G protein-coupled receptors(GPCRs)mediate cell signaling transduction of most hormones and neurological transmitters and behave as the key targets for drug research and development.Recently,the evidence of allosteric modulation of GPCRs has been revealed.Allosteric modulators have the ability to selectively tune responses only in tissues in which the endogenous agonist exerts its physiological effects,and have the potential for greater receptor subtype selectivity.The GPCRs allosteric modulators have been found and some of them have been in clinical use.Under the strategy of allosterism on structure activity relationship and target directed screening,more and more GPCRs allosteric modulators will be developed in the future.

Theapplicationofinternalextractiveelectrosprayionizationmassspectrometry(iEESI-MS)was extended to direct molecular analysis of garlic tissues. By obviating time-consuming sample preparations, fragile active garlic substances such as organosulfur compounds ( e. g. , alliin, allicin ) were successfully detected and identified via collision-induced dissociation ( CID) , together with amino acids ( e. g. , arginine) and saccharides ( glucose, polysaccharides) . Mass spectral fingerprints of different kinds of garlic cloves, as well as various post-treatment ones, were further processed via principal component analysis ( PCA) to better visualize the differences. Our experimental results indicated that iEESI-MS allowed rapid recognition of metabolic changes in the garlic tissue subject to various external stimuli. The merits included simplicity of analysis, high speed ( less than 2 min per sample ) , good specificity, and minimal disturbance to the bioactivity of analytes.

Objective To compare the image quality of portal venous system in the patients with live cirrhosis and portal hyper-tension using two different inj ection methods,so as to investigate the optimization of imaging techniques.Methods Single-phase in-jection (group A)or biphasic injection (group B)was applied by random on 40 patients for portal venous system vascular imaging, and subsequently image quality and technical advantages between the two groups were compared and analyzed respectively.Results 1.There was no significant difference in image quality between the two groups(P>0.05),while contrast agent dosage (90 mL)in group B is less than group A(100 mL).2.The CT value of Portal vein,liver parenchyma and P-L discrepancy in group B were slightly lower than those in group A,however,no statistical difference was noted(P>0.05).After 45 second,the P-L discrepancy of group B was larger than that of group A.The peak times of portal vein,liver parenchyma and the P-L discrepancy in group B were longer than those in group A(P<0.05).3.The graph of P-L discrepancy demonstrated:the threshold interval of P-L discrep-ancy in group B was longer than that in group A.Conclusion Biphasic inj ection methods could not only afford reliable imaging quali-ty on portal venous system vascular imaging in the patients with liver cirrhosis and portal hypertension,but also lead to a less total dose of contrast agent.Therefore,it could be used as an optimal choice of imaging technology for portal venous system vascular ima-ging.

OBJECTIVE: To explore the diagnostic value of brain natriuretic peptide (BNP) level in patients with sepsis of blood-stasis syndrome. METHODS: The prospective method of clinical diagnostic test and evaluation principles of diagnostic test were applied. One hundred and seventy-four patients with sepsis were divided into two groups: blood-stasis syndrome group and non blood-stasis syndrome group. The levels of serum BNP in two groups were detected. RESULTS: The level of BNP in sepsis patients was related to blood-stasis syndrome (P<0.01). BNP cut-off level was 150 ng/L, sensitivity was 85.3%, specificity was 81%, the maximum value of Youden index was 0.663, and the area under the receiver operating characteristic curve (ROC) value was (0.886+/-0.025). CONCLUSION: BNP can be used as an objective index of blood-stasis syndrome diagnosis for sepsis, and BNP with boundary value of 150 ng/L is an optimal biological index.

ObjectiveThe present study aimed to determine whether or not dual paroxysm proliferator-activated receptor (PPAR) agonist,WY14643,improved the dysfunctioned vascular endothelium in hypertension by reducing endothelium-derived contracting factors ( EDCFs ),and to explore the molecular mechanism it was involved in.MethodsIsometric tension in isolated thoracic aortic rings of spontaneously hypertensive rats was recorded.Endothelium-dependent contractions evoked by acetylcholine in the presence of L NAME were reduced by fenofibrate.Cyclooxygenase 1 ( COX1 ) activities were determined by analyzing the peroxidase activity of cyclooxygenase colorimetrically by using ELISA kit.ResultsCompared to the control group,WY14643 significantly decreased the vasoconstriction in aorta of the SHR rats(P=0.014).PPARα antagonist MK866 enhanced the vascular contractility of SHR rats that were incubated with 10.0μmol/L WY14643( P=0.021 ).PPARΥ antagonist GW9662 did not significantly affect the vascular contractility of SHR rats that were incubated with 10.0 μmol/L WY14643( P=0.061 ).The levels of serum PGFlα(P=0.012),2α( P =0.019) and TXB2(P=0.023) in SHR rats incubated with 10.0 μmol/L WY14643 were significantly lower than the control group,respectively.Under the condition of the existence of vascular endothelium,the expression of COX-1 in SHR rats incubated with WY14643 was significantly lower than that in SHR rats incubated without WY14643 (P=0.017).ConclusionsThose data showed that WY14643 reduced the release of EDCFs,it suggests that WY14643 protects against vascular diseases through the PPAR activators in spontaneous hypertension.

Aim To study the effect and investigate the underlying mechanism of astragaloside Ⅳ on contraction and relaxation in isolated rat aortic rings.Methods The relaxation effect of astragaloside Ⅳ(1～100 mg?L~(-1))on phenylephrine-preconstricted aorta ring was recorded.The effect of astragaloside Ⅳ on the contraction induced by cumulative phenylephrine,KCl or CaCl_2,was recorded respectively.Results Astragaloside Ⅳ dilated aortic vessels in a dose-dependent manner,which was partly inhibited by preincubation with non-selective nitric oxide synthase inhibitor,guanylyl cyclase inhibitor and cyclooxygenases inhibitor indomethacin.Astragaloside IV could also antagonize phenylephrine-,KCl-and CaCl_2-induced vessel contraction.Conclusion Astragaloside IV dilated aortic vessels partially though endothelium-dependent NO pathway and inhibited vessel contraction via interfering Ca~(2+) influx.

Objective To investigate action and significance of serum nitric oxide(NO) in patients with ulcerative colitis.Methods Levels of serum NO in active stage of 33 patients with ulcerative colitis and 40 healthy controls were detected.Results Levels of serum NO in patients with ulcerative colitis were significantly high and related to severe degrees of the disease (P

Objective To evaluate the level of clinical treatment in severe stable double COPD noninvasive positive pressure ventilation (BiPAP) + tiotropium + Symbicort regimen effect. Methods 210 patients with moderate to severe COPD patients as the research object, divided into group I, group II, group III, 1 BiPAP + group with tiotropium bromide in the treatment scheme, group II Implementation of tiotropium + Symbicort treatment group enabled BiPAP + tiotropium + Symbicort. Results Group comparison indexes of pulmonary function level and lung function indexes were found in the three groups after treatment showed a rising trend comparison between groups after treatment, the levels of the indicators of lung function showed the most significant increases in group I, group II indexes of pulmonary function approximation. In group 6-MWD group with the longest distance difference index (P<0.05), group II and group I but the difference between does not have statistical significance Conclusion BiPAP + tiotropium bromide + Cr is an effective treatment for moderate and severe stable COPD, which is beneficial to improve the quality of life of patients.

Pulse-taking is the most specific diagnostic method of TCM.Its significance has been recognized by ancient and modern doctors.However,at present the application and spread of pulse-taking is limited.In this paper,the author made detailed explorations of literatures and studies the value of pulse condition in guiding syndrome differentiation of liver diseases.The study shows abnormal pulse in left guan and taut pulse in cunkou location both suggest the liver is disordered.We can judge the location of diseases through pulse condition.This exploration shows pulse-taking plays important role in syndrome differentiation.But there is one thing should be paid more attention,pulse condition should be integrated with other symptoms,that will be reliable in guiding diagnosis.

Objective To explore the clinical effects of injection rhinoplasty with non-absorpted material and prevention of the complications.Methods A total of 578 patinets with rhinoplasty in Interpretation Medical Cosmetic Center of Wuhan City and Southwest Hospital from March 2010 to January 2016 were selected,who included 239 cases injected by absorbed material,213 cases injected by non-absorbed material and 126 cases implanted by silicone prosthesis.Then the clinical effects,curative keeping time and complications of three groups in 0,1,3,6 and 12 months after injected or implanted were observed.Results 578 patients of nasal shape and outline were significantly improved immediately after surgery and injection,but the adverse reaction and complication of silicone prosthesis increased more than those of other two groups,the differences were significant(P<0.01).While,the nose shape and outline and cosmetic effects of patients by silicone prosthesis or absorbed material postoperated became worse from 6 months to 1 year(P<0.05),and the non-absorbed groups had kept much better in the nose shape and outline and the satisfactory effects than the other two groups,the differences were significant(P<0.01).Conclusion Injection of rhinoplasty is safe and effective,meanwile the injection rhinoplasty with non-absorbed material is more suitable for Asian with less adverse reaction.