifungal drug resistance [ J]. Clin Microbiol Rev, 2009,22 ( 2 ) : 291-321.
  • 6Holmes AR, Keniya MV, Ivnitski-Steele I, et al. The monoamine oxidase A inhibitor clorgyline is a broad-spec- trum inhibitor of fungal ABC and MFS transporter efflux pump activities which reverses the azole resistance of Can- dida albicans and Candida glabrata clinical isolates [ J l- Antimicrob Agents Chemother ,2012,56 ( 3 ) : 1508-1515.
  • 7Sehuetzer-Muehlbauer M, Willinger B, Egner R, et al. Reversal of antifungal resistance mediated by ABC efflux pumps from Candida albicans functionally expressed in yeast[ J ]. Int J Antimicrob Agents, 2003,22 ( 3 ) : 291- 300.
  • 8Guillon R, Pagniez F, Giraud F, et al. Design, synthe- sis, and in vitro antifungal activity of 1-[ (4-substituted- benzyl ) methylamino 1-2-( 2,4-difluorophenyl ) -3-( 1 H-l, 2,4-triazol -1-yl) propan-2-ols [ J ]. Chem Med Chem, 2011,6(5) :816-825.
  • 9Maurya IK, Thota CK, Verma SD, et al. Rationally de- signed transmembrane peptide mimics of the muhidrug transporter protein Cdrl act as antagonists to selectively block drug efflux and chemosensitize azole-resistant clini- cal isolates of Candida albicans [ J 1. J Biol Chem,2013, 288 (23) : 16775-16787.
  • 10Calabrese EC, Castellano S, Santoriello M, et al. Anti-fungal activity of azole compounds CPA18 and CPA109 a- gainst azole-susceptible and-resistant strains of Candida albicans [ J ]. J Antimicrob Chemother, 2013,68 ( 5 ) : 1111-1119.

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