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Article in Chinese | WPRIM | ID: wpr-825136


@#Using ALK5 inhibitor LY-3200882 as a lead compound, ten structurally novel compounds were designed by bioisosterism, conformational restriction and molecular docking technology. All structures were synthesized and confirmed by 1H NMR and HR-MS. The results of in vitro activity screening showed that most compounds had good kinase inhibitory activity. Among them, compound B4 showed significantly better ALK5 inhibitory activity than LY-3200882 (IC50 = 1.4 nmol/L vs 41.1 nmol/L), and had good inhibitory activity against TGFβ-ALK5-SMAD2/3 signaling pathway in NIH3T3 cells (IC50 = 14.2 nmol/L). Besides, compound B4 had good pharmacokinetic properties, such as oral exposure and bioavailability, which is worthy of further development.

Article in Chinese | WPRIM | ID: wpr-687630


Coronary atherosclerotic heart disease is a serious threat to human life and health. In recent years, the main treatment for it is to implant the intravascular stent into the lesion to support blood vessels and reconstruct blood supply. However, a large number of experimental results showed that mechanical injury and anti-proliferative drugs caused great damage after stent implantation, and increased in-stent restenosis and late thrombosis risk. Thus, maintaining the integrity and normal function of the endothelium can significantly reduce the rate of thrombosis and restenosis. Stem cell mobilization, homing, differentiation and proliferation are the main mechanisms of endothelial repair after vascular stent implantation. Vascular factor and mechanical microenvironmental changes in implanted sites have a certain effect on re-endothelialization. In this paper, the process of injury caused by stent implantation, the repair mechanism after injury and its influencing factors are expounded in detail. And repairing strategies are analyzed and summarized. This review provides a reference for overcoming the in-stent restenosis, endothelialization delay and late thrombosis during the interventional treatment, as well as for designing drug-eluting and biodegradation stents.

Chongqing Medicine ; (36): 1657-1658, 2017.
Article in Chinese | WPRIM | ID: wpr-511936


Objective To analyze the epidemiological characteristics of Mycoplasma pneumoniae(MP)infection in children with acute respiratory tract infection in Haikou area and surrounding area to provide a scientific evidence for the prevention and treatment of MP infection in children.Methods A total of 1 699 children inpatients with acute respiratory tract infection in our hospital from 1 January to 1 December,2014 were collected.The serum MP antibody was detected.The MP infection status of different sites,genders,ages and months was retrospectively analyzed.Results Among 1 699 children patients with acute respiratory tract infection,the total positive rate of MP infection was 17.60%,in which male was 15.73% and female was 21.59%,the positive rate of female was higher than that of male with statistical difference(P<0.01).The lower respiratory infection rate was 18.75% and upper respiratory tract infection was 13.70%,the difference was statistically significant(P<0.05).The MP infection rates was common in children aged >1-4 years old,in which children aged >3-4 years old had the highest infection rate.MP infection was sporadic in the whole year and was highly epidemic in March and April.Conclusion MP was an important pathogen of acute respiratory tract infection for children in Haikou during 2014,and its epidemic characteristics were manifested by higher incidence in female than that in male.Children aged within 4 years old are a high onset group and MP infection occurs all year round,March and April are the relatively high onset period of MP infecting.

Article in Chinese | WPRIM | ID: wpr-616147


Objective To explore the difference in ocular biologically effective ultraviolet irradiance in two areas with different altitudes ,Xichang and Shaoxing,and provide a reference basis for ocular UV protection. Methods A self?designed rotating mannequin and dual?detector spectrome?ter were used to monitor the intensity of ocular exposure to UV irradiation under clear skies in Xichang and Shaoxing. Monitoring data were pro?cessed and analyzed with AvaSoft 7.4 USB2 software and OriginPro 8.0 software. Results The diurnal variations of ocular biologically effective ul?traviolet irradiance exhibited bimodal distribution in Xichang and Shaoxing. The maximum UVBEcorn,UVBEconj,and UVBElens of Xichang were about 1.7 times,2 times,and 1.8 times that of Shaoxing,respectively. Under the same solar elevation angle,the biologically effective ultraviolet irra?diance of the cornea,conjunctiva,and lens in Xichang were higher than those of Shaoxing. Conclusion The diurnal variations of ocular biologi?cally effective ultraviolet irradiance exhibit bimodal distribution in areas at two different altitudes. Under the same solar elevation angle ,the biologi?cally effective ultraviolet irradiance of the cornea,conjunctiva,and lens of Xichang are significantly higher than those of Shaoxing.

China Pharmacy ; (12)2007.
Article in Chinese | WPRIM | ID: wpr-533259


OBJECTIVE:To establish an ion-pair RP-HPLC method for determination of the concentration of netilmicin sulfate in human serum.METHODS:The determination was performed on Luna C18 column with column temperature set at 40℃;the mobile phase consisted of acetonitrile-water (15∶85,pH 2.0,containing 10 mmol?L-1 sodium heptanesulfonate) at a flow rate of 0.8 mL?min-1.The detection wavelength was set at 205 nm.RESULTS:The linear range of netilmicin was 2~20 mg?L-1(r=0.997 6) with a recovery rate of 93.66%~96.05%.The intra-day and inter-day RSD were both less than 10%,respectively.CONCLUSION:The method is sensitive and simple with accurate and reliable results,and it is able to satisfy the requirement for the determination of serum concentration of netilmicin.

China Pharmacy ; (12)2007.
Article in Chinese | WPRIM | ID: wpr-531372


OBJECTIVE: To establish an HPLC method for simultaneous determination of the content of sulfadiazine and dexamethasone acetate in compound nasal ointment.METHODS: The determination was performed on Inertsil C8-3 column with column temperature set at 40 ℃;the mobile phase consisted of methanol-acetonitrile-water(72∶3∶25) with a flow rate of 1.0 mL?min-1.The detective wavelength was set at 240 nm and the sample size was 20 ?L.RESULTS: The linear ranges for sulfadiazine and dexamethasone acetate were 74.65~746.5(r=0.999 9) and 1.495~14.95 ?g?mL-1(r=0.999 7),respectively.The average recoveries were 100.72%(RSD=1.7%) and 100.41%(RSD=1.6%),respectively.CONCLUSION: This method is rapid,simple,accurate and reliable and suitable for the determination of the content of sulfadiazine and dexamethasone acetate in compound nasal ointment.