Synthesis of new 4-anilinoquinazoline analogues and evaluation of their EGFR inhibitor activity / 药学学报

Thirteen of 4-anilinoquinazoline derivatives with imine groups at position 6 of quinazoline ring were synthesized and their antitumor activities were evaluated by MTT assay and Western blotting analysis. Among these compounds, 13a-131 were reported first time. The MTT assay was carried out on three human cancer cell lines (A549, HepG2 and SMMC7721) with EGFR highly expressed. Among the tested compounds, 13i and 13j exhibited notable inhibition potency and their IC50 values on three cell lines were equivalent to or less than those of gefitinib. Compound 14, without imine group substituted, displayed excellent inhibitor potency only on A549 cell line. Compounds 14 and 13j were chosen to perform Western blotting analysis on A549. The results showed that both of the compounds could inhibit the expression level of phosphorylated EGFR remarkably. It was concluded that the inhibitor potency of compound 14 was almost equivalent to that of gefitinib and the inhibitor potency of 13j was better than that of gefitinib.

Investigation of the changes of plasma interleukin-6, interleukin-8, tumor necrosis factor-alpha in acute blood loss patients / 中国医师进修杂志

Objective To investigate the changes and significance of plasma interleukin (IL)-6,IL-8,tumor necrosis factor-alpha (TNF-α) and nitric oxide synthase (NOS) in acute blood loss patients.Methods The levels of plasma IL-6,IL-8,TNF-α and NOS were determined in 25 patients with acute blood loss(blood loss group) and 25 healthy controls(control group) by enzyme linked immunosorbent assay.Result The levels of plasma IL-6,IL-8,TNF-α and NOS in blood loss group were higher than those in control group (0.284 ± 0.027 vs.0.204 ± 0.016,0.059 ± 0.079 vs.0.037 ± 0.039,0.460 ± 0.024 vs.0.372 ±0.018,0.637 ±0.054 vs.0.443 ±0.040,P＜0.05 or ＜0.01).Conclusions First,the expressions of IL-6,IL-8,TNF-α and NOS are strongly induced at the circumstances of acute early stage blood loss which can cause inflammatory reaction,aggravate the damage of soft tissues and organs,and easy to lead the blood loss to uncontrolled hemorrhagic shock.Second,the expression of NOS is strongly induced at the circumstances of acute blood loss which should reduce the damage of soft tissue,and alleviate the hemorrhagic shock.Therefore,the levels of plasma IL-6,IL-8,TNF-α and NOS can estimate the illness prognosis and curative effect,which have important clinical instruction value for effective treatment of hemorrhagic shock.

Analysis of onset age and cutaneous lesions in 54 patients with tuberous sclerosis / 中华皮肤科杂志

Objective To analyze the features of cutaneous lesions and age of onset of tuberous sclerosis(TS).Methods A total of 54 TS patients were recruited;their clinical data were analysed.Results The occurance of facial angiofibromas,periungual fibromas,hypomelanotic macules and shark macules was 72.5%,26%,70%and 48%,respectively,and the median age of onset of these lesions was 7,14,0.2 and 6 years,respectively,with a peak at 1-9,10-19,＜1 and 1-9 years,respectively.Conclusions Cutaneous lesions are commonly seen in TS,and most of them develop early in life.

Effects of photodynamic therapy on human lung adenocarcinoma cell line A549 / 中国肺癌杂志

<p><b>BACKGROUND</b>To observe the effects of photodynamic therapy (PDT) on human lung adenocarcinoma cell line A549 in vitro.</p><p><b>METHODS</b>Human lung adenocarcinoma cell line A549 was used to investigate the killing role of PDT with hematoporphyrin derivative (HPD) as photosensitizer and semiconductor successive laser as light source. The cultured cell was treated with different concentrations of HPD and different do-sages of laser, then MTT colorometric assay was applied to measure the OD492.</p><p><b>RESULTS</b>5 mg/L of HPD was confirmed no effect. 10 mg/L of HPD could produce a marked therapeutical effect under the condition of same laser dosage. When the concentration of HPD was increased, the effect was not risen obviously. 10 J/cm² of laser could lead OD492 to decrease to platform under the condition of same HPD concentration. So the killing effect was saturated when the PDT parameters were selected as 10 mg/L of HPD and 10 J/cm² of laser. Under the same laser capacity density of 10 J/cm², A549 cells were exposured to three different duty-time fabrications which were 214 mw×10 min, 428 mw×5 min and 714 mw×3 min.The outcomes showed that OD492 had no statistical difference.</p><p><b>CONCLUSIONS</b>PDT has a significant killing effect on human lung adenocarcinoma cell line A549. 10 mg/L of HPD and 10 J/cm² of laser were the best parameters of this experiment. The PDT effect is not influenced by different duty-time fabrications under the best laser capacity density.</p>

Photodynamic therapy inducing apoptosis of human lung adenocarcinoma cell line A549 / 第二军医大学学报

Objective:To observe the effect of photodynamic therapy(PDT)on apoptosis of human lung adenocarcinoma cell line A549.Methods:Human lung adenocarcinoma cell line A549was used and the optimal parameters of PDT were se-lected by MTT colorometric assay.The experiment was divided into2groups:control group and PDT group.Twenty-four hours after PDT(HPD concentration10mg/L,laser dosage10J/cm 2 ),cell cycle and apoptosis rate were estimated by flow cytometry;agarose gel electrophoresis and TUNEL were used to observe the DNA fragments and apoptosis index(AI).Re-sults:The killing effect was saturated when HPD was10mg/L and laser was10J/cm 2 .Under the same laser(10J/cm 2 ),A549cells were exposed to6different duty time fabrications and the outcomes showed that their D 492 had no statistical differ-ence.Agarose gel electrophoresis of DNA showed DNA ladder,a biochemical hallmark of apoptosis in the PDT group.Flow cytometry showed that PDT group had G 0 /G 1 stage arrest.The apoptosis rate was(18.443?7.122)%in PDT group vs (0.301?0.361)% in control group(P

The variation of blood vessel factors on pulmonary hyperation induced by monocrotaline / 中国药理学通报

AIM To explain the variation of blood vessel factors on pulmonary hypertension(PH) induced by monocrotaline(MCT). METHODS Rats were given an injection of MCT ih(60 mg?kg -1 ). The concentration of endothe line(ET), nitric oxide(NO), thromboxane B 2(TXB 2) and 6 keto prostaglandin F 1? (6 keto PGF 1? ) were measured by radioimmunoassay and colorimetric analysis after the model had been set up successfully for 4 wk. RESULTS MCT either raised 6 keto PGF 1? and NO or prevented the progression of ET and TXB 2. CONCLUSION The mechanism of PH induced by MCT probably associated with the variation of those blood vessel factors.