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1.
Organ Transplantation ; (6): 219-2022.
Article in Chinese | WPRIM | ID: wpr-920852

ABSTRACT

Objective To evaluate the effect of coagulation function changes on the incidence of acute kidney injury (AKI) after liver transplantation. Methods Clinical data of 245 liver transplant recipients who met the inclusion and exclusion criteria were retrospectively analyzed. According to the incidence of AKI after liver transplantation, all recipients were divided into the AKI group (n=99) and non-AKI group (n=146). The incidence of AKI after liver transplantation was summarized. Perioperative parameters of the recipients were collected. The risk factors of AKI after liver transplantation were assessed by univariate and multivariate analysis. Results Among 245 recipients undergoing liver transplantation, 99 cases developed AKI after operation with an incidence rate of 40.4%. Preoperative serum creatinine levels of the recipients and the in-hospital fatality were relatively high in the AKI group (all P < 0.05). Compared with the recipients in the non-AKI group, those in the AKI group presented with significantly higher liver function parameters within postoperative 24 h, significantly decreased levels of stage Ⅱ coagulation parameters including coagulation factorsⅤ, Ⅶ, Ⅸ, Ⅹ, Ⅻ and protein S, protein C and antithrombin Ⅲ, evidently elevated prothrombin time international normalized ratio (PT-INR), remarkably increased stage Ⅲ coagulation parameters including D-dimer and fibrin degradation product (FDP) levels and considerably decreased fibrinogen (FIB) level (all P < 0.05). Thrombelastogram showed that the R value was increased, the α angle was decreased and the coagulation time was prolonged in the AKI group (all P < 0.05). Logistic regression analysis demonstrated that the increased R value of postoperative thrombelastogram [odd ratio (OR) 1.116, 95% confidence interval (CI) 1.018-1.223, P=0.019], and decreased levels of antithrombin Ⅲ (OR 0.974, 95%CI 0.955-0.993, P=0.007) were the independent risk factors of incidence of AKI after liver transplantation. Conclusions The incidence of AKI after liver transplantation is high, which is associated with the coagulation function changes of the recipients. Decreased coagulation factor activity (increased R value) and declined antithrombin Ⅲ level are the independent risk factors of AKI in liver transplantat recipients.

2.
Article in Chinese | WPRIM | ID: wpr-920658

ABSTRACT

@#Topical preparations for skin, including the commonly used dosage forms of ointments, creams, gels, patches and plasters, are convenient and can avoid the first-pass effect of drugs.Rheological study, which describes the flow characteristics and mechanical properties of products relevant to their Critical Quality Attributes, has become the main focus for topical preparations.Liquid and solid behaviors of products are usually investigated via steady rheology as well as dynamic rheology.This article reviews the research on topical preparations for skin and the data analysis models based on two rheological methods, aiming to provide some references for the rheological evaluation of topical preparations.

3.
Frontiers of Medicine ; (4): 594-607, 2021.
Article in English | WPRIM | ID: wpr-888746

ABSTRACT

Psoraleae Fructus (PF) is a well-known traditional herbal medicine in China, and it is widely used for osteoporosis, vitiligo, and other diseases in clinical settings. However, liver injury caused by PF and its preparations has been frequently reported in recent years. Our previous studies have demonstrated that PF could cause idiosyncratic drug-induced liver injury (IDILI), but the mechanism underlying its hepatotoxicity remains unclear. This paper reports that bavachin isolated from PF enhances the specific stimuli-induced activation of the NLRP3 inflammasome and leads to hepatotoxicity. Bavachin boosts the secretion of IL-1β and caspase-1 caused by ATP or nigericin but not those induced by poly(I:C), monosodium urate crystal, or intracellular lipopolysaccharide. Bavachin does not affect AIM2 or NLRC4 inflammasome activation. Mechanistically, bavachin specifically increases the production of nigericin-induced mitochondrial reactive oxygen species among the most important upstream events in the activation of the NLRP3 inflammasome. Bavachin increases the levels of aspartate transaminase and alanine aminotransferase in serum and hepatocyte injury accompanied by the secretion of IL-1β via a mouse model of lipopolysaccharide-mediated susceptibility to IDILI. These results suggest that bavachin specifically enhances the ATP- or nigericin-induced activation of the NLRP3 inflammasome. Bavachin also potentially contributes to PF-induced idiosyncratic hepatotoxicity. Moreover, bavachin and PF should be evaded among patients with diseases linked to the ATP- or nigericin-mediated activation of the NLRP3 inflammasome, which may be a dangerous factor for liver injury.


Subject(s)
Adenosine Triphosphate , Animals , Chemical and Drug Induced Liver Injury/etiology , Flavonoids , Humans , Inflammasomes , Mice , NLR Family, Pyrin Domain-Containing 3 Protein , Nigericin
4.
Article in Chinese | WPRIM | ID: wpr-888154

ABSTRACT

Magnoliae Officinalis Cortex(Houpo) can treat peptic ulcer disease(PUD), the mechanism of which remains unclear. In this study, network pharmacology and molecular docking were employed to predict the mechanism of Houpo in the treatment of PUD. Through literature review and TCMSP screening, 15 main active ingredients were obtained. The SwissTargetPrediction database was used to predict the potential targets of the ingredients, and Therapeutic Target Database(TTD), DrugBank, and Human Phenotype Ontology(HPO) to screen the disease-related targets. A total of 49 potential targets were obtained by the intersection of active ingre-dients-related targets and disease-related targets. Cytoscape 3.6.1 was employed to construct the protein-protein interaction network for the targets with high confidence(score>0.700) screened out by STRING. The DAVID database was used for GO and KEGG pathway enrichment of potential targets. GO enrichment analysis showed that the treatment mechanism was mostly related to nuclear receptor activity, ligand-activated transcription factor activity, and G protein-coupled acetylcholine receptor activity. KEGG enrichment analysis found that Houpo could regulate material metabolism, endocrine system, p53 signaling pathway, and PPAR signaling pathway. Molecu-lar docking verified that all 15 ingredients had good binding activities with key targets(CHRM1, CHRM2, FABP1, mTOR, and STAT3). The results mean that Houpo can treat PUD by participating in cell metabolism, inhibiting inflammatory cytokines, and regulating cell proliferation and apoptosis.


Subject(s)
Drugs, Chinese Herbal , Humans , Molecular Docking Simulation , Peptic Ulcer , Protein Interaction Maps , Receptor, Muscarinic M1 , Signal Transduction
5.
Article in Chinese | WPRIM | ID: wpr-888112

ABSTRACT

Twenty-six compounds, including sixteen meroterpenoids(1-16), a triterpenoid(17), four terpenoid derivatives(18-21), and five aromatic compounds(22-26), were isolated from the leaves of Psidium guajava. Their structures were identified by spectroscopic analyses including NMR and MS. Compounds 21-26 were obtained from plants of Psidium for the first time. Based on the structure,(R)-2-ethylhexyl 2H-1,2,3-triazole-4-carboxylate(24 a), an α-glucosidase inhibitor recently isolated from Paramignya trimera, should be revised as compound 24. Meroterpenoids 1-16 were evaluated for their antitumor and antifungal activities. Meroterpenoids psiguajadial D(4), guapsidial A(5), 4,5-diepipsidial A(7), guadial A(14), and guadial B(15) showed cytotoxicities against five human tumor cell lines(HL-60, A-549, SMMC-7721, MCF-7, and SW-480), among which 5 was the most effective with an IC_(50) of 3.21-9.94 μmol·L~(-1).


Subject(s)
Antifungal Agents/pharmacology , Humans , Magnetic Resonance Spectroscopy , Plant Extracts , Plant Leaves , Psidium , Terpenes
6.
China Pharmacy ; (12): 2458-2466, 2021.
Article in Chinese | WPRIM | ID: wpr-887425

ABSTRACT

OBJECTIVE:To discuss the inhibitory effect of lanthanum chloride on the calcification of vascular smooth muscle cells(VSMCs)induced by high phosphorus and its mechanism. METHODS :On the basis of screening the action concentration and time of lanthanum chloride by MTT method ,human VSMCs were divided into control group (1 mmol/L phosphorus solution ), lanthanum chloride high concentration control group (1 mmol/L phosphorus solution+ 60 μmol/L lanthanum chloride),model group (3 mmol/L phosphorus solution ),sodium chloride group (3 mmol/L phosphorus solution+ 180 μmol/L sodium chloride),nuclear factor κB(NF-κB)signaling pathway agonist+lanthanum chloride group (3 mmol/L phosphorus solution+ 1 μg/mL lipopolysaccharide+ 60 μmol/L lanthanum chloride),positive control group (3 mmol/L phosphorus solution+ 100 μmol/L sodium pyrophosphate),and lanthanum chloride low ,medium,and high concentration groups (3 mmol/L phosphorus solution+ 15,30,60 μmol/L lanthanum chloride). Alizarin red S staining and Von Kossa staining were used to detect cell calcification in each group after treated with phosphorus solution for 6 d and relevant medicine for 2 d. Western blot assay was used to detect the protein expression of TNF-α receptor associated protein 6(TRAF6),nuclear factor κB inhibitor protein α(IκBα),NF-κB p65,bone morphogenetic protein 2 (BMP-2),smooth muscle 22 α(SM22α)and Runt related transcription factor 2(Runx2). Real-time fluorescence quantitative polymerase chain reaction was used to detect mRNA expression of TRAF 6,IκBα,BMP-2,SM22α and Runx2. RESULTS : Compared with control group ,no cell calcification was observed in the lanthanum chloride high concentration control group ,while obvious cell calcification and significant increase of OD value were observed in model group and sodium chloride group (P< 0.01);protein and mRNA expression of TRAF 6 and BMP- 2 in cytoplasm as well as mRNA expression of Runx 2,protein expression of NF-κB p65 and Runx 2 in nucleus were significantly increased (P<0.01);protein and mRNA expression of IκBα and SM22α as well as protein expression of NF-κB p65 in cytoplasm were significantly decreased (P<0.01). Compared with model group,cell calcification was significantly improved in lanthanum chloride groups and positive control group ,while OD values were significantly reduced ;the expression levels of the above-mentioned protein and mRNA were reversed to varying degrees (P<0.05 or P<0.01). Compared with lanthanum chloride high concentration group ,obvious cell calcification was observed in NF-κB signaling pathway agonist + lanthanum chloride group ,and OD value was significantly increased ;the above indexes were significantly reversed in cytoplasm and nucleus (P<0.05 or P<0.01). CONCLUSIONS :Lanthanum chloride can inhibit the calcification of VSMCs induced by high phosphorus ,and its mechanism may be related to the inhibition of NF-κB signaling pathway activation.

7.
China Pharmacy ; (12): 2085-2090, 2021.
Article in Chinese | WPRIM | ID: wpr-886743

ABSTRACT

OBJECTIVE:To establish the fingerprint of Adiantum capillusveneris from different producing areas ,and to conduct chemometric analysis and content determination of differential components ,so as to provide reference for quality control of A. capillusveneris . METHODS :HPLC-DAD combined with Similarity Evaluation System of TCM Chromatogramtic Fingerprint (2004 A edition )were used to establish fingerprint of 19 batches of A. capillusveneris from different producing areas (S1-S19). Common peaks were confirmed and their similarities were evaluated. Chemometric analysis methods such as cluster analysis , principle component analysis (PCA),orthogonal partial least squares discriminant analysis (OPLS-DA)were used to evaluate the quality of 19 batches of A. capillusveneris from different producing areas ,screen the differential components ,and determine the contents of some differential components. RESULTS :Among 19 batches of A. capillusveneris from different producing areas ,22 common peaks were confirmed ;peak 9 was chlorogenic acid ,peak 17 was quercetin- 3-O-β-D-glucopyranoside,peak 20 was kaempferol-3-O-rutoside;the similarity of 19 batches of sample were 0.677-0.962. Through cluster analysis ,it was found that S 7 and S 10 were clustered into one category ;S15 and S 18 were clustered into one category ;and S 1-S6,S8,S9,S11-S14,S16,S17 and S 19 were clustered into one category. PCA and OPLS-DA found that S 7 and S 10 were clustered into one category ;S15 were clustered into one category ;S18 were clustered into one category ;S1-S6,S8,S9,S11-S14,S16,S17 and S 19 were clustered into one category. Chlorogenic acid ,quercetin-3-O-β-D-glucopyranoside,kaempferol-3-O-rutoside and chemical composition represented by peak 14 were the differential components of the〔2017〕2841); medicinal material. Among 19 batches of A. capillusveneris , average contents of chlorogenic acid and quercetin- 3-O-β-D- glucopyranoside and kaempferol- 3-O-rutoside were 0.10-4.25, 0.31-7.11,0.61-12.00 mg/g,respectively. CONCLUSIONS : 电话:0851-86614212。 HPLC-DAD fingerprints of A. capillusveneris from different producing areas are establishe d in the study ,and three common peaks are identified. Four differential components affecting the quality of A. capillusveneris are screened , and the contents of chlorogenic acid , quercetin-3-O-β-D-glucopyranoside and kaempferol-3-O-rutoside in A. capillusveneris from different producing areas were significantly different.

8.
Article in Chinese | WPRIM | ID: wpr-879624

ABSTRACT

OBJECTIVE@#To explore the genetic basis for a patient with tuberous sclerosis complex.@*METHODS@#Genomic DNA was extracted from peripheral blood samples from members of his family and 100 unrelated healthy controls. The proband was subjected to next-generation sequencing, and candidate variant was confirmed by multiple ligation-dependent probe amplification (MLPA) and Sanger sequencing. Reverse transcription-PCR (RT-PCR) was carried out to determine the relative mRNA expression in the proband.@*RESULTS@#The patient was found to harbor a c.2355+1G>C splicing variant of the TSC2 gene. Sequencing of cDNA confirmed that 62 bases have been inserted into the 3' end of exon 21, which has caused a frameshift producing a truncated protein.@*CONCLUSION@#The novel splicing variant c.2355+1G>C of the TSC2 gene probably underlay the TSC in the proband. Above finding has expanded the variant spectrum of TSC2 and provided a basis for preimplantation genetic testing and/or prenatal diagnosis.


Subject(s)
Female , Humans , Mutation , Pregnancy , RNA Splicing/genetics , Tuberous Sclerosis/genetics , Tuberous Sclerosis Complex 1 Protein/genetics , Tuberous Sclerosis Complex 2 Protein/genetics
9.
Article in Chinese | WPRIM | ID: wpr-879429

ABSTRACT

OBJECTIVE@#To explore the effects of low-frequency electroacupuncture combined with aerobic exercise on sarocopenia, and the effects of IGF-I /Akt and its downstream signaling pathway-related protein.@*METHODS@#Naturally aging SD rats were used as research objects. Thirty-two 6-month-old male SD rats weighing 400 to 450 g were bred to 12-month-old and randomly divided into 4 groups according to body weight:Control group(YC, only grasp, fix, put back, without other intervention), electroacupuncture group (YA, electroacupuncture intervention), exercise group (YE, exercise intervention) and electroacupuncture+exercise group (YEA, electroacupuncture combined with exercise intervention). SD rats were continuously intervened from 12 months to 18 months of age. At the end of the experiment, the conditions of naturally aging rats in each group were observed:skeletal muscle wet weight / weight ratio;HE staining morphology of soleus muscle under light microscope; qPCR was used to detect the expression level of IGF-I mRNA in skeletal muscle;the expression of AKT, mTOR, p70S6K and p-p70S6K proteins in rat gastrocnemius was determined by Western blot.@*RESULTS@#In 18-month-old rats, the intervention period was 6 months. (1) Compared with YC group, YA group and YEA group significantly increased the wet weight / body weight ratio of gastrocnemius muscle in 18 months old rats. YEA group could significantly increase the wet weight / body weight ratio of soleus muscle compared with YC group YC group and YA group (@*CONCLUSION@#Electroacupuncture combined with aerobic exercise can attenuate sarocopenia in 18-month-old naturally aging rats. The molecular mechanism may be related to the promotion of protein synthesis by activating the IGF-I / Akt pathway.


Subject(s)
Aging , Animals , Electroacupuncture , Exercise , Insulin-Like Growth Factor I/genetics , Male , Muscle, Skeletal , Proto-Oncogene Proteins c-akt/genetics , Rats , Rats, Sprague-Dawley
10.
Article in Chinese | WPRIM | ID: wpr-922001

ABSTRACT

OBJECTIVE@#To explore the genetic basis for a pedigree affected with Nance-Horan syndrome.@*METHODS@#Clinical manifestation of the patients was analyzed. Genomic DNA was extracted from peripheral blood samples of the pedigree members and 100 unrelated healthy controls. A panel of genes for congenital cataract was subjected to next-generation sequencing (NGS), and candidate variant was verified by Sanger sequencing and bioinformatic analysis based on guidelines of American College of Medical Genetics and Genomics (ACMG). mRNA expression was determined by reverse transcriptase-PCR (RT-PCR). Linkage analysis based on short tandem repeats was carried out to confirm the consanguinity.@*RESULTS@#A small insertional variant c.766dupC (p.Leu256Profs*21) of the NHS gene was identified in the proband and his affected mother, but not among unaffected members and the 100 healthy controls. The variant was unreported in Human Gene Mutation Database (HGMD) and other databases. Based on the ACMG guideline, the variant is predicted to be pathogenic (PVS1+PM2+PM6+PP4).@*CONCLUSION@#The novel variant c.766dupC of the NHS gene probably underlay the X-linked dominant Nance-Horan syndrome in this pedigree.


Subject(s)
Cataract/genetics , Genetic Diseases, X-Linked , Humans , Mutation , Pedigree , State Medicine , Tooth Abnormalities
11.
China Pharmacy ; (12): 213-219, 2021.
Article in Chinese | WPRIM | ID: wpr-862646

ABSTRACT

OBJECTIVE:To stud y the correlatio n between the contents of active ingredients and the color of Morus alba ,to establish fingerprint and conduct cluster analysis of samples from different producing areas ,so as to provide reference for its quality control and evaluation. METHODS :HPLC and HCl-Mg reaction colorimetry were used to determine the contents of morusin and total flavonoids in M. alba . The color of M. alba was observed by naked eye ,and chromaticity values (L*,a*,b*) were measured by color difference meter and color aberration (E*ab)were calculated. Pearson correlation of the contents of morusin and total flavonoids with color indicators (L*,a*,b*,E*ab)were analyzed by SPSS 21.0 software. HPLC method was used to establish the fingerprint of 20 batches of M. alba from 3 different producing areas ,and the similarity analysis was carried out. K-means cluster analysis (based on the contents of morusin and total flavonoids and corlor index )and hierarchical cluster analysis (based on relative peak area of common peaks in fingerprint )were performed for 20 batches of samples by SPSS 21.0 software. RESULTS:The average contents of morusin and total flavonoids in M. alba were 0.096 0-0.618 6 mg/g,0.48%-1.51%,which were significantly correlated with each color index (P<0.01). The smaller L*,b*,E*ab and the larger a*were,the higher the content of morusin was ;the higher the value of L*,b*,E*ab and the smaller the value of a*were,the higher the content of total flavonoids was. The similarity between the fingerprints of 20 batches of samples and the control ranged from 0.883 to 0.983;13 common peaks were demarcated ,and No. 1 peak was identified as chlorogenic acid. K-means cluster analysis showed that 20 batches of samples could be divided into 2 categories. Category Ⅰ were mainly from Anhui province with higher content of morusin,lower content of total flavonoids ,darker and yellowish brown color ;category Ⅱ were mainly from Sichuan province and Guizhou province ,with lower content of morusin ,higher content of total flavonoids ,lighter and yellowish white color. The results of hierarchical cluster analysis were consistent with the results. CONCLUS IONS:The color of M. alba is closely related to the contents of morusin and total flavonoids. The content of morusin in yellow-brown M. albais is higher ,while the content of total flavonoids in yellow-white M. albais is higher.

12.
Acta Pharmaceutica Sinica ; (12): 585-592, 2021.
Article in Chinese | WPRIM | ID: wpr-873768

ABSTRACT

Puerarin (PUE), as an isoflavone component, has a wide range of pharmacological activities, while its poorly aqueous solubility limits the development of solid oral dosage forms. In this study, PUE along with nicotinamide (NIC) were prepared into the coamorphous system by solvent-evaporation method and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). In addition, its dissolution behavior and solubilization mechanism were also investigated. PUE-NIC coamorphous was a single homogeneous binary system, with a single glass transition temperature at 35.1 ℃. In comparison to crystalline PUE, during the dissolution process, coamorphous PUE-NIC not only exhibited the "liquid-liquid phase separation" (LLPS) phenomenon, but the formation of Ap type complexation (1∶1 and 1∶2) between PUE and NIC molecules was also verified, which significantly improved the solubility of PUE and prolonged the supersaturation time, and would benefit its absorption.

13.
Article in Chinese | WPRIM | ID: wpr-873578

ABSTRACT

@#Lenvatinib mesylate (LF), a multi-target tyrosinase inhibitor mainly used in the treatment of a variety of cancers, has low oral bioavailability mainly due to its gelation during the dissolution process. In the current study, in order to enhance dissolution and eliminate gelation of LF, a supramolecular coamorphous system of LF-baicalein (BAI) (molar ratio, 1∶1) was prepared by rotary evaporation and characterized by PLM, PXRD, DSC and FTIR. Results indicated the formation of coamorphous system with a single Tg of 118 °C. Different from original LF crystal, no gelation phenomenon was observed during the dissolution of coamorphous LF-BAI. In addition, the dissolution rate of LF was increased by 2.2-fold after coamorphization. Meanwhile, the dissolution rate of the co-former BAI was also enhanced by more than 25.4-fold. Stability test showed that the prepared coamorphous system had a good physical stability for at least 90 days under 25 °C/ 60%RH and 40 °C /75%RH conditions.

14.
Acta Pharmaceutica Sinica ; (12): 266-273, 2021.
Article in Chinese | WPRIM | ID: wpr-872628

ABSTRACT

Xianling Gubao is a common and effective medicine in the treatment of orthopedic diseases. In recent years, it has been reported to be associated with liver injury. However, through the analysis of the adverse drug reaction reports and key hospital cases, we found that there is considerable incomplete information in the reports of Xianling Gubao-related liver injury cases retrieved from the literature. Thus, it is difficult to accurately judge causality between the drug and liver injury. Six cases of liver injury related to Xianling Gubao were identified in key hospitals, two of which achieved the clinical diagnosis according to the assessment of the integrated evidence chain method. We further analyzed the public health data of all residents in Yinzhou. The gross incidence rate of Xianling Gubao-related liver injury was 0.034%, which corresponds to a level of rare incidence. This revealed that Xianling Gubao-related liver injury has significant divergence in individuals and an idiosyncratic nature. The gross incidence of liver injury related to Xianling Gubao was lower than that of other medicines for the treatment of orthopedic diseases. Based on the idiosyncratic drug-induced liver injury model mediated by immune stress, it was found that Epimedii Folium and Psoraleae Fructus were the major components that lead to liver injury, and the liver injury caused by a full prescription was less serious than that encountered with only Epimedii Folium and Psoraleae Fructus. This suggests that the other 4 herbs (Dipsaci Radix, Anemarrhenae Rhizoma, Rehmanniae Radix,Salviae Miltiorrhizae Radix et Rhizoma) can prevent/alleviate the liver injury. Through disassembled prescription analysis, we found that the attenuation efficacy of Salviae Miltiorrhizae Radix et Rhizoma was the most significant. In conclusion, Xianling Gubao may cause idiosyncratic liver injury in a tiny minority of susceptible individuals, but the incidence risk is lower than that of other commonly used drugs for orthopedic disease. Xianling Gubao should be discreetly applied to patients with immune stress. The major components that induced liver injury in Xianling Gubao were Epimedii Folium and Psoraleae Fructus, and Salviae Miltiorrhizae Radix et Rhizoma appears to attenuate this toxicity. This study provides a reference for the rational clinical medication with Xianling Gubao.

15.
Article in Chinese | WPRIM | ID: wpr-878698

ABSTRACT

Objective To compare the differences of energy spectrum CT between small cell lung cancer(SCLC)with mediastinal lymph node metastasis and mediastinal sarcoidosis.Methods Twenty-five SCLC patients with mediastinal lymph node metastasis(SCLC group)and 26 patients with mediastinal sarcoidosis(sarcoidosis group)confirmed by bronchoscopy and biopsy in Tangshan People's Hospital from January 2018 to June 2019 were selected as the research objects.The CT value,iodine concentration,water concentration and energy spectrum curve slope under different single energy levels were compared between SCLC group and sarcoidosis group.Results The single-energy CT values of 40-80 keV segments in the arterial phase of the SCLC group were significantly higher than those in the sarcoidosis group(all P 0.05).The single-energy CT values of 40-90 keV segments in venous phase of the SCLC group were significantly higher than those of the sarcoidosis group(all P 0.05).The concentrations of iodine in the arterial phase and venous phase of the SCLC group were(11.56±4.06)μg/cm


Subject(s)
Humans , Lung Neoplasms/diagnostic imaging , Lymph Nodes , Lymphatic Metastasis , Sarcoidosis/diagnostic imaging , Small Cell Lung Carcinoma/diagnostic imaging , Tomography, X-Ray Computed
16.
Article in Chinese | WPRIM | ID: wpr-905918

ABSTRACT

Cerebral ischemia/reperfusion injury (CIRI) is a common feature and the main pathophysiological mechanism of ischemic stroke(IS), which is caused by a blood reperfusion injury in ischemic brain tissues. It can aggravate brain tissue injury and cause irreversible brain damage, seriously affecting the quality of life or even the life of patients. Hence, we must find out the exact mechanism as well as the effective therapeutic drugs and targets for CIRI. The Chinese medicine effective in Xingnao (restoring consciousness) and Kaiqiao (opening orifices) has been widely used in the treatment of CIRI and serves as a classic therapy for IS. In recent years, scholars have conducted extensive and in-depth studies on the mechanism and therapeutic targets of Chinese medicine in Xingnao and Kaiqiao. They found that those drugs could interfere with a series of changes after IS and achieve the remarkable curative effect. This study summarized the effect and mechanism of Chinese medicine in Xingnao and Kaiqiao in the treatment of CIRI, including reducing the inflammatory response and oxidative stress, alleviating brain edema and the toxicity of excitatory amino acids, reducing cell apoptosis, promoting angiogenesis and neurovascular remodeling, and improving blood-brain barrier injury. It is expected to provide references to clarify the mechanism and important targets of those drugs in resisting CIRI and ideas for the in-depth investigation and application of brain protection of Chinese medicine in Xingnao and Kaiqiao.

17.
Article in Chinese | WPRIM | ID: wpr-905862

ABSTRACT

Objective:To investigate the effect of Astragalus polysaccharide (APS) on transforming growth factor-<italic>β</italic><sub>1</sub> (TGF-<italic>β</italic><sub>1</sub>)-induced epithelial mesenchymal transition (EMT) of A549/DDP lung adenocarcinoma xenograft and its potential molecular mechanism. Method:BALB/c nude mice were randomly divided into the non-loading group (A549/DDP cells not loaded with TGF-<italic>β</italic><sub>1</sub>), model group, cisplatin group, and combined group (A549/DDP cells overexpressing TGF-<italic>β</italic><sub>1</sub>). Mice in the combined group were treated with intragastric administration of APS (0.3 g·kg<sup>-1</sup>·d<sup>-1</sup>) and intraperitoneal injection of cisplatin (0.003 5 g·kg<sup>-1</sup>), while those in the cisplatin group only received intraperitoneal injection of cisplatin (0.003 5 g·kg<sup>-1</sup>). After drug intervention, the nude mice were sacrificed and the xenograft and lung were harvested, followed by the weighing of tumor and the calculation of the inhibition rate. The number of tumors metastasizing to the lung was counted under the microscope. The pathological features of tumors and their metastasis to the lung tumor were observed by hematoxylin-eosin (HE) staining. The protein and mRNA expression levels of EMT molecular markers E-cadherin, Vimentin, <italic>α</italic>-smooth muscle actin (<italic>α</italic>-SMA), and phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) in the xenograft were detected by immunohistochemistry, Western blot, and Real-time polymerase chain reaction (Real-time PCR). Result:Compared with the non-loading group, the model group exhibited increased tumor weight and pulmonary metastatic nodules (<italic>P</italic><0.05), sparse tumor cell junctions, long spindle cells, massive metastatic nodules in the lung, down-regulated E-cadherin protein and mRNA expression, and up-regulated Vimentin and <italic>α</italic>-SMA protein and mRNA expression and p-PI3K and p-Akt protein expression (<italic>P</italic><0.05). Compared with the model group and cisplatin group, the combined group displayed decreased tumor weight and pulmonary metastatic nodules (<italic>P<</italic>0.05), tight tumor cell junctions, round or oval cells, no obvious lung metastasis, up-regulated E-cadherin protein and mRNA expression (<italic>P</italic><0.05), and down-regulated Vimentin and <italic>α</italic>-SMA protein and mRNA expression (<italic>P</italic><0.05) and p-PI3K and p-Akt protein expression (<italic>P</italic><0.05). There was no significant difference in PI3K or Akt protein expression among groups. Conclusion:APS has a certain inhibitory effect against EMT in lung adenocarcinoma A549/DDP cells, which may be related to the inhibition of activated PI3K/Akt protein expression.

18.
Journal of Clinical Hepatology ; (12): 1053-1058., 2021.
Article in Chinese | WPRIM | ID: wpr-876645

ABSTRACT

ObjectiveTo investigate the clinical effect of entecavir (ETV) rescue treatment in chronic hepatitis B (CHB) patients at the onset of rtA181V/T mutation. MethodsA total of 174 CHB patients who were treated in the outpatient and inpatient departments of The Affiliated Hospital of Xuzhou Medical University from January 2012 to January 2017 and underwent the detection of drug-resistance mutations of the genes in the reverse transcription (RT) polymerase region were enrolled, among whom there were 72 previously untreated patients and 102 treatment-experienced patients with virological breakthrough or poor response. The association between the previous medication history of nucleos(t)ide analogues and the mutation pattern (including rtA181V/T) was evaluated in the treatment-experienced CHB patients. A total of 155 patients were enrolled, among whom 72 patients had no drug-resistance mutations, 45 had rtA181V/T mutation, and 38 had rtA181V/T+rtN236T mutation. The three groups were compared in terms of virologic response and biochemical parameters at baseline and at weeks 24 and 48 of ETV rescue treatment. The t-test was used for comparison of normally distributed continuous data between two groups, and a one-way analysis of variance was used for comparison between multiple groups; the Kruskal-Wallis H test was used for comparison between multiple groups. The chi-square test was used for comparison of categorical data between two groups. A logistic regression analysis was used to screen out the influencing factors for poor prognosis. ResultsA analysis of the previous medication history of NAs and the mutation patterns for all patients suggested that the patients with the medication history of multiple NAs tended to have multisite mutations and multi-drug resistance (χ2=4295, P<0.05). The level of HBV DNA at the time of virological breakthrough was lower than that at the time of initial administration of NAs in the rtA181V/T mutation group [(6.22±1.48) log10 IU/ml vs (7.08±1.59) log10 IU/ml, t=3.098, P=0.002] and the rtA181V/T+rtN236T mutation group [(5.94±1.45) log10 IU/ml vs (6.94±1.61) log10 IU/ml,t=2.850, P=0.004]. At week 48 of ETV rescue treatment, there were no significant differences between the three groups in HBV DNA negative conversion rate (83.3% vs 82.2% vs 81.6%, P>0.05) and HBeAg negative conversion rate (22.2% vs 17.8% vs 21.1%, P>0.05), and there were also no significant differences in alanine aminotransferase normalization rate (77.1% vs 85.2% vs 83.3%, P>0.05), aspartate aminotransferase normalization rate (80.4% vs 75.9% vs 76.0%, P>0.05), and total bilirubin normalization rate (80.8% vs 79.3% vs 78.1%, P>0.05). HBV DNA level at the beginning of ETV treatment was the risk factor for the treatment outcome of 48-week antiviral therapy (odds ratio = 1.655, 95% confidence interval: 1.128-2.428, P=0.01). ConclusionETV has a good antiviral effect in treatment-experienced CHB patients with rtA181 drug-resistance mutation, and HBV DNA level at the initiation of ETV treatment can predict the outcome of 48-week ETV rescue treatment.

19.
Acta Pharmaceutica Sinica ; (12): 855-864, 2021.
Article in Chinese | WPRIM | ID: wpr-876517

ABSTRACT

Compared with crystalline drugs, their amorphous forms present long-range disordered molecular arrangements, and often exhibit higher apparent solubility and dissolution. However, several small molecule amorphous drugs may exhibit gelation phenomenon during the dissolution process, and show abnormal dissolution behavior with significantly lower dissolution than crystalline drugs. The current study aims to discover the relationship between the gelation of amorphous drugs and their abnormal dissolution, and further explore the internal gelation mechanism. Amorphous simvastatin (SIM), carvedilol (CAR), and irbesartan (IRB) were prepared by melt cooling method and characterized via X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR). Gel formation causes the dissolution of these three amorphous drugs to be significantly lower than their crystalline state. The formed gels were characterized as three-dimensional dense network structures by scanning electron microscope (SEM). Furthermore, amorphous SIM, CAR and IRB showed the critical gel temperature at 8-15 ℃, 25-30 ℃ and 45-50 ℃, and amorphous CAR and IRB showed the critical gel pH at 1 and 0.25. The mechanism of gel formation was proposed to be closely related to the transformation of amorphous drugs into the supercooled liquid state (as the important driving force) and the protonation induced self-assembling under acidic conditions. In addition, the wettability and properties of amorphous drugs also affect the formation of gelation.

20.
Article in Chinese | WPRIM | ID: wpr-887944

ABSTRACT

Drynariae Rhizoma is warm in nature and bitter in taste, mainly acting on liver and kidney systems. It is a common Chinese herbal medicine for the treatment of fracture and bone injury. The chemical compositions of Drynariae Rhizoma mainly include flavonoids, triterpenoids, phenylpropanoids and lignans. At present, modern pharmacological and clinical studies have shown that Drynariae Rhizoma has the effects of anti osteoporosis, promoting fracture healing, kidney protection, anti-inflammatory, promoting tooth growth, preventing and treating aminoglycoside ototoxicity and lowering blood lipid. In addition, the toxicity evaluation experiment of Drynariae Rhizoma has also shown that it has no obvious toxic and side effects. Naringin is a kind of dihydroflavone in Drynariae Rhizoma. Many studies have shown that naringin and other total flavonoids play an important role in anti-osteoporosis, promoting fracture healing, anti-inflammation, promoting tooth growth and lowering blood lipid. In this study, the research progresses on chemical consti-tuents and pharmacological activities of Drynariae Rhizoma in recent years were reviewed, and some mechanisms of action were summarized, to provide references for the further research and development of Drynariae Rhizoma.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Flavonoids , Humans , Osteoporosis/drug therapy , Polypodiaceae , Rhizome
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