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1.
J Ethnopharmacol ; 328: 118007, 2024 Jun 28.
Article in English | MEDLINE | ID: mdl-38492791

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Rosa damascena is an ancient plant with significance in both medicine and perfumery that have a variety of therapeutic properties, including antidepressant, anti-anxiety, and anti-stress effects. Rose damascena essential oil (REO) has been used to treat depression, anxiety and other neurological related disorders in Iranian traditional medicine. However, its precise mechanism of action remains elusive. AIM OF THE STUDY: The aim of this study was to investigate the impact and mechanism underlying the influence of REO on chronic unpredictable mild stress (CUMS) rats. MATERIALS AND METHODS: Gas chromatography-mass spectrometry (GC-MS) technique coupling was used to analyze of the components of REO. A CUMS rat model was replicated to assess the antidepressant effects of varying doses of REO. This assessment encompassed behavioral evaluations, biochemical index measurements, and hematoxylin-eosin staining. For a comprehensive analysis of hippocampal tissues, we employed transcriptomics and incorporated weighting coefficients by means of network pharmacology. These measures allowed us to explore differentially expressed genes and biofunctional pathways affected by REO in the context of depression treatment. Furthermore, GC-MS metabolomics was employed to assess metabolic profiles, while a joint analysis in Metscape facilitated the construction of a network elucidating the links between differentially expressed genes and metabolites, thereby elucidating potential relationships and clarifying key pathways regulated by REO. Finally, the expression of relevant proteins in the key pathways was determined through immunohistochemistry and Western blot analysis. Molecular docking was utilized to investigate the interactions between active components and key targets, thereby validating the experimental results. RESULTS: REO alleviated depressive-like behavior, significantly elevated levels of the neurotransmitter 5-hydroxytryptamine (5-HT), and reduced hippocampal neuronal damage in CUMS rats. This therapeutic effect may be associated with the modulation of the serotonergic synapse signaling pathway. Furthermore, REO rectified metabolic disturbances, primarily through the regulation of amino acid metabolic pathways. Joint analysis revealed five differentially expressed genes (EEF1A1, LOC729197, ATP8A2, NDST4, and GAD2), suggesting their potential in alleviating depressive symptoms by modulating the serotonergic synapse signaling pathway and tryptophan metabolism. REO also modulated the 5-HT2A-mediated extracellular regulated protein kinases-cAMP-response element binding protein-brain-derived neurotrophic factor (ERK-CREB-BDNF) pathway. In addition, molecular docking results indicated that citronellol, geraniol and (E,E)-farnesol in REO may serve as key active ingredients responsible for its antidepressant effects. CONCLUSIONS: This study is the first to report that REO can effectively alleviate CUMS-induced depression-like effects in rats. Additionally, the study offers a comprehensive understanding of its intricate antidepressant mechanism from a multi-omics and multi-level perspective. Our findings hold promise for the clinical application and further development of this essential oil.


Subject(s)
Rosa , Rats , Animals , Serotonin/metabolism , Iran , Molecular Docking Simulation , Rats, Sprague-Dawley , Antidepressive Agents/pharmacology , Antidepressive Agents/therapeutic use , Depression/metabolism , Signal Transduction , Brain-Derived Neurotrophic Factor/genetics , Brain-Derived Neurotrophic Factor/metabolism , Synapses/metabolism , Stress, Psychological/drug therapy , Hippocampus , Disease Models, Animal
2.
Phytomedicine ; 128: 155472, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38461630

ABSTRACT

BACKGROUND: Cardiovascular disease (CVD) remains the leading cause of morbidity and mortality worldwide, imposing an enormous economic burden on individuals and human society. Laboratory studies have identified several drugs that target mitophagy for the prevention and treatment of CVD. Only a few of these drugs have been successful in clinical trials, and most studies have been limited to animal and cellular models. Furthermore, conventional drugs used to treat CVD, such as antiplatelet agents, statins, and diuretics, often result in adverse effects on patients' cardiovascular, metabolic, and respiratory systems. In contrast, traditional Chinese medicine (TCM) has gained significant attention for its unique theoretical basis and clinical efficacy in treating CVD. PURPOSE: This paper systematically summarizes all the herbal compounds, extracts, and active monomers used to target mitophagy for the treatment of CVD in the last five years. It provides valuable information for researchers in the field of basic cardiovascular research, pharmacologists, and clinicians developing herbal medicines with fewer side effects, as well as a useful reference for future mitophagy research. METHODS: The search terms "cardiovascular disease," "mitophagy," "herbal preparations," "active monomers," and "cardiac disease pathogenesis" in combination with "natural products" and "diseases" were used to search for studies published in the past five years until January 2024. RESULTS: Studies have shown that mitophagy plays a significant role in the progression and development of CVD, such as atherosclerosis (AS), heart failure (HF), myocardial infarction (MI), myocardial ischemia/reperfusion injury (MI/RI), cardiac hypertrophy, cardiomyopathy, and arrhythmia. Herbal compound preparations, crude extracts, and active monomers have shown potential as effective treatments for these conditions. These substances protect cardiomyocytes by inducing mitophagy, scavenging damaged mitochondria, and maintaining mitochondrial homeostasis. They display notable efficacy in combating CVD. CONCLUSION: TCM (including herbal compound preparations, extracts, and active monomers) can treat CVD through various pharmacological mechanisms and signaling pathways by inducing mitophagy. They represent a hotspot for future cardiovascular basic research and a promising candidate for the development of future cardiovascular drugs with fewer side effects and better therapeutic efficacy.


Subject(s)
Cardiovascular Diseases , Drugs, Chinese Herbal , Medicine, Chinese Traditional , Mitophagy , Humans , Mitophagy/drug effects , Cardiovascular Diseases/drug therapy , Medicine, Chinese Traditional/methods , Drugs, Chinese Herbal/pharmacology , Animals
3.
Int J Biol Macromol ; 263(Pt 1): 130206, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38373568

ABSTRACT

Hippophae rhamnoides L. (sea buckthorn) is a type of traditional Chinese medicine with a long history of clinical application. It is used in the improvement and treatment of various diseases as medicine and food to strengthen the stomach and digestion, relieving cough and resolving phlegm, promoting blood circulation, and resolving blood stasis in traditional Chinese medicine. Emerging evidence has shown that H. rhamnoides polysaccharides (HRPs) are vital bioactive macromolecules responsible for its various health benefits. HRPs possess the huge potential to develop a drug improving or treating different diseases. In this review, we comprehensively and systematically summarize the recent information on extraction and purification methods, structural features, biological activities, structure-activity relationships, and potential industry applications of HRPs and further highlight the therapeutic potential and sanitarian functions of HRPs in the fields of therapeutic agents and functional food development. Additionally, this paper also lists a variety of biological activities of HRPs in vitro and in vivo roundly. Finally, this paper also discusses the structure-activity relationships and potential applications of HRPs. Overall, this work will help to have a better in-depth understanding of HRPs and provide a scientific basis and direct reference for more scientific and rational applications.


Subject(s)
Hippophae , Hippophae/chemistry , Fruit/chemistry , Polysaccharides/pharmacology , Polysaccharides/analysis
4.
J Ethnopharmacol ; 326: 117979, 2024 May 23.
Article in English | MEDLINE | ID: mdl-38412892

ABSTRACT

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.


Subject(s)
Heat Stroke , Lamiaceae , Humans , Antioxidants/pharmacology , Antioxidants/therapeutic use , Antioxidants/chemistry , Polysaccharides/pharmacology , Polysaccharides/therapeutic use , Polysaccharides/chemistry , Lamiaceae/chemistry , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Hypoglycemic Agents
5.
Int J Biol Macromol ; 259(Pt 1): 129047, 2024 Feb.
Article in English | MEDLINE | ID: mdl-38171434

ABSTRACT

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.


Subject(s)
Platycodon , Humans , Platycodon/chemistry , Polysaccharides/pharmacology , Polysaccharides/chemistry , Medicine, Chinese Traditional , Spleen , Cough
6.
Fitoterapia ; 172: 105744, 2024 Jan.
Article in English | MEDLINE | ID: mdl-37952762

ABSTRACT

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.


Subject(s)
Colitis, Ulcerative , Colitis , Frankincense , Oils, Volatile , Sulfates , Humans , Animals , Mice , Colitis, Ulcerative/chemically induced , Colitis, Ulcerative/drug therapy , Colitis, Ulcerative/pathology , NF-kappa B/metabolism , Dextrans/metabolism , Dextrans/pharmacology , Dextrans/therapeutic use , Frankincense/metabolism , Frankincense/pharmacology , Frankincense/therapeutic use , Oils, Volatile/pharmacology , RNA-Seq , Disease Models, Animal , Molecular Structure , Dextran Sulfate/adverse effects , Dextran Sulfate/metabolism , Colon/metabolism , Colon/pathology , Mice, Inbred C57BL , Colitis/drug therapy
7.
Biomed Pharmacother ; 168: 115727, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37879216

ABSTRACT

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.


Subject(s)
Dermatitis, Atopic , Oils, Volatile , Rosmarinus , Animals , Mice , Cytokines/metabolism , Dermatitis, Atopic/drug therapy , Dinitrochlorobenzene/pharmacology , Interleukin-4/metabolism , Interleukin-6/metabolism , Mice, Inbred BALB C , Molecular Docking Simulation , NF-kappa B/metabolism , Oils, Volatile/pharmacology , Oils, Volatile/therapeutic use , Signal Transduction , Skin/metabolism , Tumor Necrosis Factor-alpha/metabolism
8.
Int J Nanomedicine ; 18: 4275-4311, 2023.
Article in English | MEDLINE | ID: mdl-37534056

ABSTRACT

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.


Subject(s)
Antineoplastic Agents , Breast Neoplasms , Curcumin , Female , Humans , Curcumin/pharmacology , Breast Neoplasms/drug therapy , Drug Delivery Systems , Antineoplastic Agents/pharmacology , Solubility , Drug Carriers/chemistry
9.
Zhongguo Zhong Yao Za Zhi ; 48(4): 966-977, 2023 Feb.
Article in Chinese | MEDLINE | ID: mdl-36872267

ABSTRACT

The present study optimized the ethanol extraction process of Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus drug pair by network pharmacology and Box-Behnken method. Network pharmacology and molecular docking were used to screen out and verify the potential active components of Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus, and the process evaluation indexes were determined in light of the components of the content determination under Ziziphi Spinosae Semen and Schisandrae Sphenantherae Fructus in the Chinese Pharmacopoeia(2020 edition). The analytic hierarchy process(AHP) was used to determine the weight coefficient of each component, and the comprehensive score was calculated as the process evaluation index. The ethanol extraction process of Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus was optimized by the Box-Behnken method. The core components of the Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus drug pair were screened out as spinosin, jujuboside A, jujuboside B, schisandrin, schisandrol, schisandrin A, and schisandrin B. The optimal extraction conditions obtained by using the Box-Behnken method were listed below: extraction time of 90 min, ethanol volume fraction of 85%, and two times of extraction. Through network pharmacology and molecular docking, the process evaluation indexes were determined, and the optimized process was stable, which could provide an experimental basis for the production of preparations containing Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus.


Subject(s)
Network Pharmacology , Plant Extracts , Technology, Pharmaceutical , Ethanol , Molecular Docking Simulation , Seeds/chemistry , Ziziphus/chemistry , Plant Extracts/chemistry , Schisandra/chemistry , Fruit/chemistry
10.
J Nanobiotechnology ; 20(1): 509, 2022 Dec 03.
Article in English | MEDLINE | ID: mdl-36463199

ABSTRACT

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.


Subject(s)
Bridged Bicyclo Compounds, Heterocyclic , Neoplasms , United States , Drug Delivery Systems , Half-Life , Biological Availability , Neoplasms/drug therapy
11.
Article in English | MEDLINE | ID: mdl-36133789

ABSTRACT

Purpose: To explore the clinical application of Baihe Dihuang Decoction. To provide certain data support and theoretical basis for the clinical application of Baihe Dihuang Decoction in the future. Methods: With "Baihe Rehmannia Tang" as the search term, the search was carried out on CNKI, VIP, Wanfang, PubMed and other databases. The statistical analysis of Baihe Dihuang decoction for treating diseases was obtained. Meta-analysis of the data was performed using RevMan 5.3 software to analyze the main therapeutic indicators of the disease. Results: According to the 83 valid literature that can be found, it is shown that 17 are used for the treatment of depression, 14 are used for the treatment of menopausal syndrome, 24 are used for the treatment of insomnia, and 28 are used for the treatment of other diseases. Conclusion: In the treatment of depression, menopausal syndrome, and insomnia combined with Baihe Dihuang Decoction can have a better therapeutic effect and diminish the incidence of adverse reactions. It provides a theoretical basis for the study and experimental study of its active components.

12.
Front Nutr ; 9: 927434, 2022.
Article in English | MEDLINE | ID: mdl-35990355

ABSTRACT

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.

13.
Drug Des Devel Ther ; 16: 83-105, 2022.
Article in English | MEDLINE | ID: mdl-35027819

ABSTRACT

PURPOSE: Aralia taibaiensis, a medicinal food plant, and total saponins from its root bark extract inhibit α-glucosidase activity, which is associated with type 2 diabetes; however, the inhibitory mechanism is unknown. Furthermore, a green extraction technique superior to conventional hot reflux extraction (HRE) is needed for the rapid and easy extraction of A. taibaiensis total saponins (TSAT) to exploit and utilize this resource. Our aim was to develop a green extraction method for obtaining TSAT and to investigate the mechanism by which TSAT inhibits α-glucosidase. MATERIALS AND METHODS: In this study, the ultrasound-assisted extraction (UAE) process was optimized using a Box-Behnken design, and the extraction mechanism was investigated using scanning electron microscopy (SEM). High-performance liquid chromatography (HPLC) was used for qualitative and quantitative analyses of TSAT. In vitro glycosylation assays, enzyme kinetics, fluorescence spectroscopy measurements, atomic force microscopy (AFM), Fourier transform infrared spectroscopy (FT-IR) and molecular docking techniques were used to investigate the mechanism by which the A. taibaiensis active ingredients inhibit α-glucosidase. RESULTS: The optimal parameters for the extraction yield were obtained as an ethanol concentration of 73%, ultrasound time of 34 min, ultrasound temperature of 61 °C and solid-liquid ratio of 16 g/mL, which were better than HRE. The SEM analysis showed that UAE effectively disrupted plant cells, thus increasing the TSAT yield. In vitro α-glucosidase inhibition experiments showed that both TSAT and its active ingredient, araloside A, inhibited α-glucosidase activity by binding to α-glucosidase, thereby changing the conformation and microenvironment of α-glucosidase to subsequently inhibit enzyme activity. CONCLUSION: The optimal extraction conditions identified here established a basis for future scale-up of ultrasound extraction parameters with the potential for obtaining maximum yields. In vitro enzyme inhibition experiments investigated the mechanism of the TSAT interaction with α-glucosidase and further explored whether araloside A may be the main contributor to the good inhibition of α-glucosidase activity by TSAT.


Subject(s)
Aralia/chemistry , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/isolation & purification , Saponins/chemistry , Saponins/isolation & purification , Sonication , Chromatography, High Pressure Liquid , Microscopy, Electron, Scanning , Molecular Docking Simulation , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Spectroscopy, Fourier Transform Infrared
14.
J Ethnopharmacol ; 282: 114650, 2022 Jan 10.
Article in English | MEDLINE | ID: mdl-34536515

ABSTRACT

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.


Subject(s)
Anthraquinones , Animals , Humans , Male , Rats , Anthraquinones/chemistry , Anthraquinones/pharmacokinetics , Area Under Curve , ATP Binding Cassette Transporter, Subfamily G, Member 2/chemistry , ATP Binding Cassette Transporter, Subfamily G, Member 2/metabolism , Biological Transport , Caco-2 Cells , Cell Survival/drug effects , Computer Simulation , Drug Interactions , Gene Expression Regulation/drug effects , Half-Life , Models, Molecular , Molecular Structure , Neoplasm Proteins/chemistry , Neoplasm Proteins/metabolism , Protein Conformation , Random Allocation , Rats, Sprague-Dawley
15.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6011-6019, 2021 Dec.
Article in Chinese | MEDLINE | ID: mdl-34951227

ABSTRACT

Solid preparations account for more than 50% of traditional Chinese medicines(TCM). TCM powder is an important raw material for solid preparations of TCM. Its powder properties directly affect the quality of solid preparations, and even clinical safety and effectiveness. Particle design technology based on the characteristics of powder in TCM is an important means to improve and enhance the quality of solid preparations. This study summarized the relevant principles, methods, characteristics, classification, equipment, and other elements of particle design technology in recent years, analyzed the difficulties in its application in the field of TCM powder, and proposed the strategies in conjunction with the development of computer data mining. The present study is expected to provide a reference for the suitability of particle design in the field of TCM powder.


Subject(s)
Drugs, Chinese Herbal , Medicine, Chinese Traditional , Powders , Technology
16.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6045-6052, 2021 Dec.
Article in Chinese | MEDLINE | ID: mdl-34951231

ABSTRACT

Targeting the poor powder characteristics of the contents in Hewei Jiangni Capsules, this study characterized the powder properties of the contents and employed particle design technique for improving the content quality. The content composite particles of Hewei Jiangni Capsules prepared by the particle design technique were evaluated by scanning electron microscopy(SEM), followed by infrared ray(IR), content uniformity, and in vitro dissolution detection. It was found that there was a good correlation between the crushed particle size of slices and the crushing time, and the calcined Haematitum was responsible for the poor content uniformity. After the fine powder of calcined Haematitum was super-finely ground for 8.5 min and those of the other contents in the capsule for 1 min, they were prepared into the composite particles, whose property characterizations were compared with those of the physical mixtures. The content uniformity of the prepared composite particles was significantly improved, and the preparation process was stable and reliable. The adoption of particle design technology to correct the poor uniformity of the physical mixture, solve the pharmaceutical defects of Hewei Jiangni Capsules, and improve the quality of prescriptions has provided important reference for the clinical application and development of Chinese medicinal preparations.


Subject(s)
Capsules , Microscopy, Electron, Scanning , Particle Size , Powders
17.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6053-6061, 2021 Dec.
Article in Chinese | MEDLINE | ID: mdl-34951232

ABSTRACT

Based on the defects in powder properties of the contents of Ziyin Yiwei Capsules, this study screened out the main medicinal slice powders causing the poor powdery properties, and introduced the powder modification process to improve the powdery properties of these slice powders, the pharmaceutical properties of the capsule contents, and the content uniformity of Ziyin Yiwei Capsules, so as to provide a demonstration for the application of powder modification technology to the preparation of Chinese medicinal solid preparations. Through the investigation on the powder properties of the contents of Ziyin Yiwei Capsules, it was clarified that the pulverized particle size of the capsule contents had a good correlation with the pulverization time. According to the measurement results of the powder fluidity and wettability, the quality defects of the capsule contents were caused by the fine powders of Taraxaci Herba and Lungwortlike Herba. "Core-shell" composite particles were prepared from medicinal excipients magnesium stearate and fine powders of Taraxaci Herba and Lungwortlike Herba slices after ultra-fine pulverization to improve the powder properties of the problematic fine powders. Powder characterization data including fluidity and wettability were measured, followed by scanning electron microscopy(SEM) and infrared ray(IR) detection. It was determined that the optimal dosage of magnesium stearate was 2%, and the compositing time was 3 min. The composite particles were then used as content components of the Ziyin Yiwei Capsules. The powder characteristics between the original capsule and the modified composite capsule including the particle size, fluidity, wettability, uniformity of bulk density, and uniformity of chromatism as well as the content uniformity and in vitro dissolution were compared. The results showed that the powder characteristics and content uniformity of the prepared composite capsule were significantly improved, while the material basis of the preparation was not changed before and after modification. The preparation process was proved to be stable and feasible. The powder modification technology solved the pharmaceutical defects that were easy to appear in the preparation of traditional capsules, which has provided experimental evidence for the use of powder modification technology for improving the quality of Chinese medicinal solid preparations and promoting the secondary development and upgrading of traditional Chinese medicinal dosage forms such as capsules.


Subject(s)
Excipients , Capsules , Particle Size , Powders , Wettability
18.
Front Pharmacol ; 12: 706836, 2021.
Article in English | MEDLINE | ID: mdl-34658853

ABSTRACT

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.

19.
Zhongguo Zhong Yao Za Zhi ; 46(18): 4757-4764, 2021 Sep.
Article in Chinese | MEDLINE | ID: mdl-34581086

ABSTRACT

A spectrum-activity relationship is established with high performance liquid chromatography(HPLC) fingerprints and the in vitro antioxidant activity to improve the quality evaluation system of Aralia taibaiensis. The HPLC profiles of 12 batches of samples were collected, and the similarity evaluation, heat map analysis and principal component analysis were conducted for the chemometric study of the fingerprint data. Combined with grey correlation analysis, the contributions of the common peaks in the fingerprints to the antioxidant activity were clarified, and the important peaks reflecting the efficacy were identified. The results showed that 17 common peaks were found in 12 batches of A. taibaiensis samples, and 6 of them were identified as saponins. Similarity evaluation, heat map analysis and principal component analysis roughly classified the A. taibaiensis herbs into two categories, i.e.,(1) S1-S10, S12 and(2) S11. Twelve batches of samples showed different antioxidant activities in a dose-dependent manner. In particular, S9 had the strongest antioxidant activity, while S11 was the weakest in antioxidant capacity, which was basically consistent with the overall score results. The results of grey correlation analysis demonstrated that the 17 common peaks scavenged DPPH radicals in the following order: X_3>X_(17)>X_4>X_8>X_7>X_(13)>X_2>X_6>X_(11)>X_(10)>X_(16)>X_(12)>X_9>X_5>X_(14)>X_1>X_(15), and scavenged ABTS radicals in the order of X_4>X_3>X_7>X_8>X_2>X_(17)>X_(13)>X_6>X_(16)>X_(11)>X_5>X_(12)>X_(10)>X_9>X_(14)>X_1>X_(15). Among them, X_3, X_4, X_7(araloside C), X_8 and X_(17) were the important peaks reflecting the efficacy of A. taibaiensis, which were basically consistent with those contained in the principal component 1. In this study, the correlation between the HPLC fingerprints of 12 batches of A. taibaiensis and its antioxidant activity provides a reference for the Q-marker screening and quality control of A. taibaiensis.


Subject(s)
Aralia , Drugs, Chinese Herbal , Saponins , Antioxidants , Chromatography, High Pressure Liquid
20.
Drug Des Devel Ther ; 15: 2179-2191, 2021.
Article in English | MEDLINE | ID: mdl-34079221

ABSTRACT

PURPOSE: Acute myocardial infarction (AMI) is a cardiovascular disease with a high fatality rate. In this study, we combined network pharmacology and experimental pharmacology and discovered the potential mechanism of action and the active ingredients of the lily, Tricyrtis maculata was discovered. The monomer compound with stronger activity was discovered through in vitro cell experiments. METHODS: Forty known compounds were isolated from T. maculata. Using TCMSP, Swiss Target Prediction, metaTarFisher, GeneCards and OMIM databases, targets of drug compositions and AMI-related genes were obtained, and the differential expression genes between AMI and normal tissues were extracted through the GEO database. Then, through an online mapping tool, the intersection genes were obtained to predict the possible effective components of T. maculata that can be used to treat AMI. The top five targets were selected for molecular docking via the protein-protein interaction (PPI) network to verify the binding activity between key compounds and target proteins. GO and KEGG enrichment analyses of the intersection genes were carried out with the program R to further screen key genes and effective compositions. On this basis, the compound with more optimal activity was screened and validated in vitro. RESULTS: In this study, 40 known monomer components were selected, and 1112 predicted genes, 1655 disease genes, 1425 differentially expressed genes, 1206 GO functions and 127 KEGG pathways were obtained. The results of molecular docking showed that the binding of MMP9 with drug components is stable. Through the comprehensive research of network pharmacology and experimental pharmacology, it was shown that T. maculata intervenes in the process of AMI through multicomponent, multitarget, and multichannel synergistic effects. It is speculated that the anti-AMI effect may be related to the regulation of the Akt/FoxO/BCl signaling pathway. Cellular experiments showed that nicotiflorin has satisfactory anti-inflammatory activity and endothelial protection and can reduce the release of nitric oxide (NO), an inflammatory medium after endothelial cell damage. CONCLUSION: This study reveals the therapeutic effect and relative mechanism of extract of T. maculata extract on AMI. Analysis revealed that nicotiflorin from T. maculata is a compound with satisfactory anti-inflammatory activity and endothelial protection, which provides a new direction and treatment basis for further experimental exploration and clinical treatment.


Subject(s)
Flavonoids/therapeutic use , Liliaceae/chemistry , Myocardial Infarction/drug therapy , Phenols/therapeutic use , Plant Extracts/therapeutic use , Acute Disease , Databases, Pharmaceutical , Flavonoids/chemistry , Flavonoids/isolation & purification , Humans , Phenols/chemistry , Phenols/isolation & purification , Plant Extracts/chemistry , Plant Extracts/isolation & purification
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