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1.
Article in English | WPRIM | ID: wpr-929262

ABSTRACT

Chemical fractionation of the n-BuOH partition, which was generated from the EtOH extract of the flower buds of Tussilago farfara, afforded a series of polar constituents including four new sesquiterpenoids (1-4), one new sesquiterpenoid glucoside (5) and one known analogue (6) of the eudesmane type, as well as five known quinic acid derivatives (7-11). Structures of the new compounds were unambiguously characterized by detailed spectroscopic analyses, with their absolute configurations being established by X-ray crystallography, electronic circular dichroism (ECD) calculation and induced ECD experiments. The inhibitory effect of all the isolates against LPS-induced NO production in murine RAW264.7 macrophages was evaluated, with isochlorogenic acid A (7) showing significant inhibitory activity.


Subject(s)
Animals , Flowers/chemistry , Glucosides/pharmacology , Mice , Sesquiterpenes/pharmacology , Sesquiterpenes, Eudesmane/pharmacology , Tussilago/chemistry
2.
Article in English | WPRIM | ID: wpr-929054

ABSTRACT

Marine fungi are important members of the marine microbiome, which have been paid growing attention by scientists in recent years. The secondary metabolites of marine fungi have been reported to contain rich and diverse compounds with novel structures (Chen et al., 2019). Aspergillus terreus, the higher level marine fungus of the Aspergillus genus (family of Trichocomaceae, order of Eurotiales, class of Eurotiomycetes, phylum of Ascomycota), is widely distributed in both sea and land. In our previous study, the coral-derived A. terreus strain C23-3 exhibited potential in producing other biologically active (with antioxidant, acetylcholinesterase inhibition, and anti-inflammatory activity) compounds like arylbutyrolactones, territrems, and isoflavones, and high sensitivity to the chemical regulation of secondary metabolism (Yang et al., 2019, 2020; Nie et al., 2020; Ma et al., 2021). Moreover, we have isolated two different benzaldehydes, including a benzaldehyde with a novel structure, from A. terreus C23-3 which was derived from Pectinia paeonia of Xuwen, Zhanjiang City, Guangdong Province, China.


Subject(s)
Acetylcholinesterase/metabolism , Animals , Anthozoa/microbiology , Anti-Inflammatory Agents/pharmacology , Aspergillus/chemistry , Benzaldehydes/pharmacology , Mice , Signal Transduction
3.
Article in Chinese | WPRIM | ID: wpr-927336

ABSTRACT

OBJECTIVE@#To observe the effect of moxibustion on skin lesions and immune inflammatory response in psoriasis mice, and to explore the possible mechanism of moxibustion for psoriasis.@*METHODS@#A total of 32 male BALB/c mice were randomly divided into a normal group, a model group, a moxibustion group and a medication group, 8 mice in each group. Psoriasis model was induced by applying 5% imiquimod cream on the back for 7 days in the model group, the moxibustion group and the medication group. At the same time of model establishment, the moxibustion group was treated with suspension moxibustion on skin lesions on the back, 20 min each time, once a day; the medication group was treated with 1 mg/kg methotrexate tablet solution by gavage, once a day. Both groups were intervened for 7 days. The daily changes of skin lesions were observed, and the psoriasis area and severity index (PASI) score was evaluated; the histopathological changes of skin lesions were observed by HE staining; the positive expression of proliferating cell nuclear antigen (PCNA) and T lymphocyte surface marker CD3 were detected by immunohistochemistry; the expression level of serum interleukin (IL) -17A was detected by ELISA, and the relative expressions of tumor necrosis factor-α (TNF-α), IL-1β and IL-6 mRNA in skin lesions were detected by real-time PCR.@*RESULTS@#The increased and hypertrophy scale, dry skin, red and swollen epidermis and obvious infiltration were observed in the model group, and each score and total score of PASI were higher than those in the normal group (P<0.01). The scale score, infiltration score, and total score of PASI in the moxibustion group were lower than those in the model group (P<0.01); the infiltration score and total score of PASI in the medication group were lower than those in the model group (P<0.01, P<0.05). The inflammatory cell infiltration in the model group was obvious, and the thickness of epidermal layer was increased compared with that in the normal group (P<0.01); the inflammatory cell infiltration and Munro micro abscess were decreased in the moxibustion group and the medication group, and the thickness of epidermal layer was decreased compared with that in the model group (P<0.01). Compared with the normal group, the positive cell number of PCNA and T was increased (P<0.01), and the body mass was decreased, and the spleen index was increased (P<0.01), and the expression of serum IL-17A and the relative expression of TNF-α, IL-1β and IL-6 mRNA in the skin lesions was increased in the model group (P<0.01). Compared with the model group, the positive cell number of PCNA and T was reduced (P<0.01), and the spleen index and the relative expression of TNF-α, IL-1β and IL-6 mRNA were reduced (P<0.01) in the moxibustion group and the medication group; the body mass of mice in the moxibustion group was higher than that in the model group (P<0.01); the content of serum IL-17A in the medication group was lower than that in the model group (P<0.01); the relative expression of TNF-α, IL-1β mRNA in the moxibustion group was higher than that in the medication group (P<0.01).@*CONCLUSION@#Moxibustion could effectively improve the scale and infiltration of skin lesions in psoriasis mice. Its mechanism may be related to inhibiting inflammatory response and regulating immunity.


Subject(s)
Animals , Imiquimod , Male , Mice , Moxibustion , Psoriasis/therapy , Skin , Spleen , Tumor Necrosis Factor-alpha/genetics
4.
Article in Chinese | WPRIM | ID: wpr-907701

ABSTRACT

Objective:To optimize the preparation technic of Chuanxiong Rhizoma with vacuum steam method, and to investigate the anti-inflammatory and analgesic activity of Chuanxiong Rhizoma decoction pieces with Central Composite Design-Response Surface Method. Methods:Taking the content of ferulic acid as the evaluation index and the moistening temperature, moistening time and vacuum time as the observation indexes, the moistening technic of Chuanxiong Rhizoma was optimized by Response Surface Method, and selected the optimized plan. The anti-inflammatory and analgesic activities of Chuanxiong Rhizoma were investigated by auricle swelling induced by xylene and writhing induced by glacial acetic acid. Results:The optimum vacuum moistening technic was that the softening temperature was 80 ℃, the softening time was 50 min and the vacuum time was 45 min. The content of ferulic acid in Chuanxiong Rhizoma produced by this technic is highand could decreased the times of wrinkle reaction induced by acetic acid in mice, prolonged the latent period, and obviously or partially inhibitied the ear swelling degree induced byxylene in rats. Conclusions:The Response Surface Method technic of Chuanxiong Rhizoma is easy to operate with high accuracy. The vacuum steam treatment was more obvious than traditional technology group. It provides reference for the subsequent production of Chuanxiong Rhizoma decoction pieces and have the certain value for its promotion and application.

5.
Acta Pharmaceutica Sinica ; (12): 3493-3502, 2021.
Article in Chinese | WPRIM | ID: wpr-906842

ABSTRACT

Caveolin-1 (CAV-1) is related to inflammation, oxidative damage, and immunity. In order to obtain a series of dibenzoylmethane halophenols with strong anti-inflammatory and antioxidant effects targeting CAV-1, twenty-nine target compounds were therefore synthesized by Baker-Ventaraman rearrangement and demethylation reaction, starting from the substituted benzoyl chloride and o-hydroxyacetophenone, and their interactions with CAV-1 were investigated by BLI technique. Their in vitro anti-inflammatory and antioxidant properties were also evaluated. The results showed that compounds A6, A17, A18, and A29 not only specifically bind to CAV-1, but also present strong anti-inflammatory and antioxidant effects. These results suggest that this class of compounds can affect the signaling pathways related to inflammation and oxidative stress by directly acting on CAV-1. In particular, these compounds exhibit the most significantly inhibitory effects on IL-1β and COX-2 release. IL-1β plays a key regulatory role in the development of arthritis. Therefore, it is worth expecting for the application of such compounds in the prevention and treatment of arthritis.

6.
Article in English | WPRIM | ID: wpr-922259

ABSTRACT

: To investigate the protective effect of (FD) against ethanol-induced gastric ulcer and its mechanism. : Human gastric epithelial GES-1 cells were divided into normal control group, model control group, FD 95% alcohol extract group, FD 50% alcohol extract group and FD decoction extract group. Gastric ulcer was induced by treatment with 1% ethanol in GES-1 cells. The cell proliferation was detected with MTT method in each group. Sixty SD rats were randomly divided into normal control group, model control group, ranitidine group and low-dose, medium-dose, high-dose FD 95% alcohol extract groups (150, 300, 600 mg/kg). The corresponding drugs were administrated by gavage for The gastric ulcer model was induced by intragastric administration of anhydrous ethanol. The gastric ulcer area and ulcer inhibition rate of rats were measured in each group; the degree of gastricmucosal damage was observed by scanning electron microscopy; the levels of tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-1β in serum and the content of malondialdehyde (MDA), superoxide dismutase (SOD), glutathione (GSH), catalase (CAT) in gastric tissues were detected by ELISA method. : 95% alcohol extract of FD had the strongest protective effect on proliferation of GES-1 cells. In animal experiments, compared with the normal control group, a large area of ulcers appeared on the gastric mucosa in the model control group, while the ulcer areas of the FD groups and ranitidine group were significantly smaller than that of the model control group (all <0.05). Compared with the model control group, FD groups and ranitidine group significantly reduced the levels of TNF-α, IL-1β, IL-6 in serum and the MDA content in the gastric tissues, and increased the activity of SOD, CAT and GSH in gastric tissues (all <0.05). : The 95% alcohol extract of FD can reduce the levels of TNF-α, IL-1β and IL-6 in serum and the content of MDA in gastric tissues, and increase the activity of SOD, CAT and GSH in gastric tissues to achieve the protective effect against gastric ulcer.


Subject(s)
Animals , Ethanol/toxicity , Gastric Mucosa , Malondialdehyde , Rats , Rats, Sprague-Dawley , Stomach Ulcer/prevention & control , Superoxide Dismutase
7.
Article in English | WPRIM | ID: wpr-888783

ABSTRACT

A large number of protease inhibitors have been found from leeches, which are essential in various physiological and biological processes. In the curret study, a novel elastase inhibitor was purified and characterized from the leech of Hirudinaria manillensis, which was named HMEI-A. Primary structure analysis showed that HMEI-A belonged to a new family of proteins. HMEI-A exerted inhibitory effects on elastase and showed potent abilities to inhibit elastase with an inhibition constant (K


Subject(s)
Amino Acid Sequence , Animals , Leeches/chemistry , Pancreatic Elastase/antagonists & inhibitors , Protease Inhibitors/pharmacology , Proteins
8.
Article in Chinese | WPRIM | ID: wpr-921712

ABSTRACT

This study aimed to investigate the anti-inflammatory, antitussive, expectorant, and anti-asthmatic effects of Qinbaohong Oral Liquid in mouse experiments and explore its action mechanism based on network pharmacology. The mouse auricle swelling was induced by xylene for detecting the anti-inflammatory effect of Qinbaohong Oral Liquid, whose antitussive effect was then examined in mice with cough after exposure to ammonium hydroxide. The expectorant effect was determined based on the excretion of phenol red into the mouse trachea. The mouse model of asthma induced by histamine phosphate and acetylcholine chloride was used to observe the anti-asthmatic effect. The chemical components of Qinbaohong Oral Liquid were retrieved from TCMSP and literature, followed by target prediction based on BATMAN-TCM. The targets of inflammation, cough, expectoration, and asthma collected from GeneCards were intersected with drug targets for GO and KEGG enrichment analysis using Metascape. The results were imported into STRING for exploring protein-protein interactions and screening the key targets. As demonstrated by our findings, Qinbaohong Oral Liquid at 4.5 and 9.0 mL·kg~(-1) obviously decreased the weight(P<0.05) and thickness(P<0.01) of the right swelling ear and also the weight diffe-rence(swelling degree) between the two ears(P<0.05), prolonged the incubation period of cough(P<0.05), reduced the frequency of cough within 3 min(P<0.05), and increased the excretion of phenol red into the mouse trachea(P<0.01). Qinbaohong Oral Li-quid at 2.3, 4.5, and 9.0 mL·kg~(-1) dramatically prolonged the incubation period of asthma(P<0.05). A total of 324 chemical components and 1 245 targets were harvested for the Qinbaohong Oral Liquid, together with 10 272 inflammation targets, 4 400 cough targets, 192 expectoration targets, and 7 533 asthma targets. Their intersection revealed that the anti-inflammatory, antitussive, expectorant and anti-asthmatic effects of Qinbaohong Oral Liquid were correlated with such GO biological processes as the regulation of ion transport and blood circulation and such KEGG pathways as cancer-related signaling pathways and neuroactive ligand-receptor interaction. Qinbaohong Oral Liquid has been confirmed by both experiments and network pharmacology analysis to be efficient in anti-inflammation, stopping cough, eliminating phlegm, and relieving asthma.


Subject(s)
Animals , Anti-Inflammatory Agents/therapeutic use , Antitussive Agents/therapeutic use , Asthma/drug therapy , Cough/drug therapy , Drugs, Chinese Herbal/therapeutic use , Mice , Network Pharmacology
9.
Article in Chinese | WPRIM | ID: wpr-909569

ABSTRACT

OBJECTIVE Forsythiae Fructus (Lianqiao) is a typical heat-clearing and detoxicating traditional Chinese medicine (TCM) herb, which has been traditionally used for treating cancer according to TCM theory. However, the under?lying mechanism has not been fully explained. METHODS In this study, we investigated the antitumor effect of Forsyth?iae Fructus aqueous extract (FAE) on B16-F10 melanoma. RESULTS FAE strongly inhibited the tumor growth and metastasis formation in B16-F10 melanoma transplanted mice. The survival time of tumor-bearing mice was also signifi?cantly prolonged by FAE. The levels of ROS, MDA, TNF-α and IL-6 decreased, while GSH increased in the FAE treat?ment group, indicating FAE possesses strong anti-oxidative and anti-inflammatory activity. Western blotting analysis demonstrated that antioxidant proteins Nrf2 and HO-1, tumor suppressors P53 and p-PTEN, and the MAPK pathways in tumor tissues were upregulated by FAE treatment. Serum metabolomics analysis further uncovered that 17 metabolites mostly involving in glycerophospholipid metabolism were correlated with the antitumor effect of FAE. Notably, several lysophosphatidylcholines (LysoPCs) significantly decreased in tumor model group, while FAE treatment restored the changes of these phospholipids to about normal condition. LysoPC acyltransferase 1 (LPCAT1) and autotaxin (ATX) highly expressed in melanoma and markedly downregulated by FAE were believed to be responsible for this modulation. CONCLUSION FAE exhibites strong antitumor activity against B16-F10 melanoma through activating MAPKs/Nrf2/HO-1 mediated anti-oxidation and anti-inflammation and modulating glycerophospholipid metabolism via downregulating LPCAT1 and ATX. Besides, it is suggested that serum LysoPCs could be potential biomarkers for the diagnosis and prog?nosis of melanoma.

10.
Article in Chinese | WPRIM | ID: wpr-906381

ABSTRACT

Angelicae Sinensis Radix, derived from a medicinal and edible plant Angelica sinensis, is one of the traditional bulk Chinese medicines. In addition to gynecological blood stagnation and deficiency, its indications also include dysmenorrhea, deficiency and cold-induced abdominal pain, and rheumatoid arthritis. With the in-depth study of Angelicae Sinensis Radix, its anti-inflammatory and analgesic activities have attracted widespread attention. However, there has been no systemic report. The present study comprehensively reviewed the anti-inflammatory and analgesic activities of Angelicae Sinensis Radix (including its compositions, extracts, and different processed products) and mechanisms published in recent 30 years. The anti-inflammatory effect of Angelicae Sinensis Radix was achieved mainly by blocking the expression of proteins and genes in nuclear factor-κB (NF-κB), mitogen-activated protein kinases (MAPK), and Janus kinase (JAK)/signal transducer and activator of transcription (STAT) signaling pathways, inhibiting the release of inflammatory mediators including tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), nitric oxide (NO), prostaglandin E2 (PGE2) and IL-1β, and maintaining the high sensitivity of immune cells in the host to external stimuli. The mechanism of analgesic effect may be related to the suppression of the production of algesic substances (such as inflammatory factors and chemokines) or blocking of the amplification and transmission of pain perception in cascade reaction. Furthermore, the study also pointed out some problems in modern research and proposed suggestions on its future research to provide references for investigation and clinical applications of Angelicae Sinensis Radix.

11.
Article in Chinese | WPRIM | ID: wpr-906151

ABSTRACT

Objective:To evaluate of modified Shentong Zhuyutang combined with celecoxib capsules in the treatment of acute discogenic low back pain due to wind-cold and stasis obstruction sydrome. Method:One hundred and forty eligible patients were randomly divided into control group (70 cases) and observation group (70 cases). Patients in both groups took the celecoxib capsules orally, 200 mg/time. On this basis, patients in the control group were further treated with Tongluo Huoxue capsule orally, 6 capsules/time, 3 times/day, while those in the observation group received the modified Shentong Zhuyutang, 1 bag/day, for three weeks. The short-form McGillpain questionnaire (SF-MPQ), including pain rating index (PRI), present pain intensity (PPI), and visual analog scale (VAS), Oswestry disability index (ODI), wind-cold obstruction and stasis syndrome, and abilities of daily living (ADL) scoring and the Schober's test were conducted before and after treatment. The tumor necrosis factor-<italic>α</italic> (TNF-<italic>α</italic>), interleukin-1<italic>β</italic> (IL-1<italic>β</italic>), IL-6, thromboxane B<sub>2</sub> (TXB<sub>2</sub>), and 6-keto prostaglandin F<sub>1</sub><italic><sub>α</sub></italic> (6-keto-PGF<sub>1</sub><italic><sub>α</sub></italic>) levels before and after treatment were measured, followed by the safety evaluation. Result:The PRI, VAS, and PPI scores in SF-MPQ of the observation group were reduced in contrast to those in the control group (<italic>P</italic><0.01). The wind-cold and stasis obstruction syndrome and ODI scores in the observation group also declined as compared with those of the control group (<italic>P</italic><0.01), while the ADL and Schober's test scores were elevated (<italic>P</italic><0.01). The TNF-<italic>α</italic>, IL-1<italic>β</italic>, IL-6, and TXB<sub>2</sub> levels in the observation group were lower than those in the control group (<italic>P</italic><0.01), whereas the 6-keto-PGF<sub>1</sub><italic><sub>α</sub></italic> was higher (<italic>P</italic><0.01). The excellent and good rate of the observation group was (51/63) 80.95%, significantly better than (39/63) 61.90% of the control group (<italic>χ</italic><sup>2</sup>=5.601, <italic>P</italic><0.05). No adverse reactions occurred after the intake of Chinese medicinal prescriptions. Conclusion:The modified Shentong Zhuyutang combined with celecoxib capsules is efficient and safe in inhibiting inflammation, easing back pain, enhancing lumbar spine mobility, and improving the ADL of patients with acute DLBP of wind-cold obstruction syndrome.

12.
Article in Chinese | WPRIM | ID: wpr-905943

ABSTRACT

Objective:To analyze the compatibility rules of prescriptions containing Forsythiae Fructus based on data mining and explore the anti-inflammatory mechanism of Forsythiae Fructus based on network pharmacology,so as to provide reference for the rational clinical application of Forsythiae Fructus and the development of health foods and new Chinese medicines. Method:The prescriptions containing Forsythiae Fructus in the<italic> Dictionary of Traditional Chinese Medicine Prescriptions</italic> were collected,based on which a clinical prescription database was constructed. The Chinese herbs combined with Forsythiae Fructus and the corresponding indications were subjected to frequency statistics,association rule analysis,and complex network analysis using SPSS Statistics 26,IBM SPSS Modeler 18.0,and Gephi 9.2. The active components and targets of Forsythiae Fructus for anti-inflammation were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP),BATMAN-TCM,and SEA,and the targets related to anti-inflammation from GeneCards,Online Mendelian Inheritance in Man (OMIM),CTD,and GenCLiP3. Following the analysis of protein-protein interactions (PPI) with STRING,a PPI network was constructed. The enrichment analysis was performed using Metascape,and the active component-anti-inflammation target-signaling pathway network of Forsythiae Fructus was constructed by Cytoscape 3.8.2. Result:According to the inclusion and exclusion criteria,2 245 prescriptions containing Forsythiae Fructus were harvested,involving 512 Chinese herbs,with a total usage frequency of 27 314. The Chinese herbs that were most frequently combined with Forsythiae Fructus (>800 times) were Glycyrrhizae Radix et Rhizoma (1 483 times),Scutellariae Radix (964 times),and Angelicae Sinensis Radix (842 times). Hence,the herbal pairs "Forsythiae Fructus-Scutellariae Radix" and "Forsythiae Fructus-Angelicae Sinensis Radix" were further explored. The prescriptions containing Forsythiae Fructus could be utilized for the treatment of 29 kinds of diseases,and three representative disease categories including "carbuncle,gangrene,sores and ulcers","ophthalmic diseases and syndromes" and "epidemic diseases" are selected for data mining. There were 19 association rules obtained with "Forsythiae Fructus-Glycyrrhizae Radix et Rhizoma-Lonicerae Japonicae Flos-Angelicae Sinensis Radix" as the core herb combination for "carbuncle,gangrene,sores and ulcers". The clustering analysis revealed one multi-herb clustering group,four herbal pairs,and single herb Lonicerae Japonicae Flos,the complex network analysis four herbal modules,and the factor analysis six common factors. There were 23 association rules obtained with "Forsythiae Fructus-Glycyrrhizae Radix et Rhizoma-Scutellariae Radix-Angelicae Sinensis Radix" as the core herb combination for "ophthalmic diseases and syndromes". The clustering analysis revealed two multi-herb clustering groups and four herbal pairs,the complex network analysis four herbal modules,and the factor analysis five common factors. There were 28 association rules obtained with "Forsythiae Fructus-Glycyrrhizae Radix et Rhizoma-Menthae Haplocalycis Herba-Lonicerae Japonicae Flos" as the core herb combination for "epidemic diseases". The clustering analysis revealed three multi-herb clustering groups,one herbal pair,and two single herbs Forsythiae Fructus and Glycyrrhizae Radix et Rhizoma,the complex network analysis four herbal modules,and the factor analysis five common factors. As demonstrated by network pharmacology-based analysis,the core anti-inflammation components of Forsythiae Fructus were quercetin,luteolin,and kaempferol,and the core targets were phosphoinositide-3-kinase regulatory subunit 1 (PIK3R1),protein kinase B 1 (Akt1),and epidermal growth factor receptor(EGFR). The biological pathways were mainly concentrated in proteoglycans in cancer,pathways in cancer,and PI3K/Akt signaling pathway,with such functions as inhibition of transcription factors,regulation of enzyme activity,and inflammation-related gene expression involved. Conclusion:This study employed a variety of data mining techniques to objectively,intuitively,and scientifically uncover the compatibility rules of Forsythiae Fructus in the treatment of high-frequency diseases. It has been found that Forsythiae Fructus is often combined with heat-clearing herbs,tonifying herbs,exterior-releasing herbs,and blood-activating and stasis-resolving herbs for diverse diseases and syndromes. Under the premise of clearing heat and removing toxin,reinforcing healthy Qi and dredging stagnation are also emphasized. According to the degree of internal heat exuberance,the heat-clearing herbs with different merits are combined. This study has revealed the unique advantages of Forsythiae Fructus in the treatment of specific diseases and syndromes as well as its multi-component,multi-target,and multi-pathway mechanisms in anti-inflammation,breaking through the limitations in modern clinical and experimental research of Forsythiae Fructus. These findings are of great significance for guiding the rational clinical application of Forsythiae Fructus and the development of health foods and new Chinese medicines,thus better accelerating the development of Chinese medicine health industry.

13.
China Pharmacy ; (12): 2635-2639, 2021.
Article in Chinese | WPRIM | ID: wpr-904523

ABSTRACT

OBJECTIVE:To stu dy the improvement effects o f Trillium tschonos kii total sapo nins(TTM)on adjuvant-induced arthritis model rats and its mechanism. METHODS :SD rats were randomly divided into model group (n=44)and blank group (n=6). Model group was given Complete Freund ’s adjuvant to induce the adjuvant-induced arthritis model ;blank group was given constant volume of normal saline with same method. Model group were divided into model group ,Tripterygium wilfordii polyglycoside tablets group (40 mg/kg),TTM low-dose ,medium-dose and high-dose groups (50,100,200 mg/kg),with 6 rats in each group. Administration groups were given relevant medicine intragastrically ;blank group and model group were given normal saline intragastrically ,once a day ,for consecutive 9 days. After last intragastric administration ,the body weight and foot swelling degree (bilateral)were detected ,and arthritis score was performed. The contents of tumor necrosis fator α(TNF-α), interleukin 1β(IL-1β)and IL- 6 were detected ;the pathomorphological changes of rat ankle were observed ;protein expression of NOD-like receptor protein 3 (NLRP3),apoptosis associated spot-like protein (ASC),caspase-1 were detected ;the protein expression of NLRP 3 in synovial tissue of ankle joint were also determined. RESULTS :Compared with blank group ,foot swelling degree,serum contents of TNF-α,IL-1β and IL-6,the protein expression of NLRP 3,ASC and caspase- 1 in knee tissue as well as the protein expression of NLRP 3 in synovial tissue of ankle joint were increased significantly in model group (P<0.05 or P< 0.01),while the body weight was decreased significantly (P<0.05). The obvious proliferation of synovial cells ,the congestion and inflammatory cell infiltration of synovial tissue were all observed. Compared with model group ,most of the above indexes were all reversed significantly in TTM groups (P<0.05 or P<0.01);the pathological changes such as synovial cell proliferation , congestion of synovial tissue and chondrocyte destruction were all relieved ,and inflammatory cell infiltration was alleviated.CONCLUSIONS:TTM can improve rheumatoid arthritis of rats, the mechanism of which may be associated with 用。E-mail:yulingling@ctgu.edu.cn inhibiting the activity of NLRP 3/caspase-1 signaling pathway and decreasing the expression of inflammatory factors TNF-α,IL-1β,IL-6.

14.
Acta Pharmaceutica Sinica B ; (6): 3465-3480, 2021.
Article in English | WPRIM | ID: wpr-922808

ABSTRACT

Glioblastoma multiforme (GBM) in the central nervous system is the most lethal advanced glioma and currently there is no effective treatment for it. Studies of sinomenine, an alkaloid from the Chinese medicinal plant,

15.
Article in Chinese | WPRIM | ID: wpr-888083

ABSTRACT

As recorded, agarwood has the function of improving qi reception and relieving asthma, but the underlying mechanism is unclear and rarely reported. Therefore, this study explored the anti-asthmatic effect of the alcohol extract of agarwood produced by the whole-tree agarwood-inducing technique(Agar-Wit) in the asthma mouse model induced by intraperitoneal injection of ovalbumin(OVA) + Al(OH)_3 combined with intranasal administration of OVA and the mechanism, and compared the anti-asthmatic effects of agarwood induced with different methods. Firstly, the anti-inflammatory and anti-asthmatic effects of Agar-Wit agarwood in mice were evaluated based on the asthma frequency, lung tissue injury, and peripheral inflammatory white blood cell(WBC) count and eosinophil count. Then, the levels of interleukin-1β(IL-1β), IL-17, and IL-10 in serum of mice were detected by enzyme-linked immunoassay(ELISA) and the expression of inflammation-and apoptosis-related genes in tissues was measured by reverse transcription polyme-rase chain reaction(RT-PCR) so as to preliminarily explore the anti-asthmatic mechanism. RESULTS:: showed that the alcohol extract of Agar-Wit agarwood significantly reduced asthma frequency, relieved pathological injury, improved peripheral WBC count and eosinophil count, decreased the levels of inflammatory cytokines IL-1β and IL-17, elevated the level of anti-inflammatory cytokine IL-10, and down-regulated the mRNA expression of IL-1 R, tumor necrosis factor receptor R(TNFR), nuclear transcription factor-kappa B(NF-κB), Bax, and caspase 3, but had no significant influence on the expression of high-mobility group box 1(HMGB1) protein, caspase 8, and Bcl-2. The effect of Agar-Wit agarwood alcohol extract was better than that of wild agarwood alcohol extract and alcohol extract of agarwood induced with the burning-chisel-drilling method at the same dose. In conclusion, Agar-Wit agarwood can significantly alleviate inflammation and asthma, which is related to its anti-inflammation and anti-apoptosis activity.


Subject(s)
Animals , Anti-Asthmatic Agents , Asthma/drug therapy , Bronchoalveolar Lavage Fluid , Disease Models, Animal , Lung , Mice , Mice, Inbred BALB C , NF-kappa B , Ovalbumin , Plant Extracts/therapeutic use
16.
Acta Pharmaceutica Sinica B ; (6): 456-475, 2021.
Article in English | WPRIM | ID: wpr-881147

ABSTRACT

Metal-based carbon monoxide (CO)-releasing molecules have been shown to exert anti-inflammatory and anti-oxidative properties maintaining gastric mucosal integrity. We are interested in further development of metal-free CO-based therapeutics for oral administration. Thus, we examine the protective effect of representative CO prodrug, BW-CO-111, in rat models of gastric damage induced by necrotic ethanol or aspirin, a representative non-steroidal anti-inflammatory drug. Treatment effectiveness was assessed by measuring the microscopic/macroscopic gastric damage area and gastric blood flow by laser flowmetry. Gastric mucosal mRNA and/or protein expressions of HMOX1, HMOX2, nuclear factor erythroid 2-related factor 2, COX1, COX2,

17.
Article in English | WPRIM | ID: wpr-881065

ABSTRACT

Chlorogenic acid (5-CQA), neochlorogenic acid (3-CQA), and cryptochlorogenic acid (4-CQA), usually simultaneously exist in many traditional Chinese medicines (TCMs). However, insufficient attentions have been paid to the comparative metabolism study on these three isomeric constituents with similar effects on anti-inflammation until now. In this study, a novel strategy was established to perform comparative analysis of their metabolic fates in rats and elucidate the pharmacological mechanism of anti-inflammation. Firstly, diagnostic product ions (DPIs) deduced from the representative reference standards were adopted to rapidly screen and characterize the metabolites in rat plasma, urine and faeces using UHPLC-Q-TOF MS. Subsequently, Network pharmacology was utilized to elucidate their anti-inflammatory mechanism. Consequently, a total of 73 metabolites were detected and characterized, including 50, 47 and 43 metabolites for 5-CQA, 4-CQA and 3-CQA, orderly. Moreover, the network pharmacology study indicated that these three isomeric constituents and their major metabolites with similar in vivo metabolic pathways exerted anti-inflammatory effects through co-owned 20 biological processes, which involved 10 major signal pathways and 159 potential targets. Our study shed light on the similarities and differences of the metabolic profiling and anti-inflammatory activity among these three isomeric constituents and set an example for the further researches on the active mechanism of isomeric constituents existing in TCMs based on comparative metabolism study.

18.
Article in Chinese | WPRIM | ID: wpr-879160

ABSTRACT

Based on the heat-clearing and detoxifying effects of Gentianae Radix et Rhizoma, the network pharmacology is mainly used to predict the potential targets of Gentianae Radix et Rhizoma for anti-inflammatory activity and to perform the experimental verification. A method for detecting the biological potency of Gentianae Radix et Rhizoma based on verifiable targets has been established to provide a reference for improving the quality evaluation and control standards of Gentianae Radix et Rhizoma. High performance liquid chromatography can be used to construct chemical fingerprints of different batches of Gentianae Radix et Rhizoma. Constructing a component-target-disease network of Gentianae Radix et Rhizoma for its anti-inflammatory activity was applied to screen potential anti-inflammatory components and related targets of Gentianae Radix et Rhizoma, and to verify the target of Gentianae Radix et Rhizoma by using biological evaluation methods. Detecting the biological potency of different batches of Gentianae Radix et Rhizoma extracts was used to inhibit COX-2 enzyme activity based the verifiable target cyclooxygenase-2(COX-2). The results showed that different batches of Gentianae Radix et Rhizoma accorded with the pharmacopoeia testing regulations, and the chemical fingerprints have a high similarity(similarity>0.93), suggesting that there is no significant difference in the characteristics of the chemical components. Based on network pharmacology predictions, 18 candidate targets were found to have potential direct interactions with the ingredients in Gentianae Radix et Rhizoma. Among them, the most important target is COX-2. Based on the experimental verification of recombinant human COX-2 protease activity inhibition, Gentianae Radix et Rhizoma can inhibit the COX-2 enzyme activity in a dose-dependent manner. It can function with a low concentration(0.75 mg·mL~(-1)), which preliminarily confirmed the accuracy of network pharmacology prediction. The biological potency detection method of Gentianae Radix et Rhizoma based on COX-2 inhibitory activity was optimized and established. The qualitative response parallel line method was used to calculate the biological potency of anti-inflammatory activity, which ranged from 23.04 to 46.60 U·mg~(-1). For network pharmacology prediction, it can screen and clarify the possible targets of traditional Chinese medicine rapidly, which can guide the establishment of a biological evaluation method for the quality of medicinal materials with related activities. Compared with chemical fingerprints, the biological potency testing can better detect quality fluctuations of traditional Chinese medicine.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Biological Assay , Drugs, Chinese Herbal/pharmacology , Humans , Medicine, Chinese Traditional , Quality Control , Rhizome
19.
Article in Chinese | WPRIM | ID: wpr-877548

ABSTRACT

OBJECTIVE@#To observe the effect of electroacupuncture (EA) at sensitized acupoints on choline acetyltransferase positive (ChAT@*METHODS@#A total of 79 male SD rats were randomized into five groups, i.e. a normal group (20 rats), a normal plus sensitized acupoint group (5 rats), a model group (34 rats), an EA@*RESULTS@#The EB extravasating areas were distributed in the segments from T@*CONCLUSION@#The segmental dominance (acupoints) from T


Subject(s)
Acupuncture Points , Animals , Cholinergic Neurons , Colon , Electroacupuncture , Male , Rats , Rats, Sprague-Dawley
20.
Article in Chinese | WPRIM | ID: wpr-847189

ABSTRACT

BACKGROUND: Studies have found that exercise can regulate neuroinflammation and adult hippocampal neurogenesis, and improve cognitive function. However, the interaction between exercise and neuroinflammation-induced changes in hippocampal neurogenesis and cognitive function is unclear. OBJECTIVE: To analyze and summarize the mechanism by which neuroinflammation-mediated exercise improves adult hippocampus neurogenesis and cognition. METHOD: Using “exercise; neuroinflammation; neurogenesis; Alzheimer’s disease; aging; depression; cerebral ischemia; traumatic brain injury; cognition” as keywords, we retrieved literature regarding the effects or mechanisms of exercise on neuroinflammation, adult hippocampus neurogenesis and cognition in CNKI and Web of Science, and logically analyzed and summarized the included studies. RESULTS AND CONCLUSION: Neuroinflammation can cause nerve damage, and may lead to cognitive impairment, while exercise can effectively produce anti-inflammatory effects in the brain, and promote adult hippocampal neurogenesis, thereby improving cognitive ability. Exercise cannot only directly increase the expression of neurotrophic factors in the hippocampus and promote hippocampal neurogenesis, but also affect the expression of neurotrophic factors in the hippocampus and the process of neurogenesis through its anti-inflammatory mechanism. However, there is still much work to be done to better understand how the neurogenic and inflammatory environment changes under exercise conditions, and how this altered process can be modulated to promote cognition.

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