OBJECTIVETo study the effects of Tongxinluo on the expressions of matrix metalloproteinase-3 (MMP-3), MMP-9 and peroxisome proliferators-activated receptor gamma (PPARgamma) in atherosclerotic rabbits and explore the mechanism of its anti-atherosclerotic effect.

METHODSTwenty-four rabbits were randomized equally into control group, atherosclerotic model group (fed with high-fat diet for 14 weeks) and Tongxinluo group. The expressions of MMP-3, 9 and PPARgamma in the 3 groups were observed by means of immunohistochemistry.

RESULTSThe expressions of MMP-3, 9 and PPARgamma in the model group and Tongxinluo group were significantly higher than those in the control group (P<0.01). After high-fat diet feeding for 14 weeks, Tongxinluo group showed significantly lower expressions of MMP-3 and 9 but higher expression of PPARgamma than the model group (P<0.01).

CONCLUSIONTongxinluo can inhibit the expression of MMP-3 and 9 and increase the expression of PPARgamma, which might be the mechanism of its anti-atherosclerotic effect.

Animals ; Atherosclerosis ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; Male ; Matrix Metalloproteinase 3 ; genetics ; metabolism ; Matrix Metalloproteinase 9 ; genetics ; metabolism ; PPAR gamma ; genetics ; metabolism ; Rabbits ; Random Allocation

BACKGROUNDNon-valvular atrial fibrillation is associated with an increased risk of ischemic stroke; however, the appropriate intensity of anticoagulation therapy for Chinese patients has not been determined. The purpose of this study was to compare the safety and the efficacy of standard-intensity warfarin therapy, low-intensity warfarin therapy, and aspirin therapy for the prevention of ischemic events in Chinese patients with non-valvular atrial fibrillation (NVAF).

METHODSA total of 786 patients from 75 Chinese hospitals were enrolled in this study and randomized into three therapy groups: standard-intensity warfarin (international normalized ratio (INR) 2.1 to 2.5) group, low-intensity warfarin (INR 1.6 to 2.0) group and aspirin (200 mg per day) group. All patients were evaluated by physicians at 1, 3, 6, 9, 12, 15, 18, 21 and 24 months after randomization to obtain a patient questionnaire, physical examination and related laboratory tests.

RESULTSThe annual event rates of ischemic stroke, transient ischemic attack (TIA) or systemic thromboembolism were 2.6%, 3.1% and 6.9% in the standard-intensity warfarin, low-intensity warfarin and aspirin groups, respectively (P = 0.027). Thromboembolic event rates in both warfarin groups were significantly lower than that in the aspirin group (P = 0.018, P = 0.044), and there was no significant difference between the two warfarin groups. Severe hemorrhagic events occurred in 15 patients, 7 (2.6%) in the standard-intensity warfarin group, 7 (2.4%) in the low-intensity warfarin group and 1 (0.4%) in the aspirin group. The severe hemorrhagic event rates in the warfarin groups were higher than that in the aspirin group, but the difference did not reach statistical significance (P = 0.101). The mild hemorrhagic and total hemorrhagic event rates in the warfarin groups (whether in the standard-intensity warfarin group or low-intensity warfarin group) were much higher than that in the aspirin group with the annual event rates of total hemorrhages of 10.2%, 7.6% and 2.2%, respectively, in the 3 groups (P = 0.001). Furthermore, there was no significant difference in all cause mortality among the three study groups.

CONCLUSIONIn Chinese patients with NVAF, the warfarin therapy (INR 1.6 - 2.5) for the prevention of thromboembolic events was superior to aspirin.

Aged ; Aged, 80 and over ; Anticoagulants ; administration & dosage ; therapeutic use ; Aspirin ; administration & dosage ; therapeutic use ; Atrial Fibrillation ; drug therapy ; Female ; Humans ; Male ; Middle Aged ; Warfarin ; administration & dosage ; therapeutic use

Qigui Tongfeng tablet (QLTFT) is a traditional Chinese medicine with good effect for treating gout. Here, network pharmacology method and molecular similarity analysis were utilized to study the effective substance basis and molecular mechanism of the QLTFT on the gout. The similarity to the medicinal compounds is reflected in the Tanimoto coefficient that gives the structural similarity of two compounds. Operationally, similar modifiers were described as pairs of concepts with a similarity score of 0. 500. The results of the molecular similarity analysis suggested that the flavonoids in QLTFT could be new leads for gout. Furthermore, complex biological systems may be represented and analyzed as computable networks. Two important properties of a network were degree and betweenness. Nodes with high degree or high betweenness may play important roles in the overall composition of a network. And the results of network analysis showed that dongbeinine, verticinone-N-oxide, verticine N-oxide, peimine, peiminine, isobaimonidine, dongbeirine, peimisine and simi-arenol which with high degree acted on xanthine dehydrogenase/oxidase, matrix metalloproteinase-9, an arachidonate 5-lipoxygenase-activating protein, tyrosine-protein kinase and etc. Inhibition of these targets can prevent the formation of uric acid, reduce inflammation by uric acid and regulate the body's immune response. Thus, these compounds may be the main effective substance basis. The research results not only reveals its molecular mechanism, but also provide a theoretical basis for the quality control of drugs and clinical application.
Gout ; drug therapy ; Humans ; Medicine, Chinese Traditional ; Pharmacology ; methods ; Tablets ; Technology, Pharmaceutical ; methods

Objective To study the relationship between peripheral blood hemoglobin (HB) and blood pres- sure.Methods We performed a cross-sectional analysis in 1153 subjects aged 29-83 years.Waist circumfer- ence,HB,blood pressure,high-density lipoprotein cholesterol(HDL-C),low-density lipoprotein cholesterol(LDL- C),triglycerides (TG),total cholesterol (TC) were determined.Results ①With the increasing of blood pres- sure,HB had a clearly increasing trend (HB,normotensive:137.5?14.7 vs prehypertension:143.4?14.4 vs hy- pertension:144.3?13.8 g/L,P

AIMTo study bioequivalences of bambuterol and its metabolites terbutaline in 20 healthy male volunteers.

METHODSA single oral dose of domestic bambuterol capsule or imported bambuterol tablet was given according to a randomized 2-way cross-over design. The plasma bambuterol and terbutaline concentrations were determined by high performance capillary zone electrophoresis (HPCZE).

RESULTSThe pharmacokinetic parameters of the capsule and tablet of bambuterol: AUC0-1 were (72 +/- 18) and (72 +/- 13) microgram.h.L-1, Cmax were (8.1 +/- 1.8) and (9.2 +/- 2.3) microgram.L-1, Tmax were (3.6 +/- 1.3) and (3.7 +/- 1.0) h, respectively; terbutaline: AUC0-t were (129 +/- 32) and (130 +/- 34) microgram.h.L-1, Cmax were (7.8 +/- 2.2) and (8.5 +/- 2.9) microgram.L-1, Tmax were (5.4 +/- 0.8) and (5.6 +/- 1.1) h, respectively. The bioavaiability of the capsule was (100 +/- 16)% (bambuterol) and (101 +/- 13)% (terbutaline).

CONCLUSIONThe results demonstrated that the two preparations of bambuterol and terbutaline were bioequivalent by analysis of variance, with two-one sided test at 90% confidential level.

Administration, Oral ; Adult ; Area Under Curve ; Biological Availability ; Capsules ; Chromatography, High Pressure Liquid ; Cross-Over Studies ; Electrophoresis, Capillary ; Humans ; Male ; Tablets ; Terbutaline ; administration & dosage ; analogs & derivatives ; blood ; pharmacokinetics ; Therapeutic Equivalency

The aim of this study was to look for the chemical constituents from the rhizomes of Dryopteris sublaeta. The fresh plant was extracted twice with boiling water, the extract was concentrated to small volume under reduced pressure at 50 degrees C. The concentrated material was partitioned with ether, ethyl acetate and n-butanol. The fraction of ethyl acetate was repeatedly chromatographied over silica gel and Sephadex LH-20 columns. Structures of pure compounds were established on the basis of their physiochemical and spectral data. Nine compounds were obtained and identified as sublaetentin A (1), sublaetentin B (2), sublaetentin C (3), sublaetentin D (4), matteuorienate A (5), matteuorienate C (6), arbutin (7), 3-methoxy-4-hydroxyphenyl-1-O-beta-D-glucopyranoside (8) and 3,4-dimethoxyphenyl-1-O-beta-D-glucopyranoside (9). Compounds 1 - 4 are new compounds, the others were isolated from this plant for the first time.
Arbutin ; chemistry ; isolation & purification ; Dryopteris ; chemistry ; Flavanones ; chemistry ; isolation & purification ; Flavonoids ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Glycosides ; chemistry ; Molecular Structure ; Plant Extracts ; chemistry ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry

OBJECTIVETo evaluate the influence of veneer application on failure behavior and reliability of lithium disilicate glass-ceramic (LDG) crowns of maxillary first molar, and thus to reveal the failure mechanism of bilayered LDG crowns.

METHODSTwenty-six LDG maxillary first molar crowns were fabricated in a dental laboratory using IPS e. max Press or IPS e. max Press/Ceram. The crowns were randomly assigned into two groups (with or without veneer application) with thirteen in each group. The crowns were cemented on composite resin dies. After storage in water for one week, the sliding-contact fatigue test was performed by sliding the steatite ceramic ball indenter (6 mm in diameter) from central fossa up to the lingual surface of disto-buccal cusp, cyclic loaded 1 200 000 times with a weight of 100 N at 2 Hz with a fatigue chewing simulator. Survived specimens were subjected to single-load-to-fracture testing using a steatite ceramic ball of 6 mm in diameter at a cross-head speed of 0.5 mm/min in a universal testing machine. Fracture load values were recorded and analyzed with t test. Weibull modulus was calculated to evaluate structure reliability. Fractographic analysis was carried out to determine fracture modes of the failed specimens by a stereomicroscope and a scanning electron microscope (SEM).

RESULTSStatistical analysis results indicated a significant difference of the fracture load values between monolithic group [(2071.23 ± 397.05) N] and bilayered group [(1483.41 ± 327.87) N] (P < 0.001). Monolithic and bilayered groups present similar Weibull modulus (95% confidence interval) as 6.15 (5.15 ∼ 7.15) and 5.54 (4.01 ∼ 7.08) respectively, with no significant difference (the confidence bounds overlapped with each other). Bulk fracture initiating from the middle of oblique ridge of the first maxilla molar was the primary failure mode of monolithic/bilayered LDG crowns. Crack propagation initiated from core-veneer interfacial defects was another major failure mode of bilayered all-ceramic crowns.

CONCLUSIONSVeneer application has some influence on fatigue failure of LDG crowns, but shows no effect on structure reliability. Accumulated damage combined with tensile stress concentration on the surface of veneer layer and defects within core-veneer interface lead to initiating of cracks. The mechanical property of veneering materials should be increased, and procedure of veneer application should be standardized and improved in order to reduce the failure rate of LDG molar crowns.

Crowns ; Dental Porcelain ; chemistry ; Dental Restoration Failure ; Materials Testing ; Molar

AIMTo study the chemical constituents of Dryopteris sublaeta Ching et Hsu.

METHODSFresh plant of Dryopteris sublaeta ching et hsu was extracted twice with boiling water, concentrated to small volume under reduced pressure at 50 degrees C. The concentrated material was partitioned with ether, ethyl acetate, and n-butanol. The fraction of ethyl acetate extract was chromatographed over macroporous adsorption resin (Diaion HP-20) eluted with a mixture of H2O and MeOH in increasing MeOH content. Their fractions from resin were repeatedly chromatographed over Toyopearl HW-40, Sephadex LH-20 and silica gel column chromatography. The compounds were identified on the basis of their physiochemical and spectral data.

RESULTSFour compounds were obtained and identified as 3,5-dihydroxy-stilbene-3-O-neohesperidoside (1), 3,5-dihydroxy-stilbene-3-O-beta-D-glucoside (2), polydotin peceid (3) and 3,5,4'-trihydroxy-bibenzyl-3-O-beta-D-glucoside (4).

CONCLUSIONCompound 1 is a new compound, the others were isolated from Dryopteris for the first time.

Dryopteris ; chemistry ; Glycosides ; chemistry ; isolation & purification ; Molecular Structure ; Plants, Medicinal ; chemistry ; Stilbenes ; chemistry ; isolation & purification

This study is to investigate the antitumor activity of CIP-36 on multidrug resistant human oral squamous carcinoma cell line (KBV200 cells) in vitro and the possible anticancer mechanisms. MTT assay, Hoechst fluorescein stain, RT-PCR and immunohistochemistry were carried out on KBV200 and KB cells. The growth of many tumor cells was obviously inhibited by CIP-36, especially the multidrug resistant cells KBV200. Obvious apoptosis could be observed in the Hoechst 33342 staining experiments. The results of RT-PCR showed that the levels of p53, p21, caspase-3 and bax mRNA increased, and meanwhile the expression of mdr-1 and bcl-2 mRNA decreased in a dose-dependent manner. The data were significantly different from that of vehicle. The expression of P-gp significantly decreased with the increasing dosage of CIP-36 examined by immunohistochemistry. It can be concluded that CIP-36 could change resistance-related genes and proteins to overcome multidrug resistance in the KBV200 cell line.
ATP Binding Cassette Transporter, Sub-Family B ; ATP-Binding Cassette, Sub-Family B, Member 1 ; genetics ; metabolism ; Antineoplastic Agents, Phytogenic ; administration & dosage ; pharmacology ; Apoptosis ; drug effects ; Carcinoma, Squamous Cell ; metabolism ; pathology ; Caspase 3 ; genetics ; metabolism ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Dose-Response Relationship, Drug ; Drug Resistance, Multiple ; Drug Resistance, Neoplasm ; Humans ; KB Cells ; Mouth Neoplasms ; metabolism ; pathology ; Podophyllotoxin ; administration & dosage ; analogs & derivatives ; pharmacology ; Proto-Oncogene Proteins c-bcl-2 ; genetics ; metabolism ; Proto-Oncogene Proteins p21(ras) ; genetics ; metabolism ; RNA, Messenger ; metabolism ; Tumor Suppressor Protein p53 ; genetics ; metabolism ; bcl-2-Associated X Protein ; genetics ; metabolism

AIMTo study the chemical constituents of Dryopteris sublaeta Ching et Hsu.

METHODSFresh plant of Dryopteris sublaeta Ching et Hsu was extracted twice with boiling water, the extract was concentrated to small volume under reduced pressure at 50 degrees C. The concentrated material was partitioned with ether, ethyl acetate, and n-butanol. The fraction of ether extract was chromatographed over silica gel column. The compounds were identified on the basis of their physiochemical and spectral data.

RESULTSFour compounds were obtained and identified as 2 (S)-5, 7, 3'-trihydroxy-6, 8-dimethyl-5'-methoxyflavanone (1), matteucinol (2), desmethoxymatteucinol (3) and 5, 7, 2'-trihydroxy-6, 8-dimethylflavanone (4).

CONCLUSIONCompound 1 is a new one, the others were isolated from Dryopteris for the first time.

Chromones ; chemistry ; isolation & purification ; Dryopteris ; chemistry ; Flavanones ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry