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1.
Chinese Journal of Pediatrics ; (12): 49-54, 2024.
Article in Chinese | WPRIM | ID: wpr-1013248

ABSTRACT

Objective: To analyze the clinical characteristics and prognosis of patients with infant acute lymphoblastic leukemia (IALL). Methods: A retrospective cohort study.Clinical data, treatment and prognosis of 28 cases of IALL who have been treated at Beijing Children's Hospital, Capital Medical University and Baoding Children's Hospital from October 2013 to May 2023 were analyzed retrospectively. Based on the results of fluorescence in situ hybridization (FISH), all patients were divided into KMT2A gene rearrangement (KMT2A-R) positive group and KMT2A-R negative group. The prognosis of two groups were compared. Kaplan-Meier method and Log-Rank test were used to analyze the survival of the patients. Results: Among 28 cases of IALL, there were 10 males and 18 females, with the onset age of 10.9 (9.4,11.8) months. In terms of immune classification, 25 cases were B-ALL (89%), while the remaining 3 cases were T-ALL (11%). Most infant B-ALL showed pro-B lymphocyte phenotype (16/25,64%). A total of 22 cases (79%) obtained chromosome karyotype results, of which 7 were normal karyotypes, no complex karyotypes and 15 were abnormal karyotypes were found. Among abnormal karyotypes, there were 4 cases of t (9; 11), 2 cases of t (4; 11), 2 cases of t (11; 19), 1 case of t (1; 11) and 6 cases of other abnormal karyotypes. A total of 19 cases (68%) were positive for KMT2A-R detected by FISH. The KMT2A fusion gene was detected by real-time PCR in 16 cases (57%). A total of 24 patients completed standardized induction chemotherapy and were able to undergo efficacy evaluation, 23 cases (96%) achieved complete remission through induction chemotherapy, 4 cases (17%) died of relapse. The 5-year event free survival rate (EFS) was (46±13)%, and the 5-year overall survival rate (OS) was (73±10)%.The survival time was 31.3 (3.3, 62.5) months. There was no significant statistical difference in 5-year EFS ((46±14)% vs. (61±18)%) and 5-year OS ((64±13)% vs. (86±13)%) between the KMT2A-R positive group (15 cases) and the KMT2A-R negative group (9 cases) (χ2=1.88, 1.47, P=0.170, 0.224). Conclusions: Most IALL patients were accompanied by KMT2A-R. They had poor tolerance to traditional chemotherapy, the relapse rate during treatment was high and the prognosis was poor.


Subject(s)
Male , Child , Infant , Female , Humans , Retrospective Studies , In Situ Hybridization, Fluorescence , Prognosis , Precursor Cell Lymphoblastic Leukemia-Lymphoma/therapy , Abnormal Karyotype , Recurrence
2.
Journal of Southern Medical University ; (12): 710-717, 2023.
Article in Chinese | WPRIM | ID: wpr-986980

ABSTRACT

OBJECTIVE@#To screen for small molecular compounds with selective inhibitory activity against cutaneous melanoma cells with BAP1 deletion.@*METHODS@#Cutaneous melanoma cells expressing wild-type BAP1 were selected to construct a BAP1 knockout cell model using CRISPR-Cas9 system, and small molecules with selective inhibitory activity against BAP1 knockout cells were screened from a compound library using MTT assay. Rescue experiment was carried out to determine whether the sensitivity of BAP1 knockout cells to the candidate compounds was directly related to BAP1 deletion. The effects of the candidate compounds on cell cycle and apoptosis were detected with flow cytometry, and the protein expressions in the cells were analyzed with Western blotting.@*RESULTS@#The p53 activator RITA from the compound library was shown to selectively inhibit the viability of BAP1 knockout cells. Overexpression of wild-type BAP1 reversed the sensitivity of BAP1 knockout cells to RITA, while overexpression of the mutant BAP1 (C91S) with inactivated ubiquitinase did not produce any rescue effect. Compared with the control cells expressing wild-type BAP1, BAP1 knockout cells were more sensitive to RITA-induced cell cycle arrest and apoptosis (P < 0.0001) and showed an increased expression of p53 protein, which was further increased by RITA treatment (P < 0.0001).@*CONCLUSION@#Loss of BAP1 results in the sensitivity of cutaneous melanoma cells to p53 activator RITA. In melanoma cells, the activity of ubiquitinase in BAP1 is directly related to their sensitivity to RITA. An increased expression of p53 protein induced by BAP1 knockout is probably a key reason for RITA sensitivity of melanoma cells, suggesting the potential of RITA as a targeted therapeutic agent for cutaneous melanoma carrying BAP1-inactivating mutations.


Subject(s)
Humans , Melanoma , Skin Neoplasms , Tumor Suppressor Protein p53 , Apoptosis , Cell Division , Tumor Suppressor Proteins/genetics , Ubiquitin Thiolesterase/genetics
3.
Acta Pharmaceutica Sinica ; (12): 405-412, 2023.
Article in Chinese | WPRIM | ID: wpr-965701

ABSTRACT

To improve the stability of amino acid ester derivatives of DB02, a series of 24 amide derivatives of DB02 amino acids as non-nucleoside HIV-1 reverse transcriptase inhibitor were designed and synthesized based on bioisosterism by replacing amino acid ester scaffold with more stable amide bond. The anti-HIV-1 activity of these compounds was evaluated by MTT assay and counting the number of syncytia. Most of the target compounds showed a potential anti-HIV-1 activity, among which compounds 2d, 2i, 2l, 2s, and 2w had better antiviral effect than lead compound DB02, with a therapeutic index > 1 000.00. Finally, the structure-activity relationship of these compounds was discussed, which provided new ideas for the further development of DB02 derivatives.

4.
Chinese Pharmacological Bulletin ; (12): 740-748, 2022.
Article in Chinese | WPRIM | ID: wpr-1014213

ABSTRACT

Aim To explore the effeets of Salvianolie aeirl A (SAA) on platelet recruitment, activation and neutrophils in heart of myocardial infarction ( Ml ) mice.Methods C57BL/6 mice were randomly divid¬ed into: Sham operation group.Ml model group, SAA (5, 10 mg • kg 1 ) group, tirofiban (Tirofiban, 0.87 mg • kg ' ) group, using tail vein injection for 3 d.Echocardiography and HE staining were used to detect mouse heart function and infarct area; 1HC, FCS, ELISA, Western blot and other methods were used to explore the inhibitory effect of SAA on platelet and neutrophil activation.Results Compared with Ml group, SAA could improve the cardiac function and cardiac physiology changes of Ml mice, reduce the ex¬pression of CD42c in myocardial tissue and CD62p in peripheral blood without affecting tail bleeding time, reduce ADP-induced platelet activation and increase p- VASP/VASP ratio, reduce the ratio of p-PI3K/PI3K and p-AKT/AKT, reduce the expression of CD45, Ly6G, CXCL1 and CXCL2 in myocardial tissue, re¬duce the expression of complement component C3aR in myocardial tissue, and reduce C3a-induced NE and MPO, MMP9, LF level.Conclusions SAA has an anti-platelet activation effect by inhibiting the PI3K/ AKT and VASP pathways and an anti-neutrophil acti¬vation effect by inhibiting the expression of C3aR and C3a.

5.
Chinese Pharmacological Bulletin ; (12): 662-668, 2021.
Article in Chinese | WPRIM | ID: wpr-1014415

ABSTRACT

Aim To explore the effect of chrysin on chondrocyte autophagy in rat chondrocyte osteoarthritis model induced by lipopolysaccharide and its mechanism. Methods Normal articular cartilage cells of 10 SPF SD rats were isolated and cultured in vitro, and the autophagy of rat chondrocytes was induced by LPS. The experiment was divided into blank control group, LPS group, chrysin (CHR) group and LPS + CHR group, the activity of cells in each group was detected by CCK-8 method, the mitochondrial membrane potential of cells in each group was detected by Rhodaminel23, and the protein expression of PI3K, AKT, p-PI3K, p-AKT, Beclin-1 and LC3 II in cells of each group was detected by reactive oxygen species, Western blot method of DCFH-DA. Results Chrysin could inhibit the autophagy induced by LPS, especially when the concentration of chrysin was 10 mmol · L

6.
Chinese Pharmacological Bulletin ; (12): 68-74, 2021.
Article in Chinese | WPRIM | ID: wpr-1014295

ABSTRACT

Aim To explore the effect of aucubin aucubin (AU), one of the effective ingredients of eucommia, plantain, rehmannia and other herbs, on cardiomyocyte apoptosis and cardiac function after acute myocardial infarction (MI) and the possible mechanisms. Methods In this study, the mouse models of MI were established by ligation of the anterior descending branch of the left coronary artery. Left ventricular function and the infarct size were detected using echocardiography and Masson staining. A Tumor necrosis factor-a (TNF-ot)/cycloheximide (C H X) model of cardiomyocyte injury was established, and the effects AU on myocardial injury were examined using IncuCyte live cell imaging, Western blot and TUNEL staining. Results AU administration dramatically improved cardiac function recovery and decreased infarct size after MI. AU inhibited the apoptosis of cardiomyocytes, reduced the expressions of caspase-3, and significantly increased the ratio of Bcl-2/Bax induced by TNF-ot/ CHX. Meanwhile, the estrogen receptor ß (ERß) protein level was elevated by AU, and the antiapoptotic effect of AU was blocked by ERß inhibitor. Conclusions AU can alleviate MI injury and improve cardiac function via inhibiting the apoptosis of cardiomyocytes, and its mechanism is the activation of ERß pathway.

7.
Journal of Southern Medical University ; (12): 401-408, 2019.
Article in Chinese | WPRIM | ID: wpr-772087

ABSTRACT

OBJECTIVE@#To explore whether bortezomib and a Bcl-2 inhibitor exhibit synergistic anti-tumor effect in human acute T lymphoblastic leukemia cells.@*METHODS@#MTT assay was used to determine the cytotoxicity of bortezomib in the absence or presence of Bcl-2 inhibitors (obatoclax, AT-101 and ABT-199) in Jurkat cells. The effects of drug treatment on the expression of Bcl-2 family proteins, LC3B, p62, ubiquitin, BiP/Grp78, p-JNK, p-p38 and CHOP proteins were examined by Western blotting. Flow cytometry was used to determine the effects of bortezomib and Bcl-2 inhibitors (obatoclax, AT-101 and ABT-199) on cell apoptosis. Quantitative real-time PCR was used to measure the mRNA expression levels of the key regulatory factors of unfolded protein reaction (UPR). A zebrafish xenograft model was used to study the anti-tumor effect of bortezomib, obatoclax and their combination in vivo.@*RESULTS@#Bortezomib or Bcl-2 inhibitors alone inhibited the cell viability of Jurkat cells, but only obatoclax and bortezomib showed synergistic cytotoxicity and pro-apoptotic effect. Obatoclax, rather than AT-101 and ABT- 199, blocked autophagic flux in the cells evidenced by concomitant accumulation of LC3B-Ⅱ and p62. Both bortezomib and obatoclax alone caused accumulation of polyubiquinated proteins, and their combination showed a synergistic effect, which was consistent with their synergistic cytotoxicity. The dual blockade of proteasome and autophagy by the combination of bortezomib and obatoclax triggered unfolded protein response followed by cell apoptosis. Preventing UPS dysfunction by tauroursodeoxycholic acid (TUDCA) significantly attenuated the cytotoxicity and pro-apoptotic effect of bortezomib in combination with obatoclax. In zebrafish xenograft models, bortezomib combined with obatoclax significantly decreased tumor foci formation.@*CONCLUSIONS@#Bortezomib and obatoclax for dual blockade of protein degradation pathways show synergistic anti-tumor effect in human acute T lymphoblastic leukemia cells.


Subject(s)
Humans , Antineoplastic Agents , Apoptosis , Bortezomib , Cell Line, Tumor , Drug Synergism , Precursor Cell Lymphoblastic Leukemia-Lymphoma , Proteolysis , Proto-Oncogene Proteins c-bcl-2 , Pyrroles
8.
Chinese Traditional and Herbal Drugs ; (24): 4099-4105, 2018.
Article in Chinese | WPRIM | ID: wpr-851733

ABSTRACT

Objective To explore the effect of astragaloside IV on the damaged blood-brain barrier (BBB) in vitro model induced by amyloid-beta protein (Aβ1-42) and the underlying mechanism. Methods Firstly, the non-contact co-culture blood-brain barrier (BBB) model was established by Aβ1-42-induced mouse brain microvascular endothelial cell (bEnd.3) and primary rat astrocyte (As). Then the mice were divided into four groups: control, model (Aβ1-42 30 μmol/L), astragaloside IV low and high dose groups (Aβ1-42 30 μmol/L with Astragaloside IV 50 and 200 μmol/L). The effect of astragaloside IV on the vitality of bEnd.3 induced by Aβ1-42 was detected by methyl thiazolyl tetrazolium (MTT) assay. The permeability of BBB in vitro was determined by detecting the quantity of fluorescein sodium through BBB in various groups. In order to explore the mechanism of its protection, the apoptosis related proteins Caspase-3, cleaved Caspase-3 and tight junction proteins ZO-1, Claudin-5 and Occludin were detected by Western blotting. Results Compared with model group, the astragaloside IV groups improved the activity of bEnd.3 cells significantly (P < 0.001). The protective effect was positively correlated with the concentration of astragaloside IV. Astragaloside IV with low and high dose decreased the permeability of BBB model in vitro (P < 0.001). According to the results of Western blotting, the ratio of cleaved Caspase-3/Caspase-3 was significantly declined, and the expression levels of ZO-1, Claudin-5 and Occludin were significantly increased in astragaloside IV groups (P < 0.05). Conclusion Astragaloside IV may play a BBB protective role by inhibiting the apoptosis of bEnd.3 cells induced by fibrous Aβ1-42 and increasing the expression of tight junction proteins.

9.
Pakistan Journal of Medical Sciences. 2017; 33 (4): 1022-1028
in English | IMEMR | ID: emr-188633

ABSTRACT

Objective: During the treatment of diseases such as angiocardiopathy, blood lipid abnormalities and metabolic syndrome, omega-3 unsaturated fatty acids [PUFA] can reduce plasma lipids and improve cardiovascular status, thus ameliorating disease severity. We aimed to explore the effects of PUFA supplementation in patients with non-alcoholic fatty liver disease [NAFLD]


Methods: A systematic literature search was performed during March 2016 for randomized controlled trials using PUFA or fish oil supplementation in patients with NAFLD or non-alcoholic steatohepatitis [NASH]


All Randomized controlled trials were retrieved from MEDLINE and EMBASE database up to date [March 2016]


A meta-analysis of key outcomes [serum level of liver enzymes and lipids] were identified in these studies. The mean difference [MD] and the corresponding 95% confidence intervals [CIs] were used as measures of effect size


Results: Thirteen studies were included, consisting of 266 patients in the PUFA group and 402 cases in the control group. Serum level of alanine aminotransferase [ALT] was lower in the PUFA group than that in in the controls [MD=-9.18, 95% Cl [-12.41, -5.96], P <0.00001]. However, PUFA treatment did not affect aspartate aminotransferase [AST] [MD=-5.Q7, 95% Cl [-12.65, 2.51], P= 0.19], gamma-glutamyl transferase [GGT] [MD=-1.91, 95% Cl [-4.15, 0.33], P <0.009]


Conclusions: PUFA supplementation may affects serum level of ALT and improve liver function in patients with NAFLD


Subject(s)
Humans , Female , Male , Fatty Acids, Omega-3/therapeutic use , Review Literature as Topic , Meta-Analysis as Topic , Randomized Controlled Trials as Topic , Alanine Transaminase
10.
Medical Journal of Chinese People's Liberation Army ; (12): 633-638, 2017.
Article in Chinese | WPRIM | ID: wpr-613689

ABSTRACT

Objective To evaluate the incidence of net adverse clinical and cerebral events (NACCE) 1 year after implantation of biodegradable polymer stents (BP-SES) in elderly patients with coronary artery disease.Methods The clinical data of patients inserted with BP-SES in I-LOVE-IT 2 Trial were retrospectively analyzed, including 1829 elderly patients admitted in the General Hospital of Shenyang Military Command from Oct. 2012 to Jun. 2013, of which 62 cases aged equal to and more than 65 years (elderly group) and 1202 cases less than 65 years (non-elderly group). The primary end-point of this research was target lesion failure (TLF) rate on 12 months and the secondary end-point was the incidence of NACCE, including all-cause death, all myocardial infarction, stroke and severe hemorrhage (BARC type ≥3), and then the multiple regression analysis was performed.Results The Baseline conditions of the two groups were significantly different (P<0.05) including BMI, diabetes, hypertension, hyperlipidemia, family history of coronary heart disease, smoking history, past stroke history, history of peripheral vascular disease and stable angina pectoris. When comparing elderly group with non-elderly group, marked differences existed on the incidence of NACCE (10.0%vs. 5.2%,P<0.01), all-cause mortality (2.7%vs. 0.7%,P<0.01), myocardial infarction (5.6%vs. 3.5%,P=0.03), stent thrombosis (1.9%vs. 0.5%,P<0.01) and stroke (2.2%vs. 0.8%,P=0.01). Multiple regression analysis revealed that elderly (age ≥65) was the independent predictive factor for NACCE (OR=1.904, 95%CI 1.304-2.781,P=0.001).ConclusionThe incidence of NACCE is increased significantly in elderly patients (age ≥65), and elderly is an independent predictive factors for 12-month NACCE in patients implanted with BP-SES

11.
Shanghai Journal of Acupuncture and Moxibustion ; (12): 1452-1454, 2017.
Article in Chinese | WPRIM | ID: wpr-664152

ABSTRACT

Objective To observe the clinical efficacy of auricular point sticking plus Chinese medication rinsing in treating allergic purpura. Method A total of 147 patients were randomized into two groups. The two groups both received conventional Western medication, while the treatment group was additionally given auricular point sticking plus Chinese medication rinsing. The therapeutic efficacy was evaluated after successive 2-week treatment. Result The total effective rate was 98.7% in the treatment group versus 88.9% in the control group, and the between-group difference was statistically significant (P<0.05). Conclusion Based on conventional treatment of Western medicine, auricular point sticking plus Chinese medication rinsing is effective in treating allergic purpura.

12.
China Pharmacist ; (12): 1723-1727, 2017.
Article in Chinese | WPRIM | ID: wpr-661209

ABSTRACT

Objective:To study the safety factors of Fuyanyu mixture. Methods: The contents of antiseptic and residual ethanol were determined by HPLC and GC, respectively, and those of heavy metals and harmful elements were detected by ICP-MS. Results:The contents of benzoic acid in 6 batches of samples were less than 0. 3%. In two thirds of samples, ethanol residue was more than 0. 5%. The total mercury exceeded 15μg/day in one of the samples, and the contents of Pb, Ge, Gr, As, Ni and Cu met the limits described in USP<232> in all of the last samples. Conclusion: The methods are accurate and reliable. It is urgent to improve the preparation process so as to reduce the residual amount of ethanol according to the detection results. It is recommended to increase the testing items that affect the safety of the preparation so as to control the preparation quality strictly.

13.
China Pharmacist ; (12): 1723-1727, 2017.
Article in Chinese | WPRIM | ID: wpr-658298

ABSTRACT

Objective:To study the safety factors of Fuyanyu mixture. Methods: The contents of antiseptic and residual ethanol were determined by HPLC and GC, respectively, and those of heavy metals and harmful elements were detected by ICP-MS. Results:The contents of benzoic acid in 6 batches of samples were less than 0. 3%. In two thirds of samples, ethanol residue was more than 0. 5%. The total mercury exceeded 15μg/day in one of the samples, and the contents of Pb, Ge, Gr, As, Ni and Cu met the limits described in USP<232> in all of the last samples. Conclusion: The methods are accurate and reliable. It is urgent to improve the preparation process so as to reduce the residual amount of ethanol according to the detection results. It is recommended to increase the testing items that affect the safety of the preparation so as to control the preparation quality strictly.

14.
China Occupational Medicine ; (6): 305-307, 2016.
Article in Chinese | WPRIM | ID: wpr-876948

ABSTRACT

OBJECTIVE: To estimate the biological dose by the chromosome aberration analysis in a victim suffered in the radioactive source-loss accident in Nanjing City. METHODS: Peripheral blood sample of the victim was collected 6 days after radioactive exposure. Individual radioactive biological dose was estimated by identifying the aberration of the dicentrics plus centric rings in the metaphase chromosome of cells. The distribution of chromosome aberration was tested by the Poisson distribution. Impure Poisson distribution was used to estimate the radiation dose. RESULTS: Among the 353 cells observed at metaphase,75 aberration of dicentrics plus centric rings were found,43 cells had 1 aberration and 7 cells had 2 aberrations. Moreover,there were 3 multi-aberration cells with 3,4 and 11 aberrations respectively. The average individual radiation dose was estimated to be 1. 52 Gy,which was consistent with the clinical diagnosis as mild acute bone marrow radiation disease. The Poisson distribution u test revealed that the patient suffered from nonhomogeneous radiation.By the impure Poisson distribution test,the radiation exposure proportion of the whole body was estimated to be 55% and the average dose was 3. 02 Gy. CONCLUSION: The biological dose estimation was successfully performed,the results showed that this was a case of nonhomogeneous irradiation.

15.
Herald of Medicine ; (12): 181-184, 2016.
Article in Chinese | WPRIM | ID: wpr-491953

ABSTRACT

Objective To establish a high performance liquid chromatographic ( HPLC) method for determination of gallic acid and ellagic acid in Melastoma dodecandrum. Methods HPLC was applied, the chromatographic column was Waters Xbidge C18(4.6 mm×250 mm,5μm);with methanol-mixed aqueous solution containing 0.3% phosphoric acid and 0.06%tetrahydrofuran as the mobile phrase;gradient elution:0–12 min,1% A ( the detection wavelength was 216 nm);12–24 min, 1% A→55% A (the detection wavelength was 254 nm);flow rate was 1.0 mL.min-1, the column temperature was 30 ℃. Results Good linear relationship of gallic acid and ellagic acid was obtained at ranges of 0.089 7-0.448 μg ( r=0.999 8) and 0.028 4-0.142 μg (r=0.999 8),respectively. The average recoveries were 96.51% (RSD=1.10%) and 96.19% (RSD=1.20%) . Conclusion The method is simple,accurate and repeatable,and it is suitable for content determination of gallic acid and ellagic acid in Melastoma dodecandrum. It provides a basis for quality evaluation of Melastoma dodecandrum.

16.
Journal of China Pharmaceutical University ; (6): 90-94, 2016.
Article in Chinese | WPRIM | ID: wpr-491909

ABSTRACT

To study the mechanisms whereby cisplatin suppresses survival of human esophageal squamous cell carcinoma cells.The cytotoxicity of cisplatin in cisplatin-resistant cell line EC109 /CDDP and its parental cell line EC109 was measured by cell viability assay.Western blotting was used to investigate the protein expression of to-tal p53 and phosphorylated p53 at Ser15.Colony formation assay was employed to evaluate the ability of cells to recover from treatments and form colonies.The results indicated that EC109 /CDDP cells were more resistant to cisplatin-induced cytotoxicity than EC109 cells,with the IC50 values of (20.4 ±4.4)μmol /L and (5.7 ±0.1 )μmol /L,respectively.Although cisplatin did not alter the total protein level of p53,it obviously increased the phosphorylation of p53 at Ser15.Cisplatin inhibited survival of both EC109 /CDDP and EC109.Notably,inhibition of p53 by Pifithrin-αsignificantly promoted recovery of cisplatin-treated EC109 and EC109 /CDDP cells to differ-ent degrees.In this respect,p53 protein was found to be activated in response to cisplatin treatment in both EC109 /CDDP and EC109,which may contribute to the cytotoxic effect of cisplatin.

17.
Chinese Journal of Interventional Cardiology ; (4): 88-95, 2016.
Article in Chinese | WPRIM | ID: wpr-487168

ABSTRACT

Objective To systematically evaluate the safety of high dose atorvastatin (80 mg daily) in Chinese patients. Methods Randomized controlled trials (RCTs) investigating 80 mg/ d atorvastatin vs. low-dose atorvastatin or placebo or blank were electionically retrieved in date bases of EMbase, PubMed, the Cochrane Library, WanFang, CNKI and WeiPu. Meta-analysis was performed using RevMan 5. 2 and Stata 11. 0 software. Results A total of 20 RCTs involving 2282 cases were included. The results of meta-analysis showed no significant differences betweent the 80 mg/ d atorvastatin group and the control group in the incidence of gastrointestinal adverse events (RR 1. 53, 95% CI 0. 85-2. 76, P = 0. 16), hepatic adverse events (RR 1. 53, 95% CI 0. 99 - 2. 36, P = 0. 05), muscular adverse events (RR 1. 51, 95% CI 0. 92 -2. 49, P = 0. 10), serious hepatic injuries ( RR 2. 33,95% CI 0. 88 - 6. 20, P = 0. 09) and serious muscular myopathies (RR 1. 40, 95% CI 0. 46 - 4. 30, P = 0. 56). Subgroup analysis by type of cotrast media used and durations of taking 80 mg/ d atorvastatin showed there were higher risks of gastrointestinal adverse events in the 80 mg/ d group when compared to blank control ( RR 4. 22, 95% CI 1. 11 - 16. 04, P = 0. 03). Conclusions The current evidence shows that 80 mg / d atorvastatin may be relatively safe in terms of adverse events in gastrointestinal tract, liver and muscular system, and relatively has risk in causing severe liver injuries and myopathies. With limited quantity and quality from the RCTs available, more high quality RCTs are needed to verify the above conclusion.

18.
China Pharmacy ; (12): 2990-2992, 2016.
Article in Chinese | WPRIM | ID: wpr-504694

ABSTRACT

OBJECTIVE:To establish a method for the simultaneous contents determination of chlorogenic acid,rutin and iso-quercitrin in Morus alba,fried M. alba and honeyed M. alba. METHODS:HPLC was performed on the column of Agilent Zorbax SB-C18 with mobile phase of acetonitrile-0.2% phosphoric acid(gradient elution)at a flow rate of 1.0 ml/min,detection wavelen-gth was 350 nm ,the column temperature was 30 ℃,and injection volume was 10 μl. RESULTS:The linear range was 8.20-82.01μg/ml for chlorogenic acid (r=0.999 9),2.76-27.60 μg/ml for rutin (r=0.999 9) and 4.74-47.39 μg/ml for isoquercitrin (r=0.999 9);RSDs of precision,stability and reproducibility tests were lower than 2%;recoveries were 98.58%-100.91%(RSD=1.02%,n=6),99.19%-101.00%(RSD=0.82%,n=6) and 98.41%-101.51%(RSD=1.08%,n=6),respectively. CONCLU-SIONS:The method is simple with good stability and reproducibility,and can be used for the simultaneous determination of chloro-genic acid,rutin and isoquercitrin in different processed drugs of M. alba.

19.
Journal of Southern Medical University ; (12): 506-513, 2016.
Article in Chinese | WPRIM | ID: wpr-264013

ABSTRACT

<p><b>OBJECTIVE</b>To explore whether MG-132 could enhance the anti-tumor activity of obatoclax against esophageal cancer cell line CaES-17.</p><p><b>METHODS</b>MTT assay was used to determine the cytotoxicity of obatoclax and MG-132 in CaES-17 cells. The IC(50) of obatoclax and MG-132 were used to determine the molar ratio (1:2.4) of the two drugs for combined treatment of the cells. The concentrations of obatoclax and MG-132 ranged from 1/8 IC(50) to 4 IC(50) after serial dilution, and their combination index (CI) was calculated using CompuSyn software. The expression of ubiquitin and the cleavage of PARP, caspase-9, phospho-histone H3 and phospho-aurora A/B/C in the exposed cells were examined with Western blotting; the cell apoptosis was measured by flow cytometry with Annexin V staining, and the percentage of cells in each cell cycle phase was also determined by flow cytometry.</p><p><b>RESULTS</b>The CI of obatoclax and MG-132 was 0.296 for a 50% inhibition of Caes-17 cells and was 0.104 for a 95% inhibition. The cells treated with obatoclax or MG-132 alone showed increased expression of ubiquitin and cleavage of PARP and caspase-9. Compared with the cells treated with obatoclax or MG-132 alone, the cells with a combined treatment exhibited significantly increased expression of ubiquitin, cleavage of PARP and caspase-9, and expression of phospho-Histone H3 (P<0.05). The combined treatment of the cells also resulted in significantly increased expression of phospho-Aurora A/B/C compared with obatoclax treatment alone. The cells with the combined treatment showed significantly higher percentages of apoptotic cells and cells in sub-G(1) and G(2)/M phases compared with the cells treated with either of the drugs (P<0.05).</p><p><b>CONCLUSION</b>Obatoclax combined with MG-132 shows a significant synergistic anti-tumor effect against esophageal cancer CaES-17 cells by inducing apoptosis and cell cycle arrest.</p>


Subject(s)
Humans , Apoptosis , Caspase 9 , Metabolism , Cell Cycle Checkpoints , Cell Line, Tumor , Esophageal Neoplasms , Pathology , Histones , Metabolism , Leupeptins , Pharmacology , Poly (ADP-Ribose) Polymerase-1 , Poly(ADP-ribose) Polymerases , Metabolism , Pyrroles , Pharmacology
20.
China Pharmacy ; (12): 5157-5159, 2015.
Article in Chinese | WPRIM | ID: wpr-501322

ABSTRACT

OBJECTIVE:To study the flavonoids in She medicine Eupatorium chinense. METHODS:Silica gel,ODS and Sep-hadex LH-20 column chromatography were conducted to isolate and purify the flavonoids in She medicine E. chinense,and com-pound structures were analyzed and identified based on the physicochemical properties and spectral data. RESULTS:From the ethyl acetate extract of E. chinense,10 flavonoids were isolated as tricin (1),quercetin(2),kaempferol(3),luteolin(4),luteo-lin-7-O-β-D-glucoside (5),4-methoxyctricin (6),quercetin-3-O-β-D-glucoside(7),kaempferol-3-O-β-D-glucoside(8),kaempfer-ol-3-O-rutinoside(9)and rutin(10). CONCLUSIONS:Compound 1-10 are isolated from E. chinense for the first time. The study provides certain basis for the quality evaluation of E. chinense.

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