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1.
J Phys Chem Lett ; 15(18): 4992-4999, 2024 May 09.
Artículo en Inglés | MEDLINE | ID: mdl-38695534

RESUMEN

The intrinsic anisotropy of NbSe2 provides a favorable prerequisite of second harmonic generation (SHG) and rich possibilities for tailoring its nonlinear optical (NLO) properties. Here we report the highly efficient SHG of mechanically exfoliated NbSe2 flakes. The nonlinear optical response changes with excitation wavelengths, layer thicknesses, and polarizations of the excitation laser. The anisotropic SHG response further exhibits the intrinsic non-centrosymmetric crystal structure and could effectively assign the crystalline orientation of NbSe2 flakes. Interestingly, although NbSe2 flakes with tens of nanometers thickness experience attenuations in SHG performance, more efficient SHG anisotropy ratios were obtained, which are around 4 times higher than that of the 5-layer counterpart. The determined second-order nonlinearities of NbSe2 flakes (monolayer: ∼1.0 × 103 pm/V; 3-layer: ∼73 pm/V) are comparable to those of the commonly reported two-dimensional materials (e.g., MoS2, WSe2, graphene) with the same number of layers and much higher than those of commercial nonlinear optical crystals.

2.
J Med Chem ; 67(9): 7373-7384, 2024 May 09.
Artículo en Inglés | MEDLINE | ID: mdl-38646851

RESUMEN

Natural product evodiamine is a multitargeting antitumor lead compound. However, clinical development of evodiamine derivatives was hampered by poor water solubility and limited in vivo antitumor potency. Herein, a series of evodiamine-glucose conjugates were designed by additional targeting glucose transporter-1 (GLUT1). Compared with the lead compound, conjugate 8 exhibited obvious enhancement in water solubility and in vivo antitumor efficacy. Furthermore, the effect of GLUT1 targeting also led to lower cytotoxicity to normal cells. Antitumor mechanism studies manifested that conjugate 8 acted by Top1/Top2 dual inhibition, apoptosis induction, and G2/M cell cycle arrest, which selectively targeted tumor cells with a high expression level of GLUT1. Thus, evodiamine-glucose conjugates showed promising features as potential antitumor agents.


Asunto(s)
Antineoplásicos , Apoptosis , Diseño de Fármacos , Glucosa , Quinazolinas , Quinazolinas/farmacología , Quinazolinas/química , Quinazolinas/síntesis química , Humanos , Animales , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/síntesis química , Glucosa/metabolismo , Apoptosis/efectos de los fármacos , Ratones , Transportador de Glucosa de Tipo 1/antagonistas & inhibidores , Transportador de Glucosa de Tipo 1/metabolismo , Relación Estructura-Actividad , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Ratones Desnudos , Ratones Endogámicos BALB C
3.
Compr Rev Food Sci Food Saf ; 23(3): e13336, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38558497

RESUMEN

Fish inevitably face numerous stressors in growth, processing, and circulation. In recent years, stress-related change in fish muscle quality has gradually become a research hotspot. Thus, the understanding of the mechanism regarding the change is constantly deepening. This review introduces the physiological regulation of fish under stress, with particular attention devoted to signal transduction, gene expression, and metabolism, and changes in the physiological characteristics of muscular cells. Then, the influences of various stressors on the nutrition, physical properties, and flavor of the fish muscle are sequentially described. This review emphasizes recent advances in the mechanisms underlying changes in muscle quality, which are believed to be involved mainly in physiological regulation under stress. In addition, studies are also introduced on improving muscle quality by mitigating fish stress.


Asunto(s)
Peces , Estado Nutricional , Animales , Peces/genética , Peces/metabolismo , Músculos
4.
Chem Biol Drug Des ; 103(3): e14511, 2024 03.
Artículo en Inglés | MEDLINE | ID: mdl-38508859

RESUMEN

Docetaxel (DTX) is a semi-synthetic analogue of paclitaxel which has attracted extensive attention in the treatment of cancer. However, the current clinically used DTX formulations display low tumor targeting ability, leading to unsatisfactory therapeutic outcomes with adverse effects, which poses significant challenges to the clinical application. In this study, three galactosamine (Gal) and docetaxel conjugates with different linkers were synthesized, namely DTX-(suc-Gal)2, DTX-(DTDPA-Gal)2, and DTX-(DSeDPA-Gal)2. These three conjugates were characterized by 1H NMR, FT-IR and HRMS. The in vitro drug release study shows that DTX-(DTDPA-Gal)2 and DTX-(DSeDPA-Gal)2 exhibit glutathione (GSH)-responsive drug release and DTX-(DSeDPA-Gal)2 displays higher GSH-responsiveness. The in vitro antitumor activity study shows that DTX-(DTDPA-Gal)2 and DTX-(DSeDPA-Gal)2 exhibit enhanced cytotoxicity, cell apoptosis rate and G2/M phase arrest against HepG2 cells as compared to DTX-(suc-Gal)2, DTX-(DSeDPA-Gal)2 displays the highest cytotoxicity, cell apoptosis rate and G2/M phase arrest among these three conjugates. In addition, DTX-(DSeDPA-Gal)2 exhibits higher selectivity to HepG2 cells as compared to free DTX. The DTX-(DSeDPA-Gal)2 developed in this study has been proven to be an effective DTX conjugate for selective killing hepatoma cells.


Asunto(s)
Antineoplásicos , Docetaxel/farmacología , Antineoplásicos/farmacología , Antineoplásicos/química , Galactosamina , Espectroscopía Infrarroja por Transformada de Fourier , Taxoides/farmacología , Taxoides/química , Portadores de Fármacos/química , Línea Celular Tumoral
5.
Chem Biol Drug Des ; 103(3): e14495, 2024 03.
Artículo en Inglés | MEDLINE | ID: mdl-38444045

RESUMEN

New indocyanine green (ICG) (IR820) is one of the ICG derivatives and attracts increasing attention for cancer management. However, the unsatisfactory tumor targeting ability of IR820 significantly limits its applications for cancer theranostics. Biotin receptor is overexpressed on the membrane of various tumor cells and biotin modified nanocarriers have been reported to enhance the tumor targeting ability on several tumor types. In this work, biotin-new ICG conjugate (Biotin-SS-IR820) was prepared for tumor-targeted IR820 delivery. Biotin and IR820 were coupled through cystamine. The synthesized Biotin-SS-IR820 was characterized by 1 H NMR, FT-IR and HRMS. The in vitro singlet oxygen generation study shows that Biotin-SS-IR820 exhibits similar singlet oxygen generation as compared to IR820 upon 660 nm laser irradiation (0.8 W/cm2 ). The cellular uptake study shows that Biotin-SS-IR820 shows enhanced cellular uptake amount as compared to IR820 on 4T1 cells. As a result, Biotin-SS-IR820 displays enhanced in vitro photodynamic therapeutic effect against 4T1 cells as compared to IR820. In in vivo biodistribution study, Biotin-SS-IR820 shows enhanced tumor accumulation as compared to IR820. Biotin-SS-IR820 developed in this work shows promising prospects for targeted delivery of IR820 to biotin receptor overexpressed tumors.


Asunto(s)
Biotina , Neoplasias , Humanos , Verde de Indocianina , Distribución Tisular , Oxígeno Singlete , Espectroscopía Infrarroja por Transformada de Fourier
6.
J Ethnopharmacol ; 322: 117645, 2024 Mar 25.
Artículo en Inglés | MEDLINE | ID: mdl-38147942

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Morus alba L. (mulberry) is a well-known medicinal species that has been used by herbalist doctors for the treatment of diabetes for a long history, and modern ethnopharmacological studies have demonstrated the ameliorating effects of different mulberry extracts toward diabetes-related symptoms and identified a number of α-glucosidase inhibitors as hypoglycemic ingredients. AIM OF THE STUDY: The present study aims to explore new potent α-glucosidase inhibitors from the root bark of M. alba (known as Sang-Bai-Pi in traditional medicine) based on an in vivo antidiabetic evaluation of its extract fractions and further characterize the preliminary mechanism of the new active constituents. MATERIALS AND METHODS: α-Glucosidase inhibitory assay and diabetic mice model were used to locate and evaluate the active fractions from the extract. Diverse separation techniques (e.g. Sephadex LH-20 column chromatograph (CC) and HPLC) and spectroscopic methods (e.g. MS, NMR and ECD) were employed to isolate and structurally characterize the obtained constituents, respectively. Fluorescence quenching, kinetics and molecular docking experiments were conducted to investigate the enzyme inhibitory mechanism of the active compounds. RESULTS: The 80% ethanol eluate from the macroporous resin CC exerted good antidiabetic effects in the tested mice. Fifty-two flavonoids including 22 new ones were then separated and identified, and most of them showed strong inhibition against α-glucosidase with their structure-activity relationship being also discussed. The four new most active ingredients were further characterized to be mixed type of α-glucosidase inhibitors, and their binding modes with the enzyme were also explored. CONCLUSIONS: Our current work has demonstrated that the root bark of M. alba is an extremely rich source of flavonoids as potent α-glucosidase inhibitors and potential antidiabetic agents, which makes it a promising candidate species to develop new natural remedies for the prevention and treatment of diabetes.


Asunto(s)
Diabetes Mellitus Experimental , Morus , Ratones , Animales , Inhibidores de Glicósido Hidrolasas/farmacología , Inhibidores de Glicósido Hidrolasas/química , alfa-Glucosidasas/metabolismo , Diabetes Mellitus Experimental/tratamiento farmacológico , Simulación del Acoplamiento Molecular , Morus/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Hipoglucemiantes/química , Extractos Vegetales/uso terapéutico , Flavonoides/farmacología , Flavonoides/uso terapéutico , Flavonoides/química
7.
Food Res Int ; 175: 113747, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38128997

RESUMEN

Multi-functional packaging materials are an important development for food preservation. Emulsion electrospinning is a novel and simple method that can be used to prepare multi-functional packaging materials, which can effectively protect the loaded active substances during the preparation process. In this study, PCL/lecithin/bacteriocin CAMT6 nanofiber films with antimicrobial and antioxidant activity were prepared by emulsion electrostatic spinning. The morphology and homogeneity of the prepared nanofibrous membranes could be improved by optimising the formulation of the emulsion for electrospinning. Analytical testing of the prepared nanofiber films revealed that the nanofibers had a core-shell structure, with bacteriocin CAMT6 effectively encapsulated in the core layer and the PCL and phospholipids homogeneously mixed to form the shell layer. Additionally, the nanofiber films had acceptable tensile properties and water absorption capacity. In chilled salmon meat, the nanofiber film effectively inhibited the growth of bacteria, slowed the oxidation of oil and slowed water loss, which was a good protective effect. This study provides a reference for the encapsulation application of food-active packaging materials and bacteriocins.


Asunto(s)
Antiinfecciosos , Bacteriocinas , Nanofibras , Animales , Bacteriocinas/farmacología , Antioxidantes/farmacología , Nanofibras/química , Lecitinas , Emulsiones , Salmón , Agua
8.
J Agric Food Chem ; 71(50): 20304-20313, 2023 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-38054284

RESUMEN

Refrigerated waterless transport at 12 °C of live shrimp (Litopenaeus vannamei) causes flesh quality deterioration, and the underlying mechanism remains unknown. Herein, proteomics and bioinformatics analyses were used to elucidate the molecular mechanism of flesh quality changes. The result showed that 33 and 44 of the differentially abundant proteins (DAPs) were, respectively, identified in the acute cold (AC) group and the combined stress of acute cold and waterless duration (AC+WD) group, which were mostly involved in the metabolism processes and cellular structure of animal tissues, and notably enriched in biological pathways such as lysosome, glycolysis/gluconeogenesis, and focal adhesion. Furthermore, the changes in color and texture properties were closely associated with tubulin, gelsolin, laminin, trypsin-1, dipeptidyl peptidase, triosephosphate isomerase, and aldehyde dehydrogenase. Therefore, these DAPs could be used as potential biomarkers to monitor the deterioration of shrimp flesh quality during refrigerated waterless transportation.


Asunto(s)
Penaeidae , Proteómica , Animales , Alimentos Marinos , Penaeidae/metabolismo
9.
Chin J Nat Med ; 21(7): 551-560, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37517822

RESUMEN

Phytochemical investigation on the ethanol extract of a well-known medicinal herb Leonurus japonicus, led to the separation of 18 labdane type diterpenoids (1-18). Through comprehensive spectroscopic analyses and quantum chemical calculations, these compounds were structurally characterized as six new interesting 5,5,5-di-spirocyclic ones (1-6), two new (7 and 8) and six known (13-18) interesting 6,5,5-di-spirocyclic ones, a new rare 14,15-dinor derivative (9), and three new ones incorporating a γ-lactone unit (10-12). An in vitro neuroprotective assay in RSC96 cells revealed that compounds 7 and 12 exhibited neuroprotective activity in a concentration-dependent way, comparable to the reference drug N-acetylcysteine.


Asunto(s)
Diterpenos , Leonurus , Plantas Medicinales , Espectroscopía de Resonancia Magnética , Leonurus/química , Diterpenos/farmacología , Diterpenos/química , Componentes Aéreos de las Plantas , Estructura Molecular
10.
Talanta ; 265: 124885, 2023 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-37421788

RESUMEN

In this work, enhanced tryptophan (Trp) isomers recognition was successfully demonstrated on (CS/PAA)3.5@PEDOT:PSS/GCE, a multilayer chiral sensor with good stability and reproducibility. The (CS/PAA)n multilayers chiral interface was first fabricated via alternating self-assembly of chiral chitosan (CS) and achiral polyacrylic acid (PAA). Conductive PEDOT:PSS was then compounded with (CS/PAA)n multilayers to obtain the chiral sensor for the electrochemical recognition of Trp isomers. The structure of the sensor and its chirality properties for Trp isomers were characterized by fourier transform infrared spectroscopy (FT-IR),scanning electron microscopy (SEM) and electrochemical methods. The SEM images showed uniform distribution of PEDOT:PSS in the multilayer films, which changed the internal structure of the (CS/PAA)3.5. Consequently, (CS/PAA)3.5@PEDOT:PSS multilayers rendered more chiral centers in addition to improved good conductivity, which significantly amplified the oxidation peak current ratio of D-Trp to L-Trp (ID/IL) up to 6.71 at 25 °C. In addition, a linear relationship was observed between the peak current and Trp enantiomer concentration in the range of 0.002-0.15 mM, and the detection limits of D-Trp and L-Trp were 0.33 and 0.67 µM, respectively. More importantly, the percentage of D-Trp in non-racemic Trp enantiomers mixture solutions were successfully determined on the chiral interface, showing its effectiveness and promising potential in practical applications.

11.
Bioorg Med Chem Lett ; 92: 129393, 2023 08 15.
Artículo en Inglés | MEDLINE | ID: mdl-37369332

RESUMEN

Nicotinamide phosphoribosyltransferase (NAMPT) has emerged as a promising target for cancer therapy due to its strong correlation with nicotinamide adenine dinucleotide (NAD+) metabolism and tumorigenesis. Proteolysis targeting chimeras (PROTACs) provided an attractive strategy for developing NAMPT-targeting NAD+-depleting cancer drugs. Herein, a series of von Hippel-Lindau (VHL)-recruiting NAMPT-targeting PROTACs were designed using NAMPT inhibitor FK866 as the warhead. Among them, compound C5 degraded NAMPT (DC50 = 31.7 nM) in a VHL- and proteasome-dependent manner. Moreover, compound C5 effectively inhibited the proliferation of A2780 cells (IC50 = 30.6 nM) and significantly reduced the general cytotoxicity of FK866 to normal cells.


Asunto(s)
Nicotinamida Fosforribosiltransferasa , Neoplasias Ováricas , Quimera Dirigida a la Proteólisis , Femenino , Humanos , Línea Celular Tumoral , Citocinas/metabolismo , NAD/metabolismo , Nicotinamida Fosforribosiltransferasa/metabolismo , Proteolisis , Quimera Dirigida a la Proteólisis/química
12.
PLoS One ; 18(5): e0284334, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37155678

RESUMEN

Since the emergence and subsequent spread of the COVID-19 pandemic, students and instructors have faced unprecedented challenges and have been forced to shift traditional face-to-face classes online. This study, based on the E-learning Success Model (ELSM), seeks to examine the e-readiness level of students/instructors, judge the impediments that students/instructors encountered in different phases-pre-course delivery, course delivery, and course completion phase of the online EFL class, search for valuable online learning elements, and recommend recommendations for promoting e-learning success in online EFL classes. The study sample consists of 5914 students and 1752 instructors. The results demonstrate that: (a) both the students' and instructors' e-readiness level were slightly lower than the ready level; (b) three valuable online learning elements were teacher presence, teacher-student interaction, and practicing problem-solving ability; (c) eight categories of impediments during different phases of the online EFL class were technical challenges, learning process, learning environments, self-control, health concern, learning materials, assignment, and learning effect and assessments; (d) seven types of recommendations for promoting e-learning success were: (1) students: infrastructure and technology, learning process, content, curriculum design, teacher skills, service, and assessment; and (2) instructors: infrastructure and technology, human resources, teaching quality, content and services, curriculum design, teacher skills, and assessment. Based on these findings, this study recommends that further studies with an action research approach should be conducted to examine whether the recommendations are effective. Institutions should take the initiative to overcome barriers to engage and stimulate students. The outcomes of this research have theoretical and practical implications for researchers and higher education institutions (HEIs). During unprecedented times such as pandemics, administrators and instructors will have insights into implementing emergency remote teaching.


Asunto(s)
COVID-19 , Instrucción por Computador , Humanos , Pandemias , COVID-19/epidemiología , Aprendizaje , Estudiantes
13.
Emerg Microbes Infect ; 12(1): 2208687, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37102336

RESUMEN

Candida auris has emerged as a serious threat of public health and caused global epidemic due to multi-drug resistance, remarkable transmissibility and high mortality. To tackle the challenging super fungus, novel benzoanilide antifungal agents were discovered by an integrated strategy of phenotypic screen, hit optimization, antifungal assays and mechanism exploration. The most promising compound A1 showed potent in vitro and in vivo efficacy against Candida auris infection. Mechanism investigation revealed that compound A1 blocked the biosynthesis of virulence factors and fungal cell walls through the inhibition of glycosylphosphatidylinositol (GPI) and GPI-anchored proteins. Thus, compound A1 represents a promising lead compound to combat drug-resistant candidiasis.


Asunto(s)
Candida , Candidiasis Invasiva , Humanos , Candida auris , Antifúngicos/farmacología , Antifúngicos/uso terapéutico , Candidiasis Invasiva/tratamiento farmacológico , Pruebas de Sensibilidad Microbiana
14.
Phytochemistry ; 210: 113646, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-36958706

RESUMEN

Twenty-two labdane-type diterpenoids, including ten pairs of 15-epimers and a pair of 13,15-epimers, were obtained from the aerial parts of a well-known medicinal plant Leonurus japonicus Houtt. While these epimers were separated by chiral HPLC, their structures were established mainly via spectroscopic methods especially NMR, X-ray crystallography and ECD techniques. Among them, seventeen compounds, encompassing three pairs of solvolysis artefacts likely due to the use of ethanol as extracting solvent, were reported for the first time in the current work. Our preliminary anti-inflammatory screening demonstrated that seven diterpenoids displayed noteworthy inhibitory effect on the NO production in LPS-induced RAW264.7 cells. In addition, the release of pro-inflammatory factors TNF-α, IL-1ß and IL-6, as well as the expression of iNOS and COX-2 proteins, was also suppressed by the unreported 15,16-epoxy-6ß-hydroxy-15α-methoxy-7,16-dioxolabd-8,13-diene. Further investigation into the preliminary anti-inflammatory mechanism of this compound indicated that it could block the activation of NF-κB signaling pathway.


Asunto(s)
Diterpenos , Leonurus , Leonurus/química , Antiinflamatorios/farmacología , Espectroscopía de Resonancia Magnética , Diterpenos/química , Componentes Aéreos de las Plantas/química , Lipopolisacáridos/farmacología
15.
Mater Today Bio ; 18: 100542, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36647538

RESUMEN

Chemo-photodynamic therapy shows great potential for cancer treatment. However, the rational integration of chemotherapeutic agents and photosensitizers to construct an intelligent nanoplatform with synergistic therapeutic effect is still a great challenge. In this work, curcumin-loaded reduction-responsive prodrug nanoparticles of new indocyanine green (Cur@IR820-ss-PEG) were developed for synergistic cancer chemo-photodynamic therapy. Cur@IR820-ss-PEG exhibit high drug loading content and special worm-like morphology, contributing to their efficient cellular uptake. Due to the presence of the disulfide bond between IR820 and PEG, Cur@IR820-ss-PEG display reduction responsive drug release behaviors. The efficient cellular uptake and reduction triggered drug release of Cur@IR820-ss-PEG lead to their enhanced in vitro cytotoxicity against 4T1cells as compared to the mixture of IR820 and curcumin (IR820/Cur) under laser irradiation. Besides, Cur@IR820-ss-PEG exhibit prolonged blood half-life time, better tumor accumulation and retention, enhanced tumor hypoxia-inducible factor-1α (HIF-1α) and vascular endothelial cell growth factor (VEGF) suppression effect as compared to IR820/Cur. In vivo antitumor activity study, Cur@IR820-ss-PEG effectively inhibit the tumor angiogenesis, which potentiates the PDT efficacy and leads to the best in vivo antitumor effect of Cur@IR820-ss-PEG. This work provides a novel and relatively simple strategy for synergistic cancer chemo-photodynamic therapy.

16.
J Sci Food Agric ; 103(8): 3882-3895, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-36324190

RESUMEN

BACKGROUND: Shrimp is one of the most popular marine foods consumed throughout the world and its freshness is a crucial indicator for consumers. However, the flesh quality degradation of shrimp during waterless live transport has been observed and the underlying mechanism remains unknown. RESULTS: The present study aimed to clarify the biochemistry mechanisms of flesh degradation with integration of quality evaluation, metabolic profiling and histopathological analysis. The flesh quality indicators such as water holding capacity, protein and lipid contents, amino acid composition and myofiber components degraded with the prolongation of combined stress. In addition, the metabolites including gamma-aminobutyric acid, Val-Ala, Trh and derivatives of carnitine, phosphocholine and prostaglandin all reduced significantly under combined stress (P < 0.05). Furthermore, Kyoto Encyclopedia of Genes and Genomes (https://www.genome.jp/kegg) analysis revealed the enrichment of neuroactive ligand-receptor interaction and estrogen signaling pathways, indicating the involvement of neuroendocrine in stress response. Moreover, architecture impairment in hepatopancreas tissue verified the accumulation of metabolic disturbance. CONCLUSION: Taken together, the findings of the present study indicate that neuroendocrine system mediates the flesh degradation of L. vannamei during waterless transport by disturbing the biochemical metabolic pathways and inducing architecture impairment of myofibril components. © 2022 Society of Chemical Industry.


Asunto(s)
Penaeidae , Penaeidae/química , Penaeidae/metabolismo , Almacenamiento de Alimentos/métodos , Agua , Animales , Metabolómica , Estrés Fisiológico , Músculos/metabolismo , Transducción de Señal , Hepatopáncreas/química , Hepatopáncreas/metabolismo
17.
Chem Biodivers ; 19(12): e202200942, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36346849

RESUMEN

Thirteen cinnamic acid derivatives (1-13), including six formerly unreported hybrids incorporating different short-chain fatty acid esters (1-6), have been obtained and structurally elucidated from an ethnological herb Tinospora sagittata. The structures of them have been established by spectroscopic data analyses and NMR comparison with known analogs, while those of 1, 2, 4 and 6 have been further supported by total synthesis, and it is the first report of this type of metabolites from the title species. All the isolates have been assessed in an array of bioassays encompassing cytotoxic, antibacterial, anti-inflammatory, antioxidant, as well as α-glucosidase and HDAC1 inhibitory models. Compound 7 showed significant inhibitory activity against α-glucosidase, and half of the isolates also displayed moderate antiradical effect.


Asunto(s)
Antineoplásicos , Tinospora , Tinospora/química , alfa-Glucosidasas , Cinamatos/farmacología , Cinamatos/química , Estructura Molecular
18.
Food Funct ; 13(22): 11615-11626, 2022 Nov 14.
Artículo en Inglés | MEDLINE | ID: mdl-36268846

RESUMEN

Alcohol-induced cognitive impairment (AICI) has become a public health concern and thus effective intervention is urgently needed. The present study aims to assess the amelioration effect of walnut protein hydrolysate (WPH) in AICI rats and elucidate the associated mechanism. The Morris water maze task verified the significant amelioration effect of WPH against learning and memory deficits. Moreover, a reduction of oxidative stress and inflammation in brain tissues was observed and the significant enhancement of brain-derived neurotrophic factor (BDNF), postsynaptic density protein (PSD95) and cAMP-response element binding protein (p-CREB) expression (P < 0.05) indicated the rescue of damaged hippocampal synaptic plasticity. In addition, after WPH administration, disorders of ERK and caspase-3 signal pathways, abnormality in the release of the neurotransmitters acetylcholine (ACh) and gamma-aminobutyric acid (GABA), and histopathological impairment in the hippocampus of AICI rats were ameliorated in a dose-dependent manner. Overall, the amelioration of AICI by WPH might result from the alleviation of oxidative stress and inflammation in brain tissue and the improvement of hippocampal synaptic plasticity.


Asunto(s)
Disfunción Cognitiva , Juglans , Animales , Ratas , Ratas Sprague-Dawley , Juglans/metabolismo , Hidrolisados de Proteína/metabolismo , Aprendizaje por Laberinto , Hipocampo/metabolismo , Plasticidad Neuronal , Factor Neurotrófico Derivado del Encéfalo/genética , Factor Neurotrófico Derivado del Encéfalo/metabolismo , Disfunción Cognitiva/metabolismo , Encéfalo/metabolismo , Estrés Oxidativo , Inflamación/metabolismo
19.
Fish Shellfish Immunol ; 131: 391-400, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36252695

RESUMEN

the combination of acute cold (AC) and waterless duration (WD) constitutes the major environmental stress and induces the damage or even mortality to shrimp L. vannamei during live transport, whereas the responding mechanism to AC + WD at molecular level remains unknown. The present study aims to clarify the responding mechanism of L. vannamei to AC + WD stress by ultrastructural observation and transcriptomic analysis on hepatopancreas tissue. The results showed that the dramatical oxidative stress induced by AC + WD significantly mediated the alteration of amino acids and energy metabolism. Furthermore, KEGG pathway enrichment analysis revealed that the genes including DDO, GOT1, IDH1 and BBOX1 involved in energy metabolism and were significantly down-regulated, while some apoptosis- and inflammation-related genes such as DRONC, AP-1, and COX-2 were significantly up-regulated under AC + WD stress in comparison with those at normal control (all p < 0.05 or 0.01). These findings suggested that metabolic processes mediate the stress-induced damages of L. vannamei during waterless transport. Moreover, the significant overexpression of apoptosis-and inflammation-related proteins, and levels of inflammation cytokines in serum of shrimps strongly demonstrated the implication of inflammation and apoptosis pathways in stress-induced ultrastructural damage. These findings deepen our understanding into the response mechanisms of L. vannamei to AC + WD stress and provide the potential controlling biomarkers for transportation management.


Asunto(s)
Penaeidae , Transcriptoma , Animales , Penaeidae/metabolismo , Hepatopáncreas/metabolismo , Respuesta al Choque por Frío , Inflamación/genética , Inflamación/metabolismo , Apoptosis
20.
Drug Dev Res ; 83(8): 1923-1933, 2022 12.
Artículo en Inglés | MEDLINE | ID: mdl-36301989

RESUMEN

New indocyanine green (IR820) is an indocyanine green analog which has attracted increasing attention in cancer phototherapy for the prominent absorbance at near-infrared region and improved stability. However, the lack of tumor targeting ability is still an obstacle that severely limits the application of IR820. Lactobionic acid (LA) is a ligand for the asialoglycoprotein receptors which are overexpressed on the membrane of hepatocellular carcinoma cells. In this work, three conjugates of LA and IR-820, namely LA-IR820, LA-SS-IR820, and LA-DEG-IR820, were developed for targeted photodynamic therapy of hepatocellular carcinoma (HCC). The in vitro photodynamic effect study shows that LA-IR820, LA-SS-IR820 and LA-DEG-IR820 exhibit similar singlet oxygen quantum yield as compared to free IR820. The cellular uptake study demonstrates that LA-IR820, LA-SS-IR820, and LA-DEG-IR820 exhibit enhanced cellular uptake amount as compared to free IR820 due to the ligand-receptor interactions between LA and asialoglycoprotein receptor overexpressed on the membrane of HepG2 cells. Among these three conjugates, LA-IR820 with hydrodynamic diameter of 154.6 ± 6.1 nm exhibits the highest cellular uptake amount. The cellular reactive oxygen species (ROS) generation study shows that LA-IR820, LA-SS-IR820 and LA-DEG-IR820 display enhanced cellular ROS level as compared to free IR820 and LA-IR820 exhibits the highest cellular ROS level upon 600 mW/cm2 660 nm laser irradiation. As a result, LA-IR820, LA-SS-IR820 and LA-DEG-IR820 exhibit enhanced photocytotoxicity against HepG2 cells as compared to free IR820 and LA-IR820 exhibits the highest photocytotoxicity. LA-IR820, LA-SS-IR820, and LA-DEG-IR820 show significant potential for the targeted photodynamic therapy of HCC.


Asunto(s)
Carcinoma Hepatocelular , Neoplasias Hepáticas , Fotoquimioterapia , Humanos , Fármacos Fotosensibilizantes/farmacología , Carcinoma Hepatocelular/tratamiento farmacológico , Verde de Indocianina , Especies Reactivas de Oxígeno , Ligandos , Neoplasias Hepáticas/tratamiento farmacológico , Línea Celular Tumoral
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