Synthetic piperidine-substituted chalcones as potential hits for α-amylase inhibitory and antioxidant activities.

Background: In medicinal chemistry, searching for new therapeutic entities to treat diabetes mellitus is of great concern. The piperidinyl-substituted chalcone scaffold has piqued our interest as a potential antidiabetic agent. Methods: A variety of piperidinyl-substituted chalcones 2-28 were synthesized and tested for α-amylase inhibitory and 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical-scavenging activities. Results: Compared with the standard acarbose, all compounds inhibited α-amylase, with IC50 values of 9.86-35.98 µM. Docking studies revealed an important binding interaction with the enzyme's catalytic site. The compounds also demonstrated promising radical-scavenging potential against  2,2-diphenyl-1-picrylhydrazyl and  2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radicals. Conclusion: This study has identified potential lead candidates for further advanced research searching for antidiabetic agents.

Decline in mild stroke presentations and intravenous thrombolysis during the COVID-19 pandemic: The Society of Vascular and Interventional Neurology Multicenter Collaboration.

BACKGROUND: To evaluate overall ischemic stroke volumes and rates, specific subtypes, and clinical presentation during the COVID-19 pandemic in a multicenter observational study from eight states across US. METHODS: We compared all ischemic strokes admitted between January 2019 and May 2020, grouped as; March-May 2020 (COVID-19 period) and March-May 2019 (seasonal pre-COVID-19 period). Primary outcome was stroke severity at admission measured by NIHSS stratified as mild (0-7), moderate [8-14], and severe (>14). Secondary outcomes were volume of large vessel occlusions (LVOs), stroke etiology, IV-tPA rates, and discharge disposition. RESULTS: Of the 7969 patients diagnosed with acute ischemic stroke during the study period, 933 (12 %) presented in the COVID-19 period while 1319 (17 %) presented in the seasonal pre-COVID-19 period. Significant decline was observed in the mean weekly volumes of newly diagnosed ischemic strokes (98 ± 3 vs 50 ± 20,p = 0.003), LVOs (16.5 ± 3.8 vs 8.3 ± 5.9,p = 0.008), and IV-tPA (10.9 ± 3.4 vs 5.3 ± 2.9,p = 0.0047), whereas the mean weekly proportion of LVOs (18 % ±5 vs 16 % ±7,p = 0.24) and IV-tPA (10.4 % ±4.5 vs. 9.9 % ±2.4,p = 0.66) remained the same, when compared to the seasonal pre-COVID-19 period. Additionally, an increased proportion of patients presented with a severe disease (NIHSS > 14) during the COVID-19 period (29.7 % vs 24.5 %,p < 0.025). The odds of being discharged to home were 26 % greater in the COVID-19 period when compared to seasonal pre-COVID-19 period (OR:1.26, 95 % CI:1.07-1.49,p = 0.016). CONCLUSIONS: During COVID-19 period there was a decrease in volume of newly diagnosed ischemic stroke cases and IV-tPA administration. Patients admitted to the hospital had severe neurological clinical presentation and were more likely to discharge home.

Comparison of 12-Hour with 72-Hour Terlipressin Therapy for Bleeding Esophageal Varices.

OBJECTIVE: To determine the efficacy of 12-hour of Terlipressin therapy as compared to 72-hour therapy in preventing rebleeding after endoscopic therapy. STUDY DESIGN: Interventional study. PLACE AND DURATION OF STUDY: Department of Gastroenterology and Hepatology, Shaikh Zayed Hospital, Lahore, from January to March 2016. METHODOLOGY: Cirrhotic patients presenting to our hospital with GI (gastrointestinal) bleeding received Terlipressin 2 mg intravenous bolus, followed by 1mg 6-hourly until undergoing endoscopy. Those with esophageal varices as the source of bleeding underwent band ligation and were recruited. Of the 93 enrolled patients, 90 remained and were randomized into 25 (27.8%) in control Group-Aand 65 (72.2%) in test Group-B. Group-Areceived 72-hour of Terlipressin while Group-B received it for 12-hour. Both groups were monitored for rebleeding for 5 days. RESULTS: Rebleeding occurred in 1 (4%) patient in Group-Aand 3 (4.6%) in Group-B during the 5-day period. All 4 (4.4%) underwent repeat endoscopy. The Group-Apatient and 2 (3%) of 3 Group-B patients showed ulcers over band ligation sites as source of bleed. The third Group-B patient showed varices requiring repeat banding. One (4%) patient (Group-A) died due to persistent encephalopathy. No drug related adverse effects were seen. CONCLUSION: A12-hour duration of Terlipressin as an adjunct to endoscopic band ligation shows similar results to 72-hour therapy.

3D Gabor wavelet based vessel filtering of photoacoustic images.

Filtering and segmentation of vasculature is an important issue in medical imaging. The visualization of vasculature is crucial for the early diagnosis and therapy in numerous medical applications. This paper investigates the use of Gabor wavelet to enhance the effect of vasculature while eliminating the noise due to size, sensitivity and aperture of the detector in 3D Optical Resolution Photoacoustic Microscopy (OR-PAM). A detailed multi-scale analysis of wavelet filtering and Hessian based method is analyzed for extracting vessels of different sizes since the blood vessels usually vary with in a range of radii. The proposed algorithm first enhances the vasculature in the image and then tubular structures are classified by eigenvalue decomposition of the local Hessian matrix at each voxel in the image. The algorithm is tested on non-invasive experiments, which shows appreciable results to enhance vasculature in photo-acoustic images.

Predictors of two months culture conversion in multidrug-resistant tuberculosis: findings from a retrospective cohort study.

BACKGROUND: Various studies have reported culture conversion at two months as a predictor of successful treatment outcome in multidrug-resistant tuberculosis (MDR-TB). OBJECTIVES: The present study was conducted with the aim to evaluate the rate and predictors of culture conversion at two months in MDR-TB patients. METHODS: All confirmed pulmonary MDR-TB patients enrolled for treatment at Lady Reading Hospital Peshawar, Pakistan from 1 January to 31 December 2012 and met the inclusion criteria were reviewed retrospectively. Rate and predictors of culture conversion at two months were evaluated. RESULTS: Eighty seven (53.4%) out of 163 patients achieved culture conversion at two months. In a multivariate analysis lung cavitation at baseline chest X-ray (P = 0.006, OR = 0.349), resistance to ofloxacin (P = 0.041, OR = 0.193) and streptomycin (P = 0.017, OR = 0.295) had statistically significant (P<0.05) negative association with culture conversion at two months. CONCLUSION: A reasonable proportion of patients achieved culture conversion at two months. Factors negatively associated with culture conversion at two months can be easily identified either before diagnosis or early in the course of MDR-TB treatment. This may help in better care of individual patients by identifying them early and treating them vigorously.