Association of phthalate metabolites with periodontitis: a population-based study.

BACKGROUND: Widespread exposure to phthalates may raise the probability of various diseases. However, the association of phthalate metabolites with periodontitis remains unclear. METHODS: Totally 3402 participants from the National Health and Nutrition Examination Survey (NHANES) 2009 to 2014 cycles were enrolled in the cross-sectional investigation. We utilized weighted logistic regression to evaluate the association of ten phthalate metabolites with periodontitis. Restricted cubic spline analysis was applied to investigate potential nonlinear relationships. RESULTS: The weighted prevalence of periodontitis in the study was 42.37%. A one standard deviation (SD) rise in log-transformed levels of mono-2-ethyl-5-carboxypenty phthalate (MECPP), mono-n-butyl phthalate (MnBP), mono-(2-ethyl-5-hydroxyhexyl) phthalate (MEHHP), mono-isobutyl phthalate (MiBP), mono-(2-ethyl-5-oxohexyl) phthalate (MEOHP), and mono-benzyl phthalate (MBzP) was associated with higher odds of periodontitis, with odds ratios (95% confidence intervals) of 1.08 (1.02-1.14), 1.07 (1.02-1.11), 1.10 (1.05-1.15), 1.05 (1.01-1.09), 1.09 (1.04-1.14), and 1.08 (1.03-1.13), respectively. Individuals with the highest quartile concentrations of MECPP, MnBP, MEHHP, MEOHP, and MBzP were associated with 32%, 20%, 30%, 25%, and 26% increased odds of periodontitis, respectively, compared to those with the lowest quartile. Additionally, mono-(3-carboxypropyl) phthalate (MCPP) demonstrated an interesting inverted J-shaped relationship with periodontitis. CONCLUSIONS: The findings indicate an association of certain phthalate metabolites with periodontitis among US adults.

Emerging concern on air pollution and health: Trade-off between air pollution exposure and physical activity.

Air pollution is a major contributor to the global disease burden, especially affecting respiratory and cardiovascular health. However, physical activity is associated with improved lung function, a slower decline in lung function, and lower mortality. The public is more likely to be exposed to air pollution during outdoor physical activity. However, studies on how long-term and short-term exposure to air pollution interacts with physical activity yield inconsistent results, and the thresholds for air pollution and physical activity remain unclear. Thus, more studies are needed to provide sufficient evidence to guide the public to safely engage in outdoor physical activity when exposed to air pollution.

Effect of insoluble dietary fiber on printing properties and molecular interactions of 3D-printed soy protein isolate-wheat gluten plant-based meats.

Insoluble dietary fiber (IDF) has been characterized to prevent chronic diseases and improve gastrointestinal health, and it has been added to 3D printing plant-based meats (PM) to enhance texture and increase nutritional properties. Therefore, the aim of this study was to investigate the effects of IDF on 3D printing properties and molecular interactions of soy protein isolate (SPI) - wheat gluten (WG) PM. Without the participation of IDF, PM appeared to collapse. When the IDF concentration increased from 0 to 10 %, PM displayed good printing properties, water holding capacity, tensile strength, and elongation at break were increased. Tensile strength and elongation at break reached a maximum at 10 % IDF, and clearly similar results were found for texture attribute indices such as hardness, gumminess, chewiness, and cohesiveness after cooking. All printing inks exhibited shear-thinning behavior and solid-like viscoelasticity, but the structural recovery properties of 3D-printed PM deteriorated when the IDF content was over 10 %. Intermolecular forces indicated that the addition of IDF enhanced the disulfide bonds so that 10 % IDF presented better printing properties. These results indicated the potential for developing PM with dietary fiber functionality through 3D printing technology.

Transformation of waste battery cathode material LiMn2O4 into efficient ultra-low temperature NH3-SCR catalyst: Proton exchange synergistic vanadium modification.

It is essential to develop the catalyst for NH3-SCR with excellent performance at ultra-low temperature (≤150 °C), and resource recycling is another important part of environmental protection. Based on the principle of environmental friendliness, the LiMn2O4, one of the waste battery cathode materials, was successfully modified into a novel high-value catalyst for ultra-low temperature NH3-SCR through hydrogen ion exchange and two-dimensional vanadic oxide modification. The optimized LiMn2O4-0.5V-10H catalyst performed the best balance of NOx conversion and N2 selectivity, with activity reaching 96 % at 150 °C and N2 selectivity exceeding 70 % at ultra-low temperature. Due to the unique three-dimensional network structural characteristics of LiMn2O4 spinel, hydrogen exchange could exchange Li+ from the lattice and increase surface acidity; and a small amount of two-dimensional vanadic oxide loading could appropriately regulate redox ability and increase acidic sites. The in-situ DRIFTS results still showed that the L-H and E-R mechanisms coexisted during the reaction. Moreover, combining first-principles calculations and in-situ DRIFTS, the dual modification of H and V could enhance the adsorption of NH3 on the surface of LiMn2O4 but weaken the adsorption of NO, and promote the decomposition of nitrites while inhibit the formation of surface nitrate species, which was the core reason for the improvement of N2 selectivity. The modification mode in this work was simple and inexpensive, which provided a new idea for the high-value utilization of waste batteries and the design of NOx purification catalyst at ultra-low temperature.

Osteoclast-Derived Exosomal miR-5134-5p Interferes with Alveolar Bone Homeostasis by Targeting the JAK2/STAT3 Axis.

Background: In chronic periodontitis, exosomes transport various informative substances between osteoclasts and osteoblasts in alveolar bone. Herein, we aimed to investigate the effect of exosomal micro-ribonucleic acid (miRNA/miR)-5134-5p derived from osteoclasts on osteoblastic proliferation and differentiation and the development of periodontitis in vivo and in vitro. Methods: The effects of OC-Exos on the proliferation and differentiation of osteoblasts were identified by Real-time quantitative reverse polymerase chain reaction (qRT-PCR), Western blot(WB), alkaline phosphatase(ALP) staining, etc. Exosomal miRNA expression was analyzed by sequencing. The sites of miRNA action were predicted through TargetScan and tested by double luciferase assay. After transfecting miR-5134-5p mimic/inhibitor into osteoblasts, we measured the proliferation and differentiation of osteoblasts by ALP staining and WB, etc. Furthermore, OC-Exos were injected into the gingival sulcus at the ligation site. Inflammation was observed by Hematoxylin-eosin (H&E) staining, the expression of inflammatory factors were detected by qRT-PCR, the resorption of alveolar bone was observed by Micro CT. Results: Osteoblastic proliferation and differentiation were negatively regulated by OC-Exos in vitro. miRNA sequencing analysis revealed that miR-5134-5p expression was significantly elevated in OC-Exos, which also increased in osteoblasts following OC-Exo intervention. The dual-luciferase assay revealed that miR-5134-5p and Janus kinase 2 (JAK2) had binding sites. miR-5134-5p-mimics could upregulate miR-5134-5p expression in osteoblasts while downregulating Runt-related transcription factor 2(Runx2), phosphorylated-JAK2 (p-JAK2), and phosphorylated-signal transducer and activator of transcription 3 (p-STAT3) expression and inhibited osteogenic differentiation. However, miR-5134-5p-inhibitor had the opposite effect. In vivo, the OC-Exo group demonstrated morphological disruption of periodontal tissue, massive inflammatory cell infiltration, upregulation of inflammatory factors mRNA expression, a significant decrease in BV/TV, and an increase in the cementoenamel junction and alveolar bone crest distance. Conclusion: Osteoclast-derived exosomal miR-5134-5p inhibits osteoblastic proliferation and differentiation via the JAK2/STAT3 pathway. OC-Exos exacerbate periodontal tissue inflammation and accelerate alveolar bone resorption in mice with experimental periodontitis.

Potential of an Aligned Porous Hydrogel Scaffold Combined with Periodontal Ligament Stem Cells or Gingival Mesenchymal Stem Cells to Promote Tissue Regeneration in Rat Periodontal Defects.

Periodontal tissue regeneration is a major challenge in tissue engineering due to its regenerated environment complexity. It aims to regenerate not only the supporting alveolar bone and cementum around teeth but also the key connecting periodontal ligament. Herein, a constructed aligned porous hydrogel scaffold carrying cells based on chitosan (CHI) and oxidized chondroitin sulfate (OCS) treated with a freeze-casting technique was fabricated, which aimed to induce the arrangement of periodontal tissue regeneration. The microscopic morphology and physical and chemical properties of the hydrogel scaffold were evaluated. The biocompatibilities with periodontal ligament stem cells (PDLSCs) or gingival-derived mesenchymal stem cells (GMSCs) were verified, respectively, by Live/Dead staining and CCK8 in vitro. Furthermore, the regeneration effect of the aligned porous hydrogel scaffold combined with PDLSCs and GMSCs was evaluated in vivo. The biocompatibility experiments showed no statistical significance between the hydrogel culture group and blank control (P > 0.05). In a rat periodontal defect model, PDLSC and GMSC hydrogel experimental groups showed more pronounced bone tissue repair than the blank control (P < 0.05) in micro-CT. In addition, there was more tissue repair (P < 0.05) of PDLSC and GMSC hydrogel groups from histological staining images. Higher expressions of OPN, Runx-2, and COL-I were detected in both of the above groups via immunohistochemistry staining. More importantly, the group with the aligned porous hydrogel induced more order periodontal ligament formation than that with the ordinary hydrogel in Masson's trichrome analysis. Collectively, it is expected to promote periodontal tissue regeneration utilizing an aligned porous hydrogel scaffold combined with PDLSCs and GMSCs (CHI-OCS-PDLSC/GMSC composite), which provides an alternative possibility for clinical application.

Long-term exposure to fine particulate matter modifies the association between physical activity and the risk of hypertension.

The trade-off between the potentially detrimental effects of fine particulate matter (PM2.5) and the benefits of physical activity (PA) is unclear. We aimed to explore the independent and interaction effects between long-term PM2.5 exposure and PA on blood pressure (BP) and hypertension. A total of 8704 adults (≥45 years) without hypertension at baseline in a nationwide cohort of the China Health and Retirement Longitudinal Study (CHARLS) were followed from 2011 to 2015. The participants were selected using a four-stage, stratified, and cluster sampling procedure. The annual PM2.5 concentrations at the residential address were estimated from a two-stage machine learning model with a 10 km × 10 km resolution. A standard questionnaire collected information on PA and potential confounders, and metabolic equivalents (MET·h/wk), which combined frequency, intensity, and duration information, were used to assess PA levels. We adopted mixed-effects regression models to explore the independent and interaction effects between long-term PM2.5 exposure and PA on BP and risk of hypertension. Systolic blood pressure (SBP) decreased by -0.84 mmHg (95% CI: -1.34, -0.34) per an IQR (interquartile range, 175.5 MET·h/wk) increase in PA, and diastolic blood pressure (DBP) decreased by -0.42 mmHg (95% CI: -0.76, -0.07). Each IQR (36.1 µg/m3) increment in PM2.5 was associated with 0.48 mmHg (95% CI: -0.24, 1.20) in SBP and -0.02 mmHg (95% CI: -0.44, 0.39) in DBP. PM2.5 showed an elevated effect with risks of hypertension (odds ratio, OR = 1.01; 95% CI: 1.00, 1.03), while PA showed the inverse result (OR = 0.98; 95% CI: 0.97, 0.99). Interaction analyses indicated PA maintained the beneficial effects on BP, but the negative association was attenuated, accompanied by the increase of PM2.5. PA decreased the BP and hypertension risks, while PM2.5 showed the opposite results. PM2.5 attenuated the beneficial effects of PA on BP and modified the association between PA and the risk of hypertension.

Acute change of lung function to short-term exposure to ambient air pollutants with and without physical activity: A real-world crossover study.

Physical activity (PA) would increase the inhalation rate and thereby inhaled dose of air pollutants. However, it's still uncertain whether the effects of air pollutants on lung function are attenuated by PA, especially in the high-polluted areas. We aimed to disentangle the interaction between air pollution and PA on lung function among healthy adults. In this study, a real-world crossover study was conducted among 74 healthy adults. Each participant underwent both rest and 15-min intermittent moderate PA exposure scenarios (consisting of 15min stationary bike riding alternating with 15min of rest), which lasted for 2 h. On the same day, the participants among active and inactive group were exposed to the same air pollution. We have monitored the fine particulate matter (PM2.5), particulate matter less than 10 µm (PM10), particulate matter less than 1 µm (PM1), black carbon (BC), nitrogen dioxide (NO2), and ozone (O3) continuously during 2-h exposure. Lung function were measured at five times points for each visit (before, immediately, 3 h, 5 h, and 24 h after the 2-h exposure scenario). Mixed-effects models were applied to explore the effects of air pollution, PA, and their interaction on lung function. The participants had a mean (standard deviation (SD)) age of 19.9 (0.9) years. The average concentration [mean ± SD] of PM2.5, PM10, PM1, BC, NO2, and O3 were 59.4 ± 45.1 µg/m3, 122.8 ± 109.0 µg/m3, 38.8 ± 29.2 µg/m3, 1.94 ± 1.17 µg/m3, 59.5 ± 26.6 µg/m3, and 74.0 ± 30.3 µg/m3, respectively. Overall, greater increasement in lung function were observed among active group compared with inactive group at all timepoints. In fully adjusted models, we observed the benefits of PA and detrimental effects of air pollutants on lung function. Our results suggested that PA, compared to rest, alleviated the detrimental effects of air pollutants on lung function. We also stressed the importance of timing of measurements for capturing association. In conclusion, our observations suggested that PA might alleviate the associations between various pollutant exposures and lung function, which would drive further research towards potential pathway.

Physical activity attenuated the associations between ambient air pollutants and metabolic syndrome (MetS): A nationwide study across 28 provinces.

The independent associations of air pollution and Physical activity (PA) with metabolic syndrome (MetS) were inconsistent, while the joint associations between PA and air pollution with MetS were still unknown. We aimed to (1) further confirm the independent associations of PA and air pollution; (2) examine whether PA would attenuate the positive associations of air pollutants with MetS. We included 13,418 adults above 45 years old in this study. We defined MetS according to the Joint Interim Societies. The concentration of air pollutants (including fine particulate matter (PM2.5), inhalable particles (PM10), ozone (O3), nitrogen dioxide (NO2), sulfur dioxide (SO2), and carbon monoxide (CO)) were estimated by ground-based measurements and satellite remote sensing products. We assessed the level of PA by metabolic equivalent (MET)-hour/week by summing the MET of all activities. We applied logistic regression models with sampling weight to explore the independent and joint associations of PA and air pollutants on MetS. Interaction plots were conducted to exhibit estimates of air pollutants on MetS as a function of PA. We found that all air pollutants were positively associated with the odds of MetS, while PA showed beneficial associations with MetS. The associations of air pollution on MetS decreased accompanied the increase of PA, while the detrimental effects between air pollutants and MetS did not be reversed by PA. In conclusion, PA may attenuate the associations of air pollutants with MetS, although in polluted areas, suggesting that keeping PA might be an effective way to reduce the adverse effects of air pollution with MetS.

Identifying the threshold of outdoor PM2.5 reversing the beneficial association between physical activity and lung function: A national longitudinal study in China.

BACKGROUND: Despite cumulative evidence reports the interaction effects of physical activity (PA) and air pollution on lung function, the findings have been inconsistent. We aimed to identify the threshold values that reverse the beneficial effects of PA on lung function. METHODS: This multistage probability sampling study examined 13,032 individuals aged ≥45 years across China from 2011 to 2015. City-level particulate matter 2.5 µm or less in diameter (PM2.5) were estimated based on a two-stage machine learning model, with a spatial resolution of 0.1° × 0.1°. We assessed PA and a range of covariates using standardized self-reported questionnaires. The peak expiratory flow (PEF) was measured using a peak flow meter. We used mixed-effects linear regression models to examine the associations between PA and PM2.5, and their interactions with PEF. RESULTS: Participants were 60.4 ± 9.4 years old [mean ± standard deviation (SD)]. The mean ± SD of PM2.5 and PEF was 54.4 ± 23.0 µg/m3 and 273 ± 116 L/min, respectively. Each 10 µg/m3 increase in PM2.5 was associated with a 1.27 L/min decrease in PEF. The PEF increased by 2.48 (95% confidence interval, CI: 0.40, 4.55) L/min, 0.74 (95% CI: -1.17, 2.66) L/min, and 1.99 (95% CI: 0.001, 3.99) L/min following a 10 h/week increment of walking, moderate intensity PA, and vigorous intensity PA, respectively. Detrimental associations between PM2.5 and PEF outweighed PA benefits for approximate PM2.5 concentrations >81 µg/m3 (95% CI: 58.9, 111) and >77 µg/m3 (95% CI: 39.7, 102) for walking and vigorous intensity PA, respectively. CONCLUSIONS: We identified the threshold of ambient PM2.5 above which the beneficial association of PA with lung function may be reversed to an adverse one. Although the threshold may vary across populations and places, the findings suggested that reducing air pollution could enhance the benefits of PA on lung function.

A novel 3-acyl isoquinolin-1(2H)-one induces G2 phase arrest, apoptosis and GSDME-dependent pyroptosis in breast cancer.

Breast cancer is the most common malignancy among women worldwide, accordingly, numerous chemotherapeutic drugs have been discovered thus far. However, the development and application of these drugs is severely constrained because of their unclear mechanism. To address this issue, our previous work has defined 3-acyl isoquinolin-1(2H)-one derivatives as potent anti-tumor agents, among which the compound 4f possessed relatively higher activity in vitro. In this study, we aim to further explore the anti-cancer effect and the underlying molecular mechanism of 4f in breast cancer cells. Therefore, CCK8 assay was used to detect cell viability and flow cytometry was used to analyze cell cycle and apoptosis. Meanwhile, related proteins that regulate cell cycle and apoptosis were detected. The results showed that 4f induced cell apoptosis and inhibited cell proliferation in breast cancer cells in a dose-depended manner without significant toxicity to human normal mammary epithelial cell. The cell cycle was arrested at G2 phase with the suppressed expression of the CDK1 protein. Additionally, 4f was confirmed to induce the cell apoptosis with the up-regulation of bax, down-regulation of bcl-2, activation of cleaved-caspase3/7/9 and cleaved-PARP, together with the inhibition of MEK/ERK and p38 MAPK pathway. Moreover, the GSDME-mediated pyroptosis was also induced by 4f in breast cancer cells. Together, these results demonstrated that 4f could serve as a new and promising candidate for the treatment of breast cancer.

Research progress on the relationship between chronic periodontitis and Parkinson's disease.

Chronic periodontitis is an infectious disease, which has a reciprocal relationship with a variety of systemic disorders. Parkinson's disease is a prevalent neurodegenerative disease in which inflammation plays an important role for its progression. A vast number of studies suggest that there is a potential connection between chronic periodontitis and neurodegenerative diseases such as Parkinson's disease. Individuals with Parkinson's disease usually have poor periodontal health, and their oral flora composition differs from that of healthy people; at the same time, patients with chronic periodontitis have a higher risk of Parkinson's disease, which can be reduced with regular periodontal treatment. In fact, the mechanism of interaction between chronic periodontitis and Parkinson's disease is not clear. According to several studies, the clinical symptoms of Parkinson's disease prevent patients to maintain oral hygiene effectively, increasing the risk of periodontitis. Neuroinflammation mediated by microglia may be the key to the influence of chronic periodontitis on Parkinson's disease. Periodontal pathogens and inflammatory mediators may enter the brain and activate microglia in various ways, and ultimately leading to occurrence and development of Parkinson's disease. This article reviews the recent research progress on the association between chronic periodontitis and Parkinson's disease, and its potential mechanism to provide information for further research.

Autophagy-Related Genes Predict the Progression of Periodontitis Through the ceRNA Network.

Purpose: The goal of this study was to identify the crucial autophagy-related genes (ARGs) in periodontitis and construct mRNA-miRNA-lncRNA networks to further understand the pathogenesis of periodontitis. Methods: We used the Gene Expression Omnibus (GEO) database and Human Autophagy Database (HADb) to identify differentially expressed mRNAs, miRNAs, and ARGs. These ARGs were subjected to Gene Ontology (GO), KEGG (Kyoto Encyclopedia of Genes and Genomes) pathway, and PPI (protein-protein interaction) network analysis. Two databases (miRDB and StarBase v2.0) were used to reverse-predict miRNAs while the miRNA-lncRNA interaction was predicted using the StarBase v2.0 and LncBase Predicted v.2 databases. After excluding the lncRNAs only present in the nucleus, a competing endogenous RNA (ceRNA) network was built. Finally, we used quantitative real-time PCR (qRT-PCR) to confirm the levels of mRNA expression in the ceRNA network. Results: The differential expression analysis revealed 10 upregulated and 10 downregulated differentially expressed ARGs. After intersecting the reverse-predicted miRNAs with the differentially expressed miRNAs, a ceRNA network consisting of 4 mRNAs (LAMP2, NFE2L2, NCKAP1, and EGFR), 3 miRNAs (hsa-miR-140-3p, hsa-miR-142-5p, and hsa-miR-671-5p), and 30 lncRNAs was constructed. In addition, qRT-PCR results revealed that EGFR expression was downregulated in diseased gingival tissue of periodontitis patients. Conclusion: Four autophagy-related genes, especially EGFR, may play a key role in periodontitis progression. The novel ceRNA network may aid in elucidating the role and the mechanism of autophagy in periodontitis, which could be important in developing new therapeutic options.

Mechanistic Insights into the Dual Directing Group-Mediated C-H Functionalization/Annulation via a Hydroxyl Group-Assisted MIII-MV-MIII Pathway.

The experimental investigations on the catalyst [Cp*Rh(OAc)2 and Cp*Ir (OAc)2)]-controlled [3 + 2] and [4 + 2] annulations of oximes with propargyl alcohols have been finished in our previous work and a supposed dual directing group-mediated reaction pathway has been deduced for the chemodivergent product synthesis. However, the detailed interaction modes of the dual directing groups binding with the corresponding metal center to achieve the above observed chemoselectivity remain unclear and even contradict. For instance, the calculational traditional dual direct coupling transition states suggested that both Cp*Rh(OAc)2- and Cp*Ir(OAc)2-catalyzed reactions would generate five-membered indenamines as the dominant products via [3 + 2] annulation. To address this concern, herein, systematic DFT calculations combined with proof-of-concept experiments have been carried out. Accordingly, a novel and more favorable MIII-MV-MIII reaction mechanism, which involves an unprecedented HOAc together with a hydroxyl group-assisted reaction pathway in which the hydroxyl group acts as double effectors for the formation of M-O coordination and [MeO···H···O(CCH3)O···H···O] bonding interactions, was deduced. Taken together, the present results would provide a rational basis for future development of the dual directing group-mediated C-H activation reactions.

Lossen Rearrangement vs C-N Reductive Elimination Enabled by Rh(III)-Catalyzed C-H Activation/Selective Lactone Ring-Opening: Chemodivergent Synthesis of Quinolinones and Dihydroisoquinolinones.

An unprecedented Rh(III)-catalyzed cascade C-H activation/Lossen rearrangement of aromatic amides with methyleneoxetanones has been realized along with a tunable C-N bond reductive elimination/trans esterification, giving divergent access to quinolinones and dihydroisoquinolinones via selective ring-opening of the four-membered lactone unit. Combined computational and experimental mechanistic studies defined the solvent-involved distinguished reaction paths, the origin of the observed chemodivergence, as well as the role of the substituent attached at the oxidizing directing group in tuning the reaction outcomes.

A Unique Energy-Saving Strategy during Hibernation Revealed by Multi-Omics Analysis in the Chinese Alligator.

Many ectotherms hibernate in face of the harsh winter conditions to improve their survival rate. However, the molecular mechanism underlying this process remains unclear. Here, we explored the hibernation mechanism of Chinese alligator using integrative multi-omics analysis. We revealed that (1) the thyroid hormone biosynthesis, nutrition absorption and metabolism, muscle contraction, urinary excretion and immunity function pathways are overall downregulated during hibernation; (2) the fat catabolism is completely suppressed, contrasting with the upregulation of hepatic fatty-acid-transporter CPT1A, suggesting a unique energy-saving strategy that differs from that in hibernating mammals; (3) the hibernation-related genes are not only directly regulated by DNA methylation but also controlled by methylation-dependent transcription networks. In addition, we identified and compared tissue-specific, species-specific, and conserved season-biased miRNAs, demonstrating complex post-transcriptional regulation during hibernation. Our study revealed the genetic and epigenetic mechanisms underlying hibernation in the Chinese alligator and provided molecular insights into the evolution of hibernation regulation.

Rh(III)-Catalyzed Redox-Neutral [4+2] Annulation for Direct Assembly of 3-Acyl Isoquinolin-1(2H)-ones as Potent Antitumor Agents.

By virtue of an efficient rhodium(III)-catalyzed redox-neutral C-H activation/ring-opening of a strained ring/[4+2] annulation cascade of N-methoxybenzamides with propargyl cycloalkanols, diverse 3-acyl isoquinolin-1(2H)-ones were directly obtained in good yields and with excellent functional group compatibility. Additionally, their antitumor activities against various human cancer cells including HepG2, A549, MCF-7 and SH-SY5Y were evaluated and the action mechanism of the selected compound was also investigated in vitro. The results revealed that these products possessed a potent efficacy, by inhibiting proliferation and inducing apoptosis in a time-dependent and dose-dependent manner, suggesting that such compounds can serve as promising candidates for anti lung cancer drug discovery.

Rh(III)-Catalyzed C-H Activation/Cycloisomerization of N-Phenoxyacetamides with Enynones for One-Pot Assembly of Furylated 2-Alkenylphenols.

An efficient and practical procedure for one-pot assembly of furylated 2-alkenylphenols has been achieved via the Cp*CyRh-catalyzed regioselective redox-neutral C-H activation/5-exo-dig cyclization cascade using N-phenoxyacetamides and enynones as the viable substrates. The synthetic application of such a protocol has also been demonstrated to highlight the versatility of this transformation.

Stereoselective ß-F Elimination Enabled Redox-Neutral [4 + 1] Annulation via Rh(III)-Catalyzed C-H Activation: Access to Z-Monofluoroalkenyl Dihydrobenzo[ d]isoxazole Framework.

An efficient and practical Rh(III)-catalyzed redox-neutral [4 + 1] annulation of N-phenoxy amides with α, α-difluoromethylene alkynes has been realized to give direct access to the Z-configured monofluoroalkenyl dihydrobenzo[ d]isoxazole framework with broad substrate compatibility and good functional group tolerance, which was further enhanced by the late-stage C-H modification of complex bioactive compounds. Subsequent density functional theory calculations revealed that the stereoselective ß-F elimination involving an allene species played a decisive role in determining the reaction outcome and such Z-selectivity.

Rhodium(iii)-catalyzed chemoselective C-H functionalization of benzamides with methyleneoxetanones controlled by the solvent.

Described herein is a Rh(iii)-catalyzed and solvent-controlled double C-H functionalization of common benzamides via selective acyl C-O cleavage (ß-H elimination) or alkyl C-O cleavage (ß-O elimination) of the methyleneoxetanone substrate, which provides a straightforward way for the divergent synthesis of chain alkylated benzamides and seven-membered 1H-benzo[c]azepine-1,3(2H)-diones in a highly chemoselective manner. Through a series of experimental investigations together with theoretical studies, the effect of the solvent has been systematically elucidated.