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1.
Acta Pharmaceutica Sinica B ; (6): 533-578, 2024.
Artigo em Inglês | WPRIM | ID: wpr-1011275

RESUMO

Epigenetic pathways play a critical role in the initiation, progression, and metastasis of cancer. Over the past few decades, significant progress has been made in the development of targeted epigenetic modulators (e.g., inhibitors). However, epigenetic inhibitors have faced multiple challenges, including limited clinical efficacy, toxicities, lack of subtype selectivity, and drug resistance. As a result, the design of new epigenetic modulators (e.g., degraders) such as PROTACs, molecular glue, and hydrophobic tagging (HyT) degraders has garnered significant attention from both academia and pharmaceutical industry, and numerous epigenetic degraders have been discovered in the past decade. In this review, we aim to provide an in-depth illustration of new degrading strategies (2017-2023) targeting epigenetic proteins for cancer therapy, focusing on the rational design, pharmacodynamics, pharmacokinetics, clinical status, and crystal structure information of these degraders. Importantly, we also provide deep insights into the potential challenges and corresponding remedies of this approach to drug design and development. Overall, we hope this review will offer a better mechanistic understanding and serve as a useful guide for the development of emerging epigenetic-targeting degraders.

2.
Acta Pharmaceutica Sinica ; (12): 2239-2249, 2023.
Artigo em Chinês | WPRIM | ID: wpr-999148

RESUMO

Toll like receptors (TLRs) are the earliest discovered natural immune pattern recognition receptors (PRRs). The abnormality of TLR signal transduction pathway is the key factor leading to chronic inflammatory, cancer, nervous system disease and cardiovascular diseases. The development of TLR agonists and inhibitors has attracted much attention. Currently known TLR2 agonists, such as lipopeptides or their derivatives, have certain limitations in drug development due to their difficult synthesis, easy hydrolysis, and triggering inflammatory cytokine storms, while inhibitors have been rarely reported. New small molecule TLR2 agonists or inhibitors with higher stability are more likely to be developed as tumor immunotherapy or anti-inflammatory drugs.

3.
Acta Pharmaceutica Sinica B ; (6): 3782-3801, 2023.
Artigo em Inglês | WPRIM | ID: wpr-1011153

RESUMO

Toll-like receptor 2 (TLR2) mediated macrophages regulate the protective immune response to infectious microorganisms, but the aberrant activation of macrophages often leads to pathological inflammation, including tissue damage. In this study, we identified antagonists of TLR2 by screening 2100 natural products and subsequently identified Taspine, an aporphine alkaloid, as an excellent candidate. Furthermore, analysis of the 10 steps chemical synthesis route and structural optimization yielded the Taspine derivative SMU-Y6, which has higher activity, better solubility, and improved drug-feasible property. Mechanistic studies and seq-RNA analysis revealed that SMU-Y6 inhibited TLR2 over other TLRs, hindered the formation of TLR2/MyD88 complex, and blocked the downstream NF-κB and MAPK signaling pathway, thus suppressing the release of inflammatory cytokines. SMU-Y6 could stabilize TLR2 and bind to TLR2 protein with a Kd of 0.18 μmol/L. Additionally, SMU-Y6 could efficiently reverse the M1 phenotype macrophage polarization, reduce the production of cytokines as well as infiltration of neutrophiles and alleviate the local inflammation in mice with acute paw edema and colitis. Collectively, we reported the first aporphine alkaloid derivative that selectively inhibits TLR2 with high binding affinity and superior drug-feasible property, thus providing an urgently-needed molecular probe and potential drug candidate for inflammatory and autoimmune disease therapy.

4.
China Journal of Chinese Materia Medica ; (24): 1117-1119, 2021.
Artigo em Chinês | WPRIM | ID: wpr-879011

RESUMO

Based on the investigation of wild medicinal plant resources in Dexing city, Jiangxi province, and the collected plant specimens, which were identified by taxonomy, two new record species of geographical distribution were found, which are Meehania zheminensis A. Takano, Pan Li & G.-H. Xia and Corydalis huangshanensis L.Q.Huang & H.S.Peng. The voucher specimens are kept in Dexing museum of traditional Chinese medicine. In this paper, the new distribution species were reported, which provides valuable information for further enriching and supplementing the species diversity of medicinal plant resources in Jiangxi province.


Assuntos
Humanos , China , Corydalis , Lamiaceae , Medicina Tradicional Chinesa , Museus , Plantas Medicinais
5.
Biomedical and Environmental Sciences ; (12): 123-132, 2020.
Artigo em Inglês | WPRIM | ID: wpr-793014

RESUMO

Objective@#The aim of this study was to update the epidemic situation of dengue fever (DF) and provide new insights for the consideration of disease control in Fujian province, China.@*Methods@#Details about DF cases in Fujian reported during 2004-2017 were collected and analyzed. The envelope (E) genes of isolates of dengue virus (DENV) were sequenced for phylogenetic analysis.@*Results@#The number of imported DF cases had increased dramatically since 2013, and the source regions expanded from Southeast Asia to South Asia, America, Oceania, and Africa, as well as the surrounding provinces. This resulted in local outbreaks and indigenous cases of DF that occurred more frequently, with 10 of 13 local outbreaks and 85.9% (1,252/1,458) of indigenous cases reported in 2013-2017. Compared with only two coastal cities before 2013, four coastal and one inland city in 2013-2017 experienced the local DF outbreaks. The phylogenetic analysis of E genes confirmed that the import of DENV, not only from abroad but also from the surrounding provinces, played an important role in dissemination and local outbreaks of DF in Fujian.@*Conclusions@#The frequent import of DF cases from not only abroad but also the surrounding provinces resulted in increased incidence, frequent local outbreaks, and expansion of distribution in Fujian in recent years. There is a need for urgent measures to improve disease control in this province.

6.
Biomedical and Environmental Sciences ; (12): 829-838, 2020.
Artigo em Inglês | WPRIM | ID: wpr-878347

RESUMO

Objective@#To develop RT-nPCR assays for amplifying partial and complete VP1 genes of human enteroviruses (HEVs) from clinical samples and to contribute to etiological surveillance of HEV-related diseases.@*Methods@#A panel of RT-nPCR assays, consisting of published combined primer pairs for VP1 genes of HEV A-C and in-house designed primers for HEV-D, was established in this study. The sensitivity of each RT-nPCR assay was evaluated with serially diluted virus stocks of five serotypes expressed as CCID @*Results@#The sensitivity of RT-nPCR assays for amplifying partial VP1 gene of HEVs was 0.1 CCID @*Conclusion@#This RT-nPCR system is capable of amplifying the partial and complete VP1 gene of HEV A-D, providing rapid, sensitive, and reliable options for molecular typing and molecular epidemiology of HEVs in clinical specimens.


Assuntos
Humanos , Proteínas do Capsídeo/genética , Enterovirus Humano A/genética , Enterovirus Humano B/genética , Enterovirus Humano C/genética , Enterovirus Humano D/genética , Epidemiologia Molecular/métodos , Tipagem Molecular/métodos , Reação em Cadeia da Polimerase Via Transcriptase Reversa/métodos
7.
Chinese Journal of Disease Control & Prevention ; (12): 911-915,937, 2019.
Artigo em Chinês | WPRIM | ID: wpr-779440

RESUMO

Objective The aim is to analyze the spatial epidemiological characteristics for human infection with avian influenza H7N9 in Fujian Province, so as to provide scientific evidence for developing and adjusting related control strategies. Methods The epidemiological data of human infection with H7N9 avian influenza in Fujian Province, from 2013 to 2017 was analyzed by SAS 9.2, ArcGIS 10.3 and SaTScan 9.4 software.Results There were a total of 108 cases and 28 deaths reported in Fujian Province, up to December 31, 2017. The case fatality rate was 25.93%.96.30% of cases were sporadic. There were more incidences in winters and springs, more incidences in rural areas. The global spatial autocorrelation and high/low clustering analysis indicated that clusters at the county level were in the shore areas (Z=3.74, P<0.001; Z=5.26, P<0.001). The cities of Changle, Fuqing, Jinjiang and Siming were the high-high clustered areas and local hot-points. There were two clusters, from December 2014 to March 2015, the most likely cluster regions was centered around Zhangpu County with a radius of 63.04 km (RR=4.72, LLR=11.41, P<0.001). The secondary cluster regions was centered around Fuqing City with a radius of 81.98 km (RR=4.07, LLR=7.96, P=0.037). Conclusions Human infection with avian influenza H7N9 in Fujian Province is spatially and temporally clustered. The measures of prevention and control should be focused on high incidence seasons and key regions, and the surveillance of etiology should be strengthened.

8.
Chinese Journal of Tissue Engineering Research ; (53): 4693-4699, 2016.
Artigo em Chinês | WPRIM | ID: wpr-495019

RESUMO

BACKGROUND:The limitations of computer technology in the study of bone biomechanics and the prediction of bone fixation strength, stability, fatigue damage and life expectancy are more difficult. OBJECTIVE:To investigate the new progress and application of finite element analysis in orthopedics. METHODS:The first author searched PubMed (http://www.ncbi.nlm.nih.gov/PubMed) and CNKI China journal ful-text database (http://www.cnki.net/) published til November 2015. Key words were“finite element analysis, orthopedics, biomechanics”. There were 51 references in English and 320 Chinese literatures. According to the inclusion criteria, 40 literatures were selected. RESULTS AND CONCLUSION:Biomechanics of human skeleton is very complex, and most of the mechanical state is a locomotive, non-static process, thus increasing the difficulty of orthopedic biomechanics research. The prediction concerning bone fixation strength, stability, fatigue damage and lifetime is more difficult. However, the finite element analysis technology, which has been widely applied and demonstrated its reliability actual y in engineering fields, can solve these problems effectively. With the rapid development of computer technology, finite element analysis in the field of orthopedic applications has increasingly been used, which also promoted the development of orthopedic technology.

9.
Journal of Biomedical Engineering ; (6): 116-136, 2015.
Artigo em Chinês | WPRIM | ID: wpr-266716

RESUMO

Studying effects of 50 Hz sinusoidal electromagnetic fields (SEMFs) with different intensities on peak bone mass (PBM) of rats may provide a theoretical basis for application of electromagnetic clinical field. 30 female SD rats, 6 weeks of age, were randomly divided into three groups: the control group, 0.1 mT electromagnetic field group (EMFs) and 0.6 mT EMFs. The EMFs groups were treated for 3 h/day. After 8 weeks, we examined their bone mineral densities (BMD) , measured their bone biomechanical properties, and made serum levels of osteocalcin (OC), tartrate-resistant acid phosphatase 5b (TRACP 5b), and histomorphometry. It was found that the BMD (P < 0.01), maximum mechanical load (P < 0.01) in the 0.1 mT group were significantly higher than those in the control group, and Yield strength (P < 0.05), the analyses of serum bone turnover markers and histomorphometric parameters were better than those in the control group (P < 0.05). However, the 0.6 mT group did not have significantly difference comparing with that in the control group. This study proved that 50 Hz 0.1 mT SEMFs can increased BMD, bone strength, and bone tissue microstructure. Therefore, 50 Hz 0.1 mT SEMFs can improve peak bone mass of rats.


Assuntos
Animais , Feminino , Ratos , Fosfatase Ácida , Sangue , Densidade Óssea , Osso e Ossos , Fisiologia , Campos Eletromagnéticos , Isoenzimas , Sangue , Osteocalcina , Sangue , Ratos Sprague-Dawley , Fosfatase Ácida Resistente a Tartarato
10.
Journal of Preventive Medicine and Public Health ; : 57-63, 2014.
Artigo em Inglês | WPRIM | ID: wpr-198650

RESUMO

OBJECTIVES: We established a Wistar rat model of asthma caused by toluene diisocyanate (TDI) exposure, and investigated the relationship between TDI exposure concentrations and respiratory hypersensitivity, airway inflammation, and cytokine secretions in animals, to better understand the mechanism of TDI induced occupational asthma. METHODS: Wistar rats were exposed to two different concentrations of TDI vapor four hours a day for five consecutive days. Bronchoalveolar lavage (BAL) was performed, and differential leucocytes from the BAL fluid were analyzed. Lung histopathological examination was carried out to investigate the inflammatory status in the airways. Production of cytokines interleukin (IL)-4 and IL-5 productions in the BAL fluid in vivo was determined with enzyme-linked immunosorbent assay kits. RESULTS: The TDI-exposed rats exhibited greater airway hypersensitivity symptoms than the control rats. The BAL differential cell count and lung histopathological examination demonstrated that inflammation reactions were present in both the central and peripheral airways, characterized with marked infiltration of eosinophils in the TDI-exposed rats. The cytokine assay showed that IL-4 and IL-5 were predominantly produced in the BAL fluid in vivo. CONCLUSIONS: These findings imply that TDI exposure concentrations may greatly affect the occurrence and extent of inflammatory events and that Th2 type cytokines may play an important role in the immunopathogenesis of TDI-induced occupational respiratory hypersensitivity.


Assuntos
Animais , Feminino , Ratos , Líquido da Lavagem Broncoalveolar/química , Ensaio de Imunoadsorção Enzimática , Eosinófilos/citologia , Gases/química , Hipersensibilidade/patologia , Interleucina-4/análise , Interleucina-5/análise , Pulmão/efeitos dos fármacos , Ratos Wistar , Tolueno 2,4-Di-Isocianato/toxicidade
11.
China Journal of Orthopaedics and Traumatology ; (12): 587-591, 2014.
Artigo em Chinês | WPRIM | ID: wpr-249311

RESUMO

<p><b>OBJECTIVE</b>To compare the ability of osthole (OST) and genistein (GEN) in enhancing bone peak bone mass of rats to prevent osteoporosis.</p><p><b>METHODS</b>Thirty-six female one-month-old SD rats of (125 +/- 3) g body weight were randomly divided into three groups, 12 rats in each group, one group was orally administered osthole at 9 mg x kg(-1) d(-1), one group was given genistein at 10 mg x kg(-1) d(-1) and another was given equal quantity of distilled water as the control. The body weight was monitored weekly and the bone mineral density (BMD) of total body was measured every month. All rats were sacrificed after three months, the femoral bone mineral density, the serum levels of osteocalcin (OC) and anti-tartaric acid phosphatase 5b (TRACP 5b) were measured by Elisa. The bone microarchitectures were analyzed with micro-CT and the bone biomechanics properties were tested with universal material machine.</p><p><b>RESULTS</b>No significant differences were observed between O-treated or GEN group and the control for the food-intake and body weight during three months. However, the rats treated with OST had significant higher BMD for both total body and femur than the control and GEN group. The O-treated rats also had higher level of serum OC and lower level of TRACP 5b. Besides, they owned bigger bone volume/tissue volume, trabecular thickness, trabecular number but smaller trabecular spacing. In the three point bending tests of femurs,they were found to have larger maximum load, the young's modulus and structural model index (SMI).</p><p><b>CONCLUSION</b>Orally administered osthole could efficiently increase the peak bone mass of rats,which provide new ideas for preventing osteoporosis.</p>


Assuntos
Animais , Feminino , Ratos , Fosfatase Ácida , Sangue , Peso Corporal , Densidade Óssea , Cumarínicos , Farmacologia , Fêmur , Diagnóstico por Imagem , Patologia , Genisteína , Farmacologia , Isoenzimas , Sangue , Osteocalcina , Sangue , Radiografia , Ratos Sprague-Dawley , Fosfatase Ácida Resistente a Tartarato
12.
China Journal of Orthopaedics and Traumatology ; (12): 933-937, 2014.
Artigo em Chinês | WPRIM | ID: wpr-249251

RESUMO

<p><b>OBJECTIVE</b>To investigate the effects of different-intensity sinusoidal electromagnetic fields (SEMFs) on bone mineral density (BMD) and histomorphometry in SD rats.</p><p><b>METHODS</b>Thirty female SD rats were randomly divided into three groups: group A (a control group), group B (0.1 mT group) and group C (0.6 mT group). The rats in group B and C were exposed to 50 Hz SEMFs 3 hours each day. However,the magnetic intensity was different between group B and group C:0.1 mT for group B and 0.6 mT for group C. After 8 weeks, all the animals were killed. Changes of BMD and histomorphometric properties were observed.</p><p><b>RESULTS</b>Compared with group A, the BMD of whole body, femur and vertebrae of rats in group B increased significantly; the area percentage, number and width of bone trabeculae in vertebrae and femur of rats in group B were larger than those of group A; but the resolution of bone trabeculae of rats in group B was lower than that of group A. The trabecular number in group C rats were significantly decreased, compared with that in group A rats. The outcome of double fluorescence labeling in group B was found to be significantly different with that in group A. But the difference between rats in group A and C was not significant.</p><p><b>CONCLUSION</b>This study demonstrates that 50 Hz 0.1 mT SEMFs can increase BMD, improve bone tissue microstructure and, promote bone formation.</p>


Assuntos
Animais , Feminino , Ratos , Densidade Óssea , Efeitos da Radiação , Campos Eletromagnéticos , Vértebras Lombares , Patologia , Efeitos da Radiação , Osteogênese , Efeitos da Radiação , Ratos Sprague-Dawley , Tíbia , Patologia , Efeitos da Radiação
13.
Journal of Preventive Medicine and Public Health ; : 281-287, 2014.
Artigo em Inglês | WPRIM | ID: wpr-131190

RESUMO

OBJECTIVES: In Fujian Province, China, gastric cancer is one of the leading causes of mortality among all malignant tumors. Nanjing county and Minqing county are located in inland Fujian and have similar general demographics. However, the adjusted mortality rate of gastric cancer in Minqing was found to be much higher than that in Nanjing. We sought to explore factors associated with this increased risk of gastric cancer between the two counties. METHODS: We recruited 231 and 224 residents from Nanjing and Minqing, respectively, and analyzed differences between their dietary habits, Helicobacter pylori infection rates, and concentrations of serum pepsinogen I, pepsinogen II, gastrin-17, and ratio of pepsinogen I:II. RESULTS: Subjects in Minqing had more first-degree relatives who had been diagnosed with upper gastrointestinal tumor, more unhealthy dietary habits, a higher Helicobacter pylori positive rate, and greater proportion of abnormal serum gastrin-17 than those in Nanjing did. CONCLUSIONS: The factors that differed between these two counties might indicate that residents in Minqing have a higher risk for developing gastric cancer than those in Nanjing do.


Assuntos
Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , China/epidemiologia , Comportamento Alimentar , Gastrinas/sangue , Infecções por Helicobacter/epidemiologia , Helicobacter pylori , Pepsinogênio A/sangue , Pepsinogênio C/sangue , Fatores de Risco , Neoplasias Gástricas/diagnóstico
14.
Journal of Preventive Medicine and Public Health ; : 281-287, 2014.
Artigo em Inglês | WPRIM | ID: wpr-131187

RESUMO

OBJECTIVES: In Fujian Province, China, gastric cancer is one of the leading causes of mortality among all malignant tumors. Nanjing county and Minqing county are located in inland Fujian and have similar general demographics. However, the adjusted mortality rate of gastric cancer in Minqing was found to be much higher than that in Nanjing. We sought to explore factors associated with this increased risk of gastric cancer between the two counties. METHODS: We recruited 231 and 224 residents from Nanjing and Minqing, respectively, and analyzed differences between their dietary habits, Helicobacter pylori infection rates, and concentrations of serum pepsinogen I, pepsinogen II, gastrin-17, and ratio of pepsinogen I:II. RESULTS: Subjects in Minqing had more first-degree relatives who had been diagnosed with upper gastrointestinal tumor, more unhealthy dietary habits, a higher Helicobacter pylori positive rate, and greater proportion of abnormal serum gastrin-17 than those in Nanjing did. CONCLUSIONS: The factors that differed between these two counties might indicate that residents in Minqing have a higher risk for developing gastric cancer than those in Nanjing do.


Assuntos
Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , China/epidemiologia , Comportamento Alimentar , Gastrinas/sangue , Infecções por Helicobacter/epidemiologia , Helicobacter pylori , Pepsinogênio A/sangue , Pepsinogênio C/sangue , Fatores de Risco , Neoplasias Gástricas/diagnóstico
15.
Chinese Journal of Virology ; (6): 37-43, 2014.
Artigo em Chinês | WPRIM | ID: wpr-356641

RESUMO

This study aims to investigate the characteristics of genomic variation of pandemic A/H1N1/2009 influenza virus isolated in Fujian Province, China. Complete genome sequence analysis was performed on 14 strains of pandemic A/H1N1/2009 influenza virus isolated from Fujian during 2009-2012. All virus strains were typical low-pathogenic influenza viruses, with resistance to amantadine and sensitivity to neuraminidase inhibitors. Eight genome fragments of all strains were closely related to those of A/California/07/2009 (H1N1) vaccine strain, with > or = 98.2% homology. Compared with the vaccine strain, the influenza strains from Fujian had relatively large variation, and variation was identified at 11 amino acid sites of the HA gene of A/Fujiangulou/SWL1155/2012 strain, including 4 sites (H138R, L161I, S185T, and S203T) involved inthree antigen determinants (Ca, Sa, and Sb). In conclusion, the influenza vaccine has a satisfactory protective effect on Fujian population, but the influenza strains from Fujian in 2012 has antigenic drift compared with the vaccine strain, more attention should therefore be paid to the surveillance of mutations of pandemic A/H1N1/2009 influenza virus.


Assuntos
Humanos , Antivirais , Farmacologia , China , Epidemiologia , Farmacorresistência Viral , Genética , Genoma Viral , Genética , Genômica , Vírus da Influenza A Subtipo H1N1 , Genética , Alergia e Imunologia , Fisiologia , Influenza Humana , Epidemiologia , Pandemias , Vacinas Virais , Alergia e Imunologia
16.
Chinese Journal of Virology ; (6): 624-629, 2014.
Artigo em Chinês | WPRIM | ID: wpr-280317

RESUMO

In order to characterize the molecular epidemiology of HFMD-associated Coxsackievirus A6 (CVA6) in Fujian Province, a total of 1340 specimens from non-EV71 non-CVA16 HFMD patients were collected during 2011-2013. Isolated virus strains were identified and subtyped. Full-length coding regions for the VP1 gene of the predominant serotype CVA6 isolates were amplified and sequenced. Among the 375 non-EV71 non-CVA16 HFMD cases confirmed by virus isolation and molecular subtyping, 182 (48.5%) were found to be caused by CVA6, accounting for 7.9%, 16.2% and 39.6% HFMD-associated enteroviruses in FujianProvince during 2011, 2012, and 2013, respectively. Compared with general features observed in the HFMD epidemic, no difference in CVA6-specificity or severity rates was observed between geographical origins, gender, or age groups. Nucleotide sequence analyses of VP1 genes revealed high diversity levels of 16.2%-18.6% among CVA6 strains from Fujian Province, in contrast to the prototype CVA6 strain, and showed low levels of diversity in the amino acid sequences (4.3%-6.2%). Phylogenetic analysis also indicated that CVA6 isolates from Fujian Province were distinct from the prototype strain and other isolates from abroad; however, it was homologous to domestic strains, although the Fujian isolates clustered into multiple branches. These results suggested that significant changes in the pathogenic spectrum of HFMD in Fujian Province occurred during 2011-2013, as CVA6 was one of the predominant serotypes of HFMD. CVA6 isolates from Fujian Province were co-circulating and co-evolving with other domestic strains as multiple closely related CVA6 transmission chains were observed in Fujian Province overall and within each prefecture.


Assuntos
Criança , Pré-Escolar , Feminino , Humanos , Lactente , Masculino , China , Epidemiologia , Enterovirus Humano A , Classificação , Genética , Evolução Molecular , Doença de Mão, Pé e Boca , Epidemiologia , Virologia , Epidemiologia Molecular , Dados de Sequência Molecular , Filogenia
17.
Chinese Pharmacological Bulletin ; (12): 1315-1319, 2014.
Artigo em Chinês | WPRIM | ID: wpr-456606

RESUMO

Aim To compare the pharmacological ac-tivity of icariin( ICA) and genistien ( GEN) against os-teoporosis after oral administration with them to growing rats and ovariectomized rats. Methods 25 mg·kg-1 icariin and 10 mg · kg-1 genistein ( equal in molar concentration) were administered to one-month-old fe-male SD rats every day for three months. Treatments at the same dosage were administered to the 6-month-old ovariectomized SD rats every day for three months. Their effects were compared on bone mineral density and biomechanical properties of femurs and vertebrae, serum levels of osteocalcin and tartaric acid phospha-tase 5b ( TRACP 5b) and histomorphometry. Results The results showed that, in young rats, icariin treat-ment significantly increased bone mineral density, the maximum mechanical loads of femurs and vertebrae as well as the bone qualities ( serum markers and microar-chitecture ) , whereas genistein treatment had little effects compared with the non-treatment control. How-ever, genistein treatment was more efficacious than icariin in preventing bone loss and deterioration of bone microarchitecture in ovariectomized rats. Conclusion Our data suggest that, since icariin has a higher os-teogenic activity but lower estrogenic activity, it has been found to be more efficacious than genistein in peak bone mass accrual only in young rats. In the ovariectimized rats, however, as the main force to pre-vent bone loss is the estrogenic activity, genistein has been found to be more efficacious than icariin in reduc-ing bone loss.

18.
International Eye Science ; (12): 1652-1655, 2014.
Artigo em Chinês | WPRIM | ID: wpr-642074

RESUMO

To research the association between primary progressive pterygium and tear film. ●METHODS: Totally 60 cases of primary progressive pterygium from September 2012 to June 2013 in our hospital were enrolled. The pterygium eye was for observation group and the contralateral eye as the control group. The differences of eye symptoms, tear film break-up time ( BUT ), Schirmer Ⅰ test ( S Ⅰ t ), corneal fluorescein staining (FL), tear ferning test (TFT) and the conjunctival impression cytology ( ClC) were compared between two groups. ●RESULTS: The eyes in observation group had higher symptoms score, FL score, grades of conjunctival squamous metaplasia, percentage of abnormal tear ferning, but had lower BUT and density of goblet cell, the differences had statistically significance (P0. 05). ● CONCLUSlON: Primary progressive pterygium can cause a decrease in tear film stability, which in turn lead to some dry eye symptoms such as dry feeling and burning sensation, and its mechanism may be caused by multi-factors, such as density change of goblet cell and the tear fluid dynamics.

19.
China Journal of Chinese Materia Medica ; (24): 1783-1788, 2013.
Artigo em Chinês | WPRIM | ID: wpr-346499

RESUMO

<p><b>OBJECTIVE</b>To compare the effect of icariin and genistein in the osteogenic differentiation of rat bone marrow stromal cells (rBMSC).</p><p><b>METHOD</b>Rat marrow stromal cells were seperated in vitro, and the optimal concentration of genisten and icriin were screened. Genistein and icariin with the concentration of 1 x 10(-5) mol x L(-1) were adopted to intereven rBMSCs cultured in vitro. Alkaline phosphatase (ALP) was determined at 3, 6, 9, 12,15 d after intervention; calcified nodule was detected with alizarin red staining at 12 d; OXS, Runx-2, bone morphogenetic protein (BMP-2) and Collagen-I mRNA expression were observed with Real-time RT-PCR at 12, 24, 48, 72, 96 h.</p><p><b>RESULT</b>Genistein and icariin with the concentration of 1 x 10(-5) mol x L(-1) could increase the activity of ALP and the content of Ca, regulate OXS, BMP-2, Runx-2 and Collagen-I mRNA expression.</p><p><b>CONCLUSION</b>Icariin showed a stronger effect in improving the osteogenic differentiation of rat bone marrow stromal cells than genistein.</p>


Assuntos
Animais , Ratos , Fosfatase Alcalina , Genética , Metabolismo , Proteína Morfogenética Óssea 2 , Genética , Metabolismo , Diferenciação Celular , Células Cultivadas , Flavonoides , Farmacologia , Expressão Gênica , Genisteína , Farmacologia , Células-Tronco Mesenquimais , Biologia Celular , Metabolismo , Osteogênese , Ratos Sprague-Dawley , Fator de Crescimento Transformador beta , Genética , Metabolismo
20.
China Journal of Chinese Materia Medica ; (24): 1992-1996, 2013.
Artigo em Chinês | WPRIM | ID: wpr-346457

RESUMO

<p><b>OBJECTIVE</b>To compare the effects of 8-prenylnaringenin (PNG) and naringenin (NG) on the activity and apoptosis of osteoclasts cultured in vitro, in order to study physiological activity of 8-prenyl perssad.</p><p><b>METHOD</b>Osteoclasts were separated from long-limb bones of newly born rabbits, cultured in alpha-MEM containing 10% FBS, and then added with PNG and NG with the concentration of 1 x 10(-5) mol x L(-1). They were stained with TRAP and determined for enzymatic activity with TRAP after 4 d, and analyzed by toluidine blue staining after 7 d. The apoptotic osteoclasts were analyzed by Annexin V-FITC staining after 2, 4, 8, 12, 24, 36, and 48 hours, to observe their apoptosis. Their total RNAs were extracted, and analyzed for TRAP and Cathepsin K expressions by Real-time RT-PCR.</p><p><b>RESULT</b>Compared with the control group, both of the PNG group and the NG group showed much less osteoclasts (TRAP positive cells), lower TRAP activity and TRAP and Cathepin K (CTSK) expression, and smaller number of bone resorption pits and areas. The PNG group show lower indexes than the NG group. Additionally, the PNG group reached the apoptotic peak of osteoclasts at 12 h after drug administration, whereas the NG group reached after 24 h. And the former had more apoptotic cells than the latter.</p><p><b>CONCLUSION</b>8-PNG is much more active than NG in inhibiting the resorption of osteoclasts and inducing apoptosis of osteoclasts. Their only difference lies in 8-prenyl perssad, which is proved to be able to enhance the anti-bone resorption activity of 8-prenylnarigenin.</p>


Assuntos
Animais , Coelhos , Fosfatase Ácida , Metabolismo , Reabsorção Óssea , Catepsina K , Metabolismo , Células Cultivadas , Flavanonas , Farmacologia , Osteoclastos
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