Natural cyclopeptides are hot spots in chemical and pharmaceutical fields because of the wide spreading bio-resources, complex molecular structures and various bioactivities. Bio-producers of cyclopeptides distribute over almost every kingdom from bacteria to plants and animals. Many cyclopeptides contain non-coded amino acids and non-pepditic bonds. Most exciting characteristic of cyclopeptides is a range of interesting bioactivities such as antibiotics gramicidin-S (2), vancomycin (3) and daptomycin (4), immunosuppressive cyclosporin-A (1) and astin-C (8), and anti-tumor aplidine (5), RA-V (6) and RA-VII (7). Compounds 1-4 are being used in clinics; compounds 5-8 are in the stages of clinical trial or as a candidate for drug research. In this review, the progress in chemical and bioactive studies on these important natural bioactive cyclopeptides 1-8 are introduced, mainly including discovery, bioactivity, mechanism, QSAR and synthesis.
Animals ; Anti-Bacterial Agents ; chemical synthesis ; chemistry ; pharmacology ; Antineoplastic Agents ; chemical synthesis ; chemistry ; therapeutic use ; Cyclosporine ; chemistry ; pharmacology ; Daptomycin ; chemical synthesis ; chemistry ; pharmacology ; Depsipeptides ; chemical synthesis ; chemistry ; therapeutic use ; Gramicidin ; chemical synthesis ; chemistry ; pharmacology ; Humans ; Immunosuppression ; Immunosuppressive Agents ; chemical synthesis ; chemistry ; pharmacology ; Molecular Structure ; Neoplasms ; drug therapy ; Peptides, Cyclic ; chemical synthesis ; chemistry ; pharmacology ; therapeutic use ; Quantitative Structure-Activity Relationship ; Vancomycin ; chemical synthesis ; chemistry ; pharmacology

Eradication regimens for Helicobacter pylori infection have some side effects, compliance problems, relapses, and antibiotic resistance. Therefore, alternative anti-H. pylori or supportive antimicrobial agents with fewer disadvantages are necessary for the treatment of H. pylori. We investigated the pH-(5.0, 6.0, 7.0, 8.0, 9.0, and 10.0) and concentration (0.032, 0.064, 0.128, 0.256, 0.514, and 1.024 mg/mL)-dependent antibacterial activity of crude urushiol extract from the sap of the Korean lacquer tree (Rhus vernicifera Stokes) against 3 strains (NCTC11637, 69, and 219) of H. pylori by the agar dilution method. In addition, the serial (before incubation, 3, 6, and 10 min after incubation) morphological effects of urushiol on H. pylori were examined by electron microscopy. All strains survived only within pH 6.0-9.0. The minimal inhibitory concentrations of the extract against strains ranged from 0.064 mg/mL to 0.256 mg/mL. Urushiol caused mainly separation of the membrane, vacuolization, and lysis of H. pylori. Interestingly, these changes were observed within 10 min following incubation with the 1 x minimal inhibitory concentrations of urushiol. The results of this work suggest that urushiol has potential as a rapid therapeutic against H. pylori infection by disrupting the bacterial cell membrane.
Anti-Bacterial Agents/chemistry/*pharmacology/therapeutic use ; Catechols/chemistry/*pharmacology/therapeutic use ; Cell Membrane/drug effects/ultrastructure ; Helicobacter Infections/drug therapy ; Helicobacter pylori/*drug effects/ultrastructure ; Humans ; Microbial Sensitivity Tests ; Microbial Viability/drug effects ; Molecular Structure ; Rhus/*chemistry

OBJECTIVETo review the progress in the study of chemical ingrediens, pharmacological effects and clinical application of Allium macrostemon Bunge.

METHODDocuments of experimental and clinical study on A. macrostemon in recent 10 years were consulted and summarized.

RESULTA. macrostemon had many active ingredients, pharmacology effects and wild clinical application.

CONCLUSIONThe results provide a rational foundation for the further development and utilization of A. macrostemon.

Allium ; chemistry ; Animals ; Anti-Asthmatic Agents ; pharmacology ; therapeutic use ; Anti-Bacterial Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; therapeutic use ; Humans ; Oils, Volatile ; isolation & purification ; pharmacology ; Phytotherapy ; Plants, Medicinal ; chemistry ; Platelet Aggregation Inhibitors ; pharmacology ; Pulmonary Disease, Chronic Obstructive ; drug therapy

No abstract available.
Adolescent ; Adult ; Aged ; Aged, 80 and over ; Anti-Bacterial Agents/pharmacology/therapeutic use ; Ceftriaxone/pharmacology/therapeutic use ; Echocardiography ; Endocarditis, Bacterial/*diagnosis/drug therapy/microbiology ; Female ; Humans ; Immunosuppressive Agents/therapeutic use ; Infant, Newborn ; Male ; Microbial Sensitivity Tests ; Micrococcaceae/drug effects/*isolation & purification ; Middle Aged ; RNA, Ribosomal, 16S/chemistry/metabolism ; Republic of Korea

No abstract available.
Adult ; Anti-Bacterial Agents/pharmacology/therapeutic use ; Bone Marrow Transplantation ; Capnocytophaga/drug effects/genetics/*isolation & purification ; Gram-Negative Bacterial Infections/complications/*diagnosis/drug therapy ; Humans ; Leukemia, Lymphocytic, Chronic, B-Cell/complications/*diagnosis ; Male ; Microbial Sensitivity Tests ; Penicillanic Acid/analogs & derivatives/pharmacology/therapeutic use ; Piperacillin/pharmacology/therapeutic use ; RNA, Ribosomal, 16S/chemistry/metabolism ; Sequence Analysis, RNA ; Sequence Homology, Nucleic Acid ; Transplantation, Homologous ; Treatment Outcome

AIMTo find new antibacterial agents of quinolone with high activity and low toxicity.

METHODSTo design and synthesize 7-(7-aminomethyl-5-azaspiro [2,4] hept-5-yl)-1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and its analogues, and to study their antibacterial activity in vitro and in vivo.

RESULTSTwenty new compounds (2 - 11, 17 - 26) were obtained including five targeted compounds (22 - 26). The structures of the compounds were confirmed by 1HNMR, MS and HRMS. Compounds 22 - 26 showed broad spectrum of antibacterial activity against Gram-positive and Gram-negative organisms. Especially for compound 24, the relevant MIC values for 13 strains of Gram-positive organisms were < 0.001 - 0.03 mg(-1), including 4 strains of S. pneumoniae, 2 strains of S. pyogenes, 3 strains of S. aureus and 2 strains of Enterococci which exhibited more potent activity than contrast agents (clinafloxacin and gatifloxacin). The MIC values of 24 for 6 strains Gram-positive organisms were 0.01 - 1 mg x L(-1), which exhibited equal or lower activity than contrast agents. They were more effective than ciprofloxacin and gatifloxacin against intraperitoneal infections caused by S. pneumoniae and S. aureus in mice.

CONCLUSIONCompounds (23, 24 and 26) showed excellent antibacterial activity in vitro and in vivo and should be worth further investigation.

Animals ; Anti-Bacterial Agents ; chemical synthesis ; pharmacology ; Ciprofloxacin ; pharmacology ; Female ; Fluoroquinolones ; pharmacology ; Male ; Mice ; Mice, Inbred ICR ; Molecular Conformation ; Molecular Structure ; Quinolines ; chemical synthesis ; chemistry ; pharmacology ; therapeutic use ; Spiro Compounds ; chemical synthesis ; chemistry ; pharmacology ; therapeutic use ; Staphylococcus aureus ; drug effects ; Streptococcus pneumoniae ; drug effects

Coagulase-negative staphylococci (CoNS) are reported to be the leading cause of nosocomial bloodstream infections. Staphylococcus pettenkoferi is a novel member of CoNS that was first isolated from the human blood and bursitis wound in 2002. We have reported cases of 6 S. pettenkoferi strains isolated from blood specimens, including one pathogen and 5 contaminants and catheter colonizers. Brucker Biotyper (Brucker Daltonics, Bremen, Germany) and molecular typing with 16S rRNA gene sequencing confirmed the 6 isolates as S. pettenkoferi. The conventional phenotypic identification of these isolates is not reliable owing to their inconsistent biochemical characteristics. Five of the 6 isolates were found to be resistant to oxacillin, and all isolates showed susceptibility to vancomycin and linezolid. For accurate identification of this novel species, advanced methods by using Brucker Biotyper or molecular methods such as 16S rRNA gene sequencing are required.
Aged ; Aged, 80 and over ; Anti-Bacterial Agents/pharmacology/therapeutic use ; DNA, Bacterial/chemistry/metabolism ; Drug Resistance, Bacterial/drug effects ; Female ; Humans ; Linezolid/pharmacology ; Male ; Microbial Sensitivity Tests ; Middle Aged ; Oxacillin/pharmacology ; Phenotype ; RNA, Ribosomal, 16S/chemistry/genetics/metabolism ; Sequence Analysis, DNA ; Staphylococcal Infections/drug therapy/*microbiology/pathology ; Staphylococcus/drug effects/*genetics/isolation & purification ; Vancomycin/pharmacology

BACKGROUND: We investigated the whole genome sequence (WGS) of a carbapenem-resistant Acinetobacter baumannii isolate belonging to the global clone 2 (GC2) and predicted resistance islands using a software tool. METHODS: A. baumannii strain YU-R612 was isolated from the sputum of a 61-yr-old man with sepsis. The WGS of the YU-R612 strain was obtained by using the PacBio RS II Sequencing System (Pacific Biosciences Inc., USA). Antimicrobial resistance genes and resistance islands were analyzed by using ResFinder and Genomic Island Prediction software (GIPSy), respectively. RESULTS: The YU-R612 genome consisted of a circular chromosome (ca. 4,075 kb) and two plasmids (ca. 74 kb and 5 kb). Its sequence type (ST) under the Oxford scheme was ST191, consistent with assignment to GC2. ResFinder analysis showed that YU-R612 possessed the following resistance genes: four β-lactamase genes bla(ADC-30), bla(OXA-66), bla(OXA-23), and bla(TEM-1); armA, aadA1, and aacA4 as aminoglycoside resistance-encoding genes; aac(6')Ib-cr for fluoroquinolone resistance; msr(E) for macrolide, lincosamide, and streptogramin B resistance; catB8 for phenicol resistance; and sul1 for sulfonamide resistance. By GIPSy analysis, six putative resistant islands (PRIs) were determined on the YU-R612 chromosome. Among them, PRI1 possessed two copies of Tn2009 carrying bla(OXA-23), and PRI5 carried two copies of a class I integron carrying sul1 and armA genes. CONCLUSIONS: By prediction of resistance islands in the carbapenem-resistant A. baumannii YU-R612 GC2 strain isolated in Korea, PRIs were detected on the chromosome that possessed Tn2009 and class I integrons. The prediction of resistance islands using software tools was useful for analysis of the WGS.
Acinetobacter Infections/*drug therapy/microbiology ; Acinetobacter baumannii/drug effects/*genetics/isolation & purification ; Anti-Bacterial Agents/pharmacology/*therapeutic use ; Bacterial Proteins/genetics ; Carbapenems/*therapeutic use ; DNA, Bacterial/chemistry/*genetics/metabolism ; Drug Resistance, Bacterial ; Genomic Islands/genetics ; Humans ; Microbial Sensitivity Tests ; Multilocus Sequence Typing ; Plasmids/genetics/metabolism ; Polymerase Chain Reaction ; Sequence Analysis, DNA

No abstract available.
Aged ; Anti-Bacterial Agents/pharmacology/therapeutic use ; Cefotaxime/analogs & derivatives/therapeutic use ; Cholangiopancreatography, Endoscopic Retrograde ; Gallstones/surgery ; Gram-Negative Anaerobic Bacteria/drug effects/genetics/*isolation & purification ; Gram-Negative Bacterial Infections/*diagnosis/drug therapy/microbiology ; Humans ; Male ; Metronidazole/therapeutic use ; Microbial Sensitivity Tests ; RNA, Ribosomal, 16S/chemistry/genetics/metabolism ; Sequence Analysis, DNA ; Tomography, X-Ray Computed

OBJECTIVETo compare the antibacterial effects of Huangqin-Tang with its metabolites produced by intestinal flora.

METHODThe antibacterial tests in vitro and in vivo were performed by agar dilution method and lethal protection of animal respectively.

RESULTHuangqin-Tang and its metabolites had antibacterial action on bacteria in vitro, however the antibacterial activity of metabolites of Huangqin-Tang on Salmomella, Dysentery bacillus and Proteus in vitro was stronger than Huangqin-Tang. The metabolites of Huangqin-Tang had protective effect on the animals infected by Staphylococcus aureus and Escherichia coli respectively from death, but Huangqin-Tang had no lethal protection action.

CONCLUSIONThe antibacterial effects of metabolites of Huangqin-Tang in vitro and in vivo are stronger than that of Huangqin-Tang, which shows that intestinal flora play a very important role in antibacterial effects of Huangqin-Tang.

Animals ; Anti-Bacterial Agents ; pharmacology ; therapeutic use ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Escherichia coli Infections ; drug therapy ; Feces ; microbiology ; Intestines ; microbiology ; Male ; Mice ; Phytotherapy ; Plants, Medicinal ; chemistry ; Proteus ; drug effects ; Salmonella ; drug effects ; Shigella dysenteriae ; drug effects ; Staphylococcal Infections ; drug therapy