1. Research progress on pharmacological effects of p-coumaric acid
Chinese Traditional and Herbal Drugs 2018;49(17):4162-4170
p-coumaric acid is mainly found in fruits, vegetables, grains, and fungi, and is also abundant in Chinese herbal medicines. The pharmacological effects of p-coumaric acid has anti-oxidant, anti-inflammatory, immunomodulatory, antitumor effects, antiplatelet aggregation, cardiovascular protection, prevention and improvement of diabetes, and neuroprotection, while the anti-oxidant activities of p-coumaric acid is the important basis of other pharmacological effects. In addition, p-coumaric acid has a certain inhibitory effect on bacteria, and also can inhibit melanin formation and delay skin aging. This paper reviews the main pharmacological effects of p-coumaric acid and provides reference for the development of both medicinal and food resources.
2.Pharmacokinetic comparison of two ozagrel polymorph forms in SD rats.
Zhi-Zhen QIN ; Qian-Xi CHEN ; Jun-Ke SONG ; Yang LÜ ; Guan-Hua DU
Acta Pharmaceutica Sinica 2015;50(2):218-221
To enhance the quality and efficiency of ozagrel by investigating the differences between the ozagrel polymorphs in bioavailability. Solid ozagrel in different polymorph forms were orally administered to SD rats. An HPLC method was established to determinate plasma level of ozagrel. The bioavailabilities of two polymorph forms were calculated and compared. The pharmacokinetic parameters of ozagrel, were as follows: Cmax was 32.72 ± 17.04 and 34.01 ± 19.13 mg · L(-1), respectively; AUC0-t was 61.14 ± 14.76 and 85.56 ± 18.08 mg · L(-1) · h, respectively; t½ was 1.53 ± 0.51 and 4.73 ± 3.00 h, respectively. There was no significant difference in pharmacokinetic parameters between form I and II polymorphs of ozagrel while the t½ of form II is longer, which indicates that the use of form II polymorph as pharmaceutical product may prolong the effective action time in clinics. This would help the polymorph quality control in drug production.
Animals
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Biological Availability
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Chromatography, High Pressure Liquid
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Methacrylates
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chemistry
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pharmacokinetics
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Rats
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Rats, Sprague-Dawley
3.An epidemiological study on multiple-injuries of bone and joint
Ang-Ru LIN ; Xi-Jun HOU ; Guan-Jun QIN ; Jionghao CHEN ; Guoxian PEI ;
Chinese Journal of Orthopaedic Trauma 2004;0(06):-
Objective To investigate the epidemiological characteristics of multiple-injuries of bone and joint in the belief that a better knowledge of such injuries may help their prevention and treatment. Methods A retrospective study was done on the data of 346 patients with multiple-injuries of bone and joint who had been ad- mitted to our department from January 2001 to December 2004. On the basis of CAI's classification, the following data were statistically analyzed: gender, age, cause of injury, injured part, number of injured parts, associated injuries and mortality. Results Of the 346 injured patients, there were 278 males and 68 females, with an av- erage age of 32.8 years (9months to 89 years). Two hundred and twenty-six cases resulted from traffic accidents, 65 from crush by a heavy object, and 52 from falling. There were 159 fractures of shaft of tibia and fibula, 96 fractures of femoral shaft, 87 fractures of shaft of ulna and radius, 58 fractures of ankle and foot, 57 chest injuries, 50 knee injuries, 50 hip injuries, 49 injuries at the pelvis region, 46 wrist and hand injuries, 36 injuries of shoulder, 36 skull fractures, 33 fractures of humeral shaft, 23 spinal fractures, and 17 elbow injuries. Two hundred and forty-two patients had two parts injured, 83 had three parts, 20 had four parts, and one had six parts. The average number of injured parts was 2.3. Two hundred and five patients suffered from close injuries, and 141 from open ones. The associated injuries included skull and brain injury in 51 cases, chest injury in 23, abdomen injury in five, urine system injury in three, nerve and vessel injury in 21, shock in 78, and fat embolism in six. Five patients died. Conclusions Male young people tend to be the majority of victims of multiple-injuries of bone and joint. Traffic accidents result in most of such injuries. Since multiple-injuries mostly involve lower limbs, they are easy to diagnose while the associated close injuries involving brain, chest, abdomen and pelvic are likely to be overlooked or misdiagnosed. Strengthening safety education and technical training of first aid is important to im- provement of treatment and to decrease of disability rate and mortality.
4.Effect of Jiangang Yishen Recipe on high insulin induced cell proliferation of human glomerular mesangial cells and the expression of insulin receptor substrate 1 and phosphatidylinositol-3-kinase.
Yong-Jun WU ; Rong YU ; Xi-Hua CHENG ; Hui WU ; Can-Rong WU ; Guan-De WEI ; Qin ZHANG
Chinese Journal of Integrated Traditional and Western Medicine 2014;34(5):597-601
OBJECTIVETo investigate the effect of Jiangtang Yishen Recipe (JTYSR) on high insulin induced cell proliferation of human glomerular mesangial cells (HMCs) and the expression of insulin receptor substrate 1 (IRS-1) and phosphatidylinositol-3-kinase (PI-3K).
METHODSHMCs were divided into 4 groups, i.e., the negative control group, the high insulin model group, the JTYSR group, and the LY294002 group. The concentration of insulin, JTYSR, and LY294002 was respectively confirmed by pre-experiment. Different culture solution was respectively added for different groups. RPMI1640 culture solution was added for HMCs in the negative control group, while HMCs in the rest 3 groups were cultured by 100 nmol/L insulin for 24 h. Meanwhile, HMCs from the JTYSR group and the LY294002 group were exposed to 125 mg/L JTYSR and 80 micromol/L LY294002 respectively for further 48 h. The proliferation of HMCs was detected by MTT and flow cytometry. The protein expression of IRS-1 and PI-3K in HMC was detected by immunohistochemical assay and Western blot. Results The proliferation of HMCs induced by high insulin could be significantly lowered, and the protein expression of IRS-1 and PI-3K could be down-regulated in the JTYSR group and the LY294002 group (P <0.01). Compared with the LY294002 group, the protein expression of IRS-1 and PI-3K could be slightly down-regulated in the JTYSR group (P <0.05).
CONCLUSIONJTYSR could lower high insulin induced proliferation of HMCs, and its mechanism might be related to insulin signaling pathway.
Cell Proliferation ; drug effects ; Chromones ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Insulin Receptor Substrate Proteins ; metabolism ; Mesangial Cells ; physiology ; Morpholines ; Phosphatidylinositol 3-Kinase ; metabolism ; Phosphatidylinositol 3-Kinases ; metabolism ; Signal Transduction
5.siRNA targeted against survivin induces apoptosis of pancreatic cancer cells.
Hai-tao GUAN ; Xing-huan XUE ; Xi-jing WANG ; Ang LI ; Zhao-yin QIN
Journal of Southern Medical University 2006;26(2):169-173
OBJECTIVETo investigate the effect of a sequence-specific small interfering RNA (siRNA) in suppressing survivin expression and cell proliferation and inducing apoptosis of PC-2 cells.
METHODSThe plasmid expression vector of siRNA targeted against survivin was constructed and transfected into PC-2 cells with Lipofectamine 2000. The changes of survivin expression were detected by semi-quantitative RT-PCR and immunohistochemical SP methods. The effect of siRNA in suppressing the proliferation of PC-2 cells was detected by MTT assay, and its role in inducing PC-2 cell apoptosis evaluated by flow cytometry.
RESULTSThe sequence-specific siRNA effectively suppressed survivin expression at both mRNA and protein levels with inhibition rate of 81.25% at mRNA level and 74.24% at protein level. Survivin expression suppression significantly inhibited the proliferation of PC-2 cells, and at 24 and 48 h after cell seeding, the proliferation inhibition rate was 28.00% and 33.38% respectively; 24, 48 h after the transfection, apoptosis occurred in 8.46% and 7.53% of the cells, respectively.
CONCLUSIONSThe plasmid expression vector for the siRNA against survivin constructed in the study can effectively and specifically suppress survivin expression in PC-2 cells, and blocking survivin expression suppresses PC-2 cell proliferation and induces cell apoptosis. siRNA targeted against survivin has a potential value in gene therapy for pancreatic cancer.
Apoptosis ; genetics ; Cell Line, Tumor ; Cell Proliferation ; Cell Survival ; genetics ; Humans ; Inhibitor of Apoptosis Proteins ; Microtubule-Associated Proteins ; biosynthesis ; genetics ; Neoplasm Proteins ; biosynthesis ; genetics ; Pancreatic Neoplasms ; genetics ; pathology ; RNA Interference ; RNA, Messenger ; biosynthesis ; genetics ; RNA, Small Interfering ; genetics ; Transfection
6.Intravenous versus articular injection of tranexamic acid for reducing hemorrhage after unilateral total knee arthroplasty
Guan-Hong CHEN ; Lei QIN ; Hui HUANG ; Zhan WANG ; Jia-Chao MA ; Ying XU ; Xi-Cheng ZHAI
Chinese Journal of Tissue Engineering Research 2018;22(3):350-355
BACKGROUND: The perioperative hemorrhage of knee surgeries is a difficulty in clinic, and the efficacy of tranexamic acid to reduce postoperative bleeding has attracted more attention, but choosing which administrations remains controversial. OBJECTIVE: To investigate the efficacy of tranexamic acid by intravenous injection or articular injection for reducing the perioperative hemorrhage of total knee arthroplasty. METHODS: Sixty patients undergoing unilateral total knee replacement were enrolled, and were then randomized into three groups (n=20 per group): no tranexamic acid administration (group A); intravenous dropping of 15 mg/kg tranexamic acid before tourniquet application plus 10 mg/kg tranexamic acid at 3 hours postoperatively (group B); articular injection of 50 mL saline diluted with 1 g tranexamic acid through a drainage tube (group C). Two-hour closure of drainage tube was performed in all patients. The postoperative dominant and hidden blood loss, blood transfusion rate, pulmonary embolism as well as lower extremity deep venous thrombosis were recorded. RESULTS AND CONCLUSION: (1) The dominant and hidden blood loss in the groups B and C were significantly less than those in the group A (P < 0.05); the dominant blood loss showed no significant difference between groups B and C (P > 0.05); the group B exhibited a significantly less hidden blood loss compared with group C (P < 0.05). (2) The blood transfusion rate in the groups B and C was significantly lower than that in the group A (P < 0.05). (3) No pulmonary embolism or lower extremity deep venous embolism occurred during 3-month follow-up. (4) That is to say, tranexamic acid can obviously reduce perioperative blood loss and blood transfusion rate without pulmonary embolism or lower extremity deep venous thrombosis, and intravenous administration exerts better clinical effectiveness.
7.Expression of cyclin dependent kinases-5 in the temporal lobes of the drug resistance epilepsy patients
Zhi-Qin XI ; Xue-Feng WANG ; Zhen-Li GUO ; Xian-Jun KE ; Ji-Jun SUN ; Yuan WU ; Jin-Mei LI ; Fei XIAO ; Xi ZHU ; Li-Feng GUAN ; Yun GONG ; Fengying LIU ; Guoming LUAN ; Jianguo ZHANG ; Yuping WANG ;
Chinese Journal of Neurology 2000;0(05):-
Objective To investigate the expression of cyclin dependent kinases 5(CDK5)in the temporal lobes of the epilepsy patients and to explore the possible roles of CDK5 in the pathogenesis of refractory epilepsy.Methods The brain tissues of intractable epilepsy(IE)were studied by fluorescence quantative polymerase chain reaction(FQ-PCR)for CDK5 mRNA,while immunohistochemistry and Western blot were used to study the protein expression.Nonepileptogenic control brain tissues were used for comparison.Results FQ-PCR analysis showed that the expression of CDK5 mRNA in epilepsy patients was significant higher than those in the control group.And immunohistochemistry showed that the protein mainly existed in the neuron and glial.At the 35000 relative molecular mass,Western blot could been seen that there is a limpid strap.The optical density of CDK5 in IE(temporal lobe 1.4293?0.1839,hippocampus 2.0733?0.4738)was significantly higher than that in the control(temporal lobe 0.9680?0.4147, hippocampus 1.4030?0.6160,P
8.Knockdown of survivin expression by small interfering RNA suppresses proliferation of two human cancer cell lines.
Hai-Tao GUAN ; Xing-Huan XUE ; Xi-Jing WANG ; Ang LI ; Zhao-Yin QIN
Chinese Medical Sciences Journal 2006;21(2):115-119
OBJECTIVETo construct an expression vector of small interfering RNA (siRNA) against survivin and observe its effects on survivin expression and proliferation of human pancreatic cancer cell line PC-2 and breast cancer cell line MCF-7.
METHODSConstructed an expression vector of siRNA against survivin and transfected it into PC-2 and MCF-7 cells using lipofectamine 2000. The expression of survivin was detected by semi-quantitive RT-PCR and immunohistochemistry, and its effects on proliferation of PC-2 and MCF-7 cells were detected by MTT assay.
RESULTSThe introduction of sequence-specific siRNA could efficiently suppress survivin expression at both mRNA and protein levels in the two cancer cell lines. In PC-2 cells, the expression inhibition rates were 81.25% at mRNA level and 74.24% at protein level. In MCF-7 cells, the expression inhibition rates were 64.91% at mRNA level and 79.72% at protein level. The proliferation of PC-2 and MCF-7 cells was also suppressed, and 24 and 48 hours after the cells were reseeded, the proliferation inhibition rates of PC-2 cells were 28.00% and 33.38%, and that of MCF-7 cells were 31.58% and 33.02%, respectively.
CONCLUSIONSThe expression vector of siRNA against survivin can block survivin expression in PC-2 and MCF-7 cells efficiently and specifically. Down regulation of survivin expression can suppress proliferation of PC-2 and MCF-7 cells. Survivin RNAi may have potential value in gene therapy of human cancers.
Base Sequence ; Breast Neoplasms ; pathology ; therapy ; Cell Line, Tumor ; Cell Proliferation ; Female ; Gene Expression ; Humans ; Inhibitor of Apoptosis Proteins ; Microtubule-Associated Proteins ; antagonists & inhibitors ; genetics ; metabolism ; Pancreatic Neoplasms ; pathology ; therapy ; Plasmids ; genetics ; RNA, Messenger ; genetics ; metabolism ; RNA, Neoplasm ; genetics ; metabolism ; RNA, Small Interfering ; genetics ; therapeutic use ; Transfection
9.Effects of siRNA targeted to survivin in suppressing proliferation and inducing apoptosis in breast cancer MCF-7 cells.
Hai-tao GUAN ; Xing-huan XUE ; Xi-jing WANG ; Ang LI ; Zhao-yin QIN
Chinese Journal of Oncology 2006;28(5):326-330
OBJECTIVEBlocking the expression of survivin with RNA interference techniques, the effects of suppressing proliferation and inducing apoptosis of breast cancer MCF-7 cells were investigated.
METHODSA siRNA eukaryotic expression vector against survivin was constructed and transfected into breast cancer MCF-7 cells with lipofectamine 2000. The changes of survivin expression were detected by semi-quantitive RT-PCR and immunohistochemistry. The effect of suppressing proliferation of MCF-7 cell was detected by MTT assay. The effect of inducing MCF-7 cell apoptosis was detected by TUNEL assay.
RESULTSThe sequence-specific siRNA can efficiently block the expression of survivin both at mRNA and protein levels. The expression inhibition rate was 64.9% at mRNA level detected by semi-quantitive RT-PCR and 79.7% at protein level detected by immunohistochemistry. Blocking the expression of survivin can suppress proliferation of MCF-7 cells significantly. At 24 and 48 h after the cells were reseeded, the proliferation inhibition rates were 31.6% and 33.0%, respectively. At 24 h after transfection, apoptosis was induced in 12.9% of the cells as detected by TUNEL assay.
CONCLUSIONBlocking the expression of survivin with RNA interference technology can significantly suppress proliferation of MCF-7 cells and induce apoptosis to a certain degree. RNAi targeted to survivin has a potential value in gene therapy of breast cancer.
Apoptosis ; Breast Neoplasms ; metabolism ; pathology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Female ; Genetic Therapy ; Genetic Vectors ; Humans ; Inhibitor of Apoptosis Proteins ; Microtubule-Associated Proteins ; biosynthesis ; genetics ; physiology ; Neoplasm Proteins ; biosynthesis ; genetics ; physiology ; RNA Interference ; RNA, Messenger ; biosynthesis ; genetics ; RNA, Small Interfering ; genetics ; metabolism ; pharmacology ; Transfection
10.Trastuzumab in combination with chemotherapy versus chemotherapy alone for first-line treatment of HER2-positive advanced gastric or gastroesophageal junction cancer: a Phase III, multi-center, randomized controlled trial, Chinese subreport.
Lin SHEN ; Jian-ming XU ; Feng-yi FENG ; Shun-chang JIAO ; Li-wei WANG ; Jin LI ; Zhong-Zhen GUAN ; Shu-kui QIN ; Jie-jun WANG ; Shi-ying YU ; Ya-jie WANG ; Ye-ning JIN ; Min TAO ; Lei-zhen ZHENG ; Liang-xi PAN
Chinese Journal of Oncology 2013;35(4):295-300
OBJECTIVETo evaluate the efficacy and safety of trastuzumab in combination with chemotherapy versus chemotherapy alone in the first-line treatment of HER-2-positive advanced gastric or gastro-oesophageal junction cancer.
METHODSFifteen Chinese research centers are involved in the BO18255 (ToGA) study. Patients with gastric or gastro-oesophageal junction cancer were eligible for inclusion if their tumor showed overexpression of HER-2 protein by immunohistochemistry +++ or FISH-positive. Patients were randomly assigned in a 1:1 ratio to receive a chemotherapy regimen consisting of capecitabine or 5-FU plus cisplatin or chemotherapy in combination with intravenous trastuzumab. The primary endpoint was overall survival.
RESULTSEighty-five Chinese patients were enrolled in this study, of whom 84 were included in the primary analysis: trastuzumab plus chemotherapy (FP/H) (n = 36) and chemotherapy alone (FP)(n = 48). The median follow-up was 15.2 months in the FP/H group and 14.2 months in the FP group. The median survival time was 12.6 months in the FP/H group compared with 9.7 months in the FP group [hazard ratio 0.72, 95%CI (0.40; 1.29)]. Grade 3/4 adverse events were higher in the FP/H(63.9%)than FP (47.9%) groups, including neutropenia, vomiting and nausea. Two mild cardiac adverse events occurred in the FP/H group. Severe adverse events occurred in 3 cases of both two groups, respectively.
CONCLUSIONSAddition of trastuzumab to chemotherapy is well tolerated and shows improved survival in Chinese patients with advanced gastric or gastro-oesophageal junction cancer. These results are consistent with the results of ToGA whole population trial. Trastuzumab in combination with chemotherapy can be considered as a new option for patients with HER-2-positive advanced gastric or gastro-oesophageal junction cancer.
Aged ; Antibodies, Monoclonal, Humanized ; administration & dosage ; adverse effects ; Antineoplastic Combined Chemotherapy Protocols ; adverse effects ; therapeutic use ; Capecitabine ; China ; Cisplatin ; administration & dosage ; adverse effects ; Deoxycytidine ; administration & dosage ; adverse effects ; analogs & derivatives ; Esophageal Neoplasms ; drug therapy ; pathology ; Esophagogastric Junction ; Female ; Fluorouracil ; administration & dosage ; adverse effects ; analogs & derivatives ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Nausea ; chemically induced ; Neoplasm Staging ; Neutropenia ; chemically induced ; Receptor, ErbB-2 ; metabolism ; Remission Induction ; Retrospective Studies ; Stomach Neoplasms ; drug therapy ; pathology ; Survival Rate ; Trastuzumab ; Vomiting ; chemically induced