Biological Significance of Ultrasound Assisted Synthesized Polycyclic Azetidine Derivatives
POLYCYCLIC AROMATIC COMPOUNDS
Authors: Chavan, Pravin; Jadhav, Shivaji; Farooqui, Mazahar; Rai, Megha
Synthesized N-(7-R)-2-oxa-8-azabicyclo[4.2.0]octan-8-yl)isonicotinamide derivatives (4a-n) and N-(2,4-dioxo-3-oxa-6-azabicyclo[3.2.0]heptan-6-yl)isonicotinamide derivatives (5a-m) were screened for biologically activity. Both azetidine derivatives (4a-n) and (5a-m) were screened for antibacterial activity by 'Disk Diffusion method' using Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Staphylococcus aureus (ATCC 25923) and antifungal activity using candida sp. Similar series of azetidine derivatives (4a-n) and (5a-m) were screened for in vitro antituberculosis activity by 'Clairo Combi method' using Mycobacterium tuberculosis and in vitro anti-inflammatory activity was evaluated using 'HRBC membrane stabilization method'. Experimented azetidine derivatives excellent biological activities, (N-(7-R)-2-oxa-6-azabicyclo [3.2.0] heptan-6-yl) isonicotinamide derivatives (4a-n) against S. aureus bacteria and N-(2,4-dioxo-3-oxa-6-azabicyclo[3.2.0] heptan-6-yl) isonicotinamide derivatives (5a-m) against M. tuberculosis (T.B.). Both series of azetidine derivatives (4a-n) and (5a-m) show potent anti-inflammatory activity. All synthesized azetidine derivatives (4a-n) and (5a-m) were characterized by IR, H-1 NMR, 13C NMR and elemental analysis.
Characterization of antibody response against 16kD and 38kD of M. tuberculosis in the assisted diagnosis of active pulmonary tuberculosis
ANNALS OF TRANSLATIONAL MEDICINE
Authors: Hao, Xiaohui; Bai, Jie; Ding, Yingying; Wang, Jinhong; Liu, Yidian; Yao, Lan; Pan, Wei
Background: In view of the inability of traditional etiological methods to diagnose pulmonary tuberculosis rapidly and effectively, the antibody responses against 38kD and 16kD-antigens of Mycobacterium tuberculosis (M. tuberculosis) were both detected in order to obtain a better serological detection method for M. tuberculosis. Methods: M. tuberculosis-secreted protein 38kD and membrane protein 16kD were prokaryotically expressed and purified, and then used as detection antigens. A novel evolved immunoglobulin-binding molecule (NEIBM)-ELISA method was used to detect antibody levels against 38kD and 16kD in active tuberculosis patients (confirmed tuberculosis cases and clinically diagnosed cases), to explore the significance of these two antigens in serological detection of M. tuberculosis, and to study the diagnostic value of the combined detection of the two antigens in active pulmonary tuberculosis. Results: The results showed that the positive detection rates of the 16kD antigen and 38kD antigen of M. tuberculosis were higher (about 44%) in the confirmed cases of tuberculosis, and there was no significant difference in the positive detection rates of the two antigens (P=0.786). The combined detection of these two antigens showed that the positive detection rate could be increased to 61.5%, which was significantly better than the detection effect of the two antigens alone. The positive detection rates of 16kD and 38kD antigens were 26-30% in clinically diagnosed tuberculosis cases, which were lower than those in confirmed tuberculosis cases, and there was no significant difference in the positive detection rates of the two antigens (P=0.242). The detection effect of the two combined antigens was better than that of the 16kD and 38kD antigens alone, but the detection rate was still lower than that of the confirmed tuberculosis cases. Conclusions: This study found that the detection effect of 16kD and 38kD antigens was similar in confirmed cases and clinically diagnosed cases of pulmonary tuberculosis, and that the detection effect needs to be further improved. The combined detection of the two antigens showed a significantly better detection effect than the two antigens alone, suggesting that the combined detection of multiple antigens can be used for serological diagnosis of M. tuberculosis infection in clinic.