In view of the facts that moderately electron withdrowing carrier might cause the triazenes increase antitnmour activity and decrease toxicity, sixteen 8-triaze-nopurines were prepared. 7-H-8-triazenopurines were synthesised by coupling the corresponding 8-diazopurines directly with appropriate secondary amines under carefully controlled conditions, while 7-alkyl-8-triazenotheophyllines were obtained by coupling 8-diazotheophylline with secondary amines to 8-triazenotheophyllmes and subsequent alkylation under suitable conditions.All sixteen compounds have been snbjected to experimental antitumour tests. Preliminary results revealed that compounds 2a, 3a, 4a and 5 possessed marked inhibitory action against L615 in mice and caused ILS of 300-400%, among them compound 4a was was shown to possess the highest activity but less toxicity. The further study is in progress.

The correlation of premature stimulation and local ventricular contraction state was studied by ultrasonic dimension gauge in the conscious dogs. When the anterior wall of LV was stimulated, the total percent thickening (TPT) the anterior wall reduced from the control value 19.6?3.2% to 6.7?6.6% (P

The relationship between the sex hormone in plasma and left ventricular performance was studied with myocardial infarction(MI) in rats. It was found that in orchidectomized rats testosterone(T) in plasma decreased significantly (P

The estradiol (E_2) and testrosterone (T) levels in the Plasma of normal male and female rats and their E_2/T ratio were measured by radioimmunoassay. We have found that in the male rats the plasma testosterone level was 270.0?46.2 ng/100ml,the estradiol level was 62.I ?2.8 pg/ml and the E_2/T ratio wa(?) 0.040?0.008; in the female rats, although the estradiol and testosterone levels of the plasma and the E_2/T ratio changed with their estrous cycle, but the mean values of estradiol,testosterone and the E_2/T ratio were 55.4?3.7 pg/ml,51.8?3.1 ng/100 ml and 0.124?0.014 respectively. We suppose that these values may serve as normal values in the basic state and may be used for reference in experimental studies.

The principle method and application of the ultrasonic technique are briefly recommended. As compared with acute experiment, this technique has the following merits: the determination is not affected by anesthesia and damage, the animal is in physiologic state, the sensitivity of apparatus is heigher, the result is more accurate, the changes in the contractory state of the ventricular wall and the parameters of cardiac function can be recorded synchronously, and the correlation analysis can be made more accurately. This method is suitable for chronic cardiovascular function experiments of physiology, Pharmacology and pathophysiology.

To observe the effect of fructote-1, 6-diphosphate (FDP) on left ventricular function after large infarcted size of myocardial infarction in male Wistar rats, rats were divided into four groups at rondom: (1) myocardial infarction (MI) by ligation of left coronary artery, (2) MI treated by FDP (FDPI), (3) sham--operated control (CS) and (4) normal control (C). The cardiac function was measured on the 3rd day after infareting.The results were: (1) The infaret size in FDPI seemed to be lesser than that in MI group. (2) There were no obvious differences in the values of heart rate, stroke volume and stroke volume index between MI and FDPI groups,cardiac output(CO)and cardiac index (CI) in FDPI group were significantly larger than those in MI group (CO: 40.6?8.3 ml/min vs 30.6?10.2ml/min; CI: 164?30.5ml/min/kg vs 127.2?36. 8ml/min/kg, all p

The immune-gold-silver stain and image analysis methods were used to check up estrodial receptor (ER) in rat heart at myocardial infarction (MI) conditions.Animals were divided randomly into four groups: one serves as normal control, another as sham-operation, the third was treated as myocardial infarction and the last one estrogen (E_2) was injected after MI. The results showed that all the parts of the heart have ER,but the distributions are not equal in atrium and ventricle, the former is less than that of the latter (0.1687?0.005, 0.2072?0.006, P

To determine the effects of testosterone (T) on hypertrophy and cardiac function of rats with myocardial infarction (MI), the rats were divided into 3 groups: ie, the sham-operated group (S group), the coronary artery ligating groups with or without the injection of T (MIT and MI group). T level of plasma was tested on all rats, by RIA on1/4, 1, 3, 9, 20 day after operation; then the nuclear profiles per unit area of myocardium N_((n)A) the average nuclear length D_((n)) and the volume fraction of number of myoeytes in the myoeardium V_((m)v) were measured under microscope; The number of myocyte nuclei per unit ovolume of myocardium N_((n)v) and average myocyte cell volume per nucleus V_((m)n) were calculated. The results were as follows: (1) Comparing with S group N_((n)A), N_((n)v) and V_((m)n) in MI had marked changes (P0.05). Of all the mentioned changes were more marked in MIT group than that in MI group. (2) The total plasma concentration of T was correlated with V_((m)n) (r=0.60, P0.05) were not found in MIT rats. These results indicated that T may improve myocardial hypertrophy and promote the recovery of eardial function of MI.

The effect of hyperestrogenemia induced by intramuscular injectied estradiol (E_2) on myocardial contractility and relaxation was observed in female rats with myocardial infarction (MI). The results showed that: (1) In MI group, the plasma estradiol level increased slyghtly and then droped, while the level of estradiol increased markedly in rats treated by E_2 in MI (MIE_2) group. (2) Diameter of myofibril in MIE_2 grows more than that of control sham operation(CS) and MI (10.65?0.59 VS 7.65?0.40 and 10.15?0.54?m, P

In recent years, the incidence and mortality rate of invasive fungal infection have increased dramatically, and it is of great significance to develop novel antifungal agents with new chemical structure and new mode of action. In this review, novel antifungal lead compounds reported from 2007 to 2009 are reviewed. Moreover, their chemical structures, antifungal activities and structure-activity relationships have been summarized, which can provide useful information for future study of antifungal agents.