21 research outputs found

    The Combination of Three Natural Compounds Effectively Prevented Lung Carcinogenesis by Optimal Wound Healing

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    <div><p>The tumor stroma has been described as “normal wound healing gone awry”. We explored whether the restoration of a wound healing-like microenvironment may facilitate tumor healing. Firstly, we screened three natural compounds (shikonin, notoginsenoside R1 and aconitine) from wound healing agents and evaluated the efficacies of wound healing microenvironment for limiting single agent-elicited carcinogenesis and two-stage carcinogenesis. The results showed that three compounds used alone could promote wound healing but had unfavorable efficacy to exert wound healing, and that the combination of three compounds made up treatment disadvantage of a single compound in wound healing and led to optimal wound healing. Although individual treatment with these agents may prevent cancer, they were not effective for the treatment of established tumors. However, combination treatment with these three compounds almost completely prevented urethane-induced lung carcinogenesis and reduced tumor burden. Different from previous studies, we found that urethane-induced lung carcinogenesis was associated with lung injury independent of pulmonary inflammation. LPS-induced pulmonary inflammation did not increase lung carcinogenesis, whereas decreased pulmonary inflammation by macrophage depletion promoted lung carcinogenesis. In addition, urethane damaged wound healing in skin excision wound model, reversed lung carcinogenic efficacy by the combination of three compounds was consistent with skin wound healing. Further, the combination of these three agents reduced the number of lung cancer stem cells (CSCs) by inducing cell differentiation, restoration of gap junction intercellular communication (GJIC) and blockade of the epithelial-to-mesenchymal transition (EMT). Our results suggest that restoration of a wound healing microenvironment represents an effective strategy for cancer prevention.</p></div

    Improvement of the Nitration Process in 2‑Amino-5-chloro-4-methylbenzenesulfonic Acid Synthesis

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    The nitration process as one step in 2-amino-5-chloro-4-methylbenzenesulfonic acid synthesis was improved by optimizing nitration reaction conditions, improving product separation method to eliminate salty scrap acid and cycle use of the concentrated sulfuric acid. The effect of various parameters such as temperature, quality of fuming sulfuric acid, quality of fuming nitric acid, and reaction time was studied for optimization of the nitration reaction condition. In the optimum conditions, the mass ratio of fuming sulfuric acid to sodium 2-chlorotoluene-4-sulfonate and molar ratio of fuming nitric acid to sodium 2-chlorotoluene-4-sulfonate were 4 and 1.05, respectively. The reaction temperature was −5 °C, and the time of reaction was 3 h. By applying the optimum reaction conditions, the yield of nitration reaction was increased to 91%, larger than that of the current industrial process whose yield is only 65.7%. The solubilities of sodium 2-chloro-5-nitrotoluene-4-sulfonate in aqueous sulfuric acid solutions were determined by a dynamic method, and the results showed that the lowest sodium 2-chloro-5-nitrotoluene-4-sulfonate solubility was exhibited in 0.7 mass fraction aqueous sulfuric acid solutions. So the product sodium 2-chloro-5-nitrotoluene-4-sulfonate of nitration reaction was separated by filtration from 0.7 mass fraction aqueous sulfuric acid solutions, and the obtained concentrated aqueous sulfuric acid solution was reused

    Synthesis of Isocoumarins from Cyclic 2‑Diazo-1,3-diketones and Benzoic Acids via Rh(III)-Catalyzed C–H Activation and Esterification

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    A mild and efficient Rh­(III)-catalyzed C–H activation/esterification reaction for the synthesis of isocoumarins has been developed. This procedure uses readily available benzoic acids and cyclic diazo-1,3-diketones as starting materials and involves domino intermolecular C–H activation in combination with intramolecular esterification to give the corresponding isocoumarins in moderate to excellent yields. This process provides a facile approach for the construction of isocoumarins containing various functional groups that does not require any additives

    PEGylated Solanesol for Oral Delivery of Coenzyme Q<sub>10</sub>

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    Coenzyme Q<sub>10</sub> (CoQ<sub>10</sub>) is widely used in preventive or curative treatment of cardiovascular diseases. However, CoQ<sub>10</sub> exhibits an extremely low solubility in aqueous medium as well as a poor oral bioavailability. Therefore, solanesyl poly­(ethylene glycol) succinate (SPGS) and CoQ<sub>10</sub> were formulated as CoQ<sub>10</sub>-SPGS micelles with a high content of CoQ<sub>10</sub> to improve the bioavailability of CoQ<sub>10</sub> in rat. Findings indicate that, in the CoQ<sub>10</sub>-SPGS micelles, SPGS is self-assembled into stable nanosized micelles with a CoQ<sub>10</sub> loading capacity of more than 39%. The CoQ<sub>10</sub>-SPGS micelles exhibit an enhanced photostability upon exposure to simulated sunlight. <i>In vivo</i> experiments demonstrate that, as compared to that of the coarse suspensions of CoQ<sub>10</sub>, there was three-fold enhancement of oral bioavailability for CoQ<sub>10</sub>-loaded SPGS micelles depending on varying molecular weight of SPGS. In the encapsulation of CoQ<sub>10</sub> by SPGS micelles, the self-assembled nanocarriers with strong muco-adhesive properties lead to increases in the solubility and oral absorption of lipophilic CoQ<sub>10</sub> nanoparticles

    The wound healing microenvironment restored GJIC but did not directly decrease tumor cells.

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    <p><b>(</b>A) The combination of three compounds reversed GJIC loss in urethane-treated BEAS-2B cells. Images were taken at ×10 magnification. (B and C) The combination of three compounds led to angiogenesis and optimal fibroblast proliferation but did not directly decrease A549 cancer cells. The results are presented as mean±SE (n = 5/group) **<i>p</i> < 0.01 <i>vs</i> control group.</p

    High Curie Temperature Bi<sub>1.85</sub>Mn<sub>0.15</sub>Te<sub>3</sub> Nanoplates

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    Bi<sub>1.85</sub>Mn<sub>0.15</sub>Te<sub>3</sub> hexagonal nanoplates with a width of ∼200 nm and a thickness of ∼20 nm were synthesized using a solvothermal method. According to the structural characterization and compositional analysis, the Mn<sup>2+</sup> and Mn<sup>3+</sup> ions were found to substitute Bi<sup>3+</sup> ions in the lattice. High-level Mn doping induces significant lattice distortion and decreases the crystal lattice by 1.07% in the <i>a</i> axis and 3.18% in the <i>c</i> axis. A high ferromagnetic state with a Curie temperature of ∼45 K is observed in these nanoplates due to Mn<sup>2+</sup> and Mn<sup>3+</sup> ion doping, which is a significant progress in the field of electronics and spintronics

    View of dose distribution of the hippocampus contoured on CT-MRI fusion.

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    <p>(A) The hippocampus was contoured on axial T1-weighted MRI. (B) Sagittal DRR image showing hippocampus. (C) Non-HPC sparing IMRT plan. (D) HPC sparing IMRT plan. Orange contour  =  hippocampus. Green dose cloud  = 60 Gy. Light green dose cloud  = 50 Gy. Sky-blue dose cloud  = 40 Gy.</p

    The screened three wound healing agents suppressed lung carcinogenesis and their combination led to optimal preventive efficacy.

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    <p>(A) Three wound healing agents were administered to animals following the first carcinogen treatment and were found to prevent lung carcinogenesis. (B) They were administered following the last carcinogen treatment but did not prevent lung carcinogenesis, whereas the combination of these three agents remained effective. (C) Summary data of lung tumor incidence (n = 20). (D) Three wound healing agents restored the lung barrier in urethane-induced lung carcinogenesis. The results are presented as mean±SE (n = 10/group). *<i>p</i> < 0.05, **<i>p</i> < 0.01, vs control group.</p

    Statistical comparison of HPC sparing and non-HPC sparing IMRT plans.

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    <p>Data presented as mean±standard deviation. Two-tailed <i>P</i> values from paired t tests. Abbreviation: PTV =  planning target volume; CI =  conformity index; TC =  target coverage; HI =  homogeneity index.</p

    FeCl<sub>3</sub>‑Catalyzed Four-Component Nucleophilic Addition/Intermolecular Cyclization Yielding Polysubstituted Pyridine Derivatives

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    We report an efficient route to pyridine derivatives via an FeCl<sub>3</sub>-catalyzed four-component nucleophilic addition/intermolecular cyclization. This simple fragment assembly strategy uses mild conditions and affords a broad range of polysubstituted pyridines in moderate to good yield from simple and readily available starting materials. A plausible mechanism for this process is proposed
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