Identification of a new azoreductase driven prodrug from bardoxolone methyl and 5-aminosalicylate for the treatment of colitis in mice / 中国天然药物

For local treatment of ulcerative colitis, a new azoreductase driven prodrug CDDO-AZO from bardoxolone methyl (CDDO-Me) and 5-aminosalicylate (5-ASA) was designed, synthesized and biologically evaluated. It is proposed that orally administrated CDDO-AZO is stable before reaching the colon, while it can also be triggered by the presence of azoreductase in the colon to fragment into CDDO-Me and 5-ASA, generating potent anti-colitis effects. Superior to olsalazine (OLS, a clinically used drug for ulcerative colitis) and CDDO-Me plus 5-ASA, CDDO-AZO significantly attenuated inflammatory colitis symptoms in DSS-induced chronic colitis mice, which suggested that CDDO-AZO may be a promising anti-ulcerative colitis agent.

Design, synthesis, and biological evaluation of ligustrazine/resveratrol hybrids as potential anti-ischemic stroke agents / 中国天然药物

To search for potent anti-ischemic stroke agents, a series of tetramethylpyrazine (TMP)/resveratrol (RES) hybrids 6a-t were designed and synthesized. These hybrids inhibited adenosine diphosphate (ADP)- or arachidonic acid (AA)-induced platelet aggregation, among them, 6d, 6g-i, 6o and 6q were more active than TMP. The most active compound 6h exhibited more potent anti-platelet aggregation activity than TMP, RES, as well as positive control ticlopidine (Ticlid) and aspirin (ASP). Furthermore, 6h exerted strong antioxidative activity in a dose-dependent manner in rat pheochromocytoma PC12 cells which were treated with hydrogen peroxide (HO) or hydroxyl radical (·OH). Importantly, 6h significantly protected primary neuronal cells suffered from oxygen-glucose deprivation/reoxygenation (OGD/R) injury, comparable to an anti-ischemic drug edaravone (Eda). Together, our findings suggest that 6h may be a promising candidate warranting further investigation for the intervention of ischemic stroke.

Synthesis and evaluation of 2-cyano-3, 12-dioxooleana-1, 9(11)-en-28-oate-13β, 28-olide as a potent anti-inflammatory agent for intervention of LPS-induced acute lung injury / 中国天然药物

The present study was designed to synthesize 2-Cyano-3, 12-dioxooleana-1, 9(11)-en-28-oate-13β, 28-olide (1), a lactone derivative of oleanolic acid (OA) and evaluate its anti-inflammatory activity. Compound 1 significantly diminished nitric oxide (NO) production and down-regulated the mRNA expression of iNOS, COX-2, IL-6, IL-1β, and TNF-α in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Further in vivo studies in murine model of LPS-induced acute lung injury (ALI) showed that 1 possessed more potent protective effects than the well-known anti-inflammatory drug dexamethasone by inhibiting myeloperoxidase (MPO) activity, reducing total cells and neutrophils, and suppressing inflammatory cytokines expression, and thus ameliorating the histopathological conditions of the injured lung tissue. In conclusion, compound 1 could be developed as a promising anti-inflammatory agent for intervention of LPS-induced ALI.

Synthesis and anti-hepatocellular carcinoma activity of novel O-vinyl diazeniumdiolate-based nitric oxide-releasing derivatives of oleanolic acid / 中国天然药物

Considering that high levels of nitric oxide (NO) exert anti-cancer effect and the derivatives of oleanolic acid (OA) have shown potent anti-cancer activity, new O-vinyl diazeniumdiolate-based NO releasing derivatives (5a-l, 11a-l) of OA were designed, synthesized, and biologically evaluated in the present study. These derivatives could release different amounts of NO in liver cells. Among them, 5d, 5i, 5j, 11g, 11h, and 11j released more NO in SMMC-7721 cells and displayed stronger proliferative inhibition against SMMC-7721 and HepG2 cells than OA and other tested compounds. The most active compound 5j showed almost 20-fold better solubility than OA in aqueous solution, released larger amounts of NO in liver cancer cells than that in normal ones, and exhibited potent anti-hepatocellular carcinoma activity but little effect on the normal liver cells. The inhibitory activity against the cancer cells was significantly diminished upon addition of an NO scavenger, suggesting that NO may contribute, at least in part, to the activity of 5j.

Advances in hydrogen sulfide and hydrogen sulfide-releasing drugs / 药学学报

Hydrogen sulfide (H2S) is considered as a new member of gasotransmitter family, following nitric oxide (NO) and carbon monoxide (CO). H2S exerts important biological effects in mammals, which has drawn more and more attention in recent years. It is proved that H2S has a role in the regulation of physiological and pathophysiological processes in the cardiovascular system and the nervous system. Several cardiovascular and nervous diseases are connected to H2S. H2S-releasing agents (also known as H2S donors) have been widely used not only as useful research tools but also potential therapeutic agents. In this review, we provide an overview of the chemistry and biology of H2S, and summarize the chemistry and biological activity of some natural and synthetic H2S donors. We introduce the developments of currently available H2S-releasing drugs including H2S-non-steroidal anti-inflammatory drugs, H2S-nervous system drugs and NO-H2S-releasing drugs. We hope this review will be a value reference in the development of H2S-releasing drugs in the treatment of cardiovascular and nervous diseases.

Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (HS) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents / 中国天然药物

In the present study, a series of novel nitric oxide-hydrogen sulfide releasing derivatives of (S)-3-n-butylphthalide ((S)-NBP) were designed, synthesized, and evaluated as potential antiplatelet agents. Compound NOSH-NBP-5 displayed the strongest activity in inhibiting the arachidonic acid (AA)- and adenosine diphosphate (ADP)-induced platelet aggregation in vitro, with 3.8- and 7.0-fold more effectiveness than (S)-NBP, respectively. Furthermore, NOSH-NBP-5 could release moderate levels of NO and HS, which would be beneficial in improving cardiovascular and cerebral circulation. Moreover, NOSH-NBP-5 could release (S)-NBP when incubated with rat brain homogenate. In conclusion, these findings may provide new insights into the development of novel antiplatelet agents for the treatment of thrombosis-related ischemic stroke.

Expression of phosphatidylinositol-3 kinase and effects of inhibitor Wortmannin on expression of tumor necrosis factor-α in severe acute pancreatitis associated with acute lung injury / 世界急诊医学杂志（英文）

@#BACKGROUND: Acute lung injury (ALI) is a common and serious complication of severe acute pancreatitis (SAP). The study aimed to investigate the protective effect and mechanism of phosphatidylinositol-3 kinase (PI3K) inhibitor Wortmannin in SAP associated with ALI. METHODS: Ninety rats were randomly divided into three groups: sham operation (SO) group (n=30), SAP group (n=30), and SAP+Wortmannin (SAP+W) group (n=30). SAP model was induced by retrograde injection of 4％ sodium taurocholate into the biliopancreatic duct of rats. The rate of lung water content, myeloperoxidase (MPO), matrix metalloproteinase 9 (MMP-9), protein kinase B (PKB), abdphosphorylation of protein kinase B (P-PKB) activity in the lung tissue were evaluated. RESULTS: In the SAP group, the p-PKB expression in the lung tissue began to rise at 3 hours after modeling, and peaked at 12 hours (P<0.05); the rate of lung water content, MPO and TNF-α activity were also gradually increased, and the degree of lung lesion gradually increased (P<0.05). In the SAP+Wortmannin group, the p-PKB expression in the lung tissue began to rise at 3 hours after modeling, and peaked at 12 hours; it was higher than that in the SO group (P<0.05), but signifi cantly lower than that in the SAP group (P<0.05). The rest indicators in the SAP+Wortmannin group were also signifi cantly decreased as compared with the SAP group (P<0.05). CONCLUSIONS: The expression of phosphatidylinositol-3 kinase/protein kinase B was elevated in severe pancreatitis rats with lung injury. This suggested that PI3K signal transduction pathway is involved in the control and release of proinfl ammatory cytokines TNF-α, which may play an important role in the pathogenesis of severe acute pancreatitis associated with lung injury. This finding indicated that Wortmannin can block the PI3K signal transduction pathway, and inhibit the release of infl ammatory factor TNF-α.

Analysis of measles immunity level in persistent populations in Beijing, 2012 / 中华预防医学杂志

<p><b>OBJECTIVE</b>To analyze the measles immunity level of persistent population in Beijing.</p><p><b>METHODS</b>A total of 2125 objects from 10 age groups, who had been living in Beijing for over 6 months, were selected from urban and rural areas in Beijing in 2012. Demographic characteristics, history of measles and vaccine immunization were investigated by questionnaire. 5 ml blood sample of each subject was collected, and the Measles IgG antibody was measured by ELISA assay.</p><p><b>RESULTS</b>Positive rate of measles antibody was 84.71% (1800/2125) and standardized positive rate was 88.07% . Median of antibody was 960.46 IU/L. Positive rate and median of measles antibody were significantly different between population from different age groups (χ(2) = 341.60, P < 0.01; H = 216.27, P < 0.01). Antibody positive rate and median were lowest in the <1 year age group, which were separately 43.06% (90/209) and 185.80 IU/L; and highest in the 1-4 (97.31% (181/186) and 2448.81 IU/L) and 5-9 years age group (96.46% (218/226) and 1910.72 IU/L). The range of antibody positive rate and median in adults of ≥ 15 years were 81.98%-90.14% and 744.38-1474.84 IU/L. Antibody positive rate and median in persistent population, which were separately 82.45% (883/1071) and 899.82 IU/L, were lower than those in migrant population, which were 87.00% (917/1054) and 166.19 IU/L, respectively (χ(2) = 8.51, P < 0.01;U = 538 704.00, P < 0.01). Antibody positive rate and median in population with vaccination history, which were separately 91.95% (891/969) and 1443.11 IU/L, were higher than those population without vaccination history and people whose history unknown (32.95% (57/173) , 127.33 IU/L; 86.67% (852/983) , 923.73 IU/L). The difference showed statistical significance (χ(2) = 399.92, P < 0.01; H = 202.11, P < 0.01).</p><p><b>CONCLUSION</b>Among the persistent population in China, measles antibody level among the children aging 1-9 years old was high enough to prevent outbreak and epidemic of measles. However, we should try our best to strengthen the measles antibody level among the babies younger than 1 year old and the migrant population aging between 15 and 40 years old.</p>

Investigation of social support for inpatients with occupational diseases / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To investigate and analyze the social support for inpatients with occupational diseases and to provide reference and basis for relevant medical and nursing interventions.</p><p><b>METHODS</b>The social support rating scale (SSRS) was used to investigate the social support for 95 inpatients with occupational diseases.</p><p><b>RESULTS</b>The total SSRS score of these patients was significantly lower than the national norm (32.5±9.31 vs 34.56±3.73, P < 0.05). The social support was mainly from the family, but medical staff and spiritual support were the main source and type of social support that are expected.</p><p><b>CONCLUSION</b>Patients with occupational diseases have gained little social support, in both economic and spiritual aspects. In clinical practice, the patient's demand for knowledge of diseases and spiritual needs should be satisfied, and appropriate social support should be provided.</p>

Effects of ozone exposure on percentage of CD4(+)CD25(high)Foxp(3+) regulatory T cells and mRNA expression of Foxp3 in asthmatic rats / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To investigate the effects of low-concentration ozone exposure on the percentage of CD4(+)CD25(high)Foxp(3+) regulatory T cells and the mRNA expression of transcription factor Foxp3 in asthmatic rats.</p><p><b>METHODS</b>Sixty male Wistar rats were randomly divided into 4 groups (n = 15 for each): normal control group, ovalbumin (OVA) exposure group, ozone exposure group, and OVA+ozone exposure group. The OVA exposure group was sensitized and challenged with OVA to establish an asthma model; the normal control group inhaled aerosolized saline; the ozone exposure group inhaled low-concentration ozone; the OVA+ozone exposure group inhaled low-concentration ozone before being challenged with aerosolized OVA every day. The percentage of CD4(+)CD25(high)Foxp(3+) regulatory T cells in CD4(+) T cells was determined by flow cytometry. The levels of interferon-γ (INF-γ) and interleukin 4 (IL-4) in peripheral blood and lung tissue were measured by enzyme-linked immunosorbent assay. The mRNA expression of Foxp3 in lung tissue was measured by PCR.</p><p><b>RESULTS</b>The percentages of CD4(+)CD25(high)Foxp(3+) regulatory T cells in OVA exposure group (6.12±1.03%) and ozone exposure group (5.87±1.26%) were significantly lower than that in normal control group (9.85±1.34%), and the percentage of CD4(+)CD25(high)Foxp(3+) regulatory T cells in OVA+ozone exposure group (3.31±0.85%) was significantly lower than those in normal control group and OVA exposure group (P < 0.01). The levels of IL-4 in plasma and lung tissue in OVA exposure group (plasma: 21.83±5.12 ng/L; lung tissue: 0.89±0.13 ng/L) were significantly higher than those in normal control group (plasma: 10.58±2.73 ng/L; lung tissue: 0.32±0.11 ng/L) (P < 0.01). The levels of IL-4 in plasma and lung tissue in OVA+ozone exposure group (plasma: 35.47±7.24 ng/L; lung tissue: 1.50±0.42 ng/L) were significantly higher than those in normal control group and OVA exposure group (P < 0.01). The levels of INF-γ in plasma and lung tissue in OVA exposure group (plasma: 61.78±23.45 ng/L; lung tissue: 0.69±0.21 ng/L] were significantly lower than those in normal control group [plasma: 158.89±60.23 ng/L; lung tissue: 1.86±0.29) (P < 0.01). The levels of INF-γ in plasma and lung tissue in OVA+ozone exposure group (plasma: 10.28±2.63 ng/L; lung tissue: 0.41±0.12 ng/L) were significantly lower than those in normal control group and OVA exposure group (P < 0.01). The mRNA expression of Foxp3 was significantly lower in the OVA+ ozone exposure group than in the normal control group (P < 0.05).</p><p><b>CONCLUSION</b>Low-concentration ozone exposure may decrease the number of CD4(+)CD25(high)Foxp(3+) regulatory T cells and inhibit the mRNA expression of Foxp3 to promote Th1/Th2 imbalance in asthmatic rats, suggesting that ozone exposure may be one of factors that induce asthma attack.</p>

Rapid identification 15 effective components of anti common cold medicine with MRM by LC-MS/MS / 药学学报

This paper reports the establishment of a method for rapid identification 15 effective components of anti common cold medicine (paracetamol, aminophenazone, pseudoephedrine hydrochloride, methylephedrine hydrochloride, caffeine, amantadine hydrochloride, phenazone, guaifenesin, chlorphenamine maleate, dextromethorphen hydrobromide, diphenhydramine hydrochloride, promethazine hydrochloride, propyphenazone, benorilate and diclofenac sodium) with MRM by LC-MS/MS. The samples were extracted by methanol and were separated from a Altantis T3 column within 15 min with a gradient of acetonitrile-ammonium acetate (containing 0.25% glacial acetic acid), a tandem quadrupole mass spectrometer equipped with electrospray ionization source (ESI) was used in positive ion mode, and multiple reaction monitoring (MRM) was performed for qualitative analysis of these compounds. The minimum detectable quantity were 0.33-2.5 microg x kg(-1) of the 15 compounds. The method is simple, accurate and with good reproducibility for rapid identification many components in the same chromatographic condition, and provides a reference for qualitative analysis illegally added chemicals in anti common cold medicine.

Large bone-flap decompressive craniotomy for treatment of serious craniocerebral injury associated with cerebral infarction / 中华创伤杂志(英文版)

<p><b>OBJECTIVE</b>To elucidate the therapeutic effect of subtemporal decompressive craniotomy with large flap resection on serious craniocerebral injury associated with cerebral infarction.</p><p><b>METHODS</b>Forty-eight cases of serious head injury accompanied by cerebral infarction were classified into two groups with each having 24 cases: treatment group, in which large bone-flap decompressive craniotomy was performed; control group, in which routine craniotomy and hematoma evacuation were adopted. The status of cerebral infarction pre- and post-operation, as well as the curative effect 3 months after operation were comparatively analysed between the two groups.</p><p><b>RESULTS</b>There was no significant difference regarding the status of cerebral infarction on the first day after operation; while one week after operation, the size of cerebral infarction was significantly smaller in treatment group than control one (P less than 0.05). Postoperative 3 months, the mortality rate was 20.8% in treatment group, being evidently superior to that of control group (33.3%, P less than 0.05). The mo- derate disability (good and fair) rate was 41.7% in treatment group, significantly higher than that in control group (25.0%, P less than 0.05).</p><p><b>CONCLUSION</b>Large bone-flap decompressive craniotomy is confirmed effective and hence it offers us a preferable alternative of treatment by which to reduce disability and fatality rates for patients with serious head injury accompanied by cerebral infarction.</p>

Analysis on the changing trends of non-communicable diseases in Xinjiang Production and Construction Corps,from 1998 to 2008 / 中华流行病学杂志

Objective To understand the changing trends of non-communicable diseases (NCDs) in Xinjiang Production and Construction Corps from 1998 to 2008.Methods A stratified-cluster random sampling based cross-sectional NCDs survey was carried out in 2008,and using the data of NCDs from the health service surveys in 1998 and 2004,in Xinjiang Production and Construction Corps.The prevalence rate of NCDs was standardization according to age proportion of the population being surveyed in 1998.Results In 1998,2004 and 2008,the prevalence rates of NCDs in Xinjiang Production and Construction Corps were 17.26%,25.61%,24.85% while the Standardized rates of NCDs were 17.26%,23.54% and 20.49% respectively.The prevalence rates of NCDs were statistically significant different in 35-,45-,55- and over 65 age groups in 1998,2004 and 2008 which showed an consecutive upward trend.The prevalence rates of hypertension,diabetes,cerebrovascular disease,coronary heart disease and chronic obstructive pulmonary disease increased significantly from 1998 to 2008.The prevalence rate of hypertensive disease among 25- age group,diabetes among 35- age group,cerebrovascular disease and coronary heart disease among 45- age groups showed an increasing trend.Conclusion Cardiovascular and cerebrovaseular diseases,together with diabetes were the fastest increasing ones over the past 10 years and becoming the major diseases,making the Xinjiang Production and Construction Corps an aging population.NCDs should be prioritized in the health development plan.Targeted health education should be carried out in the whole population,together with other interventions as well as management programs on chronic diseases to reduce the prevalence of NCDs.

Proliferation of retinal pigment epithelial cells induced by (R,R)-XY-10 and (S,S)-XY-10 and their action mechanisms / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: To investigate the mechanism of proliferation effect induced by (R,R)-XY-10 and (S,S)-XY-10 on retinal pigmented epithelial cells(ARPE-19).METHODS: Human retinal pigmented epithelial cells(ARPE-19) and human umbilical vein endothelial cells (HUVECs) were used to investigate the effect of (R,R)-XY-10 and (S,S)-XY-10 on cell growth,and their mechanisms of proliferative action by using ERK、 AKT、PI3K、Protein kinase C (PKC)and Nitric oxide synthase (NOS) inhibitors.RESULTS: (R,R)-XY-10 and (S,S)-XY-10 dose-dependently increased ARPE-19 cell proliferation,but not on HUVECs. When treated with proliferative inhibitors,H7(5μmol/L)、hypericin(20μmol/L)、PD98059(2μmol/L)、LY294002(50μmol/L)、SH-5 (10μmol/L) and L-NAME (100μmol/L),the proliferative effect was reduced by H7、hypericin、PD98059 and LY294002,but not by SH-5 and L-NAME.CONCLUSION: (R,R)-XY-10 and (S,S)-XY-10 can induce cell proliferation through MAPK and PI3K dependent pathway. KEYWORDS: age-related macular degeneration; (R,R)-XY-10; (S,S)-XY-10; ARPE-19 cells; human umbilical vein endothelial cells; proliferation

Relationship study of angiotensin II type 1 receptor gene A1166C polymorphism, food consumption and behavior on hypertension in Kazakh group, Xinjiang / 中华预防医学杂志

<p><b>OBJECTIVE</b>To investigate the polymorphism of angiotensin II type 1 receptor (AT(1R)) gene A1166C and environmental factors on hypertension of Kazakh people.</p><p><b>METHODS</b>Through the random program of SPSS 13.0, 220 cases were randomly selected from the confirmed hypertension patients, and 220 cases with normal blood pressure were selected as control group. All cases were investigated through the questionnaire and the related indexes were measured. By polymerase chain reaction (PCR) method, the genotypes were determined.</p><p><b>RESULTS</b>(1) In hypertension group, the genotype frequency of AA and AC were 78.6% (173/220) and 21.4% (47/220), respectively, compared with control groups' 81.4% (179/220) and 18.6% (41/220), no significant difference was identified between these two groups (chi(2) = 0.537, P > 0.05). In hypertension group, the frequency of A and C allele were 89.0% and 11.0%, respectively, compared with 90.3% and 9.7% in control group. There was no significant difference between these two groups (chi(2) = 0.37, P > 0.05). (2) AC genotype might interact with excessive salt consumption (hypertension group, 31/220, 15.5%; control group 10/220, 4.5%, OR: 4.67, 95%CI: 2.15 - 10.15), overweight (hypertension group, 19/220, 8.6%; control group, 9/220, 4.1%, OR: 6.96, 95%CI: 2.33 - 20.76) and drinking large volume of salty milk (hypertension group, 20/220, 9.1%; control group, 10/220, 4.5%, OR: 2.67, 95%CI: 1.11 - 6.42) which will raise hypertension hazard of AC genotype.</p><p><b>CONCLUSION</b>There is no relationship between the A1166C gene polymorphism of AT(1R) gene and hypertension of Kazakh people. AC genotypes might also interact with food consumption habit and behavior factors and increase the individual risk of hypertension.</p>

Advances in the study of nitric oxide-donating drugs / 药学学报

Nitric oxide (NO) as a messenger and/or effector plays important roles in vivo. The decreased availability of NO or dysfunction in NO signaling has often been implicated in the development and progression of diseases, and design and research of NO-donating drugs has become one of the important strategies in drug discovery. In connection with authors' scientific practice, this article reviews the recent advances in the research of NO-donating drugs.

Effects of enantiomers(R,R)-XY and(S,S)-XY on ocular blood flow in rabbits / 国际眼科杂志(Guoji Yanke Zazhi)

·AIM: To evaluate the effects of two series of enantiomers [(R, R)-XY-1 through (R, R)-XY-12 and (S,S)-XY-1 through (S, S)-XY-12] on ocular blood flow in rabbits.·METHODS; Colored microsphere technique was used for in vivo experiments to determine the ocular blood flow in various tissues of ocular hypertensive (40mmHg) rabbit eyes.·RESULTS; Of the twelve compounds of ( R, R)-XY series examined, four increased choroidal blood flow at 10g/L, 50uL instilled into eyes. All compounds of (S, S)-XY series were not effective on ocular blood flow.·CONCLUSION; Some compounds of (R, R)-XY series increased the ocular blood flow, which might be useful for the prevention and treatment of ocular blood flow related eye diseases. Among all twenty-four compounds, (R, R)-XY-1and (R, R)-XY-9 seem to be the most potent ones.KEYWORDS; ocular blood flow; ischemia; enantiomer

Effects of ZX-5 and its optical isomers on ocular blood flow in rabbits and retinal function recovery in rats / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: The effects of ZX-5, as nitric oxide (NO) donor, on ocular blood flow has been investigated using colored microsphere technique in previous study. The relationship between the production of NO by ZX-5 and ocular blood flow has been evaluated. ZX-5 has been shown to have strong positive effect on increasing choroidal blood flow. However,the effect of ZX-5 on retinal function recovery, the effects of its optical isomers, (R, R)-ZX-5 and (S, S)-ZX-5, on choroidal blood flow and retinal function recovery have not been studied and merit investigation.METHODS: Colored microsphere technique was used for in vivo experiments to determine choroidal blood flow of ocular hypertension (40mmHg) in rabbit eyes. Electroretinography was used to measure the b-wave recovery as an indication of retinal function recovery.RESULTS: (R, R)-ZX-5 increased choroidal blood flow at 10g/L, 50μL instillation into eyes at all time points (P＜0.05).(S, S)-ZX-5 was not effective in increasing choroidal blood flow. ZX-5 and (R, R)-ZX-5 showed significant effects in retinal function recovery after ischemia of the retina at all time points (P＜0.05); whereas (S, S)-ZX-5 did not show significant effect on recovery of b-wave after ischemia at most time points except at 120 and 240 minutes.CONCLUSION: ZX-5 and (R, R)-ZX-5 have high potency in increasing the choroidal blood flow and improving the retinal function recovery. It is hoped that they could be used for the prevention/treatment of ocular blood flow related eye diseases.

A novel class of anti-inflammatory and analgesic drugs--NO-donating NSAIDs / 药学学报

Traditional non-steroidal anti-inflammatory drugs (NSAIDs) and COX-2 selective inhibitors are among the most widely used drugs. However, their significant side effects in gastrointestinal and cardiovascular systems limited the use of these drugs. Recently, research and development of NO-donating NSAIDs (NO-NSAIDs) have become one of the most important strategies to reduce these side effects. NO-NSAIDs may exert a broad range of positive effects in terms of NO-mediated gastrointestinal and cardiovascular safety as well as comparable or increased anti-inflammatory, analgesic properties relative to NSAIDs. This review briefly deals with chemistry of NO-NSAIDs, more details are focused on biological significance, mechanism of action, and therapeutic potential of this novel class of drugs.

Synthesis and antithrombotic activity of acetylsalicyl ferulic acid-coupling furoxans and nitrates / 药学学报

<p><b>AIM</b>To synthesize and study the antithrombotic activity of NO-donating aspirin derivatives.</p><p><b>METHODS</b>Furoxans and nitrates were incorporated to aspirin via antioxidant ferulic acid as a linker, and the target compounds were screened for in vitro and in vivo inhibitory activities of platelet aggregation, and for inhibitory effect on A-V hypass thromhosis in rats.</p><p><b>RESULTS</b>Fourteen novel compounds I(1-14), were synthesized and their structures were confirmed Iy MS, IR, 1H NMR and elemental analysis. Biological screening results demonstrated that some tested compounds exhibited potential antithrombotic activ it.</p><p><b>CONCLUSION</b>Acetylsalicyl ferulic acid-coupling furoxans and nitrates might he used as a lead for further study.</p>