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Objective To investigate the effects of a novel enhancer of Zeste homolog 2 (EZH2) inhibitor GSK126 in vitro on the cell proliferation and apoptosis in acute leukemia and lymphoma cells. Methods CCKˉ8 assay was used to measure the effects of GSK126 with different concentrations and time on the cell proliferation in human Tˉcell acute lymphoblastic leukemia (TˉALL) CEM cell line, acute monocytic leukemia U937 cell line and Burkitt lymphoma Raji cell line. Annexin V/PI double staining method was used to determine the effects of GSK126 on the cell apoptosis. The effect of GSK126 on the mRNA levels of EZH2, bclˉ2 and bclˉxL were measured by using quantitative polymerase chain reaction (qPCR). Results After the function for 24 h, 48 h and 72 h, compared to the negative control group (0 μmol/L), 5, 10, 15, 20, 25 μmol/L GSK126 treatment showed a significant doseˉand timeˉdependent cell proliferation suppression in CEM cells; 5, 10, 15, 20 μmol/L GSK126 treatment showed a significant doseˉand timeˉdependent cell proliferation suppression in U937 cells; 5, 10, 15, 20, 25, 30 μmol/L GSK126 treatment showed a significant timeˉdependent suppression in Raji cells (all P< 0.05). The 48 h 50% inhibitory concentration ( IC 50) of GSK126 on CEM, U937, Raji cells was (13.46 ±0.83), (11.65 ±1.02), (15.00 ±0.19) μmol/L, respectively. GSK126 treatment with the doses of 8, 12 and 16 μmol/L promoted the apoptosis of CEM and U937 cells compared with the negative control group (0 μmol/L), and there were statistical differences in the apoptosis rate (F＝ 167.995, P< 0.01; F＝ 158.400, P< 0.01). In Raji cells, only 16 μmol/L GSK126 treatment had a higher cell apoptosis rate compared with the control group (t＝ 47.998, P< 0.05). Furthermore, 8, 12 and 16 μmol/L GSK126 treatment suppressed the expressions of EZH2 mRNA in CEM, U937 and Raji cells compared with the control group (F＝82.035, P<0.01; F＝ 252.712, P< 0.01; F＝ 690.536, P< 0.01), and the expressions of bclˉ2 and bclˉxL mRNA (bclˉ2: F＝ 1 900.525, P< 0.01; F＝ 431.324, P< 0.01; F＝216.184, P<0.01; bclˉxL: F＝256.751, P<0.01; F＝147.019, P<0.01; F＝209.325, P<0.01). Conclusion EZH2 plays an important role in the occurrence and development of acute leukemia and lymphoma. GSK126 as a high selective inhibitor of EZH2 might be a potential new drug in treatment of hematological malignancies.
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Objective@#To detect the characteristics of phosphatase and tensin homolog (PTEN) mutations in adult T-cell acute lymphoblastic leukemia (T-ALL) and its relationship with the prognosis.@*Methods@#Fifty-five adult T-ALL patients were enrolled in Jiangsu Province Hospital from February 2010 to April 2016. Mononuclear bone marrow cells were extracted by using Ficoll density gradient centrifugation. Genomic DNA was extracted from isolated mononuclear cells. Amplified exon 1-9 of PTEN by polymerase chain reaction (PCR) specifically amplified PTEN exon, then DNA was purified, sequenced and compared. The mutation occurrence rate, mutation types, and the relations with several clinical indicators were analyzed.@*Results@#PTEN mutations were detected in 5 patients, and 8 types of mutations were detected in 55 T-ALL patients with mutation rate of 9.1% (5/55). All the mutations were located in exon 7 of the genes. Five patients with PTEN mutations also merged other gene mutations like NOTCH1 and DNM2. The level of median lactate dehydrogenase (LDH) in patients with PTEN mutations was higher than that in patients without PTEN mutations (3 358 U/L vs. 755 U/L, Z=-2.014, P= 0.044). No significant differences were found in gender, age, white blood count, hemoglobin, platelet count, overall survival rate, event free survival, recurrence free survival between the two groups (P > 0.05).@*Conclusion@#PTEN is a tumor suppressor gene, and its mutation plays a significant role in the occurrence and development of adult T-ALL patients, which may be associated with the poor prognosis.
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Objective:To study the effects of compound preparation of Fanshiliu on lipid metabolism and pancreatic pathological changes in type 2 diabetes mellitus(T2DM)rats with insulin resistance. Methods:After fed with high-calorie food for 8 weeks,the rats received intraperitoneal injection with low dose of streptozotocin(STZ)to induce T2DM animal model,and then the rats were randomly divided into the model group,metformin group,high and low dose group of compound preparation of Fanshiliu. The normal group was given ordinary feed. The rats were sacrified after intragastric administration for six weeks,and fasted for 12 hours after the last administration. The lipid and lipoprotein indices were detected,and pathological morphology of pancreatic tissue was observed. Results:Compared with those in the model group,TC,TG,LDL-C and FFA in each treatment group were reduced,and HDL-C was increased(P < 0. 05). Fanshiliu high dose group and metformin group had obvious hypoglycemic and lipid-lowering effects. The results of pathological morphology of pancreatic tissue under a light microscope showed that the damage was the most obvious in the model group. Compound preparation of Fanshiliu groups and metformin group showed damage in varying degrees. Conclusion:Fanshiliu preparation can effectively adjust blood lipid levels,enhance the insulin sensitivity and reduce damage in pancreas in T2DM rats.
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Objective To observe the effects of Xifeng Tongnao capsules on the content of TNF-α and IL-1β in brain tissue of rats with focal cerebral ischemia-reperfusion injury. Methods A total of 120 adult SD rats were randomized into 6 groups: Xifeng Tongnao low-, middle- and high-dose groups, model control group, Buchang Naoxintong group and sham-operated group.Buchang Naoxintong group were treated with Buchang Naoxintong capsules at 0.864 g??kg-1.Xifeng Tongnao high-, middle-and low-dose groups were treated with 3.456, 1.728, and 0.864 g??kg-1 Xifeng Tongnao capsules, respectively;sham-operated group and model control group were treated with equal volume of purified water. Medications were administered intragastrically once daily for 7 days. The acute transient focal cerebral ischemia-reperfusion model was established by middle cerebral artery occlusion ( MCAO) 1 h after the final dose, and rats in the sham-operated group only received anesthesia and stripping without occlusion.All rats were sacrificed after reperfusion for 24 h, and expression levels of TNF-α and IL-1β in the brain tissue were detected by ELISA. Results TNF-αcontent in Xifeng Tongnao capsutes low-, middle-and high-dose groups were (35.34±8.95), (33.75±6.92), and (40.95±5.39) ng??L-1, respectively.IL-1β content were (1.44±0.47), (1.45± 0.23), and (1.61±0.33) ng??L-1 in low-, middle- and high-dose groups, respectively.TNF-α and IL-1β were (38.96±9.84) and (1.56±0.31) ng??L-1, respectively in Buchang Naoxintong group, (52.74±6.76) and (2.79±0.45) ng??L-1in the model control group, and (32.54±4.00) and (1.32±0.22) ng??L-1 in sham-operated group.TNF-αand IL-1βcontent were significantly higher in Buchang Naoxintong group than in sham-operated group ( P<0. 05 ) . TNF-α and IL-1β content were significantly decreased in Xifeng Tongnao high-, middle- and low-dose groups (all P<0.05). Conclusion Xifeng Tongnao capsules can protect brain tissue by supressing TNF-α and IL-1β and alleviating inflammatory injury from ischemia.
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This study was aimed to investigate the research on pharmacological effects, relevant ideas and methods of Guangdong native heat-clearing and toxin-removing herbs. Literatures on pharmacological effects of Guangdong native heat-clearing and toxin-removing herbs were collected, summarized and analyzed. The results showed that most Guangdong native heat-clearing and toxin-removing herbs had obvious effects of anti-microbial, anti-bacterial endotoxin, anti-inflammatory, and antipyretic effect. It also had obvious antivenomous and analgesia effect. Based on research ideas and methods of Guangdong native heat-clearing and toxin-removing herbs, we clarified the confusion species as soon as possible, and adhered to the whole animal experiments in combination with in vitro experiments and computer molecular docking simulations for the complementation of each other. It was concluded that the study on pharmacological effects of Guangdongnative heat-clearing and toxin-removing herbs provided strong support in its clinical application. Ideas and methods provided in this article was the main way to explain pharmacological effects of Guangdong native heat-clearing and toxin-removing herbs.
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Objective To investigate the anti-inflammatory effect of water-extract of microcos paniculata,and to provide scientific experimental evidence for clinical applications.Methods Various inflammatory models,including the swelling of ear induced by xylene and the permeability increase of capillary induced by acetic acid in mice were used to explore the anti-inflammatory of water-extract of Microcos Paniculata.Results High and middle doses of microcos paniculata could significantly inhibit ear edema,and all the three doses of microcos paniculata could significantly inhibit the permeability increase of capillary permeability.Conclusion The water-extract of microcos paniculata has significant anti-inflammatory effect.
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OBJECTIVE:To establish the quality criteria for Huangzhi oral liquid.METHODS:TLC was employed to for the qualitative identificaiton of Radix et Rhizoma Rhei,Leech and Fructus Arctii;the content of total nitrogen was determined by KjeLdahL determination and content of Chrysophanol in Radix et Rhizoma Rhei in Huangzhi oral liquids was determined by HPLC.RESULTS:The TLC chromatograms of Radix et Rhizoma Rhei,Leech and Fructus Arctii presented the spots of the same colors with those at the corresponding places in the chromatograms of the controls.There was a good linear relationship within the concentration range of 1.696～ 8.480? g? mL-1 for Chrysophanol(r=0.999 8).The average recovery was 99.60%(RSD=1.37%,n=9).CONCLUSION:The methods are accurate and reliable with a strong specificity and can be used for the quality control of Huangzhi oral liquid.
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OBJECTIVE:To evaluate the inhibitory actions of 3 traditional Chinese drugs on human nasopharyngeal carcinoma cells CNE-2 in vitro.METHODS:The IC50(50% inhibiting concentration)of 3 traditional Chinese drugs on human nasopharyngeal carcinoma cells CNE-2 in vitro was measured by MTT assay.RESULTS:The inhibitory actions of 3 traditional Chinese drugs on human nasopharyngeal carcinoma cells CNE-2 in vitro were enhanced with the increase of the concentration in a concentration-dependent manner,with formulation Ⅲ showing the most potent inhibitory action on CNE-2 cells in vitro.CONCLUSION:The heat-clearing and detoxicating traditional Chinese drugs could markedly inhibit the proliferation of CNE-2 cells.
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OBJECTIVE:To study the antipyretic and analgesic effects of Compound tuniuxi sirup.METHODS:Fever was induced by dry yeast in SD rats,then divided the rats into high-dose(33.12g/kg),medium-dose(16.56g/kg),low-dose(8.28g/kg)and control,aspirin group,observed the antipyretic effect;The mice were divided into high-dose(47.84g/kg),medium-dose(23.92g/kg),low-dose(11.96g/kg)and control,aspirin group,then were investigated with hot plate and acetic acid induced body twist.RESULTS:Compound tuniuxi sirup can markedly inhibit the fever in the model anmals 1 hour later,the effect of the high,medium groups are similar to aspirin;and could increase the pain threshold obviously(the low-dose group is obviously in 1.5h～2h(P
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OBJECTIVE: To study the action mechanism of kunzao tiaozhi capsule in the treatment of fatty liver with hyperlipidemia.METHODS: A total of 59 rats were randomly divided into normal control group(n=10),model group(n=11),positive control group(n=10) and kunzao tiaozhi capsule group(at high,medium and low doses,n=9,9,10).Rat model with fatty livers was established in all the groups except the normal control group by feeding high-fat forage and 30% alcohol,and the corresponding solvents or medicine were given during the modeling,10 weeks later,the S-phase cell percentages(SPF) of the liver cells in rats and proliferation index(PI) were determined by flow cytometry methods.RESULTS: As compared with the normal control group,PI and SPF values in the modeled rats increased significantly(P
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OBJECTIVE:To study the hemostatic,antipruritic,and anti-crissal ulcer effects of Zhishuxi lotion.METHODS:The experimental animals were randomized into four groups(normal control group,Mayinglong-branded musk hemorrhoid ointment,Zhishuxi lotion high-dose group and low-dose group).The time needed to stop bleeding in all groups were tested by cutting mouse tail;the itch-threshold in each group of guinea pigs was determined by inducing itch with histamine phosphate;and the ulceration was observed by causing crissal ulceration in mice with acetic acid.RESULTS:Zhishuxi lotion could shorten the bleeding time,increase the itch threshold in guinea pig,and had some curative effect on acetic acid-induced crissal ulcer in mouse,as compared with the control group.CONCLUSION:Zhishuxi lotion has re-markable effects of hemostasis,itch-relief and anti-crissal ulceration.
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OBJECTIVE:To lead to a rational recognition and use of Chinese herbal medicines containing aristolochic acids.METHODS:Literature in recent years concerning aristolochic acid and Chinese herbal medicines containing aristolochic acids were reviewed and analyzed.RESULTS&CONCLUSIONS:Aristolochic Acids Chinese herbal medicines should be used sen-sibly,practically and rationally.