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1.
Biomolecules ; 11(8)2021 08 23.
Artigo em Inglês | MEDLINE | ID: mdl-34439920

RESUMO

In 2019, COVID-19 emerged as a severe respiratory disease that is caused by the novel coronavirus, Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). The disease has been associated with high mortality rate, especially in patients with comorbidities such as diabetes, cardiovascular and kidney diseases. This could be attributed to dysregulated immune responses and severe systemic inflammation in COVID-19 patients. The use of effective antiviral drugs against SARS-CoV-2 and modulation of the immune responses could be a potential therapeutic strategy for COVID-19. Studies have shown that natural phenolic compounds have several pharmacological properties, including anticoronavirus and immunomodulatory activities. Therefore, this review discusses the dual action of these natural products from the perspective of applicability at COVID-19.


Assuntos
Antivirais/uso terapêutico , COVID-19/tratamento farmacológico , Flavonoides/uso terapêutico , Fatores Imunológicos/uso terapêutico , Compostos Fitoquímicos/uso terapêutico , Inibidores de Proteases/uso terapêutico , Animais , Antivirais/química , Antivirais/farmacologia , Coronavirus/efeitos dos fármacos , Flavonoides/química , Flavonoides/farmacologia , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Inibidores de Proteases/química , Inibidores de Proteases/farmacologia
2.
Molecules ; 26(12)2021 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-34203004

RESUMO

Green tea and its bioactive components, especially polyphenols, possess many health-promoting and disease-preventing benefits, especially anti-inflammatory, antioxidant, anticancer, and metabolic modulation effects with multi-target modes of action. However, the effect of tea polyphenols on immune function has not been well studied. Moreover, the underlying cellular and molecular mechanisms mediating immunoregulation are not well understood. This review summarizes the recent studies on the immune-potentiating effects and corresponding mechanisms of tea polyphenols, especially the main components of (-)-epigallocatechin-3-gallate (EGCG) and (-)-epicatechin-3-gallate (ECG). In addition, the benefits towards immune-related diseases, such as autoimmune diseases, cutaneous-related immune diseases, and obesity-related immune diseases, have been discussed.


Assuntos
Antioxidantes/farmacologia , Imunidade/efeitos dos fármacos , Fatores Imunológicos/farmacologia , Polifenóis/farmacologia , Chá/química , Animais , Antioxidantes/química , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Catequina/análogos & derivados , Catequina/química , Catequina/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Humanos , Fatores Imunológicos/química , Polifenóis/química
3.
Int J Mol Sci ; 22(13)2021 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-34281277

RESUMO

The aim of this research was to analyze the heterologous expression, purification, and immunoregulatory activity of recombinant YGP40 (rYGP40), the potential precursor of the yolkin peptide complex. The ygp40 coding sequence was codon optimized, successfully expressed in the E. coli system, and purified from inclusion bodies with a yield of about 1.1 mg/L of culture. This study showed that the protein exhibits immunomodulatory activity, expressed by the stimulation of TNF-α and IL-10 production and nitric oxide induction at a level comparable to that of the natural yolkin peptide complex obtained by other authors from hen egg yolk. At the highest dose of 100 µg/mL, rYGP40 also caused the up-regulation of iNOS expression in murine bone marrow-derived macrophages (BMDM). Moreover, no cytotoxic effects of rYGP40 on the BMDM cell line were observed.


Assuntos
Vitelogeninas/química , Animais , Sobrevivência Celular/efeitos dos fármacos , Galinhas , Clonagem Molecular , Gema de Ovo/química , Feminino , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/genética , Fatores Imunológicos/farmacologia , Técnicas In Vitro , Interleucina-10/biossíntese , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Macrófagos/metabolismo , Camundongos , Peso Molecular , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/metabolismo , Fragmentos de Peptídeos/química , Fragmentos de Peptídeos/genética , Fragmentos de Peptídeos/farmacologia , Proteínas Recombinantes/química , Proteínas Recombinantes/genética , Proteínas Recombinantes/farmacologia , Fator de Necrose Tumoral alfa/biossíntese , Vitelogeninas/genética , Vitelogeninas/farmacologia
4.
Molecules ; 26(13)2021 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-34202367

RESUMO

Carvacrol (CV) is an essential oil with numerous therapeutic properties, including immunomodulatory activity. However, this effect has not been studied in nanoemulsion systems. The objective of this study was to develop an innovative carvacrol-loaded nanoemulsion (CVNE) for immunomodulatory action. The developed CVNE comprised of 5% w/w oily phase (medium chain triglycerides + CV), 2% w/w surfactants (Tween 80®/Span 80®), and 93% w/w water, and was produced by ultrasonication. Dynamic light scattering over 90 days was used to characterize CVNE. Cytotoxic activity and quantification of cytokines were evaluated in peripheral blood mononuclear cell (PBMC) culture supernatants. CVNE achieved a drug loading of 4.29 mg/mL, droplet size of 165.70 ± 0.46 nm, polydispersity index of 0.14 ± 0.03, zeta potential of -10.25 ± 0.52 mV, and good stability for 90 days. CVNE showed no cytotoxicity at concentrations up to 200 µM in PBMCs. CV diminished the production of IL-2 in the PBMC supernatant. However, CVNE reduced the levels of the pro-inflammatory cytokines IL-2, IL-17, and IFN-γ at 50 µM. In conclusion, a stable CVNE was produced, which improved the CV immunomodulatory activity in PBMCs.


Assuntos
Cimenos , Citocinas/metabolismo , Fatores Imunológicos , Leucócitos Mononucleares/metabolismo , Nanopartículas/química , Cimenos/química , Cimenos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Emulsões , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Polissorbatos/química , Polissorbatos/farmacologia
5.
Fish Shellfish Immunol ; 115: 179-188, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34153430

RESUMO

Propolis is a viscous, waxy, resinous substance that is produced from the exudates of flowers and buds by the action of salivary enzymes of honey bees. Propolis may differ in color (brown, red or green), with color being influenced by the chemical composition and age of the product. Propolis has a special distinctive odor owing to the high concentration of volatile essential oils. It is composed of 5% pollen grains, 10% essential and aromatic oils, 30% wax, 50% resin and balsams, and other minor trace substances. Natural propolis products may be useful for a range of applications in aquaculture systems instead of relying on the application of synthetic compounds to manage many ailments that affect business profitability. It has been reported in several studies that propolis enhances performance, economics, immunity response and disease resistance in different fish species. This present review discusses the functional actions of propolis and the prospects of its use as an antimicrobial, antioxidant, immune-modulatory, antiseptic, antiparasitic, anti-inflammatory and food additive in aquaculture production. In summary, propolis could be a natural supplement that has the potential to improve fish health status and immunity thereby enhancing growth and productivity of the fish industry as well as economic efficiency.


Assuntos
Aquicultura , Peixes/fisiologia , Própole/administração & dosagem , Própole/química , Fenômenos Fisiológicos da Nutrição Animal , Animais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/química , Anti-Infecciosos Locais/administração & dosagem , Anti-Infecciosos Locais/química , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Antioxidantes/administração & dosagem , Antioxidantes/química , Antiparasitários/administração & dosagem , Antiparasitários/química , Aditivos Alimentares/administração & dosagem , Aditivos Alimentares/química , Fatores Imunológicos/administração & dosagem , Fatores Imunológicos/química
6.
Biomed Pharmacother ; 140: 111774, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34062409

RESUMO

The present article reviews and compares the immunomodulatory activities of Crocus sativus (C. sativus) and Nigella sativa (N. sativa) and their main bioactive compounds. Immunomodulatory effects of these plants, especially with respect to Th1 and Th2 cytokines, are discussed based on relevant articles, books, and conference papers published in English until the end of April 2020, that were retrieved from Web of Science, PubMed, Scopus and Google Scholar databases. C. sativus and its constituents increase immunoglobulin (Ig-)G, interleukin 2 (IL)-2, interferon gamma (IFN-γ), and IFN-γ/IL-4 ratio, but decreased IgM, IL-10 and IL-4 secretion. N. sativa extract and thymoquinone reduce the levels of IL-2, -4, -10, and -12, while enhance IFN-γ and serum IgG1 and 2a. The reviewed articles indicate that C. sativus and N. sativa and their constituents could be potentially considered promising treatments for disorders associated with immune-dysregulation such as asthma and cancer.


Assuntos
Crocus , Doenças do Sistema Imunitário/tratamento farmacológico , Fatores Imunológicos/uso terapêutico , Nigella sativa , Extratos Vegetais/uso terapêutico , Animais , Crocus/química , Humanos , Doenças do Sistema Imunitário/imunologia , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Nigella sativa/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/farmacologia
7.
Cell Physiol Biochem ; 55(S3): 108-130, 2021 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-34043299

RESUMO

Transient receptor potential vanilloid (TRPV) channels are part of the TRP channel superfamily and named after the first identified member TRPV1, that is sensitive to the vanillylamide capsaicin. Their overall structure is similar to the structure of voltage gated potassium channels (Kv) built up as homotetramers from subunits with six transmembrane helices (S1-S6). Six TRPV channel subtypes (TRPV1-6) are known, that can be subdivided into the thermoTRPV (TRPV1-4) and the Ca2+-selective TRPV channels (TRPV5, TRPV6). Contrary to Kv channels, TRPV channels are not primary voltage gated. All six channels have distinct properties and react to several endogenous ligands as well as different gating stimuli such as heat, pH, mechanical stress, or osmotic changes. Their physiological functions are highly diverse and subtype as well as tissue specific. In many tissues they serve as sensors for different pain stimuli (heat, pressure, pH) and contribute to the homeostasis of electrolytes, the maintenance of barrier functions and the development of macrophages. Due to their fundamental role in manifold physiological and pathophysiological processes, TRPV channels are promising targets for drug development. However, drugs targeting specific TRPV channels, that are suitable for drug therapy, are rare. Moreover, selective and potent compounds for further research at TRPV channels are often lacking. In this review different aspects of the structure, the different gating stimuli, the expression pattern, the physiological and pathophysiological roles as well as the modulating mechanisms of synthetic, natural and endogenous ligands are summarized.


Assuntos
Analgésicos/farmacologia , Antineoplásicos/farmacologia , Fatores Imunológicos/farmacologia , Moduladores de Transporte de Membrana/farmacologia , Canais de Cátion TRPV/metabolismo , Analgésicos/química , Analgésicos/classificação , Antineoplásicos/química , Antineoplásicos/classificação , Sítios de Ligação , Encéfalo/citologia , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/classificação , Ativação do Canal Iônico/efeitos dos fármacos , Ligantes , Pulmão/citologia , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Moduladores de Transporte de Membrana/química , Moduladores de Transporte de Membrana/classificação , Modelos Moleculares , Especificidade de Órgãos , Ligação Proteica , Isoformas de Proteínas/agonistas , Isoformas de Proteínas/antagonistas & inibidores , Isoformas de Proteínas/classificação , Isoformas de Proteínas/metabolismo , Estrutura Secundária de Proteína , Baço/citologia , Baço/efeitos dos fármacos , Baço/metabolismo , Canais de Cátion TRPV/agonistas , Canais de Cátion TRPV/antagonistas & inibidores , Canais de Cátion TRPV/classificação
8.
Chem Pharm Bull (Tokyo) ; 69(5): 421-431, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33952852

RESUMO

Rosa laevigata Michx., a medicinal and edible plant in China, has exerted a variety of medicinal values and health benefits. This present review aims to achieve a comprehensive and up-to-date investigation in the phytochemistry and pharmacology of R. laevigata. According to these findings in the literature, approximately 123 chemical ingredients covering triterpenoids, flavonoids, tannis, lignans and polysaccharides, have been characterized from various parts of this species. Among these isolates, 77 triterpenoids have been isolated and thus regarded as the primary and characteristic substance. Based on the chemical structures, most of the obtained triterpenoids can be classified into polyhydroxy triterpenoids and readily divided into four categories: ursane-type, oleanane-type, lupinane-type, as well as seco-triterpenoids. The crude extracts and the purified compounds have demonstrated various pharmacological effects in vitro and in vivo, such as antioxidant activity, immunomodulatory effect, anti-inflammatory effect, liver protection, kidney protection, cardiovascular protection, neuroprotective effect and improvement of diabetic cataract. Noticeably, these pharmacological results of R. laevigata provide evidences for its traditional uses. In addition, these different chemical ingredients existing in the title plant may have synergistic effects. In conclusion, the chemical profiles, including ingredients and structures, together with the modern pharmacological properties have been adequately summarized. These evidences have revealed this plant to be a valuable source for therapeutic foodstuff and more attention should be paid to a better utilization of this plant.


Assuntos
Compostos Fitoquímicos/farmacologia , Plantas Comestíveis/química , Plantas Medicinais/química , Rosa/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/isolamento & purificação , Fatores Imunológicos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Substâncias Protetoras/química , Substâncias Protetoras/isolamento & purificação , Substâncias Protetoras/farmacologia
9.
Int J Biol Macromol ; 183: 1753-1773, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34048833

RESUMO

The deficiency of chemical-synthesized antiviral drugs when applied in clinical therapy, such as drug resistance, and the lack of effective antiviral drugs to treat some newly emerging virus infections, such as COVID-19, promote the demand of novelty and safety anti-virus drug candidate from natural functional ingredient. Numerous studies have shown that some polysaccharides sourcing from edible and medicinal fungus (EMFs) exert direct or indirect anti-viral capacities. However, the internal connection of fungus type, polysaccharides structural characteristics, action mechanism was still unclear. Herein, our review focus on the two aspects, on the one hand, we discussed the type of anti-viral EMFs and the structural characteristics of polysaccharides to clarify the structure-activity relationship, on the other hand, the directly or indirectly antiviral mechanism of EMFs polysaccharides, including virus function suppression, immune-modulatory activity, anti-inflammatory activity, regulation of population balance of gut microbiota have been concluded to provide a comprehensive theory basis for better clinical utilization of EMFs polysaccharides as anti-viral agents.


Assuntos
Agaricales/química , Anti-Inflamatórios , Antivirais , COVID-19/tratamento farmacológico , Polissacarídeos Fúngicos , Fatores Imunológicos , SARS-CoV-2/imunologia , Anti-Inflamatórios/química , Anti-Inflamatórios/classificação , Anti-Inflamatórios/uso terapêutico , Antivirais/química , Antivirais/classificação , Antivirais/uso terapêutico , COVID-19/imunologia , COVID-19/prevenção & controle , Polissacarídeos Fúngicos/química , Polissacarídeos Fúngicos/classificação , Polissacarídeos Fúngicos/uso terapêutico , Microbioma Gastrointestinal/efeitos dos fármacos , Microbioma Gastrointestinal/imunologia , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/classificação , Fatores Imunológicos/uso terapêutico
10.
Food Chem ; 358: 129883, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-33940295

RESUMO

Lentinus edodes, an important edible mushroom cultivated in East Asia for thousands of years, has been widely used as food and medicinal ingredient worldwide. Modern phytochemistry studies have demonstrated that L. edodes is very rich in bioactive polysaccharides, especially the ß-glucans. Over the past two decades, the isolation, chemical properties, and bioactivities of polysaccharides from fruiting bodies, mycelium and fermentation broth of L. edodes have been drawing much attention from scholars around the world. It has been demonstrated that L. edodes polysaccharides possess various remarkable biological activities, including anti-oxidant, anti-tumor, anti-aging, anti-inflammation, immunomodulatory, antiviral, and hepatoprotection effects. This review summarizes the recent development of polysaccharides from L. edodes including the isolation methods, structural features, bioactivities and mechanisms, and their structure-activity relationship, which can provide useful research underpinnings and update information for their further application as therapeutic agents and functional foods.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Polissacarídeos Fúngicos/química , Polissacarídeos Fúngicos/farmacologia , Cogumelos Shiitake/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos/química , Antioxidantes/química , Antivirais/química , Antivirais/farmacologia , Alimento Funcional , Polissacarídeos Fúngicos/isolamento & purificação , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Micélio/química , Relação Estrutura-Atividade , beta-Glucanas/química , beta-Glucanas/farmacologia
11.
Carbohydr Res ; 505: 108326, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34015720

RESUMO

The viral infection caused by SARS-CoV-2 has increased the mortality rate and engaged several adverse effects on the affected individuals. Currently available antiviral drugs have found to be unsuccessful in the treatment of COVID-19 patients. The demand for efficient antiviral drugs has created a huge burden on physicians and health workers. Plasma therapy seems to be less accomplishable due to insufficient donors to donate plasma and low recovery rate from viral infection. Repurposing of antivirals has been evolved as a suitable strategy in the current treatment and preventive measures. The concept of drug repurposing represents new experimental approaches for effective therapeutic benefits. Besides, SARS-CoV-2 exhibits several complications such as lung damage, blood clot formation, respiratory illness and organ failures in most of the patients. Based on the accumulation of data, sulfated marine polysaccharides have exerted successful inhibition of virus entry, attachment and replication with known or unknown possible mechanisms against deadly animal and human viruses so far. Since the virus entry into the host cells is the key process, the prevention of such entry mechanism makes any antiviral strategy effective. Enveloped viruses are more sensitive to polyanions than non-enveloped viruses. Besides, the viral infection caused by RNA virus types embarks severe oxidative stress in the human body that leads to malfunction of tissues and organs. In this context, polysaccharides play a very significant role in providing shielding effect against the virus due to their polyanionic rich features and a molecular weight that hinders their reactive surface glycoproteins. Significantly the functional groups especially sulfate, sulfate pattern and addition, uronic acids, monosaccharides, glycosidic linkage and high molecular weight have greater influence in the antiviral activity. Moreover, they are very good antioxidants that can reduce the free radical generation and provokes intracellular antioxidant enzymes. Additionally, polysaccharides enable a host-virus immune response, activate phagocytosis and stimulate interferon systems. Therefore, polysaccharides can be used as candidate drugs, adjuvants in vaccines or combination with other antivirals, antioxidants and immune-activating nutritional supplements and antiviral materials in healthcare products to prevent SARS-CoV-2 infection.


Assuntos
Anticoagulantes/uso terapêutico , Antivirais/uso terapêutico , COVID-19/tratamento farmacológico , Fatores Imunológicos/uso terapêutico , Polissacarídeos/uso terapêutico , Embolia Pulmonar/tratamento farmacológico , Insuficiência Respiratória/tratamento farmacológico , Anticoagulantes/química , Anticoagulantes/isolamento & purificação , Antivirais/química , Antivirais/isolamento & purificação , Plaquetas/efeitos dos fármacos , Plaquetas/patologia , Plaquetas/virologia , COVID-19/complicações , COVID-19/diagnóstico , COVID-19/virologia , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/isolamento & purificação , Pulmão/irrigação sanguínea , Pulmão/efeitos dos fármacos , Pulmão/patologia , Pulmão/virologia , Feófitas/química , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Embolia Pulmonar/complicações , Embolia Pulmonar/diagnóstico , Embolia Pulmonar/virologia , Insuficiência Respiratória/complicações , Insuficiência Respiratória/diagnóstico , Insuficiência Respiratória/virologia , Rodófitas/química , SARS-CoV-2/efeitos dos fármacos , SARS-CoV-2/patogenicidade , Ésteres do Ácido Sulfúrico/química , Ligação Viral/efeitos dos fármacos , Internalização do Vírus/efeitos dos fármacos
12.
Carbohydr Polym ; 262: 117945, 2021 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-33838822

RESUMO

Alkaline extracted endopolysaccharides (MPS) from Monascus purpureus (Hong Qu) mycelium were successfully separated into four sub-fractions, namely MPS-1 (18.0 %), MPS-2 (27.1 %), MPS-3 (12.6 %) and MPS-4 (14.7 %), by DEAE-Cellulose column chromatography. By combining monosaccharide composition analysis, methylation analysis and 1D & 2D NMR, the structure of sub-fractions was systematically characterized. Both MPS-1 and MPS-2 were comprised of mannose, glucose and galactose in the molar ratio of 1.5:1.6:1.0 and 10.6:1.0:13.8, respectively. The backbone of them both consisted of 2-α-Manp with several different branched chains. However, MPS-1 contained glucose based sugar residues such as 3-Glcp and 4-Glcp which were not shown on MPS-2. The proposed structures of MPS-3 and MPS-4 were not obtained due to the fairly complex molecular structure and relatively low yield. Moreover, based on the RAW 264.7 cells model, MPS-2 could significantly promote cytokines secretion including IL-6, TNF-α, and IL-10 and improve expression levels of the related mRNA.


Assuntos
Polissacarídeos Fúngicos/química , Polissacarídeos Fúngicos/farmacologia , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Monascus/química , Micélio/química , Animais , Proliferação de Células/efeitos dos fármacos , Citocinas/metabolismo , Fermentação , Galactose/química , Glucose/química , Imunomodulação , Espectroscopia de Ressonância Magnética/métodos , Manose/química , Metilação , Camundongos , Estrutura Molecular , Monossacarídeos/análise , Células RAW 264.7
13.
Int J Biol Macromol ; 182: 136-143, 2021 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-33831454

RESUMO

The purpose of this study was to optimize modification conditions of selenized garlic polysaccharides (sGPS) and investigate its structural characterization, immune and antioxidant activities. Herein, selenized garlic polysaccharides (sGPS) were prepared using by HNO3-Na2SeO3 selenylation method. And then modification conditions of sGPS were optimized through L9 (34) orthogonal test. The structural characterization of sGPS were identified by the Fourier-transform infrared (FT-IR), Solid-State nuclear magnetic resonance (NMR) spectra, X-ray diffraction (XRD) and thermogravimetric (TGA). The morphology of sGPS was detected using scanning electron microscope (SEM) and transmission electron microscope (TEM). In vivo investigation showed that sGPS significantly improved serum hemagglutination-inhibition (HI) antibody titers against Newcastle disease virus, enhanced secretory IgA (sIgA), IFN-γ, IL-2 secretion in jejunum and trachea irrigation compared with vaccine immunized control group. Furthermore, it showed that sGPS had some effects on the antioxidant activities in livers of chickens. In conclusion, the optimal modification conditions of sGPS were as follows: reaction temperature was 70 °C, the dosage of Na2SeO3 was 400 mg and reaction time was 6 h. The selenylation modification of garlic polysaccharides (GPS) could improve its immune and antioxidant activity in chickens.


Assuntos
Alho/química , Fatores Imunológicos/química , Polissacarídeos/química , Selênio/química , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Proteínas Aviárias/sangue , Galinhas , Feminino , Imunoglobulina G/sangue , Fatores Imunológicos/farmacologia , Interferon gama/sangue , Interleucina-2/sangue , Fígado/efeitos dos fármacos , Fígado/metabolismo
14.
Int J Biol Macromol ; 183: 145-157, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-33878360

RESUMO

Two novel glucans named MIPB50-W and MIPB50-S-1 were obtained from edible Morchella importuna with molecular weights (Mw) of 939.2 kDa and 444.5 kDa, respectively. MIPB50-W has a backbone of α-(1 → 4)-d-glucan, which was substituted at O-6 position by α-d-Glcp-(1→. Moreover, MIPB50-S-1 has a backbone of α-(1 → 4)-d-glucan, which was substituted at O-6 position by α-d-Glcp-(1 → 6)-α-d-Glcp-(1→. This is the first report about glucan found in Morchella mushrooms. Furthermore, MIPB50-W and MIPB50-S-1 strengthened the phagocytosis function and the promoted secretion of interleukins (IL)-6/tumor necrosis factor-alpha (TNF-α) and nitric oxide (NO), which induced the activation of Toll-like receptor 2 (TLR2), TLR4 as well as mitogen activated protein kinase (MAPK) and nuclear factor-κB (NF-κB) pathways. Interestingly, MIPB50-S-1 performed the better immunomodulatory activity than that of MIPB50-W in almost all tests. Therefore, MIPB50-W and MIPB50-S-1 are potential immune-enhancing components of functional foods.


Assuntos
Ascomicetos/metabolismo , Carpóforos/metabolismo , Glucanos/farmacologia , Fatores Imunológicos/farmacologia , Macrófagos/efeitos dos fármacos , Animais , Glucanos/química , Glucanos/isolamento & purificação , Fatores Imunológicos/química , Fatores Imunológicos/isolamento & purificação , Interleucina-6/metabolismo , Macrófagos/imunologia , Macrófagos/metabolismo , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Estrutura Molecular , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Fagocitose/efeitos dos fármacos , Células RAW 264.7 , Transdução de Sinais , Relação Estrutura-Atividade , Receptor 2 Toll-Like/metabolismo , Receptor 4 Toll-Like/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
15.
Int J Biol Macromol ; 183: 119-131, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-33905802

RESUMO

Hedyotis diffusa polysaccharides, as the main component and an important bioactive substance of Hedyotis diffusa, are effective immunomodulators with various pharmacological activities, including antitumour, anti-inflammatory, antioxidant, anti-fatigue and immunity-enhancing activities. The total polysaccharides extracted from Hedyotis diffusa and Scutellaria barbata have great effects in treating liver cancer, gastric cancer, rectal cancer, glioma and nasopharyngeal carcinoma. Moreover, different materials and extraction methods result in differences in the structure and bioactivity of Hedyotis diffusa polysaccharides. Therefore, this paper summarizes the isolation, purification, structural characteristics, pharmacological activities, and combined action of Hedyotis diffusa polysaccharides to provide a reference for further study.


Assuntos
Hedyotis/química , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/isolamento & purificação , Fatores Imunológicos/farmacologia , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Relação Estrutura-Atividade
16.
J Med Chem ; 64(8): 5137-5156, 2021 04 22.
Artigo em Inglês | MEDLINE | ID: mdl-33797901

RESUMO

The approvals of idelalisib and duvelisib have validated PI3Kδ inhibitors for the treatment for hematological malignancies driven by the PI3K/AKT pathway. Our program led to the identification of structurally distinct heterocycloalkyl purine inhibitors with excellent isoform and kinome selectivity; however, they had high projected human doses. Improved ligand contacts gave potency enhancements, while replacement of metabolic liabilities led to extended half-lives in preclinical species, affording PI3Kδ inhibitors with low once-daily predicted human doses. Treatment of C57BL/6-Foxp3-GDL reporter mice with 30 and 100 mg/kg/day of 3c (MSD-496486311) led to a 70% reduction in Foxp3-expressing regulatory T cells as observed through bioluminescence imaging with luciferin, consistent with the role of PI3K/AKT signaling in Treg cell proliferation. As a model for allergic rhinitis and asthma, treatment of ovalbumin-challenged Brown Norway rats with 0.3 to 30 mg/kg/day of 3c gave a dose-dependent reduction in pulmonary bronchoalveolar lavage inflammation eosinophil cell count.


Assuntos
Classe I de Fosfatidilinositol 3-Quinases/química , Fatores Imunológicos/química , Pirrolidinas/química , Animais , Antígenos CD/metabolismo , Antígenos de Diferenciação de Linfócitos T/metabolismo , Linfócitos B/citologia , Linfócitos B/efeitos dos fármacos , Linfócitos B/metabolismo , Sítios de Ligação , Classe I de Fosfatidilinositol 3-Quinases/metabolismo , Modelos Animais de Doenças , Cães , Meia-Vida , Humanos , Fatores Imunológicos/metabolismo , Fatores Imunológicos/farmacologia , Fatores Imunológicos/uso terapêutico , Lectinas Tipo C/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Simulação de Dinâmica Molecular , Proteínas Proto-Oncogênicas c-akt/metabolismo , Pirrolidinas/metabolismo , Pirrolidinas/farmacologia , Pirrolidinas/uso terapêutico , Ratos , Ratos Wistar , Rinite Alérgica/tratamento farmacológico , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
17.
J Med Chem ; 64(9): 5291-5322, 2021 05 13.
Artigo em Inglês | MEDLINE | ID: mdl-33904753

RESUMO

Cells of the immune system utilize multiple proteases to regulate cell functions and orchestrate innate and adaptive immune responses. Dysregulated protease activities are implicated in many immune-related disorders; thus, protease inhibitors have been actively investigated for pharmaceutical development. Although historically considered challenging with concerns about toxicity, compounds that covalently modify the protease active site represent an important class of agents, emerging not only as chemical probes but also as approved drugs. Here, we provide an overview of technologies useful for the study of proteases with the focus on recent advances in chemoproteomic methods and screening platforms. By highlighting covalent inhibitors that have been designed to target immunomodulatory proteases, we identify opportunities for the development of small molecule immunomodulators.


Assuntos
Fatores Imunológicos/química , Peptídeo Hidrolases/química , Bibliotecas de Moléculas Pequenas/química , Calpaína/antagonistas & inibidores , Calpaína/metabolismo , Caspases/química , Caspases/metabolismo , Domínio Catalítico , Desenho de Fármacos , Humanos , Fatores Imunológicos/metabolismo , Proteína de Translocação 1 do Linfoma de Tecido Linfoide Associado à Mucosa/antagonistas & inibidores , Proteína de Translocação 1 do Linfoma de Tecido Linfoide Associado à Mucosa/metabolismo , Peptídeo Hidrolases/metabolismo , Biblioteca de Peptídeos
18.
Molecules ; 26(6)2021 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-33801096

RESUMO

The search for safe and effective anticancer therapies is one of the major challenges of the 21st century. The ineffective treatment of cancers, classified as civilization diseases, contributes to a decreased quality of life, health loss, and premature mortality in oncological patients. Many natural phytochemicals have anticancer potential. Pentacyclic triterpenoids, characterized by six- and five-membered ring structures, are one of the largest class of natural metabolites sourced from the plant kingdom. Among the known natural triterpenoids, we can distinguish lupane-, oleanane-, and ursane-types. Pentacyclic triterpenoids are known to have many biological activities, e.g., anti-inflammatory, antibacterial, hepatoprotective, immunomodulatory, antioxidant, and anticancer properties. Unfortunately, they are also characterized by poor water solubility and, hence, low bioavailability. These pharmacological properties may be improved by both introducing some modifications to their native structures and developing novel delivery systems based on the latest nanotechnological achievements. The development of nanocarrier-delivery systems is aimed at increasing the transport capacity of bioactive compounds by enhancing their solubility, bioavailability, stability in vivo and ensuring tumor-targeting while their toxicity and risk of side effects are significantly reduced. Nanocarriers may vary in sizes, constituents, shapes, and surface properties, all of which affect the ultimate efficacy and safety of a given anticancer therapy, as presented in this review. The presented results demonstrate the high antitumor potential of systems for delivery of pentacyclic triterpenoids.


Assuntos
Neoplasias/tratamento farmacológico , Triterpenos Pentacíclicos , Antibacterianos/química , Antibacterianos/uso terapêutico , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Antineoplásicos/química , Antineoplásicos/uso terapêutico , Antioxidantes/química , Antioxidantes/uso terapêutico , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/uso terapêutico , Neoplasias/metabolismo , Neoplasias/patologia , Triterpenos Pentacíclicos/química , Triterpenos Pentacíclicos/uso terapêutico
19.
Int J Mol Sci ; 22(7)2021 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-33805525

RESUMO

Food proteins and peptides are able to exert a variety of well-known bioactivities, some of which are related to well-being and disease prevention in humans and animals. Currently, an active trend in research focuses on chronic inflammation and oxidative stress, delineating their major pathogenetic role in age-related diseases and in some forms of cancer. The present study aims to investigate the potential effects of pseudocereal proteins and their derived peptides on chronic inflammation and oxidative stress. After purification and attribution to protein classes according to classic Osborne's classification, the immune-modulating, antioxidant, and trypsin inhibitor activities of proteins from quinoa (Chenopodium quinoa Willd.), amaranth (Amaranthus retroflexus L.), and buckwheat (Fagopyrum esculentum Moench) seeds have been assessed in vitro. The peptides generated by simulated gastro-intestinal digestion of each fraction have been also investigated for the selected bioactivities. None of the proteins or peptides elicited inflammation in Caco-2 cells; furthermore, all protein fractions showed different degrees of protection of cells from IL-1ß-induced inflammation. Immune-modulating and antioxidant activities were, in general, higher for the albumin fraction. Overall, seed proteins can express these bioactivities mainly after hydrolysis. On the contrary, higher trypsin inhibitor activity was expressed by globulins in their intact form. These findings lay the foundations for the exploitation of these pseudocereal seeds as source of anti-inflammatory molecules.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Fatores Imunológicos/farmacologia , Proteínas de Vegetais Comestíveis/isolamento & purificação , Proteínas de Vegetais Comestíveis/farmacologia , Sementes/química , Amaranthus/química , Anti-Inflamatórios não Esteroides/química , Antioxidantes/farmacologia , Células CACO-2 , Fracionamento Químico , Chenopodium quinoa/química , Fagopyrum/química , Humanos , Fatores Imunológicos/química , Peptídeos/isolamento & purificação , Peptídeos/farmacologia , Proteínas de Vegetais Comestíveis/farmacocinética , Inibidores da Tripsina/química , Inibidores da Tripsina/farmacologia
20.
Molecules ; 26(8)2021 Apr 07.
Artigo em Inglês | MEDLINE | ID: mdl-33917024

RESUMO

Beta glucan (ß-glucan) has promising bioactive properties. Consequently, the use of ß-glucan as a food additive is favored with the dual-purpose potential of increasing the fiber content of food products and enhancing their health properties. Our aim was to evaluate the biological activity of ß-glucan (antimicrobial, antitoxic, immunostimulatory, and anticancer) extracted from Saccharomyces cerevisiae using a modified acid-base extraction method. The results demonstrated that a modified acid-base extraction method gives a higher biological efficacy of ß-glucan than in the water extraction method. Using 0.5 mg dry weight of acid-base extracted ß-glucan (AB extracted) not only succeeded in removing 100% of aflatoxins, but also had a promising antimicrobial activity against multidrug-resistant bacteria, fungi, and yeast, with minimum inhibitory concentrations (MIC) of 0.39 and 0.19 mg/mL in the case of resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa, respectively. In addition, AB extract exhibited a positive immunomodulatory effect, mediated through the high induction of TNFα, IL-6, IFN-γ, and IL-2. Moreover, AB extract showed a greater anticancer effect against A549, MDA-MB-232, and HepG-2 cells compared to WI-38 cells, at high concentrations. By studying the cell death mechanism using flow-cytometry, AB extract was shown to induce apoptotic cell death at higher concentrations, as in the case of MDA-MB-231 and HePG-2 cells. In conclusion, the use of a modified AB for ß-glucan from Saccharomyces cerevisiae exerted a promising antimicrobial, immunomodulatory efficacy, and anti-cancer potential. Future research should focus on evaluating ß-glucan in various biological systems and elucidating the underlying mechanism of action.


Assuntos
Extração Líquido-Líquido , Saccharomyces cerevisiae/química , beta-Glucanas/isolamento & purificação , beta-Glucanas/farmacologia , Ácidos , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Humanos , Fatores Imunológicos/química , Fatores Imunológicos/isolamento & purificação , Fatores Imunológicos/farmacologia , Imunomodulação/efeitos dos fármacos , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/imunologia , Leucócitos Mononucleares/metabolismo , Extração Líquido-Líquido/métodos , Testes de Sensibilidade Microbiana , Espectroscopia de Infravermelho com Transformada de Fourier , beta-Glucanas/química
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