RESUMO
The use of direct injection ion mobility mass spectrometry (DI-IM-MS) to detect and identify betacyanin pigments in A. hortensis 'rubra' extracts was explored for the first time, with results compared to conventional LC-MS/MS analysis. The anti-inflammatory activities of leaf and seed extracts, alongside purified amaranthin and celosianin pigments, were investigated using a model of lipopolysaccharide (LPS)-activated murine macrophages. Extracts and purified pigments significantly inhibited the production of prostaglandin E2 and NO by up to 90% and 70%, respectively, and reduced the expression of Il6, Il1b, Nos2, and Cox2. Leaf and seed extracts also decreased secretion of Il6 and Il1b cytokines and reduced protein levels of Nos2 and Cox2. Furthermore, extracts and purified pigments demonstrated potent dose-dependent radical scavenging activity in a cellular antioxidant activity assay (CAA) without any cytotoxic effects. Our research highlights the promising biological potential of edible, climate-resilient A. hortensis 'rubra' as a valuable source of bioactive compounds.
Assuntos
Lipopolissacarídeos , Macrófagos , Estresse Oxidativo , Extratos Vegetais , Camundongos , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Células RAW 264.7 , Estresse Oxidativo/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Lipopolissacarídeos/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/imunologia , Ciclo-Oxigenase 2/metabolismo , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Espectrometria de Massas em TandemRESUMO
Cardamom seed (Elettaria cardamomum (L.)) is a well-appreciated spice in food and pharmaceutical industries owing to its unique rich flavor dominated by oxygenated monoterpenoids, α-terpinyl acetate and 1,8-cineole, to which most of the quality of cardamom essential oil (CEO) is attributed. CEO output is greatly influenced by different agronomic factors, processing, and EO extraction methods. In that context, the goal of this study is to provide an overarching review regarding emerged technologies along with their optimization parameters to achieve optimal oil yield with the best flavor quality. Furthermore, the recent approaches employed in CEO stabilization were highlighted alongside their pharmaceutical and food applications. Moreover, the different aspects of superlative CEO production including agricultural aspects, climatic requirements, and processing methods were also explained.
Assuntos
Elettaria , Sementes , Especiarias , Sementes/química , Sementes/crescimento & desenvolvimento , Especiarias/análise , Elettaria/química , Óleos Voláteis/química , Aromatizantes/química , Odorantes/análise , Humanos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Manipulação de AlimentosRESUMO
Hydrogels based on natural polymers have aroused interest from the scientific community. The aim of this investigation was to obtain natural extracts from mango peels and to evaluate their addition (1, 3, and 5%) on the rheological behavior of mango starch hydrogels. The total phenolic content, antioxidant activities, and phenolic acid profile of the natural extracts were evaluated. The viscoelastic and thixotropic behavior of hydrogels with the addition of natural extracts was evaluated. The total phenol content and antioxidant activity of the extracts increased significantly (p<0.05) with the variation of the ethanol-water ratio; the phenolic acid profile showed the contain of p-coumaric, ellagic, ferulic, chlorogenic acids, epicatechein, catechin, querecetin, and mangiferin. The viscoelastic behavior of the hydrogels showed that the storage modulus G' is larger than the loss modulus G'' indicating a viscoelastic solid behavior. The addition of extract improved the thermal stability of the hydrogels. 1% of the extracts increase viscoelastic and thixotropic properties, while concentrations of 3 to 5% decreased. The recovery percentage (%Re) decreases at concentrations from 0% to 1% of natural extracts, however, at concentrations from 3% to 5% increased.
Assuntos
Antioxidantes , Hidrogéis , Mangifera , Extratos Vegetais , Reologia , Amido , Mangifera/química , Hidrogéis/química , Extratos Vegetais/química , Amido/química , Antioxidantes/química , Viscosidade , Frutas/química , Fenóis/químicaRESUMO
Making health-enhancing tea from Forsythia suspensa leaves has been a tradition of Chinese folk culture for centuries. However, these leaves were not officially recognized as a new food source until 2017 by the Chinese government. In this study, ethyl acetate fractions from Forsythia suspensa fruit and leaves exhibited excellent antioxidant activity in vitro antioxidant assays and in vivo D-galactose-induced aging mice model. The antioxidant activity of the leaves was higher than that of fruit both in vitro and in vivo. The chemical constituents present in these ethyl acetate fractions were comprehensively analyzed using UHPLC-Q-Exactive-Orbitrap/MS. A total of 20 compounds were identified, among which forsythoside E, (+)-epipinoresinol, dihydromyricetin, chlorogenic acid, and ursolic acid were exclusively detected in the ethyl acetate fraction of Forsythia suspensa leaves, but absent in the ethyl acetate fraction derived from its fruit. This study provides theoretical support for the utilization of Forsythia suspensa fruit and leaves.
Assuntos
Envelhecimento , Antioxidantes , Forsythia , Frutas , Galactose , Extratos Vegetais , Folhas de Planta , Animais , Forsythia/química , Folhas de Planta/química , Camundongos , Frutas/química , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão , Antioxidantes/química , Antioxidantes/farmacologia , Envelhecimento/efeitos dos fármacos , Masculino , Humanos , Espectrometria de MassasRESUMO
Various strategies are being explored to reduce the formation of undesirable compounds during the thermal processing of foods. This study investigates the impact of incorporating annatto seed powder (Bixa orellana L.) into beef patties to reduce the formation of heterocyclic amines (HAs) during charcoal-grilling and pan-frying. A three-level full factorial design was used to assess the effect of both annatto seed powder concentration and cooking times on HAs formation. The results showed that HA formation increased with longer cooking times and decreased with higher concentrations of annatto seed powder. A significant reduction in HA content was observed in both charcoal-grilled and pan-fried beef patties when annatto seed powder was added, with a particularly notable 91 % reduction at the 1 % addition level. These findings demonstrate that the addition of annatto seed powder is a highly effective strategy for reducing HA formation in beef patties. CHEMICAL COMPOUNDS STUDIED IN THIS ARTICLE: 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) (PubChem CID: 62275); 2-amino-3,4,8-trimethylimidazo[4,5-f]quinoxaline (4,8-DiMeIQx) (PubChem CID: 104739); 2-amino-3,7,8-trimethylimidazo[4,5-f]quinoxaline (7,8-DiMeIQx) (PubChem CID: 104855); 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) (PubChem CID: 1530); 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indole (Trp-P-1) (PubChem CID: 5284474); 3-amino-1-methyl-5H-pyrido[4,3-b]indole (Trp-P-2) (PubChem CID: 5284476); 2-amino-9H-pyrido[2,3-b]indole (AαC) (PubChem CID: 62805); 2-amino-3-methyl-9H-pyrido[2,3-b]indole (MeAαC) (PubChem CID: 62244); Bixin (PubChem CID: 5281226).
Assuntos
Aminas , Carvão Vegetal , Culinária , Extratos Vegetais , Sementes , Sementes/química , Bovinos , Animais , Aminas/química , Aminas/análise , Carvão Vegetal/química , Extratos Vegetais/química , Bixaceae/química , Pós/química , Compostos Heterocíclicos/química , Compostos Heterocíclicos/análise , Temperatura Alta , Produtos da Carne/análise , CarotenoidesRESUMO
With the aim of expanding the potential application scope of mulberries, eleven pH-switchable deep eutectic solvents were screened for the ultrasonic-assisted extraction of mulberry polysaccharides, and a salt/salt aqueous two-phase system was constructed for the efficient separation of mulberry polysaccharides by regulating the system pH. DES-9 (tetraethylammonium chloride: octanoic acid molar ratio = 1: 2) with a critical response pH value of approximately 6.1 was concluded to be the best extraction solvent for extracting mulberry polysaccharides. A maximum polysaccharide extraction yield of 270.71 mg/g was obtained under the optimal conditions. The maximum polysaccharide extraction efficiency was 78.09 % for the pH-driven tetraethylammonium chloride/K2HPO4 aqueous two-phase system. An acidic ß-pyran mulberry polysaccharide with a low-molecular weight of 9.26 kDa and a confirmed monosaccharide composition were obtained. This efficient and environmentally friendly polysaccharide separation method offers a new approach for the efficient extraction and utilization of other plant polysaccharides.
Assuntos
Solventes Eutéticos Profundos , Morus , Extratos Vegetais , Polissacarídeos , Morus/química , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Concentração de Íons de Hidrogênio , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Solventes Eutéticos Profundos/química , Fracionamento Químico/métodos , Peso Molecular , Frutas/química , Cloreto de Sódio/químicaRESUMO
Dried citrus peel (DCP), also called "Chen Pi", has edible and medicinal value. However, the specific differences among various sources remain unknown. Herein, we collected six DCP species, namely, one Citrus reticulata 'Chachi' (CZG) and five Citrus reticulata Blanco (CRB). Targeted high-performance liquid chromatography and untargeted ultra-high-performance liquid chromatography-tandem mass spectrometry were employed to comprehensively compare the phenolic compounds and metabolites in DCP. Interestingly, 13 different phenolic compounds were noted in DCP. The total phenolic compound content in all CRB samples (58.86-127.65 mg/g) was higher than that of CZG (39.47 mg/g). Untargeted metabolomic revealed 1495 compounds, with 115 differentially expressed metabolites for CRBs and CZG, particularly flavonoids (38), terpenoids (15), and phenolic acids and derivatives (9). Lastly, antioxidant assays revealed that all CRB samples exhibited higher antioxidant activities compared with CZG. Therefore, our study results provide a theoretical basis for the high-value utilization of citrus peels and their metabolites.
Assuntos
Antioxidantes , Citrus , Frutas , Metabolômica , Extratos Vegetais , Espectrometria de Massas em Tandem , Citrus/química , Citrus/metabolismo , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/análise , Cromatografia Líquida de Alta Pressão , Frutas/química , Frutas/metabolismo , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Fenóis/metabolismo , Fenóis/química , Fenóis/análise , Flavonoides/metabolismo , Flavonoides/química , Flavonoides/análiseRESUMO
Phytopharmaceuticals are the newly termed herbal medicine, which includes standardized extract, bioactive fraction, and phytoconstituent. They have been practiced to cure, treat, and mitigate diseases. Phytopharmaceuticals have many health benefits, but their therapeutic efficacy is limited due to poor absorption, low bioavailability, and early elimination profile. A novel phospholipid complex is a newly introduced patented technology developed to incorporate the standardized plant extracts/fractions or water-soluble phytoconstituents into phospholipids to produce lipid compatible molecular complex, called phytosome, which improves their absorption and bioavailability. In herbal formulations, phytosome is the most advanced dosage form that has an upgraded absorption rate and enhanced pharmacokinetics compared with conventional products. The phospholipid complex results from hydrogen bonding between phospholipids and phytoconstituents, offering the maximum incorporation of herbal active ingredients into the lipidic layer and core. The increased therapeutic efficacy is due to the formation of amphiphilic phospholipid-complex of herbal medicine. This review highlights the role of phospholipids on delivery of herbal bioactives and natural extracts with particular emphasis on phytosomes. Moreover, the status of bioavailabilities, commercial products, patents, and clinical trials of phytosomal systems of phytopharmaceuticals were addressed.
Assuntos
Disponibilidade Biológica , Ensaios Clínicos como Assunto , Fosfolipídeos , Extratos Vegetais , Humanos , Fosfolipídeos/química , Fosfolipídeos/farmacocinética , Extratos Vegetais/química , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacocinética , Animais , Compostos Fitoquímicos/farmacocinética , Compostos Fitoquímicos/administração & dosagem , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Patentes como Assunto , Sistemas de Liberação de MedicamentosRESUMO
Curcumae Radix (CR) is a widely used traditional Chinese medicine with significant pharmaceutical importance, including enhancing blood circulation and addressing blood stasis. This study aims to establish an integrated and rapid quality assessment method for CR from various botanical origins, based on chemical components, antiplatelet aggregation effects, and Fourier transform near-infrared (FT-NIR) spectroscopy combined with multivariate algorithms. Firstly, ultra-performance liquid chromatography-photodiode array (UPLC-PDA) combined with chemometric analyses was used to examine variations in the chemical profiles of CR. Secondly, the activation effect on blood circulation of CR was assessed using an in vitro antiplatelet aggregation assay. The studies revealed significant variations in chemical profiles and antiplatelet aggregation effects among CR samples from different botanical origins, with constituents such as germacrone, ß-elemene, bisdemethoxycurcumin, demethoxycurcumin, and curcumin showing a positive correlation with antiplatelet aggregation biopotency. Thirdly, FT-NIR spectroscopy was integrated with various machine learning algorithms, including Artificial Neural Network (ANN), K-Nearest Neighbors (KNN), Logistic Regression (LR), Support Vector Machine (SVM), and Subspace K-Nearest Neighbors (Subspace KNN), to classify CR samples from four distinct sources. The result showed that FT-NIR combined with KNN and SVM classification algorithms after SNV and MSC preprocessing successfully distinguished CR samples from four plant sources with an accuracy of 100%. Finally, Quantitative models for active constituents and antiplatelet aggregation bioactivity were developed by optimizing the partial least squares (PLS) model with interval combination optimization (ICO) and competitive adaptive reweighted sampling (CARS) techniques. The CARS-PLS model achieved the best predictive performance across all five components. The coefficient of determination (R2p) and root mean square error (RMSEP) in the independent test sets were 0.9708 and 0.2098, 0.8744 and 0.2065, 0.9511 and 0.0034, 0.9803 and 0.0066, 0.9567 and 0.0172 for germacrone, ß-elemene, bisdemethoxycurcumin, demethoxycurcumin and curcumin, respectively. The ICO-PLS model demonstrated superior predictive capabilities for antiplatelet aggregation biotency, achieving an R2p of 0.9010, and an RMSEP of 0.5370. This study provides a valuable reference for the quality evaluation of CR in a more rapid and comprehensive manner.
Assuntos
Curcuma , Inibidores da Agregação Plaquetária , Agregação Plaquetária , Espectroscopia de Luz Próxima ao Infravermelho , Curcuma/química , Espectroscopia de Luz Próxima ao Infravermelho/métodos , Agregação Plaquetária/efeitos dos fármacos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Inibidores da Agregação Plaquetária/análise , Inibidores da Agregação Plaquetária/química , Animais , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/análise , Algoritmos , Extratos Vegetais/químicaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Morus alba L. are widely used as ethnomedicine and functional food in China, Japan, Korea and other Asian countries. Morus alba L. have a variety of pharmacological activity such as antiviral, antioxidation, anti-cholesterol, anticancer, hypoglycemia, and neuroprotection. Morus alba L. has demonstrated antiviral efficacy against influenza viruses, SARS-CoV-2 and so on, but its potential activity against pseudorabies virus (PRV) remains uncertain. AIM OF THE STUDY: This study endeavors to delve into the anti-pseudorabies virus (PRV) potential of the ethanol extract of Morus alba L. leaves (MLE), while simultaneously elucidating its underlying mechanism of action. MATERIALS AND METHODS: The anti-PRV activities of Morus alba L. extracts at different concentrations were evaluated by qPCR and immunoblotting. The inhibitory effects of MLE on PRV replication in three distinct treatment modes (pretreatment, co-treatment, and post-treatment) were detected by qPCR and indirect immunofluorescence assays. qPCR was used to investigate the effects of MLE on PRV attachment, entrance, and cytokine expression in PRV-infected cells. The chemical components in MLE were analyzed by UPLC-MS/MS. RESULTS: MLE significantly inhibits PRV replication and protein expression in a dose-dependent manner. MLE displays inhibitory effects against PRV at three different modes of treatment. The most significant inhibitory effect of MLE was observed when used in co-treatment mode, resulting in an inhibition rate of 99.42%. MLE inhibits PRV infection in the early stage. MLE inhibits PRV infection by affecting viral attachment and viral entry. Furthermore, MLE exerts its inhibition on PRV replication by mitigating the heightened expression of cytokines (TNF-α and IFN-α) triggered by PRV. Analysis of its chemical composition highlights phenolic acids and flavonoids as the principal constituents of MLE. CONCLUSION: The results illustrate that MLE effectively impedes PRV infection by suppressing viral adsorption and entry, while also curbing the expression of antiviral cytokines. Therefore, MLE may be a potential resource for creating new medications to treat human and animal PRV infections.
Assuntos
Antivirais , Herpesvirus Suídeo 1 , Morus , Extratos Vegetais , Folhas de Planta , Replicação Viral , Herpesvirus Suídeo 1/efeitos dos fármacos , Morus/química , Antivirais/farmacologia , Antivirais/isolamento & purificação , Extratos Vegetais/farmacologia , Animais , Replicação Viral/efeitos dos fármacos , Folhas de Planta/química , Citocinas/metabolismo , Cães , Células Madin Darby de Rim Canino , Internalização do Vírus/efeitos dos fármacos , Ligação Viral/efeitos dos fármacosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Acute lung injury (ALI) can lead to respiratory failure and even death. KAT2A is a key target to suppress the development of inflammation. A herb, perilla frutescens, is an effective treatment for pulmonary inflammatory diseases with anti-inflammatory effects; however, its mechanism of action remains unclear. AIM OF THE STUDY: The purpose of this study was to investigate the therapeutic effect and underlying mechanism of perilla frutescens leaf extracts (PLE), in the treatment of ALI by focusing on its ability to treat inflammation. MATERIALS AND METHODS: In vivo and in vitro models of ALI induced by LPS. Respiratory function, histopathological changes of lung, and BEAS-2B cells damage were assessed upon PLE. This effect is also tested under conditions of KAT2A over expression and KAT2A silencing. RESULTS: PLE significantly attenuated LPS-induced histopathological changes in the lungs, improved respiratory function, and increased survival rate from LPS stimuation background in mice. PLE remarkably suppressed the phosphorylation of STAT3, AKT, ERK (1/2) and the release of cytokines (IL-6, TNF-α, and IL-1ß) induced by LPS via inhibiting the expression of KAT2A. CONCLUSIONS: PLE has a dose-dependent anti-inflammatory effect by inhibiting KAT2A expression to suppress LPS-induced ALI n mice. Our study expands the clinical indications of the traditional medicine PLE and provide a theoretical basis for clinical use of acute lung injury.
Assuntos
Lesão Pulmonar Aguda , Lipopolissacarídeos , Perilla frutescens , Extratos Vegetais , Folhas de Planta , Animais , Lesão Pulmonar Aguda/tratamento farmacológico , Lesão Pulmonar Aguda/patologia , Lesão Pulmonar Aguda/induzido quimicamente , Perilla frutescens/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Masculino , Camundongos , Humanos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/uso terapêutico , Citocinas/metabolismo , Linhagem Celular , Camundongos Endogâmicos C57BL , Pulmão/efeitos dos fármacos , Pulmão/patologia , Pulmão/metabolismo , Modelos Animais de DoençasRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Sea buckthorn (Hippophae rhamnoides), a traditional Tibetan medicinal herb, exhibits protective effects against cardiovascular and respiratory diseases. Although Sea buckthorn extract (SBE) has been confirmed to alleviate airway inflammation in mice, its therapeutic effect and underlying mechanism on chronic obstructive pulmonary disease (COPD) requires further clarification. AIM OF THE STUDY: To elucidate the alleviative effect and molecular mechanism of SBE on lipopolysaccharides (LPS)/porcine pancreatic elastase (PPE)-induced COPD by blocking ferroptosis. METHODS: The anti-ferroptotic effects of SBE were evaluated in human BEAS-2B bronchial epithelial cells using CCK8, RT-qPCR, western blotting, and transmission electron microscopy. Transwell was employed to detect chemotaxis of neutrophils. COPD model was induced by intranasally administration of LPS/PPE in mice and measured by alterations of histopathology, inflammation, and ferroptosis. RNA-sequencing, western blotting, antioxidant examination, flow cytometry, DARTS, CETSA, and molecular docking were then used to investigate its anti-ferroptotic mechanisms. RESULTS: In vitro, SBE not only suppressed erastin- or RSL3-induced ferroptosis by suppressing lipid peroxides (LPOs) production and glutathione (GSH) depletion, but also suppressed ferroptosis-induced chemotactic migration of neutrophils via reducing mRNA expression of chemokines. In vivo, SBE ameliorated LPS/PPE-induced COPD phenotypes, and inhibited the generation of LPOs, cytokines, and chemokines. RNA-sequencing showed that p53 pathway and mitogen-activated protein kinases (MAPK) pathway were implicated in SBE-mediated anti-ferroptotic action. SBE repressed erastin- or LPS/PPE-induced overactivation of p53 and MAPK pathway, thereby decreasing expression of diamine acetyltransferase 1 (SAT1) and arachidonate 15-lipoxygenase (ALOX15), and increasing expression of glutathione peroxidase 4 (GPX4) and solute carrier family 7 member 11 (SLC7A11). Mechanistically, erastin-induced elevation of reactive oxygen species (ROS) was reduced by SBE through directly scavenging free radicals, thereby contributing to its inhibition of p53 and MAPK pathways. CETSA, DARTS, and molecular docking further showed that ROS-generating enzyme nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 4 (NOX4) may be the target of SBE. Overexpression of NOX4 partially impaired the anti-ferroptotic activity of SBE. CONCLUSION: Our results demonstrated that SBE mitigated COPD by suppressing p53 and MAPK pro-ferroptosis pathways via directly scavenging ROS and blocking NOX4. These findings also supported the clinical application of Sea buckthorn in COPD therapy.
Assuntos
Ferroptose , Hippophae , Extratos Vegetais , Doença Pulmonar Obstrutiva Crônica , Espécies Reativas de Oxigênio , Proteína Supressora de Tumor p53 , Ferroptose/efeitos dos fármacos , Doença Pulmonar Obstrutiva Crônica/tratamento farmacológico , Animais , Humanos , Espécies Reativas de Oxigênio/metabolismo , Hippophae/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Proteína Supressora de Tumor p53/metabolismo , Camundongos , Masculino , Camundongos Endogâmicos C57BL , Linhagem Celular , Lipopolissacarídeos/toxicidade , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Modelos Animais de Doenças , Simulação de Acoplamento MolecularRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Mountain-cultivated Panax ginseng C.A.Mey. (MCG) with high market price and various properties was valuable special local product in Northeast of Asia. MCG has been historically used to mitigate heart failure (HF) for thousand years, HF is a clinical manifestation of deficiency of "heart-qi" in traditional Chinese medicine. However, there was little report focus on the activities of extracted residue of MCG. AIM OF THE STUDY: A novel glycopeptide (APMCG-1) was isolated from step ethanol precipitations of alkaline protease-assisted extract from MCG residue. MATERIALS AND METHODS: The molecular weight and subunit structure of APMCG-1 were determined by FT-IR, HPLC and GPC technologies, as well as the H9c2 cells, Tg (kdrl:EGFP) zebrafish were performed to evaluated the protective effect of APMCG-1. RESULTS: APMCG-1 was identified as a glycopeptide containing seven monosaccharides and seven amino acids via O-lined bonds. Further, in vitro, APMCG-1 significantly decreased reactive oxygen species production and lactate dehydrogenase contents in palmitic acid (PA)-induced H9c2 cells. APMCG-1 also attenuated endoplasmic reticulum stress and mitochondria-mediated apoptosis in H9c2 cells via the PI3K/AKT signaling pathway. More importantly, APMCG-1 reduced the blood glucose, lipid contents, the levels of heart injury, oxidative stress and inflammation of 5 days post fertilization Tg (kdrl:EGFP) zebrafish with type 2 diabetic symptoms in vivo. CONCLUSIONS: APMCG-1 protects PA-induced H9c2 cells while reducing cardiac dysfunction in zebrafish with type 2 diabetic symptoms. The present study provides a new insight into the development of natural glycopeptides as heart-related drug therapies.
Assuntos
Diabetes Mellitus Tipo 2 , Glicopeptídeos , Insuficiência Cardíaca , Panax , Peixe-Zebra , Animais , Panax/química , Insuficiência Cardíaca/tratamento farmacológico , Insuficiência Cardíaca/prevenção & controle , Diabetes Mellitus Tipo 2/tratamento farmacológico , Ratos , Linhagem Celular , Glicopeptídeos/farmacologia , Glicopeptídeos/química , Apoptose/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Cardiotônicos/farmacologia , Cardiotônicos/química , Cardiotônicos/isolamento & purificação , Cardiotônicos/uso terapêutico , Miócitos Cardíacos/efeitos dos fármacos , Estresse do Retículo Endoplasmático/efeitos dos fármacosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Gelsemium dynamized dilutions (GDD) are known as a remedy for a wide range of behavioral and psychological symptoms of depression and anxiety at ultra-low doses, yet the underlying mechanisms of the mode of action of G. sempervirens itself are not well understood. AIM OF THE STUDY: The present study was designed to examine the neuroprotective effects of Gelsemium preparations in counteracting stress-related mitochondrial dysfunctions in neuronal cells. MATERIALS AND METHODS: We started by studying how serum deprivation affects the mitochondrial functions of human neuroblastoma (SH-SY5Y) cells. Next, we looked into the potential of various Gelsemium dilutions to improve cell survival and ATP levels. After identifying the most effective dilutions, 3C and 5C, we tested their ability to protect SH-SY5Y cells from stress-induced mitochondrial deficits. We measured total and mitochondrial superoxide anion radicals using fluorescent dyes dihydroethidium (DHE) and the red mitochondrial superoxide indicator (MitoSOX). Additionally, we assessed total nitric oxide levels with 4,5-diaminofluorescein diacetate (DAF-2DA), examined the redox state using pRA305 cells stably transfected with a plasmid encoding a redox-sensitive green fluorescent protein, and analyzed mitochondrial network morphology using an automated high-content analysis device, Cytation3. Furthermore, we investigated bioenergetics by measuring ATP production with a bioluminescence assay (ViaLighTM HT) and evaluated mitochondrial respiration (OCR) and glycolysis (ECAR) using the Seahorse Bioscience XF24 Analyzer. Finally, we determined cell survival using an MTT reduction assay. RESULTS: Our research indicates that Gelsemium dilutions (3C and 5C) exhibited neuroprotective effects by: - Normalizing total and mitochondrial superoxide anion radicals and total nitric oxide levels. - Regulating the mitochondrial redox environment and mitochondrial networks morphology. - Increasing ATP generation as well as OCR and ECAR levels, thereby reducing the viability loss induced by serum withdrawal stress. CONCLUSIONS: These findings highlight that dynamized Gelsemium preparations may have neuroprotective effects against stress-induced cellular changes in the brain by regulating mitochondrial functions, essential for the survival, plasticity, and function of neurons in depression.
Assuntos
Sobrevivência Celular , Mitocôndrias , Neurônios , Fármacos Neuroprotetores , Humanos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Trifosfato de Adenosina/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Óxido Nítrico/metabolismo , Extratos Vegetais/farmacologia , Relação Dose-Resposta a Droga , Superóxidos/metabolismoRESUMO
ETHNOPHARMACOLOGY RELEVANCE: Palm buds are a natural green resource of the forest, which are not only rich in nutrients but contain a large number of phenolic acids and flavonoids, among other components. It has a variety of biological activities such as antioxidant and uterine smooth muscle stimulation. AIM OF THE STUDY: To evaluate the safety of palm buds for use as a nutraceutical product and food by evaluating the toxicity, subacute toxicity and genotoxicity of the young palm buds. Also studied for its immune-enhancing activity. MATERIALS AND METHODS: Acute toxicity tests were performed in mice using the maximum tolerance method, and the manifestations of toxicity and deaths were recorded after administration of 10,000 mg/mL for 14 consecutive d (days) of observations. To assess subacute toxicity, mice were treated with palm buds (750, 1500, or 3000 mg/mL) daily for 28 days. The teratogenicity of palm buds was assessed by the Ames test, the mouse bone marrow cell micronucleus test, and the mouse spermatozoa malformation test. In addition, we evaluated the immune-enhancing ability of palm buds by the mouse carbon profile test, delayed-type metamorphosis reaction, and serum hemolysin assay. RESULTS: In the acute toxicity study, the Median Lethal Dose (LD50) was greater than 10,000 mg/kg bw in both male and female rats. There were also no deaths or serious toxicities in the subacute study. The no-observed-adverse-effect level (NOAEL) was 3000 mg/kg bw. However, the mice's food intake decreased after one week. The medium and high dose groups had a reducing effect on body weight in mice of both sexes. In addition, the changes in organ coefficients of the liver, kidney and stomach in male mice were significantly higher in the high-dose group (3.23 ± 0.35, 0.75 ± 0.05, 0.57 ± 0.05 g) than in the control group (2.94 ± 0.18, 0.58 ± 0.05, 0.50 ± 0.02 g). Hematological analyses showed that all the indices of the rats in each palm sprout dose group were within the normal range. The results of blood biochemical indicators showed that there was a significant reduction in TP in the blood of male mice in the high-dose group (44.6 ± 7.8 g/L) compared to the control group (58.3 ± 15.1 g/L). In histopathological analysis, none of the significant histopathological changes were observed. The results of the immunological experiment in mice showed that the liver coefficient and thymus coefficient of the high-dose group (8400 mg/kg) were significantly lower than the control group. There was no remarkable difference in auricle swelling between each dose palm bud group (1400, 2800, or 8400 mg/kg) and the control group. The anti-volume number of the high-dose group was significantly increased. CONCLUSION: Palm buds have non-toxic effects in vivo and have little effect on non-specific and cellular immunity in the test mice within the dose range of this experiment. The immunoenhancement in mice is mainly achieved through humoral immunity. In conclusion, our results suggest that palm buds are safe for use as healthcare products and food.
Assuntos
Arecaceae , Testes de Toxicidade Aguda , Animais , Feminino , Masculino , Arecaceae/química , Camundongos , Extratos Vegetais/toxicidade , Extratos Vegetais/farmacologia , Extratos Vegetais/administração & dosagem , Fatores Imunológicos/toxicidade , Ratos , Testes de Toxicidade Subaguda , Relação Dose-Resposta a Droga , Testes para Micronúcleos , Testes de Mutagenicidade , Proteínas Hemolisinas/toxicidade , Dose Letal MedianaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Acute lung injury (ALI) is a serious health-threatening syndrome of intense inflammatory response in the lungs, with progression leading to acute respiratory distress syndrome (ARDS). Dachengqi decoction dispensing granule (DDG) has a pulmonary protective role, but its potential modulatory mechanism to alleviate ALI needs further excavation. AIM OF THE STUDY: This study aims to investigate the effect and potential mechanism of DDG on lipopolysaccharide (LPS)-induced ALI models in vivo and in vitro. MATERIALS AND METHODS: LPS-treated Balb/c mice and BEAS-2B cells were used to construct in vivo and in vitro ALI models, respectively. Hematoxylin-eosin (HE), Wet weight/Dry weight (W/D) calculation of lung tissue, and total protein and Lactic dehydrogenase (LDH) assays in BALF were performed to assess the extent of lung tissue injury and pulmonary edema. Enzyme-linked immunosorbent assay (ELISA) was used to detect the levels of tumor necrosis factor-alpha (TNF-α), interleukin-1ß (IL-1ß), and interleukin-18 (IL-18) in BALF, serum, and cell supernatant. The qRT-PCR was used to detect inflammatory factors, Z-DNA binding protein 1 (ZBP1), and receptor-interacting protein kinase 1 (RIPK1) expression in lung tissues and BEAS-2B cells. Double immunofluorescence staining and co-immunoprecipitation were used to detect the relative expression and co-localization of ZBP1 and RIPK1. The effects of LPS and DDG on BEAS-2B cell activity were detected by Cell Counting Kit-8 (CCK-8). Western blot (WB) was performed to analyze the expression of PANoptosis-related proteins in lung tissues and BEAS-2B cells. RESULTS: In vivo, DDG pretreatment could dose-dependently improve the pathological changes of lung tissue in ALI mice, and reduce the W/D ratio of lung, total protein concentration, and LDH content in BALF. In vitro, DDG reversed the inhibitory effect of LPS on BEAS-2B cell viability. Meanwhile, DDG significantly reduced the levels of inflammatory factors in vitro and in vivo. In addition, DDG could inhibit the expression levels of PANoptosis-related proteins, especially the upstream key regulatory molecules ZBP1 and RIPK1. CONCLUSION: DDG could inhibit excessive inflammation and PANoptosis to alleviate LPS-induced ALI, thus possessing good anti-inflammatory and lung-protective effects. This study establishes a theoretical basis for the further development of DDG and provides a new prospect for ALI treatment by targeting PANoptosis.
Assuntos
Lesão Pulmonar Aguda , Lipopolissacarídeos , Camundongos Endogâmicos BALB C , Animais , Lesão Pulmonar Aguda/tratamento farmacológico , Lesão Pulmonar Aguda/induzido quimicamente , Lesão Pulmonar Aguda/metabolismo , Lesão Pulmonar Aguda/patologia , Lipopolissacarídeos/toxicidade , Humanos , Masculino , Camundongos , Linhagem Celular , Pulmão/efeitos dos fármacos , Pulmão/patologia , Pulmão/metabolismo , Líquido da Lavagem Broncoalveolar/química , Extratos Vegetais/farmacologia , Citocinas/metabolismo , Anti-Inflamatórios/farmacologia , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêuticoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Melastoma dodecandrum Lour. (MD), a traditional Chinese medicine used by the She ethnic group, has been used to treat cerebral ischemia-reperfusion (CIR) injury due to its efficacy in promoting blood circulation and removing blood stasiss; however, the therapeutic effects and mechanisms of MD in treating CIR injury remain unclear. AIM: To investigate the protective effects of MD on CIR injury, in addition to its impact on oxidative stress, endoplasmic reticulum (ER) stress, and cell apoptosis. MATERIALS AND METHODS: The research was conducted using both cell experiments and animal experiments. The CCK-8 method, immunofluorescence staining, and flow cytometry were used to analyze the effects of MD-containing serum on oxygen-glucose deprivation/reperfusion (OGD/R)-induced PC12 cell viability, reactive oxygen species (ROS) clearance, anti-inflammatory, neuroprotection and inhibition of apoptosis. Furthermore, 2,3,5-Triphenyl tetrazolium chloride staining, hematoxylin and eosin staining, Nissl staining, and immunohistochemistry were used to detect infarct size, pathological changes, Nissl corpuscula and neuronal protein expression in middle cerebral artery occlusion (MCAO) rats. Polymerase chain reaction and Western Blotting were conducted in cell and animal experiments to detect the expression levels of ER stress-related genes and proteins. RESULTS: The MD extract enhanced the viability of PC12 cells under OGD/R modeling, reduced ROS and IL-6 levels, increased MBP levels, and inhibited cell apoptosis. Furthermore, MD improved the infarct area in MCAO rats, increased the number of Nissl bodies, and regulated neuronal protein levels including Microtubule-Associated Protein 2 (MAP-2), Myelin Basic Protein (MBP), Glial Fibrillary Acidic Protein (GFAP), and Neurofilament 200 (NF200). Additionally, MD could regulate the expression levels of oxidative stress proteins malondialdehyde (MDA), nitric oxide (NO), superoxide dismutase (SOD), and catalase (CAT). Both cell and animal experiments demonstrated that MD could inhibit ER stress-related proteins (GRP78, ATF4, ATF6, CHOP) and reduce cell apoptosis. CONCLUSION: This study confirmed that the therapeutic mechanism of the MD extract on CIR injury was via the inhibition of oxidative stress and the ER stress pathway, in addition to the inhibition of apoptosis.
Assuntos
Apoptose , Estresse do Retículo Endoplasmático , Fármacos Neuroprotetores , Estresse Oxidativo , Ratos Sprague-Dawley , Traumatismo por Reperfusão , Animais , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Traumatismo por Reperfusão/tratamento farmacológico , Traumatismo por Reperfusão/metabolismo , Traumatismo por Reperfusão/prevenção & controle , Estresse Oxidativo/efeitos dos fármacos , Ratos , Células PC12 , Masculino , Fármacos Neuroprotetores/farmacologia , Apoptose/efeitos dos fármacos , Infarto da Artéria Cerebral Média/tratamento farmacológico , Espécies Reativas de Oxigênio/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Isquemia Encefálica/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêuticoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Calyptrochilum emarginatum (Afzel. Ex Sw.) Schltr. (Orchidaceae) is a traditional medicinal plant known for its antimicrobial properties and efficacy in managing convulsive fever and menstrual disorders and addressing conditions such as malaria, tuberculosis, and cough. AIM OF THE STUDY: The study aims to examine the memory-enhancing and neuroprotective properties of ethanol extract of Calyptrochilum emarginatum leaves (EECEL) in scopolamine-induced amnesia mice model. MATERIALS AND METHODS: Forty-two male mice were divided into six groups (n = 7). Group 1 served as control, administered distilled water (10 mL/kg, p. o), group 2 received scopolamine only (3 mg/kg, i. p.), groups 3 to 6 received pretreatments of EECEL (50, 100, and 200 mg/kg, p. o.) and donepezil (1 mg/kg, p. o.) 30 min before scopolamine (3 mg/kg), for seven days. Following treatments, behavioral (learning and memory) assessments were carried out, while biochemical (acetylcholinesterase activity, oxidative stress markers, inflammatory cytokines markers) and histological evaluations were done after euthanasia. RESULTS: Scopolamine significantly impaired spatial, long term and recognition memory. Nevertheless, administration of EECEL (50, 100, and 200 mg/kg orally) enhanced memory function in mice, as observed in the Y maze [F (5, 30) = 20.23, p < 0.0001], Morris water maze [F (10, 90) = 3.105, p = 0.0019; [F (5, 30) = 21.13, p < 0.0001]], and novel object recognition tasks [F (5, 30) = 37.22, p < 0.0001)]. Scopolamine-treated mice exhibited significant dysfunction in the cholinergic system, as evidenced by elevated AChE activity [0.099 ± 0.005 vs. 0.063 ± 0.004 mol/min/g] with an elevation in oxidative stress. On the other hand, administration of EECEL counteracted these consequences by reducing AChE activity, mitigating oxidative damage, reducing pro-inflammatory cytokines, and preventing degeneration of neurons. CONCLUSION: The results demonstrated that EECEL effectively mitigates scopolamine-induced memory impairment via an oxido-inflammatory mechanism and modulation of the central cholinergic system.
Assuntos
Amnésia , Etanol , Fármacos Neuroprotetores , Orchidaceae , Extratos Vegetais , Folhas de Planta , Escopolamina , Animais , Masculino , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Camundongos , Amnésia/tratamento farmacológico , Amnésia/induzido quimicamente , Etanol/química , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Fármacos Neuroprotetores/isolamento & purificação , Orchidaceae/química , Estresse Oxidativo/efeitos dos fármacos , Acetilcolinesterase/metabolismo , Aprendizagem em Labirinto/efeitos dos fármacos , Modelos Animais de Doenças , Memória/efeitos dos fármacos , Solventes/química , Donepezila/farmacologia , Donepezila/uso terapêuticoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The popularity of herbal medicine is expanding globally due to the common belief that herbal products are natural and nontoxic. Thymelaea hirsuta leaves are traditionally used for the treatment of recurrent abortion in humans and animals. However, a lack of safety evaluation of the plant, particularly in pregnant women, raises serious concerns regarding its potential embryotoxic effects. AIM OF THE STUDY: Therefore, the present study investigated the safety of Thymelaea hirsuta leaves aqueous extract (THLE) during pregnancy and lactation following maternal rat treatment. MATERIALS AND METHODS: THLE phytochemical compounds were identified using high-performance liquid chromatography (HPLC). THLE was orally administered to pregnant rats and lactating dams at dosages of 0, 250, 500, and 1000 mg/kg/day. At the end of the study, dam s' and pups' body weights, serum biochemical and hematological indices, and histopathological changes were investigated. For the fetal observation and histopathological changes were also evaluated. RESULTS: Our findings revealed that THLE is rich in different phenolic and flavonoid compounds. However, biochemical and hormonal parameters such as ALT, AST, and prolactin were significantly increased in dams treated with a higher dosage of THLE when compared to the control dams (P ≤ 0.05). Additionally, external, visceral and skeletal examinations of fetuses revealed a marked increase of malformation rates in treated fetuses. CONCLUSIONS: The results revealed that higher oral dosing of THLE during pregnancy could affect embryonic development in rats, while lower doses are safe and can be used during pregnancy and lactation to attain its beneficial effects.
Assuntos
Extratos Vegetais , Folhas de Planta , Ratos Wistar , Thymelaeaceae , Animais , Extratos Vegetais/toxicidade , Extratos Vegetais/farmacologia , Feminino , Gravidez , Ratos , Thymelaeaceae/química , Lactação , Reprodução/efeitos dos fármacos , Masculino , Relação Dose-Resposta a DrogaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The Chinese traditional medicine frankincense, which can promote blood circulation, is often used to treat skin lesions, including frostbite. AIM OF THE STUDY: To explore the properties of frankincense oil extract (FOE) and its active ingredients and their effect on frostbite wound recovery as an approach to understand the mechanism associated with microcirculation-improvement therapy. MATERIALS AND METHODS: The microcirculation-improving effects of FOE and its active ingredients were evaluated using liquid nitrogen-induced frostbite animal models. The rewarming capacity of FOE on the skin was determined through infrared detection, and frostbite wound healing was evaluated following haematoxylin and eosin (H&E) staining and fibre analysis. Moreover, related factors were examined to determine the anti-apoptotic, anti-inflammatory, and microcirculatory properties of FOE and its active ingredients on affected tissue in the context of frostbite. RESULTS: FOE and its active ingredients rapidly rewarmed wound tissue after frostbite by increasing the temperature. Moreover, these treatments improved wound healing and restored skin structure through collagen and elastin fibre remodelling. In addition, they exerted anti-apoptotic effects by decreasing the number of apoptotic cells, reducing caspase-3 expression, and eliciting anti-inflammatory effects by decreasing COX-2 and ß-catenin expression. They also improved microcirculatory disorders by decreasing HIF-1α expression and increasing CD31 expression. CONCLUSIONS: FOE and its active components can effectively treat frostbite by enhancing microcirculation, inhibiting the infiltration of inflammatory cells, decreasing cell apoptosis, and exerting antinociceptive effects. These findings highlight FOE as a new treatment option for frostbite, providing patients with an effective therapeutic strategy.