Synthesis and biological evaluation of 3-aromatic Shiff base-5-fluoroindol-2-one derivatives / 药学学报

Based on the structure of 5-fluoroindol-2-one and fragments from thirteen multi-target tyrosine kinase inhibitors which have been marketed or in the phase of clinical research, eleven 3-aromatic Shiff base-5-fluoroindol-2-one derivatives were designed and synthesized. Their structures were identified by 1H NMR, MS and elemental analysis. In vitro antitumor bioactivities evaluation was done by MTT method. It was shown that most of synthesized compounds had antitumor activities and compounds 1b, 1g, 1i and 1h were better than or equal to the antitumor activity of positive control.

Effect of earthworm decoction on airway inflammation of bronchial asthma in guinea pigs / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the effect of Earthworm decoction on the airway inflammation of experimental bronchial asthma in guinea pigs and inquire into the mechanism in the decoction.</p><p><b>METHOD</b>Forty-eight guinea pigs were randomly divided into six groups: the control group, the model group, the dexamethasone group, the Xiaoqinglong decoction group, the earthworm decoction large dosage group and the Earthworm decoction low dosage group, 8 guinea pigs in each group. Except the control group, the other groups were sensitized with ovalbumin (OVA) by a combination of intraperitional injection and repeated intranasal challenges to establish the guinea pigs asthma model. However, in the control group, normal saline was used. The morphological changes of bronchial tube, the lung tectology and the inflammation germ cell quantity of eosinophils (Eos), lymphocytes (Ly), neutrophils (Neu) and total blood cells in the blood and bronchoalveolar lavaga fluid (BALF) were examinated in each group respectively.</p><p><b>RESULT</b>The levels of Eos, Ly, Neu and total cell quantity in the blood and BALF after the earthworm decoction treatment in the large dosage group were significantly lower than those in the model group (P <0.01), and in the low dosage group were lower too (P <0.05). The Earthworm decoction large dosage could obviously improve the bronchial tube epidermis damage, the mucous membrane gland proliferation and hydrops, asthma pathology change and basilar membrane accumulation. Eos apoptosis was obsered in the bronchoalveolar, blood and BALF. The Earthworm decoction small dosage had a similar effect but slightly to the large dosage.</p><p><b>CONCLUSION</b>The Earthworm decoction can lighten the airway inflammation in asthmatic guinea pigs, its mechanism is related with the inhibition of Eos infiltration, acceleration of Eos apoptosis and improvement of the bronchial tube and the lung tectology changes. The effect of the decoction is dose-dependent.</p>

Expression of hepatocyte growth factor and its receptor in gastric cancer / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the role of expression of hepatocyte growth factor (HGF) and its receptor (c-Met) in gastric cancer.</p><p><b>METHODS</b>The expression of HGF and c-Met was detected with SABC immunohistochemistry in 44 specimens of gastric cancer, 20 chronic superficial gastritis, 10 chronic atrophic gastritis and 16 gastric ulcer tissues.</p><p><b>RESULTS</b>No positive expression of HGF/c-Met was found in the chronic superficial gastritis specimens. The positivity rates of HGF in the gastric cancer was 72.7% (32/44), significantly higher than that in chronic atrophic gastritis [20% (2/10), P<0.005] and gastric ulcer [37.5% (6/16). P<0.025]. The positivity rates of c-Met in gastric cancer [77.3% (34/44)] was also significantly higher than that in chronic atrophic gastritis [40% (4/10), P<0.05] and gastric ulcer [37.5% (6/16), P<0.025].</p><p><b>CONCLUSION</b>Co-expression of HGF and c-Met in gastric cancer may promote the progression of the malignancy, and also opens a new pathway for the therapy of gastric cancer.</p>