Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 28
Filtrar
Mais filtros











Base de dados
Intervalo de ano de publicação
1.
Biomed Pharmacother ; 177: 117118, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-39002440

RESUMO

Hepatocellular carcinoma (HCC) is one of the most prevalent malignant tumors in the contemporary era, representing a significant global health concern. Early HCC patients have mild symptoms or are asymptomatic, which promotes the onset and progression of the disease. Moreover, advanced HCC is insensitive to chemotherapy, making traditional clinical treatment unable to block cancer development. Sorafenib (SFB) is a first-line targeted drug for advanced HCC patients with anti-angiogenesis and anti-tumor cell proliferation effects. However, the efficacy of SFB is constrained by its off-target distribution, rapid metabolism, and multi-drug resistance. In recent years, nanoparticles based on a variety of materials have been demonstrated to enhance the targeting and therapeutic efficacy of SFB against HCC. Concurrently, the advent of joint drug delivery systems has furnished crucial empirical evidence for reversing SFB resistance. This review will summarize the application of nanotechnology in the field of HCC treatment over the past five years. It will focus on the research progress of SFB delivery systems combined with multiple therapeutic modalities in HCC treatment.


Assuntos
Antineoplásicos , Carcinoma Hepatocelular , Sistemas de Liberação de Medicamentos , Neoplasias Hepáticas , Sorafenibe , Humanos , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/patologia , Sorafenibe/administração & dosagem , Sorafenibe/uso terapêutico , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia , Antineoplásicos/administração & dosagem , Antineoplásicos/uso terapêutico , Sistemas de Liberação de Medicamentos/métodos , Animais , Nanopartículas , Resistencia a Medicamentos Antineoplásicos
2.
J Ethnopharmacol ; 335: 118615, 2024 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-39069030

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Amomum villosum Lour. is a widely esteemed species of medicinal plant on a global scale. Its medicinal properties have been documented as early as the Tang Dynasty, particularly the fruit, which holds significant medicinal and culinary value. This plant is extensively found in tropical and subtropical regions across Asia. It possesses the properties of warming the middle and dispelling cold, regulating Qi to invigorate the spleen, harmonizing the stomach to alleviate vomiting, and nourishing deficiencies. In recent years, A. villosum has garnered global attention for its remarkable biological activity. Currently, numerous bioactive compounds have been successfully isolated and identified, showcasing a diverse array of pharmacological activities and medicinal benefits. AIM OF THE WORK: This review aims to provide a comprehensive analysis of the research advancements in the geographical distribution, botany, traditional applications, phytochemistry, pharmacological activity, quality control, clinical applications, and toxicology of A. villosum. Furthermore, a critical summary of the current research and future prospects of this plant is presented. MATERIALS AND METHODS: Obtain information about A. villosum from ancient literature, doctoral and master's theses, and scholarly databases including Google Scholar, Web of Science, PubMed, China National Knowledge Infrastructure (CNKI), ScienceDirect, plant directories, and clinical reports. RESULTS: At present, about 500 compounds have been isolated and identified from various organs of A. villosum, including monoterpenoids, sesquiterpenoids, diterpenoids, flavonoids, phenols, polysaccharides, and other components. Modern pharmacological studies have revealed that A. villosum exhibits exceptional biological activities in vitro and in vivo, such as anti-inflammatory, antioxidant, liver protection, anti-tumor, hypoglycemic, anti-microbial, regulating gastrointestinal activity, immune regulation, regulating flora, anti-obesity, estrogen, and more. Some of these activities have found extensive application in clinical practice. CONCLUSION: A. villosum, as a well-established medicinal herb, holds significant therapeutic potential and is also valued for its culinary applications. Currently, the research on the active components or crude extracts of A. villosum and their potential mechanisms of action remains limited. Furthermore, certain pharmacological activities require further elucidation for a comprehensive understanding of its internal mechanisms. Moreover, it is strongly recommended to prioritize research on pharmacokinetics and toxicity studies. These efforts will facilitate a thorough exploration of the potential of A. villosum and establish a robust foundation for its potential clinical applications.

3.
J Ethnopharmacol ; 332: 118403, 2024 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-38821137

RESUMO

ETHNOPHARMACOLOGIC RELEVANCE: Valeriana jatamansi Jones, belongs to the Valerianaceae family, is widely used in traditional Chinese medicine (TCM) and Ayurveda, traditional Indian medicine (TIM). This traditional herb has been officially listed in the pharmacopoeia of sixteen countries. Its usage was first described in Diannan Bencao, also known as "Zhizhuxiang", is a famous folk medicine herb with a long history of medicinal usage in China, and it was used to treat indigestion, flu, and mental disorders in the Han, Achang, Bai, Blang, Dai, Jingpo, Naxi, and Wa ethnic groups. In recent years, V. jatamansi has attracted worldwide attention as an important medicinal due to its pharmacological activity especially in nervous and digestive systems, and multiple uses. AIM OF THE STUDY: The current review aims to provide a comprehensive analysis of the botany, traditional uses, phytochemistry, pharmacology, toxicity, and quality control of V. jatamansi. MATERIALS AND METHODS: The relevant information of V. jatamansi was obtained from several databases including Web of Science, PubMed, ACS Publications, Google Scholar, Baidu Scholar, CNKI, Ph.D. and MSc dissertations, using "Valeriana jatamansi Jones", "Valeriana jatamansi", and "" as keywords. After eliminating repetitive and low-quality reports, the remaining reports were analyzed and summarized to prepare this review. Plant information was retrieved by www.worldfloraonline.org and www.gbif.org using "Valeriana jatamansi Jones" as keyword. RESULTS: V. jatamansi has been historically utilized as a traditional medicine to treat various diseases, including infectious, inflammatory, neurological, and gastrointestinal disorders. More than 400 compounds have been identified in V. jatamansi including iridoids, volatile oils, lignans, flavonoids, phenolic acids, phenylpropanoids, sesquiterpenes, sesquiterpene hydrocarbons, triterpenes as well as other compounds. The plant extracts and compounds showed various pharmacological activities such as antitumor, cytotoxic, antivirus, etc. In addition, V. jatamansi has found various applications in the agricultural, food, and cosmetics industry. CONCLUSION: A review of literature shows V. jatamansi has pharmacological properties valuable in treating diseases, particularly for antianxiety and gastrointestinal disorders. Despite a wide spectrum of effects from specific compounds, research mainly focuses on in vitro and in vivo, with a lack of pharmacokinetics, clinical trials and underlying mechanisms. Consequently, it becomes important to embark on additional researchs to elucidate the pharmacokinetics, material basis and mechanisms of V. jatamansi, thereby realizing the aspiration of its comprehensive utilization and sustainable development.


Assuntos
Etnofarmacologia , Compostos Fitoquímicos , Controle de Qualidade , Valeriana , Valeriana/química , Humanos , Animais , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Fitoterapia , Medicina Tradicional
4.
ACS Omega ; 9(19): 20773-20790, 2024 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-38764633

RESUMO

Lingzhu Pulvis is a classic formulation for treating febrile convulsions in children. However, Acorus tatarinowii essential oil (AT-EO) in this prescription is prone to volatilization and oxidation, compromising the efficacy and quality control of this formulation. Herein, based on the concept of "combination of medicine and adjuvant", Pickering emulsion technology was applied to enhance the stability of AT-EO using modified amber as a stabilizer. Amber was a resinous medicinal powder in Lingzhu Pulvis and was modified into a suitable stabilizer for Pickering emulsion through surface modification. A thermal stability study indicated that Pickering emulsion, stabilized by modified amber, exhibited a higher retention rate of AT-EO and lower levels of peroxide value and malondialdehyde content compared to those of the pure AT-EO group after heat treatment at 40 °C for 1, 3, and 8 h. Additionally, component analysis in content and composition revealed that the volatile components of AT-EO in the Pickering emulsion were more stable during the thermal treatment process. This study convincingly illustrates the potential of a Pickering emulsion stabilized with modified medicinal powders to improve the thermal stability of the essential oil.

5.
J Ethnopharmacol ; 326: 117979, 2024 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-38412892

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Mesona chinensis Benth. (or Platostoma palustre (Blume) A. J. Paton) is an important medicinal and edible plant also known as the Hsian-tsao in China and Southeast Asian countries. It is cold in nature and sweet in taste, with the effects of clearing heat, relieving heatstroke and diuretic, and traditionally used to treat heatstroke, erysipelas, hypertension, joint pain and other diseases in folk medicine. It is also a popular supplement with the function of detoxifying and heat-clearing use in Asia. It is used to be processed into the popular tea, Bean jelly, and so on. Published studies have demonstrated that polysaccharides from M. chinensis (MCPs) are one of the principal bioactive ingredients with a variety of health-promoting effects in the prevention and treatment of diseases, including antioxidant, immunomodulation, anti-inflammatory, hepatoprotective, anti-tumor, hypoglycemic, regulation of gut microbiota, and other pharmacological properties. AIM OF THE REVIEW: This review aims to compile the extraction and purification methods, structural characteristics, pharmacological activities including the mechanism of action of MCPs, and to further understand the applications of M. chinensis in order to lay the foundation for the development of MCPs. MATERIALS AND METHODS: By inputting the search term "Mesona chinensis polysaccharides", relevant research information was obtained from databases such as PubMed, Google Scholar, Web of Science, and China National Knowledge Infrastructure (CNKI). RESULTS: More than 40 polysaccharides have been extracted from M. chinensis, different extraction and purification methods have been described, as well as the structural features and pharmacological activities of MCPs have been systematically reviewed. Polysaccharides, as important components of M. chinensis, were mainly extracted by methods such as hot water dipping method, hot alkali extraction method, enzyme-assisted extraction method and ultrasonic-assisted extraction method, subsequently obtained by decolorization, deproteinization, removal of other small molecules and separation on various chromatographic columns. The chemical composition and structure of MCPs show diversity and have a variety of pharmacological activities, including antioxidant, immunomodulation, anti-inflammatory, hepatoprotective, anti-tumor, hypoglycemic, regulation of gut microbiota, and so on. CONCLUSIONS: This article systematically reviews the research progress of MCPs in terms of extraction and purification, structural characteristics, rheological gel properties, pharmacological properties, and safety assessment. The potentials and roles of M. chinensis in the field of medicine, functional food, and materials are further highlighted to provide references and bases for the high-value processing and utilization of MCPs.

6.
Int J Biol Macromol ; 262(Pt 2): 130030, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38336330

RESUMO

Schisandra chinensis, as a famous medicinal and food homologous plant, has a long history of medicinal and dietary therapy. It has the functions of nourishing the kidney, calming the heart, tranquilising the mind, tonifying Qi and producing fluid to relieve mental stress, based on the theory of traditional Chinese medicine. Accumulating evidence has shown that S. chinensis polysaccharides (SCPs) are one of the most important bioactive macromolecules and exhibit diverse biological activities in vitro and in vivo, including neuroprotective, hepatoprotective, immunomodulatory, antioxidant, hypoglycemic, cardioprotective, antitumour and anti-inflammatory activities, etc. This review aims to thoroughly review the recent advances in the extraction and purification methods, structural features, biological activities and structure-activity relationships, potential applications and quality assessment of SCPs, and further highlight the therapeutic potentials and health functions of SCPs in the fields of therapeutic agents and functional food development. Future insights and challenges of SCPs were also critically discussed. Overall, the present review provides a theoretical overview for the further development and utilization of S. chinensis polysaccharides in the health food and pharmaceutical fields.


Assuntos
Extratos Vegetais , Schisandra , Extratos Vegetais/química , Schisandra/química , Antioxidantes/farmacologia , Dieta , Polissacarídeos/química
7.
Int J Biol Macromol ; 259(Pt 1): 129047, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38171434

RESUMO

Platycodon grandiflorum, a globally recognized medicinal and edible plant, possesses significant nutritional value and pharmacological value. In traditional Chinese medicine, it has the effects of tonifying the spleen and replenishing the Qi, moistening the lung and relieving the cough, clearing the heat and detoxifying, and relieving the pain. Accumulating evidence has revealed that the polysaccharides from P. grandiflorum (PGPs) are one of the major and representative biologically active macromolecules and have diverse biological activities, such as immunomodulatory activity, anti-inflammatory activity, anti-tumor activity, regulation of the gut microbiota, anti-oxidant activity, anti-apoptosis activity, anti-angiogenesis activity, hypoglycemic activity, anti-microbial activity, and so on. Although the polysaccharides extracted from P. grandiflorum have been extensively studied for the extraction and purification methods, structural characteristics, and pharmacological activities, the knowledge of their structures and bioactivity relationship, toxicologic effects, and pharmacokinetic profile is limited. The main purpose of the present review is to provide comprehensively and systematically reorganized information on extraction and purification, structure characterizations, and biological functions as well as toxicities of PGPs to support their therapeutic potentials and sanitarian functions. New valuable insights for future research regarding PGPs were also proposed in the fields of therapeutic agents and functional foods.


Assuntos
Platycodon , Humanos , Platycodon/química , Polissacarídeos/farmacologia , Polissacarídeos/química , Medicina Tradicional Chinesa , Baço , Tosse
8.
Int J Biol Macromol ; 259(Pt 2): 129193, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38191106

RESUMO

Dandelion (Taraxacum mongolicum Hand.-Mazz), as a famous medicinal and edible plant, has the effects of clearing heat and detoxifying, diuresis, and resolving masses. Phytochemistry investigations revealed that T. mongolicum has various bioactive ingredients, mainly including flavonoids, sterols, polysaccharides, phenolic acids and volatile oils. There is growing evidence have shown that the polysaccharides from T. mongolicum (TMPs) are a class of representative pharmacologically bioactive macromolecules with a variety of biological activities both in vitro and in vivo, such as immunomodulatory, anti-inflammatory, anti-oxidant, anti-tumor, hepatoprotective, hypolipidemic and hypoglycemic, anti-bacterial, regulation of intestinal microbial, and anti-fatigue activities, etc. Additionally, the structural modification and potential applications of TMPs were also outlined. The present review aims to comprehensively and systematically collate the recent research progress on extraction and purification methods, structural characteristics, biological activities, mechanism of action, structural modification, and potential industry applications of TMPs to support their therapeutic potential and health care functions. Overall, the present review provides a theoretical overview for further development and utilization of TMPs in the fields of pharmaceutical and health food.


Assuntos
Taraxacum , Taraxacum/química , Polissacarídeos/farmacologia , Polissacarídeos/química , Flavonoides/química , Antioxidantes/farmacologia
9.
Fitoterapia ; 172: 105744, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37952762

RESUMO

PURPOSE: Frankincense has been shown in studies to have healing benefits for people with ulcerative colitis (UC). However, its underlying mechanisms have not been fully investigated. The objective of this study was to explore the potential molecular mechanisms of Frankincense essential oil (FREO) in improving dextran sodium sulfate (DSS)-induced UC from multiple perspectives. METHODS: The FREO components were analyzed by GC-MS, and the interactions between the key active components and the mechanism of FREO were determined based on RNA-seq, "quantity-effect" weighting coefficient network pharmacology, WGCNA and pharmacodynamic experiments. The protection of FREO against DSS-induced UC mice was assessed by behavioral and pathological changes through mice. The expression of pro-inflammatory cytokines was measured using enzyme-linked immunosorbent assay. The expression of MAPK and NF-κB-related proteins by the Western Blotting and immunohistochemistry method. RESULTS: Treatment with FREO significantly improved the symptoms of weight loss, diarrhea, stool blood, and colon shortening in UC mice. Reduced intestinal mucosal damage and the degree of inflammatory cell infiltration in the colon. Decreased TNF-α and IL-6 levels in mice's serum and inhibited phosphorylation of ERK, p65 in MAPK and NF-κB signaling. CONCLUSION: FREO may decrease the inflammatory response to reduce the symptoms of UC by modulating the MAPK/ NF-κB pathway. This may be due to the synergistic interaction of the effective ingredient Hepten-2-yl tiglate, 6-methyl-5-, Isoneocembrene A and P-Cymene. This study provides a promising drug candidate and a new concept for the treatment of UC.


Assuntos
Colite Ulcerativa , Colite , Franquincenso , Óleos Voláteis , Sulfatos , Humanos , Animais , Camundongos , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/patologia , NF-kappa B/metabolismo , Dextranos/metabolismo , Dextranos/farmacologia , Dextranos/uso terapêutico , Franquincenso/metabolismo , Franquincenso/farmacologia , Franquincenso/uso terapêutico , Óleos Voláteis/farmacologia , RNA-Seq , Modelos Animais de Doenças , Estrutura Molecular , Sulfato de Dextrana/efeitos adversos , Sulfato de Dextrana/metabolismo , Colo/metabolismo , Colo/patologia , Camundongos Endogâmicos C57BL , Colite/tratamento farmacológico
10.
Biomed Pharmacother ; 168: 115727, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37879216

RESUMO

OBJECTIVE: The purpose of this study was to investigate the mechanism through which rosemary essential oil treats atopic dermatitis. METHODS: A dinitrochlorobenzene (DNCB)-induced atopic dermatitis mouse model was established and treated with low (1%), medium (2%), and high (4%) doses of Rosmarinus officinalis essential oil (EORO). Serum levels of interleukin (IL)-6 and tumor necrosis factor-alpha (TNF-α) in each group were determined using enzyme-linked immunosorbent assay (ELISA). Skin tissues were stained with hematoxylin-eosin and toluidine blue. We used network pharmacology and molecular docking techniques to verify the biological activity of essential proteins and their corresponding compounds in the pathway. Gas chromatography-mass spectrometry (GC-MS) was used for metabolomics analysis and multivariate statistical analysis of mouse serum to screen differential metabolites and metabolic pathway analysis. Protein expression of p-JAK1, CD4+ cells, and IL-4 in the skin tissue was detected by immunohistochemistry analysis. Protein levels of STAT3, p-STAT3, P65, and p-P65 in damaged skin tissues were detected using western blotting. RESULT: The skin of mice in the model group showed different degrees of erythema, dryness, scratches, epidermal erosion and shedding, and crusting. After treatment, the serum levels of IL-6 and TNF-α in EORO group were significantly decreased, and the expression of p-JAK1,CD4 + cells, IL-4, p-P65 / P65 and p-STAT3 / STAT3 proteins in skin tissues were decreased. CONCLUSION: EORO can effectively improve DNCB-induced AD-like skin lesions in mice by regulating the JAK/STAT/NF-κB signaling pathway, thereby reducing the production of downstream arachidonic acid metabolites, inhibiting skin inflammation, and restoring epidermal barrier function.


Assuntos
Dermatite Atópica , Óleos Voláteis , Rosmarinus , Animais , Camundongos , Citocinas/metabolismo , Dermatite Atópica/tratamento farmacológico , Dinitroclorobenzeno/farmacologia , Interleucina-4/metabolismo , Interleucina-6/metabolismo , Camundongos Endogâmicos BALB C , Simulação de Acoplamento Molecular , NF-kappa B/metabolismo , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Transdução de Sinais , Pele/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
11.
Int J Nanomedicine ; 18: 4275-4311, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37534056

RESUMO

Breast cancer (BC) is the most prevalent type of cancer in the world and the main reason women die from cancer. Due to the significant side effects of conventional treatments such as chemotherapy and radiotherapy, the search for supplemental and alternative natural drugs with lower toxicity and side effects is of interest to researchers. Curcumin (CUR) is a natural polyphenol extracted from turmeric. Numerous studies have demonstrated that CUR is an effective anticancer drug that works by modifying different intracellular signaling pathways. CUR's therapeutic utility is severely constrained by its short half-life in vivo, low water solubility, poor stability, quick metabolism, low oral bioavailability, and potential for gastrointestinal discomfort with high oral doses. One of the most practical solutions to the aforementioned issues is the development of targeted drug delivery systems (TDDSs) based on nanomaterials. To improve drug targeting and efficacy and to serve as a reference for the development and use of CUR TDDSs in the clinical setting, this review describes the physicochemical properties and bioavailability of CUR and its mechanism of action on BC, with emphasis on recent studies on TDDSs for BC in combination with CUR, including passive TDDSs, active TDDSs and physicochemical TDDSs.


Assuntos
Antineoplásicos , Neoplasias da Mama , Curcumina , Feminino , Humanos , Curcumina/farmacologia , Neoplasias da Mama/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Antineoplásicos/farmacologia , Solubilidade , Portadores de Fármacos/química
12.
J Nanobiotechnology ; 20(1): 509, 2022 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-36463199

RESUMO

Norcantharidin (NCTD) is a demethylated derivative of cantharidin (CTD), the main anticancer active ingredient isolated from traditional Chinese medicine Mylabris. NCTD has been approved by the State Food and Drug Administration for the treatment of various solid tumors, especially liver cancer. Although NCTD greatly reduces the toxicity of CTD, there is still a certain degree of urinary toxicity and organ toxicity, and the poor solubility, short half-life, fast metabolism, as well as high venous irritation and weak tumor targeting ability limit its widespread application in the clinic. To reduce its toxicity and improve its efficacy, design of targeted drug delivery systems based on biomaterials and nanomaterials is one of the most feasible strategies. Therefore, this review focused on the studies of targeted drug delivery systems combined with NCTD in recent years, including passive and active targeted drug delivery systems, and physicochemical targeted drug delivery systems for improving drug bioavailability and enhancing its efficacy, as well as increasing drug targeting ability and reducing its adverse effects.


Assuntos
Compostos Bicíclicos Heterocíclicos com Pontes , Neoplasias , Estados Unidos , Sistemas de Liberação de Medicamentos , Meia-Vida , Disponibilidade Biológica , Neoplasias/tratamento farmacológico
13.
Int J Nanomedicine ; 17: 5027-5046, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36303804

RESUMO

Background: Ulcerative colitis (UC) is one of the intractable diseases recognized by the World Health Organization, and paeonol has been proven to have therapeutic effects. However, the low solubility of paeonol limits its clinical application. To prepare and optimize paeonol liposome, study its absorption mechanism and the anti-inflammatory activity in vitro and in vivo, in order to provide experimental basis for the further development of paeonol into an anti-inflammatory drug in the future. Methods: Paeonol loaded liposomes were prepared and optimized by thin film dispersion-ultrasonic method. The absorption mechanism of paeonol-loaded liposomes was studied by pharmacokinetics, in situ single-pass intestinal perfusion and Caco-2 cell monolayer model, the anti-inflammatory activity was studied in a mouse ulcerative model. Results: Box-Behnken response surface methodology permits to screen the best formulations. The structural and morphological characterization showed that paeonol was entrapped inside the bilayer in liposomes. Pharmacokinetic studies found that the AUC0-t of Pae-Lips was 2.78 times than that of paeonol suspension, indicating that Pae-Lips significantly improved the absorption of paeonol. In situ single intestinal perfusion and Caco-2 monolayer cell model results showed that paeonol was passively transported and absorbed, and was the substrate of P-gp, MRP2 and BCRP, and the Papp value of Pae-Lips was significantly higher than that of paeonol. In vitro and in vivo anti-inflammatory experiments showed that compared with paeonol, Pae-Lips exhibited excellent anti-inflammatory activity. Conclusion: In this study, Pae-Lips were successfully prepared to improve the oral absorption of paeonol. Absorption may involve passive diffusion and efflux transporters. Moreover, Pae-Lips have excellent anti-inflammatory activity in vitro and in vivo, which preliminarily clarifies the feasibility of further development of Pae-Lips into oral anti-inflammatory drugs.


Assuntos
Lipossomos , Proteínas de Neoplasias , Humanos , Camundongos , Animais , Lipossomos/química , Células CACO-2 , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Modelos Animais de Doenças
14.
Front Nutr ; 9: 927434, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35990355

RESUMO

Valerian volatile oil can be used in the treatment of insomnia; however, the active components and mechanisms of action are currently unclear. Therefore, we used transcriptome sequencing and weight coefficient network pharmacology to predict the effective components and mechanism of action of valerian volatile oil in an insomnia model induced by intraperitoneal injection of para-Chlorophenylalanine (PCPA) in SD rats. Valerian essential oil was given orally for treatment and the contents of 5-hydroxytryptamine receptor 1 A (5-HT1AR), γ-aminobutyric acid (GABA), cyclic adenosine monophosphate (cAMP), and protein kinase A (PKA) in the hippocampus of rats in each group were detected by enzyme-linked immunosorbent assay (ELISA), western blot, Polymerase Chain Reaction (PCR), and immunohistochemistry. The results showed that after treatment with valerian essential oil, insomnia rats showed significantly prolonged sleep duration and alleviated insomnia-induced tension and anxiety. Regarding the mechanism of action, we believe that caryophyllene in valerian essential oil upregulates the 5-HT1AR receptor to improve the activity or affinity of the central transmitter 5-HT, increase the release of 5-HT, couple 5-HT with a G protein coupled receptor, convert adenosine triphosphate (ATP) into cAMP (catalyzed by ADCY5), and then directly regulate the downstream pathway. Following pathway activation, we propose that the core gene protein kinase PKA activates the serotonergic synapse signal pathway to increase the expression of 5-HT and GABA, thus improving insomnia symptoms and alleviating anxiety. This study provides a theoretical basis for the application of valerian volatile oil in health food.

15.
Drug Des Devel Ther ; 16: 2407-2422, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35923932

RESUMO

Purpose: To investigate the effective components and possible mechanism of action of Lavandula angustifolia Mill. essential oil (LEO) in preventing vomiting through the olfactory pathway. Materials and Methods: A new network pharmacology-based method was established to analyze main components and pathways of LEO involved in antiemetic effects by introducing component content; biological activities of key proteins of the olfactory pathway and their corresponding compounds were verified by molecular docking technique; and finally pica in a rat model was established to verify the molecular mechanism of antiemetic effects of LEO by enzyme-linked immunosorbent assay (ELISA) to determine the serum 5-HT, substance P, and DA levels in each group and by immunohistochemistry to determine the contents of 5-HT3R, CaMKII and ERK1/2 proteins in the medulla oblongata tissue. Results: Network pharmacology combined with molecular docking analysis showed that the mechanism of the antiemetic effect of LEO may be related to (2Z)-3,7-dimethyl-2,6-octadienyl acetate, linalyl acetate, butanoic acid, hexyl ester, 4-hexen-1-ol, 5-methyl-2-(1-methylethenyl)-, acetate, .tau.-cadinol and other active ingredients, which regulate the cyclic adenosine monophosphate (cAMP) signaling pathway and the expression of BRAF, PDE and other targets on the pathway. An ELISA revealed that LEO reduced the levels of 5-hydroxytryptamine (5-HT), substance P, and dopamine in serum compared with the model group (P <0.05). Immunohistochemical analysis showed that LEO decreased the expression of 5-HT3R, CaMKII, and ERK1/2 proteins in the medulla oblongata of rats compared with the model group (P <0.01). Conclusion: LEO may achieve the antiemetic effect by reducing the content of 5-HT and inhibiting its related receptors, thereby regulating downstream Ca2+/CaMKII/ERK1/2 pathway of the cAMP signaling pathway.


Assuntos
Antieméticos , Lavandula , Óleos Voláteis , Acetatos , Animais , Antieméticos/farmacologia , Cálcio/metabolismo , Proteína Quinase Tipo 2 Dependente de Cálcio-Calmodulina , Lavandula/química , Sistema de Sinalização das MAP Quinases , Simulação de Acoplamento Molecular , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Ratos , Serotonina , Substância P
16.
Food Chem ; 397: 133731, 2022 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-35908464

RESUMO

Phellinus spp., an important medicinal fungus mushroom extensively cultivated and consumed in East Asia for over 2000 years, is traditionally considered a precious food supplement and medicinal ingredient. Published studies showed that the polysaccharides are major bioactive macromolecules from Phellinus spp. (PPs) with multiple health-promoting effects, including immunomodulatory, anti-cancer, anti-inflammatory, hepatoprotective, hypoglycemic, hypolipidemic, antioxidant, and other bioactivities. Although the polysaccharides extracted from the fruiting body, mycelium, and fermentation broth of Phellinus spp. have been extensively studied for the extraction and purification methods, structural characteristics, and pharmacological activities, the knowledge for their structures and bioactivity relationship, toxicologic effects, and pharmacokinetic profile is limited. This review systematically summarizes the recent progress in the isolation and purification, chemical structures, bioactivities, and the underlying mechanisms of PPs. Information from this review provides insights into the further development of polysaccharides from PPs as therapeutic agents and functional foods.


Assuntos
Agaricales , Agaricales/química , Anti-Inflamatórios , Antioxidantes/química , Micélio , Phellinus , Polissacarídeos/química
17.
J Transl Med ; 20(1): 135, 2022 03 18.
Artigo em Inglês | MEDLINE | ID: mdl-35303878

RESUMO

Urokinase-type plasminogen activator receptor (uPAR) is an attractive target for the treatment of cancer, because it is expressed at low levels in healthy tissues but at high levels in malignant tumours. uPAR is closely related to the invasion and metastasis of malignant tumours, plays important roles in the degradation of extracellular matrix (ECM), tumour angiogenesis, cell proliferation and apoptosis, and is associated with the multidrug resistance (MDR) of tumour cells, which has important guiding significance for the judgement of tumor malignancy and prognosis. Several uPAR-targeted antitumour therapeutic agents have been developed to suppress tumour growth, metastatic processes and drug resistance. Here, we review the recent advances in the development of uPAR-targeted antitumor therapeutic strategies, including nanoplatforms carrying therapeutic agents, photodynamic therapy (PDT)/photothermal therapy (PTT) platforms, oncolytic virotherapy, gene therapy technologies, monoclonal antibody therapy and tumour immunotherapy, to promote the translation of these therapeutic agents to clinical applications.


Assuntos
Neoplasias , Receptores de Ativador de Plasminogênio Tipo Uroquinase , Humanos , Neoplasias/terapia , Prognóstico , Receptores de Ativador de Plasminogênio Tipo Uroquinase/genética , Receptores de Ativador de Plasminogênio Tipo Uroquinase/metabolismo , Transdução de Sinais , Ativador de Plasminogênio Tipo Uroquinase/genética , Ativador de Plasminogênio Tipo Uroquinase/metabolismo
18.
J Ethnopharmacol ; 282: 114650, 2022 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-34536515

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: In traditional Chinese Medicine, Rehmannia glutinosa (Gaertn.) DC., as the principle herb of ShengDiHuang Decotion (SDHD), has the effect of cooling blood and hemostasis, and tonifying the yin and kidney. Rheum L., as adjuvant herbs, assist Rehmannia glutinosa (Gaertn.) DC. to promote blood circulation to remove blood stasis. AIM OF STUDY: To study the mechanism of Rhein (RH) involved in the promotion of Rehmannioside D (RD) absorption by pharmacokinetic studies, single-pass intestinal perfusion, Caco-2 cell models, molecular docking technique and western blotting. MATERIALS AND METHODS: Initially, the intestinal absorption of RD in the presence or absence of RH was conducted through pharmacokinetic studies. Thereafter, the intestinal absorption of RD and RH was studied using the single-pass intestinal perfusion and Caco-2 cell models. Finally, using molecular docking technique and western blotting. RESULTS: We found that the promotion of RD absorption by RH was mediated by breast cancer resistance and multidrug resistance-associated protein 2, thereby affecting the permeability of the intestinal epithelium. Additionally, RH and RD can competitively bind to breast cancer resistance and multidrug resistance-associated protein 2, and that RH inhibits the expression of breast cancer resistance and multidrug resistance-associated protein 2 in the ileum to promote the intestinal absorption of RD. CONCLUSION: This study reveals the mechanisms associated with the RH-mediated promotion of RD absorption and provides a basis for further exploring the synergistic effect of Rehmannia glutinosa (Gaertn.) DC and rhubarb.


Assuntos
Antraquinonas , Animais , Humanos , Masculino , Ratos , Antraquinonas/química , Antraquinonas/farmacocinética , Área Sob a Curva , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/química , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo , Transporte Biológico , Células CACO-2 , Sobrevivência Celular/efeitos dos fármacos , Simulação por Computador , Interações Medicamentosas , Regulação da Expressão Gênica/efeitos dos fármacos , Meia-Vida , Modelos Moleculares , Estrutura Molecular , Proteínas de Neoplasias/química , Proteínas de Neoplasias/metabolismo , Conformação Proteica , Distribuição Aleatória , Ratos Sprague-Dawley
19.
Front Pharmacol ; 12: 706836, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34658853

RESUMO

To determine the active ingredients in German chamomile volatile oil and the mechanism of action in the treatment of eczema, this study used two parameters (ingredient content and oil-water partition coefficient) and established a new network pharmacology method based on the dose-effect weight coefficient. Through the new network pharmacology method, we found that German chamomile volatile oil regulated T-cell lymphatic subpopulations to inhibit the Th17 cell differentiation signaling pathway. This resulted in a reduction of interleukin 17 (IL-17), thereby inhibiting the activation of the nuclear factor kappa beta (NF-κB) and MAPK pathways, decreasing the secretion of the pro-inflammatory factors (tumor necrosis factor alpha (TNF-α) and interleukin 6 (IL-6)), and reducing inflammation. In this study, a new dose-effect relationship synergistic network pharmacology method was established to provide a new method for the screening of effective ingredients and pathways of drugs, and to provide a basis for the follow-up studies of German chamomile volatile oil in the treatment of eczema.

20.
Drug Des Devel Ther ; 15: 4025-4042, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34594101

RESUMO

AIM: Aralia taibaiensis is a natural medicinal and food plant that is rich in triterpenoid saponins with hypoglycaemic, antioxidant, hepatoprotective, anti-gastric ulcer and anti-inflammatory effects. This study has significance in terms of the antioxidant, anti-aging and organ protective effects of Aralia taibaiensis total saponins (TSAT) in D-galactose-induced aging rats. METHODS: The saponin composition of TSAT was determined and quantified by high performance liquid chromatography (HPLC). We consolidated the antioxidant and enzyme inhibitory activities of TSAT in vitro and assessed the effects of TSAT on daily mobility, body weight, behaviour, organ indices, oxidation-related indices and pathological changes in aging rats. RESULTS: In vitro experiments showed that TSAT had a scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), tyrosinase, hydroxyl radicals (HO•) and superoxide radicals (•O2-) and was closely related to the dose of TSAT. In vivo experiments showed that after 8 weeks of continuous gavage administration, the rats gradually recovered their body weight, daily activity ability, learning and memory ability and organ index and effectively improved D-gal-induced organ injury. Specifically, TSAT significantly increased the levels of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px) and total antioxidant capacity (T-AOC) and significantly decreased malondialdehyde (MDA) levels in the serum, brain, heart, lung, spleen and kidney of aging rats compared to the model group. In addition, TSAT significantly inhibited the D-gal-induced upregulation of hepatic alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. The histopathological results showed that TSAT reversed D-gal-induced damage to the brain, heart, lung, kidney, liver and spleen to varying degrees. CONCLUSION: TSAT is a high-quality natural product with antioxidant and anti-aging properties that can alleviate D-gal-induced aging damage in rats.


Assuntos
Envelhecimento/efeitos dos fármacos , Antioxidantes/farmacologia , Aralia/química , Saponinas/farmacologia , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Sequestradores de Radicais Livres/administração & dosagem , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Masculino , Malondialdeído/metabolismo , Ratos , Ratos Sprague-Dawley , Saponinas/administração & dosagem , Saponinas/isolamento & purificação
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA