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

To observe the development of Chinese medicine syndromes of rats with type 2 diabetes and insulin resistance by detecting dynamic changes of laboratory parameters.

Aim Tostudytheinfluencesofsulfated polysaccharides ( SPPM60-D) on the regulation of free calcium concentration ( [ Ca2+] i ) of T lymphocytes of mice in vitro and explore the mechanisms involved. Methods Polysaccharides(PPM60)wereextracted from masson pine pollen with hot water and 60% etha-nol. PPM60-D was separated and purified from PPM60 with Sephacryl S-400HR. Sulfated polysaccharides ( SPPM60-D ) were derivated by chlorosulfonic acid-pyridine method and the [ Ca2+] i of T lymphocytes were measured by fluorescence spectrophotometer. IL-2 and IL-4 were measured by ELISA kits. Results ConAandSPPM60-Dcouldincrease[Ca2+]iinT lymphocytes by 211. 5% and 201. 8% respectively ( P<0. 01). 2-APB, LY294002, U73122 and verapamil rather than TAK-242 could significantly inhibit the in-crease of [ Ca2+] i induced by SPPM60-D. SPPM60-D could significantly increase the level of IL-2 and IL-4 in supernatant ( P <0. 01 ) . 2-APB rather than TAK-242 could significantly inhibit the increase of cyto-kines.Conclusion ItisspeculatedthatSPPM60-D could increase [ Ca2+ ] i via TCR/CD3-PI3K-PLC-IP3 R-Ca2+ signal pathway through TCD/CD3 receptor in T lymphocytes so that it could improve the level of IL-2 and IL-4 in supernatant in T lymphocytes.

Objective: To evaluate the depression and anxiety in patients with sleep apnea-hypopnea syndrome (SAHS). Methods: Fifty patients with SAHS were diagnosed with polysomnography (PSG) and 30 healthy controls underwent whole-night PSG monitory and evaluated by Zung Self-rating Depression Scale (SDS) and Zung Self-rating Anxiety Scale (SAS). Results: The total scores of SAS and SDS in SAHS group were significantly higher than those in control group ( P

AIM:To explore the cataract suspensory ligament rupture and artificial lens implantation suture fixation into capsular bag without capsular tension ring(CTR).METHODS:We reviewed 20 cases of 20 cataract suspensory ligament rupture without CTR intraocular lens (IOL) implantation fixation in our department from Jan.2012 to Dec.2016.The needle crossed into ocular ciliary sulcus, in the equator of the eye ball which suspensory ligament rupture from, then the needle crossed out 1.5mm away from the angle of sclera.Sutures fixed on the IOL, then the artificial lens implantation in the pouch, carried out in accordance with the Z type suture, or to the beforehand prepared triangle scleral flap.The visual acuity, intraocular pressure, the anterior chamber and the IOL position were measured after operations.RESULTS:All of the postoperative visual acuity improved different level.The postoperative best corrected visual acuity(BCVA) was ≥0.8 in 4 eyes(20%), 0.5-0.6 in 7 eyes(35%), 0.3-0.4 in 8 eyes(40%), 0.1 in 1 eye(5%) because of the glaucoma optic atrophy.There were 12 cases with mild corneal endothelium edema, 4 cases exudation membrane in the pupil area, 2 cases hyphema, all of which recovered after treatment.There were 2 eyes with vitreous prolapse in the pupil, 1 case appeared mild IOL center deviation and no special treatment for the vision did not be involved.Followed up for 6mo, displaced stitches or artificial lens shift did not occur.CONCLUSION:Without CTR, the IOL implantation and suture fixation in capsular bag during cataract surgery is a surgical method for basic-level hospitals.

To study the correlation between traditional Chinese medicine (TCM) syndrome type and the ultrasound imaging changes in patients with limb lymphedema, and to provide evidence for TCM syndrome differentiation.

Cone-Beam Computed Tomography ; methods ; Humans ; Nasopharyngeal Neoplasms ; diagnostic imaging ; radiotherapy ; Radiotherapy Planning, Computer-Assisted ; Radiotherapy, Intensity-Modulated ; methods

Humans ; Occupational Health ; Refuse Disposal

Objective To investigate the clinical value of homocysteine(Hcy) ,coagulation function ,platelet parameters and he-morheology detection in patients with cerebral infarction .Methods 114 patients with cerebral infarction were served as cerebral in-farction group ,while 112 healthy people as control group .Their platelet parameters ,coagulation function ,Hcy and hemorheology were detected .Results Hcy ,Fibrinogen(Fib) and D-dimer(D-D) of patients in cerebral infarction group were higher than those in control group(P<0 .05) ,while the differences of prothrombin time(PT) ,activated partial thromboplastin time(APTT) and throm-bin time(TT) between the two groups showed no statistically significant (P> 0 .05) .In cerebral infarction group ,platelet count (PLT) of patients was lower ,and platelet distribution width(PDW) and mean platelet volume(MPV) were higher than those in the control group(P<0 .05) while plateletcrit(PCT) showed no statistically significant difference between the two groups (P<0 .05) . Whole blood viscosity ,plasma viscosity and hematocrit of patients in the cerebral infarction group were higher than those in the con-trol group(P< 0 .05) .Conclusion Hcy ,coagulation function ,platelet parameters and hemorheology detection have important significance for prediction and early diagnosis and treatment of cerebral infarction .

Objective To investigate the effect of Kaixin-San (KXS) on behavior, brain monoamine transmitters, and hippocampal brain-derived neurotrophic factor (BDNF) in mice receiving tail suspension test (TST), so as to explore the correlation of the antidepressant effect of KXS and hippocampal BDNF level. Methods The effect of KXS on the immobility time of mice in the TST was observed. The levels of norepinephrine (NE), dopamine (DA) and 5-hydroxytryptamine (5-HT) in the brain were determined by high-performance liquid chromatography (HPLC). Western blotting analysis was used to examine the expressions of cAMP-response element-binding protein (CREB), p-CREB, and BDNF in the hippocampus. BDNF mRNA expression was also examined by RT-PCR. Pearson's correlation analysis was used to evaluate relationship between anti-depression effect of Kaixin-San and hippocampal BDNF level. Results KXS reduced the immobility time of mice in the TST (P<0.05); it also increased the brain levels of monoamine transmitters (DA and 5-HT) and hippocampal levels of CREB, p-CREB and BDNF compared with the control mice(P<0.05). Moreover, the anti-depression effect of KXS was correlated with BDNF level (protein:r=-0.694, P<0.01; mRNA:r=-0.547, P<0.01) in the hippocampus. Conclusion The anti-depression effect of KXS is positively correlated with the hippocampal BDNF level, indicating KXS may exert anti-depression effect via increasing hippocampal BDNF.