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Evaluating omadacycline dosing regimens against drug-resistant pathogens including Staphylococcus aureus , Streptococcus pneumoniae and Haemophilus influenzae in adults: a pharmacokinetic/pharmacodynamic analysis using Monte Carlo simulation
In conclusion, approved oral/intravenous loading and maintenance doses of omadacycline showed enough efficacy in the treatment of ABSSI and CABP caused by the main drug-resistant pathogens.PMID:38591989 | DOI:10.1080/1120009X.2024.2339706 (Source: Journal of Chemotherapy)
Source: Journal of Chemotherapy - April 9, 2024 Category: Cancer & Oncology Authors: Xiao-Chen Wei Ming-Feng Zhao Xia Xiao Source Type: research

Poly(amino acid)-based drug delivery nanoparticles eliminate Methicillin resistant Staphylococcus aureus via tunable release of antibiotic
Colloids Surf B Biointerfaces. 2024 Mar 28;239:113882. doi: 10.1016/j.colsurfb.2024.113882. Online ahead of print.ABSTRACTBacterial infections threaten public health, and novel therapeutic strategies critically demand to be explored. Herein, poly(amino acid) (PAA)-based drug delivery nanoparticles (NPs) were designed for eliminating Methicillin resistant Staphylococcus aureus (MRSA) via tunable release of antibiotic. Using N-acryloyl amino acids (valine, valine methyl ester, aspartic acid, serine) as monomers, four kinds of amphiphilic PAAs were synthesized via photoinduced electron/energy transfer-reversible addition frag...
Source: Colloids and Surfaces - April 9, 2024 Category: Biotechnology Authors: Haofei Li Longlong Yang Wenli Feng Weilin Liu Meng Wang Fang Liu Guofeng Li Xing Wang Source Type: research

Antiseptics in otorhinolaryngology-a substance overview
HNO. 2024 Apr 9. doi: 10.1007/s00106-024-01456-5. Online ahead of print.ABSTRACTFor preoperative skin antisepsis, alcohol-containing iodine solutions and octenidine are suitable. For wound antisepsis, polyhexanide and hypochlorous acid (HOCL) are also available, but only PVP-iodine and HOCL can be applied to cartilage. Chlorhexidine should only be used as mouth- and bodywash for Staphylococcus aureus (MRSA) decolonization. For the many other throat antiseptics, evidence of clinical efficacy is lacking. For decolonization of the nares, polyhexanide and octenidine are available as nasal gels, but these are inferior to mupiro...
Source: HNO - April 9, 2024 Category: ENT & OMF Authors: Bernhard Olzowy Sarina M üller Natascha Antonia Cidlinsky Daniela Guderian Source Type: research

Discovery of olimycin E from Streptomyces sp. 11695
Nat Prod Res. 2024 Apr 8:1-6. doi: 10.1080/14786419.2024.2337131. Online ahead of print.ABSTRACTA new natural product olimycin E (1), together with two known compounds of divergolide R (2) and olimycin B (3), were obtained from the marine-derived Streptomyces sp. 11695. The structures of 1-3 were established on the basis of HRESIMS as well as 1D and 2D NMR datasets. The absolute configuration of 1 is identified as 4 R, 6S, 7S, 10 R by comparison the experiment ECD with that of the theoretical ECD. Antibacterial results showed that compound 2 have antibacterial activities against Staphylococcus aureus and MRSA with the MIC ...
Source: Natural Product Research - April 8, 2024 Category: Biochemistry Authors: Lirong Tu Shumei Shen Zhenyang Yan Xiaoxia Li Kai Liu Jin Xu Minghe Luo Source Type: research

Bioisosteric replacement strategy leads to novel DNA gyrase B inhibitors with improved potencies and properties
In this study, a series of N-heteroaryl-substituted 4-hydroxy-2-quinolone-3-carboxamides were developed using the bioisosteric replacement strategy. As a result of our research, we discovered the two most potent GyrB inhibitors (WBX7 and WBX18), with IC50 values of 0.816 µM and 0.137 µM, respectively. Additional antibacterial activity screening indicated that WBX18 possesses the best antibacterial activity against MRSA, VISA, and VRE strains, with MIC values rangingbetween0.5and 2 µg/mL, which was 2 to over 32 times more potent than that of vancomycin. In vitro safety and metabolic stability, as well as in vivo pharmaco...
Source: Bioorganic Chemistry - April 6, 2024 Category: Chemistry Authors: Wenjie Xue Xueping Zuo Xueqi Zhao Xiaomin Wang Xiangyu Zhang Jie Xia Maosheng Cheng Huali Yang Source Type: research

Endophytes: a uniquely tailored source of potential antibiotic adjuvants
Arch Microbiol. 2024 Apr 6;206(5):207. doi: 10.1007/s00203-024-03891-y.ABSTRACTMultidrug microbial resistance is risking an annual loss of more than 10 million people' lives by 2050. Solutions include the rational use of antibiotics and the use of drugs that reduce resistance or completely obliterate them. Here endophytes come to play due to their high-yield production and inherent nature to produce antimicrobial molecules. Around 40%, 45% and 17% of antibacterial agents were obtained from fungi, actinomycetes, and bacteria, respectively, whose secondary metabolites revealed effectiveness against resistant microbes such as...
Source: Archives of Microbiology - April 6, 2024 Category: Microbiology Authors: Ashaimaa Y Moussa Source Type: research

Antibacterial activity of a short de novo designed peptide against fish bacterial pathogens
Amino Acids. 2024 Apr 5;56(1):28. doi: 10.1007/s00726-024-03388-4.ABSTRACTIn the face of increasing antimicrobial resistance in aquaculture, researchers are exploring novel substitutes to customary antibiotics. One potential solution is the use of antimicrobial peptides (AMPs). We aimed to design and evaluate a novel, short, and compositionally simple AMP with potent activity against various bacterial pathogens in aquaculture. The resulting peptide, KK12YW, has an amphipathic nature and net charge of + 7. Molecular docking experiments disclosed that KK12YW has a strong affinity for aerolysin, a virulence protein produced b...
Source: Amino Acids - April 5, 2024 Category: Biochemistry Authors: Raja Aadil Hussain Bhat Victoria C Khangembam Vinita Pant Ritesh Shantilal Tandel Pramod Kumar Pandey Dimpal Thakuria Source Type: research

Evaluation of the in vitro and in vivo antimicrobial activity of alkaloids prepared from Chelidonium majus L. using MRSA- infected C. elegans as a model host
This study aimed to extract alkaloids from C. majus L. (total alkaloids) and evaluate their antibacterial activity both in vitro and in vivo. Reflux extraction was carried out on C. majus L., and the extract was purified with HPD-600 macroporous resin and 732 cation exchange resin exchange columns. Infection modeling of Caenorhabditis elegans (C. elegans) was established to investigate the impact of Methicillin-resistant Staphylococcus aureus (MRSA) and Methicillin-sensitive Staphylococcus aureus (MSSA) on the motility, longevity, and reactive oxygen species (ROS) levels of wild-type worms (N2 strain). The effects of total...
Source: Fitoterapia - April 5, 2024 Category: Biochemistry Authors: Jinchai Qi Xinyun Zhang Xiaochen Guo Yuping Yang Xiaoxiao Fan Yunfeng Han Yonggang Liu Source Type: research

Discovery of a novel class of rosmarinic acid derivatives as antibacterial agents: Synthesis, structure-activity relationship and mechanism of action
Bioorg Chem. 2024 Mar 28;146:107318. doi: 10.1016/j.bioorg.2024.107318. Online ahead of print.ABSTRACTTwenty-seven rosmarinic acid derivatives were synthesized, among which compound RA-N8 exhibited the most potent antibacterial ability. The minimum inhibition concentration of RA-N8 against both S. aureus (ATCC 29213) and MRSA (ATCC BAA41 and ATCC 43300) was found to be 6 μg/mL, and RA-N8 killed E. coli (ATCC 25922) at 3 μg/mL in the presence of polymyxin B nonapeptide (PMBN) which increased the permeability of E. coli. RA-N8 exhibited a weak hemolytic effect at the minimum inhibitory concentration. SYTOX Green assay, SEM...
Source: Bioorganic Chemistry - April 5, 2024 Category: Chemistry Authors: Yong Wang Zhiguang Liang Yihui Cao Cheung-Hin Hung Ruolan Du Alan Siu-Lun Leung Pui-Kin So Pak-Ho Chan Wing-Leung Wong Yun-Chung Leung Kwok-Yin Wong Source Type: research