Rreb1 is a key transcription factor in Sertoli cell maturation and function and spermatogenesis in mouse.

Spermatogenesis is a developmental process driven by interactions between germ cells and Sertoli cells. This process depends on appropriate gene expression, which might be regulated by transcription factors. This study focused on Rreb1, a zinc finger transcription factor, and explored its function and molecular mechanisms in spermatogenesis in a mouse model. Our results showed that RREB1 was predominantly expressed in the Sertoli cells of the testis. The decreased expression of RREB1 following injection of siRNA caused impaired Sertoli cell development, which was characterized using a defective blood-testis barrier structure and decreased expression of Sertoli cell functional maturity markers; its essential trigger might be SMAD3 destabilization. The decreased expression of RREB1 in mature Sertoli cells influenced the cell structure and function, which resulted in abnormal spermatogenesis, manifested as oligoasthenoteratozoospermia, and we believe RREB1 plays this role by regulating the transcription of Fshr and Wt1. RREB1 has been reported to activate Fshr transcription, and we demonstrated that the knockdown of Rreb1 caused a reduction in follicle-stimulating hormone receptor (FSHR) in the testis, which could be the cause of the increased sperm malformation. Furthermore, we confirmed that RREB1 directly activates Wt1 promoter activity, and RREB1 downregulation induced the decreased expression of Wt1 and its downstream polarity-associated genes Par6b and E-cadherin, which caused increased germ-cell death and reduced sperm number and motility. In conclusion, RREB1 is a key transcription factor essential for Sertoli cell development and function and is required for normal spermatogenesis.

Dopants Induce Persistent Room Temperature Phosphorescence in Triarylamine Boronate Esters.

Purely organic materials exhibiting room temperature phosphorescence (RTP) are promising candidates for oxygen sensors and information encryption owing to their cost-effective and environmentally friendly nature. Herein, we report a bimolecular RTP system where DTBU acts as the guest and TBBU serves as the host. In contrast to previously reported results, we find that both pure DTBU and TBBU do not exhibit RTP in the solid state even under N2 atmosphere. A DTBU/TBBU system with a low doping ratio (0.1 mol %) exhibits persistent yellowish-green afterglow with a lifetime of 340 ms and is highly sensitive to oxygen. A DTBU/TBBU system with a higher doping ratio (10 mol %) maintains a phosphorescence lifetime of 179 ms under air. Applications of DTBU/TBBU at varied doping ratios in both oxygen sensing and information encryption are demonstrated. We propose that the T1 state of TBBU acts as an energy transfer intermediate between Tn and T1 of DTBU, ultimately leading to the generation of persistent RTP. Overall, this work demonstrates the critical importance of material purity in the design of RTP systems, and how an understanding of host-guest doping enables their photophysical properties to be precisely tuned.

The Radical Anion and Dianion of Benzo[3,4]cyclobuta[1,2-b]phenazine.

We present the reduction of two azaacenes (a benzo-[3,4]cyclobuta[1,2-b]phenazine and a benzo[3,4]cyclobuta[1,2-b]naphtho[2,3-i]phenazine derivative), featuring a single cyclobutadiene unit, to their radical anions and dianions. The reduced species were produced using potassium naphthalenide in the presence of 18-crown-6 in THF. Crystal structures of the reduced representatives were obtained and their optoelectronic properties evaluated. Charging these 4n Hückel systems gives dianionic 4n + 2 π-electron systems with increased antiaromaticity, according to NICS(1.7)zz calculations, featuring unusually red-shifted absorption spectra.

Achieving White-Light Emission Using Organic Persistent Room Temperature Phosphorescence.

Artificial lighting currently consumes approximately one-fifth of global electricity production. Organic emitters with white persistent RTP have potential for applications in energy-efficient lighting technologies, due to their ability to harvest both singlet and triplet excitons. Compared to heavy metal phosphorescent materials, they have significant advantages in cost, processability, and reduced toxicity. Phosphorescence efficiency can be improved by introducing heteroatoms, heavy atoms, or by incorporating luminophores within a rigid matrix. White-light emission can be achieved by tuning the ratio of fluorescence to phosphorescence intensity or by pure phosphorescence with a broad emission spectrum. This review summarizes recent advances in the design of purely organic RTP materials with white-light emission, describing single-component and host-guest systems. White phosphorescent carbon dots and representative applications of white-light RTP materials are also introduced.

Photocatalyzed Borylcyclopropanation of Alkenes with a (Diborylmethyl)iodide Reagent.

Cyclopropane skeletons play a prominent role in the development of organic synthesis and pharmaceutical chemistry. Herein, we report the design and synthesis of a stable, multifunctional (diborylmethyl)iodide reagent (CHI(Bpin)2 ) for the photoinduced cyclopropanation of alkenes, providing an array of 1,2-substituted cyclopropylboronates in good yields. This α-haloboronic ester can be readily synthesized on a multigram scale from commercially available starting materials. Furthermore, the protocol displays high chemo- and diastereoselectivity, excellent functional-group tolerance, and allows for late-stage borylcyclopropanation of complex molecules. Mechanistic studies reveal that the borylcyclopropanation proceeds through a radical addition/polar cyclization pathway mediated by the photocatalyst fac-Ir(ppy)3 and visible light.

Aggregation-Induced Dual Phosphorescence from (o-Bromophenyl)-Bis(2,6-Dimethylphenyl)Borane at Room Temperature.

Designing highly efficient purely organic phosphors at room temperature remains a challenge because of fast non-radiative processes and slow intersystem crossing (ISC) rates. The majority of them emit only single component phosphorescence. Herein, we have prepared 3 isomers (o, m, p-bromophenyl)-bis(2,6-dimethylphenyl)boranes. Among the 3 isomers (o-, m- and p-BrTAB) synthesized, the ortho-one is the only one which shows dual phosphorescence, with a short lifetime of 0.8 ms and a long lifetime of 234 ms in the crystalline state at room temperature. Based on theoretical calculations and crystal structure analysis of o-BrTAB, the short lifetime component is ascribed to the T1 M state of the monomer which emits the higher energy phosphorescence. The long-lived, lower energy phosphorescence emission is attributed to the T1 A state of an aggregate, with multiple intermolecular interactions existing in crystalline o-BrTAB inhibiting nonradiative decay and stabilizing the triplet states efficiently.

The Radical Anion, Dianion and Electron Transport Properties of Tetraiodotetraazapentacene.

Tetraiodotetraazapentacene I4 TAP, the last missing derivative in the series of halogenated silylated tetraazapentacenes, was synthesized via condensation chemistry from a TIPS-ethynylated diaminobenzothiadiazol in three steps. Single and double reduction furnished its air-stable monoanion and relatively air-stable dianion, both of which were characterized by crystallography. All three species are structurally and spectroscopically compared to non-halogenated TAP and Br4 TAP. I4 TAP is an n-channel material in thin-film transistors with average electron mobilities exceeding 1 cm2 (Vs)-1 .

Tubulin alpha 1c promotes aerobic glycolysis and cell growth through upregulation of yes association protein expression in breast cancer.

Tubulin alpha 1c (TUBA1C) as a member of α-tubulin was identified to take part in the occurrence and development of hepatocellular carcinoma and pancreatic cancer. Using the bioinformatics, we noticed that TUBA1C level was also increased in breast cancer was also demonstrated. Here, we explored TUBA1 role in modulation of breast cancer cell aerobic glycolysis, growth and migration and explored whether yes association protein (YAP) was involved. Fifty-five matched breast cancer tissues and the para-carcinoma normal tissues were included in this study and used to verify TUBA1C expression using quantitative reverse transcription-PCR and western blotting. ATP level, lactate secretion and glucose consumption were used to assess aerobic glycolysis. Cell growth, invasion, migration and tumorigenesis were detected using cell count kit-8, transwell, wound healing and animal assays. TUBA1 was upregulated in breast cancer, which associated with advanced primary tumor, lymph node, metastasis stage and tumor size. Silencing of TUBA1C with sh-TUBA1C infection led to significant inhibitions in ATP level, lactate secretion, glucose consumption, cell growth, migration, invasion and tumorigenesis, as well as declined YAP expression, while TUBA1C overexpression induced a opposite result. And, the above tendencies induced by TUBA1C downregulation were reversed by YAP overexpression. This study revealed that TUBA1C was overexpressed in breast cancer and promoted aerobic glycolysis and cell growth through upregulation of YAP expression.

The older, the less potential benefit for type 2 diabetes from weight control.

BACKGROUND: Although moderate weight loss improves outcomes of type 2 diabetes mellitus (T2DM) in young and middle-aged adults, there is a lack of high-quality evidence to support the strong relationship between obesity and T2DM in older people. This study aims to investigate whether the association of obesity with T2DM changes with aging. METHODS: In this cross-sectional study, we recruited 63,180 Chinses and US subjects from 3 datasets. Subjects were divided into young & middle-aged (≤59 years), young-old (60-75 years), and old-old (≥75 years). Logistic regression was used to determine the odds ratio (OR) and 95% confidence intervals (95% CI) for the association between obesity and T2DM, stratified by common confounders. A sliding-window based algorithm and restricted cubic splines were used to smoothly estimate the changes with aging. RESULTS: The OR (95% CI) for the associations between general obesity and T2DM were decreased from the young & middle-aged group (OR, 5.91; 95% CI, 5.33-6.56) to the young-old group (OR, 3.98; 95% CI, 3.56-4.45) and then to the old-old group (OR, 3.06; 95% CI, 2.57-3.66). The trend for this reduced association with aging persisted after stratification by obesity type, region, gender, recruiting time, hypertension, and hyperlipidemia in both Chinese and Americans. We also identified a weakened gender disparity for this association between the young & middle-aged subjects (P for disparity < 0.001) and the old-old group (P for disparity = ~ 0.36). CONCLUSIONS: The obesity-T2DM association is clearly reduced with aging, which indicates that the elderly may gain fewer potential benefits in weight lose than the younger patients. Considering this attenuated association, as well as the increased incidence of geriatric syndrome in the elderly, clinicians should comprehensively balance the benefits and side effects of weight loss in geriatric T2DM interventions.

Analysis of the therapeutic effect of artificial leather embedding combined with fascial sleeve flap transplantation on chronic wounds of lower limbs with bone and plate exposure.

BACKGROUND: After severe trauma of lower limbs, bone, tendon or plate graft exposure is common. The traditional repair method is to use a variety of skin flap transplantation to cover the exposed part, but the wound often can not heal after operation, or the wound is cracked, ulcer, sinus, bone and steel plate are exposed again after wound healing. The reason for this result is that when the flap is covered, the space around the bone plate is not well closed, forming a dead cavity, blood and exudate accumulation, hematoma formation or infection, and finally the wound ruptures again. In addition, due to the swelling and contracture of the flap after operation, the suture tension between the flap and the receiving area becomes larger, the skin becomes thinner and broken, and then the wound is formed. In order to solve the above problems, we carried out the study of artificial true skin embedding combined with fascial sleeve flap transplantation in the treatment of chronic bone plate exposed wounds of lower limbs. METHODS: In this paper, 11 cases of chronic wounds with bone exposure and skin necrosis after steel plate implantation were selected. First stage is the wound bed preparation including primary wound expansion, removal of necrotic tissue and incision of sinus wall, removal of deep necrotic bone and fibrotic scarred skin on the outer wall of steel plate to normal tissue on the outer edge of the wound, removal of precipitated peptone and purulent fur in the hole, periphery and bone space of the steel plate, and removal of tendon tissue with basal necrosis and disintegration of the wound. After vacuum sealing drainage (VSD) 1-2 weeks, the peritraumatic basal granulation tissue grew well and there was no necrotic tissue in the wound. In the second stage, the exposed bone was covered with artificial dermis, the steel plate hole or the periphery and the basal space were filled, and the exposed steel plate was completely embedded, and then the fascia sleeve flap was transplanted to cover the wound. The sural neurovascular flap was performed in nine cases and the lateral superior malleolar artery perforator flap in two case. RESULTS: The flap survived well in all 11 cases. During the follow-up of 6 months to the removal of the plate, there was no case of rupture, exposure and sinus formation. CONCLUSIONS: Artificial dermal covering combined with fascial sleeve flap transplantation can effectively avoid wound dehiscence or sinus formation caused by foreign body retention, infection and flap contracture. It has good effect in repairing chronic wounds with bone plate exposure after severe trauma of lower limbs.

Pure Boric Acid Does Not Show Room-Temperature Phosphorescence (RTP).

Boric acid (BA) has been used as a transparent glass matrix for optical materials for over 100 years. However, recently, apparent room-temperature phosphorescence (RTP) from BA (crystalline and powder states) was reported (Zheng et al., Angew. Chem. Int. Ed. 2021, 60, 9500) when irradiated at 280 nm under ambient conditions. We suspected that RTP from their BA sample was induced by an unidentified impurity. Our experimental results show that pure BA synthesized from B(OMe)3 does not luminesce in the solid state when irradiated at 250-400 nm, while commercial BA indeed (faintly) luminesces. Our theoretical calculations show that neither individual BA molecules nor aggregates would absorb light at >175 nm, and we observe no absorption of solid pure BA experimentally at >200 nm. Therefore, it is not possible for pure BA to be excited at >250 nm even in the solid state. Thus, pure BA does not display RTP, whereas trace impurities can induce RTP.

Clinical features and molecular epidemiology of carbapenem-resistant Enterobacterales infection in children. / å„¿ç«¥ç¢³é’éœ‰çƒ¯ç±»è€è¯è‚ æ†èŒç›®ç»†èŒæ„ŸæŸ“çš„ä¸´åºŠç‰¹å¾åŠåˆ†å­æµè¡Œç ”ç©¶.

OBJECTIVES: To study the clinical features of children with carbapenem-resistant Enterobacterales (CRE) infection and the molecular characteristics of isolated strains. METHODS: A retrospective analysis was performed on the clinical data and infection status of the children who were hospitalized in Guangdong Provincial People's Hospital from January 2018 to June 2021. A total of 1 098 non-repetitive strains of Enterobacterales were obtained. Drug sensitivity test, PCR amplification, and resistance-related gene sequencing were performed for 66 isolated CRE strains to observe molecular epidemiology. RESULTS: Among the 1 098 strains of Enterobacterales, the detection rate of CRE was 6.01% (66/1 098). The 66 CRE strains were isolated from 66 children, among whom there were 37 boys (56%) and 29 girls (44%), with an age of 2 days to 14 years. Among these 66 children, 16 (24%) had an age of <1 month, 28 (42%) had an age of 1-12 months, 11 (17%) had an age of 12-36 months, and 11 (17%) had an age of >36 months. The children with CRE were mainly distributed in the department of neonatology (38 children, 58%) and the pediatric intensive care unit (17 children, 26%). The top three types of specimens with CRE detection were respiratory specimens (48%), midstream urine specimens (21%), and blood specimens (17%). The CRE strains were mainly Klebsiella pneumoniae (45 strains, 68%), Escherichia coli (12 strains, 18%), and Enterobacter cloacae (6 strains, 9%), with high resistance to carbapenems (such as imipenem and ertapenem), penicillin, and cephalosporins, slightly high resistance to commonly used antibiotics, and relatively low resistance to amikacin (14%), levofloxacin (23%), and tobramycin (33%). The carbapenemase genotypes of Klebsiella pneumoniae strains were mainly blaNDM (20 strains, 44%), blaIMP (10 strains, 22%), and blaKPC (5 strains, 11%), and the carbapenemase genotypes of Escherichia coli strains were mainly blaNDM (10 strains, 83%). After sequencing, there were 24 blaNDM-1 strains, 6 blaNDM-5 strains, 5 blaIMP-4 strains, and 3 blaKPC-2 strains, and some genotypes were not identified. CONCLUSIONS: There is a high incidence rate of CRE infection among children, mainly those aged 1-12 months. CRE generally has high resistance to antibacterial drugs, and metalloenzymes are the main type of carbapenemases for CRE strains in children.

Ni-Catalyzed Borylation of Aryl Sulfoxides.

A nickel/N-heterocyclic carbene (NHC) catalytic system has been developed for the borylation of aryl sulfoxides with B2 (neop)2 (neop=neopentyl glycolato). A wide range of aryl sulfoxides with different electronic and steric properties were converted into the corresponding arylboronic esters in good yields. The regioselective borylation of unsymmetric diaryl sulfoxides was also feasible leading to borylation of the sterically less encumbered aryl substituent. Competition experiments demonstrated that an electron-deficient aryl moiety reacts preferentially. The origin of the selectivity in the Ni-catalyzed borylation of electronically biased unsymmetrical diaryl sulfoxide lies in the oxidative addition step of the catalytic cycle, as oxidative addition of methoxyphenyl 4-(trifluoromethyl)phenyl sulfoxide to the Ni(0) complex occurs selectively to give the structurally characterized complex trans-[Ni(ICy)2 (4-CF3 -C6 H4 ){(SO)-4-MeO-C6 H4 }] 4. For complex 5, the isomer trans-[Ni(ICy)2 (C6 H5 )(OSC6 H5 )] 5-I was structurally characterized in which the phenyl sulfinyl ligand is bound via the oxygen atom to nickel. In solution, the complex trans-[Ni(ICy)2 (C6 H5 )(OSC6 H5 )] 5-I is in equilibrium with the S-bonded isomer trans-[Ni(ICy)2 (C6 H5 )(SOC6 H5 )] 5, as shown by NMR spectroscopy. DFT calculations reveal that these isomers are separated by a mere 0.3 kJ/mol (M06/def2-TZVP-level of theory) and connected via a transition state trans-[Ni(ICy)2 (C6 H5 )(η2 -{SO}-C6 H5 )], which lies only 10.8 kcal/mol above 5.

Continuous Renal-Replacement Therapy in Critically Ill Children: Practice Changes and Association With Outcome.

OBJECTIVES: This study was designed to evaluate practice changes and outcomes over a 10-year period in a large single-center PICU cohort that received continuous renal-replacement therapy. DESIGN: Retrospective study design. SETTING: A multidisciplinary tertiary PICU of a university-affiliated hospital in Guangzhou, China. PATIENTS: All critically ill children who were admitted to our PICU from January 2010 to December 2019 and received continuous renal-replacement therapy were included in this study. MEASUREMENTS AND MAIN RESULTS: A total of 289 patients were included in the study. Of the two study periods, 2010-2014 and 2015-2019, the proportion of continuous renal-replacement therapy initiation time greater than 24 hours was significantly reduced ([73/223] 32.73% vs. [40/66] 60.60%, p < 0.001), the percentage of fluid overload at continuous renal-replacement therapy initiation was lower (3.8% [1.6-7.2%] vs. 12.1% [6.6-23.3%], p < 0.001), the percentage of regional citrate anticoagulation protocol was increased ([223/223] 100% vs. [15/66] 22.7%, p < 0.001), and the ICU survival rate was significantly improved ([24/66] 36.4% vs. [131/223] 58.7%, p = 0.001) in the latter period compared with the former. In addition, subgroup analysis found that survival were higher in patients with continuous renal-replacement therapy initiation time less than 24 hours, regional citrate anticoagulation protocol, and fluid overload less than 10%. CONCLUSIONS: The survival rate of patients received continuous renal-replacement therapy treatment in our center has improved over past 10 years, and some changes have taken place during these periods. Among them, early initiation of continuous renal-replacement therapy, lower fluid overload, and regional citrate anticoagulation method seems to be related to the improvement of outcome. Ongoing evaluation of the practice changes and quality improvement of continuous renal-replacement therapy for critically ill pediatric patients still need attention.

Copper exposure association with prevalence of non-alcoholic fatty liver disease and insulin resistance among US adults (NHANES 2011-2014).

BACKGROUND: Excessive copper (Cu) has risky effect on insulin resistance (IR), oxidative stress and inflammation. Instead, some studies reported serum Cu to be protective for non-alcoholic fatty liver disease (NAFLD). The aim of this study was to reevaluate the evidence for a potential risky correlation of serum Cu to NAFLD in large-scale and non-institutionalized American subjects. METHODS: A cross-sectional study of 3211 subjects was from the National Health and Nutrition Examination Survey (NHANES). Logistic regression and cubic spline-based curve-fitting analyses were used to estimate the independent risky effect of Cu to hepatic steatosis index (HSI), US fatty liver index (USFLI) and NAFLD and their dose-effect relationship. Moreover, this association was analyzed in stratification of HOMA-IR, Metabolic syndrome (MetS) and severity of NAFLD, besides age and gender. RESULTS: The average level of serum Cu was 18.67 µmol/L and the prevalence of NAFLD was 54.53% and 32.60%, respectively defined by HSI and USFLI. Generally, the level of Cu was higher in females than males. Serum Cu was positively associated with higher HSI, USFLI index and risk of NAFLD. In fully adjusted models, compared with the lowest quartile, the risk of NAFLD increased 97% in the highest quartile of Cu. Interestingly, stratified analysis showed that the risky effect of Cu to NAFLD was more prominent in the middle-aged, females and subjects with improved status of IR (lower HOMA-IR and non-Mets) compared with their counterparts. Moreover, we further found that circulating copper was correlated to severity of NAFLD only in males. CONCLUSION: Excess serum Cu is significantly associated with risk of NAFLD, which is prominent in females, middle-aged and subjects with improved status of IR, and seems to be related to the severity of NAFLD, additionally. It is necessary to be cautious of the toxic effect of Cu and prospective cohort and mechanism studies are needed to verify the causal effect of Cu to NAFLD.

For nasotracheal intubation, which nostril results in less epistaxis: right or left?: A systematic review and meta-analysis.

BACKGROUND: Nasotracheal intubation is usually required in patients undergoing oromaxillofacial, otolaryngological or plastic surgery to prevent the airway encroaching into the operating field. Epistaxis is the most common complication, but which nostril is associated with a lower incidence and severity of epistaxis is still unclear. OBJECTIVE: When both nostrils are patent, to determine the preferred nostril for nasotracheal intubation under general anaesthesia. DESIGN: A systematic review and meta-analysis of randomised controlled trials (RCTs). The primary outcome was the incidence of epistaxis and the secondary outcomes included the incidence of severe epistaxis, the time required to pass the tube through the nasal passage and total intubation time. DATA SOURCES: PubMed, Embase and the Cochrane Register of Controlled Trials were searched from database inception to 1 March 2020. ELIGIBILITY CRITERIA: The only studies included were RCTs comparing epistaxis related to nasotracheal intubation via right or left nostril, in adult surgery patients undergoing general anaesthesia. RESULTS: Ten RCTs with 1658 patients were included. Compared with the left nostril, intubation via the right nostril was associated with a significantly lower incidence of epistaxis: risk ratio (RR) and 95% confidence intervals (CI) were 0.78 (0.62 to 0.99), P = 0.04: a lower incidence of severe epistaxis (five studies, n=923), RR 0.40 (0.22 to 0.75), P = 0.004: and a shorter intubation time (three studies, n=345), mean difference -7.28 (-14.40 to -0.16) seconds, P = 0.05. In two studies (n=310), no significant difference between the right and left nostril was observed in the time to pass the tube through the nasal passages, mean difference -0.59 (-1.95 to 0.77) s, P = 0.40. CONCLUSION: On the basis of the current available evidence, when both nostrils are patent, the right nostril is more appropriate for nasotracheal intubation, with a lower incidence and severity of epistaxis and faster intubation time. TRIAL REGISTRATION: The study protocol has been registered in PROSPERO (CRD42020169949).

Visible-Light-Induced Ni-Catalyzed Radical Borylation of Chloroarenes.

A highly selective and general photoinduced C-Cl borylation protocol that employs [Ni(IMes)2] (IMes = 1,3-dimesitylimidazoline-2-ylidene) for the radical borylation of chloroarenes is reported. This photoinduced system operates with visible light (400 nm) and achieves borylation of a wide range of chloroarenes with B2pin2 at room temperature in excellent yields and with high selectivity, thereby demonstrating its broad utility and functional group tolerance. Mechanistic investigations suggest that the borylation reactions proceed via a radical process. EPR studies demonstrate that [Ni(IMes)2] undergoes very fast chlorine atom abstraction from aryl chlorides to give [NiI(IMes)2Cl] and aryl radicals. Control experiments indicate that light promotes the reaction of [NiI(IMes)2Cl] with aryl chlorides generating additional aryl radicals and [NiII(IMes)2Cl2]. The aryl radicals react with an anionic sp2-sp3 diborane [B2pin2(OMe)]- formed from B2pin2 and KOMe to yield the corresponding borylation product and the [Bpin(OMe)]•- radical anion, which reduces [NiII(IMes)2Cl2] under irradiation to regenerate [NiI(IMes)2Cl] and [Ni(IMes)2] for the next catalytic cycle.

Ni-Catalyzed Traceless, Directed C3-Selective C-H Borylation of Indoles.

A highly efficient and general protocol for traceless, directed C3-selective C-H borylation of indoles with [Ni(IMes)2] as the catalyst is reported. Activation and borylation of N-H bonds by [Ni(IMes)2] is essential to install a Bpin moiety at the N-position as a traceless directing group, which enables the C3-selective borylation of C-H bonds. The N-Bpin group which is formed is easily converted in situ back to an N-H group by the oxidative addition product of [Ni(IMes)2] and in situ-generated HBpin. The catalytic reactions are operationally simple, allowing borylation of a variety of substituted indoles with B2pin2 in excellent yields and with high selectivity. The C-H borylation can be followed by Suzuki-Miyaura cross-coupling of the C-borylated indoles in an overall two-step, one-pot process providing an efficient method for synthesizing C3-functionalized heteroarenes.

Potential Genes Related to Levofloxacin Resistance in Mycobacterium tuberculosis Based on Transcriptome and Methylome Overlap Analysis.

Drug-resistant Mycobacterium tuberculosis (M. tuberculosis) has become an increasingly serious public health problem and has complicated tuberculosis (TB) treatment. Levofloxacin (LOF) is an ideal anti-tuberculosis drug in clinical applications. However, the detailed molecular mechanisms of LOF-resistant M. tuberculosis in TB treatment have not been revealed. Our study performed transcriptome and methylome sequencing to investigate the potential biological characteristics of LOF resistance in M. tuberculosis H37Rv. In the transcriptome analysis, 953 differentially expressed genes (DEGs) were identified; 514 and 439 DEGs were significantly downregulated and upregulated in the LOF-resistant group and control group, respectively. The KEGG pathway analysis revealed that 97 pathways were enriched in this study. In the methylome analysis, 239 differentially methylated genes (DMGs) were identified; 150 and 89 DMGs were hypomethylated and hypermethylated in the LOF-resistant group and control group, respectively. The KEGG pathway analysis revealed that 74 pathways were enriched in this study. The overlap study suggested that 25 genes were obtained. It was notable that nine genes expressed downregulated mRNA and upregulated methylated levels, including pgi, fadE4, php, cyp132, pckA, rpmB1, pfkB, acg, and ctpF, especially cyp132, pckA, and pfkB, which were vital in LOF-resistant M. tuberculosis H37Rv. The overlapping genes between transcriptome and methylome could be essential for studying the molecular mechanisms of LOF-resistant M. tuberculosis H37Rv. These results may provide informative evidence for TB treatment with LOF.

Organocatalytic Asymmetric Aldol Reaction of Arylglyoxals and Hydroxyacetone: Enantioselective Synthesis of 2,3-Dihydroxy-1,4-diones.

A highly efficient quinine-derived primary-amine-catalyzed asymmetric aldol addition of hydroxyacetone to arylglyoxals is described. Structurally diverse anti-2,3-dihydroxy-1,4-diones were generated in high yields, with good diastereoselectivities and enantioselectivities.