Ten glycosidic compounds were isolated from an ethanol extract of Machilus wangchiana by a combination of various chromatographic techniques including column chromatography over silica gel and Sephadex LH-20 and reversed-phase flash chromatography and HPLC. Their structures were identified by spectroscopic data analysis (IR, MS, and NMR) as icariside B1 (1), boscialin-3-O-β-D-glucopyranoside (2), pisumionoside (3), isolariciresinol-9'-O-β-D-xylopyranoside (4), 5'-methoxyisolariciresinol-9'-O-β-D-xylopyranoside (5), lyoniresinol-9'-O-β-D-xylopyranoside (6), (E) -4-hydroxyphenylprop-7-ene 4-O-β-D-glucopyranoside (7), (E) - 4-hydroxy-3-methoxyphenylprop-7-ene 4-O-α-L-rhamnopyranosyl-(1 --> 6) -β-D-glucopyranoside (8), 4-hydroxy-3-methoxyphenylprop-8-ene 4-O-β-D-xylopyraosyl-(1 --> 6) -β-D-glucopyranoside (9), and 4-hydroxy-3,5-dimethoxyphenylprop-8-ene 4-O-α-L-rhamnpyranosyl-(1 --> 6)-β-D- glucopyranoside (10), respectively.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Glycosides ; chemistry ; isolation & purification ; Lauraceae ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization

OBJECTIVETo investigate the effects of a new anticoagulant, annexin V derivative (AND) on anticoagulation and antithrombosis.

METHODSHigh and low doses of AND were given to rabbits (groups 1 and 2 respectively) by intravenous (iv) bolus injections followed by half the respective AND doses by iv infusion over 2 hours. Control groups were iv given heparin (group 3) and saline (group 4) of the same volume and procedure as that in group 1 and 2. Blood cell count, activated partial thromboplastin time (APTT), prothrombin time (PT), thrombin time (TT) and fibrinogen level were examined before and 15, 30 and 60 min after iv bolus and 2 hours after the end of iv infusion. A 3.0 mm x 15 mm balloon was put into femoral artery to induce endothelial denudation 15 min after IV bolus and the blood pressure of femoral artery was monitored until the pulse pressure recorded 0 mm Hg when the vessel was occluded completely by a thrombus. The femoral arteries were collected and the thrombi were stripped off for measuring their lengths, wet and dry weights.

RESULTSAnticoagulation parameters: APTT at 15 min after iv bolus in AND group was significantly longer than that in group 4 (P < 0.05) but shorter than that in group 3 (P < 0.05); APTT and TT in group 3 were significantly longer than those in groups 1, 2 and 4. Fibrinogen: 0.70 mg/kg AND may decrease fibrinogen. Antithrombosis values: the wet and dry weights in AND groups were significantly lighter than those in group 3 and 4 (P < 0.05). The dry weight in high-dose AND group was remarkably lighter than that in low-dose group (P = 0.029). The length of thrombus in low-dose AND group was remarkably shorter than that in group 4 (P = 0.013), but not for group 3 (P > 0.05). It was remarkably shorter in high-dose AND group than in both group 3 (P < 0.001) and 4 (P = 0.015). The time when pulse pressure equaled to 0 was longer in AND group than in group 4 (P < 0.05), but not in 3.

CONCLUSIONAND is an effective anticoagulant and antithrombosis agent, the highest anticoagulation effect occurs at 15 min after IV bolus. Its anticoagulation effect is not more potent than that of standard heparin, while antithrombosis capacity is more effective. AND in treating thrombosis clinically might be promising.

Animals ; Annexin A5 ; administration & dosage ; pharmacology ; Anticoagulants ; administration & dosage ; pharmacology ; Blood Coagulation ; drug effects ; Disease Models, Animal ; Fibrinogen ; analysis ; Humans ; Injections, Intravenous ; Male ; Partial Thromboplastin Time ; Prothrombin Time ; Rabbits ; Random Allocation ; Thrombin Time ; Thrombosis ; prevention & control

BACKGROUNDDyslipidemia, a well-known risk factor for cardiovascular disease, is common in patients with kidney disease. Recent studies discerned that dyslipidemias play a critical role in renal damage progression in renal diseases, but the association between dyslipidemias and chronic kidney disease (CKD) in the general population remains unknown. Thus, we assessed whether the growing prevalence of dyslipidemia could increase the risk of CKD.

METHODSA total of 4779 middle-aged and elderly participants participated in this study. Dyslipidemias were defined by the 2007 Guidelines in Chinese Adults. Incident CKD was defined as albuminuria and/or reduced estimated glomerular filtration rate (eGFR, < 60 ml×min(-1)×1.73 m(-2)). Regression analysis was used to evaluate the association between dyslipidemia and albuminuria/reduced eGFR.

RESULTSParticipants with hypercholesterolemia exhibited a greater prevalence of albuminuria and reduced eGFR (10.0% vs. 6.1%, P = 0.001; 4.0% vs. 2.4%, P = 0.028, respectively). Both hypercholesterolemia and low high density lipoprotein cholesterol (HDL-C) were independently associated with albuminuria (odds ratio (OR) 1.49; 95% confidence interval (CI) 1.08 - 2.07 and OR 1.53; 95%CI 1.13 - 2.09, respectively). The multivariable adjusted OR of reduced eGFR in participants with hypercholesterolemia was 1.65 (95%CI 1.03 - 2.65). As the number of dyslipidemia components increased, so did the OR of CKD: 0.87 (95%CI 0.65 - 1.15), 1.29 (95%CI, 0.83 - 2.01), and 7.87 (95%CI, 3.75 - 16.50) for albuminuria, and 0.38 (95%CI 0.21 - 0.69), 1.92 (95%CI 1.14 - 3.25), and 5.85 (95%CI 2.36 - 14.51) for reduced eGFR, respectively.

CONCLUSIONSOur findings indicate that dyslipidemias increase the risk of CKD in the middle-aged and elderly Chinese population. Hypercholesterolemia plays an important role in reducing total eGFR. Both low HDL-C and hypercholesterolemia are associated with an increased risk for albuminuria.

Aged ; Albuminuria ; epidemiology ; etiology ; physiopathology ; Cross-Sectional Studies ; Dyslipidemias ; complications ; epidemiology ; physiopathology ; Female ; Glomerular Filtration Rate ; physiology ; Humans ; Male ; Middle Aged ; Renal Insufficiency, Chronic ; epidemiology ; etiology ; physiopathology

OBJECTIVETo investigate the change pattern of substance P (SP) in the portal vein during the rectoanal inhibitory reflex (RAIR), and its physiologic significance; the influence of external splanchnic nerve of rectum and anal to the RAIR.

METHODSThe rats were divided into seven groups, among them there were six groups, which were first divided into two big groups according to whether the external splanchnic nerve to the rectum and anal were cut off, one is no cut-off external splanchnic nerve group, the other is cut-off external splanchnic nerve group. Each group were further divided, according to the distance of the balloon-sac on Foley's tube in the rectum away from anal verge, into 2, 4, 6 centimeter groups; A control group with Foley's tube put into the rectum, but the balloon-sac on Foley's tube did not pumped up with water. Measure and compare the value and change of SP in the portal vein during the RAIR.

RESULTSThe comparison of SP in portal vein, among the 2, 4 centimeter groups with cut-off external splanchnic nerve, all groups with intact external splanchnic nerve supply and control group, had no statistic difference (P>0.05). The comparison between the 6 centimeter group with intact external splanchnic nerve group and the 2, 4 centimeter groups with cut-off external splanchnic nerve, P<0.01, the statistic difference was significant. The comparison between 6 centimeter group of intact and cut-off external splanchnic nerve, P<0.01, the difference was significant.

CONCLUSIONThe reason for the stimulation on upper rectum dose not induce the RAIR is related with this stimulation result in the release of SP, the exciting mediator to internal sphincter. The external splanchnic nerve supply of rectum and anal canal have influence on the change of SP of the portal vein during RAIR.

Anal Canal ; physiology ; Animals ; Female ; Male ; Portal Vein ; physiology ; Rats ; Rats, Sprague-Dawley ; Rectum ; physiology ; Substance P ; metabolism

OBJECTIVETo study the rule of syndrome differentiation in the patients with thoracic diseases at perioperation stage.

METHODSA standard was created referring to the related literature, and it was applied to differentiate the Chinese medicine syndrome in 150 patients before and three days after thoracic operation.

RESULTSBefore operation, Chinese medicine syndromes were as differentiated as phlegm type in 45.3%, blood stasis type in 17.3%, and qi-stagnancy type in 16.0%. The patients with asthenia syndrome markedly increased after operation, accounting for 34.0% (51 patients, including qi-, yin-, and blood-deficiency syndromes). The most frequently seen intermixed syndromes were qi-deficiency with phlegm-stasis syndrome and Pi ()-deficiency with phlegm-dampness syndrome. The intermixed syndromes revealed in 37.5% and 42.0% of the patients before and after operation, respectively.

CONCLUSIONSThe syndrome in the patients with thoracic disease before operation was mostly the excessive syndrome, mainly the phlegm syndrome type; at postoperation stage, Chinese medicine syndrome in patients become asthenia in essence with excessive superficiality, which is mostly revealed as Pi-deficiency with phlegm-dampness.

Diagnosis, Differential ; Humans ; Medicine, Chinese Traditional ; Perioperative Care ; Postoperative Care ; Syndrome ; Thoracic Diseases ; diagnosis ; surgery

AIMTo study the chemical constituents of Marsdenia tenacissima (Roxb.) Wight et Arn.

METHODSTo separate compounds with various chromatography technology and to elucidate their structures by chemical and spectral analysis.

RESULTSTwo compounds were isolated from Marsdenia tenacissima and their stuctures were determined as tenacissosides J (I) and tenacissosides K (II).

CONCLUSIONCompounds I and II are new C21 steroidal glycosides.

Glycosides ; chemistry ; isolation & purification ; Marsdenia ; chemistry ; Molecular Conformation ; Molecular Structure ; Plant Stems ; chemistry ; Plants, Medicinal ; chemistry ; Steroids ; chemistry ; isolation & purification

OBJECTIVETo investigate the effects and mechanism of postoperative insulin resistance in gastrectomy patients with preoperative oral carbohydrate.

METHODSFrom April to October 2011, 60 consecutive gastric cancer patients met inclusion criteria were divided into oral carbohydrate group and placebo group by randomized double-blind principles. Resting energy expenditure (REE), fasting blood glucose, insulin and triglyceride level were detected in 4 hours preoperatively. The 500 ml carbohydrate or placebo were administrated orally 2-3 hours before anaesthesia. Two group patients underwent radical distal subtotal gastrectomy under epidural compounded intravenous anesthesia. After laparotomy and before the abdomen was closed, a piece of rectus abdominis was taken and fixed in 3% glutaraldehyde. REE, fasting blood glucose, insulin and triglyceride level were detected immediately after surgery. The changes of insulin resistance index, blood triglycerides level, REE and respiratory quotient were compared pre- and post-operatively. The changes of rectus abdominis mitochondrial ultrastructure were observed by transmission electron microscopy respectively.

RESULTSThere were 48 patients (34 males and 14 females) completed the trial. The 24 and 24 patients in oral placebo and carbohydrate groups respectively. In oral placebo group, post-operative insulin resistance index, REE, respiratory quotient, serum triglyceride level and the rectus abdominis mitochondrial damage index were 12.68 ± 3.13, (1458 ± 169) kcal/d, 0.73 ± 0.42, (0.53 ± 0.24) g/L and 1.14 ± 0.33, respectively. And the above items were 5.67 ± 1.40, (1341 ± 110) kcal/d, 0.79 ± 0.22, (1.04 ± 0.97) g/L and 0.92 ± 0.19 in oral carbohydrate groups respectively. All difference was statistically significant (t = 6.646, 2.851, 6.546, 2.542 and 2.730, all P < 0.05). Oral placebo group showed a markedly swollen mitochondria, steep membrane was not clear, mitochondria appeared vacuolated changes.

CONCLUSIONSPreoperative oral carbohydrate could reduce the insulin resistance and REE, improve the material metabolism status in radical gastrectomy patients. The possible mechanisms should be related to promotion of insulin release and protection of mitochondrial function.

Administration, Oral ; Aged ; Basal Metabolism ; Carbohydrates ; administration & dosage ; therapeutic use ; Double-Blind Method ; Female ; Gastrectomy ; Humans ; Insulin Resistance ; Male ; Middle Aged ; Mitochondria ; ultrastructure ; Postoperative Complications ; prevention & control ; Stomach Neoplasms ; surgery

AIMTo improve the profile of 20 (S)-camptothecin, a series of 20-O-linked camptothecin phenoxyacetic acid ester derivatives have been designed.

METHODSThese derivatives were synthesized by the method of acylation. Their chemical structures were confirmed with 1HNMR, IR, MS, and HRMS. The cytotoxicities of the compounds were tested by MTT assay. The in vivo antitumor activities of these esters were evaluated against mouse liver tumor H22 in mice.

RESULTSTwelve derivatives of camptothecin ester are new compounds.

CONCLUSIONIn vitro and in vivo antitumor activity has indicated that some derivatives appeared significantly more effective than topotecan in the H22 mouse liver tumoral model.

Animals ; Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Camptothecin ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; drug effects ; Esters ; chemistry ; Female ; Humans ; Inhibitory Concentration 50 ; Liver Neoplasms ; pathology ; Mice ; Mice, Inbred ICR ; Molecular Structure ; Neoplasm Transplantation ; Topotecan ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Tumor Burden ; drug effects ; Xenograft Model Antitumor Assays

Aged ; Coronary Angiography ; Coronary Artery Disease ; Coronary Disease ; diagnostic imaging ; pathology ; physiopathology ; Female ; Humans ; Male ; Middle Aged ; Tomography, Emission-Computed, Single-Photon

Animals ; Cells, Cultured ; Cyclosporine ; antagonists & inhibitors ; Fibronectins ; biosynthesis ; genetics ; Hepatocytes ; cytology ; drug effects ; PPAR gamma ; biosynthesis ; genetics ; Protective Agents ; pharmacology ; RNA, Messenger ; biosynthesis ; genetics ; Rats ; Thiazolidinediones ; pharmacology ; Transforming Growth Factor beta1 ; biosynthesis ; genetics