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1.
J Mol Cell Biol ; 2021 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-34609489

RESUMO

Skin, as the outmost layer of human body, is frequently exposed to environmental stressors including pollutants and ultraviolet (UV), which could lead to skin disorders. Generally, skin response process to ultraviolet B (UVB) irradiation is a nonlinear dynamic process, with unknown underlying molecular mechanism of critical transition. Here, the landscape dynamic network biomarker (l-DNB) analysis of time series transcriptome data on 3D skin model was conducted to reveal the complicated process of skin response to UV irradiation at both molecular and network levels. The advanced l-DNB analysis approach showed that: (i) there was a tipping point before critical transition state during pigmentation process, validated by 3D skin model; (ii) 13 core DNB genes were identified to detect the tipping point as a network biomarker, supported by computational assessment; (iii) core DNB genes such as COL7A1 and CTNNB1 can effectively predict skin lightening, validated by independent human skin data. Overall, this study provides new insights for skin response to repetitive UVB irradiation, including dynamic pathway pattern, bi-phasic response, and DNBs for skin lightening change, and enables us to further understand the skin resilience process after external stress.

2.
Eur J Med Res ; 26(1): 119, 2021 Oct 03.
Artigo em Inglês | MEDLINE | ID: mdl-34602082

RESUMO

BACKGROUND: For a patient presenting with fever, multiple lymphadenopathy and splenomegaly, pathogen infection should be preferentially considered, followed by lymphoid malignancies. When traditional laboratory and pathological detection cannot find the pathogenic microorganism, metagenomic sequencing (MGS) which targets the person's genome for exceptional genetic disorders may detect a rare pathogen. CASE PRESENTATION: Here, we introduced the diagnostic clue of a case of multicentric Castleman disease (MCD) with hemophagocytic syndrome which was elicited from the detection of human herpesvirus-8 in the blood of a HIV-1 infected person by MGS technology during pathogen inspection. This case highlights the need to increase the awareness of MCD among clinicians and pathologists. CONCLUSIONS: MGS technology may play a pivotal role in providing diagnostic clues during pathogen inspection, especially when pathogens are not detectable by conventional methods.

3.
Org Lett ; 2021 Oct 13.
Artigo em Inglês | MEDLINE | ID: mdl-34644098

RESUMO

Here, we report an unprecedented catalytic enantioselective cyanation of ketonitrones enabled by the bifunctional cyanating reagent Me2(CH2Cl)SiCN. This approach allows facile access to optically active N-hydroxyl-α-amino nitriles that are of high synthetic value but difficult to acquire by other methods. The use of bifunctional cyanating reagent Me2(CH2Cl)SiCN not only achieves an enantioselectivity higher than that with TMSCN but also enables various diversification reactions of the resulting silylated adducts. This represents the first enantioselective catalytic nucleophilic addition reaction of unactivated ketone-derived nitrones, exhibiting the potential of such tetrasubstituted C═N bonds for asymmetric synthesis of N-hydroxy α-amino acids and other N-hydroxy tertiary amines.

4.
Plant Physiol Biochem ; 167: 980-989, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34583133

RESUMO

Calcineurin B-like protein (CBL) and CBL-interacting protein kinase (CIPK) play important roles in plant environmental stress responses. However, the biological functions of the CBL-CIPK signaling pathway in the tolerance of soybean (Glycine max) to drought stress remain elusive. Here, we characterized the GmCIPK2 gene in soybean, and its expression was induced by drought stress and exogenous abscisic acid (ABA) treatments. The overexpression of GmCIPK2 enhanced drought tolerance in transgenic Arabidopsis and soybean hairy roots, whereas downregulation of GmCIPK2 expression in soybean hairy roots by RNA interference resulted in increased drought sensitivity. Further analysis showed that GmCIPK2 was involved in ABA-mediated stomatal closure in plants under drought stress conditions. GmCIPK2 increased the expression of ABA- and drought-responsive genes during drought stress. Additionally, yeast two-hybrid, pull-down, and bimolecular fluorescence complementation assays demonstrated that a positive regulator of drought stress, GmCBL1, physically interacted with GmCIPK2 on the plasma membrane. Collectively, our results demonstrated that GmCIPK2 positively regulates drought tolerance and ABA signaling in plants, providing new insights into the underlying mechanisms of how the CBL-CIPK signaling pathway contributes to drought tolerance in soybean.


Assuntos
Secas , Proteínas Quinases , Proteínas de Soja , Soja , Ácido Abscísico , Regulação da Expressão Gênica de Plantas , Plantas Geneticamente Modificadas/metabolismo , Proteínas Quinases/genética , Proteínas Quinases/metabolismo , Proteínas de Soja/genética , Proteínas de Soja/metabolismo , Soja/genética , Soja/metabolismo , Estresse Fisiológico
5.
Curr Microbiol ; 78(11): 3877-3890, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34510225

RESUMO

Huagaimu (Manglietiastrum sinicum) trees are critically endangered species and classified as a plant species with extremely small populations in China. Rhizospheres and bulk soils prokaryotic communities play an important role to protect and promote plants health and growth. However, the compositions and structures of prokaryotic communities in wild and reintroduced M. sinicum rhizospheres and bulk soils are still poorly understood. In the present study, prokaryotic communities in wild and reintroduced M. sinicum rhizospheres and bulk soils were compared using high-throughput sequencing. Thirty-two phyla, 76 classes, 193 orders, 296 families, and 470 genera of prokaryotes were obtained. Proteobacteria and Acidobacteria were the two most abundant phyla in all soil samples. The compositions and structures of prokaryotic communities were overall similar, and the abundance of some taxa varied significantly among soil samples. Soil prokaryotic communities were significantly affected by soil pH, total nitrogen, total phosphorus, and total potassium. Eleven of predicted functions were significantly different among the four soil groups. This study provides for the first insights into the compositions, structures, and potential functions of prokaryotic communities associated with wild and reintroduced M. sinicum rhizospheres and bulk soils, and providing a foundation for future research to help protect this endangered species.


Assuntos
Espécies em Perigo de Extinção , Rizosfera , Acidobacteria , Animais , Humanos , Células Procarióticas , Solo
6.
J Food Sci ; 86(10): 4288-4302, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34533219

RESUMO

To understand the relationship between flavor and energy, the flavor, energy, and enzyme activity related to energy metabolism in shiitake mushrooms harvested at different developmental stages were investigated. The results indicated that the adenosine triphosphate level increased significantly in developing mushrooms and was strongly correlated with the fresh weight. The levels of equivalent umami concentration (EUC), total aroma compounds, energy charge, adenosine triphosphatase, cytochrome c oxidase, and succinic dehydrogenase varied with maturity. In addition, a strong correlation was observed between aroma compounds, EUC, and energy status (p < 0.05). Our results suggest that the unique flavor of developing shiitake mushroom is closely related to energy. The findings may provide a new strategy to improve the flavor of mushrooms by regulating their energy levels. PRACTICAL APPLICATION: The unique flavor of shiitake mushroom, which has a significant impact on consumer preferences, is one of its key characteristics. This research paper provides a theoretical foundation for determining the optimal harvest period for shiitake mushrooms with high quality and a new strategy to improve the flavor of mushrooms by regulating their energy levels.


Assuntos
Agricultura , Cogumelos Shiitake , Agricultura/métodos , Comportamento do Consumidor , Cogumelos Shiitake/química , Cogumelos Shiitake/crescimento & desenvolvimento , Cogumelos Shiitake/metabolismo , Paladar
7.
Signal Transduct Target Ther ; 6(1): 342, 2021 09 16.
Artigo em Inglês | MEDLINE | ID: mdl-34531370

RESUMO

While some individuals infected by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) present mild-to-severe disease, many SARS-CoV-2-infected individuals are asymptomatic. We sought to identify the distinction of immune response between asymptomatic and moderate patients. We performed single-cell transcriptome and T-cell/B-cell receptor (TCR/BCR) sequencing in 37 longitudinal collected peripheral blood mononuclear cell samples from asymptomatic, moderate, and severe patients with healthy controls. Asymptomatic patients displayed increased CD56briCD16- natural killer (NK) cells and upregulation of interferon-gamma in effector CD4+ and CD8+ T cells and NK cells. They showed more robust TCR clonal expansion, especially in effector CD4+ T cells, but lack strong BCR clonal expansion compared to moderate patients. Moreover, asymptomatic patients have lower interferon-stimulated genes (ISGs) expression in general but large interpatient variability, whereas moderate patients showed various magnitude and temporal dynamics of the ISGs expression across multiple cell populations but lower than a patient with severe disease. Our data provide evidence of different immune signatures to SARS-CoV-2 in asymptomatic infections.


Assuntos
COVID-19 , Portador Sadio/imunologia , Linfócitos/imunologia , SARS-CoV-2/imunologia , Análise de Célula Única , Transcriptoma/imunologia , Adolescente , Adulto , COVID-19/genética , COVID-19/imunologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Receptores de Antígenos de Linfócitos B/genética , Receptores de Antígenos de Linfócitos B/imunologia , Receptores de Antígenos de Linfócitos T/genética , Receptores de Antígenos de Linfócitos T/imunologia , SARS-CoV-2/genética
8.
Cancer Cell Int ; 21(1): 501, 2021 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-34535128

RESUMO

BACKGROUND: Recent reports suggest that the long non-coding RNA LBX2 antisense RNA 1 (LBX2-AS1) acts as an important regulator in cancer progression, but its significance in colorectal cancer (CRC) remains undetermined. METHODS: LBX2-AS1 expression levels in CRC were determined from the GEPIA database and CRC tissues to investigate clinical relevance. meRIP-PCR assays investigated the molecular mechanisms underlying the function of m6A in LBX2-AS1. Loss of function experiments was used to define the role of LBX2-AS1 in the progression of CRC. The ceRNA function of LBX2-AS1 was evaluated by RNA immunoprecipitation. In vitro and PDX models were used to determine if LBX2-AS1 promotes 5-fluorouracil resistance. RESULTS: Data from the TCGA and our institutional patient cohorts established that LBX2-AS1 levels were significantly upregulated in most CRC tissues relative to normal adjacent colon tissues. Moreover, LBX2-AS1 levels were positively correlated with aggressive disease characteristics, constituting an independent prognostic indicator of overall patient survival. Mechanistic investigations suggested that the increased LBX2-AS1 in CRC was mediated by METTL3-dependent m6A methylation. In vitro experiments indicated that knockdown of LBX2-AS1 inhibited CRC proliferation, migration and invasion with this phenotype linked to LBX2-AS1-mediated regulation of AKT1, acting as a ceRNA to sponge miR-422a. Ex vivo analysis of patient-derived CRC xenografts showed that low LBX2-AS1 expression cases exhibited 5-FU responsiveness and clinical investigations confirmed that low LBX2-AS1 expression was associated with improved clinical benefits from 5-FU therapy. CONCLUSIONS: Together these results suggest that LBX2-AS1 may serve as a therapeutic target and predictor of 5-FU benefit in CRC patients.

9.
J Cancer ; 12(19): 5760-5771, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34475990

RESUMO

S100 calcium binding protein A1 (S100A1) is an important member of the S100 family and known to express in a variety of cancers. However, the biological functions of S100A1 in thyroid carcinoma have not been thoroughly studied. In this report, bioinformatics analyses and immunohistochemistry assays were applied to assess the expression profile of S100A1 as well as its relationship with the pathological features and prognosis of papillary thyroid carcinoma (PTC). Meanwhile, functions of S100A1 in PTC cells were analyzed with either in vitro or in vivo experiments. S100A1 was significantly up-regulated in PTC tissues compared with adjacent non-cancerous tissues. S100A1 protein expression was significantly associated with tumor size (p=0.0032) or lymph node metastasis (p=0.0331). More importantly, an elevated S100A1 expression was significantly correlated with a worse recurrence-free survival (RFS) (HR=2.26, p=0.042). Further, knockdown of S100A1 dramatically inhibited cell proliferation and migration as well as increased apoptosis of PTC cells. S100A1 knockdown inhibited tumor progression as seen in in vivo experiments. In terms of mechanism, down-regulation of S100A1 induced yes associated protein (YAP) phosphorylation in the cytoplasm and diminished Hippo/YAP pathway activation. Therefore, S100A1 may serve as a novel oncogene and a promising biomarker for PTC diagnosis and prognosis.

10.
Phytochemistry ; 192: 112929, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34481176

RESUMO

From the aerial extracts of Coptosapelta diffusa (Champ. ex Benth.) Steenis, twenty-one compounds were isolated and identified by means of column chromatography and NMR and MS techniques, respectively. Amongst, ten ones were determined to be undescribed compounds including six seco-iridoid glucosides (1-6), 2-(hydroxymethyl)-1,2,3,4-tetrahydroanthracene-9,10-dione (7) and three guaiane-type sesquiterpenes (15-17). Compounds 7, 8 and 9 exhibited inhibitory activities against Staphylococcus aureus ATCC25923 with MIC of 8, 4 and 8 µg/mL. The use of 1-6 (iridoids), 7-14 (anthraquinones) and 15-17 (sesquiterpenes) as chemotaxonomic markers for this species was evidenced. Structurally, 7-14 are similar to those anthraquinones isolated from other species of the family Rubiaceae, confirming their close phylogenetic relationship. Whereas, these iridoids and sesquiterpenes with unique structures provided chemotaxonomic evidence to support the genus Coptosapelta (the tribe Coptosapelteae) as a sister of the subfamily Rubioideae. These results contrast with the general producing tendency of indole alkaloids by the species of the subfamily Cinchonoideae, and merit chemotaxonomic significance for the delimitation of Coptosapelta.

11.
Oral Dis ; 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-34337826

RESUMO

OBJECTIVE: This study was conducted to investigate key long noncoding RNAs (lncRNAs) involved in competitive endogenous RNA (ceRNA) network associated with laryngeal squamous cell carcinoma (LSCC). MATERIALS AND METHODS: Three mRNA datasets, two miRNA datasets, and one lncRNA dataset of LSCC were downloaded from GEO database. Following the identification of differentially expressed mRNAs (DEmRNAs), (microRNAs) miRNAs (DEmiRNAs), and lncRNAs (DElncRNAs) in LSCC compared with adjacent tissues, functional enrichment of DEmRNAs was performed. Then, construction of the ceRNA (DElncRNA-DEmiRNA-DEmRNA) regulatory network and functional analyses of all DEmRNAs in ceRNA regulatory network were conducted. Quantitative real-time polymerase chain reactions (qRT-PCR) were used to detect the expression levels of selected DEmRNAs, DEmiRNAs, and DElncRNAs. RESULTS: A total of 3449 DEmRNAs, 40 DEmiRNAs, and 100 DElncRNAs were identified in LSCC. The ceRNA networks, which contained 132 DElncRNA-DEmiRNA pairs and 287 DEmiRNA-DEmRNA pairs, involving 44 lncRNAs, 3 miRNAs, and 271 mRNAs, were obtained. DEmRNAs in ceRNA regulatory networks were significantly enriched in pathways in cancer, prostate cancer, and aldosterone-regulated sodium reabsorption. Except for HCG22 and hsa-miR-1246, expressions of the others in the qRT-PCR results played the same pattern with that in our integrated analysis, generally. CONCLUSIONS: We concluded that HCG22/EGOT-hsa-miR-1275-FAM107A and HCG22/EGOT-hsa-miR-1246-Glycerol-3-phosphate dehydrogenase 1 like interaction pairs may play a central role in LSCC.

12.
Zhongguo Zhong Yao Za Zhi ; 46(13): 3388-3393, 2021 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-34396759

RESUMO

To study the mechanism of polysaccharides from seeds of Vaccaria segetalis( PSV) in the treatment of bacterial cystitis through the NLRP3 inflammasome pathway. The rat model of urinary tract infection was used and treated with PSV,and the urine and bladders were collected. The level of interleukin-10( IL-10) in rat urine was detected by enzyme linked immunosorbent assay( ELISA). Western blot and immunofluorescence staining were used to detect the expressions of sonic hedgehog( SHH) and NLRP3 inflammasome [NOD-like receptor thermoprotein domain 3( NLRP3),apoptosis associated speck like protein( ASC) and pro-caspase-1]. The expression of Toll-like receptor pathway was detected by RT-PCR. The death of 5637 cells induced by uropathogenic Escherichia coli( UPEC) and lactate dehydrogenase( LDH) release were evaluated using live/dead staining. The results showed that in the rat bladder,the expressions of SHH,NLRP3 inflammasomes and Toll-like receptors were significantly up-regulated,and NLRP3 inflammasomes were significantly activated by UPEC infection. The administration with PSV could significantly increase the concentration of IL-10 in urine,inhibit the expressions of SHH,NLRP3 inflammasomes and Toll-like receptors in bladder,and inhibit the activation of NLRP3 inflammasomes. A large number of 5637 cells were dead after UPEC infection and caused LDH production. PSV could significantly inhibit the death of 5637 cells and the release of LDH. In conclusion,PSV could inhibit the expression and activation of NLRP3 inflammasomes by inhibiting the Toll-like receptor pathway,thereby mitigating the bladder injury.


Assuntos
Infecções Urinárias , Vaccaria , Animais , Proteínas Hedgehog , Inflamassomos/genética , Interleucina-1beta , Proteína 3 que Contém Domínio de Pirina da Família NLR/genética , Polissacarídeos/farmacologia , Ratos , Sementes , Bexiga Urinária , Infecções Urinárias/tratamento farmacológico
13.
J Agric Food Chem ; 69(28): 8038-8049, 2021 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-34236846

RESUMO

Appropriately increasing intramuscular fat content can help improve meat quality, so it is necessary to explore the internal molecular mechanism of preadipocyte differentiation. The role of heme oxygenase 1 (HO1) in cell oxidative stress, energy metabolism, cell proliferation, and differentiation has gradually been revealed. Here, we used 3'RACE to identify the full-length 3' untranslated region (3'UTR) of HO1 and found that a very short 3'UTR variant was produced by alternative polyadenylation (APA). HO1 with a long 3'UTR variant was identified as a direct target of miR155-5P and miR377-3P. Our experimental results verified the inhibitory effect of HO1 on preadipocyte differentiation. In addition, our research confirms that by escaping microRNA inhibitory effects, the HO1 3'UTR short variant produced by APA has a higher level of expression. Thus, the HO1 3'UTR short variant has a stronger inhibitory effect on the preadipocyte differentiation than the HO1 3'UTR long variants in 3T3-L1.


Assuntos
MicroRNAs , Poliadenilação , Regiões 3' não Traduzidas , Células 3T3-L1 , Adipogenia/genética , Animais , Heme Oxigenase-1/genética , Proteínas de Membrana , Camundongos , MicroRNAs/genética , MicroRNAs/metabolismo
14.
Blood ; 2021 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-34255814

RESUMO

YTHDC1 has distinct functions as a nuclear N6-methyladenosine (m6A) reader in regulating RNA metabolism. Here we show that YTHDC1 is overexpressed in Acute Myeloid Leukemia (AML) and that it is required for proliferation and survival of human AML cells. Genetic deletion of Ythdc1 markedly blocks AML development and maintenance as well as self-renewal of leukemia stem cells (LSCs) in vivo in mice. We find that Ythdc1 is also required for normal hematopoiesis and hematopoietic stem/progenitor cell (HSPC) maintenance in vivo. Notably, Ythdc1 haploinsufficiency reduces self-renewal of LSCs, but not HSPCs in vivo. YTHDC1 knockdown has a strong inhibitory effect on proliferation of primary AML cells. Mechanistically, YTHDC1 regulates leukemogenesis through MCM4, which is a critical regulator of DNA replication. Our study provides the compelling evidence to show an oncogenic role and a distinct mechanism of YTHDC1 in AML.

15.
Front Pediatr ; 9: 670887, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34277518

RESUMO

Aim: To compare the diagnostic values by using transthoracic echocardiography (ECHO) and multi-slice spiral CT coronary angiography (CTCA) for identifying coronary artery thrombosis in children with Kawasaki disease (KD). Methods: Total 97 KD children with coronary artery dilation complications in our hospital from June 2012 to December 2020 were included in the study. CTCA and ECHO were performed after over 1 month of illness. Results: Coronary artery thrombosis was found in 14 out of 97 patients. Among them, 10 were identified as positive by CTCA, 9 were identified as positive by ECHO, and 5 were identified as positive by both CTCA and ECHO. Conclusion: Both CTCA and ECHO can be used to diagnose coronary artery thrombosis. ECHO has advantage in identifying low-density thrombus, and CTCA is better for the clot in distal coronary artery. They can complement each other.

16.
ACS Appl Mater Interfaces ; 13(27): 31624-31634, 2021 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-34219452

RESUMO

Solar steam generation is considered as an efficient way for addressing water shortage issues via seawater desalination and wastewater purification. In a solar evaporator, an absorber would convert optical energy to heat for evaporating nearby water. In this process, many low-boiling-point contaminants can also be evaporated along with water steam, which compromises the effectiveness of purification. There is, so far, no study on the removal of such low-boiling-point contaminants such as organic pesticides in wastewater. To address this problem, we demonstrate a versatile carbon hybrid aerogel (CHA) as a solar powered water purification platform. With an elaborate absorber design, the maximum solar evaporation rate of 2.1 kg m-2 h-1 is achieved under 1 sun illumination. More importantly, CHA can effectively suppress the evaporation of low-boiling-point contaminants including common pesticides and mercury ion via its strong adsorption and retention effect. Synergetic steaming and the adsorption of CHA will inspire more paradigms of solar steam generation technologies for applications relevant to detoxification and water remediation.

17.
Front Cardiovasc Med ; 8: 646306, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34124190

RESUMO

Objective: Myocardial ischemia/reperfusion (I/R) injury is one of the causes of most cardiomyocyte injuries and deaths. Berberine (BBR) has been suggested a potential to exert protective effects against myocardial I/R injury. This systematic review aims to determine the intrinsic mechanisms of BBR's protective effects in myocardial I/R injury. Methods: Seven databases were searched for studies performed from inception to July 2020. Methodological quality was assessed by SYRCLE's-RoB tool. Results: Ten studies including a total of 270 animals were included in this study. The methodology quality scores of the included studies ranged from 5 to 7 points. The meta-analysis we conducted demonstrated that BBR significantly reduced myocardial infarct size and the incidence of ventricular arrhythmia, compared to control groups (P < 0.00001). Cardiac function of animals in the BBR treatment group was also markedly increased (P < 0.00001). The index of myocardial apoptosis and the levels of biomarkers of myocardial infarction (LDH and CK) were also decreased in the BBR treatment groups compared to the control groups (P < 0.00001). Conclusions: The pre-clinical evidence, according to our study, showed that BBR is a promising therapeutic agent for myocardial I/R injury. However, this conclusion should be further investigated in clinical studies.

18.
Artigo em Inglês | MEDLINE | ID: mdl-34156465

RESUMO

OBJECTIVE: To investigate the utility of 18F-fluorodeoxyglucose positron emission tomography/computed tomography (18F-FDG-PET/CT) in assessing disease activity in Takayasu arteritis (TA). METHODS: Ninety-one patients with TA, were recruited from a Chinese cohort. Clinical data, acute-phase reactants (APRs), and 18F-FDG-PET/CT findings were simultaneously recorded. The value of using 18F-FDG-PET/CT to identify active disease was evaluated, using erythrocyte sedimentation rate (ESR) as a reference. Disease activity assessment models were constructed and concordance index (C-index), net reclassification index (NRI), and integrated discrimination index (IDI) were evaluated to compare the benefits of the new modes with ESR and Kerr score. RESULTS: In total, 64 (70.3%) cases showed active disease. Higher levels of ESR and CRP, and lower interleukin (IL)-2R levels, were observed in active cases. 18F-FDG-PET/CT parameters, including SUVmean, SUVratio1, SUVratio2, sum of SUVmean, and sum of SUVmax, were significantly higher in active disease groups. The C index threshold of ESR to indicate active disease was 0.78 (95% CI: 0.69-0.88). The new activity assessment model combining ESR, sum of SUVmean, and IL-2R showed significant improvement in C index over the ESR method (0.96 vs 0.78, p < 0.01; NRI 1.63, p < 0.01; and IDI 0.48, p < 0.01). The new model also demonstrated modest superiority to Kerr score assessment (0.96 vs 0.87, p = 0.03; NRI 1.19, p < 0.01; and IDI 0.33 p < 0.01). CONCLUSIONS: A novel 18F-FDG-PET/CT-based method that involves combining the sum of SUVmean with ESR score and IL-2R levels demonstrated superiority in identifying active TA compared with conventional methods.

19.
Org Lett ; 23(12): 4864-4869, 2021 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-34080874

RESUMO

We report an efficient Au(I)-catalyzed formal allylation of diazo(thio)oxindoles using allyltrimethylsilane to give 3-allyl (thio)oxindoles, which are difficult to access by using traditional alkylation methods under basic conditions. The approach enables a highly stereoselective synthesis of quaternary (thio)oxindoles via a formal allylation-asymmetric Michael addition sequence. These adducts are versatile synthons for spirocyclic (thio)oxindoles. Initial biological studies reveal that chiral thiooxindoles show promising antiproliferation activity that is better than that of the corresponding oxindoles.

20.
J Org Chem ; 86(13): 9206-9217, 2021 07 02.
Artigo em Inglês | MEDLINE | ID: mdl-34126743

RESUMO

An unprecedented catalyst-free reaction of benzo[b]thiophene-2,3-diones with difluoroenoxysilanes has been developed using either MeOH or H2O as the solvent, which constitutes a facile and efficient protocol for the solvent-controlled divergent synthesis of five- and seven-membered S-heterocycles featuring a gem-difluoromethylene group. A gram-scale synthesis and the diversification of the product transformations to other difluorinated S-heterocycles further highlight its utility.


Assuntos
Solventes , Catálise
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