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1.
Acta Pharmaceutica Sinica B ; (6): 1100-1125, 2022.
Article in English | WPRIM | ID: wpr-929369

ABSTRACT

Due to the special physiological and pathological characteristics of gliomas, most therapeutic drugs are prevented from entering the brain. To improve the poor prognosis of existing therapies, researchers have been continuously developing non-invasive methods to overcome barriers to gliomas therapy. Although these strategies can be used clinically to overcome the blood‒brain barrier (BBB), the accurate delivery of drugs to the glioma lesions cannot be ensured. Nano-drug delivery systems (NDDS) have been widely used for precise drug delivery. In recent years, researchers have gathered their wisdom to overcome barriers, so many well-designed NDDS have performed prominently in preclinical studies. These meticulous designs mainly include cascade passing through BBB and targeting to glioma lesions, drug release in response to the glioma microenvironment, biomimetic delivery systems based on endogenous cells/extracellular vesicles/protein, and carriers created according to the active ingredients of traditional Chinese medicines. We reviewed these well-designed NDDS in detail. Furthermore, we discussed the current ongoing and completed clinical trials of NDDS for gliomas therapy, and analyzed the challenges and trends faced by clinical translation of these well-designed NDDS.

2.
Article | WPRIM | ID: wpr-943109

ABSTRACT

Hepatoma is one of the most common malignant tumors of digestive system worldwide, and a main factor leading to cancer-related deaths. Its incidence is increasing year by year, posing a serious threat to human health. Currently, hepatoma is mainly treated by surgical resection, liver transplantation, radiation and drugs, but there are certain adverse reactions and problems of high recurrence rate and low survival rate. Chinese medicine has unique advantages in improving the comprehensive curative effect of hepatoma and reducing adverse reactions. With a variety of active ingredients, Chinese medicine can induce hepatoma cell apoptosis, inhibit the proliferation, migration and reverse multidrug resistance through multiple targets, thus exerting anti-hepatoma effect. It has become an important means for the prevention and treatment of hepatoma as well as a rich resource for anti-hepatoma drug research and development. Wnt/β-catenin signaling pathway, one of the most classical pathways in cancer, is involved in tumor cell proliferation, cell cycle, migration, invasion and tumor angiogenesis. Recently, many studies have reported that the active ingredients of Chinese medicine can play an anti-hepatoma role through this pathway. Therefore, this paper summarized the domestic and foreign literature in recent years, analyzed the relationship between wnt/β-catenin signaling pathway and the specific mechanism of hepatoma occurrence and development, and combed the literature on the effect of flavonoids, terpenoids, alkaloids, polysaccharides and other active ingredients of Chinese medicine on inducing hepatoma cell apoptosis, regulating cell cycle and inhibiting the invasion and metastasis through Wnt/β-catenin signaling pathway. In addition, the paper summarized the research progress of relevant active ingredients of Chinese medicine against hepatoma, to explore their specific mechanism against hepatoma through Wnt/β-catenin signaling pathway, so as to provide theoretical reference for further development of anti-hepatoma drugs.

3.
Article in Chinese | WPRIM | ID: wpr-943105

ABSTRACT

Alzheimer's disease (AD) is a common degenerative disease of the central nervous system in the elderly, with memory impairment and behavioral changes as the main clinical manifestations. Modern research has demonstrated that many herbs with both medicinal and edible values have anti-oxidation and anti-aging activities. In addition, these herbs are naturally safe and play a role in disease prevention and health care. The 110 medicinal and edible herbs announced by the National Health Commission of the People's Republic ofChina in 2021 were studied. The relevant papers published in the last five years were searched against CNKI, VIP, Wanfang Data, PubMed and other databases. The effects, mechanism, and active ingredients of the medicinal and edible herbs against Alzheimer's disease were summarized. The results showed that more than 30 herbs including Ginseng Radix et Rhizoma, Curcumae Longae Rhizoma, Astragali Radix, Corni Fructus, Gastrodiae Rhizoma, Angelicae Sinensis Radix, Cistanches Herba, Croci Stigma, Glycyrrhizae Radix et Rhizoma, Ganoderma and their active ingredients were effective in the prevention and treatment of Alzheimer's disease. Among them, ten herbs that met the requirements were screened out for analysis. The medicinal and edible herbs and their active ingredients can act on multiple targets and treat Alzheimer's disease via multiple signaling pathways such as nuclear factor-κB (NF-κB), mitogen-activated protein kinase 5 (MEK5)/extracellular signal-regulated kinase 5 (ERK5), cytochrome C (CytC) and cysteine aspartate-specific protease (Caspase)-3/(Caspase)-9, Wnt/β-catenin, and brain-derived neurotrophic factor (BDNF)/tyrosine kinase receptor B (TrkB)/phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt), thus improving learning, cognitive ability, and memory ability. Most of the medicinal and edible herbs have the tropism to the heart, spleen, liver, and kidney meridians and tonifying effect.

4.
Article in Chinese | WPRIM | ID: wpr-940716

ABSTRACT

Traditional Chinese medicine (TCM), which owns abundant chemical components and complex action pathways, has been widely recognized in the prevention and treatment of diseases. Some analysis methods have been emerged in order to ensure the quality of TCM and to develop new TCM drugs. Matrix-assisted laser desorption ionization mass spectrometry (MALDI-MS) is a soft ionization mass spectrometric technique with the advantages of high throughput, high sensitivity, low cost and so on. It provides technical support for the molecular level study on TCM. At present, this technique has been used in the field of composition analysis and metabonomics research of TCM, and plays an important role in the identification of Chinese herbal medicines, real-time molecular screening and the construction of metabolic network pathway of active ingredients. Among them, the selection of appropriate matrix and sample preparation technology is the key to ensure the detection effect of MALDI-MS. With the development and optimization of new matrix, the continuous improvement of sample preparation technology and the combination of MALDI-MS with various analytical methods will greatly improve the detection effect. Based on this, this paper discusses the application of MALDI-MS in TCM, including high-throughput detection of active ingredients in TCM, monitoring of the original medicines and their metabolites in vivo, and in situ visualization and characterization of tissue distribution information of active ingredients in TCM. It also discusses the application prospect and existing problems of MALDI-MS in TCM, so as to provide technical support for the identification of active ingredients in TCM, drug utilization and metabolism.

5.
Article in Chinese | WPRIM | ID: wpr-940641

ABSTRACT

As a traditional Chinese medicinal material, Glycyrrhizae Radix et Rhizoma has been extensively used in various formulae. According to modern pharmacological research, it has anti-tumor, anti-inflammatory, anti-viral, liver-protecting, anti-heart failure, immunoregulatory, and anti-fibrosis effects. Caused by the interaction of various factors, cancer features complex pathogenesis. It is a global challenge and one of the main causes of death in China. Statistics show that the morbidity and mortality of malignant tumors have been on the rise, particularly for the young, which threaten the health of human beings. At the moment, radiotherapy and chemotherapy are the main countermeasures. Most clinical anti-tumor drugs demonstrate non-selective toxicity. To be specific, they damage normal cells while killing tumor cells, thus injuring vital organs. In addition, long-term medication will reduce the sensitivity of tumor cells. However, traditional Chinese medicine, which is characterized by treatment based on syndrome differentiation, multiple components, and multiple targets, is superior in the treatment of tumor. Studies have shown that the combination of anti-tumor drugs with Chinese medicine can not only enhance the anti-tumor effect but also alleviate toxicity. Therefore, it has been a research hotspot to develop anti-tumor drugs based on traditional Chinese medicine. In recent years, major headway has been made in the research on active ingreddients of Glycyrrhizae Radix et Rhizoma in anti-liver cancer, anti-breast cancer, anti-lung cancer, and anti-colon cancer and the combination with other drugs for anti-tumor. On this basis, we summarized the mechanisms of active ingredients of Glycyrrhizae Radix et Rhizoma in inducing apoptosis, interfering with cell cycle, inducing autophagy, inhibiting glycolysis, regulating immunity, and modulating miRNA and signaling pathways, as well as the combination with other drugs in anti-tumor efficiency, toxicity reduction, and sensitivity enhancement, hoping to lay a theoretical basis for the further development and clinical application of active ingredients of Glycyrrhizae Radix et Rhizoma.

6.
Article in Chinese | WPRIM | ID: wpr-940473

ABSTRACT

Acute lung injury is a common critical respiratory disease, which can further develop into acute respiratory distress syndrome (ARDS) with a high fatality rate, but there is no effective drug at present. Phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) signaling pathway is involved in cell proliferation, metabolism, survival, and motility through phosphorylation of numerous downstream effector molecules. It plays an important role in the development of acute lung injury by regulating mitochondrial function, apoptosis, autophagy, oxidative stress, and inflammatory response. The active ingredients in Chinese medicinals alleviate acute lung injury by targeting the PI3K/Akt signaling pathway. There has been an explosion of research on the treatment of acute lung injury by active ingredients in Chinese medicinals via PI3K/Akt signaling pathway, which is of great clinical research value. The article presented the first summary of studies exploring the correlation between PI3K/Akt signaling pathway and acute lung injury in recent years and summed up the protective effect of the active ingredients in Chinese medicinals against acute lung injury via PI3K/Akt signaling pathway, providing innovative mindsets and strategies for clinical application of active ingredients in Chinese medicinals in the treatment of acute lung injury.

7.
Article in Chinese | WPRIM | ID: wpr-940372

ABSTRACT

The occurrence and development of malignant tumors seriously affect the survival time and quality of life of people all over the world, and finding proper treatment methods has been a focus for doctors. Especially in recent years, traditional Chinese medicine (TCM) has developed and attracted the attention of doctors and patients. From the perspective of TCM syndrome differentiation and treatment, deficiency and stasis are the most fundamental causes of malignant tumors, and supplementing deficiency and removing stasis can be regarded as the basic criteria of TCM treatment of malignant tumors. TCM prescriptions can treat diseases by means of multiple components and multiple targets, with the characteristics of slight side effect and high efficacy, safety and cost performance, as well as easiness to be accepted and taken. As a classic recipe for invigorating Qi and generating blood, Danggui Buxuetang consists of Astragali Radix -Angelicae Sinensis Radix 5∶1. It has excellent effects in anti-tumor, bone marrow suppression after chemotherapy, immune function decline, anemia, heart and cerebral vessels protection, blood deficiency-led fever, diabetes, anti-atherosclerosis, anti-fatigue, anti-radiation, myocardial ischemia alleviation, inhibition of platelet aggregation, liver damage, etc. In addition, with many active anti-tumor ingredients, Danggui Buxuetang can exert anti-tumor effects via acting on multiple targets in different binding sites. However, there has been a lack of reviews on the role of Danggui Buxuetang in malignant tumors so far. Therefore, in this paper, the functions of Danggui Buxuetang in malignant tumors were reviewed. Besides, molecular docking technology was used to analyze the main active anti-tumor ingredients and action targets of Danggui Buxuetang.

8.
Article in Chinese | WPRIM | ID: wpr-906319

ABSTRACT

Prostatic carcinoma (PCa) is one of the most common male malignancies, accounting for 10% of all male cancers, and has become a global health problem. At present, it is mainly tackled with radical prostatectomy and endocrine therapy. However, most patients will develop drug resistance, allowing the progression of PCa into castration-resistant prostate cancer (CRPC). Guided by the principles of holism and treatment based on syndrome differentiation, traditional Chinese medicine (TCM) alleviates cancer pain, regulates immune balance, and improves the quality of life of patients via multiple targets, multiple pathways, and multiple mechanisms without inducing obvious side effects, thus better exerting the preventive and therapeutic effects against PCa. This paper retrieved relevant articles concerning PCa intervention with TCM published in recent five years from PubMed and China National Knowledge Infrastructure (CNKI), and summarized the molecular mechanism of PCa, its etiology and pathogenesis in TCM, and TCM interventions. The findings showed that the active ingredients of Chinese medicinals, single Chinese medicinals and Chinese medicinal compounds inhibited PCa by interfering with not only the classical pathways of PCa such as androgen receptor(AR), Wnt/β-catenin, PI3K/Akt/mTOR, and NF-κB but also other pathways like ERS/UPR, RIPK, CIP2A/PP2A/ERK, EGFR, etc. The intervention of active ingredients from Chinese medicinals in PCa has been explored extensively, but there are fewer studies on single Chinese medicinals and Chinese medicinal compounds that can better reflect the unique advantages of TCM. Further research is needed to provide an important theoretical and experimental basis for the development of novel anti-PCa Chinese medicinal products and their clinical application.

9.
Article in Chinese | WPRIM | ID: wpr-906040

ABSTRACT

As a new technology with unique drug delivery advantages, nanoemulsion has been widely used in the field of traditional Chinese medicine (TCM) preparations. By searching, classifying and sorting out the literature reports at home and abroad in recent years, this paper systematically expounded the application advantages and production mechanism of nanoemulsion in delivering effective components of TCM from three aspects of improving oral bioavailability, enhancing targeting effect and delaying drug release. The current formulation optimization strategies, preparation processes and quality evaluation indicators commonly used in TCM nanoemulsion were summarized. Based on the research status of TCM nanoemulsion with different active components, the common problems and possible solutions in the development of TCM nanoemulsion were discussed, and the future research hotspots and directions of TCM nanoemulsion were prospected. This article clarifies the feasibility of nanoemulsion for enriching the selection of TCM dosage forms, which can provide reference for the subsequent rational design and improvement of TCM preparations. At the same time, it is revealed that the research focus of TCM nanoemulsion in the future lies in the integrated research of TCM compounds, and shows a trend of multi-disciplinary joint and targeted research.

10.
Article in Chinese | WPRIM | ID: wpr-905850

ABSTRACT

Succus Bambusae, regarded as the holy medicine for the treatment of phlegm by traditional Chinese medicine experts, has the functions of clearing heat and resolving phlegm, resuscitating and relieving convulsions. In clinical practice, it is mainly used to treat phlegm-heat cough, phlegm yellow and shortness of breath, stroke with exuberant phlegm and other syndromes. The research of its processing procedure and quality standard is the key issue to realize the process modernization and quality standardization of this traditional medicine resource. On the basis of literature research, this paper conducted the herbal textual research on Succus Bambusae, sorted out its medicinal history, and compared the advantages and disadvantages of its traditional and modern preparation procedure. Based on the historical records, it is pointed out that there are still many problems in the traditional and modern processing procedure of Succus Bambusae, such as low-yield processing procedure and extensive production technology that cannot meet the requirements of large-scale green manufacturing. At present, there are a lot of literature on the comparative study of the origin, variety and processing procedure of Succus Bambusae, but most of them are limited to the chemical components, and lack of in-depth study on its pharmacodynamic substance basis and mechanism. Meanwhile, the pharmacological effects of Succus Bambusae are mostly limited to antitussive and expectorant, and few other pharmacological effects have been reported. Based on the above analysis, it is suggested that the follow-up research work can be carried out from these five aspects:①Clarifying the original source, enriching and perfecting the medicinal resources. ②Standardizing the processing procedure, establishing relevant quality standards. ③Clarifying the pharmacological mechanism, strengthening the basic research on the pharmacological effect and clinical application. ④Inheriting ancient processing, researching and developing special preparation equipment and standardizing production operation rules. ⑤Comprehensive utilization of the by-products in preparation process.

11.
Article in Chinese | WPRIM | ID: wpr-888015

ABSTRACT

In this paper,metabolomics and network pharmacology were used to investigate the bioactive components of Harrisonia perforata and their possible mechanisms of action. Metabolites in the flowers,fruits,branches,leaves and stalks of H. perforata were analyzed by ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry. Meanwhile,multiple statistical analysis methods including principal component analysis( PCA) and orthogonal partial least squares discriminant analysis( OPLS-DA)were applied to screen and identify differential compounds. With metabolomics method,9 differential compounds were preliminarily identified from leaves and other non-traditional medicinal parts. Subsequently,these compounds were explored by using network pharmacology. With gastrointestinal absorption and drug-likeness as limiting conditions,they were imported into the Swiss ADME,from which 7 compounds with potential medicinal activity were obtained. Then,their targets were predicted by PharmMapper,with Human Protein Targets Only and Normalized Fit Score>0. 9 set as limiting conditions,and 60 standardized potential targets were identified with Uniprot. KEGG( Kyoto encyclopedia of genes and genomes) pathway data was obtained using metascape and the " potential active ingredients-target-pathway" network was constructed with Cytoscape 3. 7. 2. The enrichment analysis of KEGG demonstrated that the 60 targets were enriched in 78 signaling pathways( min overlap: 3,P value cutoff: 0. 01,min enrichment: 1. 5),many of which are related to anti-bacteria,anti-inflammation and anti-virus,such as IL-17 signaling pathway,RIG-I-like receptor signaling pathway and NOD-like receptor signaling pathway. Finally,depending on the clinical activity of H. perforata,the relevant signaling pathways were analyzed through experimental data and literature. Dehydroconiferyl alcohol was reported to have the anti-inflammatory effect and perforamone D to possess the antimycobacterial activity. The KEGG pathway enrichment analysis showed that dehydroconiferyl alcohol could act on the Alzheimer's disease( AD) signaling pathway by targeting CDK5 R1 and BACE1. ACh E inhibitor is the most promising drug to treat AD,while dehydroconiferyl alcohol has been proved to inhibit ACh E according to literature. The experimental results revealed that the extract of leaves of H. perforata can effectively inhibit the growth of Staphylococcus aureus. These are consistent with the enrichment analysis results of KEGG. This study explored the bioactive components and pharmacodynamics of the leaves of the H. perforata,laying a theoretical foundation for its in-depth development and rational application.


Subject(s)
Amyloid Precursor Protein Secretases , Aspartic Acid Endopeptidases , Drugs, Chinese Herbal/pharmacology , Humans , Metabolomics , Simaroubaceae
12.
Article in Chinese | WPRIM | ID: wpr-878982

ABSTRACT

In order to explore the effect of different drying methods(drying-in-the-shade, sun-drying, and hot air drying) on appearance characteristics, internal structure and composition of Belamcandae Rhizoma, so as to provide a theoretical basis for screening out suitable drying methods for primary processing. In this study, the Belamcandae Rhizoma's dynamic changes of the moisture content ratio and drying rate with different drying time under different drying methods, as well as the effects of different drying methods on the appearance, drying rate, density, ash, extractives and the contents of six flavonoids(mangiferin, tectoridin, iridin, tectorigenin, irigenin, irisflorentin) were compared. The results showed that fresh Belamcandae Rhizoma consumed the longest time to reach the water balance point by traditional dry drying in the shade, whiche was about 311 h; that by sun drying was 19.3%, which was shorter than drying in the shade; both drying curves were smoother. The section color of the sun drying samples was the closest to that of fresh samples, but the interior is full of holes, with a low density and loose structure. Hot air drying(40, 60, 80 ℃) could save about 27% to 88% of the drying time, which was greatly shorter, with less pores, a larger density and compact structure. Compared with the traditional drying method, the drying rate of hot air drying was reduced by 13.7%. Ash was affected by temperature, the drying conditions under 40 ℃ and below were not significantly different from those of conventional drying. The ash content decreased by 7.73% to 18.5% compared with conventional drying at 60,80 ℃. After conventional drying and 40 ℃ hot air drying, the contents of tectoridin and iridin(glycosides) in the samples were significantly higher than those in 60,80 ℃ hot air drying, while the contents of tectorigenin, irigenin and irisflorentin(aglycones) dried at 60 ℃ were the best. Therefore, considering comprehensive appearance characteristics and content of medicinal ingredients, traditional Chinese medicinal materials after 60 ℃ hot air drying show a solid texture, tight internal structure, good appearance, appropriate reduction of toxic parasides and higher aglycone content.


Subject(s)
Desiccation , Drugs, Chinese Herbal , Rhizome
13.
Article in Chinese | WPRIM | ID: wpr-878975

ABSTRACT

Liver is the main place of drug metabolism. Mitochondria of hepatocytes are important targets of drug-induced liver injury. Mitochondrial autophagy could maintain the healthy operation of mitochondria in cells and the stable proliferation of cells. Therefore, the use of mitochondrial autophagy to remove damaged mitochondria is an important strategy of anti-drug-induced liver injury. Active ingredients that could enhance mitochondrial autophagy are contained in many traditional Chinese medicines, which could regulate the mitochondrial autophagy to alleviate relevant diseases. However, there are only a few reports on how to accurately and efficiently identify and evaluate such components targeting mitochondria from traditional Chinese medicine. Liquid chromatography-mass spectro-metry(LC-MS) combined with serum pharmacology in vivo can be used to accurately and efficiently find active ingredients of traditional Chinese medicine acting on mitochondrial targets. This paper reviewed the research ideas and methods of traditional Chinese medicine ingredients for increasing the hepatotoxicity of mitochondrial autophagy, in order to provide new ideas and methods for the study of active ingredients of traditional Chinese medicine targeting mitochondria.


Subject(s)
Chemical and Drug Induced Liver Injury , Drug-Related Side Effects and Adverse Reactions , Drugs, Chinese Herbal/toxicity , Humans , Medicine, Chinese Traditional , Mitochondria
14.
Article in Chinese | WPRIM | ID: wpr-878972

ABSTRACT

In this study, 24 copies of samples of Chrysanthemum morifolium and soil from two main production towns in Macheng city were collected, and the contents of 13 mineral elements, 5 effective components and 14 soil nutrient factors in Ch. morifolium were determined. The enrichment characteristics of available soil nutrients by mineral elements were analyzed and the dominant factors affecting the effective components of Ch. morifolium were screened. The results showed that the content of mineral elements and soil nutrients and effective components are very different, and variation of soil fertility was much greater than that of inorganic elements in chrysanthemum plants. In general, the level of element content in Ch. morifolium from different producing areas is K>N>P>Mg>Ca>Fe>Mn>Zn>Cu>Ni>Cr>Pb>Cd. The content of K, N and Mg is higher than that of common crops, and the content of Cu, Cd and Pb in Ch. morifolium from various producing areas does not exceed the relevant standards. The N, P and K enrichment capacity in soil was stronger than that of other elements, and the Ca enrichment ability was the worst. The content of AvCu in the soil was positively correlated with the contents of N, Mg, K, Fe and Cu elements in Ch. morifolium. The contents of chlorogenic acid, luteolin, 3,5-O-dicaffeoylquinic acid reached the pharmacopoeia standard. The percentage of chlorogenic acid and 3,5-O-dicaffeoylquinic acid in Ch. morifolium that from Huangtugang town in the active components were generally higher than that from Futianhe town, and the diffe-rences of luteolin contents in the two producing areas were relatively small. The correlation and regression analysis showed that the contents of Cu, Zn and Cr in Ch. morifolium were positively correlated with the active components, while the contents of Fe, Mn and Ni were negatively correlated with the contents of AvP, AvK, TK, AvMn and AvCu in soil. In general, Zn and Ca fertilizer should be added to the ecological planting of Ch. morifolium, K fertilizer should be added, and N and P fertilizer should be applied appropriately.


Subject(s)
Chrysanthemum , Fertilizers , Minerals , Nutrients , Soil
15.
China Pharmacy ; (12): 1215-1223, 2021.
Article in Chinese | WPRIM | ID: wpr-876889

ABSTRACT

OBJECTIVE:To predict the potenti al target and mechanism of Astragali Radix in the treatment of ulcerative colitis (UC),and to provide reference for the clinical application of Astragali Radix in the treatment of UC. METHODS :The active components and their corresponding target genes of Astragali Radix were retrieved by TCMSP and UniProt KB database.related target genes of UC were searched by Gene Cards GZK-2018-5) database. The intersection target genes of Astragali Radix and were obtained by Venny 2.1.0 online mapping tool ,and interaction network of “drug-compound-intersection target ” was constructed by using Cytoscape 3.7.0 software. PPI network of intersecting targets was obtained by using STRING 结合动物模型。E-mail:172924249@qq.com database, and the visualization analysis and topological analysis w ere carried out by using Cytoscape 3.7.0 software to obtain the core target genes. By using DAVID database ,the gene ontology (GO) function annotation and KEGG pathway enrichment of intersecting target genes were carried out ,and the “target-pathway”enrichment network was constructed by using Cytoscape 3.7.0 software. Through Auto Dock vina 1.1.2 software, the top five active components in the list of degree value were linked with the protein encoded by the core target genes ;Discovery Studio 3.5 software was applied to draw out binding pattern map. RESULTS :There were 143 compounds in Astragali Radix ,20 active components were screened out ,and 189 corresponding target genes were selected ;there were 4 356 UC disease related target genes. There were 126 intersection target genes of Astragali Radix (involving 14 active components )and UC. The core target genes in PPI network were AKT1,MAPK1,RB1,JUN,etc. A total of 2 294 GO items (q value<0.05)were obtained from GO functional annotation ,including 2 093 biological process items (e.g. response to lipopolysaccharide ,response to molecule of bacterial origin ),49 cell composition items (e.g. membrane raft ,membrane microdomain ),and 152 molecular function items (e.g. nuclear receptor activity ,ligand-activated transcription factor activity ). KEGG pathway enrichment analysis yielded 160 items(q value<0.05),such as fluid shear stress and atherosclerosis signaling pathway ,phosphatidylinositol 3 kinase/protein kinase B (PI3K/Akt) signaling pathway ,interleukin-17 (IL-17) signaling pathway. Molecular docking results showed that top 5 active ingredients (quercetin,kaempferol,formenonetin,isorhamnetin,7-O-methylisomucronulatol) in the list of degree value had binding energies <5.0 kcal/mol with the protein encoded core targets. CONCLUSIONS :Quercetin,kaempferol,formononetin and other active components in Astragali Radix may play a role in the treatment of UC through the action of MAPK14,JUN,AKT1 and other target genes ,and then on the signal pathways such as PI 3K/Akt and IL- 17.

16.
China Pharmacy ; (12): 578-583, 2021.
Article in Chinese | WPRIM | ID: wpr-873672

ABSTRACT

OBJECTIVE:To study the effects and active ingr edients of Tibetan medicine Lamiophlomis rotata against rheumatoid arthritis (RA). METHODS :Fifty-six SD rats were randomly divided into normal control group (0.5% sodium carboxymethylcellulose),model group (0.5% sodium carboxymethylcellulose ),methotrexate group (positive control group ,3 mg/kg),L. rotata water extract low-dose ,medium-dose and high-dose groups (0.5,1,2 g/kg,by crude drug ),L. rotata total flavonoid group (200 mg/kg,by flavonoid extat ),with 8 rats in each group. Except for normal control group ,other groups were given Freund ’s complete adjuvant (FCA)on the rat ’s right hind footpad to induce adjuvant-induced arthritis model. The next day after injection of FCA ,rats in all groups were given relevant medicine intragastrically ,once a day (once every 3 days for methotrexate group )for 30 days. At 15th and 30th day of administration ,the degree of paw swelling of left hind foot was measured,and the arthritis index ,spleen index were calculated. At the end of 30th day of administration ,the levels of TNF-α,IL-1β, IL-6 and IL- 10 in rat serum were determined by ELISA assay ,the thymus index and spleen index were calculated ,the pathological changes of the ankle joints were observed by HE staining. RESULTS :Compared with normal control group ,degree of paw swelling,arthritis index at 15th and 30th day of administration as well as the spleen index and the levels of TNF-α,IL-1β, msxmX0146) IL-6 in serum at 30th day of administration were significantly com increased in model group (P<0.01);while the thymus indexyunbinji- and IL- 10 level at 30th day of administration were ang@swu.edu.cn significantly decreased(P<0.01);synovial cell proliferation and infiltration of articular cavity were observed in ankle joint. Compared with model group ,degree of paw swelling ,arthritis index at 15th and 30th day of administration as well as the spleen index and the levels of TNF-α,IL-1β,IL-6 in serum at 30th day of administration were significantly decreased in each medicine group (P<0.01);while the thymus index and IL- 10 level at 30th day of administration were significantly increased (P<0.01);the pathological changes of arthritis were significantly improved. Compared with L. rotata water extract high-dose group ,there were no significant differences in degree of paw swelling at 15th day of administration as well as the arthritis index ,spleen index ,levels of inflammatory cytokines and pathological changes of ankle joint in L. rotata total flavonoid group (P>0.05). CONCLUSIONS :Tibetan medicine L. rotata shows well anti-RA activity ,and total flavonoids may be the active ingredients of its efficacy.

17.
J Environ Biol ; 2020 May; 41(3): 556-562
Article | IMSEAR | ID: sea-214510

ABSTRACT

Aim: The effects of UV-B pretreatment on biosynthesis of active ingredients in Prunella vulgaris L. were studied from three aspects: active ingredients, physiological and biochemical parameters and key enzymes of rosmarinic acid metabolism pathway.Methodology: In greenhouse, the seedlings of P. vulgaris were subjected to UV-B treatment for 30 min from 10:30 a.m. to 11:00 a.m. every day for 10 days and then transplanted to field. After ripening, the leaves were harvested for physiological and biochemical estimations and the expression of key enzyme genes and the contents of active ingredients were measured by ear picking. Results: The results of active ingredient content showed that artificial UV-B radiation increased the contents of phenolic acids and individual flavonoids at mature fruiting stage compared with control plants. Physiological and biochemical results indicated that increase in peroxidase, ascorbate peroxidase, and superoxide dismutase activities seem to be active responses to alleviate the deleterious effects of UV-B in P. vulgaris. Under UV-B pre-treatment, genes related to rosmarinic acid/phenolic acid biosynthesis were significantly (p<0.05) over-expressed at seedling stage of P. vulgaris. Interpretation: This study indicated that UV-B pre-treatment in the seedling stage before transplantation to field is effective for inducing phenolic acid and flavonoid accumulation in P. vulgaris ears at mature fruiting stage.

18.
Article in Chinese | WPRIM | ID: wpr-828919

ABSTRACT

OBJECTIVE@#To explore the pharmacologically active ingredients in granules (TJQW) for treatment of coronavirus disease 2019 (COVID-19) in light of systemic pharmacology.@*METHODS@#We performed database search, literature mining and drug-like index screening to identify the bioactive components in TJQW, the positive drugs for disease treatment and their therapeutic targets. The core disease target was investigated based on the cross-linking interaction of the bioactive components, positive drug and potential disease target, and the target proteins at the key nodes were analyzed by GO and KEGG analyses. Based on the therapeutic targets for COVID-19, virtual screening was conducted to screen the compounds in TJQW and construct the network cross-linking the key bioactive molecules in TJQW, key node targets of the disease, and the related biological pathways.@*RESULTS@#We identified 159 compounds in TJQW and obtained 18 core proteins based on the cross-linking of the bioactive components, positive drugs and disease targets. The key node targets consisted of 22 targets including the latest 4 COVID-19 proteins. Virtual screening results showed that at least 14 compounds could bind with the core disease target proteins. The material basis of TJQW for COVID-19 treatment was explained in multi-pathway, multi-component and multi-target perspectives. In terms of the structural characteristics of the compounds, we screened the top 30 molecules with strong binding with the target proteins, among which flavonoids were the predominant components.@*CONCLUSIONS@#This investigation reveals the therapeutic mechanism of TJQW for COVID-19 involving multiple components, targets and pathways from the perspective of key bioactive molecules, disease key node targets and related biological pathways. We screened 30 active precursors from TJQW, which provides reference for the clinical application and further development of TJQW.


Subject(s)
Betacoronavirus , Coronavirus Infections , Drug Therapy , Drugs, Chinese Herbal , Humans , Medicine, Chinese Traditional , Pandemics , Pneumonia, Viral , Drug Therapy
19.
Article in Chinese | WPRIM | ID: wpr-846713

ABSTRACT

Traditional solvents have the shortcomings of toxic, easy to cause environmental pollution, volatile and low extraction rate. In recent years, there have been a lot of researches focusing on deep eutectic solvents (DESs) studies in the field of Chinese materia medica (CMM), especially in the extraction of active ingredients and improvement of stability of unstable compounds. This paper mainly reviews and sorts out the researches on DESs in the field of CMM reported at home and abroad in recent years, so as to provide references for the application of DESs in the field of CMM in the future.

20.
Article in Chinese | WPRIM | ID: wpr-846638

ABSTRACT

Objective: Active ingredients of 47 Asarum samples from different habitats with different phenotypes were analyzed in this paper in order to reveal the relationship between the formation of active ingredients and genetics and geography, and provide some scientific basis for the breeding and untilizing of Asarum. Methods: Ethanol extract and volatile oil were extracted according to the methods of Chinese Pharmacopoeia. Asarinin was detected by HPLC. Volatile oil compositon was determined by GC-MS. The between-groups linkage clustering method was carried out. Results: Volatile oil content of 47 samples was 0.81%-3.32%, and five samples’ volatile oil content exceeded 3.0 %. Ethanol extract content of samples was 9.87%-29.40%, and ethanol extract content of 30 resources accounting for 63.8 percent of all samples exceeded 20%. Asarinin content of 26 resources was more than 0.25%. Totally 48-77 compounds from the volatile oil could be determined and relative content of each compound was different. Forty-seven samples from different habitats with different phenotypes were divided to ten groups by between-groups linkage clustering method according to the active ingredients. All the accessions could be classified clearly. The cluster of accessions was associated with resource region. Asarum heterotropoides var. mandshuricum and Asarum sieboldii var. seoulense from the same origin were grouped together. Conclusion: There were much more differences in active ingredients content among Asarum resources which were in different regions cultivated with same way and environment with different phenotypes. We could select the perfect fundamental material according to the phenotypes and introduce germplasm from different regions for breeding and utilizing of Asarum. Most of samples clustered together associated with their origins instead of phenotype or specie.

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