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1.
Sheng Li Xue Bao ; 73(3): 501-508, 2021 Jun 25.
Artigo em Chinês | MEDLINE | ID: mdl-34230951

RESUMO

Atherosclerosis is a chronic inflammatory disease. Cytokine-related research provides an important direction for the prevention and treatment of atherosclerosis. Cytokines, produced by different types of cells and acting on a range of targets, play a key role in the pathogenesis and progression of atherosclerosis. This review summarizes the main pro-inflammatory and anti-inflammatory cytokines related to atherosclerosis and their underlying mechanism. We also outline current anti-atherosclerosis treatments targeting cytokines. The research and treatment prospects of cytokines in the prevention and treatment of atherosclerosis are discussed briefly as well.


Assuntos
Aterosclerose , Citocinas , Anti-Inflamatórios/uso terapêutico , Aterosclerose/tratamento farmacológico , Humanos , Inflamação/tratamento farmacológico
2.
Int J Mol Sci ; 22(12)2021 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-34205487

RESUMO

Coronavirus disease 2019 (COVID-19) caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been associated with excess mortality worldwide. The cardiovascular system is the second most common target of SARS-CoV-2, which leads to severe complications, including acute myocardial injury, myocarditis, arrhythmias, and venous thromboembolism, as well as other major thrombotic events because of direct endothelial injury and an excessive systemic inflammatory response. This review focuses on the similarities and the differences of inflammatory pathways involved in COVID-19 and atherosclerosis. Anti-inflammatory agents and immunomodulators have recently been assessed, which may constitute rational treatments for the reduction of cardiovascular events in both COVID-19 and atherosclerotic heart disease.


Assuntos
Aterosclerose/patologia , COVID-19/patologia , Corticosteroides/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Aterosclerose/complicações , Aterosclerose/tratamento farmacológico , Aterosclerose/prevenção & controle , COVID-19/complicações , COVID-19/tratamento farmacológico , COVID-19/virologia , Quimiocinas/metabolismo , Síndrome da Liberação de Citocina/etiologia , Citocinas/metabolismo , Humanos , Prognóstico , SARS-CoV-2/isolamento & purificação , SARS-CoV-2/metabolismo
3.
Acta Biomed ; 92(3): e2021250, 2021 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-34212899

RESUMO

I am a professor and attending pharmacist in the field of pharmaceutical sciences and writer or co-author of at least 5 manuscripts about different aspects of COVID-19. More than 15 months from the first report of COVID-19, over 120 million people all over the world infected by this virus, and more than 2.5 million of them have died. Although different treatment approaches have been proposed, management of the COVID-19 patients is steal remained controversial. In this regard, I want to share my personal experience from the exposure to the coronavirus and the consequence of this infection on my health status. I am a 51 years old male, known case of hypertension, dyslipidemia, and chronic kidney disease. During working hours of colleagues in the Faculty of Pharmacy, I visited one of my colleagues in his office. After leaving the Faculty, my colleague declares that his RT-PCR test of COVID-19 is positive and it took 3 days for me to experience the first sign of the COVID-19 as fever. Many complications have occurred for me during the different stages of COVID-19 infection that I shared and explained in detail with the suggested pharmacotherapies. According to the pathophysiology of COVID-19 infection and my personal experience during COVID-19 infection, I want to emphasize the necessity of early initiation of anti-inflammatory agents including corticosteroids and colchicine in high-risk patients with mild-to-moderate COVID-19 pneumonia who shows respiratory system involvement, in order to prevent progression to the severe and critical stages of this disease.


Assuntos
COVID-19 , Anti-Inflamatórios , Humanos , Masculino , Pessoa de Meia-Idade , Farmacêuticos , SARS-CoV-2 , Resultado do Tratamento
4.
Sheng Wu Gong Cheng Xue Bao ; 37(6): 1952-1967, 2021 Jun 25.
Artigo em Chinês | MEDLINE | ID: mdl-34227287

RESUMO

Cadinanes are a class of bicyclic sesquiterpenes with complex stereochemistry and broad pharmacological activities, such as antibacterial, anti-inflammatory, and hypoglycemic activities. To date, structurally diverse and bioactive cadinane sesquiterpenes have been isolated and identified from a variety of plants and microorganisms. Moreover, deeper understandings on cadinane sesquiterpene synthases have been made. This article categorized the 124 new cadinanes which were published in the literatures in the past four years (2017-2020) into five structural types, and presented their pharmacological activities. We also illustrated the elucidation of the biosynthetic pathways for typical cadinanes, summarized the research progress on cadinane sesquiterpene synthases. Finally, current challenges and future prospects were proposed and discussed.


Assuntos
Sesquiterpenos , Anti-Inflamatórios , Sesquiterpenos Policíclicos
5.
Tuberk Toraks ; 69(2): 253-260, 2021 Jun.
Artigo em Turco | MEDLINE | ID: mdl-34256517

RESUMO

Chronic rhinosinusitis with nasal polyps often accompanies severe asthma. Uncontrolled nasal polyp does not only impair the quality of life, but also makes it difficult to control the accompanying asthma. Eosinophilic chronic sinusitis dominated by type 2 inflammation is phenotypically manifested by nasal polyps. In recent years, approaches towards phenotype and endotype have developed in patients with chronic sinusitis as well as in asthma; biological treatments come into question in uncontrolled patients with appropriate endotype. Randomized controlled trials conducted on treatments that antagonize the Ig-E, IL-5, and IL-4a pathways in these patients are promising. The effectiveness of biological treatments, which we think will be more involved in clinical practice in the management of nasal polyp patients in the near future, will become clear with the increase in real life data in the literature.


Assuntos
Anti-Inflamatórios/uso terapêutico , Asma/terapia , Produtos Biológicos/uso terapêutico , Pólipos Nasais/terapia , Humanos , Qualidade de Vida , Ensaios Clínicos Controlados Aleatórios como Assunto
6.
Int J Mol Sci ; 22(13)2021 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-34198981

RESUMO

Recently, adipose-derived stem cells (ADSCs) are considered to be ideal for application in cell therapy or tissue regeneration, mainly due to their wide availability and easy access. In this study, we examined the anti-inflammatory effects of membrane-free stem cell extract (MFSC-Ex) derived from ADSCs against lipopolysaccharide (LPS)/interferon-gamma (IFN-γ) on RAW 264.7 macrophage cells. Exposure of RAW macrophages to LPS and IFN-γ stimuli induced high levels of nitric oxide (NO), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) production. However, pretreatment with MFSC-Ex inhibited LPS/IFN-γ-induced these pro-inflammatory mediators. To clarify the molecular mechanisms underlying the anti-inflammatory property of MFSC-Ex, we analyzed nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinases (MAPKs) protein expressions by Western blotting. Our study showed that treatment of MFSC-Ex significantly down-regulated inducible nitric oxide synthase (iNOS) and COX-2 protein expressions. Furthermore, phosphorylation of extracellular signal-regulated kinase (ERK) and p38 was also blocked by treatment with MFSC-Ex, indicating that inhibitory effect of MFSC-Ex on MAPK signaling cascade may attribute to inactivation of NF-κB. From these findings, we suggest that MFSC-Ex exert anti-inflammatory activities, which suppressed LPS/IFN-γ-induced production of NO, COX-2 and PGE2 by regulation of NF-κB and MAPK signaling pathway in RAW 264.7 macrophages. In conclusion, MFSC-Ex might provide a new therapeutic opportunity to treatment of inflammatory-related diseases.


Assuntos
Tecido Adiposo/citologia , Anti-Inflamatórios/farmacologia , Interferon gama/farmacologia , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Células-Tronco/metabolismo , Animais , Anti-Inflamatórios/química , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/biossíntese , Dinoprostona/biossíntese , Lipopolissacarídeos/imunologia , Macrófagos/imunologia , Camundongos , Modelos Biológicos , Substâncias Protetoras/metabolismo , Células RAW 264.7
7.
Int J Mol Sci ; 22(11)2021 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-34200169

RESUMO

BACKGROUND: Fullerenes and metallofullerenes can be considered promising nanopharmaceuticals themselves and as a basis for chemical modification. As reactive oxygen species homeostasis plays a vital role in cells, the study of their effect on genes involved in oxidative stress and anti-inflammatory responses are of particular importance. METHODS: Human fetal lung fibroblasts were incubated with aqueous dispersions of C60, C70, and Gd@C82 in concentrations of 5 nM and 1.5 µM for 1, 3, 24, and 72 h. Cell viability, intracellular ROS, NOX4, NFκB, PRAR-γ, NRF2, heme oxygenase 1, and NAD(P)H quinone dehydrogenase 1 expression have been studied. RESULTS & CONCLUSION: The aqueous dispersions of C60, C70, and Gd@C82 fullerenes are active participants in reactive oxygen species (ROS) homeostasis. Low and high concentrations of aqueous fullerene dispersions (AFD) have similar effects. C70 was the most inert substance, C60 was the most active substance. All AFDs have both "prooxidant" and "antioxidant" effects but with a different balance. Gd@C82 was a substance with more pronounced antioxidant and anti-inflammatory properties, while C70 had more pronounced "prooxidant" properties.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Fibroblastos/metabolismo , Fulerenos/farmacologia , Regulação da Expressão Gênica/efeitos dos fármacos , Células Cultivadas , Feto/efeitos dos fármacos , Feto/metabolismo , Fibroblastos/efeitos dos fármacos , Humanos , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Nanopartículas , Estresse Oxidativo , Espécies Reativas de Oxigênio/metabolismo , Água/química
8.
Int J Mol Sci ; 22(13)2021 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-34201683

RESUMO

Natural product is an excellent candidate for alternative medicine for disease management. The bulb of E. bulbosa is one of the notable Iridaceae family with a variety therapeutic potential that is widely cultivated in Southeast Asia. The bulb has been used traditionally among the Dayak community as a folk medicine to treat several diseases like diabetes, breast cancer, nasal congestion, and fertility problems. The bulb is exceptionally rich in phytochemicals like phenolic and flavonoid derivatives, naphthalene, anthraquinone, and naphthoquinone. The electronic database was searched using various keywords, i.e., E. bulbosa, E. americana, E. palmifolia, E. platifolia, and others due to the interchangeably used scientific names of different countries. Scientific investigations revealed that various pharmacological activities were recorded from the bulb of E. bulbosa including anti-cancer, anti-diabetic, anti-bacterial, anti-fungi, anti-viral, anti-inflammatory, dermatological problems, anti-oxidant, and anti-fertility. The potential application of the bulb in the food industry and in animal nutrition was also discussed to demonstrate its great versatility. This is a compact study and is the first study to review the extensive pharmacological activities of the E. bulbosa bulb and its potential applications. The development of innovative food and pharma products from the bulb of E. bulbosa is of great interest.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Iridaceae/química , Extratos Vegetais/farmacologia , Animais , Humanos
9.
Molecules ; 26(12)2021 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-34202929

RESUMO

Mexico is the center of origin of the species popularly known as toronjil or lemon balm (Agastache mexicana Linton & Epling). Two subspecies have been identified and are commonly called purple or red (Agastache mexicana Linton & Epling subspecies. mexicana) and white (Agastache mexicana subspecies xolocotziana Bye, E.L. Linares & Ramamoorthy). Plants from these subspecies differ in the size and form of inflorescence and leaves. They also possess differences in their chemical compositions, including volatile compounds. Traditional Mexican medicine employs both subspecies. A. mexicana exhibits a broad range of pharmacological properties, such as anti-inflammatory, anxiolytic, and antioxidant. A systematic vision of these plant's properties is discussed in this review, exposing its significant potential as a source of valuable bioactive compounds. Furthermore, this review provides an understanding of the elements that make up the species' holistic system to benefit from lemon balm sustainably.


Assuntos
Agastache/química , Agricultura , Anti-Inflamatórios/farmacologia , Biologia/normas , Inflorescência/efeitos dos fármacos , Compostos Fitoquímicos/química , Extratos Vegetais/farmacologia , Animais , Humanos , México , Fitoterapia , Extratos Vegetais/química , Folhas de Planta/química
10.
Artigo em Inglês | MEDLINE | ID: mdl-34204785

RESUMO

Although corticosteroids can serve as an effective anti-inflammatory adjuvant therapy, the role of adjunctive steroid therapy in pediatric bacterial meningitis in Taiwan remains under-investigated. Cases of acute bacterial meningitis, aged between 1 month and 20 years, were divided into a steroid group (empirical antibiotics with adjunctive steroid therapy) and a non-steroid group (empirical antibiotics only). Data were identified from the annual hospitalization discharge claims of the National Health Insurance Research Database using the International Classification of Diseases, Ninth Revision codes. Of the 8083 episodes enrolled in this study, 26% (2122/8083) and 74% (5961/8083) were divided into the steroid and non-steroid groups, respectively. The fatality rates were 7.9% in the steroid group and 1.7% in the non-steroid group during hospitalization (p < 0.0001). In the steroid and non-steroid groups, the median length of hospital stay was 13 and 6 days, respectively (p < 0.0001). Medical costs (median (interquartile range)) of hospitalization were 77,941 (26,647-237,540) and 26,653 (14,287-53,421) New Taiwan dollars in the steroid and non-steroid groups, respectively (p < 0.0001). The steroid group had a more fulminant course at baseline, a higher fatality rate, length of hospital stay, and medical cost of hospitalization. Therefore, the beneficial effects of the adjunctive use of corticosteroids in pediatric bacterial meningitis are inconclusive, and additional prospective multicenter investigations are required to clarify this issue.


Assuntos
Meningites Bacterianas , Anti-Inflamatórios/uso terapêutico , Criança , Humanos , Lactente , Meningites Bacterianas/tratamento farmacológico , Meningites Bacterianas/epidemiologia , Estudos Prospectivos , Esteroides/uso terapêutico , Taiwan/epidemiologia
11.
Biomolecules ; 11(6)2021 06 08.
Artigo em Inglês | MEDLINE | ID: mdl-34201172

RESUMO

The phytotherapeutic properties of Glycyrrhiza glabra (licorice) extract are mainly attributed to glycyrrhizin (GR) and glycyrrhetinic acid (GA). Among their possible pharmacological actions, the ability to act against viruses belonging to different families, including SARS coronavirus, is particularly important. With the COVID-19 emergency and the urgent need for compounds to counteract the pandemic, the antiviral properties of GR and GA, as pure substances or as components of licorice extract, attracted attention in the last year and supported the launch of two clinical trials. In silico docking studies reported that GR and GA may directly interact with the key players in viral internalization and replication such as angiotensin-converting enzyme 2 (ACE2), spike protein, the host transmembrane serine protease 2, and 3-chymotrypsin-like cysteine protease. In vitro data indicated that GR can interfere with virus entry by directly interacting with ACE2 and spike, with a nonspecific effect on cell and viral membranes. Additional anti-inflammatory and antioxidant effects of GR cannot be excluded. These multiple activities of GR and licorice extract are critically re-assessed in this review, and their possible role against the spread of the SARS-CoV-2 and the features of COVID-19 disease is discussed.


Assuntos
Anti-Inflamatórios/farmacologia , Antivirais/farmacologia , COVID-19/tratamento farmacológico , Ácido Glicirretínico/farmacologia , Ácido Glicirrízico/farmacologia , SARS-CoV-2/efeitos dos fármacos , Enzima de Conversão de Angiotensina 2/metabolismo , Animais , Anti-Inflamatórios/uso terapêutico , Antivirais/uso terapêutico , COVID-19/metabolismo , Ácido Glicirretínico/uso terapêutico , Glycyrrhiza/química , Ácido Glicirrízico/uso terapêutico , Humanos , SARS-CoV-2/metabolismo , Glicoproteína da Espícula de Coronavírus/metabolismo , Internalização do Vírus/efeitos dos fármacos
12.
Molecules ; 26(12)2021 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-34205312

RESUMO

In the current study, in vitro antimicrobial and antioxidant activities and in vivo anti-inflammatory and analgesic activities of Scutellaria edelbergii Rech. f. (crude extract and subfractions, i.e., n-hexane, ethyl acetate (EtOAc), chloroform, n-butanol (n-BuOH) and aqueous) were explored. Initially, extraction and fractionation of the selected medicinal plant were carried out, followed by phytochemical qualitative tests, which were mostly positive for all the extracts. EtOAc fraction possessed a significant amount of phenolic (79.2 ± 0.30 mg GAE/g) and flavonoid (84.0 ± 0.39 mg QE/g) content. The EtOAc fraction of S. edelbergii exhibited appreciable antibacterial activity against Gram-negative (Escherichia coli and Klebsiella pneumoniae) strains and significant zones of inhibition were observed against Gram-positive bacterial strains (Bacillus subtilis and Staphylococcus aureus). However, it was found inactive against Candida Albicans and Fusarium oxysporum fungal strains. The chloroform fraction was the most effective with an IC50 value of 172 and 74 µg/mL against DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays, in comparison with standard ascorbic acid 59 and 63 µg/mL, respectively. Moreover, the EtOAc fraction displayed significant in vivo anti-inflammatory activity (54%) using carrageenan-induced assay and significant (55%) in vivo analgesic activity using acetic acid-induced writing assay. In addition, nine known compounds, ursolic acid (UA), ovaul (OV), oleanolic acid (OA), ß-sitosterol (BS), micromeric acid (MA), taraxasterol acetate (TA), 5,3',4'-trihydroxy-7-methoxy flavone (FL-1), 5,7,4'-trihydroxy-6,3'-dimiethoxyflavone (FL-2) and 7-methoxy catechin (FL-3), were isolated from methanolic extract of S. edelbergii. These constituents have never been obtained from this source. The structures of all the isolated constituents were elucidated by spectroscopic means. In conclusion, the EtOAc fraction and all other fractions of S. edelbergii, in general, displayed a significant role as antibacterial, free radical scavenger, anti-inflammatory and analgesic agents which may be due to the presence of these constituents and other flavonoids.


Assuntos
Extratos Vegetais/farmacologia , Scutellaria/química , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Pesquisa Biomédica/métodos , Flavonoides/farmacologia , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Fenóis/farmacologia , Compostos Fitoquímicos/farmacologia , Plantas Medicinais/química
13.
Molecules ; 26(12)2021 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-34205626

RESUMO

Alkaloids are a group of secondary metabolites that have been widely studied for the discovery of new drugs due to their properties on the central nervous system and their anti-inflammatory, antioxidant and anti-cancer activities. Molecular docking was performed for 10 indole alkaloids identified in the ethanol extract of Tabernaemontana cymosa Jacq. with 951 human targets involved in different diseases. The results were analyzed through the KEGG and STRING databases, finding the most relevant physiological associations for alkaloids. The molecule 5-oxocoronaridine proved to be the most active molecule against human proteins (binding energy affinity average = -9.2 kcal/mol) and the analysis of the interactions between the affected proteins pointed to the PI3K/ Akt/mTOR signaling pathway as the main target. The above indicates that indole alkaloids from T. cymosa constitute a promising source for the search and development of new treatments against different types of cancer.


Assuntos
Alcaloides Indólicos/farmacologia , Extratos Vegetais/farmacologia , Tabernaemontana/química , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Humanos , Simulação de Acoplamento Molecular , Transdução de Sinais/efeitos dos fármacos
14.
Molecules ; 26(12)2021 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-34201056

RESUMO

The present investigation aimed to provide novel information on the chemical composition and in vitro bioaccessibility of bioactive compounds from raw citrus pomaces (mandarin varieties Clemenule and Ortanique and orange varieties Navel and Valencia). The effects of the baking process on their bioaccessibility was also assessed. Samples of pomaces and biscuits containing them as an ingredient were digested, mimicking the human enzymatic oral gastrointestinal digestion process, and the composition of the digests were analyzed. UHPLC-MS/MS results of the citrus pomaces flavonoid composition showed nobiletin, hesperidin/neohesperidin, tangeretin, heptamethoxyflavone, tetramethylscutellarein, and naringin/narirutin. The analysis of the digests indicated the bioaccessibility of compounds possessing antioxidant [6.6-11.0 mg GAE/g digest, 65.5-97.1 µmol Trolox Equivalents (TE)/g digest, and 135.5-214.8 µmol TE/g digest for total phenol content (TPC), ABTS, and ORAC-FL methods, respectively; significant reduction (p < 0.05) in Reactive Oxygen Species (ROS) formation under tert-butyl hydroperoxide (1 mM)-induced conditions in IEC-6 and CCD-18Co cells when pre-treated with concentrations 5-25 µg/mL of the digests], anti-inflammatory [significant reduction (p < 0.05) in nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 macrophages], and antidiabetic (IC50 3.97-11.42 mg/mL and 58.04-105.68 mg/mL for α-glucosidase and α-amylase inhibition capacities) properties in the citrus pomaces under study. In addition, orange pomace biscuits with the nutrition claims "no-added sugars" and "source of fiber", as well as those with good sensory quality (6.9-6.7, scale 1-9) and potential health promoting properties, were obtained. In conclusion, the results supported the feasibility of citrus pomace as a natural sustainable source of health-promoting compounds such as flavonoids. Unfractionated orange pomace may be employed as a functional food ingredient for reducing the risk of pathophysiological processes linked to oxidative stress, inflammation, and carbohydrate metabolism, such as diabetes, among others.


Assuntos
Citrus sinensis/química , Citrus/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Linhagem Celular , Cromatografia Líquida de Alta Pressão/métodos , Digestão/fisiologia , Flavonoides/química , Flavonoides/farmacologia , Frutas/química , Trato Gastrointestinal/fisiologia , Humanos , Camundongos , Estresse Oxidativo/efeitos dos fármacos , Células RAW 264.7 , Espectrometria de Massas em Tandem/métodos
15.
Molecules ; 26(12)2021 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-34201147

RESUMO

Many plants that are commonly used in folk medicine have multidirectional biological properties confirmed by scientific research. One of them is Aerva lanata (L.) Juss. (F. Amaranthaceae). It is widely used, but there are very few scientific data about its chemical composition and pharmacological activity. The aim of the present study was to investigate the chemical composition of phenolic acid (PA)-rich fractions isolated from methanolic extracts of A. lanata (L.) Juss. herb using the liquid/liquid extraction method and their potential antioxidant, anti-inflammatory, and anti-diabetic properties. The free PA fraction (FA), the PA fraction (FB) released after acid hydrolysis, and the PA fraction (FC) obtained after alkaline hydrolysis were analysed using liquid chromatography/electrospray ionization triple quadrupole mass spectrometry (LC-ESI-MS/MS). The phenolic profile of each sample showed a high concentration of PAs and their presence in A. lanata (L.) Juss. herb mainly in bound states. Thirteen compounds were detected and quantified in all samples, including some PAs that had not been previously detected in this plant species. Bioactivity assays of all fractions revealed high 2,2-diphenyl-1-picrylhydrazyl (DPPH•) (2.85 mM Trolox equivalents (TE)/g) and 2,2-azino-bis-3(ethylbenzthiazoline-6-sulphonic acid) (ABTS•+) (2.88 mM TE/g) scavenging activity. Fraction FB definitely exhibited not only the highest antiradical activity but also the strongest xanthine oxidase (XO) (EC50 = 1.77 mg/mL) and lipoxygenase (LOX)(EC50 = 1.88 mg/mL) inhibitory potential. The fraction had the best anti-diabetic properties, i.e., mild inhibition of α-amylase (EC50 = 7.46 mg/mL) and strong inhibition of α-glucosidase (EC50 = 0.30 mg/mL). The activities of all analysed samples were strongly related to the presence of PA compounds and the total PA content.


Assuntos
Amaranthaceae/química , Anti-Inflamatórios/química , Antioxidantes/química , Hidroxibenzoatos/química , Hipoglicemiantes/química , Extratos Vegetais/química , Flavonoides/química , Lipoxigenase/química , Medicina Tradicional/métodos , Metanol/química , Fenóis/química , Xantina Oxidase/química , alfa-Amilases/química , alfa-Glucosidases/química
16.
Molecules ; 26(12)2021 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-34201193

RESUMO

Ehretia laevis Roxb. (Boraginaceae) has been extensively used as a traditional remedy for the treatment of a diverse range of ailments related to the respiratory system, the gastrointestinal tract, the reproductive system, and against several infections. This review critically assesses and documents, for the first time, the fragmented information on E. laevis, including its botanical description, folklore uses, bioactive phyto metabolites and pharmacological activities. The goal is to explore this plant therapeutically. Ethnomedicinal surveys reveal that E. laevis has been used by tribal communities in Asian countries for the treatment of various disorders. Quantitative and qualitative phytochemical investigations of E. laevis showed the presence of important phytoconstituents such as pentacyclic triterpenoids, phenolic acids, flavonoids, fatty acids, steroids, alkaloids, aliphatic alcohols, hydrocarbons, amino acids, carbohydrates, vitamins and minerals. Fresh plant parts, crude extracts, fractions and isolated compounds have been reported to exhibit broad spectrum of therapeutic activities viz., antioxidant, antiarthritic, antidiabetic, anti-inflammatory, antiulcer, antidiarrheal, antidysenteric, wound healing and anti-infective activities. E. laevis is shown to be an excellent potential source of drugs for the mitigation of jaundice, asthma, dysentery, ulcers, diarrhea, ringworm, eczema, diabetes, fissure, syphilis, cuts and wounds, inflammation, liver problems, venereal and infectious disorders. Although few investigations authenticated its traditional uses but employed uncharacterized crude extracts of the plant, the major concerns raised are reproducibility of therapeutic efficacy and safety of plant material. The outcomes of limited pharmacological screening and reported bioactive compounds of E. laevis suggest that there is an urgent need for in-depth pharmacological investigations of the plant.


Assuntos
Boraginaceae/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Ásia , Etnofarmacologia/métodos , Humanos , Medicina Tradicional/métodos , Reprodutibilidade dos Testes
17.
Int J Mol Sci ; 22(12)2021 Jun 17.
Artigo em Inglês | MEDLINE | ID: mdl-34204506

RESUMO

Ergosta-7, 9 (11), 22-trien-3ß-ol (EK100) was isolated from Cordyceps militaris, which has been used as a traditional anti-inflammatory medicine. EK100 has been reported to attenuate inflammatory diseases, but its anti-inflammatory mechanism is still unclear. We were the first to investigate the effect of EK100 on the Toll-like receptor 4 (TLR4)/nuclear factor of the κ light chain enhancer of B cells (NF-κB) signaling in the lipopolysaccharide (LPS)-stimulated RAW264.7 cells and the green fluorescent protein (GFP)-labeled NF-κB reporter gene of Drosophila. EK100 suppressed the release of the cytokine and attenuated the mRNA and protein expression of pro-inflammatory mediators. EK100 inhibited the inhibitor kappa B (IκB)/NF-κB signaling pathway. EK100 also inhibited phosphatidylinositol-3-kinase (PI3K)/Protein kinase B (Akt) signal transduction. Moreover, EK100 interfered with LPS docking to the LPS-binding protein (LBP), transferred to the cluster of differentiation 14 (CD14), and bonded to TLR4/myeloid differentiation-2 (MD-2) co-receptors. Compared with the TLR4 antagonist, resatorvid (CLI-095), and dexamethasone (Dexa), EK100 suppressed the TLR4/AKT signaling pathway. In addition, we also confirmed that EK100 attenuated the GFP-labeled NF-κB reporter gene expression in Drosophila. In summary, EK100 might alter LPS docking to LBP, CD14, and TLR4/MD-2 co-receptors, and then it suppresses the TLR4/NF-κB inflammatory pathway in LPS-stimulated RAW264.7 cells and Drosophila.


Assuntos
Anti-Inflamatórios/farmacologia , Drosophila/metabolismo , Receptores de Lipopolissacarídeos/metabolismo , Antígeno 96 de Linfócito/metabolismo , NF-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos , Receptor 4 Toll-Like/metabolismo , Animais , Anti-Inflamatórios/química , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Citocinas/metabolismo , Mediadores da Inflamação/metabolismo , Receptores de Lipopolissacarídeos/química , Lipopolissacarídeos/química , Lipopolissacarídeos/imunologia , Antígeno 96 de Linfócito/química , Macrófagos/imunologia , Macrófagos/metabolismo , Camundongos , Modelos Moleculares , Conformação Molecular , Óxido Nítrico Sintase Tipo II/metabolismo , Fosforilação , Ligação Proteica , Relação Estrutura-Atividade , Receptor 4 Toll-Like/química
18.
Molecules ; 26(11)2021 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-34200200

RESUMO

Epilobium angustifolium L. is a popular and well-known medicinal plant. In this study, an attempt to evaluate the possibility of using this plant in preparations for the care and treatment of skin diseases was made. The antioxidant, antiaging and anti-inflammatory properties of ethanolic extracts from Epilobium angustifolium (FEE) were assessed. Qualitative and quantitative evaluation of extracts chemically composition was performed by gas chromatography with mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC). The total polyphenol content (TPC) of biologically active compounds, such as the total content of polyphenols (TPC), flavonoids (TFC), and assimilation pigments, as well as selected phenolic acids, was assessed. FEE was evaluated for their anti-inflammatory and antiaging properties, achieving 68% inhibition of lipoxygenase activity, 60% of collagenase and 49% of elastase. FEE also showed high antioxidant activity, reaching to 87% of free radical scavenging using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 59% using 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Additionally, in vitro penetration studies were performed using two vehicles, i.e., a hydrogel and an emulsion containing FEE. These studies showed that the active ingredients contained in FEE penetrate through human skin and accumulate in it. The obtained results indicate that E. angustifolium may be an interesting plant material to be applied as a component of cosmetic and dermatological preparations with antiaging and anti-inflammatory properties.


Assuntos
Cosméticos/química , Fármacos Dermatológicos/química , Epilobium/química , Extratos Vegetais/química , Anti-Inflamatórios/química , Antioxidantes/química , Compostos de Bifenilo/química , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Humanos , Plantas Medicinais/química , Polifenóis/química , Pele/efeitos dos fármacos
19.
Molecules ; 26(12)2021 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-34200764

RESUMO

The cyclooxygenase-2 (COX-2) enzyme is an important target for drug discovery and development of novel anti-inflammatory agents. Selective COX-2 inhibitors have the advantage of reduced side-effects, which result from COX-1 inhibition that is usually observed with nonselective COX inhibitors. In this study, the design and synthesis of a new series of 7-methoxy indolizines as bioisostere indomethacin analogues (5a-e) were carried out and evaluated for COX-2 enzyme inhibition. All the compounds showed activity in micromolar ranges, and the compound diethyl 3-(4-cyanobenzoyl)-7-methoxyindolizine-1,2-dicarboxylate (5a) emerged as a promising COX-2 inhibitor with an IC50 of 5.84 µM, as compared to indomethacin (IC50 = 6.84 µM). The molecular modeling study of indolizines indicated that hydrophobic interactions were the major contribution to COX-2 inhibition. The title compound diethyl 3-(4-bromobenzoyl)-7-methoxyindolizine-1,2-dicarboxylate (5c) was subjected for single-crystal X-ray studies, Hirshfeld surface analysis, and energy framework calculations. The X-ray diffraction analysis showed that the molecule (5c) crystallizes in the monoclinic crystal system with space group P 21/n with a = 12.0497(6)Å, b = 17.8324(10)Å, c = 19.6052(11)Å, α = 90.000°, ß = 100.372(1)°, γ = 90.000°, and V = 4143.8(4)Å3. In addition, with the help of Crystal Explorer software program using the B3LYP/6-31G(d, p) basis set, the theoretical calculation of the interaction and graphical representation of energy value was measured in the form of the energy framework in terms of coulombic, dispersion, and total energy.


Assuntos
Inibidores de Ciclo-Oxigenase 2/química , Indolizinas/química , Anti-Inflamatórios/química , Cristalografia por Raios X/métodos , Ciclo-Oxigenase 2/metabolismo , Humanos , Interações Hidrofóbicas e Hidrofílicas , Indometacina/química , Relação Estrutura-Atividade
20.
Molecules ; 26(12)2021 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-34200882

RESUMO

The occurrence of microbial challenges in commercial poultry farming causes significant economic losses. Antibiotics have been used to control diseases involving bacterial infection in poultry. As the incidence of antibiotic resistance turns out to be a serious problem, there is increased pressure on producers to reduce antibiotic use. With the reduced availability of antibiotics, poultry producers are looking for feed additives to stimulate the immune system of the chicken to resist microbial infection. Some ß-glucans have been shown to improve gut health, to increase the flow of new immunocytes, increase macrophage function, stimulate phagocytosis, affect intestinal morphology, enhance goblet cell number and mucin-2 production, induce the increased expression of intestinal tight-junctions, and function as effective anti-inflammatory immunomodulators in poultry. As a result, ß-glucans may provide a new tool for producers trying to reduce or eliminate the use of antibiotics in fowl diets. The specific activity of each ß-glucan subtype still needs to be investigated. Upon knowledge, optimal ß-glucan mixtures may be implemented in order to obtain optimal growth performance, exert anti-inflammatory and immunomodulatory activity, and optimized intestinal morphology and histology responses in poultry. This review provides an extensive overview of the current use of ß glucans as additives and putative use as antibiotic alternative in poultry.


Assuntos
Antibacterianos/farmacologia , beta-Glucanas/farmacologia , Ração Animal , Animais , Anti-Inflamatórios/farmacologia , Humanos , Fatores Imunológicos/farmacologia , Carne , Aves Domésticas
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