A rapid in vitro prescreen for Fe-binding chelators has been developed with growth of Crithidia fasciculata and the sparing of its heme requirement in a defined medium as a test system. The prescreen functions as an index of chelator-mediated Fe transport and as an index of growth inhibition, presumably by the interference with Fe and/or heme metabolism at intracellular chelatable sites. Of 161 chelators examined, 84 were active heme-sparers; 32 of these inhibited growth at low chelator concentrations. Twenty-eight other chelators inhibited growth and another 49 were inactive. Such chelating activity directed at Fe and heme targets in hemoflagellates may provide leads for chemotherapy.

Download full-text PDF

Source
http://dx.doi.org/10.1111/j.1550-7408.1981.tb02869.xDOI Listing

Publication Analysis

Top Keywords

rapid vitro
8
vitro prescreen
8
growth crithidia
8
crithidia fasciculata
8
inhibited growth
8
growth
5
chelators
4
prescreen chelators
4
chelators potential
4
potential trypanocides
4

Similar Publications

The fluorescent imaging of pathologically accumulated β-amyloid (Aβ) proteins is of significant importance to the diagnosis of Alzheimer's disease (AD). In the paper, we prepared two new NIR probes, NIR-1 and NIR-2, through hydrophilic modification of introducing water-soluble bioactive groups such as polyethylene glycol (PEG) and morpholine to tune in vivo pharmacokinetics for specific detection of soluble and insoluble Aβ species. The in vitro assessments confirm that both NIR-1 and NIR-2 display strong near-infrared (NIR) fluorescence (FL) enhancement upon association with Aβ42 monomers, oligomers or aggregates (λem > 670 nm) and show high sensitive, rapid and selective response towards Aβ42 species.

View Article and Find Full Text PDF

Massive blood loss is the main cause of prehospital trauma-related death, the development of rapid and effective hemostatic materials is imminent. Injectable hydrogels have the advantages of covering irregular bleeding sites and quickly closing the wound. However, its inherent viscosity can easily precipitate tissue adhesion and other complications.

View Article and Find Full Text PDF

Background: Contezolid (CZD) is an analog of Linezolid (LZD) that has demonstrated potent in vitro and in vivo activity against tuberculosis (TB) while presenting a safer side-effect profile. In this study, we evaluated the early bactericidal activity (EBA) of CZD compared to LZD, with LZD serving as a control.

Methods: Naive, smear-positive pulmonary TB patients were enrolled and randomly assigned to receive either a 14-day monotherapy regimen of 600 mg LZD once daily (QD) or 800 mg CZD twice daily (BID).

View Article and Find Full Text PDF

RNA polymerase II (RNAPII) is regulated by sequence-specific transcription factors (TFs) and the pre-initiation complex (PIC): TFIIA, TFIIB, TFIID, TFIIE, TFIIF, TFIIH, Mediator. TFs and Mediator contain intrinsically-disordered regions (IDRs) and form phase-separated condensates, but how IDRs control RNAPII function remains poorly understood. Using purified PIC factors, we developed a Real-time In-vitro Fluorescence Transcription assay (RIFT) for second-by-second visualization of RNAPII transcription at hundreds of promoters simultaneously.

View Article and Find Full Text PDF

Doxycycline post-exposure prophylaxis (doxy-PEP) is a preventative strategy demonstrated to reduce bacterial sexually transmitted infections in high-risk populations. However, the impact of doxy-PEP on antibiotic resistance acquisition in key members of our microbiomes, is as of yet unclear. For example, commensal are known reservoirs of resistance for gonococci through horizontal gene transfer (HGT), and are more likely to experience bystander selection due to doxy-PEP as they are universally carried.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!