A General Synthesis of Cross-Conjugated Enynones through Pd Catalyzed Sonogashira Coupling with Triazine Esters.

The palladium-catalyzed Sonogashira coupling of α, ß-unsaturated acid derivatives offers a diversity-oriented synthetic strategy for cross-conjugated enynones. However, the susceptibility of the unsaturated C-C bonds adjacent to the carbonyl group toward Pd catalysts makes the direct conversion of α, ß-unsaturated derivatives as acyl electrophiles to cross-conjugated ketones rare. This work presents a highly selective C-O activation approach to prepare cross-conjugated enynones using α, ß-unsaturated triazine esters as acyl electrophiles. Under base and phosphine ligand-free conditions, NHC-Pd(II)-Allyl precatalyst alone catalyzed the cross-coupling of α, ß-unsaturated triazine esters with terminal alkynes efficiently, yielding 31 cross-conjugated enynones with diverse functional groups. This method demonstrates the potential of triazine-mediated C-O activation for preparing highly functionalized ketones.

The Intercalation of CORM-2 with Pharmaceutical Clay Montmorillonite (MMT) Aids for Therapeutic Carbon Monoxide Release.

The pharmaceutical clay montmorillonite (MMT) is, for the first time, explored as a carbon monoxide-releasing material (CORMat). MMT consists of silicate double layered structure; its exfoliation feature intercalate the CORM-2 [RuCl(µ-Cl)(CO)3]2 inside the layers to suppress the toxicity of organometallic segment. The infrared spectroscopy (IR) confirmed the existence of ruthenium coordinated carbonyl ligand in MMT layers. The energy-dispersive X-ray spectroscopy (EDX) analysis showed that ruthenium element in this material was about 5%. The scanning electron microscopy (SEM) and transmission electron microscope (TEM) images showed that the layer-structure of MMT has been maintained after loading the ruthenium carbonyl segment. Moreover, the layers have been stretched out, which was confirmed by X-ray diffraction (XRD) analysis. Thermogravimetric (TG) curves with huge weight loss around 100-200 °C were attributed to the CO hot-release of ruthenium carbonyl as well as the loss of the adsorbed solvent molecules and the water molecules between the layers. The CO-liberating properties have been assessed through myoglobin assay. The horse myoglobin test showed that the material could be hydrolyzed to slowly release carbon monoxide in physiological environments. The half-life of CO release was much longer than that of CORM-3, and it has an excellent environmental tolerance and slow release effect.

The role of diet in diabetes gastroparesis treatment: a systematic review and meta-analysis.

Background: Diabetic gastroparesis is a common complication in patient with diabetes. Dietary intervention has been widely used in the treatment of diabetic gastroparesis. The aim of this study is to evaluate the role of diet in the treatment of diabetic gastroparesis. Methods: This systematic review was conducted a comprehensive search of randomized controlled trials using dietary interventions for the treatment of diabetic gastroparesis up to 9 November 2023. The primary outcomes were gastric emptying time and clinical effect, while fasting blood glucose, 2-hour postprandial blood glucose and glycosylated hemoglobin were secondary outcomes. Data analysis was performed using RevMan 5.4 software, and publication bias test was performed using Stata 15.1 software. Results: A total of 15 randomized controlled trials involving 1106 participants were included in this review. The results showed that patients with diabetic gastroparesis benefit from dietary interventions (whether personalized dietary care alone or personalized dietary care+routine dietary care). Compared with routine dietary care, personalized dietary care and personalized dietary care+routine dietary care can shorten the gastric emptying time, improve clinical efficacy, and reduce the level of fasting blood glucose, 2-hour postprandial blood glucose and glycosylated hemoglobin. Conclusions: Limited evidence suggests that dietary intervention can promote gastric emptying and stabilize blood glucose control in patients with diabetic gastroparesis. Dietary intervention has unique potential in the treatment of diabetic gastroparesis, and more high-quality randomized controlled trials are needed to further validate our research results. Systematic review registration: https://www.crd.york.ac.uk/prospero/, identifier CRD42023481621.

Acupuncture for postoperative gastrointestinal dysfunction in cancer: a systematic review and meta-analysis.

Background: Postoperative gastrointestinal dysfunction (PGD) in cancer is the commonest and most severe postoperative complication in patients with cancer. Acupuncture has been widely used for PGD in cancer. This study aimed to evaluate the efficacy and safety of acupuncture for PGD in cancer. Methods: We comprehensively searched eight randomised controlled trials (RCTs) of acupuncture for PGD in cancer published until November 2022. Time to first flatus (TFF) and time to first defecation (TFD) were the primary outcomes, and time to bowel sound recovery (TBSR) and the length of hospital stay (LOS) were the secondary outcomes. The Cochrane Collaboration Risk of Bias Tool was used to assess the quality of the RCTs, and the Grading of Recommendations Assessment, Development, and Evaluations (GRADE) system was used to evaluate the certainty of the evidence. The meta-analysis was performed using RevMan 5.4, and a publication bias test was performed using Stata 15.1. Results: Sixteen RCTs involving 877 participants were included in this study. The meta-analysis indicated that acupuncture could effectively reduce the TFF, TFD, and TBSR compared with routine treatment (RT), sham acupuncture, and enhanced recovery after surgery (ERAS). However, acupuncture did not shorten the LOS compared with RT and ERAS. The subgroup analysis revealed that acupuncture could significantly reduce the TFF and TFD. Acupuncture effectively reduced the TFF and TFD in all cancer types included in this review. Besides, local acupoints in combination with distal acupoints could reduce the TFF and TFD, and distal-proximal acupoints could significantly reduce the TFD. No trial reported adverse events of acupuncture. Conclusions: Acupuncture is an effective and relatively safe modality for treating PGD in cancer. We anticipate that there will be more high-quality RCTs involving more acupuncture techniques and cancer types, focusing on combining acupoints for PGD in cancer, further determining the effectiveness and safety of acupuncture for PGD in patients with cancer outside China. Systematic review registration: https://www.crd.york.ac.uk/prospero, identifier CRD42022371219.

Palladium-catalysed Suzuki-Miyaura coupling of α,ß-unsaturated superactive triazine esters.

Palladium-catalysed Suzuki-Miyaura couplings of α,ß-unsaturated acid derivatives are challenging due to the susceptibility of their CC bonds adjacent to carbonyl groups. In this work, we describe a highly selective C-O activation approach to this transformation using superactive triazine esters and organoborons as coupling partners. 42 α,ß-unsaturated ketones with diverse functional groups have been prepared with this method. The mechanistic investigation unveiled that the dual function of triazine for activating the C-O bond and stabilizing non-covalent interactions between the catalyst and substrate is critical for the reaction's success. The method's efficiency, functional group compatibility and unique mechanism make it a valuable alternative to classic methods.

Acupuncture and moxibustion in patients with cancer-related insomnia: A systematic review and network meta-analysis.

Objectives: Cancer-related insomnia (CRI) is one of the most common and serious symptoms in patients with cancer. Acupuncture and moxibustion have been widely applied in the treatment of CRI. Nevertheless, the comparative efficacy and safety of different acupuncture and moxibustion techniques remain unclear. This study aimed to evaluate and compare the efficacy and safety of different acupuncture and moxibustion techniques in the treatment of CRI. Methods: Eight medical databases were comprehensively searched for relevant randomized controlled trials (RCTs) as of June 2022. Two independent reviewers assessed the risk of bias and conducted the research selection, data extraction, and quality assessment of the included RCTs. A network meta-analysis (NMA) was performed using frequency models, combining all available direct and indirect evidence from RCTs. The Pittsburgh Sleep Quality Index (PSQI) was set as the primary outcome, and adverse events and effective rates were set as the secondary outcomes. The efficacy rate was calculated as the ratio of patients with insomnia symptom relief to the total number of patients. Results: Thirty-one RCTs with 3,046 participants were included, including 16 acupuncture- and moxibustion-related therapies. Transcutaneous electrical acupoint stimulation [surface under the cumulative ranking curve (SUCRA) 85.7%] and acupuncture and moxibustion (SUCRA 79.1%) were more effective than Western medicine, routine care, and placebo-sham acupuncture. Furthermore, Western medicine showed significantly better effects than placebo-sham acupuncture. In the NMA, the acupuncture and moxibustion treatments with the best therapeutic effects for CRI were transcutaneous electrical acupoint stimulation (SUCRA 85.7%), acupuncture and moxibustion (SUCRA 79.1%), auricular acupuncture (SUCRA 62.9%), routine care combined with intradermal needling (SUCRA 55.0%), and intradermal needling alone (SUCRA 53.3%). No serious acupuncture- or moxibustion-related adverse events were reported in the included studies. Conclusion: Acupuncture and moxibustion are effective and relatively safe in treating CRI. The relatively conservative recommended order of acupuncture- and moxibustion-related therapies for CRI is as follows: transcutaneous electrical acupoint stimulation, acupuncture and moxibustion, and auricular acupuncture. However, the methodological quality of the included studies was generally poor, and further high-quality RCTs are needed to strengthen the evidence base.

Vitamin D deficiency affects the immunity against Mycobacterium tuberculosis infection in mice.

The aim of the study is to investigate the immunological changes after stimulation with bacillus Calmette-Guerin (BCG) in mice with vitamin D deficiency. After weaning, mice were divided into the vitamin D-deficient group (-D group), the normal group (N group), and the vitamin D-supplemented group (+D group). Twelve-week-old mice were intraperitoneally injected with 0.5 mg/ml BCG (≥1.0 × 10(6) CFU/mg) and maintained for 6 weeks. Spleen lymphocytes were isolated, and the percentages of CD4(+) and CD8(+) lymphocytes were determined by flow cytometry. IFN-γ levels, IL-10 levels, and the TB-PPD-specific antibody titer were determined by ELISA. The inter-group difference was analyzed using one-way ANOVA, and multiple comparisons were analyzed using the LSD test. The percentage of CD4(+) cells was 27.1 ± 0.6 in the -D group, 23.62 ± 0.42 in the N group, and 19.46 ± 0.32 in the +D group (P < 0.05). The percentage of CD8(+) lymphocytes was 12.15 ± 0.61 in the -D group, 8.7 ± 0.64 in the N group, and 7.12 ± 0.48 in the +D group (P < 0.05). The CD4(+)/CD8(+) ratio was 2.23 ± 0.15 in the -D group, 2.71 ± 0.21 in the N group, and 2.73 ± 0.31 in the +D group (P < 0.05). The plasma IFN-γ levels were 416.42 ± 16.42 pg/ml in the -D group, 325.41 ± 11.16 pg/ml in the N group, and 276.26 ± 25.32 pg/ml in the +D group (P < 0.005). The plasma IL-10 levels were 16.45 ± 1.58 pg/ml in the -D group, 24.31 ± 2.16 pg/ml in the N group, and 26.28 ± 0.42 pg/ml in the +D group (P < 0.005). The serum TB-PPD-specific antibody level was significantly higher in the -D group than in the N and +D groups. Vitamin D deficiency affects the immunity against Mycobacterium tuberculosis infection in mice.