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Objective: To investigate the clinical potential and safety of Moluodan to reverse gastric precancerous lesions. Methods: Patients aged 18–70 years diagnosed with moderate‐to‐severe atrophy and/or moderate‐to‐severe intestinal metaplasia, with or without low‐grade dysplasia, and negative for Helicobacter pylori were recruited in this randomized, double‐blind, parallel‐controlled trial. The primary outcome was the improvement of global histological diagnosis at 1‐year follow‐up endoscopy using the operative link for gastritis assessment, the operative link for gastric intestinal metaplasia assessment, and the disappearance rate of dysplasia. Results: Between November 3, 2017 and January 27, 2021, 166 subjects were randomly assigned to the Moluodan group, 168 to the folic acid group, 84 to the combination group, and 84 to the high‐dose Moluodan group. The improvement in global histological diagnosis was achieved in 60 (39.5%) subjects receiving Moluodan, 59 (37.8%) receiving folic acid, 26 (32.1%) receiving the combined drugs, and 36 (47.4%) receiving high‐dose Moluodan. Moluodan was non‐inferior to folic acid (95% confidence interval: −9.2 to 12.5; P = 0.02). High‐dose Moluodan had a trend for better protective efficacy, though there was no statistical significance. The disappearance rate of dysplasia was 82.8% in the Moluodan group, which was superior to folic acid (53.9%; P = 0.006). No drug‐related serious adverse events were observed. Conclusions: One pack of Moluodan three times daily for 1 year was safe and effective in reversing gastric precancerous lesions, especially dysplasia. Doubling its dose showed a better efficacy trend. [ABSTRACT FROM AUTHOR]

Gut microbiome is integral to the pathogenesis of ulcerative colitis. A novel probiotic Lactobacillus intestinalis (L. intestinalis) exerts a protective effect against dextran sodium sulfate‐induced colitis in mice. Based on flow cytometry, colitis‐associated Th17 cells are the target of L. intestinalis, which is supported by the lack of protective effects of L. intestinalis in T cell‐null Rag1−/− mice or upon anti‐IL‐17‐A antibody‐treated mice. Although L. intestinalis exerts no direct effect on T cell differentiation, it decreases C/EBPA‐driven gut epithelial SAA1 and SAA2 production, which in turn impairs Th17 cell differentiation. Cometabolism of L. intestinalis ALDH and host ALDH1A2 contributed to elevated biosynthesis of retinoic acid (RA), which accounts for the anti‐colitis effect in RAR‐α ‐mediated way. In a cohort of ulcerative colitis patients, it is observed that fecal abundance of L. intestinalis is negatively associated with the C/EBPA‐SAA1/2‐Th17 axis. Finally, L. intestinalis has a synergistic effect with mesalazine in alleviating murine colitis. In conclusion, L. intestinalis and associated metabolites, RA, have potential therapeutic effects for suppressing colonic inflammation by modulating the crosstalk between intestinal epithelia and immunity. [ABSTRACT FROM AUTHOR]

Catalytic tandem cyclization of ynamides has attracted considerable interest in organic synthesis because of its atom economy in the rapid formation of polycyclic compounds. However, examples on the construction of pentacyclic spiroindolines are quite scarce. Herein, we described a BiCl3‐mediated tandem cyclization reaction of tryptamine‐ynamides, which led to the formation of appealing pentacyclic spiroindoline scaffolds in moderate to excellent yields. In addition, such a reaction can lead to the divergent synthesis of tricyclic indole derivatives with moderate yields by engineering substrate structures. The synthetic utility of this methodology has also been demonstrated by further interesting transformations. [ABSTRACT FROM AUTHOR]

An interesting β‐isoquinidine catalyzed divergent reaction was developed to produce either spirocyclopentene oxindoles, spirocyclopentadiene oxindoles or bisoxindoles in a high enantioselective fashion. The utility of this protocol was demonstrated by the versatile transformations of the products. This work not only represents the first highly stereoselective intermolecular catalytic asymmetric allylic alkylation reaction between two isatin‐derived MBH carbonate molecules but also constitutes a rare example of isatin‐derived MBH carbonate‐based enantioselective and α‐regioselective [3+2] cycloaddition reactions. [ABSTRACT FROM AUTHOR]

The development of catalytic enantioselective isocyanide‐based reactions is currently of great interest because the resulting products are valuable in organic synthesis, pharmacological chemistry, and materials science. This review assembles and comprehensively summarizes the recent achievements in this rapidly growing area according to the reaction types. Special attention is paid to the advantages, limitations, possible mechanisms, and synthetic applications of each reaction. In addition, a personal outlook on the opportunities for further exploration is given at the end. [ABSTRACT FROM AUTHOR]

We have developed a palladium‐catalyzed cross‐coupling reaction of isocyanides with α‐diazoacetates to form active ketenimines and following a 1,4‐diazabicyclo[2.2.2]octane (DABCO) catalyzed aza‐Mannich type reaction with various 2‐mercaptoimidazoles for the synthesis of 1,3‐bis(β‐aminoacrylate)‐substituted 2‐mercaptoimidazole derivatives with structural diversity. In addition, the use of 1H‐benzo[d]imidazol‐2‐ol as the reaction partner also allowed the formation of 1,3‐bis(β‐aminoacrylate)‐substituted 2‐benzimidazolinone derivatives with moderate yields (34–52%). In the aza‐Mannich reaction, the regioselective N‐attack rather than S‐attack or O‐attack at the electrophilic central carbon of ketenimines was observed. This tandem sequence is efficient since two C=C and two C−N bonds are consecutively created in one‐pot. [ABSTRACT FROM AUTHOR]

Tandem reactions of Pd‐catalyzed cross‐coupling of 3‐(2‐isocyanoethyl)indoles with diazoacetates and subsequent spirocyclization/Mannich‐type reaction have been developed to assemble polycyclic spiroindoline skeletons. Formation of spiroindolenines has been proven as the crucial step for the following Mannich‐type cyclization reaction. Accordingly, a novel approach on chiral phosphoric acid catalyzed Mannich‐type cyclization toward the formation of diastereomerically and enantiomerically enriched pentacyclic spiroindolines has been established. Moreover, the products of the reaction are versatile building blocks in synthetic chemistry, as demonstrated by the synthesis of the key framework of aspidosperma and kopsia alkaloids. [ABSTRACT FROM AUTHOR]

Objective To investigate the accuracy of the cytological Ki-67 index in distinguishing intermediate and high-grade (G2 + G3) from low-grade (G1) pancreatic neuroendocrine tumors (PNETs). Methods Two investigators independently searched databases to identify eligible studies using the following term: ('Ki-67') AND ('pancreatic endocrine tumor' OR 'pancreatic neuroendocrine tumor' OR 'pancreatic endocrine tumour' OR 'pancreatic neuroendocrine tumour' OR 'pancreatic endocrine tumors' OR 'pancreatic neuroendocrine tumors' OR 'pancreatic endocrine tumours' OR 'pancreatic neuroendocrine tumours'), and meta-analysis was performed to calculate the pooled sensitivity, specificity, positive (PLR) and negative likelihood ratio (NLR), and diagnostic odds ratio (DOR). Results A total of 263 lesions from 13 studies were included in the study. The pooled sensitivity and specificity of Ki-67 (cut-off value: 2%) in the differential diagnosis of G2 + G3 from G1 PNETs were 64% and 87%, respectively. The pooled PLR, NLR and DOR were 3.96, 0.42 and 11.21, respectively. The area under the summary receiver operating characteristic curve (AUROC) was 0.8397. While the cut-off value of Ki-67 index was set as 5%, the sensitivity and specificity were increased up to 69% and 93%, respectively, and the AUROC was increased to 0.955. Conclusion The cytological Ki-67 index is very useful in distinguishing intermediate and high-grade from low-grade PNETs, and a cut-off value of 5% had a better predictive value compared with that of 2%. [ABSTRACT FROM AUTHOR]

Cytomegalovirus, regarded as a trigger of several autoimmune diseases, is an opportunistic pathogen. Patients with ulcerative colitis ( UC) undergoing steroid treatment are susceptible to this infection. In the presence of cytomegalovirus, inflammation becomes more complex. Patients with active UC who are infected with cytomegalovirus are usually non-responders to steroid, while antiviral drugs could induce remission. Cytomegalovirus should be suggested as a probable cause of steroid-refractory UC based on the clinical data in the literatures. [ABSTRACT FROM AUTHOR]

Keywords: [3+2] cycloaddition; cascade reactions; catalytic asymmetric; insertion reaction; isocyanide EN [3+2] cycloaddition cascade reactions catalytic asymmetric insertion reaction isocyanide 1 1 1 04/19/21 20210416 NES 210416 B The development of catalytic b enantioselective isocyanide-based reactions leading to products, which are valuable in organic synthesis, pharmacological chemistry, and materials science is currently of great interest. [3+2] cycloaddition, cascade reactions, catalytic asymmetric, insertion reaction, isocyanide Recent achievements in this rapidly growing area according to the reaction types, with special attention being paid to the advantages, limitations, possible mechanisms, and synthetic applications of each reaction is given in the Review by Y.-L. [Extracted from the article]

While indoles are regioselectively mono-methylated at C-3, pyrroles give mixtures of mono-, di-, and (in the case of unsubstituted pyrrole) polymethylated products. [ABSTRACT FROM AUTHOR]

The presented approach allows direct usage of allylic alcohols as starting material without prior activation. [ABSTRACT FROM AUTHOR]

A diagram is presented which shows the quinolines synthesis from allylic alcohols through tandem isomerization/cyclization of catalyzed iridium combined with potassium hydroxide.

Depending on the base, a wide range of α,β-unsaturated ketones are reduced to saturated ketones or alcohols by using a simple homogeneous catalytic system based on the commercially available Iridium catalyst under optimized reaction conditions. [ABSTRACT FROM AUTHOR]