The objective of this paper is to discover new potent inhibitors against EphB4 for cancer therapy via computer-aided drug design strategies including building 3D-QSAR models,virtual screening and molecular doc-king means.The first step is to generate pharmacophore models based on Catalyst/HypoGen algorithm.The best model,Hypo1,has the highest Correl value (0.96),the lowest RMS value (0.89),the closest total cost (101.26) to fixed cost (89.20),and the best Δcost (89.14).Subsequently,Hypo1 was subjected to test set validation and Fischer′s randomization verification and then was used as a 3D query to screen database.In order to further nar-row the number of hits,drug-likeness screening and molecular docking techniques were applied.Finally,23 novel molecules with diverse scaffolds were selected as possible candidates against EphB4 for further studies based on predicted activity analysis,docking scores,and binding modes analysis methods.

Objective To evaluate the effect of intravitreal injection of triamcinolone for diffuse diabetic macular edema with optical coherence tomography (OCT). Methods 24 patients (25 eyes) with diffuse diabetic macular edema that failed to respond to previous treatment with of laser photocoagulation received an intravitreal injection of 4mg/0.1ml triamcinolone to each eye. The visual acuity, founds fluorescein angiography (FFA), and measurement of the macular retinal thickness with OCT were examined before and after the therapy. Mean follow-up time was 4.6 months (range 3-6 months ). Results Mean best-corrected visual acuity was improved from 0.12?0.07 to 0.30?0.16, the visual acuity improvement was statistically significant(P

OBJECTIVETo observe effects of treatment from the lung and treatment from the intestine on the level of vasoactive intestinal peptide (VIP) in the lung and intestine of ulcerative colitis (UC) rats.

METHODSThe UC rat model was established in 52 rats by using rabbit intestine mucosa tissue allergen combined TNBS-ethanol model (with the model successful rate of 78.0%). Eight rats randomly selected from 40 successfully modeled rats and 8 of 16 rats from the normal group were recruited as the model group and the normal control group before intervention (at week 0). The rest 32 successfully modeled rats were randomly divided into the model group, the Western medicine treatment group (salazosulfapyridine), the treatment from lung group (Huangqi Jiegeng Decoction), and the treatment from intestine group (Huangqi Huanglian Decoction), 8 in each group. Rats in each treatment group were administered with corresponding medication 8 times the dose of a 60 kg adult human. Another 8 normal rats were recruited as the normal group. Equal volume of pure water was given to rats in the model group and the normal group by gastrog avage, once per day. Contents of VIP in the lung tissue and the intestinal tissue were detected at week 0 and 4 after 4-week consecutive intervention. Pathomorphological changes of the lung tissue and the colon tissue were observed under light microscope.

RESULTSCompared with the normal control group at week 0, evenly distributed diffuse inflammation could be seen in the pulmonary interstitial tissue; the bronchial wall was thickened; a huge amount of infiltration surrounded bronchi and blood vessels; a large area of necrosis of intestinal mucosa and inflammatory cell infiltration could also be seen in the model group. Pathological injuries of the lung and the colon were more alleviated in each treatment group than in the model group at the same time point. Compared with the normal control group at the same time point, VIP contents in the lung tissue significantly decreased in the model group at the end of week 4 (P<0.05); VIP contents in the colon tissue significantly increased in the model group at the end of week 0 and 4 (P <0.05). Compared with the model group, VIP contents in the lung tissue significantly increased in the Western medicine treatment group and the treatment from lung group at the end of week 4 (P<0.01); VIP contents in the colon tissue significantly decreased in the treatment from lung group and the treatment from intestine group (P<0.05, P<0.01).

CONCLUSIONTreatment from the lung and treatment from the intestine showed predominant advantage in improving local inflammation of the lung and the intestinal tract, alleviating pathological injuries, promoting repair of injuries through regulating VIP contents in the lung tissue and the colon tissue.

Animals ; Colitis, Ulcerative ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Intestinal Mucosa ; metabolism ; Intestines ; Lung ; Male ; Rabbits ; Rats ; Vasoactive Intestinal Peptide

Objective To investigate the effect of Dexamethasone on microtubule - associated protein 1 light chain 3(LC3)expression of cells and neurons in cerebral cortex of juvenile Wistar rats with sepsis. Methods Models of juvenile Wistar rats with sepsis were established through cecal ligation and puncture(CLP). Totally 60 cases of 30 -day - old juvenile male Wistar rats were randomly divided into sham - operation group(10 cases),non - treated group (25 cases)and Dexamethasone group(25 cases). Twelve hours after CLP,rats in Dexamethasone group were injected with Dexamethasone(1 mg / kg)via tail vein every other day,with a total of 3 times. The same dose of saline was used in the non - treated group. All rats were killed at the age of 40 days. Expressions of LC3 and neuronal nuclei(NeuN)of cells in cerebral cortex of rats were detected by using immunofluorescence assay,and the number of positive cells was calculated by using image analysis system software. Expressions of LC3 - Ⅰ and LC3 - Ⅱ protein were measured by a-dopting Western blot. Results Three hours after CLP,rats appeared to be curled up and showed piloerection and shi-vering and the neurobehavioral score in non - treated group was significantly lower than that in sham - operation group (t = 9. 895,P = 0. 000). Twelve of 25 rats in Dexamethasone group died in 10 days after CLP(48% ),while 8 of 25 rats in non - treated group died(32% ),and the difference was not statistically significant between the 2 groups(χ2 =1. 333,P = 0. 248). The immunofluorescence staining and image analysis showed the percentage of LC3 positive cells in non - treated group was significantly increased(0. 606 7 ± 0. 030 1 vs 0. 353 3 ± 0. 025 8,t = 15. 644,P = 0. 000;0. 606 7 ± 0. 030 1 vs 0. 270 3 ± 0. 019 4,t = 22. 450,P = 0. 000). In non - treated group,the LC3 expression of cells in the cerebral cortex of rats was up - regulated,and the LC3 - Ⅱ/ LC3 - Ⅰ ratio was significantly higher than that in sham operation group and Dexamethasone group(0. 413 3 ± 0. 022 5 vs 0. 205 0 ± 0. 015 2,t = 18. 802,P = 0. 000;0. 413 3 ± 0. 022 5 vs 0. 185 0 ± 0. 023 5,t = 17. 206,P = 0. 000). The LC3 positive neurons in the cerebral cortex of rats were less in sham operation group and Dexamethasone group. The LC3 positive neurons were more in non - treated group than that in sham operation group and Dexamethasone group(0. 580 0 ± 0. 020 0 vs 0. 298 3 ± 0. 014 7,t =27. 783;P = 0. 000;0. 580 0 ± 0. 020 0 vs 0. 261 7 ± 0. 017 2,t = 28. 614;P = 0. 000). Conclusions The LC3 expres-sion of cells in the cerebral cortex of juvenile Wistar rats with sepsis was up - regulated,LC3 - Ⅱ/ LC3 - Ⅰ ratio in-creased,and the number of LC3 positive neurons also increased,while Dexamethasone could have inhibitory effect on them.

This paper primarily discusses such information of microwave-induced thermoacoustic tomography a new medical functional imaging method as its principle hardware structure reconstruction algorithm and imaging results in which research and advance of Wang LV's research team are introduced. The application perspective of microwave-induced thermoacoustic tomography is also included.

Objective To discuss the treatment after orthotopic heart transplantation and the experiences in deal- ing with ins complications.Methods To summarize the postoperative monitoring and management of 9 cases of patients af- ter heart transplantation.Results All 9 cases got out of hospital after recovery with better postoperative cardiac function and life quality.Among of them acute rejection appeared in 1 case earlier and 2 cases later after operation.1 case died later and 1 case had acute renal failure earlier after operation.Conclusion The effective monitoring for immunity and the scientific use of immunosuppressive agents after orthotopie heart transplantation,the active prevention and treannent of complications and its consanguineous follow-up are key factors for improving the survival rate.

Objective To study the meaning of breast cancer staging system by AJCC eighth edition to invasive lobular carcinoma and analysis the clinical pathological characteristics.Methods According to the eighth edition of the AJCC staging to evaluate the TNM stage and prognosis evaluation of invasive lobular carcinoma cancer patient in Peking University Shenzhen Hospital from 2011 to 2016,and compared with others in clinical pathological data.Results There were 21 cases of invasive lobular carcinoma,accounting for 2.7％ of all invasive breast cancer.We found that invasive lobular carcinoma shows no significant difference (P ＞ 0.05) in ages,menstrual status,molecular features and anatomic staging and prognosis staging with others;histological grade were significantly different (P ＜ 0.05).There were significant differences in the prognosis and staging of invasive lobular carcinoma.Conclusions Eighth AJCC staging systemn provides a new reference for the clinical treatment of breast cancer,should be evaluated with anatomic stage.Histological grade is relatively good in invasive lobular carcinoma and the prognosis is good,needs more research to the individualized treatment of invasive lobular carcinoma.

AIM:To observe and compare clinical effects of coaxial 1. 8mm microincision phacoemulsification and 3. 2mm small incision phacoemulsification.
●METHODS:A total of 117 eyes of 85 patients with age-related cataract in our hospital were divided randomly into two groups:43 patients (59 eyes) in the coaxial 1. 8 mm microincision cataract surgery group ( C - MlCS ) , 42 patients (58 eyes) in the coaxial 3. 2 mm traditional small incision cataract surgery group (C-SlCS). A total of 117 eyes were received phacoemulsification with intraocular lens implantation. Uncorrected visual acuity was recorded preoperatively and postoperatively at 1, 7, 30 and 90d. The effective phacoemulsification time and average ultrasound energy were recorded in surgery. Corneal endothelial cell and corneal topography were recorded preoperatively and postoperatively at 90 d.
●RESULTS:Uncorrected visual acuity ( logMAR) was no overall statistical significance difference between C-MlCS group and C-SlCS group (P>0. 05), but was significant statistical difference in different time-point within both groups(P<0. 05). Uncorrected visual acuity in different time-point had nothing to do with corneal wound size in cataract surgery(P>0. 05). On the 1 day after surgery, uncorrected visual acuity was 0. 16±0. 11 in C-MlCS group and 0. 22±0. 18 in C-SlCS group(P<0. 05). AVE was (7. 00± 2.72)% in C-MlCS group and (6. 16±3. 16)% in C-SlCS group (P>0. 05). EPT was (3. 09±1. 61)s in C-MlCS group and (3. 20±1. 92)s in C-SlCS group (P>0. 05). At 90 d after surgery, corneal endothelial cell loss percentage was (5. 81±2. 28)% in C-MlCS group and (5. 69±2. 38)% in C-SlCS group (P>0.05), SlA was (0.35±0.11) Din C-MlCS group and (0. 61±0. 13) D in C-SlCS group (P<0. 05).
● CONCLUSION: Compared with coaxial 3. 2mm traditional small incision cataract surgery, 1. 8mm coaxial microincision cataract surgery can get earlier visual rehabilitation and significantly reduce SlA. The coaxial 1. 8mm microincision cataract surgery is safe, effective and deserves further clinical applications.

BACKGROUND:Clinical y, bone marrow mesenchymal stem cel s combined with artificial bones for early osteonecrosis of the femoral head have a wonderful outcome.
OBJECTIVE:To review the biological properties of bone marrow mesenchymal stem cel s and to summarize the application progress of bone marrow mesenchymal stem cel s combined with different artificial bones in the treatment of early osteonecrosis of the femoral head.
METHODS:PubMed (2003-2013), FMJS (2003-2013), Wanfang (2005-2013), CNKI (2005-2013) and CBM (2005-2013) databases were retrieved by computer using the keywords of“bone marrow mesenchymal stem cel s;artificial bone;osteonecrosis of the femoral head”in Chinese and English.
RESULTS AND CONCLUSION:It wil lower the pressure of the femoral head, accelerate repair of the blood capil ary, improve the blood supply, osteoblast proliferation and differentiation, and thus delay or even prevent artificial joint replacement after osteonecrosis of the femoral head by applying bone marrow mesenchymal stem cel s combined with different artificial bones, such as corl ine hydroxyapatite, calcium hydroxylaptite, biological ceramics and calcium sulfate bones. But now, there are stil a lot of problems which need to be solved, including pathological mechanism underlying bone marrow mesenchymal stem cel s for treatment of osteonecrosis of the femoral head, obvious difference between the quantity and quality of seed cel s because of individual difference, different sites and culture techniques. So, artificial bone materials are under review, and large-sample randomized control trials are required. Its long-term outcomes also lack for fol ow-up observation, as wel as there is no a unified quantitative standard for the appropriate selection of indication, curative effect evaluation and the awareness of the operation.

Objective To evaluate effect of en bloc resection of malignant sacral tumor involving partial sacrum and ipsilateral sacroiliac joint with reservation of contralateral sacral foramina.Methods Between February 2005 and July 2010,16 patients with malignant sacral tumor involving partial sacrum and ipsilateral sacroiliac joint underwent hemi-sacrectomy and functional reconstruction.The operation achieved en bloc resection of tumor with reservation of contralateral sacral foramina.There were 10 males and 6 females,aged from 17 to 70 years (average,37.9 years).There were 5 cases of chondrosarcoma,3 cases of Ewing's sarcoma,2 cases of malignant schwannoma,2 cases of osteosarcoma,1 case of malignant giant cell tumor of bone,1 case of lymphoma and 2 cases of metastatic tumor.Results The surgical time ranged from 4 to 11.5 hours (average,6.5 hours).The average blood loss was 3600 ml (range,1500 to 5500 ml).Five patients underwent type Ⅰ resection,while 11 patients underwent type Ⅱ resection.All patients were followed up for 21 to 59 months (average,34.4 months).Three months after operation,13 patients had difficulty with ankle plantar flexion,while sphincter function was more or less reserved in 16 patients.Four patients (25％)had wound healing complications,which was cured after debridement and drainage.Local recurrence occurred in 7 patients.There were 5 cases of local recurrence among 6 patients who had intralesional margin;4 recurrence lesions located in the sacrum and 1 in soft tissue.Eight patients (50.0％) survived without tumor,2 patients (12.5％)survived with tumor,and 6 patients (37.5％) died of tumor.Conclusion The en bloc resection of tumor involving partial sacrum and ipsilateral sacroiliac joint with reservation of contralateral sacral foramina was feasible and had better outcome compared with total sacrectomy.