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1.
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
2.
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.

3.
Inflammopharmacology ; 32(3): 1659-1704, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38520574

RESUMO

Curcumol (Cur), a guaiane-type sesquiterpenoid hemiketal, is an important and representative bioactive component extracted from the essential oil of the rhizomes of Curcumae rhizoma which is also known as "Ezhu" in traditional Chinese medicine. Recently, Cur has received considerable attention from the research community due to its favorable pharmacological activities, including anti-cancer, hepatoprotective, anti-inflammatory, anti-viral, anti-convulsant, and other activities, and has also exerted therapeutic effect on various cancers, liver diseases, inflammatory diseases, and infectious diseases. Pharmacokinetic studies have shown that Cur is rapidly distributed in almost all organs of rats after intragastric administration with high concentrations in the small intestine and colon. Several studies focusing on structure-activity relationship (SAR) of Cur have shown that some Cur derivatives, chemically modified at C-8 or C-14, exhibited more potent anti-cancer activity and lower toxicity than Cur itself. This review aims to comprehensively summarize the latest advances in the pharmacological and pharmacokinetic properties of Cur in the last decade with a focus on its anti-cancer and hepatoprotective potentials, as well as the research progress in drug delivery system and potential applications of Cur to date, to provide researchers with the latest information, to highlighted the limitations of relevant research at the current stage and the aspects that should be addressed in future research. Our results indicate that Cur and its derivatives could serve as potential novel agents for the treatment of a variety of diseases, particularly cancer and liver diseases.


Assuntos
Sistemas de Liberação de Medicamentos , Sesquiterpenos , Animais , Sesquiterpenos/farmacologia , Sesquiterpenos/farmacocinética , Sesquiterpenos/administração & dosagem , Humanos , Relação Estrutura-Atividade , Sistemas de Liberação de Medicamentos/métodos , Antineoplásicos/farmacocinética , Antineoplásicos/farmacologia , Antineoplásicos/administração & dosagem
4.
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
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.


Assuntos
Golpe de Calor , Lamiaceae , Humanos , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/química , Polissacarídeos/farmacologia , Polissacarídeos/uso terapêutico , Polissacarídeos/química , Lamiaceae/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Hipoglicemiantes
6.
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
7.
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
8.
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
9.
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
10.
Sci Rep ; 13(1): 8362, 2023 05 24.
Artigo em Inglês | MEDLINE | ID: mdl-37225858

RESUMO

Intrahepatic cholangiocarcinoma (ICC) is the second common primary hepatic malignancy tumor. In this study, an integrative analysis of differentially expressed genes (DEGs) and miRNAs from the ICC onset and adjacent normal tissues were performed to explore the regulatory roles of miRNA-mRNA interaction. A total of 1018 DEGs and 39 miRNAs were likely involved in ICC pathogenesis, suggesting the changes in cell metabolism in ICC development. The built network indicated that 30 DEGs were regulated by 16 differentially expressed miRNA. The screened DEGs and miRNA together were probably considered the biomarkers of ICC, and their important roles in ICC pathogenesis remain to be elucidated. This study could provide a good basis to uncover the regulatory mechanism of miRNA and mRNAs in ICC pathogenesis.


Assuntos
Neoplasias dos Ductos Biliares , Colangiocarcinoma , MicroRNAs , Segunda Neoplasia Primária , Humanos , Colangiocarcinoma/genética , MicroRNAs/genética , RNA Mensageiro/genética , Neoplasias dos Ductos Biliares/genética , Ductos Biliares Intra-Hepáticos
11.
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
12.
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
13.
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.

14.
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
15.
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
16.
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.

17.
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
18.
Front Pharmacol ; 12: 644140, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33981227

RESUMO

This study aimed to introduce a new weight coefficient combined with network pharmacology to predict the potential active components, action targets, and signal pathways of lavender essential oil and to investigate the therapeutic effect of lavender essential oil on colitis through animal experiments. The component targets of lavender essential oil were mined from the Pubchem and SwissTargetPrediction databases, and the relative content of lavender essential oil was compared with OB (oral bioavailability) to establish a "quantity-effect" weight coefficient. Online databases such as GeneCards and String were used to construct a "lavender essential oil compound target disease target" network to extract the key targets of core compounds acting on diseases. The clusterProfiler package in R language programming of Rstudio software was used to analyze the enrichment of the related targets by Gene Ontology and the Kyoto Encyclopedia of Genes and Genomes (KEGG), and the enriched pathways were reordered according to the "quantity-effect" weight coefficient of the targets they participated in. Following up on the findings, the pharmacodynamic test showed that, after injecting lavender essential oil into mice, the levels of inflammatory cytokines including EGFR, TNF-α, and IFN-γ in serum and colon tissue decreased, and lavender essential oil could mediate Th17 cell differentiation by reducing dextran sulfate sodium (DSS)-induced ulcerative colitis (UC) colonic mucosal damage. The results indicated that lavender essential oil can alleviate DSS-induced colonic mucosal injury in ulcerative Colitis mice. Based on the network pharmacology of the "quantity-effect" weight coefficient, this study indicated that lavender essential oil can regulate the level of inflammatory factors, inhibit inflammatory reactions through a multicomponent and multitarget strategy, and ultimately alleviate the colonic mucosal injury of UC mice. Through the weight coefficient network pharmacology mining, it was concluded that the Th17 cell differentiation, PI3K-Akt signaling pathway, and Th1 and Th2 cell differentiation of lavender essential oil in the treatment of UC may be the key pathway for the treatment of the disease. Through the establishment of a weight coefficient combined with network pharmacology and the combination of dose and effect, it shows that network pharmacology may provide a better basis for the treatment of disease mechanism.

19.
Mol Med Rep ; 22(6): 4531-4540, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33174034

RESUMO

In order to improve the water solubility of the volatile oils extracted from Flos magnoliae (FM) and Centipeda minima (CM), they were prepared as a microemulsion (ME), which were then used in the development of an FM and CM volatile oil ME for the treatment of allergic rhinitis (AR). ME was prepared by phase inversion emulsification, and the prescription factors such as emulsifier, co­emulsifier, oil phase, Km, which represents the ratio of the mass of emulsifier to that of the co­emulsifier, and preparation factors such as temperature affecting the formation of the ME were selected according to the formation area of ME in a pseudo­ternary phase diagram. The quality of the ME was evaluated based on its appearance, particle size, Zeta potential and stability. The content of eucalyptol in ME was determined by gas chromatography­mass spectrometry (GC­MS). The cumulative permeability of the ME within 24 h was measured with a transdermal diffusion tester. The results revealed that the best formula for preparation of the ME was as follows: Castor oil polyoxyethylene ether (EL­40) was the emulsifier; the co­emulsifier was anhydrous ethanol; the Km was 2:1; the mixed phase of volatile oil and isopropyl myristate with mass ratio of 1:1 was used as oil phase; and the preparation temperature was 25˚C. The content of eucalyptol in the ME was 2.57 mg/g, and the cumulative permeability of the ME in 24 h was significantly increased compared with that of the reference oil solution. The appearance of the ME was uniform, and the solution was transparent. In conclusion, compared with traditional preparations, FM and CM volatile oil ME is a novel, improved and more effective preparation for the treatment of AR.


Assuntos
Medicina Tradicional Chinesa/métodos , Óleos Voláteis/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Asteraceae/metabolismo , China , Emulsões , Magnoliaceae/metabolismo , Óleos Voláteis/química , Tamanho da Partícula , Permeabilidade , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Rinite Alérgica/tratamento farmacológico , Solubilidade
20.
Biomed Pharmacother ; 130: 110563, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32745908

RESUMO

Carthamus tinctorius L.(Safflower), a herbal formula from Traditional Chinese Medicine (TCM), has been widely used for the treatment of cardio-cerebrovascular diseases, particularly cerebral infarction (CI) or cerebral ischemia-reperfusion injury. However, we know very little about the specific mechanisms associated with the therapeutic effect of Safflower on CI. In this study, we used a network pharmacology-based approach, together with rat model of CI, to gain more insight into of such mechanisms. Our analysis showed that Safflower contains 52 active compounds that target 247 genes, which were also cross-referenced with 299 genes associated with CI. Consequently, we identified 52 target genes in Safflower that were associated with CI. These 52 target genes were analyzed by gene ontology (GO) enrichment analysis, leading to the identification of 1491 biological process items, 90 molecular function items and 19 cell assembly items. Eighty-nine pathways were generated by KEGG enrichment (P < 0.05). Next, we investigated the effect of the extract of safflower (ES) and Safflower extract phospholipid complex (ESPC), delivered via the nasal route, on an animal model of the middle cerebral artery occlusion (MCAO). Our data confirmed that Safflower was able to treat CI by the regulating the TNF-α/MAPK pathway via CASP3. The therapeutic effect of ES and ESPC on CI acts by improving the circulation of blood in the central nervous system, reducing the inflammatory reaction, inhibiting apoptosis, and by protecting brain nerve cells from injury.


Assuntos
Carthamus tinctorius/química , Infarto Cerebral/tratamento farmacológico , Infarto Cerebral/genética , Quinases de Proteína Quinase Ativadas por Mitógeno/genética , Extratos Vegetais/uso terapêutico , Transdução de Sinais/efeitos dos fármacos , Fator de Necrose Tumoral alfa/genética , Administração Intranasal , Animais , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Infarto Cerebral/mortalidade , Encefalite/tratamento farmacológico , Infarto da Artéria Cerebral Média/tratamento farmacológico , Infarto da Artéria Cerebral Média/genética , Infarto da Artéria Cerebral Média/mortalidade , Masculino , Medicina Tradicional Chinesa , Neurônios/efeitos dos fármacos , Fosfolipídeos/química , Extratos Vegetais/administração & dosagem , Desempenho Psicomotor/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Transdução de Sinais/genética
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