Enantioselective formal total synthesis of dihydrospirotryprostatin B.

Spirotryprostatins are representative members of medicinally interesting bioactive molecules of the spirooxindole natural products. In this communication, we present a novel enantioselective total synthesis of the spirooxindole alkaloid dihydrospirotryprostatin B. The synthesis takes advantage of copper-catalyzed tandem reaction of o-iodoanilide chiral sulfinamide derivatives with alkynone to rapidly construct the key quaternary carbon stereocenter of the natural product dihydrospirotryprostatin B.

Short pathways to highly active antimicrobial: structurally diverse polyamines derivatives from Amino-Aldehyde condensation strategy.

BACKGROUND: Chemical fungicides are the mainstay of plant disease control in agricultural production, but there are a very limited number of drugs that can effectively control plant diseases. Two series of secondary amine derivatives were synthesized using the diamine skeleton combined with saturated aromatic and aliphatic aldehydes, and their antibacterial and antifungal activities against plant pathogens were determined. In addition, the antimicrobial mechanism of the highly active compound A26 was preliminarily examined against Xanthomonas oryzae (Xoo). RESULTS: Compound A26 exhibited the highest antibacterial potency among all the target compounds, with MIC values of 3.12, 3.12 and 12.5 µg mL-1 against Xoo, Xanthomonas axonopodis pv. Citri and Pseudomonas sollamacearum, respectively. In addition, compound A26 had powerful curative and protective effects against Xoo at 200 µg mL-1 , and was better than the control agent Xinjunan. Preliminary mechanistic studies showed that compound A26 reduced the bacterial pathogenicity by targeting cell membranes and inhibiting the secretion of extracellular polysaccharides. Meanwhile, the toxicity of compound A26 to Human Embryonic Kidney 293 cells and Human Liver-7702 was similar to that of Xinjunan, and it had moderate toxicity according to the World Health Organization classification standard of oral exogenous toxicity, with an LD50 of 245.47 mg kg-1 . CONCLUSION: Secondary amines have efficient and broad-spectrum antibacterial activity against plant pathogenic bacteria and are expected to be a new class of candidate compounds for antibacterial drugs. © 2023 Society of Chemical Industry.

Co-Extraction of Flaxseed Protein and Polysaccharide with a High Emulsifying and Foaming Property: Enrichment through the Sequence Extraction Approach.

A new focus with respect to the extraction of plant protein is that ingredient enrichment should target functionality instead of pursuing purity. Herein, the sequence aqueous extraction method was used to co-enrich five protein-polysaccharide natural fractions from flaxseed meal, and their composition, structure, and functional properties were investigated. The total recovery rate of flaxseed protein obtained by the sequence extraction approach was more than 80%, which was far higher than the existing reports. The defatted flaxseed meal was soaked by deionized water to obtain fraction 1 (supernatant), and the residue was further treated to get fraction 2 (supernatant) and 3 (precipitate) through weak alkali solubilization. Part of the fraction 2 was taken out, followed by adjusting its pH to 4.2. After centrifuging, the albumin-rich supernatant and precipitate with protein content of 73.05% were gained and labeled as fraction 4 and fraction 5. The solubility of fraction 2 and 4 exceeded 90%, and the foaming ability and stability of fraction 5 were 12.76 times and 9.89 times higher than commercial flaxseed protein, respectively. The emulsifying properties of fractions 1, 2, and 5 were all greater than that of commercial sodium caseinate, implying that these fractions could be utilized as high-efficiency emulsifiers. Cryo-SEM results showed that polysaccharides in fractions were beneficial to the formation of network structure and induced the formation of tighter and smoother interfacial layers, which could prevent emulsion flocculation, disproportionation, and coalescence. This study provides a reference to promote the high-value utilization of flaxseed meals.

Room-Temperature Large and Reversible Modulation of Photoluminescence by in Situ Electric Field in Ergodic Relaxor Ferroelectrics.

Ferroelectric oxides with luminescent ions hold great promise in future optoelectronic devices because of their unique photoluminescence and inherent ferroelectric properties. Intriguingly, the photoluminescence performance of ferroelectric ceramics could be modulated by an external electric field. However, researchers face a current challenge of the diminutive extent and degree of reversibility of the field-driven modification that hinder their use in room-temperature practical applications. Within the scope of current contribution in rare-earth-doped bismuth sodium titanate relaxors, the most important information to be noted is the shifting of the depolarization temperature toward room temperature and the resulting considerable enhancement in ergodicity, as evidenced by the dielectric properties, polarization, and strain hysteresis, as well as the in situ Raman/X-ray diffraction studies. After the introduction of 1 mol % Eu, the induced composition and charge disorders disrupt the original long-range ferroelectric macrodomains into randomly dynamic and weakly correlated polar nanoregions, which facilitates a reversible transformation between polar nanoregions and unstable ferroelectric state under an electric field, engendering a large strain. By virtue of this, both the extent and degree of reversibility of photoluminescence modulation are enhanced (∼60%) considerably, and room-temperature in situ tunable photoluminescence response is then achieved under electric field. These should be helpful for the realization of regulating the physical couplings (photoluminescent-ferroelectrics) in multifunctional inorganic ferroelectrics with a high ergodic state by reversibly tuning the structural symmetry.

Hypoxia-inducible factor 1α in breast cancer prognosis.

BACKGROUND: Recent studies have assessed the relationship between hypoxia-inducible factor 1α (HIF-1α) expression and prognosis in breast cancer patients with inconsistent conclusions. To comprehensively and quantitatively summarize the evidence on the survival of patients with breast cancer, a meta-analysis was performed. METHODS: Systematic literature searching was applied to the databases of PubMed, Embase and Web of science until April 1, 2013. Pooled HR with 95% CI was used to evaluate the association between HIF-1α expression and survival in breast cancer patients. RESULTS: Fourteen papers including 2933 patients were subjected to the final analysis. Of these, 7 provided data on overall survival (OS), 8 on disease-free survival (DFS), 3 on distant metastasis-free survival (DMFS) and 3 on relapse-free survival (RFS). We observed that high expression of HIF-1α in breast cancer patients was an indicator of poor prognosis on OS (HR = 1.46, 95% CI: 1.12-1.92, P = 0.006), DFS (HR = 1.91, 95% CI: 1.43-2.57, P<0.001), DMFS (HR=2.17 95% CI: 1.16-4.05, P=0.015) and RFS (HR=1.33 95% CI: 1.09-1.61, P=0.005). Significant heterogeneity was observed in the analyses of OS and DFS. Subgroup analyses by the cut-off value and antibody for IHC were conducted. CONCLUSION: High expression of HIF-1α indicated a poor prognosis for patients with breast cancer.

The value of spatiotemporal image correlation technique in the diagnosis of fetal ventricular septal defect.

OBJECTIVE: To investigate the value of spatiotemporal image correlation (STIC) technique in the ventricular septal defect diagnosis. METHODS: A total of 1,163 fetuses were enrolled in this study, diagnosed by fetal echocardiography and analyzed by STIC technique. We obtained effective STIC volumes from the fetus according to the Goncalves' report, and judged fetal cardiac structure from STIC volume information again with a double-blind method. Another echocardiography was obtained during neonatal or infant period as follow-up. RESULTS: (1) As much as 1,062 cases were diagnosed to have normal fetal heart by fetal echocardiography, 43 cases had congenital heart disease without VSD, and 58 cases had VSD [21 cases (36.2%) were simple VSD and 37 cases (63.8%)were VSD with other heart malformation]. (2) Three fetal VSD cases (0.26%) were missed and one normal case was diagnosed as VSD after two-dimensional (2D) echocardiography. STIC technique corrected the diagnosis for two cases: one case of VSD after fetal 2D echocardiography was confirmed to be normal with STIC and neonatal heart examination; one case that was diagnosed as normal by fetal 2D echocardiography was confirmed to have VSD with STIC and neonatal heart examination. CONCLUSIONS: The special value of STIC technique in the diagnosis of VSD had been confirmed by this study, and it had been proved as the best additional method to fetal echocardiography.

Thermal reactive hazards of HMX with contaminants.

In the past, many unexpected runaway accidents occurred in manufacturing processes, involving volatile chemical and explosive storage and transportation. Incompatible product reactions of high explosives must be carefully considered using loss prevention strategies for thermal hazards risk analysis. High explosive reactions vary via environmental changes, contact materials, or process situations, such as onset temperature and shifts in reaction type when high explosives are in contact with contaminants. Therefore, the manufacture and handling of high explosives require the utmost in safety and loss prevention. HMX (cyclotetramethyene tetranitramine) is one kind of high explosive widely used around the world which is stable with high detonation strength properties. In this study, the influences of contaminants on HMX are investigated. The studied contaminants include ferrous chloride tetrahydrate, ferric chloride hexahydrate, acetone solution, acetic acid, and nitric acid. DSC thermal curves and incompatible reaction kinetic evaluations were preformed using iron, chlorine and acid. Organic acetone solution has lesser effects on HMX. Hopefully, this study will lead to improved thermal hazards risk analysis and reduce accidents.