Diversity-oriented synthesis (DOS) aims to efficiently generate collections of small molecules with diverse appendages, functional groups, stereochemistry and skeletons, thus yielding diverse biological activities capable of modulating a wide variety of biological processes. In this review, we discussed the common strategies employed in DOS with specific examples from recent literature, including reagent-based approach, substrate-based approach, build-couple-pair strategy and privileged substructure-based DOS. The application of some DOS libraries in drug discovery is also presented.
Drug Design ; Drug Discovery ; Small Molecule Libraries

Adult ; Aged ; Airway Obstruction ; therapy ; Cricoid Cartilage ; surgery ; Female ; Humans ; Laryngeal Diseases ; therapy ; Male ; Middle Aged ; Punctures ; methods ; Thyroid Cartilage ; surgery

Adenocarcinoma ; genetics ; metabolism ; Angiomyolipoma ; etiology ; Antibiotics, Antineoplastic ; therapeutic use ; Astrocytoma ; etiology ; Brain Neoplasms ; etiology ; Breast Neoplasms ; genetics ; metabolism ; Gene Expression Regulation, Neoplastic ; Genes, Tumor Suppressor ; Humans ; Kidney Neoplasms ; etiology ; Lung Neoplasms ; genetics ; metabolism ; Mutation ; Sirolimus ; therapeutic use ; TOR Serine-Threonine Kinases ; antagonists & inhibitors ; metabolism ; Tuberous Sclerosis ; complications ; drug therapy ; genetics ; metabolism ; Tumor Suppressor Proteins ; genetics ; metabolism

10.3969/j.issn.1007-3969.2013.05.004

BACKGROUND:The growth of mesenchymal stem cells in vitro in different conditioned media is different evidently. So it is necessary to choose a more suitable medium. OBJECTIVE:To contrast and observe the proliferation of human umbilical cord mesenchymal stem cells in three kinds of media and to check the immunophenotype and differentiation ability of mesenchymal stem cells. METHODS:Human umbilical cord mesenchymal stem cells were col ected by explant method in sterile conditions. After subculturing by T75 incubation bottles, the third generation of mesenchymal stem cells were cultured in Dulbecco’s modified Eagle’s medium/Ham’s nutrient mixture F-12 medium containing 5%fetal bovine serum, Dulbecco’s modified Eagle’s medium/Ham’s nutrient mixture F-12 containing 10%fetal bovine serum and Mesen PRO RSTM medium. After 1, 3, 5, 7 days of culture, the cells were counted to draw a growth curve. Immunophenotype of the third generation of umbilical cord mesenchymal stem cells were determined by flow cytometry and the ability of osteogenic and adipogenic differentiation was also detected. RESULTS AND CONCLUSION:The third generation of cells cultured highly expressed CD44, CD73, CD90, CD105, but did not express CD29, CD31, CD34, HLA-DR. The oil red O staining showed a lot of little red lipid drops after adipogenic induction;alizarin red staining showed osteoblast-like cells after osteogenic induction, indicating umbilical cord mesenchymal stem cells in vitro have the potential of multi-directional differentiation. After observation and counting, the colony and shape of cells cultured in Dulbecco’s modified Eagle’s medium/Ham’s nutrient mixture F-12 containing 10%fetal bovine serum were superior to those cultured in the other two media. Therefore, it is concluded that Dulbecco’s modified Eagle’s medium/Ham’s nutrient mixture F-12 containing 10%fetal bovine serum is preferred for cellsubculture.

Purpose To explore the CT features of renal cell carcinoma with cystic change and to compare them with pathological ifndings, so as to improve its diagnostic accuracy. Materials and Methods A retrospective study was carried out in 44 cases of renal cell carcinoma with cystic change conifrmed surgically and pathologically, among which 10 were multilocular cystic renal cell carcinoma, 21 were renal clear cell carcinoma and 13 were papillary renal cell carcinoma. The CT features of these 3 kinds of diseases were analyzed comparatively. Results All of 10 cases of multilocular cystic renal cell carcinoma appeared to have multilocular cysts with thin cystic walls and septa. The mean CT value of cyst was (15.8±5.6) HU. The diameter of wall nodule was larger than 5 mm in 4 cases. The contrast-enhanced CT scan showed that the cystic walls and septa had early moderate enhancement in 8 cases. Among 21 cases of renal clear cell carcinoma, 9 presented to have multilocular cysts with thick cystic walls and septa. The mean CT value of cyst was (32.5±6.7) HU. The diameter of wall nodule was larger than 5 mm in 19 cases. The cystic walls and septa had obvious early enhancement in 20 cases. As to the 13 cases of papillary renal cell carcinoma, 4 appeared to have multilocular cysts with thick cystic walls and septa. The mean CT value of cyst was (26.1±5.6) HU. The diameter of wall nodule was larger than 5mm in 12 cases, and 12 cases appeared to have slight to moderate delayed enhancement. Conclusion The CT features of renal cell carcinoma with cystic change could be used in differential diagnosis, such as with or without pseudocapsule, mean CT value of cyst, thickness of cystic wall and septum, size, boundary, and enhancement of nodule.

The clinical comprehensive ability is the core of the cultivation of professional degree graduate tralning. It includes the ability of clinical analysis, the ability of clinical operation and the ability of clinical communication, which is compatible with the core of the evaluation of post compe-tency in knowledge, technology and attitude. Teaching Section of Internal Medicine of the First Clinical College of Harbin Medical University combined the professional Degree Graduate tralning with the resident tralning with the post competency as the direction. We adopted a series of effective methods such as strict management of clinical rotation and multiple dimensioned evaluation system. We organized clinical discussion and set up clinical skill tralning course and standardize teaching ward inspection et al. to improve the comprehensive clinical ability of the postgraduates. The formative evaluation and summative assessment were combined in department rotation examination and the feedback system was set up. By the above tralning, the comprehensive clinical ability of the postgraduates has improved effectively, which can match the level of the first phrase resident physician. Combined with the tralning of other department, the postgraduates can be qualified for the general physician.

OBJECTIVE:To investigate the risk,advantages and disadvantages and countermeasures of new drugs,generic drugs and imported drugs in different transfer opportunities,and to provide basis for improvement of development strategy for phar-maceutical enterprises. METHODS:The analysis was done in accordance with relevant regulations on transferable projects in the process of applying for registrations of new drugs,generic drugs and imported drugs. The transfer period and risk were explored and countermeasures were put forward. RESULTS & CONCLUSIONS:Transferable projects included intellectual property rights (patents,patent application,technical secrets,application information,non-disclosed data,etc.)and ownership rights(clinical tri-al approvals,new drug certificates,drug approval number,pharmaceutical product registration certificates,imported product regis-tration certificates,etc.)in the process of applying for registrations. There are 4 opportunities for drug technology transfer,opportu-nity 1 is before applying clinical trial approvals after the completion of non-clinical research such as pharmacology,toxicology;op-portunity 2 is ahead of clinical trial after the acquirement of clinical trial approvals;opportunity 3 is new drug technology transfer;opportunity 4 is production technology transfer. The new drugs have 4 transfer opportunities,generic drugs and imported drugs can transfer in opportunity 1,2,4. Different transfer opportunities present different risks and profits. The risk gradually decreases with the further promotion of drug registration process,while the innovation decreases at the same time. Pharmaceutical enterprises should combine with the policy,market and their own features to select a suitable transfer period.

Object To investigate the features of health related quality of life ( HRQOL) among elderly hypertensive patients with different body mass index (BMI) so s to provide evidence for the health promotion of hypertensive. Methods A cross-sectional survey of health status data from a population of 1281 elderly hypertensive patients from Beijing and 8 provinces of China ( Jiangsu, Anhui, Gansu, Qinghai, Fujian, Jilin, Jiangxi, and Henan) was made in the study. Analysis of variance was applied to compare the differences in HRQOL of elderly hypertensive patients in different BMI categories. Results For the elderly hypertensive patients with low body mass index, the scores of 8 dimensions and scores in physical component summary (PCS) and mental component summary( MCS) of SF-36 were the lowest;except the role-emotional(RE) dimension,the scores of other 7 dimensions,PCS and MCS were significantly different(PF,RP,BP,GH,VT,MH, P<0.01; SF,PCS,MCS, P<0.01). Comparing the scores between any two groups in PCS, the scores of patients with low body mass index were significantly lower than normal weight group (62.30 ± 22. 12 vs72.40 ±20.86, P<0.05) .overweight group (62.30 ± 22.12 vs 74.97 ± 19.20, P<0.05 ) and obese group (62.30 ± 22.12 vs 74.57 ± 19. 22, P < 0.05 ). Comparing the scores between any two groups in MCS,the scores of patients with low body mass index were significantly lower than normal weight group (68. 81 ± 20. 48 vs 74. 70 ± 20.41, P < 0. 05), overweight group (68. 81 ± 20. 48 vs 78.08 ±18.23, P<0.05) and obese group (68.81 ±20.48 vs 78. 69 ± 17.77, P<0.05); the score of normal weight group was significantly lower than the overweight group (74. 70 ±20. 41vs 78. 08 ±18.23, P<0.05). Gender Stratification showed that females with low body mass index had worse HRQOL than males. Conclusion The HRQOL of elderly hypertensive patients with low body mass index is significantly lower than normal weight patients, overweight patients and obese patients, the health promotion of elderly hypertensive patients with low body mass index should be paid more attentions, especially females with low body mass index.

From cooperation between World Federation of Acupuncture-Moxibustion Societies (WFAS) and World Health Organization, works of academics and standardization, acupuncture-moxibustion education, technique service, organization development, etc., the 27-year development of WFAS since 1987 was summarized and reviewed in details. The growth of WFAS witnesses and promotes the development of acupuncture and moxibustion in the world, so by learning the experience and lessons, WFAS could have a wider path, becoming a core organization for communicating and promoting the development of acupuncture, even the traditional medicine in the world.
Acupuncture ; education ; history ; organization & administration ; standards ; Acupuncture Therapy ; history ; standards ; Global Health ; history ; History, 20th Century ; History, 21st Century ; Humans ; Moxibustion ; history ; standards ; Societies ; history ; World Health Organization