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.

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

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

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

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

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 evaluate the validity, reliability, and clinical applicability of Chinese medicine syndrome diagnostic standards for coronary heart disease (CHD) patients after percutaneous coronary intervention (PCI), which was established by expert consultation.

METHODSA total of 1 050 CHD patients after PCI were recruited from 23 hospitals. The sensitivity, specificity, accuracy, positive likelihood ratio, and area under ROC curve were used to evaluate the validity of diagnostic standards for Chinese medical syndrome types. The observable agreement rate and Kappa value were used to evaluate the reliability. Positive predictive value and negative predictive value were used to evaluate the clinical applicability.

RESULTSThe sensitivity, specificity, accuracy, positive likelihood ratio, area under ROC curve, observable agreement rate, Kappa value, positive predictive value, and negative predictive value of each Chinese medicine syndrome in CHD patients after PCI were as follows: 95.26%, 93.70%, 94.86%, 15.13, 0.924, 98.76%, 0.969, 97.76%, and 87.24% for blood stasis syndrome; 96.42%, 95.34%, 96.00%, 20.70, 0.957, 99.52%, 0.990, 97.02%, and 94.42% for qi deficiency syndrome; 88.19%, 96.46%, 94.19%, 24.89, 0.923, 96.67%, 0.915, 90.39%, and 95.58% for phlegm turbidity syndrome; 91.06%, 98.77%, 97.05%, 74.22, 0.950, 98.67%, 0.960, 95.54%, and 97.46% for cardiac blood stasis syndrome; 98.41%, 96.73%, 97.33%, 30.10, 0.976, 98.86%, 0.976, 94.40%, and 99.09% for qi deficiency blood stasis syndrome; 94.81%, 94.75%, 94.76%, 18.07, 0.948, 97.71%, 0.918, 72.73%, and 99.20% for phlegm-stasis stagnation syndrome.

CONCLUSIONThe validity, reliability, and clinical applicability of Chinese medicine syndrome diagnostic standards for CHD patients after PCI were rational and considerable in clinical practice.

Coronary Disease ; diagnosis ; etiology ; Humans ; Medicine, Chinese Traditional ; methods ; Percutaneous Coronary Intervention ; adverse effects ; Predictive Value of Tests ; Sensitivity and Specificity

In recent years a huge amount of clinical studies have proved that fluctuant hypertension could aggravate the damage of target organs and increase the incidence of acute cardio-/cerebrovascular events, when compared with stable hypertension [increased mean artery blood pressure (MBP)]. How to prevent and treat fluctuant hypertension and its damage of target organs has become one of the hot and difficult problems in the field of hypertension studies all over the world. Hypertensive patients often suffer from thromboembolic target organ damage. Platelet activation plays a key role in this progress, but its concrete mechanisms have not been clearly clarified. Based on the in-depth discussions on progress of fluctuant hypertension, its relationship with platelet activation and blood stasis syndrome of Chinese medicine (CM) in recent three years, we proposed, under the fluctuant hypertensive state, the prethrombotic state has occurred in the organisms, i.e., a pathological state featured by platelet activation, liable to have vulnerable thrombopoiesis, and accompanied by endothelial dysfunction. Blood stasis syndrome might occupy an important position in CM syndrome typing of fluctuant hypertension. Herbs for activating blood circulation and removing stasis might have an extensive application prospect.
Humans ; Hypertension ; blood ; prevention & control ; Integrative Medicine ; Platelet Activation