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@#Abstract: In order to search for coumarin-based anti-platelet aggregation compounds with high efficacy and good druggability, twenty-five 3-acetyl-7-hydroxy-coumarin oxime derivatives (6a-6y) were synthesized via Vilsmeier-Haack reaction, Knoevenagel reaction, Williamson reaction, electrophilic substitution reaction and oximation reaction from resorcinol. Their structures were confirmed by HRMS and 1H NMR spectra. The anti-platelet aggregation activity of the target compounds was evaluated using Born’s turbidimetric method. The results revealed that most of them could significantly inhibit platelet aggregation induced by adenosine diphosphate (ADP), collagen, arachidonic acid (AA) and thrombin. Among them, the target compounds 6a and 6b not only had strong inhibitory activity on platelet aggregation induced by the four inducers, but also exhibited good water solubility (3.46 mg/mL and 3.85 mg/mL, respectively) and lipid-water partition coefficient (2.56 and 2.85, respectively) and were expected to become a preclinical candidate compound with multi-target action against platelet aggregation.
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Objective:To investigate the clinical efficacy of a 1 064 nm picosecond laser combined with intense pulsed light in the treatment of melasma.Methods:From May to August 2022, ninety-two female patients with melasma were admitted to the Medical Cosmetology Center, Xi′an International Medical Center Hospital, aged 25-50 years, with an average age of (35.0±3.5) years. The were divided by random number table method. Forty-six cases were divided into laser combined group, which were treated with precise intense pulsed light combined with a 1 064 nm picosecond laser. Forty-six cases in the laser group were treated with a 1 064 nm picosecond laser. The area and severity score of melasma (MASI), VISIA score and clinical efficacy were evaluated.Results:The MASI scores of laser combined group were 12.58 (11.04, 13.99) before treatment, and the MASI scores of laser group were 13.16 (11.47, 14.14) before treatment. The MASI scores of laser combined group were 5.75 (3.79, 7.19), and the MASI scores of laser group were 7.15 (5.42, 5.85) after treatment. The MASI scores of the two groups were decreased compared with those before treatment, and the MASI score of the laser combined group was lower than that of the laser group. The difference was statistically significant ( Z=-4.05, P<0.01). The median VISIA scores of the laser combined group were (173.72±43.77), and the median VISIA scores of the laser group were (175.65±34.9) before treatment. The median VISIA scores of the laser combined group were (135.46±41.63), and the median VISIA scores ofthe laser group were (145.26±33.33) after treatment. The VISIA scores of the two groups were decreased compared with those before treatment. The scores of the laser combined group were lower than those of the laser group. The difference was statistically significant ( t=-2.52, P<0.05). The effective rate of the laser combined group (80.43%, 37/46) was higher than that of the laser group (69.56%, 22/46, P<0.05). Conclusions:The curative effect of 1 064 nm picosecond laser combined with precise intense pulsed light in the treatment of melasma is better than that of a 1 064 nm picosecond laser alone.
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Objective:Evaluation of the efficacy and safety of ultra-picosecond 1 064 nm laser treatment for enlarged facial pores.Methods:From November 2022 to April 2023, 31 female patients with enlarged facial pores, aged between 28 and 52 (35.2±5.5) years old, were treated at the Medical Aesthetics Center of Xi′an International Medical Center Hospital. They received ultra-picosecond 1 064 nm laser fractional handpiece treatment once every 4 weeks for a total of 3 times. One month after the last treatment, facial pore changes were evaluated using facial pore scores and VISIA pore feature count absolute values, and adverse reactions were assessed.Results:All 31 patients completed the treatment. The facial pore scores before and after treatment were 4 (4, 5) and 2 (2, 3), respectively, indicating a statistically significant ( Z=-4.99, P<0.001) decrease in facial pore scores compared to before treatment. The absolute values of VISIA facial pore counts before and after treatment were 859 (829, 1147) and 652 (632, 731), respectively. The absolute value of VISIA pore count after treatment was lower than that before treatment, and the difference was statistically significant ( Z=-4.86, P<0.05 ). Conclusions:Ultra-picosecond laser can effectively improve enlarged facial pores without significant adverse reactions.
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Objective·To investigate the effects of interleukin-1β (IL-1β) on neonatal rat alveolar arrest induced by intra-amniotic injection of lipopolysaccharide (LPS). Methods·A neonatal SD rat model of bronchopulmonary dysplasia (BPD) was constructed by intra-amniotic injection of LPS in pregnant rats. The pregnant rats (E19) were randomly assigned to Saline group, LPS group and LPS+anti-IL-1β group. The lungs of the neonatal rats were randomly collected 1, 3 and 7 days after birth. Pathological changes in the lungs were observed by hematoxylin-eosin (H-E) staining, and expression of IL-1β mRNA and protein was detected by real-time PCR and ELISA, respectively. Rat bone marrow derived primary macrophage was cultured in vitro, and given LPS intervention, then genes related with IL-1β were detected through whole transcriptome sequencing. Results·Compared with the Saline group, the alveolar counts and secondary septa counts significantly decreased, and mean liner intercept significantly increased in LPS group. Moreover, the expression of IL-1β mRNA and protein in lungs significantly increased in LPS group. The LPS-induced pathological changes of lung tissues in neonatal rats were improved by anti-IL-1β. LPS could up-regulate the expression of genes including Gbp5, Ccl3, Nod2, Ccr5, Mefv, Casp4 and Ifnar1, but down-regulate Lgals9 and Gstp1. Among these genes Gbp5, Ccl3, Nod2, Ccr5, Casp4, Ifnar1 and Lgals9 could positively regulate IL-1βproduction. Conclusion·LPS can induce alveolar arrest through up-regulating the expression of IL-1β in macrophages in neonatal rat BPD model. Whole transcriptome sequencing reveals that LPS can regulate the expression of IL-1β in macrophages through several paths.
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Objective To synthesize a photoacoustic contrast agent loaded with gold nanorod and liquid perflurocarbon which was used to observe its photoacoustic imaging in vitro,and then investigate the variation of the photoacoustic signal during and after the vaporization.Methods The PLGA nanoparticle (GNP)loaded with gold nanorod(GNR) and liquid perflurocarbon was synthesized via double emulsion technology.The experiments were divided into three groups:1)GNP group:PLGA nanoparticle loaded with gold nanorod and liquid perflurocarbon; 2) GNR group:gold nanorod ; 3) control group:PLGA nanoparticle unloaded with gold nanorod.A pulsed laser system was used to trigger the three samples.The photoacoustic image and time-signal intensity kinetics were acquired by the photoacoustic microscope.The optical microscope was used to observe the image after the vaporization.Results The gold nanoparticle was successfully prepared,the average size of the gold nanoparticle was 504.9 nm.after triggered by the pulsed laser system,the vaporized image of the GNP group could be observed by the optical microscope.The photoacoustic signal was detected in both GNP and GNR groups,and the signal intensity increased along with the concentration of the GNR.However,the photoacoustic signal of PLGA group was not detected.The photoacoustic signal kinetics of GNP group showed a descending trend from high signal amplitude to steadystate.The GNR group photoacoustic signal kinetics only showed a steady-state signal amplitude.Conclusions The PLGA nanoparticle loaded with gold nanorod and liquid perflurocarbon emerged a phase transient which produces a strong photoacoustic signal after triggered by pulsed laser system.This kind of phenomenon leads the nanoparticle to be a better photoacoustic contrast agent and lays a foundation for in vivo research and photothermal therapy in vivo.
