The main protease (Mpro) is a major protease having an important role in viral replication of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the novel coronavirus that caused the pandemic of 2020. Here, active Mpro was obtained as a 34.5 kDa protein by overexpression in E. coli BL21 (DE3). The optimal pH and temperature of Mpro were 7.5 and 37 °C, respectively. Mpro displayed a Km value of 16 μM with Dabcyl-KTSAVLQ↓SGFRKME-Edans. Black garlic extract and 49 polyphenols were studied for their inhibitory effects on purified Mpro. The IC50 values were 137 μg/mL for black garlic extract and 9–197 μM for 15 polyphenols. The mixtures of tannic acid with puerarin, daidzein, and/or myricetin enhanced the inhibitory effects on Mpro. The structure–activity relationship of these polyphenols revealed that the hydroxyl group in C3′, C4′, C5′ in the B-ring, C3 in the C-ring, C7 in A-ring, the double bond between C2 and C3 in the C-ring, and glycosylation at C8 in the A-ring contributed to inhibitory effects of flavonoids on Mpro.
The risk factors for perforations during ESD could differ according to the type of perforation. Therefore, although macroperforation did not develop during ESD, it would be necessary to consider the possibility of microperforation in case of old age, long procedure time, and (deep) depth of invasion.
Tumor number at the time of ESD and age could be predictive factors for the presence of missed synchronous lesions after ESD. Careful endoscopic surveillance should be performed after ESD for multiple lesions or for elderly patients.
Background/AimsThe placement of self expandable metal stent (SEMS) is one of the palliative therapeutic options for patients with unresectable malignant biliary obstruction. The aim of this study was to compare the effectiveness of a covered SEMS versus the conventional plastic stent.MethodsWe retrospectively evaluated 44 patients with unresectable malignant biliary obstruction who were treated with a covered SEMS (21 patients) or a plastic stent (10 Fr, 23 patients). We analyzed the technical success rate, functional success rate, early complications, late complications, stent patency and survival rate.ResultsThere was one case in the covered SEMS group that had failed technically, but was corrected successfully using lasso. Functional success rates were 90.5% in the covered SEMS group and 91.3% in the plastic stent group. There was no difference in early complications between the two groups. Median patency of the stent was significantly prolonged in patients who had a covered SEMS (233.6 days) compared with those who had a plastic stent (94.6 days) (p=0.006). During the follow-up period, stent occlusion occurred in 11 patients of the covered SEMS group. Mean survival showed no significant difference between the two groups (covered SEMS group, 236.9 days; plastic stent group, 222.3 days; p=0.182).ConclusionsThe patency of the covered SEMS was longer than that of the plastic stent and the lasso of the covered SEMS was available for repositioning of the stent.
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