Objective To compare analgesic efficacy of intravenous postoperative and preemptive analgesia with flurbiprofen axetil combined with small dose of morphine and with morphine alone. Methods One hundred and twenty patients were randomly divided into four groups: group A,morphine 30 mg +0.9% NaCl for postoperative analgesia,n=30;group B,morphine 20 mg +0.9% NaCl for postoperative analgesia,n=30;group C,flurbiprofen axetil 100 mg + morphine 20 mg +0.9% NaCl for postoperative analgesia,n=30;group D,flurbiprofen axetil 100 mg before operation + morphine 20 mg +0.9% NaCl for postoperative analgesia,n=30.The drugs in each group were diluted to 100 mL and infused by a pump at a rate of 2 mL/h with a patient-controlled analgesia(PCA)bolus of 2 mL after a loading dose of 5 mL.The visual analogue scale(VAS),demanding times for PCA and incidence of side effects were recorded during the period of postoperative 24 h. Results The VAS of group B at 3 h after operation was significantly higher than those of the other three groups(P

Pain is one of the common clinical symptom, previous studies have implicated sodium channels as a key constituent in pain signaling. Sodium channel blockers with efficient sodium channel blockade effect play an important role in analgesic treatment. However, most drugs used in clinic have many drawbacks and can not meet the demand of the clinical use. Therefore, for the development of new generation of sodium channel blockers, it is of great significance to find small molecule sodium channel blocking lead compounds with novel chemical scaffolds and new structures, sodium channel blocking activity and structure-activity relationship are discussed in detail, and current problems and trends in future research are also emphasized.
Analgesics ; chemistry ; pharmacology ; therapeutic use ; Animals ; Drug Design ; Humans ; Molecular Structure ; Neuralgia ; drug therapy ; Pain ; drug therapy ; Pain Measurement ; Sodium Channel Blockers ; chemistry ; pharmacology ; therapeutic use ; Sodium Channels ; drug effects ; Structure-Activity Relationship

OBJECTIVETo investigate the effect of ursolic acid (UA) on the alloxan-induced myocardial fibrosis in mice and discuss the possible mechanism.

METHODSDiabetes was produced by a single injection of alloxan (70 mg/kg, i.v.) in mice. The mice were randomly divided into four groups: normal control group, model group, ursolic acid group (UA, 35 mg/kg, p.o.) and benazepril group (5 mg/kg, p. o.), and continuous administrated for 8 weeks. The blood glucose was measured 24 hours after the last administration. Detected the specific biochemical of myocardial tissue: superoxide dismutase (SOD), malondialdehyde (MDA) and hydroxyproline(HYP). Using masson staining to observe the morphology of the myocardial tissue. Immunohistochemistry was employed to determine the protein levels of TGF-beta1.

RESULTSCompared to normal group, the blood glucose, heart index, myocardial tissue MDA, HYP level were increased, and SOD activities were decreased in the diabetic mice, Masson stain showed that myocardial cells disarranged, myocardial collagen fibrosis hyperplasia. Meanwhile, the protein expression of TGF-beta1 was increased in model group. The UA group improved all the above significantly.

CONCLUSIONUA improves the myocardial collagen fibrosis in diabetic mice induced by alloxan, its mechanism may be related to inhibiting the expression of TGF-beta1 and antioxidation.

Animals ; Blood Glucose ; Collagen ; metabolism ; Diabetes Mellitus, Experimental ; metabolism ; pathology ; Fibrosis ; Hydroxyproline ; metabolism ; Male ; Malondialdehyde ; metabolism ; Mice ; Mice, Inbred Strains ; Myocardium ; metabolism ; pathology ; Oxidative Stress ; Superoxide Dismutase ; metabolism ; Transforming Growth Factor beta1 ; metabolism ; Triterpenes ; pharmacology

OBJECTIVETo investigate the influence of total flavonoids of epimedium (TFE) on the streptozocin (STZ)-induced kidney injury in diabetic rats and discuss the possible mechanism.

METHODSDiabetes was produced by a single injection of streptozocin (40 mg/kg, iv) in male SD rats. The rats were randomly divided into three groups (n = 10): control group, model group and TFE group (100 mg/kg, ig). Animals were sacrificed 12 weeks later. The level of blood glucose, blood urea nitrogen (BUN) and creatinine (Cr) as well as the renal index were determined. Detect the specific biochemical of renal tissue: superoxide dismutase (SOD), malondialdehyde (MDA). Use masson staining to observe the morphology of the renal tissue. Immunohistochemistry was employed to determine the protein levels of transforming growth factor-beta1 (TGF-beta1).

RESULTSCompared to control group, the enhancement of blood glucose, renal index, BUN and Cr was found in model group, which was significantly attenuated by treatment with TFE. Meanwhile, elevated MDA level in renal tissue as well as decreased SOD activities in renal tissue were significantly remitted by TFE. Furthermore, TFE decreased the expression of TGF-beta1.

CONCLUSIONTFE can evidently relieve renal damage in rats with diabetic nephropathy induced by STZ, which might be related to antioxidation and modulating the expression of TGF-beta1 protein.

Animals ; Diabetes Mellitus, Experimental ; metabolism ; Diabetic Nephropathies ; metabolism ; prevention & control ; Epimedium ; chemistry ; Flavonoids ; pharmacology ; Kidney ; drug effects ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley

Undifferentiated and differentiated 3T3-L1 adipocytes were treated with 100 ng/ml tumor necrosis factor-?(TNF-?),and peroxisome proliferator-activated receptor-?2 (PPAR-?2) mRNA expression and adiponectin secretion in cultured cells were measured.The results showed that TNF-?suppressed PPAR-?2 mRNA expression and adiponeetin secretion in 3T3-L1 adipocytes (P

The growth curve of single cell organisms in batch cultivation could divide into 6 phases, lag phase, acceleration phase, log phase, deceleration phase, stationary phase, and death phase, based on specific growth rate during cultivation process. There were significantly differences between deceleration phase and the other phases in cell growth, substrate consumption, product formation, and genes express profile. The deceleration phase was highly important to fermentation process. However, cognizing and teaching to the deceleration phase had been considerably weakened since a long period. So it should be strengthened.

Objective: To evaluate the therapeutic effect of cystic de compression (CD) operation autosomal dominant polycystic kidney disease(APKD) based on clinical material, experience and related theory. Methods: Thirty-nine APKD received CD operation(unilateral 31 cases, bilateral 8 cas e s) in our hospital from 1985 to 1995. Four main parameters, cystic renal enlargi ng rate(CRER)，lumbar pain recurring rate(LPRR)，blood pressure elevating rate(B PER) and renal function abnormal rate(RFAR), were observed 3, 6, 12, 36 and 60 months after CD operation. And the changes were analyzed based on related theory . Results: The changes of 4 main parameters on 5 different time points post operation in unilateral 31 cases were:（1）CRER 19.4%,38.7%,61.3%,1 0 0% and 100%; （2）LPRR 12.9%,48.4%,71.0%,100% and 100%; （3）BPER 6.5%,22.6%,4 1.9%,71.0% and 96.8%;（4） RFAR 3.2%, 12.9%,22.6%,74.2% and 96.8% respectively. Conclusion: During a short period, CD operation can relieve th e lumbar pain, but it is not certain for improving CRER,BPER and RFAR. in the lo ng run, the therapeutic effect is not sure.

The active ingredient of traditional Chinese medicine, silybin (SBN), can inhibit the proliferation of cancer cells and enhance the anticancer effect of doxorubicin (DOX). However, due to non-targeting and short half-life of SBN and DOX, as well as different administration routes and pharmacokinetic processes, this combination drug cannot act on the tumor in the set order, seriously eliminating the synergistic effect between them and limiting the effect in vivo. Therefore, we intended to construct a nano-delivery system based on molybdenum disulfide (MoS₂), modified by polyethylene glycol (PEG) and sialic acid (SA), and co-loaded with SBN and DOX. The system induced the release of combined drugs under the dual-stimulation of pH and near infra-red (NIR), increased the free concentration of intracellular drugs, so as to achieve the synergistic effect between them. The animal welfare and experimental procedures were in accordance with the regulations of the Animal Ethics Committee of Fujian University of Traditional Chinese Medicine. MoS₂-PEG-SA-SBN/DOX circulated in vivo, and effectively accumulated at tumor sites through enhanced permeability and retention effect (EPR) and SA-mediated active targeting. Under near infrared light irradiation, MoS₂-PEG-SA-SBN/DOX realized the combination of synergistic chemotherapy and photothermal therapy for tumor, thus achieving excellent anti-tumor effect in vivo. This study can provide a new idea and strategy for the clinical treatment of lung cancer. Taken together, MoS₂-PEG-SA-SBN/DOX can offer a new idea and strategy for the clinical treatment of lung cancer.

AIMTo design and synthesize new methoxyl carbazole analogues as antitumor compounds.

METHODSMethoxyl-nitrobiphenyls (3a-3c) were prepared through the Ullmann reaction of 4,5-dimethoxyl-2-bromonitrobenzene and methoxyl-iodobenzene compounds with the catalysis of copper powder, and then reduced by P(EtO)3 to obtain methoxyl carbazoles 4a-4c. The modification at 9-position of the methoxyl carbazoles (4a-4c) gives 16 carbazole derivatives (5a-5p). These compounds were confirmed by 1HNMR, MS, IR and elemental analysis.

RESULTIn vitro antitumor activities evaluation in vitro demonstrated that IC50 value of the target compounds 4c, 5a, 5b, 5g, 5h, 5i, 5l, 5n and 5p against HT-29 cells were 12.1, 10.6, 8.1, 3.1, 4.4, 10.1 and 9.2 micromol x L(-1) respectively, and IC50 value of the target compound 4a against KB was 17.7 micromol x L(-1).

CONCLUSIONSome of the target compounds have better inhibitory effects against H-29 and KB cells.

Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Carbazoles ; chemical synthesis ; chemistry ; pharmacology ; HT29 Cells ; drug effects ; Humans ; KB Cells ; drug effects ; Molecular Structure

OBJECTIVETo study the related factors of right recurrent nerve nodal involvement in esophageal cancer.

METHODS280 patients with thoracic esophageal cancer received esophagectomy and right recurrent nerve node dissection. The clinicopathological data were analyzed retrospectively. Univariate data were analyzed by chi-square test, and multivariate data were analyzed by logistic regression.

RESULTSThe right recurrent nerve nodal metastasis was found in 76 cases (27.1%, 76/280). In the 979 excised right recurrent nerve nodes, metastases were found in 118 nodes (12.1%). The tumor staging, the total number of involved lymph nodes, vascular invasion, the number of lymph node metastases in the thorax, the number of lymph node metastasis in the abdomen, subcarinal node metastasis, and peri-esophageal lymph node metastasis were independent risk factors of right recurrent nerve node metastasis in esophageal carcinoma.

CONCLUSIONRight recurrent nerve lymph nodes should be dissected in those patients with high risk factors of lymph node metastasis in thoracic esophageal carcinoma.

Adult ; Aged ; Esophageal Neoplasms ; pathology ; surgery ; Esophagectomy ; Female ; Humans ; Logistic Models ; Lymph Node Excision ; Lymph Nodes ; pathology ; surgery ; Lymphatic Metastasis ; Male ; Middle Aged ; Recurrent Laryngeal Nerve ; pathology ; Retrospective Studies ; Risk Factors