ABSTRACT
Microspore cell death and low green plant production efficiency are an integral obstacle in the development of doubled haploid production in wheat. The aim of the current study was to determine the effect of anti-apoptotic recombinant human B-cell lymphoma-2 (Bcl-2â³21) and caspase-3-inhibitor (Ac-DEVD-CHO) in microspore cell death in bread wheat cultivars AC Fielder and AC Andrew. Induction medium containing Bcl-2â³21 and Ac-DEVD-CHO yielded a significantly higher number of viable microspores, embryo-like structures and total green plants in wheat cultivars AC Fielder and AC Andrew. Total peroxidase activity was lower in Bcl-2â³21 treated microspore cultures at 96 h of treatment compared to control and Ac-DEVD-CHO. Electron paramagnetic resonance study of total microspore protein showed a different scavenging activity for Bcl-2â³21 and Ac-DEVD-CHO. Bcl-2â³21 scavenged approximately 50% hydroxyl radical (HOâ¢) formed, whereas Ac-DEVD-CHO scavenged approximately 20% of HOâ¢. Conversely, reduced caspase-3-like activities were detected in the presence of Bcl-2â³21 and Ac-DEVD-CHO, supporting the involvement of Bcl-2â³21 and Ac-DEVD-CHO in increasing microspore viability by reducing oxidative stress and caspase-3-like activity. Our results indicate that Bcl-2â³21 and Ac-DEVD-CHO protects cells from cell death following different pathways. Bcl-2â³21 prevents cell damage by detoxifying HO⢠and suppressing caspase-3-like activity, while Ac-DEVD-CHO inhibits the cell death pathways by modulating caspase-like activity.
ABSTRACT
In an effort to develop new and more effective therapies to treat tuberculosis, a series of benzothiadiazine 1,1-dioxide derivatives were synthesized and their in vitro activity against Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium intracellulare was evaluated. One of the compounds, 8c, exhibited potent anti-tubercular activity, particularly for the resistant strains and thus prompted us to investigate its in vivo profile. However, the in vivo testing in a mouse model of tuberculosis infection did not show significant anti-tubercular activity, probably because of its poor bioavailability.
Subject(s)
Antitubercular Agents/chemical synthesis , Antitubercular Agents/pharmacology , Benzothiadiazines/chemical synthesis , Benzothiadiazines/pharmacology , Mycobacterium/drug effects , Animals , Antitubercular Agents/chemistry , Benzothiadiazines/chemistry , Drug Design , Drug Resistance, Bacterial , Female , In Vitro Techniques , Mice , Microbial Sensitivity Tests , Mycobacterium avium/drug effects , Mycobacterium avium Complex/drug effects , Mycobacterium tuberculosis/drug effects , Tuberculosis/drug therapyABSTRACT
A series of aryloxy/thioaryloxy oxazolidinone derivatives has been synthesized and tested for in vitro antibacterial activity by MIC determination against a panel of susceptible and resistant Gram-positive and Gram-negative microorganisms, some of which are resistant to methicillin and vancomycin. Compounds 12a, 12b, 14a, and 14b from this series were found to be equipotent or more potent than linezolid in vitro.
