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1.
Bioorg Chem ; 146: 107320, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38569323

RESUMEN

Spleen tyrosine kinase (Syk) plays a crucial role as a target for allergy treatment due to its involvement in immunoreceptor signaling. The purpose of this study was to identify natural inhibitors of Syk and assess their effects on the IgE-mediated allergic response in mast cells and ICR mice. A list of eight compounds was selected based on pharmacophore and molecular docking, showing potential inhibitory effects through virtual screening. Among these compounds, sophoraflavanone G (SFG) was found to inhibit Syk activity in an enzymatic assay, with an IC50 value of 2.2 µM. To investigate the conformational dynamics of the SYK-SFG system, we performed molecular dynamics simulations. The stability of the binding between SFG and Syk was evaluated using root mean square deviation (RMSD) and root mean square fluctuation (RMSF). In RBL-2H3 cells, SFG demonstrated a dose-dependent suppression of IgE/BSA-induced mast cell degranulation, with no significant cytotoxicity observed at concentrations below 10.0 µM within 24 h. Furthermore, SFG reduced the production of TNF-α and IL-4 in RBL-2H3 cells. Mechanistic investigations revealed that SFG inhibited downstream signaling proteins, including phospholipase Cγ1 (PLCγ1), as well as mitogen-activated protein kinases (AKT, Erk1/2, p38, and JNK), in mast cells in a dose-dependent manner. Passive cutaneous anaphylaxis (PCA) experiments demonstrated that SFG could reduce ear swelling, mast cell degranulation, and the expression of COX-2 and IL-4. Overall, our findings identify naturally occurring SFG as a direct inhibitor of Syk that effectively suppresses mast cell degranulation both in vitro and in vivo.


Asunto(s)
Interleucina-4 , Mastocitos , Ratones , Animales , Interleucina-4/metabolismo , Interleucina-4/farmacología , Mastocitos/metabolismo , Anafilaxis Cutánea Pasiva , Simulación del Acoplamiento Molecular , Inmunoglobulina E/metabolismo , Inmunoglobulina E/farmacología , Ratones Endogámicos ICR , Ratones Endogámicos BALB C
2.
Pharmacol Res ; 175: 106029, 2022 01.
Artículo en Inglés | MEDLINE | ID: mdl-34896248

RESUMEN

The leaves of Morus alba L. (called Sangye in Chinese, ML), which belong to the genus Morus., are highly valuable edible plants in nutrients and nutraceuticals. In Asian countries including China, Japan and Korea, ML are widely used as functional foods including beverages, noodles and herbal tea because of its biological and nutritional value. Meanwhile, ML-derived products in the form of powders, extracts and capsules are widely consumed as dietary supplements for controlling blood glucose and sugar. Clinical studies showed that ML play an important role in the treatment of metabolic diseases including the diabetes, dyslipidemia, obesity, atherosclerosis and hypertension. People broadly use ML due to their nutritiousness, deliciousness, safety, and abundant active benefits. However, the systematic pharmacological mechanisms of ML on metabolic diseases have not been fully revealed. Therefore, in order to fully utilize and scale relevant products about ML, this review summarizes the up-to-date information about the ML and its constituents effecting on metabolic disease.


Asunto(s)
Enfermedades Metabólicas/tratamiento farmacológico , Morus , Preparaciones de Plantas/uso terapéutico , Animales , Etnobotánica , Humanos , Enfermedades Metabólicas/metabolismo , Enfermedades Metabólicas/prevención & control , Fitoterapia , Hojas de la Planta , Preparaciones de Plantas/química , Preparaciones de Plantas/farmacología
3.
Pharmacol Res ; 180: 106231, 2022 06.
Artículo en Inglés | MEDLINE | ID: mdl-35462011

RESUMEN

Several studies demonstrate the beneficial effects of dietary flavonoids on the cardiovascular system. Since perivascular adipose tissue (PVAT) plays an active role in the regulation of vascular tone in both health and diseases, the present study aimed to assess the functional interaction between PVAT and flavonoids in vitro on rat aorta rings. Several flavonoids proved to display both antispasmodic and spasmolytic activities towards noradrenaline-induced contraction of rings deprived of PVAT (-PVAT). However, on PVAT-intact (+PVAT) rings, both actions of some flavonoids were lost and/or much decreased. In rings-PVAT, the superoxide donor pyrogallol mimicked the effect of PVAT, while in rings+PVAT the antioxidant mito-tempol restored both activities of the two most representative flavonoids, namely apigenin and chrysin. The Rho-kinase inhibitor fasudil, or apigenin and chrysin concentration-dependently relaxed the vessel active tone induced by the Rho-kinase activator NaF; the presence of PVAT counteracted apigenin spasmolytic activity, though only in the absence of mito-tempol. Similar results were obtained in rings pre-contracted by phenylephrine. Finally, when ß3 receptors were blocked by SR59230A, vasorelaxation caused by both flavonoids was unaffected by PVAT. These data are consistent with the hypothesis that both noradrenaline and apigenin activated adipocyte ß3 receptors with the ensuing release of mitochondrial superoxide anion, which once diffused toward myocytes, counteracted flavonoid vasorelaxant activity. This phenomenon might limit the beneficial health effects of dietary flavonoids in patients affected by either obesity and/or other pathological conditions characterized by sympathetic nerve overactivity.


Asunto(s)
Superóxidos , Quinasas Asociadas a rho , Tejido Adiposo , Animales , Aorta , Apigenina , Flavonoides/farmacología , Humanos , Norepinefrina/farmacología , Parasimpatolíticos , Ratas
4.
Pharmacol Res ; 169: 105604, 2021 07.
Artículo en Inglés | MEDLINE | ID: mdl-33845125

RESUMEN

Diabetes mellitus is one of the biggest health emergencies of the 21st century worldwide, characterized by deficiency in insulin secretion and/or action, leading to hyperglycemia. Despite the currently available antidiabetic therapeutic options, 4.2 million people died in 2019 due to diabetes. Thus, new effective interventions are required. Polyphenols are plant secondary metabolites and have been recognized for their vast number of biological activities, including potential antidiabetic effects. However, the poor bioavailability and high metabolization of polyphenols restrict their biological effects in vivo. Nanotechnology is a promising area of research to improve the therapeutic effect of several compounds. Therefore, this review provides an overview of the literature about the utility of nano-based drug delivery systems as vehicles of polyphenols in diabetes treatment. It was possible to conclude that, in general, nano-based drug delivery systems can potentiate the beneficial antidiabetic properties of polyphenols, when compared with the free compounds, opening a new field of research in diabetology.


Asunto(s)
Diabetes Mellitus Tipo 1/tratamiento farmacológico , Hipoglucemiantes/administración & dosificación , Sistema de Administración de Fármacos con Nanopartículas , Animales , Humanos , Hipoglucemiantes/uso terapéutico , Sistema de Administración de Fármacos con Nanopartículas/administración & dosificación
5.
Pharmacol Res ; 174: 105919, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-34601080

RESUMEN

With the coming of the era of the aging population, hypertension has become a global health burden to be dealt with. Although there are multiple drugs and procedures to control the symptoms of hypertension, the management of it is still a long-term process, and the side effects of conventional drugs pose a burden on patients. Flavonoids, common compounds found in fruits and vegetables as secondary metabolites, are active components in Chinese Herbal Medicine. The flavonoids are proved to have cardiovascular benefits based on a plethora of animal experiments over the last decade. Thus, the flavonoids or flavonoid-rich plant extracts endowed with anti-hypertension activities and probable mechanisms were reviewed. It has been found that flavonoids may affect blood pressure in various ways. Moreover, despite the substantial evidence of the potential for flavonoids in the control of hypertension, it is not sufficient to support the clinical application of flavonoids as an adjuvant or core drug. So the synergistic effects of flavonoids with other drugs, pharmacokinetic studies, clinical trials and the safety of flavonoids are also incorporated in the discussion. It is believed that more breakthrough studies are needed. Overall, this review may shed some new light on the explicit recognition of the mechanisms of anti-hypertension actions of flavonoids, pointing out the limitations of relevant research at the current stage and the aspects that should be strengthened in future researches.


Asunto(s)
Antihipertensivos/uso terapéutico , Medicamentos Herbarios Chinos/uso terapéutico , Flavonoides/uso terapéutico , Animales , Antihipertensivos/clasificación , Medicamentos Herbarios Chinos/clasificación , Flavonoides/clasificación , Humanos , Medicina Tradicional China , Fitoterapia
6.
Pharmacol Res ; 158: 104939, 2020 08.
Artículo en Inglés | MEDLINE | ID: mdl-32445956

RESUMEN

The Coronavirus Disease 2019 (COVID-19) has been declared as a global pandemic, but specific medicines and vaccines are still being developed. In China, interventional therapies with traditional Chinese medicine for COVID-19 have achieved significant clinical efficacies, but the underlying pharmacological mechanisms are still unclear. This article reviewed the etiology of COVID-19 and clinical efficacy. Both network pharmacological study and literature search were used to demonstrate the possible action mechanisms of Chinese medicines in treating COVID-19. We found that Chinese medicines played the role of antivirus, anti-inflammation and immunoregulation, and target organs protection in the management of COVID-19 by multiple components acting on multiple targets at multiple pathways. AEC2 and 3CL protein could be the direct targets for inhibiting severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Quercetin, kaempferol, luteolin, isorhamnetin, baicalein, naringenin, and wogonin could be the main active ingredients of Chinese medicines for the management of COVID-19 by targeting on AEC2 and 3CL protein and inhibiting inflammatory mediators, regulating immunity, and eliminating free radicals through COX-2, CASP3, IL-6, MAPK1, MAPK14, MAPK8, and REAL in the signaling pathways of IL-17, arachidonic acid, HIF-1, NF-κB, Ras, and TNF. This study may provide meaningful and useful information on further research to investigate the action mechanisms of Chinese medicines against SARS-CoV-2 and also provide a basis for sharing the "China scheme" for COVID-19 treatment.


Asunto(s)
Betacoronavirus/efectos de los fármacos , Infecciones por Coronavirus/tratamiento farmacológico , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Fitoterapia , Neumonía Viral/tratamiento farmacológico , COVID-19 , Humanos , Modelos Biológicos , Pandemias , SARS-CoV-2 , Tratamiento Farmacológico de COVID-19
7.
Pharmacol Res ; 160: 105101, 2020 10.
Artículo en Inglés | MEDLINE | ID: mdl-32739428

RESUMEN

Influenza is a major public health problem worldwide. Mutations and resistance development make the use of antiviral therapy challenging. Chinese patent medicines are often used to treat influenza in China and well tolerable. However, the misuse of Chinese patent medicines is common. We therefore aimed to develop an evidence-based guideline on treating influenza with Chinese patent medicines in adults to guide clinical practice. We formed a steering committee, a consensus panel, a consultants' group and an evidence synthesis team to guide the development of the guideline. We formulated the clinical questions through two rounds of survey, and finally selected five questions. We then systematically searched the related evidence and conducted meta-analyses, evidence summaries and GRADE decision tables to draft the recommendations, which the consensus panel then voted on using the Delphi method. Finally, we formulated six recommendations based on the evidence synthesis and experts' consensus. For treating mild influenza, we suggest either Lianhua Qingwen capsule, Jinhua Qinggan granule, Banlangen granule, Shufeng Jiedu capsule, or Jinfang Baidu pill, depending on the manifestations. For severe influenza, or mild influenza in patients at high risk of developing severe influenza, we suggest Lianhua Qingwen capsule in combination with antiviral medications and supportive therapy. The strength of all recommendations was weak. Traditional Chinese medicine has great potential to help in the fight against influenza worldwide, but more high-quality studies are still needed to strengthen the evidence.


Asunto(s)
Medicamentos Herbarios Chinos/uso terapéutico , Gripe Humana/tratamiento farmacológico , Medicina Tradicional China , Medicamentos sin Prescripción/uso terapéutico , Adulto , Guías como Asunto , Humanos
8.
Pharmacol Res ; 159: 104795, 2020 09.
Artículo en Inglés | MEDLINE | ID: mdl-32278035

RESUMEN

Cerebral ischemia reperfusion injury (CIRI), one of the major causes of death from stroke in the world, not only causes tremendous damage to human health, but also brings heavy economic burden to society. Current available treatments for CIRI, including mechanical therapies and drug therapies, are often accompanied by significant side-effects. Therefore, it is necessary to discovery new strategies for treating CIRI. Many studies have confirmed that the herbal medicine has the advantages of abundant resources, good curative effect and little side effects, which can be used as potential drug for treatment of CIRI through multiple targets. It's known that oral administration commonly has low bioavailability, and injection administration is inconvenient and unsafe. Many drugs can't delivery to brain through routine pathways due to the blood-brain-barrier (BBB). Interestingly, increasing evidences have suggested the nasal administration is a potential direct route to transport drug into brain avoiding the BBB and has the characteristics of high bioavailability for treating brain diseases. Therefore, intranasal administration can be treated as an alternative way to treat brain diseases. In the present review, effective methods to treat CIRI by using active ingredients derived from herbal medicine through nose to brain drug delivery (NBDD) are updated and discussed, and some related pharmacological mechanisms have also been emphasized. Our present study would be beneficial for the further drug development of natural agents from herbal medicines via NBDD.


Asunto(s)
Isquemia Encefálica/tratamiento farmacológico , Encéfalo/efectos de los fármacos , Mucosa Nasal/metabolismo , Preparaciones de Plantas/administración & dosificación , Daño por Reperfusión/tratamiento farmacológico , Administración Intranasal , Animales , Disponibilidad Biológica , Encéfalo/metabolismo , Encéfalo/patología , Isquemia Encefálica/metabolismo , Isquemia Encefálica/patología , Composición de Medicamentos , Humanos , Preparaciones de Plantas/metabolismo , Daño por Reperfusión/metabolismo , Daño por Reperfusión/patología , Distribución Tisular
9.
Pharmacol Res ; 148: 104409, 2019 10.
Artículo en Inglés | MEDLINE | ID: mdl-31446039

RESUMEN

It is a common phenomenon that people are in a sub-health condition and facing "unexplained fatigue", which seriously affects their health, work efficiency and quality of life. Meanwhile, fatigue is also a common symptom of many serious diseases such as HIV/AIDS, cancer, and schizophrenia. However, there are still no official recommendations for the treatment of various forms of fatigue. Some traditional natural medicines are often used as health care products, such as ginseng, Cordyceps militaris (L.ex Fr.Link) and Rhodiola rosea L., and these have been reported to have specific anti-fatigue effects with small toxic and side effects and rich pharmacological activities. It may be promising treatment strategy for sub-health. In this review, we first outline the generation of fatigue. Furthermore, we put emphasis on the anti-fatigue mechanism, bioactive components, and clinic trials of natural medicines, which will contribute to the development of potential anti-fatigue agents and open up novel treatments for sub-health.


Asunto(s)
Productos Biológicos/farmacología , Productos Biológicos/uso terapéutico , Fatiga/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Animales , Humanos , Medicina Tradicional/métodos , Fitoterapia/métodos , Calidad de Vida
10.
Pharmacol Res ; 142: 176-191, 2019 04.
Artículo en Inglés | MEDLINE | ID: mdl-30818043

RESUMEN

As an important component of complementary and alternative medicines, traditional Chinese medicines (TCM) are gaining more and more attentions around the world because of the powerful therapeutic effects and less side effects. However, there are still some doubts about TCM because of the questionable TCM theories and unclear biological active compounds. In recent years, gut microbiota has emerged as an important frontier to understand the development and progress of diseases. Together with this trend, an increasing number of studies have indicated that drug molecules can interact with gut microbiota after oral administration. In this context, more and more studies pertaining to TCM have paid attention to gut microbiota and have yield rich information for understanding TCM. After oral administration, TCM can interact with gut microbiota: (1) TCM can modulate the composition of gut microbiota; (2) TCM can modulate the metabolism of gut microbiota; (3) gut microbiota can transform TCM compounds. During the interactions, two types of metabolites can be produced: gut microbiota metabolites (of food and host origin) and gut microbiota transformed TCM compounds. In this review, we summarized the interactions between TCM and gut microbiota, and the pharmacological effects and features of metabolites produced during interactions between TCM and gut microbiota. Then, focusing on gut microbiota and metabolites, we summarized the aspects in which gut microbiota has facilitated our understanding of TCM. At the end of this review, the outlooks for further research of TCM and gut microbiota were also discussed.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Microbioma Gastrointestinal/efectos de los fármacos , Medicina Tradicional China , Animales , Humanos
11.
Pharmacol Res ; 147: 104367, 2019 09.
Artículo en Inglés | MEDLINE | ID: mdl-31344423

RESUMEN

The dynamic and delicate interactions amongst intestinal microbiota, metabolome and metabolism dictates human health and disease. In recent years, our understanding of gut microbial regulation of intestinal immunometabolic and redox homeostasis have evolved mainly out of in vivo studies associated with high-fat feeding induced metabolic diseases. Techniques utilizing fecal transplantation and germ-free mice have been instrumental in reproducibly demonstrating how the gut microbiota affects disease pathogenesis. However, the pillars of modern drug discovery i.e. evidence-based pharmacological studies critically lack focus on intestinal microflora. This is primarily due to targeted in vitro molecular-approaches at cellular-level that largely overlook the etiology of disease pathogenesis from the physiological perspective. Thus, this review aims to provide a comprehensive understanding of the key notions of intestinal microbiota and dysbiosis, and highlight the microbiota-phytochemical bidirectional interactions that affects bioavailability and bioactivity of parent phytochemicals and their metabolites. Potentially by focusing on the three major aspects of gut microbiota i.e. microbial abundance, diversity, and functions, I will discuss phytochemical-microbiota reciprocal interactions, biotransformation of phytochemicals and plant-derived drugs, and pre-clinical and clinical efficacies of herbal medicine on dysbiosis. Additionally, in relation to phytochemical pharmacology, I will briefly discuss the role of dietary-patterns associated with changes in microbial profiles and review pharmacological study models considering possible microbial effects. This review therefore, emphasize on the timely and critically needed evidence-based phytochemical studies focusing on gut microbiota and will provide newer insights for future pre-clinical and clinical phytopharmacological interventions.


Asunto(s)
Microbioma Gastrointestinal/efectos de los fármacos , Fitoquímicos/farmacología , Fitoterapia , Animales , Biotransformación , Dieta , Humanos , Fitoquímicos/farmacocinética
12.
Pharmacol Res ; 130: 273-291, 2018 04.
Artículo en Inglés | MEDLINE | ID: mdl-29305909

RESUMEN

Inflammation is one of the major causative factor of cancer and chronic inflammation is involved in all the major steps of cancer initiation, progression metastasis and drug resistance. The molecular mechanism of inflammation driven cancer is the complex interplay between oncogenic and tumor suppressive transcription factors which include FOXM1, NF-kB, STAT3, Wnt/ß- Catenin, HIF-1α, NRF2, androgen and estrogen receptors. Several products derived from natural sources modulate the expression and activity of multiple transcription factors in various tumor models as evident from studies conducted in cell lines, pre-clinical models and clinical samples. Further combination of these natural products along with currently approved cancer therapies added an additional advantage and they considered as promising targets for prevention and treatment of inflammation and cancer. In this review we discuss the application of multi-targeting natural products by analyzing the literature and future directions for their plausible applications in drug discovery.


Asunto(s)
Antineoplásicos/uso terapéutico , Productos Biológicos/uso terapéutico , Neoplasias/tratamiento farmacológico , Polifenoles/uso terapéutico , Factores de Transcripción/metabolismo , Animales , Humanos , Terapia Molecular Dirigida , Neoplasias/metabolismo
13.
J Ethnopharmacol ; 332: 118395, 2024 Oct 05.
Artículo en Inglés | MEDLINE | ID: mdl-38801915

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Rosmarinus officinalis L. (Rosemary) is a popular herb with reported effectiveness against diarrhea, anxiety and constipation, albeit with limited pharmacological evidence. AIM OF THE STUDY: The current study was aimed at evaluating the therapeutic potential, possible pharmacological mechanisms of action and active constituents of hydro-ethanolic extract of rosemary (Rs.Cr), as potential anti-diarrheal, laxative and anxiolytic agent. METHOD: Rs.Cr was analyzed through reverse-phase high pressure liquid chromatography (RP-HPLC). Laxative, antidiarrheal, and anxiolytic activities were assessed using in vivo models. Spasmogenic and spasmolytic mechanisms were studied on isolated guinea pig ileum and rabbit jejunum tissues, respectively. Possible role of diosmetin, one of the active constituents of Rs.Cr was also evaluated. RESULTS: RP-HPLC analysis revealed presence of diosmetin, rutin and apigenin in Rs.Cr. Laxative effect was seen at low doses, which was partially reversed in atropinized mice. The spasmogenic mechanism was mediated by cholinergic and histaminergic receptors stimulation. At higher doses, antidiarrheal activity was evident, with reduction in gastrointestinal motility and secretions using charcoal meal and enteropooling assays, respectively. Rs.Cr also showed dose-dependent anxiolytic effect. The antispasmodic mechanisms were mediated by anti-muscarinic and K+ channel opening-like effect (predominant KATP-dependent). Diosmetin exhibited antidiarrheal and antispasmodic activities, but spasmogenic effect was not seen. CONCLUSION: Rosemary leaves have dual antidiarrheal and laxative effects, and as well as anxiolytic activity. In addition, the possible modulation of muscarinic and histaminergic receptors, and KATP channels show it as potential herb to be explored for irritable bowel syndrome. Diosmetin is possibly one of its constituents that contributes to its antidiarrheal activity.


Asunto(s)
Ansiolíticos , Motilidad Gastrointestinal , Íleon , Extractos Vegetales , Rosmarinus , Animales , Cobayas , Rosmarinus/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Ratones , Masculino , Motilidad Gastrointestinal/efectos de los fármacos , Conejos , Ansiolíticos/farmacología , Ansiolíticos/aislamiento & purificación , Ansiolíticos/química , Íleon/efectos de los fármacos , Íleon/metabolismo , Íleon/fisiología , Antidiarreicos/farmacología , Antidiarreicos/aislamiento & purificación , Flavonoides/farmacología , Parasimpatolíticos/farmacología , Parasimpatolíticos/aislamiento & purificación , Laxativos/farmacología , Laxativos/aislamiento & purificación , Yeyuno/efectos de los fármacos , Yeyuno/metabolismo , Diarrea/tratamiento farmacológico , Femenino
14.
J Ethnopharmacol ; 325: 117768, 2024 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-38253275

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Atherosclerosis (AS), a lipid-induced inflammatory condition of the arteries, is a primary contributor to atherosclerotic cardiovascular diseases including stroke. Arctium lappa L. leaf (ALL), an edible and medicinal herb in China, has been documented and commonly used for treating stroke since the ancient times. However, the elucidations on its anti-AS effects and molecular mechanism remain insufficient. AIM OF THE STUDY: To investigate the AS-ameliorating effects and the underlying mechanism of action of an ethanolic extract of leaves of Arctium lappa L. (ALLE). MATERIALS AND METHODS: ALLE was reflux extracted using with 70% ethanol. An HPLC method was established to monitor the quality of ALLE. High fat diet (HFD) and vitamin D3-induced experimental AS in rats were used to determine the in vivo effects; and oxidized low-density lipoprotein-induced RAW264.7 macrophage foam cells were used for in vitro assays. Simvatatin was used as positive control. Biochemical assays were implemented to ascertain the secretions of lipids and pro-inflammatory mediators. Haematoxylin-eosin (H&E) and Oil red O stains were employed to assess histopathological alterations and lipid accumulation conditions, respectively. CCK-8 assays were used to measure cytotoxicity. Immunoblotting assay was conducted to measure protein levels. RESULTS: ALLE treatment significantly ameliorated lipid deposition and histological abnormalities of aortas and livers in AS rats; improved the imbalances of serum lipids including total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C) and high-density lipoprotein cholesterol (HDL-C); notably attenuated serum concentrations of inflammation-associated cytokines/molecules including TNF-α, IL-6, IL-1ß, VCAM-1, ICAM-1and MMP-9. Mechanistic studies demonstrated that ALLE suppressed the phosphorylation/activation of PI3K, Akt and NF-κB in AS rat aortas and in cultured foam cells. Additionally, the PI3K agonist 740Y-P notably reversed the in vitro inhibitory effects of ALLE on lipid deposition, productions of TC, TNF-α and IL-6, and protein levels of molecules of PI3K/Akt and NF-κB singnaling pathways. CONCLUSIONS: ALLE ameliorates HFD- and vitamin D3-induced experimental AS by modulating lipid metabolism and inflammatory responses, and underlying mechanisms involves inhibition of the PI3K/Akt and NF-κB singnaling pathways. The findings of this study provide scientific justifications for the traditional application of ALL in managing atherosclerotic diseases.


Asunto(s)
Arctium , Aterosclerosis , Fragmentos de Péptidos , Receptores del Factor de Crecimiento Derivado de Plaquetas , Accidente Cerebrovascular , Ratas , Animales , FN-kappa B/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Transducción de Señal , Fosfatidilinositol 3-Quinasas/metabolismo , Metabolismo de los Lípidos , Factor de Necrosis Tumoral alfa/metabolismo , Interleucina-6/metabolismo , Aterosclerosis/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Lípidos , Colesterol/farmacología , Etanol/farmacología , Lipoproteínas LDL/metabolismo , Colecalciferol/farmacología , Colecalciferol/uso terapéutico
15.
Food Chem ; 438: 137863, 2024 Apr 16.
Artículo en Inglés | MEDLINE | ID: mdl-37980871

RESUMEN

Unripe tomatoes are among the main waste produced during tomato cultivation and processing. In this study, unripe tomatoes from seven different Italian cultivars have been investigated to evaluate their nutraceutical potential. Phytochemical investigation allowed shedding light on the identification of seventy-five bioactive compounds. The highest amount of polyphenolic and glycoalkaloids along with the high level of antioxidant activities was found in the Datterini tomatoes variety. The peculiarity of this variety is the high chlorogenic acid content, being ten times higher compared to the other cultivars examined. Moreover, the total α-tomatine amount has been found substantially higher (34.699 ± 1.101 mg/g dry weight) with respect to the other tomato varieties analyzed. Furthermore, the cultivars metabolomic profiles were investigated with the PCA approach. Based on Datterini cultivar's metabolomic profile, its waste-recovery could represent a good option for further added value products in pharmaceutical and nutraceutical areas with a high α-tomatine content.


Asunto(s)
Antioxidantes , Solanum lycopersicum , Antioxidantes/química , Ácido Clorogénico , Fitoquímicos , Extractos Vegetales/química
16.
Food Chem ; 398: 133849, 2023 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-35985240

RESUMEN

A promising drying technology, namely combined freeze-drying and far-infrared drying (FD-FIRD) was employed to dehydrate seed-used pumpkin (SUP) and its effects on physical characteristics (color, microstructure, texture, shrinkage), bioactive components (phenolics and carotenoids) of SUP were evaluated. The low-field nuclear magnetic resonance (LF-NMR) was used to analyze moisture state and distribution during FD process, which is beneficial for choosing appropriate moisture transfer point. Results showed that most free water (87.29 %) was removed when drying time reached 25 h, thus retaining original tissue structure of sample with almost no deformation during later FIRD process. Therefore, FD for 25 h followed by FIRD for 2 h (FD25-FIRD2) sample exhibited similar appearance with FD sample. The free phenolics content of FD-FIRD samples was 14.97 %-26.60 % higher than that of FD depending on FIRD duration. Especially, p-coumaric acid content of FD25-FIRD2 sample increased of 32.23 %. Besides, FD-FIRD performed higher retention for carotenoids showing 3.00-3.39 folds than FIRD.


Asunto(s)
Cucurbita , Antioxidantes/química , Carotenoides/análisis , Fenoles/análisis , Semillas/química , Tecnología
17.
Carbohydr Polym ; 304: 120491, 2023 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-36641178

RESUMEN

BACKGROUND: Chitosan-based particles are one of the most promising Pickering emulsions stabilizers due to its cationic properties, cost-effective, biocompatibility, biodegradability. However, there are currently no comprehensive reviews analyzing the role of chitosan to develop Pickering emulsions, and the bioavailability and multiple uses of these emulsions. SCOPE AND APPROACH: This review firstly summarizes the types, preparation and functional properties of chitosan-based Pickering emulsion stabilizers, followed by in vivo and in vitro bioavailability, main regulations, and future application and trends. KEY FINDINGS AND CONCLUSIONS: Stabilizers used in chitosan-based Pickering emulsions include 6 categories: chitosan self-aggregating particles and 5 types of composites (chitosan-protein, chitosan-polysaccharide, chitosan-fatty acid, chitosan-polyphenol, and chitosan-inorganic). Chitosan-based Pickering emulsions improved the bioavailability of different compounds compared to traditional emulsions. Current applications include hydrogels, microcapsules, food ingredients, bio-based films, cosmeceuticals, porous scaffolds, environmental protection agents, and interfacial catalysis systems. However, due to current limitations, more research and development are needed to be extensively explored to meet consumer demand, industrial manufacturing, and regulatory requirements. Thus, optimization of stabilizers, bioavailability studies, 3D4D printing, fat substitutes, and double emulsions are the main potential development trends or research gaps in the field which would contribute to increase adoption of these promising emulsions at industrial level.


Asunto(s)
Quitosano , Emulsiones , Disponibilidad Biológica , Tamaño de la Partícula
18.
Food Chem ; 414: 135646, 2023 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-36841106

RESUMEN

An environmentally friendly physical processing method, hydrothermal treatment (HT), was used to increase the content of specific compounds and antioxidant activities of seed-used pumpkin byproducts. The influence of hydrothermal temperature (80 °C-160 °C) and time (30-150 min) on changes in polyphenols and antioxidation was evaluated. The results revealed that the maximum free polyphenol content (140 °C for 120 min) was 3.96-fold higher than the untreated samples. Elevated temperature and long duration changed phenolic acid contents. For example, p-coumaric acid, rutin and chlorogenic acid exhibited a decreasing trend, and p-hydroxybenzoic acid, quercetin and cinnamic acid showed an increasing trend. Compared to controls, HT was significantly associated with increased antioxidant activities. To comprehensively reveal the influence of hydrothermal temperature and time on changes in polyphenolic content, back propagation artificial neural network (BP-ANN) models with accurate prediction ability were developed, and the results exhibited well-fitted and strong approximation ability (R2 > 0.95 and RMSE < 2 %) and stability.


Asunto(s)
Antioxidantes , Cucurbita , Fenoles/análisis , Extractos Vegetales , Polifenoles/análisis , Semillas/química
19.
Food Chem X ; 19: 100812, 2023 Oct 30.
Artículo en Inglés | MEDLINE | ID: mdl-37780323

RESUMEN

Harvested jujube (Zizyphus jujuba Mill) is prone to softening due to active metabolism. This study investigated the effects of acidic electrolyzed water (AEW), high-voltage electrostatic field (HVEF) and their combination (AEW + HVEF) on softening and associated cell wall degrading enzymes (CWDEs), cell membrane integrity and antioxidant system of 'Huping' jujube during storage at 0 ± 1 °C. The results indicated that fruit subjected to AEW + HVEF, AEW or HVEF treatments maintained firmness 15.7%, 10.7%, and 5.3% higher than that of untreated control fruit at the end of 90 days cool storage. Fruit treated with AEW + HVEF could better maintain cell membrane integrity and exhibit lower activities of CWDEs and higher antioxidant capacity than that treated with either AEW or HVEF. Correlation analysis suggested that inhibition of softening was associated with reduction of CWDEs activities, and maintenance of membrane integrity and antioxidant system.

20.
J Ethnopharmacol ; 302(Pt A): 115870, 2023 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-36341819

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Rubus idaeus Linnaeus (RI) is a Chinese herbal medicine that has been widely used in China for a long time to reinforce the kidney, nourish the liver, improve vision, and arrest polyuria. AIM OF THE STUDY: This work aims to evaluate the recent progress of the chemical composition, pharmacological activity, pharmacokinetics, metabolism, and quality control and of Rubus idaeus, which focuses on the insufficiency of existing research and will shed light on future studies of Rubus idaeus. METHODS: Literatures about "Rubus idaeus","Red raspberry" and "Fupenzi"are retrieved by browsing the database, such as Web of Science (http://www.webofknowledge.com/wos), Pubmed (https://pubmed.ncbi.nlm.nih.gov/), CNKI (http://www.cnki.net/), and Wanfang Data (http://www.wanfangdata.com.cn). In addition, related textbooks and digital documents are interrogated to provide a holistic and critical review of the topic. The period of the literature covered from 1981 to 2022. RESULTS: Approximately 194 compounds have been isolated from Rubus idaeus, which is rich in phenols, terpenoids, alkaloids, steroids, and fatty acids. Numerous investigations have demonstrated that Rubus idaeus exhibits many pharmacological activities, including hypoglycemic and hypolipidemic, anti-Alzheimer effect, anti-osteoporosis, hepatoprotective, anti-cancer, neuroprotective, anti-bacteria and skin care, etc. However, it is worth noting that most of the research is not associated with the conventional effect, such as reducing urination and treating opacity of the cornea. CONCLUSION: The effectiveness of Rubus idaeus has been proved by its long-term clinical application. The research on the pharmacological activity of Rubus idaeus has flourished. In many pharmacological experiments, only the high-dose group can achieve the corresponding efficacy, so the efficacy of Rubus idaeus needs to be further interrogated. Meanwhile, the relationship between pharmacological activity and specific compounds of Rubus idaeus has not been clarified yet. Last but not least, studies involving toxicology and pharmacokinetics are very limited. Knowledge of bioavailability and toxicological behavior of Rubus idaeus can help understand the herb's pharmacodynamic and safety profile.


Asunto(s)
Etnobotánica , Rubus , Etnofarmacología , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Control de Calidad , Fitoterapia
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