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1.
Front Psychol ; 15: 1407885, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39021655

RESUMO

Two studies were conducted to explore the differences in the effect of adolescents' strategies for expressing academic emotions. In Study 1 a total of 65 adolescents participated in the study of the relationship between academic emotions and strategies for expressing them in competitive and cooperative situations. In Study 2 a total of 113 adolescents participated in the study of the relationship between the strategies and peer acceptance in competitive and cooperative situations. The results showed that the relationship between academic emotions and strategies for expressing them in competitive and cooperative situations was situation stable while the relationship between the strategies and peer acceptance was situation specific. Furthermore, emotional expression may be more adaptive when experiencing positive academic emotions. When adolescents experience negative academic emotions, expressing them is more adaptive from the perspective of their own academic emotional experience; whereas suppressing them is more adaptive from the perspective of peer acceptance. These findings (a) clarify how to use more adaptive strategies for emotional expression in various situations and (b) serve as a guide for helping adolescents use strategies to express emotions flexibly according to the situation.

2.
3.
RSC Med Chem ; 15(6): 2114-2126, 2024 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-38911165

RESUMO

Inflammation is the body's response to defence against infection or injury, and is associated with the progression of many diseases, such as inflammatory bowel disease (IBD) and rheumatoid arthritis (RA). LCA, a dibenzylbutane lignan extracted from the roots of traditional medicinal plant Litsea cubeba (Lour.) Pers., has demonstrated promising anti-inflammatory activity. In this study, a series of novel LCA derivatives were designed, synthesized, and evaluated for anti-inflammatory activity. Lipopolysaccharide (LPS)-induced RAW 264.7 cell model experiments showed that compound 10h (at 20 µM of concentration) had the strongest inhibitory effect on NO release, and inhibited the secretion and gene expression levels of interleukin (IL)-1ß, IL-6, and tumor necrosis factor (TNF)-α in vitro. In addition, western blot, immunofluorescence, and molecular docking showed that the anti-inflammatory mechanism of compound 10h may be related to the nuclear factor (NF)-κB signalling pathway. In vivo studies based on a carrageenan-induced mouse paw edema model have shown significant anti-inflammatory activity of compound 10h at 20 mg kg-1. Preliminary in vitro and in vivo studies indicate that compound 10h has the potential to be developed as a novel anti-inflammatory agent.

4.
Health Educ Behav ; : 10901981241255366, 2024 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-38798091

RESUMO

Hazardous/harmful drinking among college students is increasingly becoming a global health concern. Previous studies have mostly paid more attention to the prevalence and risk factors of alcohol use disorder based on the public health approach, and less is understood about psychological mechanisms and protective factors of problem drinking behavior. Grounded in the framework of developmental assets, this study explored the predictive effect of external assets (i.e., social connectedness) and internal assets (i.e., self-concept clarity and drinking refusal self-efficacy) on hazardous/harmful drinking among Chinese college students. Participants were 598 college students with a mean age of 19.41 (SD = 1.21) years. The results of structural equation modeling showed that social connectedness negatively predicted college students' hazardous/harmful drinking. Moreover, our path analyses revealed a serial mediation among these variables: students with high social connectedness tended to report high self-concept clarity, which in turn increased drinking refusal self-efficacy, and consequently decreased the level of hazardous/harmful drinking. This study revealed the mechanisms underlying how external and internal assets predict risky drinking among college students. These findings made significant contributions to prevention and precision interventions for college-aged youth with drinking problems.

5.
J Med Chem ; 67(6): 4889-4903, 2024 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-38485922

RESUMO

Directly blocking the Keap1-Nrf2 pathway is a promising strategy for the mitigation of acute lung injury (ALI). Peptide Keap1-Nrf2 inhibitors have been reported to have a high Keap1 binding affinity. However, these inhibitors showed weak activity in cells and/or animals. In this study, we designed a series of linear peptides from an Nrf2-based 9-mer Ac-LDEETGEFL-NH2. To improve the cellular activity, we further designed cyclic peptides based on the crystal complex of Keap1 with a linear peptide. Among them, cyclic 9-mer ZC9 targeting Keap1 showed a better affinity (KD2 = 51 nM). Specifically, it exhibited an acceptable water solubility (>38 mg/mL), better cell permeability, cell activity, and metabolic stability (serum t1/2 > 24 h). In the in vitro LPS-induced oxidative damages and ALI model, ZC9 showed significant dose-response reversal activity without apparent toxicity. In conclusion, our results suggested ZC9 as a lead cyclic peptide targeting the Keap1-Nrf2 pathway for ALI clinical treatment.


Assuntos
Lesão Pulmonar Aguda , Peptídeos Cíclicos , Animais , Peptídeos Cíclicos/farmacologia , Peptídeos Cíclicos/uso terapêutico , Peptídeos Cíclicos/metabolismo , Proteína 1 Associada a ECH Semelhante a Kelch/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Peptídeos/farmacologia , Peptídeos/uso terapêutico , Peptídeos/química , Lesão Pulmonar Aguda/tratamento farmacológico
6.
Eur J Med Chem ; 268: 116272, 2024 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-38402749

RESUMO

Acute lung injury (ALI) is a serious public health problem associated with high morbidity and mortality. However, few efficacious drugs are clinically available. Inhibition of proinflammatory cytokines is considered to be a promising method for the treatment of inflammatory diseases. Herein, the total synthesis of a dibenzylbutane lignan, 9'-O-di-(E)-feruloyl-meso-5,5'-dimethoxysecoisolariciresinol (LCA), was completed. A series of LCA derivatives were designed and synthesized, and their anti-inflammatory activities were evaluated. Derivative 14r significantly inhibited LPS-induced expression of NO and the proinflammatory cytokines TNF-α, IL-6, and IL-1ß in RAW 264.7 cells and inhibited activation of the NF-κB pathway. Compound 14r reduced LPS-induced pulmonary inflammation and ALI in mice. It showed significant protective effects against LPS-induced ALI in mice and significantly reduced levels of proinflammatory cytokines in serum and bronchoalveolar lavage fluid. The ratio of wet weight to dry weight of lung tissue was normalized by compound 14r, which was consistent with suppression of neutrophil infiltration and production of proinflammatory cytokines. Compound 14r reduced the mRNA expression of some proinflammatory cytokines, improved histopathologic changes, and reduced macrophage infiltration in lung tissues. Collectively, these results suggest a new series of LCA derivatives that could be promising anti-inflammatory agents for ALI treatment.


Assuntos
Lesão Pulmonar Aguda , Lipopolissacarídeos , Animais , Camundongos , Lipopolissacarídeos/farmacologia , Lipopolissacarídeos/metabolismo , Lesão Pulmonar Aguda/induzido quimicamente , Lesão Pulmonar Aguda/tratamento farmacológico , Lesão Pulmonar Aguda/metabolismo , Pulmão/metabolismo , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , NF-kappa B/metabolismo , Citocinas/metabolismo
7.
Bioorg Med Chem Lett ; 99: 129627, 2024 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-38272189

RESUMO

Metastasis is one of the major causes of death in patients with cancer, and cell invasion plays a fundamental part in this process. Because of the absence of efficacious treatments, caring for these patients is challenging. Recently, we optimized the structure of the naturally occurring lasso peptide sungsanpin. We identified two peptides, octapeptide S3 and cyclic peptide S4, which inhibited invasion into A549 cells effectively. We undertook an alanine scan of S3 to explore the structure-activity relationship. The linear octapeptide S3-4 and cyclic peptide S4-1 exhibited improved inhibition of invasion into A549 cells. We modified S3-4 to obtain S3-4K, which displayed much higher inhibitory activity against invasion into A549 cells than S3-4. Of all peptides tested, S4-1 upregulated significantly mRNA of tissue inhibitor matrix metalloproteinase TIMP-1 and TIMP-2.


Assuntos
Peptídeos , Inibidor Tecidual de Metaloproteinase-1 , Humanos , Inibidor Tecidual de Metaloproteinase-1/genética , Metaloproteinases da Matriz , Células A549 , Peptídeos Cíclicos
8.
Bioorg Med Chem ; 97: 117543, 2024 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-38071944

RESUMO

In order to develop antifungal drugs, a series of novel azole analogues were designed and synthesized based on our previous work. Most of the target compounds had broad-spectrum antifungal activity, which showed excellent to moderate inhibitory activity against the tested strains, except A. fum 0504656. Among these, compounds B3, B7, B8, B11, B12 and E9 showed excellent activity against C. alb Y0109 and C. alb SC5314 (with the MIC80: 0.0156 ug/mL). In addition, compound B3 showed the best inhibitory activity against fluconazole-resistant strains C. alb 901 and C. alb 904, and had low toxicity against NIH/3T3 cells at the effective MIC range against fungi. Structure-activity relationship and docking studies of the derivatives suggest that the presence of the 2-fluoro-4-hydroxyphenyl and 1,2,3-triazole group enhance the antifungal activity of the compounds, which may be related to the interaction of the key groups with the amino acids surrounding the target enzyme.


Assuntos
Antifúngicos , Azóis , Animais , Camundongos , Antifúngicos/química , Azóis/farmacologia , Candida albicans , Testes de Sensibilidade Microbiana , Fluconazol/farmacologia , Relação Estrutura-Atividade
9.
Patient Educ Couns ; 116: 107948, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-37672920

RESUMO

OBJECTIVES: To explore the considerations and barriers to implementing shared decision-making (SDM) in infertility treatment among female infertility patients, their male spouses, and fertility clinicians. METHODS: Participants were recruited from a reproductive medicine hospital in China's Shandong Province using purposive sampling. One-on-one interviews were held with female infertility patients and their spouses. In addition, a focus group discussion was conducted with fertility clinicians. Data analysis was subjected to open, axial, and selective coding. RESULTS: Nineteen female infertility patients and 10 male spouses were interviewed one-on-one. Five clinicians participated in the focus group discussion. Most female patients wanted to participate in the decision-making process, and that spouses and fertility clinicians supported SDM. Furthermore, key barriers were identified from the perspectives of multiple stakeholders, including communication difficulties, psychological pressure on female patients, patient preferences, multiple treatment stages, male spousal participation, clinician-patient trust, and subjective patient factors. CONCLUSIONS/PRACTICE IMPLICATIONS: This study explored the considerations of and barriers to implementing SDM in infertility treatment. Key barriers were identified from the perspectives of multiple stakeholders. Based on the findings, clinicians should encourage patients and their spouses to actively participate in decision-making, and provide objective and realistic guidance.


Assuntos
Infertilidade Feminina , Humanos , Masculino , Feminino , Relações Médico-Paciente , Participação do Paciente/psicologia , Tomada de Decisão Compartilhada , Pesquisa Qualitativa , Tomada de Decisões
10.
Bioorg Chem ; 135: 106500, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-37003134

RESUMO

Blocking the interaction between Ras and Son of Sevenless homolog 1 (SOS1) has been an attractive therapeutic strategy for treating cancers involving oncogenic Ras mutations. K-Ras mutation is the most common in Ras-driven cancers, accounting for 86%, with N-Ras mutation and H-Ras mutation accounting for 11% and 3%, respectively. Here, we report the design and synthesis of a series of hydrocarbon-stapled peptides to mimic the alpha-helix of SOS1 as pan-Ras inhibitors. Among these stapled peptides, SSOSH-5 was identified to maintain a well-constrained alpha-helical structure and bind to H-Ras with high affinity. SSOSH-5 was furthermore validated to bind with Ras similarly to the parent linear peptide through structural modeling analysis. This optimized stapled peptide was proven to be capable of effectively inhibiting the proliferation of pan-Ras-mutated cancer cells and inducing apoptosis in a dose-dependent manner by modulating downstream kinase signaling. Of note, SSOSH-5 exhibited a high capability of crossing cell membranes and strong proteolytic resistance. We demonstrated that the peptide stapling strategy is a feasible approach for developing peptide-based pan-Ras inhibitors. Furthermore, we expect that SSOSH-5 can be further characterized and optimized for the treatment of Ras-driven cancers.


Assuntos
Antineoplásicos , Neoplasias , Humanos , Proteína SOS1/química , Proteína SOS1/genética , Proteína SOS1/metabolismo , Peptídeos/farmacologia , Transdução de Sinais , Mutação , Antineoplásicos/farmacologia
11.
Int Nurs Rev ; 70(3): 315-321, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37071893

RESUMO

AIMS: The purpose of this study was to identify the mediating and moderating mechanisms by which social connectedness predicts life satisfaction among Chinese nurses. BACKGROUND: Previous researchers have primarily focused on sociodemographic and occupational domain risk factors for nurses' life satisfaction with relatively little insight into facilitative and protective factors and underlying psychological mechanisms. METHODS: We investigated 459 Chinese nurses' social connectedness, work-family enrichment, self-concept clarity, and life satisfaction via a cross-sectional design. We explored the underlying predictive mechanisms among these variables by creating a moderated mediation model. We followed STROBE checklist. RESULTS: Work-family enrichment played a mediating role in understanding the positive effects of social connectedness on nurses' life satisfaction. In addition, the moderating effect of self-concept clarity was manifested itself in the association between work-family enrichment and life satisfaction. DISCUSSION AND CONCLUSION: Interpersonal asset (social connectedness) and the positive aspect of the work-family interface (work-family enrichment) were significant contributors to nurses' life satisfaction. In particular, high self-concept clarity can enhance the beneficial effect of work-family enrichment on life satisfaction. IMPLICATIONS FOR NURSING POLICY AND PRACTICE: Strengthening social connectedness, promoting synergy in work-family roles, and maintaining a clarity of self-concept are important intervention pathways to enhance the health and well-being of nurses.


Assuntos
Enfermeiras e Enfermeiros , Recursos Humanos de Enfermagem Hospitalar , Humanos , Estudos Transversais , População do Leste Asiático , Satisfação no Emprego , Recursos Humanos de Enfermagem Hospitalar/psicologia , Inquéritos e Questionários , Satisfação Pessoal
12.
J Res Adolesc ; 33(2): 564-574, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-36588193

RESUMO

Within the framework of positive youth development (PYD) and life course theory, this study was designed to examine patterns of PYD and promotive factors over the first semester of Chinese high school with a sample of 480 students (boys, 43.96%). The growth mixture model identified four trajectories of PYD, labeled high start-fast decreasing, high start-low decreasing, low start-low increasing, and mid-persistent. Results also showed that membership in a PYD trajectory is significantly related to three promotive factors: parental involvement, teacher involvement, and intentional self-regulation. These findings have important theoretical and practical insights for a deeper understanding of the underlying mechanisms of positive development in adolescents following the critical period surrounding the transition to high school.


Assuntos
Desenvolvimento do Adolescente , Instituições Acadêmicas , Masculino , Humanos , Adolescente , Pais , China/epidemiologia , Estudantes
13.
Chem Biodivers ; 20(2): e202201221, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36651671

RESUMO

Cancer metastasis, including cell invasion, is a major cause of poor clinical outcomes and death in numerous cancer patients. In recent years, many efforts have been made to develop potent therapeutic molecules from naturally derived peptides. Sungsanpin is a naturally derived lasso peptide that inhibits A549 cell invasion. We aimed to evaluate the potential of sungsanpin derivatives as candidates for anti-invasion drugs. We synthesized an analog of sungsanpin (Sun A) using a solid-phase peptide synthesis strategy (SPPS) and further modified its structure to improve its anti-invasion activity. All peptides were tested for their proliferative inhibition and anti-invasion activities in the A549 cell lines. Octapeptide S3 and cyclooctapeptide S4 upregulated the expression of TIMP-1 and TIMP-2 mRNA effectively and thus improved the inhibitory effect on the invasion of A549 cells. The two peptides can inhibit the invasion of A549 cells by up to 60 %, suggesting that they have potential as lead molecules for the development of peptide inhibitors.


Assuntos
Neoplasias Pulmonares , Peptídeos , Humanos , Peptídeos/química , Células A549 , Linhagem Celular Tumoral , Neoplasias Pulmonares/tratamento farmacológico
14.
Front Nutr ; 9: 1036295, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36562043

RESUMO

Sea buckthorn (Hippophae rhamnoides L.), an ancient miraculous plant, is of great interest because of its tenacity, richness in nutritional active substances, and biological activity. Sea buckthorn is a deciduous shrub or tree of the genus Hippophae in the family Elaeagnaceae. It is a pioneer tree species for soil improvement, wind and sand control, and soil and water conservation. Sea buckthorn contains many nutritional active components, such as vitamins, carotenoids, polyphenols, fatty acids, and phytosterols. Moreover, sea buckthorn has many health benefits, such as antioxidant, anticancer, anti-hyperlipidemic, anti-obesity, anti-inflammatory, antimicrobial, antiviral, dermatological, neuroprotective, and hepatoprotective activities. Sea buckthorn not only has great medicinal and therapeutic potential, but also is a promising economic plant. The potential of sea buckthorn in the human food industry has attracted the research interest of researchers and producers. The present review mainly summarizes the phytochemistry, nutrients, health benefits, and food applications of sea buckthorn. Overall, sea buckthorn is a dietary source of bioactive ingredients with the potential to be developed into functional foods or dietary supplements for the prevention and treatment of certain chronic diseases, which deserves further research.

15.
Nutrients ; 14(19)2022 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-36235731

RESUMO

Sesame (Sesamum indicum L.), of the Pedaliaceae family, is one of the first oil crops used in humans. It is widely grown and has a mellow flavor and high nutritional value, making it very popular in the diet. Sesame seeds are rich in protein and lipids and have many health benefits. A number of in vitro and in vivo studies and clinical trials have found sesame seeds to be rich in lignan-like active ingredients. They have antioxidant, cholesterol reduction, blood lipid regulation, liver and kidney protection, cardiovascular system protection, anti-inflammatory, anti-tumor, and other effects, which have great benefits to human health. In addition, the aqueous extract of sesame has been shown to be safe for animals. As an important medicinal and edible homologous food, sesame is used in various aspects of daily life such as food, feed, and cosmetics. The health food applications of sesame are increasing. This paper reviews the progress of research on the nutritional value, chemical composition, pharmacological effects, and processing uses of sesame to support the further development of more functionalities of sesame.


Assuntos
Lignanas , Sesamum , Animais , Anti-Inflamatórios/análise , Antioxidantes/análise , Humanos , Lignanas/farmacologia , Lipídeos/análise , Valor Nutritivo , Compostos Fitoquímicos/análise , Sementes/química , Sesamum/química
16.
Bioorg Chem ; 129: 106216, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36283177

RESUMO

In order to develop new triazole derivatives, we optimized the lead compound a6 by structural modifications to obtain a series of (2R,3R)-3-((1-substituted-1H-1,2,3-triazol-4-yl) methoxy)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl) butan-2-ol, compounds 5-36. Most of the target compounds exhibited excellent in vitro antifungal activity against Candida albicans 10231 and Candida glabrata 537 with MIC ≤ 0.125 µg/mL. Of particular note, compounds 6, 22, 28, 30 and 36 were highly active against Candida neoformans 32609 with MIC ≤ 0.125 µg/mL and showed broad-spectrum antifungal activity including against fluconazole-resistant Candida auris 891. In addition, compounds 6 and 22 demonstrated inhibitory effects on filamentation in the azole-resistant C. albicans isolate. Moreover, compounds 6 and 22 were minimally toxic to HUVECs and possessed weak inhibitory effects on the human CYP3A4 and CYP2D6. SARs and docking study further indicated that ortho-substituted groups in the terminal phenyl ring can promote the compounds to improve their antifungal activity.


Assuntos
Antifúngicos , Triazóis , Humanos , Antifúngicos/química , Triazóis/química , Testes de Sensibilidade Microbiana , Fluconazol/farmacologia , Candida albicans , Relação Estrutura-Atividade
17.
Bioorg Med Chem Lett ; 76: 128986, 2022 11 15.
Artigo em Inglês | MEDLINE | ID: mdl-36113670

RESUMO

Herein, the di- and trisaccharide mimics of the hexasaccharide antigen related to Bacillus anthracis were synthesized and covalently coupled with carrier proteins, such as keyhole limpet hemocyanin (KLH) and bovine serum albumin (BSA), to form the corresponding glycoconjugates 1-6. 2,3,4,6-Tetra-O-benzyl thioglycoside and 2-deoxyl-2-phthalylamino-3,4,6-tri-O-benzyl thioglycoside were applied as glycosyl donors to guarantee α or ß-configuration of the newly formed glycosidic bonds. Glutaraldehyde was used as a homobifunctional cross-linker for high-efficiency coupling. The synthetic KLH-glycoconjugates 2, 4 and 6 were also used to vaccinate female Balb/c mice and the preliminary results of ELISA uncovered that all three KLH-conjugates could induce immune responses and generate oligosaccharide-specific total IgG antibodies. The trisaccharide 8, the glycosyl part of glycoconjugate 4, is of great immunogenicity.


Assuntos
Bacillus anthracis , Tioglicosídeos , Camundongos , Animais , Feminino , Trissacarídeos , Soroalbumina Bovina , Glutaral , Antígenos , Camundongos Endogâmicos BALB C , Imunoglobulina G , Glicoconjugados , Oligossacarídeos , Proteínas de Transporte
18.
Phytomedicine ; 106: 154422, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36087526

RESUMO

BACKGROUND: The traditional Chinese medicine Platycodon grandiflorum (Jacq.) A. DC. (PG, balloon flower) has medicinal and culinary value. It consists of a variety of chemical components including triterpenoid saponins, polysaccharides, flavonoids, polyphenols, polyethylene glycols, volatile oils and mineral components, which have medicinal and edible value. PURPOSE: The ultimate goal of this review is to summarize the phytochemistry, pharmacological activities, safety and uses of PG in local and traditional medicine. METHODS: A comprehensive search of published literature up to March 2022 was conducted using the PubMed, China Knowledge Network and Web of Science databases to identify original research related to PG, its active ingredients and pharmacological activities. RESULTS: Triterpene saponins are the primary bioactive compounds of PG. To date, 76 triterpene saponin compounds have been isolated and identified from PG. In addition, there are other biological components, such as flavonoids, polyacetylene and phenolic acids. These extracts possess antitussive, immunostimulatory, anti-inflammatory, antioxidant, antitumor, antiobesity, antidepressant, and cardiovascular system activities. The mechanisms of expression of these pharmacological effects include inhibition of the expression of proteins such as MDM and p53, inhibition of the activation of enzymes, such as AKT, the secretion of inflammatory factors, such as IFN-γ, TNF-α, IL-2 and IL-1ß, and activation of the AMPK pathway. CONCLUSION: This review summarizes the chemical composition, pharmacological activities, molecular mechanism, toxicity and uses of PG in local and traditional medicine over the last 12 years. PG contains a wide range of chemical components, among which triterpene saponins, especially platycoside D (PD), play a strong role in pharmacological activity, representing a natural phytomedicine with low toxicity that has applications in food, animal feed and cosmetics. Therefore, PG has value for exploitation and is an excellent choice for treating various diseases.


Assuntos
Antitussígenos , Óleos Voláteis , Platycodon , Saponinas , Triterpenos , Proteínas Quinases Ativadas por AMP , Animais , Antioxidantes/farmacologia , Etnofarmacologia , Flavonoides , Interleucina-2 , Medicina Tradicional Chinesa , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Platycodon/química , Polímero Poliacetilênico , Polietilenoglicóis , Proteínas Proto-Oncogênicas c-akt , Saponinas/química , Saponinas/farmacologia , Fator de Necrose Tumoral alfa , Proteína Supressora de Tumor p53
19.
Foods ; 11(18)2022 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-36140986

RESUMO

Hawthorn (Crataegus) is a plant of the Rosaceae family and is widely grown throughout the world as one of the medicinal and edible plants, known as the "nutritious fruit" due to its richness in bioactive substances. Preparations derived from it are used in the formulation of dietary supplements, functional foods, and pharmaceutical products. Rich in amino acids, minerals, pectin, vitamin C, chlorogenic acid, epicatechol, and choline, hawthorn has a high therapeutic and health value. Many studies have shown that hawthorn has antioxidant, anti-inflammatory, anticancer, anti-cardiovascular disease, and digestive enhancing properties. This is related to its bioactive components such as polyphenols (chlorogenic acid, proanthocyanidin B2, epicatechin), flavonoids (proanthocyanidins, mucoxanthin, quercetin, rutin), and pentacyclic triterpenoids (ursolic acid, hawthornic acid, oleanolic acid), which are also its main chemical constituents. This paper briefly reviews the chemical composition, nutritional value, food applications, and the important biological and pharmacological activities of hawthorn. This will contribute to the development of functional foods or nutraceuticals from hawthorn.

20.
Bioorg Chem ; 127: 105908, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35728291

RESUMO

Thirty-two novel DG F-spiroacetal ring-opening derivatives, including 24 acetylated derivatives and 8 nitrogenous derivatives, were designed and synthesized from diosgenin (DG). The cytotoxicity of the novel derivatives was evaluated by MTT assay, except for compounds 4a, 4e, 4i, 4 l, 5a and 5 h, which were potentially cytotoxic to RAW264.7 cells, all the other derivatives had no significant cytotoxicity. The NO release inhibitory activities of novel derivatives were screened by Griess method. The results showed that the anti-inflammatory activity of the DG acetylated derivatives was stronger than the nitrogenous derivatives, and 4a-4 m containing acetyl groups at the 3-position may have better anti-inflammatory effects than 5a-5 k containing free hydroxyl groups. In ELISA assay, compound 4 m exhibited potent anti-inflammatory activity by inhibiting the production of NO in RAW264.7 cells activated by LPS with IC50 values 0.449 ± 0.050 µM. The results of docking experiments showed that 4 m has a good affinity for p65 protein.


Assuntos
Antineoplásicos , Diosgenina , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Diosgenina/farmacologia , Desenho de Fármacos , Simulação de Acoplamento Molecular , Estrutura Molecular , Relação Estrutura-Atividade
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