Objective: To study the potential apoptotic effect of arundoin on human prostatic cancer cells. Methods: Arundoin was isolated and purified from the crude ethanol extract of Imperatae Rhizoma. Human prostatic cancer cell line PC3 was treated with arundoin. The relative cell viabilities were determined by MTT assay; Apoptosis was analyzed by Annexin V/PI dual staining with flow cytometry; The protein expression levels of Poly ADP ribose polymerase (PARP) and other apoptotic related proteins were detected by Western blotting. Results: Arundoin (20, 40, and 80 μmol/L) reduced the viability of PC3 cells dose- and time-dependently. Moreover, arundoin induced apoptosis in PC3 cells. Western blotting analysis showed that arundoin up-regulated the expression level of PARP in a dose-dependent manner. In addition, apoptosis related proteins such as Bax, Bcl-2, and casapases were all affected by arundoin. Conclusion: Arundoin could induce apoptosis in human prostatic cancer cells, which provides novel information for clinical application of arundoin and its preparations for the prostatic cancer patients.

Contemporary Chinese medicine supposes that the blood stasis is a pivotal pathogenic mechanism of coronary heart disease (CHD). The presentation and pathological changes in acute cardiovascular events of CHD, however, seem to exceed the etiological category of blood stasis. The toxin or the combination and transformation of toxin and blood stasis of Chinese medicine are involved in the pathogenesis of CHD according to the basic theory of Chinese medicine. Therefore, to establish a criterion of differentiation and diagnosis for stable CHD caused by etiological toxin of Chinese medicine applying clinical epidemiological method, which is correlated to concept of evidence based medicine, is significant in early recognizing high risk patients and improving treatment of CHD.
Coronary Disease ; diagnosis ; pathology ; Humans ; Integrative Medicine ; Medicine, Chinese Traditional

Objective To investigate the effects of fosinopril sodium pre-treatment combined with ischemic postconditioning on rat serum and myocardial oxidative stress and proinflammatory cytokines post ischemia/reperfusion. Methods Sixty Sprague-Dawley rats were randomly divided into sham group ( n = 15 ) , ischemia/reperfusion group ( 30 minutes in situ occlusion of the left anterior descending artery followed by 1 hour nitrotetrazolium blue chloride staining, SOD content was examined by colorimetric method, MDA content was detected using thiobarbituric acid method, serum levels of Interleukin-1α (IL-lα), Interleukin-6 (IL-6) and tumor necrosis factor-a (TNF-α) were examined by radioimmunoassay, IL-lα, IL-6 and TNF-α levels of myocardial tissue were detected by ELISA. Results Compared with I/R group, myocardial enzymes and infarction size were significantly decreased ( P < 0. 05, P < 0.01) , serum SOD content was increased and MDA content was decreased (allP<0.01), serum and myocaidial levels of IL-1α, IL-6 and TNF-α were significantly reduced (P<0. 05,P<0.05, P<0.01) in IPoC group. Compared with IPoC group, fosinopril sodium pretreatment further reduced infarction size and myocardial enzyme CK-MB ( P < 0.05 ) , increased SOD content ( P < 0. 05 ) while reduced serum IL-6 and myocaidial tissue TNF-a (P <0. 05, P <0.01). Conclusion Pretreatment with fosinopril sodium enhanced the protective effect of IPoC on rat myocardium underwent I/R injury, possibly by reducing oxidative stress and early inflammatory reaction.

OBJECTIVETo observe the effect of Tribuli saponins (TS) on left ventricular remodeling after acute myocardial infarction (AMI) in rats with hyperlipemia.

METHODSA composite model of myocardial infarction and hyperlipemia was established and treated with TS to observe its effect on cardiac structure and function by echocardiography.

RESULTS(1) Cardiac function: As compared with the model group, the fractional shortening (FS) and ejection fraction (EF) got increased, and the left ventricular end diastolic volume (LVEDV) and systolic volume (LVESV) got lower in the groups treated with high dose TS and simvastatin (P < 0.05 or P < 0.01), but difference between the two treated groups was insignificant. (2) Cardiac structure: As compared with the model group, the left ventricular dimension end diastole (LVDd) and systole (LVDs) in the groups treated with high dose TS and simvastatin got lower (P < 0.05 or P < 0.01). No treatment showed any effect on the thickness of ventricular wall. (3)Ventricular weight index: Both high dose TS and simvastatin could decrease the left ventricular weight index (LVWI) (P < 0.05).

CONCLUSIONTS could attenuate the left ventricular remodeling after acute myocardial infarction to certain extent, and improve cardiac function in the early phase after AMI, thus playing an important role in controlling morbidity and mortality of cardiac events and long-term prognosis.

Animals ; Cardiomegaly ; drug therapy ; pathology ; Drugs, Chinese Herbal ; pharmacology ; Echocardiography ; Heart Ventricles ; pathology ; Hyperlipidemias ; blood ; complications ; drug therapy ; Lipids ; blood ; Male ; Myocardial Infarction ; complications ; diagnostic imaging ; drug therapy ; Organ Size ; Rats ; Rats, Sprague-Dawley ; Saponins ; pharmacology ; Tribulus ; Ventricular Remodeling ; drug effects

To study the drug-drug interaction of morinidazole and warfarin and its application, a sensitive and rapid liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the determination of R-warfarin/S-warfarin in human plasma. In a random, two-period crossover study, 12 healthy volunteers received a single oral dose of 5 mg racemic warfarin in the absence and presence of morinidazole. Blood samples were collected according to a pre-designed time schedule. R-warfarin, S-warfarin and methyclothiazide were extracted with ethylether : methylenechloride (3 : 2), then separated on a Astec Chirobiotic V (150 mm x 4.6 mm ID, 5 microm) column using 5 mmol x L(-1) ammonium acetate (pH 4.0) - acetonitrile as mobile phase at a flow-rate of 1.5 mL x min(-1). The mobile phase was splitted and 0.5 mL x min(-1) was introduced into MS. A tandem mass spectrometer equipped with electrospray ionization source was used as detector and operated in the negative ion mode. Quantification was performed using multiple reaction monitoring (MRM). The resolution of warfarin enantiomers is 1.56. The linear calibration curves for R-warfarin and S-warfarin both were obtained in the concentration range of 5 - 1 000 ng x mL(-1). Intra- and inter-day relative standard deviation (RSD) for R-warfarin and S-warfarin over the entire concentration range across three validation runs was both less than 10%, and relative error (RE) ranged from -4.9% to 0.7%, separately. The method herein described is effective and convenient, and suitable for the study of metabolic interaction between morinidazole and warfarin. The results showed that coadministration of warfarin with morinidazole did not affect the pharmacokinetics of either R-warfarin or S-warfarin.
Anticoagulants ; blood ; pharmacokinetics ; Chromatography, Liquid ; Drug Interactions ; Humans ; Nitroimidazoles ; blood ; pharmacokinetics ; Spectrometry, Mass, Electrospray Ionization ; Stereoisomerism ; Tandem Mass Spectrometry ; Warfarin ; blood ; pharmacokinetics

OBJECTIVETo observe the efficacy and safety of Yigu capsule (YGC, a Chinese herbal compound preparation) in treating postmenopausal osteoporosis (PMO) and to explore its possible mechanism.

METHODSThe clinical study was conducted adopting prospective, randomized, double blinded method for 6 months with placebo and positive controls. Two hundred and ten PMO patients with confirmed diagnosis were divided into the YGC group, the osteocalcin group and the placebo group, they were treated with YGC, osteocalcin capsule and placebo capsule, respectively. The symptoms, as new fracture and ostealgia, bone mineral density (BMD) of the 2nd to the 4th lumbar vertebrae (L24) and upper segment of femur, blood and urinary indexes for bone metabolism, sex hormone level and adverse reaction were observed.

RESULTSIn the YGC group, the total effective rate was 95.50%, no new fracture occurred, which was significantly better than that in the other two groups (P < 0.05). The increase of BMD was 9.83% in L2-4, 4.09% in femoral neck, 4.60% in Wards triangle, 3.00% in greater trochanter, which were better than those in the placebo group (P < 0.05, P < 0.01). As compared with the placebo group, in the YGC group, levels of urinary oxyproline hydroxyproline/creatinine, urinary calcium/creatinine were lower, serum and bone alkaline phosphatase, osteocalcin, estradiol, and estradiol/testosterone were higher, but with no difference in level of testosterone. In the observation period, no abnormal findings in blood and urine routine examination as well as in liver and renal function were found. Mild, transient gastro-intestinal response occurred in individual patients but it didn't affect the treatment.

CONCLUSIONYGC could treat PMO effectively, it could obviously increase the BMD of lumbar vertebrae and hip, elevate the alleviating rate of ostealgia and incessant motion time, without new compressive fracture of vertebrae, and without any related adverse reaction. YGC could not only promote the formation, but also inhibit the absorption of bone, and increase the sex hormone level, therefore, it is a pure Chinese herbal compound preparation that worths further deep research and development.

Absorptiometry, Photon ; Bone Density ; Capsules ; Double-Blind Method ; Drugs, Chinese Herbal ; therapeutic use ; Estradiol ; blood ; Female ; Humans ; Middle Aged ; Osteoporosis, Postmenopausal ; drug therapy ; physiopathology ; Phytotherapy ; Prospective Studies ; Testosterone ; blood

Since 1980s, the treatment of acute myocardial infarction (AMI) has entered the era of revascularization of infarction-related artery. There is still shortness of ideal strategy in modern medicine for comprehensive intervention aiming at the complex pathological links such as myocardial no-reflow, slow-reflow and reperfusion injury after revascularization. Therefore, combining traditional Chinese medicine with modern medicine, selecting effective drugs or prescriptions, and exploring their effective ingredients and portions of them as well as the mechanisms of the combinations in promoting myocardial capillary angiogenesis and cardiac muscle cell differentiation, and regulating the repairing process of inflammatory reaction will provide new intervening target directions and comprehensive intervening patterns for the prevention and treatment of AMI.
Angioplasty, Balloon, Coronary ; Combined Modality Therapy ; Drug Therapy ; methods ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Medicine, Chinese Traditional ; Myocardial Infarction ; therapy ; Phytotherapy ; methods

In the research and development of new drugs, it is very important to investigate the in vitro metabolism of candidate drugs. Traditional models such as liver microsomes have many limitations, while the in vitro model of recombinant human drug metabolizing enzymes is considered as an important and useful approach because of its convenient access, stable activity and low cost. In this study, six major human UDP-glucuronosyltransferases (UGTs) genes (UGT1A1, 1A3, 1A4, 1A6, 1A9 and 2B7) were cloned from human liver cDNA and heterologously expressed in Saccharomyces cerevisiae and baculovirus-infected insect cell. UGT1A1, 1A3, 1A6 and 1A9 were successfully expressed in yeast and showed glucuronidation activity against a variety of different structural types of substrates, but their activities were low. All six UGTs were successfully expressed and exhibited significantly improved glucuronidation activity when Trichopolusia ni cells BTI-TN5B1-4 (High Five) were used as the host. The recombinant human UGTs expressed in insect cells can catalyze the glucuronidation of their specific substrates, and the glucuronidation products were synthesized at milligram-scale with yields of 13%-66% for the first time, of which the structures were identified via MS, ¹H NMR, and ¹³C NMR spectroscopic analysis. Above all, the recombinant human UGTs yeast and insect cell expression systems constructed in this study can be used for in vitro metabolism evaluation in the early stage of new drugs research and development, and also provide a new tool for the synthesis of glucuronide metabolites.

OBJECTIVETo investigate the predictive value of elevated fibrinogen and high-sensitivity C-reaction protein (hs-CRP) level on cardiovascular events in patients with stable coronary artery disease (CAD).

METHODSFrom January 2002 to November 2002, 185 patients (aged 47 - 85 years) with stable CAD referred for coronary angiography were enrolled and divided into control-F (fibrinogen level < or = 4.0 g/L, n = 104) and elevated-F (fibrinogen level > 4.0 g/L, n = 81), or control-hs (hs-CRP < or = 3.0 mg/L, n = 99) and elevated-hs (hs-CRP> 3.0 mg/L, n = 86). Exclusion criteria included cardiomyopathy, New York Heart Association class IV congestive heart failure, recent myocardial infarction or coronary artery revascularization and cancer. During three years follow-up, cardiovascular death, myocardial infarction, congestive heart failure, stroke and other vascular events were assessed.

RESULTSA total of 21 cardiovascular nonfatal events and 10 cardiovascular deaths were observed. Cardiovascular events was significantly higher in patients in elevated-F group than that in control-F group [23.46% vs. 11.54%, cholesterol-, body mass index-, smoking-, and hypertension-adjusted relative risk 1.97, 95% CI (1.68 to 2.40), P < 0.05] and in elevated-hs group than in control-hs group [24.42% vs. 10.10%, adjusted relative risk 2.32, 95% CI (1.76 to 2.89), P < 0.05]. The relative risk of cardiovascular events for patients with fibrinogen > 4.0 g/L and hs-CRP > 3.0 mg/L was 3.84 (P < 0.05), 95% CI (2.80 to 4.99) compared with patients with fibrinogen < or = 4.0 g/L and hs-CRP < or = 3.0 mg/L.

CONCLUSIONBoth fibrinogen and hs-CRP are independent important predictors of cardiovascular nonfatal and fatal events in patients with stable CAD. Combination of elevated fibrinogen and hs-CRP increased their predictive value for cardiac events.

Aged ; Aged, 80 and over ; C-Reactive Protein ; metabolism ; Coronary Angiography ; Coronary Artery Disease ; blood ; pathology ; Female ; Fibrinogen ; metabolism ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Predictive Value of Tests ; Risk Factors

OBJECTIVETo investigate hereditary susceptibility to coronary heart disease (CHD) in apolipoprotein E(apo E) and apo B polymorphisms of youths.

METHODSPolymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) was used to analyze apoE, apoB Xba I, apoB 3' variable number of tandem repeat (VNTR) genotypes for 244 healthy Han students (among them were 109 students with positive CHD family history).

RESULTSThe allele frequencies of apo e4, XbaI x(+), 3'VNTR-B(hypervariable element, HVE>38) in the positive group were obviously higher than those in the negative group(P<0.05), and were significantly correlated with the increase in TC, LDL-C, apoB100 levels (P<0.05).

CONCLUSIONThe alleles for apo e4, XbaI x(+), 3'VNTR-B may be the important genetic markers of Han CHD.

Adolescent ; Alleles ; Apolipoproteins B ; genetics ; Apolipoproteins E ; genetics ; Coronary Disease ; genetics ; Female ; Gene Frequency ; Humans ; Male ; Polymerase Chain Reaction ; Polymorphism, Genetic ; Young Adult