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1.
Chinese Journal of Applied Clinical Pediatrics ; (24): 702-705, 2022.
Article in Chinese | WPRIM | ID: wpr-930500

ABSTRACT

Objective:To analyze the influential factors of hypothermia in congenital heart disease (CHD) after cardiopulmonary bypass (CPB) rewarming using the decision tree model, thus providing theoretical basis for medical staff.Methods:A total of 711 CHD children who underwent surgery in the Shanghai Children′s Medical Center from January 1, 2019 to April 30, 2019 were retrospectively analyzed.A decision tree model was established to predict the risk factors for hypothermia in CHD children following CPB.Results:The decision tree model showed that CPB program, preoperative nutrition score and body surface area were the high-risk factors for hypothermia in CHD children after CPB rewarming.The accuracy, sensitivity, specificity of the decision tree model were 86.45%, 77.14% and 90.97%, respectively, and the area under the receiver operating characteristic curve was 0.851(95% CI: 0.798-0.904). Conclusions:Decision tree model has a high application value in predicting hypothermia in CHD children following CPB.It contributes to identify the influential factors of hypothermia, and provides references for performing preventive treatment and nursing measures to control the risk of hypothermia.

2.
Chinese Journal of Clinical Infectious Diseases ; (6): 46-53,80, 2021.
Article in Chinese | WPRIM | ID: wpr-884834

ABSTRACT

Objective:To analyze the distribution of clinically isolated fungal strains and their resistance to common antifungal drugs in Shandong province.Methods:Through the Shandong Children’s Bacterial & Fungal Drug Resistance Surveillance and Research Collaborative Network, a total of 1 030 fungi were collected in 46 hospitals of Shandong province from January 1 to December 31, 2018. The source and type of strains were analyzed, and antifungal drug sensitivity tests were performed by using the micro-dilution method. Whonet 5.6 and SPSS 22.0 were applied to analyze the data.Results:The overall main strains were Candida albicans (38.74%, 399/1 030), Candida tropicalis (16.99%, 175/1 030) and Candida parapsilosis (16.41%, 169/1 030); the main fungi strains in child patients were C. albicans (52.50%, 63/120), C. parapsilosis (12.50%, 15/120) and C. tropicalis (9.17%, 11/120); the main fungi strains in adult patients were C. albicans (36.37%, 331/910), C. tropicalis (17.03%, 155/910) and C. parapsilosis (15.27%, 139/910). The isolation rate of main Candida strains from January to March and August to December was much higher than that of other months. The drug resistance rates of C. albicans to fluconazole and voriconazole were 7.14% and 7.43%, respectively, and the drug resistance rates to itraconazole were 50.44%. The resistance rates of C. tropicalis to fluconazole, voriconazole and itraconazole were 29.05%, 23.29% and 48.65%, respectively. The sensitivity rates of C. parapsilosi to fluconazole, voriconazole and itraconazole were 93.06%, 93.75% and 94.44%, respectively. Candida glabrata showed a dose-dependent sensitivity rate of 2.33% to fluconazole. Analysis of 244 blood fungi strains showed that non-candida albicans bacteremia accounted for 70.08%. In the pathogen spectrum covering 92.22%, fluconazole was sensitive to 64.65% of the pathogens, voriconazole was 68.88%, and amphotericin B was 88.75%. After quantification, the effective rates of fluconazole, voriconazole and amphotericin B in the clinical treatment of fungal bacteremia were 70.10%, 74.69% and 96.23%, respectively. Among them, the sensitivity rate of voriconazole to C. tropicalis was lower than that of fluconazole. Conclusions:Candida is the main clinical fungus isolates in hospitals of Shandong province. The resistance rate of C. tropicalis to azole antifungal drugs is on the rise, and the sensitivity of other Candida species to clinically used antifungal drugs is basically stable.

3.
Journal of Biomedical Engineering ; (6): 875-884, 2020.
Article in Chinese | WPRIM | ID: wpr-879215

ABSTRACT

Glaucoma is the leading cause of irreversible blindness, but its early symptoms are not obvious and are easily overlooked, so early screening for glaucoma is particularly important. The cup to disc ratio is an important indicator for clinical glaucoma screening, and accurate segmentation of the optic cup and disc is the key to calculating the cup to disc ratio. In this paper, a full convolutional neural network with residual multi-scale convolution module was proposed for the optic cup and disc segmentation. First, the fundus image was contrast enhanced and polar transformation was introduced. Subsequently, W-Net was used as the backbone network, which replaced the standard convolution unit with the residual multi-scale full convolution module, the input port was added to the image pyramid to construct the multi-scale input, and the side output layer was used as the early classifier to generate the local prediction output. Finally, a new multi-tag loss function was proposed to guide network segmentation. The mean intersection over union of the optic cup and disc segmentation in the REFUGE dataset was 0.904 0 and 0.955 3 respectively, and the overlapping error was 0.178 0 and 0.066 5 respectively. The results show that this method not only realizes the joint segmentation of cup and disc, but also improves the segmentation accuracy effectively, which could be helpful for the promotion of large-scale early glaucoma screening.


Subject(s)
Humans , Diagnostic Techniques, Ophthalmological , Fundus Oculi , Glaucoma/diagnostic imaging , Neural Networks, Computer , Optic Disk/diagnostic imaging
4.
Acta Pharmaceutica Sinica ; (12): 565-573, 2019.
Article in Chinese | WPRIM | ID: wpr-780127

ABSTRACT

Disulfiram (DSF) is a traditional anti-alcohol drug, but it was recently found that DSF has strong inhibitory effect on the growth of a variety of cancer cells. However, its clinical application is greatly limited due to its poor solubility, instability in gastrointestinal tract and short plasma half-life. In this study, DSF is fabricated into nanosuspensions with the aim of trying to solve these problems. DSF nanosuspensions (DSF-NSps) were prepared by the anti-solvent precipitation method under ultrasonication, and the suitable stabilizer was screened according to the size, polydispersity index (PDI), and zeta potential of the resultant nanosuspensions, along with their particle size change during the storage at room temperature. The particle size, PDI, and zeta potential of DSF-NSps were determined using dynamic light scattering method, while the morphology of DSF-NSps was observed by transmission electronic microscope (TEM). The stability of DSF-NSps in media was examined according to their particle size change in different physiological media. The concentration of DSF was measured by HPLC assay. The in vitro drug release was evaluated on basis of dialysis. MTT assay was employed to evaluate the in vitro cytotoxicity of DSF-NSps against cancer cell lines. The 4T1 tumor-bearing mouse model was used to evaluate the in vivo therapeutic efficacy of DSF-NSps. All the animal experiments were acquired according to the Regulations for Animal Experiments and Guidelines for Ethical as defined by Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College. As a result, the combinational use of soyabean lecithin (SPC) and D-alpha tocopherol acid polyethyene glycol succinate (TPGS) was determined to best stabilize DSF-NSps when the ratio of DSF-SPC-TPGS was 24∶20∶4 (weight ratio), with small particle size and good storage stability. The resultant DSF-NSps showed a regular spherical morphology and drug loading content of (45.36 ± 2.09) %, with average particle size of 175.00 ± 0.75 nm, PDI of 0.24 ± 0.07 and zeta potential of -14.3 mV. DSF-NSps displayed good particle size stability in a variety of biological media including phosphate buffer saline, normal saline, 5% glucose, artificial gastric fluid, artificial intestinal fluid and plasma, which would meet the demand of both intravenous and oral administration. The in vitro study demonstrated that nano-encapsulation greatly increased the stability of DSF in aqueous media, DSF-NSps exhibited sustained release of the encapsulated drug and significantly inhibited 4T1 cells compared to free DSF (IC50, 1.07 vs 5.53 μg·mL-1, P<0.01). DSF-NSps showed a good dose-response relationship on the 4T1 tumor-bearing mice with the tumor inhibition rates at the three doses being 80.22%, 75.14% and 66.10%, all higher than that of paclitaxel injections (55.01%, P<0.05). The in vivo biodistribution study displayed that DSF-NSps were mainly distributed into liver, spleen and tumor. In sum, disulfiram nanoparticles could be expected to provide an effective anti-cancer drug for the treatment of breast cancer.

5.
China Journal of Chinese Materia Medica ; (24): 774-780, 2019.
Article in Chinese | WPRIM | ID: wpr-777496

ABSTRACT

In this experiment,the antioxidant capacity of raspberry extract and the protective effect on liver injury induced by ConA in mice were investigated. Balb/C male mice were randomly divided into six groups: normal group,model group,bicyclol control group( 200 mg·kg~(-1)),low-dose raspberry extract group( 200 mg·kg~(-1)),middle-dose raspberry extract group( 400 mg·kg~(-1)),and highdose raspberry extract group( 800 mg·kg~(-1)). Each group was intragastrically administered with drugs according to the body weight once a day. Seven days later,all of the groups except for the normal group were treated with ConA( 20 mg·kg~(-1)) through tail vein injection to establish the acute liver injury model. The mice were put to death 8 hours later. The organ indexes were calculated. These rum levels of ALT,AST and LDH and the activities of SOD,CAT,GSH and MDA in liver tissue were detected. HE staining was used to observe the pathological changes of liver tissue in mice. Western blot was used to detect the expressions of Bax,Bcl-2,Nrf2 and Keap-1. The antioxidant capacity of raspberry extract was measured by CAA assay. The results showed that,raspberry extract had a strong antioxidant capacity. Simultaneously,compared with the model group,raspberry extract can significantly improve the pathological conditions of liver,and significantly reduce ALT,AST and LDH activities in serum of liver injury mice( P<0. 01). The activities of SOD,CAT in liver homogenate supernatant were significantly increased in the high-dose group,the content of GSH increased,while the content of MDA was sharply declined in the high-dose group( P<0. 01). Meanwhile,raspberry extract down-regulated the expressions of Bax and Keap-1 and up-regulated the expressions of Bcl-2 and Nrf2. CAA showed that the compound raspberry extract had a strong antioxidant capacity. Therefore,raspberry extract has an obvious protective effect on acute liver injury induced by ConA in mice.


Subject(s)
Animals , Male , Mice , Antioxidants , Chemical and Drug Induced Liver Injury , Liver , Mice, Inbred BALB C , Protective Agents , Rubus
6.
Chinese Pharmacological Bulletin ; (12): 648-653, 2019.
Article in Chinese | WPRIM | ID: wpr-857257

ABSTRACT

Aim To study the protective effect of scutellarin (Scu) on ischemia/reperfusion (I/R) injury in isolated rat hearts and its mechanism. Methods Acute myocardial I/R injury was induced by Lange-ndorff perfusion in isolated rat hearts. SD rats were randomly divided into five groups; blank group, model group, low, medium and high dose group of Scu (0.3, 3, 30 mg • kg-1). The drug experimental group was perfused with K-H solution containing Scu (0. 3, 3, 30 mg • L-1) in vitro perfusion. Myocardial contractile function was recorded; AST, CK and LDH activities in rat myocardium were detected by kit; ICAM-1, IL-ip, IL-6, IL-18 and TNF-α were detected by ELISA; the morphological changes of myocardium were observed by HE staining; and the expressions of IL-1 p, NLRP3 and NF-kB were detected by Western blot. Results Compared with blank group, the contractile function of isolated rat heart in model group significantly decreased, the activities of AST, CK and LDH in myocardium significantly increased, and the contents of inflammatory factors such as ICAM-1, IL-lp, IL-6, IL-18 and TNF-a significantly increased. The expression of IL-1 (3 and NLRP3 and the nuclear translocation of NF-kB significantly increased. Scu significantly improved the above pathological changes. Conclusion The protective effect of Scu on myocardial I/R injury may be related to the inhibition of NF-KB/NLRP3/IL-1 p pathway.

7.
Chinese Journal of Radiation Oncology ; (6): 509-513, 2019.
Article in Chinese | WPRIM | ID: wpr-755061

ABSTRACT

Objective To systematically evaluate the efficacy and safety of brachytherapy (BT) combined with external beam radiation therapy (EBRT) and EBRT alone for prostate cancer.Methods Databases including PubMed,Web of Science,Cochrane Library,CNKI,WanFang Data and VIP were searched from the inception to July 2018 to collect the clinical trials which comparatively analyzed the efficacy and safety between EBRT plus BT and EBRT alone for prostate cancer.According to the inclusion and exclusion criteria,data of the included studies were extracted and the methodological quality was evaluated.Then,a meta-analysis was performed using RevMan 5.3.Results Ten studies of 23 393 patients were included,in which 6 were randomized controlled trials (RCTs) and the other 4 were non-RCTs.The 3-year biochemical progression-free survival (b-PFS)[OR=2.03(95%CI:1.11 to 3.73),P=0.02] and the 5-year b-PFS of intermediate-risk patients[OR=2.27(95%CI:1.49 to 3.45),P<0.01] in the EBRT+BT group were significantly higher compared with those in the EBRT group.The 3-and 5-year b-PFS,5-year overall survival and 5-year metastasis-free survival did not differ between two groups.in the incidence of ≥ grade 2 acute[OR=1.44(95%CI:1.11 to 1.38),P<0.01] and chronic genitourinary adverse reactions [OR=3.06(95%CI:1.37 to 6.80),P<0.01],≥ grade 3 acute[OR=1.75 (95%CI:1.14 to 2.69),P=0.01] and chronic genitourinary adverse reactions[OR=3.41(95%CI:2.42 to 4.82),P<0.01] in the EBRT group were significantly lower than those in the EBRT+BT group.The incidence of gastrointestinal adverse reactions did not significantly differ between two groups.Conclusion Compared with EBRT alone,EBRT combined with BT can effectively improve the 3-and 5-year b-PFS,whereas increase the incidence of genitourinary adverse reactions for patients with intermediate-risk prostate cancer.

8.
Chinese Traditional and Herbal Drugs ; (24): 368-373, 2018.
Article in Chinese | WPRIM | ID: wpr-852249

ABSTRACT

Objective To investigate the effects of cultivated Cordyceps sinensis on inhibiting the proliferation and migration of B16 melanoma cells. Methods MTT assay and clone formation assay were used to examine the inhibitory effect of cultivated C. sinensis on the proliferation of B16 cells; Scratching test and transwell assay were used to detect its effect on migration; Cell adhesion assay was used to detect its effect on adhesion. Flow cytometry was used to detect its effect on cell cycle arrest; Western blotting was used to detect its effect on the expression of the proteins of MMP-2, MMP-9, Bax, Bcl-2, CyclinD1, CDK2, CDK4, P21, and p-Akt. Results The results showed that cultivated C. sinensis can significantly inhibit the proliferation and clone formation of B16 cells via arresting cells at G1/S phase in a dose-dependent manner. Moreover, cell migration was also substantially inhibited in a dose-dependent manner. Western blotting analysis showed that cultivated C. sinensis obviously increased the levels of Bax and P21, and meanwhile, decreased the expression of Bcl-2, MMP-2, MMP-9, CDK2, CDK4, CyclinD1, and p-Akt. Conclusion The inhibitory effects of cultivated C. Sinensis on the proliferation and migration of B16 cells probably associated with the expression of related regulating proteins, MMPs family proteins and p-Akt protein in cell cycle.

9.
Chinese Traditional and Herbal Drugs ; (24): 1525-1532, 2018.
Article in Chinese | WPRIM | ID: wpr-852064

ABSTRACT

Objective: Based on structural modification of monomeric compound calenduloside E from Aralia elata, to evaluate anti-inflammatory activity of the analogues. Methods: Applying oleanolic acid as starting material, the target compounds were prepared by seven steps reactions and evaluated for anti-inflammatory effects by RAW264. 7 cells in vitro. Results: Ten analogues G1-G5 and H1-H5 were synthesized. The structures of the target compounds were identified by spectrum. Pharmacological results showed that all of the compounds had different levels potency of anti-inflammatory effects in cells. In particular, compounds G1-G4 and H1-H3 showed significant anti-inflammatory activity comparing wiht lead compounds. Conclusion: The new compounds G1-G5 and H1-H5 which showed potential of anti-inflammatory biological activity, had not been reported in any literatures and deserved further research.

10.
Chinese Traditional and Herbal Drugs ; (24): 4507-4512, 2018.
Article in Chinese | WPRIM | ID: wpr-851650

ABSTRACT

Objective To evaluate the anti-lipid metabolic disorder activities of these compounds in vitro, the natural caffeic acid amide derivatives were designed and synthesized. Methods Using caffeic acid as start material, BOP as a condensing agent, and the target compounds were sequentially prepared with fourteen amines, and then the lipid-regulating effect was evaluated using HepG2 cells. Results Fourteen caffeic acid amide compounds CA1-CA14 were synthesized. The structures of the target compounds were identified by spectrum. Pharmacological results showed that fourteen derivatives have potency of lipid-regulating in different levels. In particular, compound CA6 showed significant lipid-regulating effects compared to the lead compounds caffeic acid and Simvastatin. Conclusion Compound CA6, CA7, and CA11 had not been reported in any literatures before. Among them, the novel compounds CA6 and CA11 have showed potential of lipid-regulating activities, and deserved further research.

11.
Chinese Traditional and Herbal Drugs ; (24): 4945-4948, 2018.
Article in Chinese | WPRIM | ID: wpr-851643

ABSTRACT

Sophocarpine is an alkaloid extracted from the dry roots and ground parts of Leguminous Sophora flavescens or S. alopecuroides. Sophocarpine has a wide range of sources, it is abundant in S. flavescens and S. alopecuroides, and it is easy to extract. Sophocarpine has a wide range of pharmacological effects, such as antitumor, anti-inflammatory and analgesia, antivirus, liver protection, cardiovascular protection and so on. In this paper, the pharmacological effects of sophocarpine were reviewed in order to provide references for the treatment of related diseases and new drug research and development.

12.
Chinese Pharmacological Bulletin ; (12): 544-550, 2018.
Article in Chinese | WPRIM | ID: wpr-705082

ABSTRACT

Aim To probe into the bavachinin toxic mechanisms in HepaRG cells. Methods MTT assay was used to determine toxicity and dose. After treated with 6.25,12.5 and 25 μmol·L-1bavachinin for 24 h,the cell death was investigated by Hoechst 33342/PI,LDH,caspase-3 activity,and Bax,Bcl-2 expression levels. Mitochondrial damage was detected by mito-chondrial membrane potential,ATP content,openness of mitochondrial permeability transition pore and cyto-chrome C level. Results Bavachinin administration up-regulated Bax/Bcl-2 ratio and caspase-3 activity with increase of drug concentration after 24 h. Apop-totic rate increased in a dose-dependent manner be-tween 6.25 and 25 μmol·L-1,but when reached to 25 μmol·L-1,cells showed more necrosis. Mitochon-drial injury indicators significantly increased after 24h. Conclusion Bavachinin induces HepaRG cell apopto-sis and necrosis through mitochondria injury.

13.
Chinese Journal of Tissue Engineering Research ; (53): 2227-2232, 2018.
Article in Chinese | WPRIM | ID: wpr-698687

ABSTRACT

BACKGROUND:Various surface modification techniques have been utilized as an attempt to improve the osteointegration of Ti-based implants, which is a hotspot research concerning the artificial joint prosthesis. OBJECTIVE:To evaluate the effect of silicon doped zirconia film on the titanium surface on relevant factors of osteoblast-like MG63 cells. METHODS:Silicon doped zirconia and zirconia films were respectively prepared on the titanium surface by cathodic arc deposition. Osteoblast-like MG63 cells were cultured on silicon doped zirconia film, zirconia film and pure titanium, respectively. After 1, 4, 7, 10 days of incubation, samples were collected for assay. Osteoprotegerin (OPG) and receptor activator of nuclear factor κB ligand (RANKL) at mRNA and protein levels were detected using real-time PCR and ELISA, respectively. RESULTS AND CONCLUSION:(1) At 1 day of inoculation, there was no significant difference in the OPG mRNA and protein expression among the three groups. At 4 days of inoculation, the expression of OPG mRNA and protein in the silicon doped zirconia film and zirconia film groups was significantly higher than that in the pure titanium group (P<0.05), but there was no significant difference between the former two groups. At 7 and 10 days of inoculation, the expression of OPG mRNA and protein in the silicon doped zirconia film growp was highest among the three groups (P<0.05). (2) At 1 day of inoculation, there was no significant difference in the RANKL mRNA and protein expression among the three groups. At 4 and 7 days of inoculation, the expression of RANKL mRNA and protein in the silicon doped zirconia film group was significantly lower than that in the other two groups (P<0.05). At 10 days of inoculation, the expression of OPG mRNA and protein in the silicon doped zirconia film and zirconia film groups was significantly higher than that in the pure titanium group (P<0.05), but there was no significant difference between the former two groups. To conclude, silicon doped zirconia film fabricated by cathodic arc deposition can enhance the expression of OPG and reduce the expression of RANKL at the same time.

14.
Acta Pharmaceutica Sinica ; (12): 2113-2121, 2018.
Article in Chinese | WPRIM | ID: wpr-780095

ABSTRACT

Annonaceous acetogenins (ACGs) are effective part extracted and separated from Annona squamosa seeds, they have good antitumor activity against a variety of tumor cells. However, the solubility of ACGs is poor with serious toxic and side effects, which greatly limits their application in clinical practice. In this study poloxamer 188 (P188) was selected as a drug carrier or a stabilizer to prepare ACGs nanosuspensions (ACGs-NSps) using anti-solvent precipitation. The nanosuspensions were examined via dynamic light scattering (DLS) method to examine size of the nanosuspensions. Transmission electron microscopy was used to observe their morphology. HPLC assay was used to measure their drug loading content and the in vitro drug release. The stability of ACGs-NSps at room temperature, in various physiological media and plasma, and the hemolytic test and lyophilization were all investigated. MTT assay was performed to study the cytotoxocity of ACGs-NSps against four tumor cell lines. 4T1 bearing tumor model was used to assess their in vivo antitumor therapeutic efficacy. The obtained ACGs-NSps were spherical, the average particle size was 169.4±1.25 nm, the polydispersity index (PDI) value was 0.130±0.020, the zeta potential was -19.8 mV and the drug loading content was 48.18%. ACGs-NSps were stable at room temperature for at least 15 days. They could be lyophilized in the presence of 0.5% glucose and 2.0% P188. ACGs-NSps showed sustained in vitro drug release, and the cumulative drug release reached 80.82% within 144 hours. ACGs-NSps maintained their particle size in various physiological media, and plasma with no hemolysis and then met demands of both oral and intravenous administration. In contrast to free ACGs, ACGs-NSps displayed significantly higher cytotoxicity against 4T1 (IC50, 0.892±0.124 μg·mL-1 vs 2.495±0.108 μg·mL-1, P 50, 0.747±0.051 μg·mL-1 vs 2.204±0.064 μg·mL-1, P 50, 2.265±0.081 μg·mL-1 vs 4.159±0.071 μg·mL-1, P 50, 0.473±0.024 μg·mL-1 vs 1.196±0.022 μg·mL-1, P in vivo study demonstrated that the daily oral administration of ACGs-NSps (3 mg·kg-1) resulted in higher tumor inhibition rate compared to ACGs/oil solution (67.23% vs 53.11%), comparable to the intravenous injection of 0.5 mg·kg-1 ACGs-NSps every other day (70.34%). Nanosuspensions effectively solved the problem of ACGs insolubility and difficulty in drug delivery. Using P188, a pharmaceutic adjuvant approved by FDA for iv injection, the resultant ACGs-NSps appear promising as an anti-tumor drug that can be used in clinic.

15.
Acta Pharmaceutica Sinica ; (12): 453-459, 2018.
Article in Chinese | WPRIM | ID: wpr-779896

ABSTRACT

Gambogic acid (GA), the main active ingredient in gamboge, has been reported to have good anti-tumor activity with excellent selectivity. However, its clinical application is limited by the poor water solubility. GA nanosuspensions were designed in this study in order to solve this problem. GA nanosuspensions were prepared by microprecipitation method based on pH adjustment. Suitable stabilizer was screened according to the size and polydispersity index (PDI) of the resultant nanosuspensions. Dynamic light scattering method was used to measure the particle size and transmission electron microscopy was used to observe the morphology. The stability was studied in different medium. The drug release was evaluated using a dialysis method. MTT assay was used to assess their cytotoxicity in vitro against cancer cell line. Anti-tumor effect in vivo was investigated on H22-bearing mice. In result, Poloxamer (P188) was found to be a good stabilizer. The resultant GA nanosuspensions (GA-NSps) were 135.9 ±5.1 nm in diameter, with PDI value being 0.26 ±0.01 and the zeta potential being −35.1 ±1.36) mV. GA-NSps were nearly spherical. They were quite stable in various physiological media. GA-NSps exhibited a sustained drug release pattern, with the cumulative release reaching 90.26% within 312 h. In MTT assay, GA-NSps had a stronger cytotoxicity against HepG2 cells than the free drug (IC50, 0.851 8 μg·mL−1 vs 2.104 μg·mL−1, P vs 66.80%, P < 0.01). In summary, we prepared GA-NSps with high drug loading capacity, small particle size and good stability, and provided a solid basis for the effective dosage form of gambogic acid.

16.
Acta Pharmaceutica Sinica ; (12): 133-140, 2018.
Article in Chinese | WPRIM | ID: wpr-779856

ABSTRACT

Honokiol (HK) have extensive pharmacological activities, but its poor solubility and instability restricted its clinical application and efficacy exertion. HK nanosuspensions (HK-NSps) were designed in this study in order to solve the problems. HK-NSps were prepared by antisolvent precipitation method, using poly-vinylpyrrolidone (PVP) and bovine serum albumin (BSA) as a combined stabilizer. The particle size was measured using dynamic light scattering method, the morphology was observed by transmission electron microscopy. The size change and drug content of HK-NSps in various physiological media during the storage at ambient temperature was examined to evaluate their storage stability. Dialysis method was used to study their drug release in vitro. MTT assay was used to assess their in vitro cytotoxicity against 4T1 breast cancer cell line. Anti-tumor effect in vivo was also investigated in 4T1 tumor-bearing mice. HK-NSps were prepared with high drug loading content of 48.62%, nearly spherical shape and good storage stability. The average particle size was (83.40 ±1.042) nm, the polydispersity index (PDI) value was 0.223 ±0.011, the zeta potential was (-42.2 ±1.2) mV. HK-NSps showed sustained in vitro drug release and enhanced cytotoxicity in contrast to free HK against 4T1 cells (IC50, 8.36 μg·mL-1 vs 37.58 μg·mL-1, Pin vivo study on 4T1 tumor-bearing mice demonstrated that HK-NSps showed good dose-dependent tumor inhibition rate (TIR). In contrast to 4 mg·kg-1 of PTX injection (TIR, 47.9%), medium and high dose of HK-NSps displayed improved therapeutic efficacy (TIR, 55.67% for 40 mg·kg-1, 67.28% for 60 mg·kg-1, P-1) had TIR of only 54.13% even administrated every day. In conclusion, HK-NSps were prepared with small size, high drug-loading capacity, and good stability. The improved in vitro and in vivo antitumor efficacy demonstrated that HK can be a promising antitumor drug in combination with nanosuspensions technology.

17.
China Journal of Chinese Materia Medica ; (24): 755-759, 2018.
Article in Chinese | WPRIM | ID: wpr-771672

ABSTRACT

Trace chemical constituents from the ethyl acetate extract of Red Yeast Rice were investigated. Four phenolic compounds were isolated by various column chromatographies, and their structures were identified on the basis of spectroscopic analysis including UV, MS, IR and NMR. The four compounds were identified as 2-methyl-5-(2'R-methyl-4'-hydroxy-butyl)-cinnamic acid(1), 5-(2'-hydroxy-6'-methyl phenyl)-3-methylfuran-2-carboxylic acid(2), daidzein(3), and genistein(4). Compound 1 was new and 2 was firstly discovered from the genus Monascus, while 3-4 were obtained from Red Yeast Rice for the first time.


Subject(s)
Biological Products , Chemistry , Magnetic Resonance Spectroscopy , Monascus , Phenols , Chemistry
18.
Chinese Traditional and Herbal Drugs ; (24): 5270-5275, 2017.
Article in Chinese | WPRIM | ID: wpr-852332

ABSTRACT

Tetrahydroberberine (THB) belongs to the alkaloid of tetrahydroisoquinoline, which is derived from the roots of Corydalis yanhusuo and can also be hydrogenated from berberine. THB has a variety of significant biological activities compared to berberine. It is reported that THB has the effects of anti-hypertension, anti-arrhythmia, anti-fibrillation and against acute myocardial infarction, and also can treat and protect the injury of ischemic and reperfusion. Moreover, other research has found its effects upon anti-oxidant and regulating the functions of gastrointestinal tract. By searching literature of domestic and foreign from Pubmed, CNKI and other databases, pharmacological activities of THB were summarized in this paper, in order to provide reference for the further study of THB.

19.
Chinese Journal of Tissue Engineering Research ; (53): 296-302, 2017.
Article in Chinese | WPRIM | ID: wpr-508492

ABSTRACT

BACKGROUND:Silicon plays an essential role in bone development and bioactive silicate glasses pioneered the current era of bioactive materials. Various biomaterials have been developed based on the biological function of silicon. OBJECTIVE:To explore the biological function of silicon and research process of silicon in biomaterials. METHODS: A computer-based retrieval of CNKI, PubMed, SpringerLink and Elsevier ScienceDirect databases was performed to search the relevant literatures concerning the biological function of silicon and its application in biomaterials. Al data were primarily screened to exclude repeated and irrelevant articles. Literatures about the application of silicon in biomaterials were included. RESULTS AND CONCLUSION:A total of 68 eligible English articles are enroled. Silicon plays important chemical and biological roles in bone. Silicon in the extracelular matrix interacts with glycosaminoglycans and proteoglycans during their synthesis and form ionic substitutions in the crystal lattice structure of hydroxyapatite. In addition, the dissolution products of bioactive glass (mainly silicic acid) expose significant influence on the molecular biology of osteoblasts in vitro, and can regulate the expressions of several genes including osteoblastic markers, cel cycle regulators and extracelular matrix proteins. Silicon has been proved to improve the bioactivity of numerous materials and do no harm to their mechanical properties and without cytotoxicity.

20.
Chinese Journal of Tissue Engineering Research ; (53): 5382-5387, 2017.
Article in Chinese | WPRIM | ID: wpr-668610

ABSTRACT

BACKGROUND: Human amniotic mesenchymal stem cells (hAMSCs) are adult stem cells with multipotential differentiation, which can be induced to differentiate into bone, cartilage and other connective tissues. Meanwhile, as a highly specific marker of tenocytes, Scleraxis is involved in aggregation and differentiation of tendon progenitor cells as well as the formation of tendon extracellular matrix. OBJECTIVE: To investigate whether hAMSCs have the ability of differentiation into tenocytes by ectopic expression of Scleraxis. METHODS: Agreed by puerpera, the amniotic membrane from the full-term placenta was separated, and hAMSCs were isolated by a two-step enzyme digestion, observed under inverted phase contrast microscope, and identified by flow cytometry. Passage 3 cells were induced via plasmid-mediated Scleraxis overexpression in overexpression group. Untransfected cells cultured in normal medium served as blank control group, and those with empty plasmid transfection were defined as empty plasmid group. Cell proliferation was tested in each group using cell counting kit-8 within 7 days of culture. Real-time quantitative PCR and western blot were used to assess the tenogenic differentiation of hAMSCs in each group at 3 and 7 days of culture. RESULTS AND CONCLUSION: Findings from the cell counting kit-8 indicated that the cell viability had no significant differences among the groups within 7 days of culture (P > 0.05). Western blot results showed the protein expression of Scleraxis in the treatment group was significantly higher than that in the other two groups (P < 0.05). Real-time PCR results showed, at 3 days of culture, the expression of collagen type I, collagen type III, Fibronectin and Tenascin-C in the overexpression group was significantly higher than that in the empty plasmid group (P < 0.05), but the expression of Tenomodulin had no difference (P > 0.05); at 7 days of culture, the expressions of collagen type I, collagen type III, Fibronectin, Tenascin-C and Tenomodulin in the overexpression group were significantly higher than those in the empty plasmid group (P < 0.05). In summary, hAMSCs can be differentiated into tenocytes by ectopic expression of Scleraxis.

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