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1.
Skin Res Technol ; 30(9): e70073, 2024 Sep.
Article de Anglais | MEDLINE | ID: mdl-39324311

RÉSUMÉ

PURPOSE: The study explored the enhanced skin moisturizing capabilities and moisture retention effects achieved by forming a polyion complex using sulfated glycosaminoglycan (GAG), specifically chondroitin sulfate (CS), and amino acids (AA) such as glutamine (Q) and arginine (R). The overall hydration effect of this CS-AA complex was examined. METHODS: After analyzing the CS-AA polyion complex structure using spectroscopic methods, the ex vivo moisture retention ability was assessed under dry conditions using porcine skin samples. Additionally, the efficacy of the CS-AA polyion complex in reducing transepidermal water loss (TEWL) and improving skin hydration was evaluated on human subjects using a digital evaporimeter and a corneometer, respectively. RESULTS: Validating a systematic reduction in particle size, the following order was observed: CS > CS/AA simple mixture > CS-AA complex based on dynamic light scattering (DLS) and transmission electron microscopy (TEM) analysis. Furthermore, observations revealed that the CS-AA complex exhibits negligible surface charge. Additionally, Fourier-transform infrared spectroscopy (FT-IR) analysis demonstrated a distinct peak shift in the complex, confirming the successful formation of the CS-AA complex. Subsequently, the water-holding effect through porcine skin was assessed, revealing a notable improvement in moisture retention (weight loss) for the CS-Q complex: 40.6% (1 h), 20.5% (2 h), and 18.7% (4 h) compared to glycerin. Similarly, the CS-R complex demonstrated enhancements of 50.2% (1 h), 37.5% (2 h), and 33% (4 h) compared to glycerin. Furthermore, TEWL improvement efficacy on human skin demonstrated approximately 25% improvement for both the CS-Q complex and CS-R complex, surpassing the modest 12.5% and 18% improvements witnessed with water and glycerin applications, respectively. Finally, employing a corneometer, hydration changes in the skin were monitored over 4 weeks. Although CS alone exhibited nominal alterations, the CS-Q complex and CS-R complex showed a significant increase in moisture levels after 4 weeks of application. CONCLUSION: In this study, polyion complexes were successfully formed between CS, a sulfated GAG, and AA. Comparisons with glycerin, a well-known moisturizing agent, confirmed that the CS-AA complex exhibits superior moisturizing effects in various aspects. These findings suggest that the CS-AA complex is a more effective ingredient than CS or AA alone in terms of efficacy.


Sujet(s)
Chondroïtines sulfate , Cosmétiques , Perte insensible en eau , Humains , Animaux , Suidae , Perte insensible en eau/effets des médicaments et des substances chimiques , Cosmétiques/pharmacologie , Cosmétiques/composition chimique , Chondroïtines sulfate/composition chimique , Chondroïtines sulfate/pharmacologie , Femelle , Peau/composition chimique , Peau/effets des médicaments et des substances chimiques , Peau/métabolisme , Adulte , Acides aminés/composition chimique , Acides aminés/pharmacologie , Émollient/pharmacologie , Émollient/administration et posologie , Émollient/composition chimique , Polymères/pharmacologie , Polymères/composition chimique , Glutamine/pharmacologie , Polyélectrolytes
2.
Psychiatry Investig ; 21(7): 792-802, 2024 Jul.
Article de Anglais | MEDLINE | ID: mdl-39089705

RÉSUMÉ

OBJECTIVE: Various patient placement criteria (PPC) have been developed to address alcohol use disorder (AUD), which has a high relapse rate and imposes substantial socioeconomic costs. Although research has shown PPC to be an effective tool, evidence supporting the Korean-PPC (K-PPC) is insufficient. This paper investigated whether treatment matching with the K-PPC was effective, based on variables related to AUD. METHODS: In total, 524 participants were evaluated using the 6 dimensions of the K-PPC and levels of care (LoC) were recommended based on the results. Participants whose treatment matched with the recommended LoC were classified into the matched group, and those whose treatment did not match were classified into the mismatched group. Subsequently, treatment was planned according to the determined LoC, and a total of 3 follow-up evaluations were conducted at 1 month, 3 months, and 6 months. RESULTS: There was no significant difference in the follow-up rate between the K-PPC matched group and the mismatched group. Of the variables measured by the 6 dimensions of the K-PPC, alcohol-related variables, depression, insight, and biomedical outcomes showed the most significant results (especially alcohol-related variables) from the baseline evaluation to the 6-month follow-up. In addition, the average adherence to the treatment program in the 6-month period was found to be higher in the matched group than in the mismatched group. CONCLUSION: The K-PPC could be effective for placing patients and providing treatment by matching patient characteristics. Enhancing treatment program retention can also have a positive effect on clinical outcomes.

3.
Small ; : e2404958, 2024 Aug 13.
Article de Anglais | MEDLINE | ID: mdl-39136205

RÉSUMÉ

Organic-inorganic hybrid perovskites have attracted significant attention for optoelectronic applications due to their efficient photoconversion properties. However, grain boundaries and irregular crystal orientations in polycrystalline films remain issues. This study presents a method for producing crystalline-orientation-controlled perovskite single-crystal films using retarded solvent evaporation. It is shown that single-crystal films, grown via inverse temperature crystallization within a confined space, exhibit enhanced optoelectronic property. Using interfacial polymer layer, this method produces high-quality perovskite single-crystalline films with varying crystal orientations. Density functional theory calculations confirm favorable adsorption energies for (110) surfaces with methylammonium iodide and PbI2 terminations on poly(3-hexylthiophene), and stronger adsorption for (224) surfaces with I and methylammonium terminations on polystyrene, influenced by repulsive forces between the thiophene group and the perovskite surface. The correlation between charge transport characteristics and perovskite single-crystalline properties highlights potential advancements in perovskite optoelectronics, improving device performance and reliability.

4.
Sensors (Basel) ; 24(16)2024 Aug 06.
Article de Anglais | MEDLINE | ID: mdl-39204784

RÉSUMÉ

This paper proposes a heuristic association algorithm between access points (APs) and user equipment (UE) in user-centric cell-free massive multiple-input-multiple-output (MIMO) systems, specifically targeting scenarios where UEs share the same frequency and time resources. The proposed algorithm prevents overserving APs and ensures the connectivity of all UEs, even when the number of UEs is significantly greater than the number of APs. Additionally, we assume the use of low-resolution analog-to-digital converters (ADCs) to reduce fronthaul capacity. While realistic massive access scenarios, such as those in Internet-of-Things (IoT) environments, often involve hundreds or thousands of UEs per AP using multiple access techniques to allocate different frequency and time resources, our study focuses on scenarios where UEs within each AP cluster share the same frequency and time resources to highlight the impact of pilot contamination in dense network environments. The proposed algorithm is validated through simulations, confirming that it guarantees the connection of all UEs and prevents overserving APs. Furthermore, we analyze the required fronthaul capacity based on quantization bits and confirm that the proposed algorithm outperforms existing algorithms in terms of SE and average SE performance for UEs.

5.
Materials (Basel) ; 17(16)2024 Aug 20.
Article de Anglais | MEDLINE | ID: mdl-39203308

RÉSUMÉ

This paper presents an optimized design approach using nonlinear dynamic analysis and finite element methods to ensure the structural integrity of square-shaped containers made from ductile cast iron for intermediate- and low-level radioactive waste packaging. Ductile cast iron, with its spherical graphite structure, effectively distributes stress throughout the material, leading to a storage capacity increase of approximately 18%. Considering the critical need for containers that maintain integrity under extreme conditions like earthquakes, the design focuses on mitigating stress concentrations at the corners of square structures. Nonlinear dynamic analyses were conducted in five drop directions: three specified by ASTM-D5276 standards and two additional directions to account for different load patterns. Fractures were observed in four out of the five scenarios. For each direction where fractures occurred, equivalent loads causing similar displacement fields were applied to linear static models, which were then used for multi-load topology optimization. Three optimized models were derived, each increasing the volume by 1.4% to 1.6% compared to the original model, and the design that best met the structural integrity requirements during drop scenarios was selected. To further enhance the optimization process, weights were assigned to different load conditions based on numerical analysis results, balancing the impact of maximum stress, average stress, and plastic deformation energy. The final model, with its increased storage capacity and enhanced structural integrity, offers a practical solution for radioactive waste management, overcoming limitations in previous designs by effectively addressing complex load conditions.

6.
Int J Mol Sci ; 25(14)2024 Jul 21.
Article de Anglais | MEDLINE | ID: mdl-39063213

RÉSUMÉ

Human pluripotent stem cell-derived cardiomyocytes (hPSC-CMs) have emerged as a promising tool for studying cardiac physiology and drug responses. However, their use is largely limited by an immature phenotype and lack of high-throughput analytical methodology. In this study, we developed a high-throughput testing platform utilizing hPSC-CMs to assess the cardiotoxicity and effectiveness of drugs. Following an optimized differentiation and maturation protocol, hPSC-CMs exhibited mature CM morphology, phenotype, and functionality, making them suitable for drug testing applications. We monitored intracellular calcium dynamics using calcium imaging techniques to measure spontaneous calcium oscillations in hPSC-CMs in the presence or absence of test compounds. For the cardiotoxicity test, hPSC-CMs were treated with various compounds, and calcium flux was measured to evaluate their effects on calcium dynamics. We found that cardiotoxic drugs withdrawn due to adverse drug reactions, including encainide, mibefradil, and cetirizine, exhibited toxicity in hPSC-CMs but not in HEK293-hERG cells. Additionally, in the effectiveness test, hPSC-CMs were exposed to ATX-II, a sodium current inducer for mimicking long QT syndrome type 3, followed by exposure to test compounds. The observed changes in calcium dynamics following drug exposure demonstrated the utility of hPSC-CMs as a versatile model system for assessing both cardiotoxicity and drug efficacy. Overall, our findings highlight the potential of hPSC-CMs in advancing drug discovery and development, which offer a physiologically relevant platform for the preclinical screening of novel therapeutics.


Sujet(s)
Différenciation cellulaire , Évaluation préclinique de médicament , Myocytes cardiaques , Cellules souches pluripotentes , Humains , Myocytes cardiaques/effets des médicaments et des substances chimiques , Myocytes cardiaques/métabolisme , Myocytes cardiaques/cytologie , Évaluation préclinique de médicament/méthodes , Différenciation cellulaire/effets des médicaments et des substances chimiques , Cellules souches pluripotentes/effets des médicaments et des substances chimiques , Cellules souches pluripotentes/cytologie , Cellules souches pluripotentes/métabolisme , Agents cardiovasculaires/pharmacologie , Calcium/métabolisme , Cardiotoxicité , Tests de criblage à haut débit/méthodes , Cellules HEK293 , Signalisation calcique/effets des médicaments et des substances chimiques
7.
Bioorg Chem ; 150: 107603, 2024 Sep.
Article de Anglais | MEDLINE | ID: mdl-38968905

RÉSUMÉ

Inhibition of LSD1 was proposed as promising and attractive therapies for treating osteoporosis. Here, we synthesized a series of novel TCP-(MP)-Caffeic acid analogs as potential LSD1 inhibitors to assess their inhibitory effects on osteoclastogenesis by using TRAP-staining assay and try to explore the preliminary SAR. Among them, TCP-MP-CA (11a) demonstrated osteoclastic bone loss both in vitro and in vivo, showing a significant improvement in the in vivo effects compared to the LSD1 inhibitor GSK-LSD1. Additionally, we elucidated a mechanism that 11a and its precursor that 11e directly bind to LSD1/CoREST complex through FAD to inhibit LSD1 demethylation activity and influence its downstream IκB/NF-κB signaling pathway, and thus regulate osteoclastic bone loss. These findings suggested 11a or 11e as potential novel candidates for treating osteoclastic bone loss, and a concept for further development of TCP-(MP)-Caffeic acid analogs for therapeutic use in osteoporosis clinics.


Sujet(s)
Acides caféiques , Ostéoclastes , Ostéoclastes/effets des médicaments et des substances chimiques , Ostéoclastes/métabolisme , Acides caféiques/pharmacologie , Acides caféiques/composition chimique , Acides caféiques/synthèse chimique , Animaux , Relation structure-activité , Souris , Structure moléculaire , Relation dose-effet des médicaments , Découverte de médicament , Humains , Ostéoporose/traitement médicamenteux , Résorption osseuse/traitement médicamenteux , Cellules RAW 264.7 , Antienzymes/pharmacologie , Antienzymes/composition chimique , Antienzymes/synthèse chimique
8.
Opt Express ; 32(9): 16235-16247, 2024 Apr 22.
Article de Anglais | MEDLINE | ID: mdl-38859256

RÉSUMÉ

Radiative cooling is an energy-efficient technology without consuming power. Depending on their use, radiative coolers (RCs) can be designed to be either solar-transparent or solar-opaque, which requires complex spectral characteristics. Our research introduces a novel deep learning-based inverse design methodology for creating thin-film type RCs. Our deep learning algorithm determines the optimal optical constants, material volume ratios, and particle size distributions for oxide/nitride nanoparticle-embedded polyethylene films. It achieves the desired optical properties for both types of RCs through Mie Scattering and effective medium theory. We also assess the optical and thermal performance of each RCs.

9.
Skin Res Technol ; 30(6): e13788, 2024 Jun.
Article de Anglais | MEDLINE | ID: mdl-38881052

RÉSUMÉ

PURPOSE: This study aimed to develop a novel exfoliating material with high efficacy and low irritation by synthesizing the Mandelic acid_Carnitine ion pairing complex (M_C complex) and evaluating its exfoliating properties. Additionally, the study assessed the skin improvement effects of the M_C complex through clinical evaluations. METHODS: The M_C complex was synthesized in a 1:1 molar ratio of Mandelic acid and Carnitine. Structural characterization was performed using dynamic light scattering and Fourier-transform infrared spectroscopy. Exfoliating efficacy was evaluated on porcine skin, and clinical assessments were conducted on human subjects to measure various skin improvement parameters. RESULTS: The formation of the M_C complex was confirmed through particle size analysis, zeta-potential measurements, and FT-IR spectroscopy. The M_C complex demonstrated superior exfoliating efficacy compared to Mandelic acid alone, especially at pH 4.5. Clinical evaluations showed significant improvements in blackheads, whiteheads, pore volume, depth, density, count, and affected area, as well as skin texture. No adverse reactions were observed. CONCLUSION: The M_C complex exhibits high exfoliating efficacy and minimal irritation, making it a promising cosmetic ingredient for improving skin health. These findings support its potential as a low-irritation exfoliating material under mildly acidic conditions, contributing to overall skin health enhancement.


Sujet(s)
Carnitine , Cosmétiques , Acides mandéliques , Acides mandéliques/composition chimique , Acides mandéliques/pharmacologie , Humains , Carnitine/pharmacologie , Carnitine/composition chimique , Animaux , Suidae , Cosmétiques/pharmacologie , Cosmétiques/composition chimique , Femelle , Adulte , Peau/effets des médicaments et des substances chimiques , Peau/composition chimique , Mâle , Adulte d'âge moyen , Spectroscopie infrarouge à transformée de Fourier
10.
Clin Exp Otorhinolaryngol ; 17(3): 226-233, 2024 Aug.
Article de Anglais | MEDLINE | ID: mdl-38898811

RÉSUMÉ

OBJECTIVES: The supine sleep position and the rapid eye movement (REM) stage are widely recognized to exacerbate the severity of obstructive sleep apnea (OSA). Position-dependent OSA is generally characterized by an apnea-hypopnea index (AHI) that is at least twice as high in the supine position compared to other sleep positions. However, this condition can be misdiagnosed if a particular sleep stage-REM or non-REM (NREM)-predominates in a specific position. We explored the impact of the sleep stage on positional dependency in OSA. METHODS: Polysomnographic data were retrospectively analyzed from 111 patients with OSA aged 18 years or older, all of whom had an AHI exceeding five events per hour and slept in both supine and non-supine positions for at least 5% of the total sleep time. The overall ratio of non-supine AHI to supine AHI (NS/S-AHI ratio) was compared between total, REM, and NREM sleep. Additionally, a weighted NS/S-AHI ratio, reflecting the proportion of time spent in each sleep stage, was calculated and compared to the original ratio. RESULTS: The mean NS/S-AHI ratio was consistent between the entire sleep period and the specific sleep stages. However, the NS/S-AHI ratios for individual patients displayed poor agreement between total sleep and the specific stages. Additionally, the weighted NS/S-AHI ratio displayed poor agreement with the original NS/S-AHI ratio, primarily due to discrepancies in patients with mild to moderate OSA. CONCLUSION: The weighted NS/S-AHI ratio may help precisely assess positional dependency.

11.
Materials (Basel) ; 17(7)2024 Mar 22.
Article de Anglais | MEDLINE | ID: mdl-38611981

RÉSUMÉ

This study presents a methodology to prevent the overdesign of electric dispensers for dental impression materials by analyzing the necessary load and determining the appropriate pressurization speed and drive motor capacity. We derived an equation to calculate the required torque and rotational speed of the motor based on the extrusion load and the speed of the impression material. A specialized load measurement system was developed to measure the load necessary to extrude the impression material. Through experiments and image processing, we measured the radius of curvature of the trajectory of the impression material and correlated it with the pressurization speed. Techniques such as position coordinate plotting, curve fitting, and circle fitting were employed to determine the pressurization speed that aligns with the manufacturer's recommended curvature radius. These findings led to a substantial decrease in the necessary motor torque and rotational speed compared with the current standards. This research provides a systematic approach to sizing drive motors using extrusion load and pressurization speed, aiming to reduce overdesign, power consumption, and the weight and size of the motor and battery, thereby contributing to the development of more efficient and compact dental impression material dispensers.

12.
Kidney Res Clin Pract ; 43(1): 101-110, 2024 Jan.
Article de Anglais | MEDLINE | ID: mdl-38311360

RÉSUMÉ

BACKGROUND: The pathophysiological mechanism of cardiovascular disease in patients with chronic kidney disease (CKD) is complicated. Mediation analysis is an important statistical tool for gaining insight into the complex mechanisms of exposure-outcome effects. We investigated the potential mediating role of the left ventricular mass index (LVMI) on the association between fluid balance (overhydration/extracellular water, OH/ECW) and left ventricular diastolic function (E/e´ ratio) in patients with CKD not yet on dialysis. METHODS: Bioimpedance spectroscopy, echocardiography, and laboratory evaluations were performed on 425 consecutive patients on the same day. The patients were classified into two groups according to the estimated glomerular filtration rate corresponding to CKD stages 3 and 5. Mediation analysis was performed using the PROCESS macro and bootstrapping methods. RESULTS: OH/ECW and LVMI were positively correlated with the E/e´ ratio in both the CKD stages 3 and five groups. In CKD stage 5, there was a statistically significant association between OH/ECW and LVMI, whereas no correlation was observed in CKD stage 3. In the mediation analysis, LVMI positively mediated the relationship between OH/ECW and E/e´ ratio when controlling for confounders in patients with CKD stage 5 (B = 2.602; Boot 95% confidence interval, 1.313-4.076). CONCLUSION: In our analysis, the indirect effect of mediators was significant in patients with advanced CKD. Therefore, our study suggests that further research on several other risk factors may be needed to determine the underlying mechanisms of association between the associated factors in all CKD stages.

13.
Plants (Basel) ; 12(21)2023 Nov 01.
Article de Anglais | MEDLINE | ID: mdl-37960101

RÉSUMÉ

12-oxo-phytodienoic acid (OPDA) is a primary precursor of jasmonates, able to trigger autonomous signaling cascades that activate and fine-tune plant defense responses, as well as growth and development. However, its mechanism of actions remains largely elusive. Here we describe a dual-function messenger of OPDA signaling, reduced glutathione (GSH), that cross-regulates photosynthesis machinery and stress protection/adaptation in concert, optimizing plant plasticity and survival potential. Under stress conditions, the rapid induction of OPDA production stimulates GSH accumulation in the chloroplasts, and in turn leads to protein S-glutathionylation in modulating the structure and function of redox-sensitive enzymes such as 2-cysteine (Cys) peroxiredoxin A (2CPA), a recycler in the water-water cycle. GSH exchanges thiol-disulfides with the resolving CysR175, while donating an electron (e-, H+) to the peroxidatic CysP53, of 2CPA, which revives its reductase activity and fosters peroxide detoxification in photosynthesis. The electron flow protects photosynthetic processes (decreased total non-photochemical quenching, NPQ(T)) and maintains its efficiency (increased photosystem II quantum yield, ΦII). On the other hand, GSH also prompts retrograde signaling from the chloroplasts to the nucleus in adjusting OPDA-responsive gene expressions such as Glutathione S-Transferase 6 (GST6) and GST8, and actuating defense responses against various ecological constraints such as salinity, excess oxidants and light, as well as mechanical wounding. We thus propose that OPDA regulates a unique metabolic switch that interfaces light and defense signaling, where it links cellular and environmental cues to a multitude of plant physiological, e.g., growth, development, recovery, and acclimation, processes.

14.
Am J Cancer Res ; 13(9): 4021-4038, 2023.
Article de Anglais | MEDLINE | ID: mdl-37818053

RÉSUMÉ

Glioblastoma multiforme (GBM) is the most aggressive type of brain tumor, with an extremely poor prognosis due to resistance to standard-of-care treatments. Strong evidence suggests that the small population of glioma stem cells (GSCs) contributes to the aggressiveness of GBM. One of the mechanisms that promote GSC progression is the dysregulation of membrane transporters, which mediate the influx and efflux of substances to maintain cellular homeostasis. Here, we investigated the role of multidrug and toxin extrusion transporter gene SLC47A1 in GSCs. Results show that SLC47A1 is highly expressed in GSCs compared to non-stem cell glioma cells, and non-tumor cells. Additionally, in-silico analysis of public datasets showed that high SLC47A1 expression is linked to malignancy and a poor prognosis in glioma patients. Further, SLC47A1 expression is correlated with important biological processes and signaling pathways that support tumor growth. Meanwhile, silencing SLC47A1 by short-hairpin RNA (shRNA) influenced cell viability and self-renewal activity in GSCs. Interestingly, SLC47A1 shRNA knockdown or pharmacological inhibition potentiates the effect of temozolomide (TMZ) in GSC cells. The findings suggest that SLC47A1 could serve as a useful therapeutic target for gliomas.

15.
Plant Sci ; 337: 111895, 2023 Oct 12.
Article de Anglais | MEDLINE | ID: mdl-37838156

RÉSUMÉ

Drought has become the most important limiting factor to crop productions. Research thus far has been devoted to identifying drought-responsive genes (DRGs) via breeding and engineering approaches. Still, these efforts have not resulted in a solution to combat drought's effects because the ectopic expression of most DRGs causes adverse effects that reduce plant growth and yields. Lately, we discovered that two DRGs, Response to Desiccation (RD)29A and RD29B, induced by Paenibacillus polymyxa CR1, a plant growth-promoting rhizobacterium capable of priming drought tolerance and concurrently stimulating plant growth, play pivotal roles in defense responses against drought. In this study, we employ the ChlP and qRT-PCR analyses and further clarify that P. polymyxa CR1 reformats the chromatin/transcriptional memory of RD29s, positioned as upstream controllers that fine-tune the temporal dynamic of stress-regulating transcription factors (TFs) in elaborating induced systemic drought tolerance without growth penalties. Two genes coordinate the upregulation of NAC TFs, while feedback inhibiting CBF TFs, which regulate downstream DRG expressions. This supports that RD29s are unique, feasible transgene candidates for improving plants' survival capacity in both optimal and drought conditions. However, the mode of action of RD29A and RD29B are partly independent, exerting distinct roles in disparate ecological states. When subjected to increasing NaCl concentrations, the KO mutant of RD29A (rd29a) displayed enhanced tolerance compared to WT and rd29b plants, proposing that RD29B, but not RD29A, a key player in conferring WT-like tolerance to salinity stress; further studies will be needed to optimize/maximize their applications in engineering for-profit drought and/or broad-spectrum stress tolerant crops.

16.
Eur J Med Chem ; 260: 115767, 2023 Nov 15.
Article de Anglais | MEDLINE | ID: mdl-37651877

RÉSUMÉ

Abnormal osteoclast differentiation causes various bone disorders such as osteoporosis. Targeting the formation and activation of osteoclasts has been recognized as an effective approach for preventing osteoporosis. Herein, we synthesized eleven 2-NMPA derivatives which are (2-(2-chlorophenoxy)-N-(4-alkoxy-2-morpholinophenyl) acetamides, and evaluated their suppression effects on osteoclastogenesis in vitro by using TRAP-staining assay. Among the synthesized eleven novel 2-NMPAs, 4-(2-(2-chlorophenoxy)acetamido)-3-morpholinophenyl trifluoromethanesulfonate (11b), 4-(2-(2-chlorophenoxy) acetamido)-3-morpholinophenyl-3-(N-(2-oxo-2-((2-(phenylthio) phenyl) amino) ethyl)methylsulfonamido)benzoate (11d), and 4-(2-(2-chlorophenoxy) acetamido)-3-morpholinophenyl 4-acetamidobenzenesulfonate (11h) displayed highly inhibitory bioactivity on the differentiation of primary osteoclasts. 11h was selected for further investigation of the inhibitory effects and potential mechanism involved in the suppression of osteoclastogenesis. In vitro analysis suggested that 11h inhibited osteoclastogenesis with an IC50 of 358.29 nM, decreased the formation of F-action belts and bone resorption, without interfering cell viability and osteoblast differentiation. Furthermore, the mRNA expressions of osteoclast-specific genes such as Acp5, Nfatc1, Dc-stamp, Atp6v0d2, Mmp9, and Ctsk significantly decreased following 11h treatment. RANKL-induced osteoclast-specific proteins analysis demonstrated that 11h suppressed osteoclast differentiation by downregulating of RANKL-mediated TRAF6 expression, followed by inactivation of PI3K/AKT and IκBα/NF-κB signaling pathways. Finally, 11h inhibited ovariectomy-induced bone loss in vivo. Therefore, the current work highlighted the therapeutic potential of 11h as an anti-osteoporosis lead compound.


Sujet(s)
Ostéoporose , Phosphatidylinositol 3-kinases , Femelle , Humains , Ostéoclastes , Ostéogenèse , Ostéoporose/traitement médicamenteux , Ostéoporose/prévention et contrôle
17.
Skin Res Technol ; 29(7): e13406, 2023 Jul.
Article de Anglais | MEDLINE | ID: mdl-37522492

RÉSUMÉ

BACKGROUND: Salicylic acid has been used as an anti-acne agent with its comedolytic property and antimicrobial activity. However, there is a limit to use for leave-on cosmetics because of the transient skin irritation and low efficacy at neutral pH condition. We prepared a salicylic acid-based ionic pair with L -carnitine (we named, IP-BHA) overcoming the limitation of salicylic acid. We examined the effect of IP-BHA as well as the combination effect with magnolol, a bioactive organic lignan, in order to clarify their efficacy as anti-acne agents. METHODS: After verifying the structure of IP-BHA, we confirmed anti-acne activities including the regulation of exfoliation, lipogenesis, bacterial growth, and inflammation with IP-BHA and/or magnolol. RESULTS: The antibacterial activity of IP-BHA and magnolol was evaluated by determining the minimum antibacterial inhibitory concentration. Magnolol showed strong activity against Cutibacterium acnes, which was better than a medical antibiotic acne drug, clindamycin. The combined application with IP-BHA was more effective in antibacterial activity by 2.5 times. It was confirmed that testosterone-induced lipogenesis was significantly inhibited by treatment with IP-BHA and magnolol, while single treatment had no significant inhibitory effect. Interestingly, MMP-1 and VEGF were induced by C. acnes lysate in human keratinocytes. We found that these inflammatory molecules were completely inhibited by combined application of IP-BHA and magnolol. Through ex vivo test, the dose-dependent exfoliation effect of IP-BHA was confirmed at pH 5.5, and the synergic exfoliation effect was shown in the combined application of IP-BHA and magnolol. When topically applied, the emulsion containing IP-BHA and magnolol relieved the sodium dodecyl sulfate-induced erythema and improved inflamed acne with papule and pustule. CONCLUSION: Our data demonstrate that the ionic paired salicylic acid with L -carnitine can overcome the limitations of salicylic acid at low concentration and natural skin pH. Based on the dual administration effects, we suggest that IP-BHA and magnolol may be the potential agent for acne by improving inflammatory skin condition.


Sujet(s)
Acné juvénile , Lignanes , Humains , Carnitine/usage thérapeutique , Lipogenèse , Acné juvénile/traitement médicamenteux , Lignanes/pharmacologie , Lignanes/usage thérapeutique , Acide salicylique/usage thérapeutique , Antibactériens/pharmacologie , Inflammation
18.
Stem Cell Res ; 71: 103167, 2023 09.
Article de Anglais | MEDLINE | ID: mdl-37481965

RÉSUMÉ

A TNFRSF11B (TNF Receptor Superfamily Member 11b) gene encodes a soluble decoy receptor, osteoprotegerin (OPG), which has a key role in repressing osteoclast differentiation. In this report, we generated a biallelic knock-out hiPSC line for the TNFRSF11B gene via CRISPR/Cas9. When TNFRSF11B Knock-out hiPSCs were differentiated into mesenchymal progenitor cells (MPCs), the expression level of OPG was significantly decreased compared to normal hiPSC-derived MPCs. This knock-out hiPSCs will provide a chance to study Paget disease of bone 5 (juvenile Paget disease).


Sujet(s)
Cellules souches pluripotentes induites , Maladie de Paget des os , Humains , Ostéoprotégérine/génétique , Ostéoprotégérine/métabolisme , Cellules souches pluripotentes induites/métabolisme , Systèmes CRISPR-Cas/génétique , Maladie de Paget des os/génétique , Maladie de Paget des os/métabolisme
19.
Sensors (Basel) ; 23(14)2023 Jul 12.
Article de Anglais | MEDLINE | ID: mdl-37514631

RÉSUMÉ

Reconfigurable intelligent surface (RIS) has emerged as a promising technology to enhance the spectral efficiency of wireless communication systems. However, if there are many obstacles between the RIS and users, a single RIS may not provide sufficient performance. For this reason, a double RIS-aided communication system is proposed in this paper. However, this system also has a problem: the signal is attenuated three times due to the three channels created by the double RIS. To overcome these attenuations, an active RIS is proposed in this paper. An active RIS is almost the same as a conventional RIS, except for the included amplifier. Comprehensively, the proposed system overcomes various obstacles and attenuations. In this paper, an active RIS is applied to the second RIS. To reduce the power consumption of active elements, a partially active RIS is applied. To optimize the RIS elements, the sum of the covariance matrix is found by using channels related to each RIS, and the right singular vector is exploited using singular value decomposition for the sum of the covariance matrix. Then, the singular value of the sum of the covariance value is checked to determine which element is the active element. Simulation results show that the proposed system has better sum rate performance compared to a single RIS system. Although it has a lower sum rate performance compared to a double RIS with fully active elements, the proposed system will be more attractive in the future because it has much better energy efficiency.

20.
Int J Mol Sci ; 24(9)2023 May 03.
Article de Anglais | MEDLINE | ID: mdl-37175895

RÉSUMÉ

Biocontrol strategies are gaining tremendous attention in insect pest management, such as controlling termite damage, due to the growing awareness of the irreparable harm caused by the continuous use of synthetic pesticides. This study examines the proteolytic and chitinolytic activities of Bacillus velezensis CE 100 and its termiticidal effect through cuticle degradation. The proteolytic and chitinolytic activities of B. velezensis CE 100 systematically increased with cell growth to the respective peaks of 68.3 and 128.3 units/mL after seven days of inoculation, corresponding with the highest cell growth of 16 × 107 colony-forming units (CFU)/mL. The in vitro termiticidal assay showed that B. velezensis CE 100 caused a rapid and high rate of termite mortality, with a median lethal time (LT50) of >1 h and the highest mortality rates of 91.1% and 92.2% recorded at 11 h and 12 h in the bacterial broth culture and crude enzyme fraction, respectively. In addition to broken setae and deformed sockets, termites treated with the bacterial broth culture exhibited degraded epicuticles, while the crude enzyme fraction caused severe disintegration of both the epicuticle and endocuticle. These results indicate the tremendously higher potential of B. velezensis CE 100 in the biological control of subterranean termites compared to the previously used entomopathogenic bacteria.


Sujet(s)
Bacillus , Isoptera , Animaux , Bacillus/métabolisme , Insectes , République de Corée
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