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1.
Chinese Journal of Preventive Medicine ; (12): 197-202, 2022.
Article in Chinese | WPRIM | ID: wpr-935270

ABSTRACT

Objective: To systematically evaluate the acceptance of pre-exposure prophylaxis (PrEP)among men who have sex with men (MSM) in China, so as to provide reference for the promotion of preventive drug use before human immunodeficiency virus exposure in China. Methods: By searching the databases of China national knowledge infrastructure, VIP database, Wanfan knowledge service platform, PubMed, Web of Science, Embase and The Cochrane Library with key words of "men who have sex with men" "pre-exposure prophylaxis" "PrEP" and "MSM". The literature on the willingness of Chinese MSM population to accept PrEP was systematically collected, and the data of the literature meeting the inclusion criteria were extracted for Meta analysis. Results: A total of 12 articles were selected in this study, including 6 articles in English and 6 in Chinese. The score of bias risk assessment of eligible articles was 14-18, which was more than 70% of the total score. The total number of samples was 11 269. The overall acceptance rate of PrEP was 0.77(95%CI:0.71-0.82). In subgroup analysis, the acceptance rates of different nationalities, marriage, household registration, age, education background, income, sexual orientation, sexual behavior and awareness of PrEP were statistically significant. Conclusion: In general, the acceptance rate of PrEP in MSM population is higher, but the awareness rate is low. There are differences in the acceptance rate among different groups.


Subject(s)
Female , Humans , Male , China/epidemiology , HIV Infections/prevention & control , Health Knowledge, Attitudes, Practice , Homosexuality, Male , Patient Acceptance of Health Care , Pre-Exposure Prophylaxis , Sexual Behavior , Sexual and Gender Minorities
2.
Acta Pharmaceutica Sinica ; (12): 958-966, 2020.
Article in Chinese | WPRIM | ID: wpr-821695

ABSTRACT

Hypoxia-activated prodrugs that specifically target tumor tissues were designed by attaching the nitro-aromatic ring carrier molecules that can be degraded in the hypoxic microenvironment of the tumor to the hydroxyamidine group of IDO1 inhibitor compound B and epacadostat. Eleven prodrug compounds were synthesized and their structures were confirmed by 1H NMR and HR-MS. Compounds F-1 and F-6, which had a higher stability and drug release rate, were identified by an in vitro stability assay, nitroreductase reduction assay, MTT assay, and an in vivo tumor tissue hypoxia degradation assay, and then evaluated for anti-tumor efficacy in vivo. The results showed that prodrug F-1 inhibited tumor growth by 67.41%, which was significantly higher than 42.31% for the starting drug group. It appeared that the inhibition of IDO1 in the tumor tissue was different from the overall inhibition of IDO1 in vivo. Animal treatment procedures were carried out with the approval of the Animal Care and Use Committee of the Chinese Academy of Medical Sciences and Peking Union Medical College.

3.
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 99-105, 2019.
Article in Chinese | WPRIM | ID: wpr-802305

ABSTRACT

Objective:To explore the effect of celastrol in inhibiting the lipid metabolism disorder in hepatic L02 cells and its possible mechanism on endoplasmic reticulum stress (ERS) of non-alcoholic fatty liver cells by intervening non-alcoholic fatty liver disease(NAFLD) cell model with celastrol. Method:Hepatic L02 cells were divided into control group, model group, low-dose celastrol treatment group (Cel 0.5 mg·L-1), high-dose celastrol treatment group (Cel 1 mg·L-1) and simvastatin group (SIM 6 mg·L-1) for cultivation. The contents of total cholesterol (TC) and total triglyceride (TG) in hepatic L02 cells were detected, and the oil red staining was used to detected the lipid accumulation in hepatic L02 cells. Reverse transcription polymerase chain reaction (RT-PCR) and Western blot were used to detect the mRNA and protein expression levels of endoplasmic reticulum stress (ERS)-related signal molecules activating transcription factor 6 (ATF6), glucose regulated protein 78 (GRP78), inositol-requiring enzyme 1 (IRE1), sterol regulatory element-binding protein cleavage-activating protein (SCAP), sterol regulatory element-binding protein-1c (SREBP-1c) and sterol regulatory element-binding protein-2 (SREBP-2) in hepatic L02 cell model respectively. Result:The contents of TC and TG in hepatic L02 cells of NAFLD group were significantly higher than those in control group (P-1 group, Cel 1 mg·L-1 group and SIM 6 mg·L-1 group were significantly lower than those in NAFLD group (P-1 group, the Cel 1 mg·L-1 group, and the SIM 6 mg·L-1 group were lower than the NAFLD group to different degrees. According to the results of RT-PCR and Western blot, the mRNA transcription and protein expression levels of ERS-related signaling molecules ATF6, GRP78, IRE1, SCAP, SREBP-1c and SREBP-2 in hepatic L02 cells of NAFLD group were higher than those of control group (P-1 group, Cel 1 mg·L-1 group and SIM 6 mg·L-1 group were lower than those of NAFLD group (P-1 group and the SIM 6 mg·L-1 group. Conclusion:Celastrol can reduce the lipid metabolism disorder in hepatic L02 cells by down-regulating the expressions of ERS-related signaling molecules ATF6, GRP78, IRE1, SCAP, SREBP-1c and SREBP-2 in hepatic L02 cells, so as to improve NAFLD.

4.
Journal of Sun Yat-sen University(Medical Sciences) ; (6): 257-263, 2019.
Article in Chinese | WPRIM | ID: wpr-817746

ABSTRACT

@#【Objective】To explore colonoscopy adherence and related factors among preliminary screened-positive population in Guangzhou. 【Methods】This study was a part of the Guangzhou Community-based Colorectal Cancer Screening Program. We retrospectively analyzed the 1-year follow-up data of population aged 50~74 years old and positive in preliminary colorectal cancer screening in 2015. Kaplan- Meier method was used to describe the respond time to colonoscopy examination. Cox proportional hazard model was performed to identify factors associated with colonoscopy adherence. The effect of studied factors on colonoscopy adherence was reported according to hazard ratio(HR).【Results】 A total of 18 604 preliminary screened-positive residents were included ,among whom 4 014 completed colonoscopy examination within one year,with a colonoscopy adherence of 21.6% . Colorectal lesions were found in 2 012 cases (50.1%),of which 96(2.4%)were colorectal cancers. The adherence of 1 month,3 months and 6 months were 9.7% ,15.8% ,and 18.6% respectively. Multivariate Cox regression analysis showed that those who were female ,in older age , unmarried/widowed/divorced,without health insurance,and had a history of chronic cholecystitis or cholecystectomy were less likely to undergo colonoscopy;while those who were fecal occult blood test- positive,had colonoscopy preferential policies,worked in government or public institution,had medical insurance for urban workers,had a history of chronic diarrhea,a history of chronic constipation,a history of mucous and/or blood stool,and a history of bad life incidents were more likely to undergo colonoscopy. 【Conclusions】 This study suggested that the colonoscopy adherence of preliminary screened- positive population in Guangzhou was low and such low adherence was associated with different factors. Community health workers should timely track the completion of colonoscopy of preliminary screened-positive residents , and take targeted measures to promote colonoscopy adherence.

5.
Acta Pharmaceutica Sinica ; (12): 1113-1121, 2018.
Article in Chinese | WPRIM | ID: wpr-779978

ABSTRACT

The abnormal activation of hedgehog (HH) signaling pathway plays an important role in the development and progression of glioblastoma (GBM). As a transcription factor at the end of the HH pathway, the final effector of glioma-associated oncogene homoglog-1 (GLI1) is an important target in the treatment of GBM. The study was designed to evaluate the anti-tumor activities and mechanisms of a novel GLI1 inhibitor FL18 in GBM. MTT and colony formation assay were performed to determine anti-proliferation activity of FL18 in vitro. The effect of FL18 on cell apoptosis was measured by flow cytometry (FCM) analysis. Transwell experiment was used to explore the inhibitory activity of FL18 in cell invasion. In vivo experiments, the subcutaneously transplanted and orthotopic U-87 MG GBM xenograft model were used to study the activity of FL18 on tumor growth. The optimized dual report gene screening model was used to detect the effect of FL18 on the transcriptional activity of GLI1. Western blot assay was used to study the mechanisms of action of FL18. The results showed that the IC50 of FL18 in glioblastoma was in the nanomole level in vitro. It was observed that 22.5 and 45 mg·kg-1 FL18 reduced the tumor volume with the rate of 55.4% and 89.8% in xenograft model in mice in situ. The IC50 of FL18 on the inhibition of GLI1 transcriptional activity was 3.32×10-11 mol·L-1 analyzed by the optimized dual report gene screening model. By the Western blot experiments, it was proved that FL18 inhibited expression of GLI1 without influencing the upstream canonical HH/SMO signaling and cross-talk oncogenic pathway, such as ERK and AKT signaling. The results also demonstrated that FL18 significantly downregulated GLI1 target genes such as Bcl-2, MMP2 and MMP9 and increased the expression of c-caspase3, c-PARP and Bax. These data suggest that FL18 may generate the anti-glioma activity by inhibition of GLI1.

6.
Acta Pharmaceutica Sinica ; (12): 1424-1431, 2017.
Article in Chinese | WPRIM | ID: wpr-779744

ABSTRACT

Recent studies indicate that insulin-sensitizing activity of TZDs occurs through the inhibition of PPARγ Ser273 phosphorylation mediated by cyclin-dependent kinase 5(Cdk5), which is resulted from the binding activity for PPARγ. While, the side effects of TZDs may be related to the agonistic potency for PPARγ. In this article, 15 target compounds were designed and synthesized based on the structure of PPAR γ partial agonist INT131, with the aim of maintaining the insulin-sensitizing activity and reducing the side effects of INT131. The structures of these compounds were confirmed by 1H NMR and ESI-MS, and their binding activities and agonistic potencies for PPARγ were measured. The binding activity of compound 15 is 88.47% of rosiglitazone, which is similar to INT131 (98.55%), but the agonistic potency of compound 15 is 1.41% of rosiglitazone, obviously lower than INT131 (15.18%).

7.
Journal of Southern Medical University ; (12): 947-951, 2017.
Article in Chinese | WPRIM | ID: wpr-360157

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the impact of cement distribution index on the occurrence of refracture in the adjacent segments after percutaneous vertebroplasty.</p><p><b>METHODS</b>This retrospective analysis was conducted among 143 patients who received percutaneous vertebroplasty for osteoporotic vertebral compression fracture between April, 2011 and April, 2014. Of the 134 patients with complete follow-up data, 18 had adjacent segment fracture within 1 year following the surgeries (re-fracture group), and 116 patients without new fracture served as the control group. All the patients underwent X-ray examinations after the surgery and according to the position and shape, the cement in the vertebrae were classified into 5 types (I to V), and the volume-cubage index was computed based on the cement volume and vertebral cubage. Age, gender, bone mineral density (BMD), cement distribution index, volume-cubage index, and cement leakage were evaluated in the 2 groups, and the variables with significant differences between the 2 groups were analyzed in Logistic regression analysis.</p><p><b>RESULTS</b>BMD was significantly lower and the rate of cement leakage was significantly higher in the re-fracture group than in the control group (P<0.05). Significant difference was found in cement distribution index between the 2 groups (P<0.05) but not in age, gender, cement volume or volume-cubage index (P>0.05). Logistic regression analysis indicated that BMD, cement leakage and cement distribution index all significantly affected the occurrence of adjacent vertebral fractures following percutaneous vertebroplasty.</p><p><b>CONCLUSION</b>A low BMD, cement leakage and a low cement distribution index are all risks factor of adjacent vertebral fracture after percutaneous vertebroplasty.</p>

8.
Asian Pacific Journal of Tropical Medicine ; (12): 53-59, 2015.
Article in English | WPRIM | ID: wpr-820402

ABSTRACT

OBJECTIVE@#To investigate the synergistic effect and mechanism of the combined application of recombinant human bone morphogenetic protein-2 (rhBMP-2) and basic fibroblast growth factor (bFGF).@*METHODS@#24 KM male mice were randomly divided into 6 groups with 4 mice in each group, namely, Group A (control group), Group B (only treated with collagen), Group C (treated with 2 ng bFGF+collagen), Group D (treated with 4 μ g rhBMP-2+collagen), Group E (treated with 4 μ g rhBMP-2+2 ng bFGF+collagen) and Group F (treated with 4 μ g rhBMP-2+4 ng bFGF+collagen). The composites were implanted into the intermuscular septum of hind legs mice; whereas in control group, intermuscular septum of mice was separated and no implantation was performed. General observation, detection of concentration of calcium content, micro computed tomography (Micro-CT), three-dimensional reconstruction scan, measurement of bone mineral density (BMD), bone volume fraction (BVF) and trabecular thickness (Tb.Th), as well as histological observation with HE staining and ALP and CD34 immumohistochemical staining were performed.@*RESULTS@#Ectopic osteogenesis was found in Groups D, E and F mice. The difference in concentration of calcium contents was statistically significant between Groups D and E (P0.05). Micro-CT and three-dimensional reconstruction revealed continuous newborn bone substance in external surface of ectopic bone formation, and the center of bone formation did not show obvious substantial filling by bone substance. The differences in BMD, BVF and Tb.Th were statistically significant between Groups D and E or F (P<0.01 or <0.05). HE staining showed that in Groups D, E and F, newborn bone substance was mainly located at the edge of ectopic bone formation, and the bone formation in Groups E and F was better than that in Group D. ALP and CD34 immumohistochemical staining revealed the positive expression mainly at the edge of ectopic bone formation, and area of positive expression in Groups E and F was larger than that in Groups D.@*CONCLUSIONS@#rhBMP-2 possesses the capacity to induce ectopic osteogenesis independently, but bFGF does not have this ability; the combined application of rhBMP-2 and bFGF can enhance the synergetic effect on inducing ectopic osteogenesis.

9.
Acta Pharmaceutica Sinica ; (12): 854-860, 2015.
Article in Chinese | WPRIM | ID: wpr-257056

ABSTRACT

The aim of this study is to evaluate anti-tumor activities and mechanism of a novel kinase inhibitor ZLJ213 which targeted Aurora A and vascular endothelial growth factor receptor (VEGFR) in vitro and in vivo against human colon cancer. Results showed that ZLJ213 inhibited cell proliferation and induced cell cycle arrest and apoptosis of HCT1 16 and SW48 cell lines. In HCT116-derived xenograft, ZLJ213 dosed at 100 mg · kg(-1) inhibited tumor growth by 73.24%. The IC50 of ZLJ213 on the expression of p-Aurora A was 0.258 µmol · L(-1) analyzed by ELISA. Under the concentration of 0.08 µmol · L(-1), ZLJ213 could inhibit the activities of Aurora A, Histone H3 and VEGFR of HCT116 and SW48 cell lines. Simultaneously, ZLJ213 induced activation of Caspase 3 and PARP cleavage. Above data suggested that ZLJ213 had the ability to inhibit cell proliferation and induce cell apoptosis both in vitro and in vivo in colon cancer, and down-regulate the expression of p-Aurora A and p-VEGFR. ZLJ213 might be a potential therapeutic agent against colon cancer.


Subject(s)
Animals , Humans , Apoptosis , Aurora Kinase A , Cell Cycle Checkpoints , Cell Line, Tumor , Cell Proliferation , Colonic Neoplasms , Pathology , Protein Kinase Inhibitors , Pharmacology , Receptors, Vascular Endothelial Growth Factor , Metabolism , Xenograft Model Antitumor Assays
10.
Asian Pacific Journal of Tropical Medicine ; (12): 53-59, 2015.
Article in Chinese | WPRIM | ID: wpr-951541

ABSTRACT

Objective: To investigate the synergistic effect and mechanism of the combined application of recombinant human bone morphogenetic protein-2 (rhBMP-2) and basic fibroblast growth factor (bFGF). Methods: 24 KM male mice were randomly divided into 6 groups with 4 mice in each group, namely, Group A (control group), Group B (only treated with collagen), Group C (treated with 2 ng bFGF+collagen), Group D (treated with 4 μ g rhBMP-2+collagen), Group E (treated with 4 μ g rhBMP-2+2 ng bFGF+collagen) and Group F (treated with 4 μ g rhBMP-2+4 ng bFGF+collagen). The composites were implanted into the intermuscular septum of hind legs mice; whereas in control group, intermuscular septum of mice was separated and no implantation was performed. General observation, detection of concentration of calcium content, micro computed tomography (Micro-CT), three-dimensional reconstruction scan, measurement of bone mineral density (BMD), bone volume fraction (BVF) and trabecular thickness (Tb.Th), as well as histological observation with HE staining and ALP and CD34 immumohistochemical staining were performed. Results: Ectopic osteogenesis was found in Groups D, E and F mice. The difference in concentration of calcium contents was statistically significant between Groups D and E (. P0.05). Micro-CT and three-dimensional reconstruction revealed continuous newborn bone substance in external surface of ectopic bone formation, and the center of bone formation did not show obvious substantial filling by bone substance. The differences in BMD, BVF and Tb.Th were statistically significant between Groups D and E or F (. P<0.01 or <0.05). HE staining showed that in Groups D, E and F, newborn bone substance was mainly located at the edge of ectopic bone formation, and the bone formation in Groups E and F was better than that in Group D. ALP and CD34 immumohistochemical staining revealed the positive expression mainly at the edge of ectopic bone formation, and area of positive expression in Groups E and F was larger than that in Groups D. Conclusions: rhBMP-2 possesses the capacity to induce ectopic osteogenesis independently, but bFGF does not have this ability; the combined application of rhBMP-2 and bFGF can enhance the synergetic effect on inducing ectopic osteogenesis.

11.
Acta Pharmaceutica Sinica ; (12): 1022-1028, 2014.
Article in Chinese | WPRIM | ID: wpr-299173

ABSTRACT

Curcumin has been reported to possess antitumor activity with low toxicity. However, the clinical application of curcumin has been significantly limited by its instability and poor metabolic property. In order to overcome these limitations and discover novel small molecules with potential antitumor activity, 29 curcumin mimics were synthesized, which were confirmed by 1H NMR and HR-MS, and their cytotoxic property was evaluated against five human cancer cell lines in vitro. Compounds 16, 18 and 19 exhibited good cytotoxic property, their IC50 value were even below 5 micromol x L(-1) to some cancer cell lines, 5-9 times better than curcumin.


Subject(s)
Humans , Antineoplastic Agents , Pharmacology , Cell Line, Tumor , Curcumin , Pharmacology , Drug Screening Assays, Antitumor , Inhibitory Concentration 50
12.
Acta Pharmaceutica Sinica ; (12): 1658-1664, 2014.
Article in Chinese | WPRIM | ID: wpr-251839

ABSTRACT

In-vitro assay methods were established to evaluate transactivation and binding activity of compounds on peroxisome proliferator-activated receptor y (PPARγ). Firstly, plasmids were constructed for transactivation assay of PPARγ response element (PPRE) triggered reporter gene expression, and for cell-based binding activity assay of the chimeric receptor, which was fused with PPARγ ligand binding domain (LBD) and yeast transcriptional activator Gal4. Secondly, by using PPARy competitive binding assay based on time resolved-fluorescence resonance energy transfer (TR-FRET), affinities of compounds and drugs to PPARγ were evaluated. In application of these above methods, the PPARγ activating potency and characteristics of different compounds were evaluated, and a novel benzeneselfonamide derivative, ZLJ01, was found to have comparable binding activity and affinity with the well-known PPARy agonist, but lack of PPRE mediated transactivation activity. In preliminary study on in-vitro hypoglycemic activity, ZLJ1 was found to promote insulin-stimulated glucose uptake by liver cells. Therefore, we believe that combining transactivation and binding activity as well as affinity evaluation, the system could be used to screen non-agonist PPARγ ligand as anovel PPARγ modulator


Subject(s)
Genes, Reporter , Hepatocytes , Hypoglycemic Agents , Chemistry , Ligands , PPAR gamma , Chemistry , Plasmids , Response Elements , Sulfonamides , Chemistry , Transcriptional Activation
13.
Acta Pharmaceutica Sinica ; (12): 639-643, 2014.
Article in Chinese | WPRIM | ID: wpr-245034

ABSTRACT

A series of novel sorafenib analogues were designed and synthesized. The cytotoxic activities of these compounds were tested in four tumor cell lines. Some of the compounds showed potent antiproliferative activity against the tested cell lines with IC50 = 4-20 micromol x L(-1). Some compounds demonstrated competitive antiproliferative activities to sorafenib against tested cancer cell lines. Among them, compound 7c demonstrated significant inhibitory activities on ACHN, HCT116 and MDA-MB-231 cell lines with IC50 values of 9.01, 4.97, 6.61 micromol x L(-1), respectively.


Subject(s)
Humans , Antineoplastic Agents , Chemistry , Pharmacology , Cell Line, Tumor , Cell Proliferation , Inhibitory Concentration 50 , Molecular Structure , Niacinamide , Chemistry , Pharmacology , Phenylurea Compounds , Chemistry , Pharmacology , Structure-Activity Relationship
14.
Acta Pharmaceutica Sinica ; (12): 861-868, 2014.
Article in Chinese | WPRIM | ID: wpr-245002

ABSTRACT

The purpose of this study is to investigate the activity and mechanism of a new anti-tumor agent T03. MTT and colony formation assay were performed to determine anti-proliferation activity of T03 in vitro. Antitumor activity was observed by Renca xenograft model in vivo. The effect of T03 on cell cycle and apoptosis were measured by FCM analysis. Western blotting was performed to investigate the expression level of proteins in HepG2 cell lines treated with T03. T03 had anti-tumor activity by inhibiting tumor cell growth and colony formation in vitro, especially on hepatocellular carcinoma cells (HCC). At the concentration of 10 micromol x L(-1), T03 induced cell apoptosis and cell cycle arrest in HCC. Moreover, it proved that T03 reduced the tumor weight with the rate of 42.30% without any obviously side effect in Renca xenograft model. At the concentration of 2.0 micromol x L(-1), T03 was able to reduce the level of p-c-Raf (Ser259), and thus blocked Raf/MEK/ERK and AKT signaling in HepG2 cell lines. The result suggested that T03 has the potential to inhibit cell proliferation and induce cell apoptosis both in vitro and in vivo, particularly active against HCC, indicating T03 and its analogues may serve as a new anti-cancer drug against hepatocellular carcinoma.


Subject(s)
Animals , Humans , Antineoplastic Agents , Pharmacology , Apoptosis , Carcinoma, Hepatocellular , Pathology , Cell Cycle Checkpoints , Cell Proliferation , Hep G2 Cells , Liver Neoplasms , Pathology , Signal Transduction , Xenograft Model Antitumor Assays
15.
Acta Pharmaceutica Sinica ; (12): 888-895, 2014.
Article in Chinese | WPRIM | ID: wpr-244998

ABSTRACT

A series of 2-(3-butynoicamidophenyl)benzothiazole derivatives were synthesized starting from 4-fluoro-3-nitrobenzoic acid. Structures of all the synthesized compounds were confirmed by 1H NMR and HR-MS. Their antitumor activities against human tumor cells lines (HCT116, Mia-PaCa2, U87-MG, A549, NCI-H1975) were evaluated by MTT assay. The results revealed that most of the synthesized compounds showed potent activities against HCT116, Mia-PaCa2, U87-MG tumor cells lines. Particularly, compounds 14c and 14h exhibited better activity with IC50 values of 1 x 10(-8) mol x L(-1) against U87-MG and HCT116 respectively. The structure-activity relationship of compounds was also discussed preliminarily.


Subject(s)
Humans , Antineoplastic Agents , Pharmacology , Benzothiazoles , Pharmacology , Cell Line, Tumor , Drug Screening Assays, Antitumor , Nitrobenzoates , Structure-Activity Relationship
16.
Asian Pacific Journal of Tropical Medicine ; (12): 884-888, 2013.
Article in English | WPRIM | ID: wpr-819954

ABSTRACT

OBJECTIVE@#To explore the effect of sustained-release recombinant human bone morphogenetic protein-2 (rhBMP-2) on ectopic osteogenesis in the muscle pouches of rats through preparing rhBMP-2 sustained-release capsules by wrapping morphogenesis protein bones-2 (BMP-2) using chitosan nanoparticles, and compositing collagen materials.@*METHODS@#Twenty four Sprague-Dawley rats were randomly divided into four groups with six rats in each group, that is Group A (control group), Group B (only treated with collagen), Group C (rhBMP-2+collagen treated group) and Group D (rhBMP-2/cs+collagen treated group). The composite materials for each group were implanted in the bilateral peroneal muscle pouches in rats. The peroneal muscles were only separated without implanting any materials in control group. Rats were sacrificed 2 weeks and 4 weeks post treatment and samples were cut off for general observation, Micro CT scans and histological observation.@*RESULTS@#General observation showed no new bone formation in Groups A and B mice, while new bones were formed in Groups C and D mice. Two weeks after treatment Micro CT scans showed that The bone volume fraction (BVF), trabecular thickness (Tb.Th), bone mineral density (BMD) in Group C mice were all higher than that in Group D (P<0.05). At the fourth week, the BVF, Tb.Th and BMD were significantly higher than that at the second week (P<0.01).@*CONCLUSIONS@#The slow-release effect of rhBMP-2/cs sustained-release capsules can significantly promote ectopic osteogenesis. Its bone formation effect is better than that of rhBMP-2 burst-release group.


Subject(s)
Animals , Rats , Bone Morphogenetic Protein 2 , Pharmacology , Collagen , Pharmacology , Delayed-Action Preparations , Pharmacology , Drug Carriers , Pharmacology , Intercellular Signaling Peptides and Proteins , Muscle, Skeletal , Nanocapsules , Osteogenesis , Rats, Sprague-Dawley , Recombinant Proteins , Pharmacology , Tissue Engineering , Methods , Transforming Growth Factor beta , Pharmacology , X-Ray Microtomography
17.
Acta Pharmaceutica Sinica ; (12): 514-520, 2013.
Article in Chinese | WPRIM | ID: wpr-235635

ABSTRACT

Glucokinase (GK) is a new target for the treatment of type II diabetes mellitus (T2DM). In order to find a structure-simplified small molecule GK activator, 19 salicylic acid derivatives were designed and synthesized based on new lead compound (1). Experimental results showed that the potency of compound 8h is superior to control RO-28-0450 in GK activation.


Subject(s)
Drug Design , Enzyme Activation , Enzyme Activators , Chemistry , Pharmacology , Glucokinase , Metabolism , Hypoglycemic Agents , Chemistry , Pharmacology , Molecular Structure , Salicylates , Chemistry , Pharmacology , Thiazoles , Pharmacology
18.
Acta Pharmaceutica Sinica ; (12): 1623-1629, 2012.
Article in Chinese | WPRIM | ID: wpr-274612

ABSTRACT

A novel series of sorafenib analogs containing 2-picolinyl hydrazide moiety were designed and synthesized. In vitro, most of synthesized compounds have antiproliferation activity on MDA-MB-231, ACHN, HepG2, Mia-PaCa-2 and SW1990 cell lines tested by MTT assay. It is worth noting that the antitumor activities of compounds 2c, 2d and 2f are more potent than that of sorafenib on pancreatic cancer cells Mia-PaCa-2 and SW1990, and the activities of compounds 3f and 3g are 2-3 times than that of sorafenib on human hepatocellular carcinoma HepG2 cell line.


Subject(s)
Humans , Antineoplastic Agents , Chemistry , Pharmacology , Cell Line, Tumor , Cell Proliferation , Drug Design , Drug Screening Assays, Antitumor , Molecular Structure , Niacinamide , Chemistry , Pharmacology , Phenylurea Compounds , Chemistry , Pharmacology , Structure-Activity Relationship
19.
Chinese Journal of Stomatology ; (12): 414-418, 2012.
Article in Chinese | WPRIM | ID: wpr-281597

ABSTRACT

<p><b>OBJECTIVE</b>To compare the efficacy of computer-navigated surgery and the 3-D skull models and guide plates for the treatment of unilateral delayed zygomatic fractures.</p><p><b>METHODS</b>Eleven patients with unilateral delayed zygomatic fractures were treated by computer-navigated surgery (test group) and another 12 patients were treated by 3-D skull models and guide plates as the control group. Quality of reduction was assessed by examination of postoperative axial CT scans through zygomatic arch, the malar prominence and the width of zygomatic arch were measured in both groups.</p><p><b>RESULTS</b>The difference between bilateral malar prominence was (0.94 ± 0.73) mm in the test group and (1.88 ± 1.82) mm in the control group, there was no significant difference between the two groups (P > 0.05). The difference between bilateral width of zygomatic arch was (0.77 ± 0.51) mm in the test group, less than (3.00 ± 1.81) mm in the control group (P < 0.05). Excessive malar prominence was observed in 6 cases (6/11) in the test group and in 7 cases (7/12) in the control group, whereas malar depression was observed in 5 cases (5/11) in the test group and in 5 cases (5/12) in the control group. Overcorrection of the width of zygomatic arch was observed in 6 cases (6/11) in the test group and in 12 cases (12/12) in the control group, whereas under correction was observed in 5 cases (5/11) in the test group and in 0 cases (0/12) in the control group.</p><p><b>CONCLUSIONS</b>In the treatment of unilateral delayed zygomatic fractures, symmetry of malar prominence can be achieved by application of computer-navigated surgery or the 3-D skull models and guide plates. Symmetry of the width of zygomatic arch achieved with the computer-navigated surgery is better than that achieved with 3-D skull models and guide plates.</p>


Subject(s)
Adult , Female , Humans , Male , Middle Aged , Young Adult , Fracture Fixation, Internal , Surgery, Computer-Assisted , Tomography, X-Ray Computed , Zygoma , Diagnostic Imaging , General Surgery , Zygomatic Fractures , Diagnostic Imaging , General Surgery
20.
Chinese Journal of Stomatology ; (12): 657-661, 2012.
Article in Chinese | WPRIM | ID: wpr-260215

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate the efficiency of navigation system for orbital wall reconstruction in unilateral orbital fractures.</p><p><b>METHODS</b>Fifteen patients (7 male and 8 female) with unilateral orbital fracture underwent orbital reconstruction with the help of intraoperative navigation system. The average age was 34.3 ± 9.5 years. All patients underwent spiral CT scanning preoperatively, and the CT data was imported to the BrainLab navigation system (Germany, BrainLab company). The orbit of the intact side was mirrored to the opposite side as the reference for pre-operative planning. The titanium mesh was mounted on the resin template made by rapid prototyping machine based on the mirrored CT data. When the injury was limited, the hydroxyapatite sheet was used for the orbital wall reconstruction. During the operation, the real-time navigation helped to ensure precise placement. The re-establishing result was assessed based on the postoperative CT data with the following four variables: the volumetric difference between the bilateral orbit, the volume of the herniated soft tissue, the global projection and the discrepancy between the simulated and the achieved position of the reconstructed orbital wall. The reconstructive discrepancy was measured only in the titanium plate grafting cases.</p><p><b>RESULTS</b>There were no serious complications such as infection, graft rejection and optic nerve injury in any case. Preoperatively, the average degree of enophthalmos was (3.5 ± 1.6) mm, the average volumetric difference between the injured and the unaffected orbit was (4.5 ± 1.8) ml, and the average volume of the herniated orbital soft tissue was (2.1 ± 0.7) ml. Postoperatively, the three values were respectively reduced to (1.3 ± 0.6) mm, (1.8 ± 0.9) ml and (0.7 ± 0.3) ml. The discrepancy of the medial and inferior wall were (2.5 ± 0.6) mm and (2.1 ± 0.4) mm.</p><p><b>CONCLUSIONS</b>The intraoperative use of navigation system for the orbital wall reconstruction in unilateral orbital fractures can provide reliable accuracy and achieve satisfactory results.</p>


Subject(s)
Adult , Female , Humans , Male , Computer Simulation , Enophthalmos , Diagnostic Imaging , General Surgery , Orbit , Diagnostic Imaging , General Surgery , Orbital Fractures , Diagnostic Imaging , General Surgery , Plastic Surgery Procedures , Methods , Surgery, Computer-Assisted , Surgical Mesh , Titanium , Tomography, X-Ray Computed
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