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2.
Chem Commun (Camb) ; 60(52): 6679-6682, 2024 Jun 25.
Artículo en Inglés | MEDLINE | ID: mdl-38860866

RESUMEN

Two complementary regiodivergent C-H alkynylations of 2-arylthiazoles are reported. When RuII catalysis is employed, an aryl ortho-alkynylation process is favored. The alkynylated products are gained in good yields. With the use of PdII catalysis, a thiazole C5-alkynylation process is developed, allowing for the construction of C5-alkynylated products. This strategy not only expands the methods for the functionalization of 2-arylthiazoles, but also provides new opportunities for the rapid assembly of complex molecular structures, which may have great potential in organic synthesis, medicinal chemistry, and materials science.

3.
NPJ Sci Food ; 8(1): 37, 2024 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-38902297

RESUMEN

Bitter gourd has numerous health-promoting effects on the human body. However, its use has been greatly limited due to its poor acceptance by consumers, resulting from its strong bitterness. This study investigated the effects of five wall materials, namely, soybean protein isolate, gum arabic, maltodextrin, resistant starch, and a soybean lecithin calcium caseinate mixture, on the physicochemical properties of spray-dried bitter gourd powders. The results showed that all five wall materials reduced the moisture content, water activity, browning degree, agglomeration, and bitterness of the spray-dried bitter gourd powder. Maltodextrin was found to be the most effective at reducing water activity, while soybean protein isolate was best at protecting the colour, and the soybean lecithin calcium caseinate mixture was best at reducing hygroscopicity and masking bitterness. Additionally, all five wall materials improved the preservation of flavonoids, saponins, and vitamin C, with soybean protein isolate being the most effective in improving the total flavonoid retention ratio and the soybean lecithin calcium caseinate mixture being the best in improving the retention ratios of total saponins and vitamin C. The spray-dried bitter gourd powder prepared with soybean protein isolate had the highest antioxidant activity and α-glucosidase inhibitory activity. These results are significant for understanding the relationship between wall materials and the physicochemical properties of spray-dried powder. Additionally, these materials provide bitter gourd product manufacturers with useful guidance for producing high-quality products. Furthermore, the results could provide useful insights for processing fruits with similar product characteristics, thus contributing to the enrichment of food processing knowledge.

4.
J Hazard Mater ; 475: 134774, 2024 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-38870850

RESUMEN

Currently, the low cost and effective purification toward heavy metal ions in wastewater has garnered global attention. Herein, we used hydrothermal method to prepare highly dispersed calcium silicate hydrate in fluorite tailings. And the stacking thickness of calcium silicate hydrate layered morphology was less than 5 nm. For high concentration Cu2+ purification investigation in wastewater, we found that the equilibrium adsorption capacity reached 797.92 mg/g via the CSH with 3:2 Ca/Si molar ratio, be 1.43-21.8 times than that of reported data. Therein, the metal-metal exchange and deposition are the primary pathways for Cu2+ adsorption, and electrostatic attraction is the secondary pathway. And the relative ∼100 % removal rate of high-concentration Ni2+ and Cr3+ ions were confirmed via CSH prepared from different tailings. This method offers a cost-effective way to utilize tailings for preparing highly efficient adsorbents toward HMIs removal in wastewater.

5.
Food Chem ; 454: 139805, 2024 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-38810442

RESUMEN

The poor thermal stability and ion tolerance of whey protein hydrolysates (WPH) restrict its application in emulsions, while glycosylation shows potential benefits in improving WPH stability. However, the relationship between saccharides with different Mw and the glycosylation behavior of WPH rich in short peptides is unclear. In response, the effect of different saccharides on glycosylated WPH rich in short peptides and its emulsion stability were investigated. Grafted small Mw saccharides were more beneficial to the emulsion stability of WPH. Specifically, grafting xylose effectively inhibited 121 °C sterilization and 5 mM CaCl2-induced coalescence of WPH emulsion (687.50 nm) by comprehensively enhancing steric hindrance, conformational flexibility and electrostatic repulsion, and dissociating large aggregates into small aggregates. Conversely, grafting maltodextrin (30,590 Da) reduced thermal stability of WPH emulsion (4791.80 nm) by steric shielding and bridging flocculation. These findings provide new sights into glycosylation mechanism for WPH and achieving its application in nutritional emulsions.


Asunto(s)
Calcio , Emulsiones , Calor , Hidrolisados de Proteína , Proteína de Suero de Leche , Proteína de Suero de Leche/química , Emulsiones/química , Glicosilación , Hidrolisados de Proteína/química , Calcio/química , Tamaño de la Partícula
6.
Front Endocrinol (Lausanne) ; 15: 1393251, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38752180

RESUMEN

Objective: Research data suggests that ultrasound-assisted wound debridement (UAWD) can effectively promote the healing of diabetic foot ulcers (DFU). However, existing research is not consistent with this viewpoint. Therefore, we conducted this study to investigate the effect of UAWD on the healing of diabetic foot ulcers. Methods: From the establishment of the database to January 2024, we searched 8 databases to study the effectiveness and safety of UAWD in the treatment of DFU. Two authors independently screened the qualifications of the articles, while two authors extracted relevant data. Statistical analysis was conducted using Review Manager 5.4 and STATA 18.0 software. Results: A total of 11 randomized controlled studies were included, with 6 countries and 696 participants participating. Our findings showed that UAWD was associated with a significant benefit in healing rate (OR = 2.60, 95% CI: [1.67, 4.03], P < 0.0001, I2 = 25%), wound healing time (MD = -11.94, 95% CI: [-23.65, -0.23], P = 0.05, I2 = 99%), percentage reduction in wound size (MD = 14.2, 95% CI: [10.8, 17.6], P = 0.47, I2 = 32%), effectiveness of treatment (OR = 10.3, 95% CI: [4.68, 22.66], P < 0.00001, I2 = 0%). Moreover, UAWD did not cause any significant adverse reactions. However, there was no obvious difference in wound blood perfusion (MD = 0.25, 95% CI: [-0.01, 0.52], P = 0.06, I2 = 90%), transcutaneous oxygen partial pressure (MD = 14.34, 95% CI: [-10.03, 38.71], P = 0.25, I2 = 98%). Conclusion: UAWD can significantly improve wound healing rate, shorten wound healing time, accelerate wound area reduction, and improve clinical treatment effectiveness without significant adverse reactions. Although there is no significant difference in transcutaneous oxygen pressure and wound blood flow perfusion between UAWD and SWC. So we look forward to more scientifically blinded, placebo-controlled, high-quality studies in the future, to enable researchers to obtain more complete and accurate analytical data, in order to improve the scientific and credibility of the evidence. Systematic review registration: https://www.crd.york.ac.uk/prospero/, identifier CRD42024501198.


Asunto(s)
Desbridamiento , Pie Diabético , Ensayos Clínicos Controlados Aleatorios como Asunto , Terapia por Ultrasonido , Cicatrización de Heridas , Pie Diabético/terapia , Humanos , Desbridamiento/métodos , Terapia por Ultrasonido/métodos , Resultado del Tratamiento
7.
Foods ; 13(9)2024 Apr 23.
Artículo en Inglés | MEDLINE | ID: mdl-38731660

RESUMEN

Oil bodies (OBs) are naturally occurring pre-emulsified oil droplets that have broad application prospects in emulsions and gels. The main purpose of this research was to examine the impact of the OB content on the structure and functional aspects of acid-mediated soy protein isolate (SPI) gel filled with OBs. The results indicated that the peanut oil body (POBs) content significantly affected the water holding capacity of the gel. The rheological and textural analyses showed that POBs reduced the gel strength and hardness. The scanning electron and confocal laser scanning microscopy analyses revealed that POBs aggregated during gel formation and reduced the gel network density. The Fourier transform infrared spectrum (FTIR) analysis demonstrated that POBs participated in protein gels through hydrogen bonds, steric hindrance and hydrophobic interactions. Therefore, OBs served as inactive filler in the acid-mediated protein gel, replaced traditional oils and provided alternative ingredients for the development of new emulsion-filled gels.

8.
World J Clin Cases ; 12(11): 1990-1995, 2024 Apr 16.
Artículo en Inglés | MEDLINE | ID: mdl-38660553

RESUMEN

BACKGROUND: When an anorectal foreign body is found, its composition and shape should be evaluated, and a timely and effective treatment plan should be developed based on the patient's symptoms to avoid serious complications such as intestinal perforation caused by displacement of the foreign body. CASE SUMMARY: A 54-year-old male was admitted to our outpatient clinic on June 3, 2023, due to a rectal foreign body that had been embedded for more than 24 h. The patient reported using a glass electrode tube to assist in the recovery of prolapsed hemorrhoids, however, the electrode tube was inadvertently inserted into the anus and could not be removed by the patient. During hospitalization, the patient underwent surgery, and the foreign body was dragged into the rectum with the aid of colonoscopy. The anus was dilated with a comb-type pulling hook and an anal fistula pulling hook to widen the anus and remove the foreign body, and the local anal symptoms were then relieved with topical drugs. The patient was allowed to eat and drink, and an entire abdominal Computed tomography (CT) and colonoscopy were reviewed 3 d after surgery. CT revealed no foreign body residue and colonoscopy showed no metal or other residues in the colon and rectum, and no apparent intestinal tract damage. CONCLUSION: The timeliness and rationality of the surgical and therapeutic options for this patient were based on a literature review of the clinical signs and conceivable conditions in such cases. The type, material and the potential risks of rectal foreign bodies should be considered.

9.
Aging (Albany NY) ; 16(8): 6757-6772, 2024 Mar 28.
Artículo en Inglés | MEDLINE | ID: mdl-38656882

RESUMEN

USP15, a pivotal member of the deubiquitinase family, plays a crucial role in orchestrating numerous vital biological processes, including the regulation of NF-κB signaling pathway and deubiquitination of proto-oncogenes. In various cancers, USP15 has been validated to exhibit up-regulated expression, impacting the initiation and progression of cancer. However, its precise mechanism in bladder cancer remains elusive. Our study shed light on the significant overexpression of USP15 in bladder cancer cells compared to normal bladder cells, correlating with a poorer prognosis for bladder cancer patients. Strikingly, attenuation of USP15 expression greatly attenuated the proliferation, migration, and invasion of bladder cancer cells. Moreover, upregulation of USP15 was found to drive cancer progression through the activation of the NF-κB signaling pathway. Notably, USP15 directly deubiquitinates BRCC3, heightening its expression level, and subsequent overexpression of BRCC3 counteracted the antitumoral efficacy of USP15 downregulation. Overall, our findings elucidated the carcinogenic effects of USP15 in bladder cancer, primarily mediated by the excessive activation of the NF-κB signaling pathway, thereby promoting tumor development. These results underscore the potential of USP15 as a promising therapeutic target for bladder cancer in the future.


Asunto(s)
FN-kappa B , Transducción de Señal , Proteasas Ubiquitina-Específicas , Neoplasias de la Vejiga Urinaria , Animales , Humanos , Línea Celular Tumoral , Movimiento Celular/genética , Proliferación Celular , Progresión de la Enfermedad , Regulación Neoplásica de la Expresión Génica , FN-kappa B/metabolismo , Proteasas Ubiquitina-Específicas/metabolismo , Proteasas Ubiquitina-Específicas/genética , Ubiquitinación , Neoplasias de la Vejiga Urinaria/metabolismo , Neoplasias de la Vejiga Urinaria/patología , Neoplasias de la Vejiga Urinaria/genética
10.
Int J Surg ; 110(5): 2679-2691, 2024 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-38489548

RESUMEN

AIMS: Chemotherapy resistance is an important cause of neoadjuvant therapy failure in pancreatic ductal adenocarcinoma (PDAC). BiTP (anti-PD-L1/TGF-ß bispecific antibody) is a single antibody that can simultaneously and dually target transforming growth factor-beta (TGF-ß) and programmed cell death ligand 1 (PD-L1). We attempted in this study to investigate the efficacy of BiTP in combination with first-line chemotherapy in PDAC. METHODS: Preclinical assessments of BiTP plus gemcitabine and nab-paclitaxel were completed through a resectable KPC mouse model (C57BL/6J). Spectral flow cytometry, tissue section staining, enzyme-linked immunosorbent assays, Counting Kit-8, transwell, and Western blot assays were used to investigate the synergistic effects. RESULTS: BiTP combinatorial chemotherapy in neoadjuvant settings significantly downstaged PDAC tumors, enhanced survival, and had a higher resectability for mice with PDAC. BiTP was high affinity binding to targets and reverse chemotherapy resistance of PDAC cells. The combination overcame immune evasion through reprogramming tumor microenvironment via increasing penetration and function of T cells, natural killer cells, and dendritic cells and decreasing the function of immunosuppression-related cells as regulatory T cells, M2 macrophages, myeloid-derived suppressor cells, and cancer-associated fibroblasts. CONCLUSION: Our results suggest that the BiTP combinatorial chemotherapy is a promising neoadjuvant therapy for PDAC.


Asunto(s)
Carcinoma Ductal Pancreático , Desoxicitidina , Gemcitabina , Ratones Endogámicos C57BL , Terapia Neoadyuvante , Paclitaxel , Neoplasias Pancreáticas , Factor de Crecimiento Transformador beta , Animales , Carcinoma Ductal Pancreático/tratamiento farmacológico , Carcinoma Ductal Pancreático/inmunología , Carcinoma Ductal Pancreático/terapia , Terapia Neoadyuvante/métodos , Ratones , Neoplasias Pancreáticas/tratamiento farmacológico , Neoplasias Pancreáticas/inmunología , Neoplasias Pancreáticas/terapia , Desoxicitidina/análogos & derivados , Desoxicitidina/farmacología , Desoxicitidina/administración & dosificación , Factor de Crecimiento Transformador beta/metabolismo , Factor de Crecimiento Transformador beta/antagonistas & inhibidores , Paclitaxel/farmacología , Paclitaxel/administración & dosificación , Antígeno B7-H1/antagonistas & inhibidores , Antígeno B7-H1/inmunología , Anticuerpos Biespecíficos/farmacología , Anticuerpos Biespecíficos/administración & dosificación , Modelos Animales de Enfermedad , Albúminas/farmacología , Albúminas/administración & dosificación , Humanos , Protocolos de Quimioterapia Combinada Antineoplásica/farmacología , Microambiente Tumoral/efectos de los fármacos , Microambiente Tumoral/inmunología , Sinergismo Farmacológico , Línea Celular Tumoral
11.
Carbohydr Polym ; 334: 122039, 2024 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-38553236

RESUMEN

Biological processes, such as bone defects healing are precisely controlled in both time and space. This spatiotemporal characteristic inspires novel therapeutic strategies. The sustained-release systems including hydrogels are commonly utilized in the treatment of bone defect; however, traditional hydrogels often release drugs at a consistent rate, lacking temporal precision. In this study, a hybrid hydrogel has been developed by using sodium alginate, sucrose acetate isobutyrate, and electrospray microspheres as the base materials, and designed with ultrasound response, and on-demand release properties. Sucrose acetate isobutyrate was added to the hybrid hydrogel to prevent burst release. The network structure of the hybrid hydrogel is formed by the interconnection of Ca2+ with the carboxyl groups of sodium alginate. Notably, when the hybrid hydrogel is exposed to ultrasound, the ionic bond can be broken to promote drug release; when ultrasound is turned off, the release returned to a low-release state. This hybrid hydrogel reveals not only injectability, degradability, and good mechanical properties but also shows multiple responses to ultrasound. And it has good biocompatibility and promotes osteogenesis efficiency in vivo. Thus, this hybrid hydrogel provides a promising therapeutic strategy for the treatment of bone defects.


Asunto(s)
Alginatos , Sistemas de Liberación de Medicamentos , Microesferas , Alginatos/química , Regeneración Ósea , Osteogénesis , Hidrogeles/química
12.
IEEE Trans Image Process ; 33: 1285-1298, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38319769

RESUMEN

Food computing brings various perspectives to computer vision like vision-based food analysis for nutrition and health. As a fundamental task in food computing, food detection needs Zero-Shot Detection (ZSD) on novel unseen food objects to support real-world scenarios, such as intelligent kitchens and smart restaurants. Therefore, we first benchmark the task of Zero-Shot Food Detection (ZSFD) by introducing FOWA dataset with rich attribute annotations. Unlike ZSD, fine-grained problems in ZSFD like inter-class similarity make synthesized features inseparable. The complexity of food semantic attributes further makes it more difficult for current ZSD methods to distinguish various food categories. To address these problems, we propose a novel framework ZSFDet to tackle fine-grained problems by exploiting the interaction between complex attributes. Specifically, we model the correlation between food categories and attributes in ZSFDet by multi-source graphs to provide prior knowledge for distinguishing fine-grained features. Within ZSFDet, Knowledge-Enhanced Feature Synthesizer (KEFS) learns knowledge representation from multiple sources (e.g., ingredients correlation from knowledge graph) via the multi-source graph fusion. Conditioned on the fusion of semantic knowledge representation, the region feature diffusion model in KEFS can generate fine-grained features for training the effective zero-shot detector. Extensive evaluations demonstrate the superior performance of our method ZSFDet on FOWA and the widely-used food dataset UECFOOD-256, with significant improvements by 1.8% and 3.7% ZSD mAP compared with the strong baseline RRFS. Further experiments on PASCAL VOC and MS COCO prove that enhancement of the semantic knowledge can also improve the performance on general ZSD. Code and dataset are available at https://github.com/LanceZPF/KEFS.


Asunto(s)
Benchmarking , Aprendizaje , Semántica
13.
Cell Biochem Biophys ; 82(1): 271-278, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38214811

RESUMEN

Diallyl disulfide (DADS) is effective at suppressing tumour cell growth and proliferation. This study verified the morphology and growth activity of MDCC-MSB-1 cells by using an MTT assay to detect the effect of DADS on the proliferation of MDCC-MSB-1 cells and a CCK8 assay to detect the effect of DADS on the viability and proliferation of MDCC-MSB-1 cells. We found that the viability and proliferation of MDCC-MSB-1 cells decreased with increasing DADS concentrations. MDC staining and Western blotting were used to analyse autophagy, the associated protein LC3 and the MEK/ERK pathway proteins MEK and ERK and to investigate changes in cellular autophagy based on cell morphology and molecular biology. With increasing concentrations of DADS, MDCC-MSB-1 cell autophagy increased in a gradient manner. Additionally, the conversion of the autophagy marker protein LC3-I increased with increasing drug concentrations, and the relative expression of LC3-II steadily increased, as did the expression of key protein components of the MEK/ERK signalling pathway, including P-MEK1/2 and P-ERK1/2. These results suggest that DADS induces autophagy through the MEK/ERK pathway, thereby inhibiting the proliferation of MDCC-MSB-1 cells.


Asunto(s)
Ácido 4-Acetamido-4'-isotiocianatostilbeno-2,2'-disulfónico/análogos & derivados , Compuestos Alílicos , Disulfuros , Sistema de Señalización de MAP Quinasas , Línea Celular Tumoral , Disulfuros/farmacología , Autofagia , Proliferación Celular , Quinasas de Proteína Quinasa Activadas por Mitógenos , Apoptosis
14.
J Hazard Mater ; 465: 133402, 2024 Mar 05.
Artículo en Inglés | MEDLINE | ID: mdl-38183937

RESUMEN

Soils contaminated by per- and polyfluoroalkyl substances (PFAS) present a significant threat to both ecological and human health. Extensive research efforts are currently underway to develop effective strategies for immobilizing these chemicals in soils. In this study, calcium montmorillonite was modified with cetylpyridinium chloride (CPC-CM) to enhance its electrostatic and hydrophobic interactions with PFAS. CPC-CM exhibited high adsorption for perfluorooctanoate acid (PFOA), perfluorooctane sulfonate (PFOS) and 8:2 fluorotelomer sulfonic acids (8:2 FTSA) across initial concentrations of 50-1000 µg/L, outperforming both the parent CM and L-carnitine modified CM. Soil leaching tests demonstrated the superior immobilization capabilities of the CPC-CM, maintaining an average PFAS leaching rate below 7% after 120-day incubation. In the context of human exposure scenarios, the in vitro bioaccessibility and in vivo bioavailability of PFAS in soils were measured by gastrointestinal extraction and mouse assay. CPC-CM treatment effectively reduced the bioaccessibility (by up to 84%) and bioavailability (by up to 76%) of PFAS in soils. Furthermore, the safety and efficacy of CPC-CM were evaluated using enteric microorganisms of mice. CPC-CM treatment mitigated PFAS-induced changes in the abundance of Bacteroidetes and Firmicutes, thereby reducing PFAS-induced health risks for humans. Overall, CPC-CM synthesized in this study demonstrated superior adsorption performance and application safety, offering a highly promising approach for remediating PFAS-contaminated soil.


Asunto(s)
Ácidos Alcanesulfónicos , Fluorocarburos , Humanos , Animales , Ratones , Arcilla , Cetilpiridinio , Suelo/química , Bentonita , Disponibilidad Biológica
15.
Environ Res ; 244: 117898, 2024 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-38092242

RESUMEN

Sorption by soil is the fundamental basis for environment fate of hydrophobic organic contaminants (HOCs), which varies significantly depending on diverse properties of soils. Therefore, a generalized approach to predict HOC sorption by soils is required. In this study, 488 data points were extracted from references and adopted to develop models for estimating the sorption capacities of phenanthrene in soils using six different machine learning (ML) approaches. The extreme gradient boosting (XGBT) model demonstrated the most favorable performance, achieving a coefficient of determination of 0.91 and root-mean-square errors of 0.24 for the testing dataset. The XGBT model's performance was further demonstrated by comparing with experimental data from batch sorption tests conducted on 20 soil samples collected from 17 provinces of China. The differences between the predicted values and the experimental values were statistically equal to zero (p = 0.14). Leveraging the XBGT model together with soil properties from the Harmonized World Soil Database, the distribution of sorption capacities in Chinese soils was successfully depicted on a national scale. This research is expected to contribute to a deeper understanding of the migration of persistent organic pollutants in terrestrial system. Furthermore, the established model holds implications for more precise and scientific soil environmental management.


Asunto(s)
Fenantrenos , Contaminantes del Suelo , Suelo , Adsorción , Contaminantes del Suelo/análisis , Interacciones Hidrofóbicas e Hidrofílicas , Fenantrenos/química
16.
J Colloid Interface Sci ; 657: 705-715, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38071819

RESUMEN

Alkaline electrochemical water splitting has been considered as an efficient way for the green hydrogen production in industry, where the electrocatalysts play the critical role for the electricity-to-fuel conversion efficiency. Phosphate salts are widely used as additives in the fabrication of electrocatalysts with improved activity, but their roles on the electrocatalytic performance have not been fully understood. Herein, we fabricate Co, Fe dual-metal incorporated Ni hydroxide on Ni foam using NaH2PO4 ((Co, Fe)NiOxHy-pi) and NaH2PO2 ((Co, Fe)NiOxHy-hp) as additive, respectively. We find that (Co, Fe)NiOxHy-hp with NaH2PO2 in the fabrication shows high activity and stability for both HER and OER (a overpotential of -0.629 V and 0.65 V at 400 mA cm-2 for HER and OER, respectively). Further experiment reveals that the reconstructed structures of electrocatalyst by using NaH2PO2 (hp) endow high electrocatalytic performances: (1) in-situ generated active metal improves the accumulation, transportation and activity of hydrogen species in the HER process; and (2) in-situ generated poor-crystalline hydroxide endows superior charge/mass transportation and kinetics improvements in the OER process. Our study may provide an insightful understanding on the catalytic performance of non-precious metal electrocatalysts by controlling additives and guidance for the design and synthesis of novel electrocatalysts.

17.
Naunyn Schmiedebergs Arch Pharmacol ; 397(4): 2083-2103, 2024 04.
Artículo en Inglés | MEDLINE | ID: mdl-37870581

RESUMEN

Constipation is a prevalent clinical ailment of the gastrointestinal system, yet its pathogenesis remains ambiguous. Despite the availability of numerous treatment modalities, they are insufficient in resolving the issue for patients. This work conducted a comprehensive review of the existing literature pertaining to the utilization of natural products for the treatment of constipation, with a focus on the efficacy of natural products in treating constipation, and to provide a comprehensive summary of their underlying mechanisms of action. Upon conducting a thorough review of the extant literature, we found that natural products can effectively treat constipation as modern synthetic drugs and compounded drugs with acetylcholinesterase (AChE) effects, rich in fiber and mucus, and the effects of increasing the tension of the ileum and gastrointestinal tract muscle, mediating signaling pathways, cytokine, excitability of the smooth muscle of the gastrointestinal tract, and regulating the homeostasis of intestinal flora. However, there is a wide variety of natural products, and there are still relatively few studies; the composition of natural products is complex, and the mechanism of action of natural products cannot be clarified. In the future, we need to further improve the detailed mechanism of natural products for the treatment of constipation.


Asunto(s)
Productos Biológicos , Microbioma Gastrointestinal , Humanos , Acetilcolinesterasa , Productos Biológicos/uso terapéutico , Estreñimiento/tratamiento farmacológico , Estreñimiento/etiología , Íleon
18.
J Biol Inorg Chem ; 29(1): 87-99, 2024 02.
Artículo en Inglés | MEDLINE | ID: mdl-38141090

RESUMEN

Six aroylhydrazone di-m-chlorobenzyltin complexes {[X-C6H4(O)C=N-N=C(Me)COO](MeOH)(m-Cl-C6H4CH2)2Sn}2 (X = p-Me- (1), p-MeO- (2), p-t-Bu- (3), p-NO2- (4), p-OH- (5) or o-OH- (6)) were synthesized and characterized by HRMS (high-resolution mass spectrometry), NMR (nuclear magnetic resonance spectroscopy), IR (Fourier transform infrared spectroscopy), and TGA (thermogravimetric analysis) techniques. The molecular structure of complexes 1-6 was confirmed by single-crystal X-ray crystallography. The structure of complexes showed a distorted pentagonal bipyramidal configuration around the tin atom center, and the ligands adopted a tridentate chelating mode. Fascinatingly, either one-dimensional infinite chain structures or two-dimensional network structures were observed in the complexes through hydrogen bonds. Complex 2 has the strongest inhibitory effect on MCF7 and HepG2 cell proliferation, its effect was superior to that of the positive control drug cisplatin. The interaction of ct-DNA (calf-thymus DNA) with complex 2 was explored using UV absorption (ultraviolet absorption) and fluorescence spectroscopy. Complex 2 exhibited a moderate affinity for ct-DNA through intercalation modes. The interaction of complex 2 with ct-DNA has also been supported by molecular docking studies.


Asunto(s)
Complejos de Coordinación , ADN , Hidróxidos , Simulación del Acoplamiento Molecular , Estructura Molecular , Espectroscopía de Resonancia Magnética , ADN/química , Cristalografía por Rayos X , Complejos de Coordinación/química , Ligandos
19.
Food Sci Nutr ; 11(12): 7626-7637, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-38107145

RESUMEN

The antidiabetic activity of saponins extracted from Momordica charantia (MCS) on streptozotocin-induced diabetic mice was investigated in order to elucidate the mechanism of MCS for exerting hypoglycemic effects. Saponins were first extracted from M. charantia L. and their composition was analyzed. The diabetic Kunming mice were fed low-dose saponins from M. charantia L. and high-dose MCS, using normal mice and diabetic mice as controls. Body weight, blood glucose level, oral glucose tolerance, serum C-peptide level, hepatic antioxidant capacity, hepatic glycogen and hexokinase in liver tissues, serum blood lipid level, and alpha-glucosidase activity in small intestines were measured, and microstructure of pancreatic islet was analyzed. The results showed that the total content of seven triterpenoid compounds in MCS was 18.24 µg/mg, with Momordicoside K having the highest content at 11.66 µg/mg. Diabetic mice treated with MCS at 100 and 200 mg/kg body weight daily for 30 days showed a maximum glucose reduction (p < .05) of 12.63% and 26.47%, respectively. MCS significantly decreased levels of postprandial hyperglycemia, serum lipid, α-glucosidase activity, and liver malondialdehyde. Additionally, levels of serum C-peptide and liver glycogen, as well as hexokinase and antioxidant enzyme activity, were significantly increased compared to the diabetic control groups. Histopathological results showed that MCS markedly reduced degenerative changes in islet ß-cells. It is concluded that MCS exerts antidiabetic effects by improved hypoglycemic, hypolipidemic, and antioxidant effects, increased hexokinase activity and glycogen synthesis, and enhanced reparative effects on the histological architecture and insulin secretion function of the pancreas.

20.
Exp Mol Med ; 55(11): 2376-2389, 2023 11.
Artículo en Inglés | MEDLINE | ID: mdl-37907740

RESUMEN

Osteoarthritis (OA) is a full-joint, multifactorial, degenerative and inflammatory disease that seriously affects the quality of life of patients due to its disabling and pain-causing properties. ER stress has been reported to be closely related to the progression of OA. The inositol-requiring enzyme 1α/X-box-binding protein-1 spliced (IRE1α/XBP1s) pathway, which is highly expressed in the chondrocytes of OA patients, promotes the degradation and refolding of abnormal proteins during ER stress and maintains the stability of the ER environment of chondrocytes, but its function and the underlying mechanisms of how it contributes to the progression of OA remain unclear. This study investigates the role of IRE1α/ERN1 in OA. Specific deficiency of ERN1 in chondrocytes spontaneously resulted in OA-like cartilage destruction and accelerated OA progression in a surgically induced arthritis model. Local delivery of AdERN1 relieved degradation of the cartilage matrix and prevented OA development in an ACLT-mediated model. Mechanistically, progranulin (PGRN), an intracellular chaperone, binds to IRE1α, promoting its phosphorylation and splicing of XBP1u to generate XBP1s. XBP1s protects articular cartilage through TNF-α/ERK1/2 signaling and further maintains collagen homeostasis by regulating type II collagen expression. The chondroprotective effect of IRE1α/ERN1 is dependent on PGRN and XBP1s splicing. ERN1 deficiency accelerated cartilage degeneration in OA by reducing PGRN expression and XBP1s splicing, subsequently decreasing collagen II expression and triggering collagen structural abnormalities and an imbalance in collagen homeostasis. This study provides new insights into OA pathogenesis and the UPR and suggests that IRE1α/ERN1 may serve as a potential target for the treatment of joint degenerative diseases, including OA.


Asunto(s)
Cartílago Articular , Osteoartritis , Humanos , Proteínas Serina-Treonina Quinasas/genética , Proteínas Serina-Treonina Quinasas/metabolismo , Progranulinas/metabolismo , Endorribonucleasas/genética , Endorribonucleasas/metabolismo , Calidad de Vida , Osteoartritis/metabolismo , Condrocitos/metabolismo , Cartílago Articular/metabolismo , Colágeno/metabolismo , Homeostasis , Proteína 1 de Unión a la X-Box/genética , Proteína 1 de Unión a la X-Box/metabolismo
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