【病毒外文文獻】2005 A7_3 Inhibition of SARS coronavirus 3C-like protease by Isatis indigotica root and plant-derived phenolic compounds

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Free Papers International Journal of Antimicrobial Agents 26S 2005 65 Sl12 79 Conclusion Mupirocin is a potentially effective antibiotic against Helieobaeter pylori including elarithromycin metronidazole resistant strains A7 3 Inhibition of SARS Coronavirus 3C Like Protease by lsatis indigotica Root and Plant derived Phenolic Compounds Cheng Wen LIN Fuu Jen TSAI Chang Hai TSAI China Medical Universi Taiehung Taiwan Objectives To test Isatis imiigotica root extract five major compounds of Isatis indigotica root and seven plant derived phenolic compounds for anti SARS CoV 3CLpro effects using cell free and cell based cleavage assays Significance Tile 3C like protease 3CLpro of SARS coronavirus mediates tile proteolytic processing of mplicase polypeptides la and lab into functional proteins becoming an important target for tile drug devdopment Study Design Analytical Methodology Cell free cleavage assay was eawied out using tran scleavage of substrate fusion protein by SARS CoV 3CLpro whereas cell based cleavage assay was according to the cis cleavage of tile 3CLpro substrate luciferase fusion protein in Veto cells Results Cleavage assays with the 3CLpro demonstrated that IC50 values were in micromolar ranges for Isatis indigotica root extract indigo sinigrin aloe emodin and hesperetin Sinigrin IC50 of 217 microM was more efficient on blocking the cleavage processing of the 3Clpro than indigo IC50 of 752 microM and beta sitosterol IC50 of 1210 microM in tile cell based assay Only two phenolic compounds aloe emodin and hespeletin dose dependently inliibited cleavage activity of tile 3CLpro in which the IC50 value was 366 microM for aloe emodin and 8 3 microM for hesperetin in the cell based assay In addition MqW cell proliferation assay indicated that these compounds had no effect on cell viability Conclusiml Hesperetin with IC50 of 8 3 M on tile 3CLpro could be a potent inliibitor on SARS CoV Tliis study will be useful for development of anti SARS drugs A7 4 In V tro Antibacterial Activity of DX 619 A Novel Des Fluoro 6 Quinolone Against Multidrug resistant Gram positive Bacteria Katsuko FUJIKAWA Hiroko ISHIDA Megumi CHIBA Mayumi TANAKA Keniclii SATO New Product Research Laboratories I Daiichi Pharmaceutical Co Ltd Tok2 o Japan Objectives To determine tile antibacteiial and bactelicidal activity propensity of acquired resistance mid mode of action of DX 619 against Gram positive bacteria including older quinolone resistant pathogens Significance Emergence of multidrng resistant Gram positive bacteria has generated worldwide concern in the medical community DX 619 is a novel des F 6 quinolone with expanded activity against Gram positive pathogens Study Design Analytical study on clinical isolates Setting Laboratory Population Gram positive bacteria from clinical isolates Methodology Bacterial strains isolated clinically in Japan in 1994 2000 and 2002 were used Detelmination of MICs mid time 2 g yeth Pharmaceuticals Collegeville PA USA Objective To evaluate tile antibactelial activity of tigecycline against Gram positive and Gram negative pathogens in Asia Significance Tigecycline a member of a new class of antimicrobials glycylcyclines has been shown to have potent expanded broad spectrum activity against most commonly encountered species lesponsible for com munity and hospital acquired infections The T E S T program detelmined the in vitro activity of tigecycline compared to amikacin ampicillin imipenem cefepime ceftazidime ceftliaxone levofloxacin minocycline and piperacillin tazobactam against Gram negative rods in addition to linezolid penicillin and vancomycin for the Gram positive species Isolates were collected from hospitals located in Asia throughout 2004 Study Design In vitro antibiotic susceptibility testing of clinical isolates Population Clinicai isolates Methodology A total of 424 clinical isolates were identified to the species level at each participating site and confirmed by the central laboratory Minimum Inhibitory Concentration MICs were determined by tile local laboratoiy using supplied broth microdilution panels and interpreted according to NCCLS guidelines Results Tigecycline s activity was similar to imipenem against enter obacteriaceae with MICS0 MIC90 of 0 25 1 mcg ml Resistance to third generation cephalosporin was found in 63 2 of E eoli and 77 8 of K pneumoniae consistent with ESBL phenotype Tigecycline inhibited ESBL and AmpC producers with MICs equal or lesser than 1 mcg ml Although similar to other classes of broad spectnml antimicrobial agents against glucose non femrenters tigecycline was especially active against Aemetobaeter spp presenting the lowest MIC90 of 1 mcg ml Tigecycline successfully inhibited S aureus with MIC90 of 0 25 mcg ml regardless of sensitivity or resistance to methicillin The same phenomenon was noticed against enterococci where tigecycline s MIC90 of 0 12 mcg ml was consistent regardless of vmlcomycin susceptibility Conclusion Tigecycline s in vitro activity was comparable to or greater than most commonly prescribed antimicrobials The presented data suggest that tigecycline may be an effective and reliable therapeutic option against both aerobic Gram positive and aerobic Gram negative bacteria including multi drug lesistant strains regardless of degree or type of resistance