OBJECTIVE: To synthesize desmosdumotin C derivatives on B-ring with antitumor activity. METHODS: The target compounds were synthesized from 2, 4, 6-trihydroxyacetophenone via methylation, O-methylation and aldol reaction. Their antiproliferative activities were tested against six human tumor cell lines. RESULTS: Fourteen target compounds were synthesized, nine of which were new compounds. All of them were characterized using 1H-NMR, 13C-NMR and MS. CONCLUSION: Preliminary pharmacological test showed that all the title compounds except 1i exhibited potent antitumor activities. 1h and 1n were better than desmosdumotin C in vitro. Introducing two fluoro atom on B-ring would benefit its activity against some tumor cells.

No abstract available.
Angiotensin II* ; Angiotensins* ; Hydrocortisone* ; Insulin*

OBJECTIVETo investigate the effects and regulatory mechanism of ILK on angiogenesis in hypertrophic scar.

METHODSThe human scar microvascular endothelial cells (HSMECs) were isolated from 6 patients' hypertrophic scar in vitro. The HSMECs with good condition in 2nd to 4th generation were selected as experimental objectives. (1) HSMECs were divided into the blank control group (treated with routine culture), negative control group (treated with only Lipofectamine 2000), LY294002 group (incubated with 50 nmol/L LY294002), ILK siRNA group (incubated with 20 nmol/L ILK siRNA). RT-PCR and Western Blot were used to detect the expression of ILK mRNA and its protein after transfecion for 48 h. (2) The digested HSMECs of four groups were resuspended with DMEM without serum and then seeded onto the upper compartment of transwell insert which contained complete medium in its lower compartment. The cell migration experiment was stopped in 10 h and then the migrated cells were counted to analyze the effects of different interventions on the migration ability of HSMECs. (3) The thawed ECMatrix was put into each well of pre-colled 48-well tissue culture plate, and then the plate was put into the incubator at 37 degrees C to make it to become gel. The HSMECs of four groups were seeded onto the surface of the ECMatrix gel and were put into incubator. Eight random view-fields per well should be valued by the sheet of pattern recognition about angiogenesis after 8 hours to evaluate the ability of angiogenesis in vitro between four groups.

RESULTS(1) The expression of ILK mRNA (ILK mRNA = 0.829 +/- 0.109, t = 13.151, P = 0.006) and protein (ILK protein = 0.096 +/- 0.049, t = 36.656, P = 0.000) were both inhibited obviously in ILK siRNA group compared with the blank control group (ILK mRNA = 0.829 +/- 0.109, ILK protein = 1). And, the expression of ILK in LY294002 group was slightly lower than that of black control group, but there was no statistical difference. (2) The number of migrated cells in ILK siRNA group (88.111 +/- 3.079) and LY294002 group (138. 667 +/- 2.404) were respectively lower than that in blank control group (322.333 +/- 3.712, P < 0. 05) in 10th hour. (3) Compared to blank control group (4.333 +/- 0.191), the ability of angiogenesis in vitro decreased significantly ILK siRNA group (2.625 +/- 0.125) and LY294002 group (3.125 +/- 0.250), in which, the vascular network structures were not formed perfectly in 8th hour (P < 0.05).

CONCLUSIONSThe ability of HSMECs' migration and angiogenesis in vitro are inhibited significantly when the expression of ILK is down-regulated. It reveals that ILK may play an role in the regulation of scar angiogenesis.

Cell Movement ; Cell Proliferation ; Chromones ; pharmacology ; Cicatrix, Hypertrophic ; enzymology ; pathology ; Endothelial Cells ; cytology ; drug effects ; Humans ; Lipids ; pharmacology ; Morpholines ; pharmacology ; Neovascularization, Pathologic ; etiology ; pathology ; Protein-Serine-Threonine Kinases ; genetics ; physiology ; RNA, Messenger ; analysis ; RNA, Small Interfering ; metabolism

With the diversion rate of ginkgolide A, B, K as comprehensive evaluation indexes, the amount of activated carbon, ad- sorption time, mix rate, and adsorption temperature were selected as factors, orthogonal design which based on the evaluation method of information entropy was used to optimize activated carbon adsorption technology of ginkgo diterpene lactones meglumine injection. Opti- mized adsorption conditions were as follows: adsorbed 30 min with 0.2% activated carbon in 25 °C, 40 r ·min⁻¹, validation test re- sult display. The optimum extraction condition was stable and feasible, it will provide a basis for ginkgo diterpene lactone meglumine injection' activated carbon adsorption process.
Adsorption ; Charcoal ; chemistry ; Chemistry, Pharmaceutical ; instrumentation ; methods ; Diterpenes ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Ginkgo biloba ; chemistry ; Lactones ; chemistry ; isolation & purification

OBJECTIVETo establish an enzyme-linked immunosorbent assay (ELISA) for determining anti-themocyte globulin (ATG) levels in serum samples.

METHODSThe microplate was coated with mouse anti-rabbit IgG monoclonal antibody, and sheep anti-rabbit polyclonal antibody conjugated with HRP was used as the second antibody for detecting the serum ATG levels in patients undergoing allogeneic hematopoietic stem cell transplantation.

RESULTSThe optimal concentration of the coating antibody and dilution ratios of the serum samples and IgG-HRP conjugate were 0.2 microg/ml, 1:40 and 1:2500, respectively. The lower sensitivity limit of the assay was 31.25 ng/ml for ATG detection. A linear relationship was established within the concentration range from 40 to 1000 ng/ml, with the coefficients of variation of 7.91 within assay and 5.22 between assays, respectively. Seven patients undergoing stem cell transplantation with ATG pretreatment showed gradually decreased concentration of ATG, and after 90 days ATG could still be detected.

CONCLUSIONThe sandwich ELISA we established provides a specific and sensitive method for quantitative measurement of ATG in the clinical setting. In patients undergoing stem cell transplantation with ATG pretreatment, the ATG concentration gradually decreases but remains detectable 90 days after the administration.

Adolescent ; Adult ; Antilymphocyte Serum ; blood ; therapeutic use ; Child ; Enzyme-Linked Immunosorbent Assay ; methods ; Female ; Humans ; Leukemia ; blood ; therapy ; Male ; Sensitivity and Specificity ; Stem Cell Transplantation ; Young Adult

Objective To explore the effect of group mind-games and group counseling on training burnout among soldiers who quickly marched to the plateau for the first time .Methods Totally 399 soldiers who quickly marched to the plateau for the first time were divided randomly into to the control group ( n=201 ) and test group ( n=198 ) .The test group had particinated in group mind-games and psychological counseling twice a week for a total of 5 weeks, while the control group received no counseling .Soldier training fatigue questionnairs were used to compare the difference between the two groups before and after group mind-games and psychological counseling .Results ①The total scores of training burnout and the scores of all the factors of soldiers before counseling in the two groups was of no statistical significance (P>0.05). After counseling , the total scores of training burnout and the scores of all factors in test group were remarkably lower than those in control group,and the difference was of statistical significance (P<0.05).The total scores of training burnout and the scores of physical and psychologica exhaustion and alienaties decreased significantly after training in test group ( P<0.05), but the change was of no statistical significance in control group (P>0.05).②Soldiers who had served 1 to 2 years or over 9 years had significant difference in the scores of training burnout , physical and psychologica exhaustion ( P<0.05).Soldiers who had served 3 to 8 years had significant difference in the scores of training and the scores of each factor after counseling(P<0.05).Conclusion Group mind-games and psychological counseling can effectively help alleviate the training burnout of soldiers who quickly march to the plateau for the first time.

Objective To explore the changes in neuroglobin(NGB)expression in rat cerebral cortex induced by acute and chronic hypoxia at high altitude.Methods Seventy SD rats were randomly divided into normal control and experimental groups,and in the latter group,the rats kept in a high-altitude research base in Kekexili(4600 m),while the control rats were kept in a facility at the altitude of 2295 m.The rats in the experimental group were divided into 6 groups with the exposure time of 12,24,48,72 h,1 week and 1 month.An oximeter was used to measure the SaO2 level.Semi-quantitative PCR and Western blotting were performed to detect the expression levels of NGB mRNA and protein in the cortical neurons of the rats after the exposure.Results After explosure of the rats to hypoxia at high altitude for 12h,the SaO2 was lowered to(70.70±2.83)%and increased gradually as exposure time prolonged,but remained lower than that in the control group throughout the exposure.RT-PCR showed a rapid increase of NGB mRNA expression after 24-h exposure to hypoxia,followed by gradual decrease till recovery of the normal level at 1 week;the expression slowly increased after 1 week and maintained a high level till 1 months.showing significant difference from that in the control group(P＜0.05).Western blotting showed an identical pattem of NGG protein expression alterations during the experiment.Conclusion NGB expressions in the cerebral cortex increase significantly after acute and chronic hypoxia at an altitude of 4600 m to enhance the tolerance to hypobaric hypoxia,suggesting the possible role of NGB as an important endogenous mechanism for protecting the neural tissues against hypoxic injuries.

Objective To evaluate the effect of comprehensive prevention programs on HIV,HBV and syphilis transmission from mother to child and between premarital couples. Methods HIV, HBV and syphilis were screened among pregnant women with interventional measure for infected women; HIV, HBV and syphilis (TP) were screened among premarital couples with medical advice. Results The HIV,HBsAg and TP positive rates were 8.4‰(111/13 280) ,54‰(711/13 186)and 12.8‰( 159/12 401 ) respectively among pregnant women and the total positive rate of the three diseases was 73.8‰ which was significantly higher than HIV positive rate (P＜0.001). The positive rates of HIV, HBsAg and TP were 17.6‰(464/26 324), 95.3‰( 1826/19 152) and 18.6‰(355/19 099) respectively among premarital couples and the total positive rate of the three diseases was 131.5‰ which was significantly higher than HIV positive rate alone (P＜0.001).Comprehensive prevention was more economical than prevention for HIV alone. Conclusion The comprehensive strategies for prevention of HIV, HBV and syphilis was feasible, effective and economical that could help to actively conduct the preventive measures.

Neuroglobin (Ngb) is a respiratory protein that is preferentially expressed in brain of mouse and man. In this article, Tibetan antelope, living at altitude of 3 000-5 000 m for millions of years, was selected as the model of hypoxia-tolerant adaptation species. Using reverse transcription polymerase chain reaction (RT-PCR) and Western blot techniques, expression of Ngb gene was amplified and analyzed in antelope brain tissue. Our results showed that Ngb homology protein in Tibetan antelope was identified with more sequence similarity with cattle (96%), sheep (95%), and human (95%). We detected that there were some mutations occurred in the Open Reading Frame of Ngb in Tibetan antelope compared with sheep. Phylogenetic analysis of Ngb chain showed that it was closer to cattle than the others. This study suggests possible roles of central nervous system enriched Ngb in adaptation of Tibetan antelope to extremely high altitude.
Acclimatization ; genetics ; Altitude ; Animals ; Antelopes ; genetics ; Cattle ; Globins ; genetics ; Humans ; Hypoxia ; genetics ; Mice ; Nerve Tissue Proteins ; genetics ; Phylogeny ; Sheep

Energy metabolism plays an important role in life survival for species living in high altitude hypoxia condition. Air-breathing organisms require oxygen to create energy. Tibetans are the well-adapted highlanders in Qinghai-Tibetan Plateau. It was thought that different metabolic approaches could lead to different adaptation traits to high altitude hypoxia. Recently identified hypoxia inducible factors pathway regulators, endothelial PAS domain protein1 (EPAS1)/HIF-2a and PPARA, were involved in decreasing hemoglobin concentrations in Tibetans. Because EPAS1 and PPARA also modulated the energy metabolism during hypoxia, we hypothesized that positive selected EPAS1 and PPARA genes were also involved in unique energy metabolisms in Tibetans. In this brief review, we take a look into genetic determinations to energy metabolisms for hypoxia adaptations traits in Tibetans and mal-adaptive conditions such as high altitude diseases.
Acclimatization ; genetics ; Altitude ; Basic Helix-Loop-Helix Transcription Factors ; metabolism ; Energy Metabolism ; Hemoglobins ; analysis ; Humans ; Hypoxia ; metabolism ; Oxygen ; metabolism ; Phenotype ; Tibet