目的观察祝氏降糖对药方对社区慢性阻塞性肺疾病(COPD)合并糖尿病患者血糖水平及呼吸功能影响。方法研究纳入社区收治的114例慢性阻塞性肺疾病合并糖尿病患者(2022年3月—2023年2月收治)作为本次研究对象,以随机数字表法将患者分为观察...目的观察祝氏降糖对药方对社区慢性阻塞性肺疾病(COPD)合并糖尿病患者血糖水平及呼吸功能影响。方法研究纳入社区收治的114例慢性阻塞性肺疾病合并糖尿病患者(2022年3月—2023年2月收治)作为本次研究对象,以随机数字表法将患者分为观察组与对照组,各组57例,对照组患者给予社区常规疗法,观察组患者在社区常规疗法治疗基础上给予患者祝氏降糖对药方治疗,各组数据观察:治疗前后患者空腹血糖(FPG)及餐后2h血糖(2 h PG)、糖化血红蛋白(HbA1c)指标变化,用力肺活量(FVC)及一秒用力呼气容积(FEV_(1))、FEV_(1)/FVC等呼吸功能指标、6 min步行距离变化及慢性阻塞性肺疾病评估测试(CAT)评分变化、改良英国医学研究委员会呼吸困难指数(mMRC)变化、患者治疗前后生活质量(SF-36)评分变化、治疗满意率。结果治疗前,各组患者FPG、2 h PG、HbA1c、FVC、FEV_(1)、FEV_(1)/FVC、6 min步行距离、CAT及mMRC评分、SF-36评分比较,P>0.05,治疗后各组患者FPG、2 h PG、HbA1c、FVC、FEV_(1)、FEV_(1)/FVC、6 min步行距离、CAT及mMRC评分、SF-36评分等指标均改善,观察组患者治疗后FPG、2 h PG、HbA1c、FVC、FEV_(1)、FEV_(1)/FVC、6 min步行距离、CAT及mMRC评分、SF-36评分等指标优于对照组,P<0.05;观察组患者治疗满意率(98.25%)均高于对照组患者(85.96%),P<0.05。结论祝氏降糖对药方有助于稳定COPD合并糖尿病患者病情,患者血糖水平降低,呼吸功能改善,生活质量提升,患者较为认可与满意,值得应用。展开更多
[Objective]The aim was to study cold-resistant indexes and physiological characters of three different cold-resisitant tomato strains selected under natural conditions. [Method]With 3-4 weeks tomato seedlings as teste...[Objective]The aim was to study cold-resistant indexes and physiological characters of three different cold-resisitant tomato strains selected under natural conditions. [Method]With 3-4 weeks tomato seedlings as tested materials,through simulating external environment conditions by the cold treatment in lab,the survival ratio and growth status of seedlings were identified; by studying the morphological change of in vitro leaves after cold treatment and determining the relative conductivity,the cold-resistant degree of different tomato strains was identified and the correlation between conductivity and survival rate was analyzed; the variation of soluble sugar and praline content in plant of tomato was determined under the condition of cold stress. [Result]The results showed that leaf morphological changes,size of conductivity and growth status of different tomato strains after cold treatment have significant differences; the variation of soluble sugar contents in plant has significant differences,while the variation of proline content has no significant differences. [Conclusion]There is a certain correlation between conductivity and survival rate under cold treatment conditions,and plant cold tolerance is related to accumulation of soluble sugar content.展开更多
β-N-Acetyl-D-glucosaminidase (NAGase, EC.3.2.1.52) is chitinolytic enzymes and disintegrate dimmer and trimer a composition of oligomers of N-acetyl-β-D-glucosamine (NAG) into monomer. Prawn (P. vannamei) NAG...β-N-Acetyl-D-glucosaminidase (NAGase, EC.3.2.1.52) is chitinolytic enzymes and disintegrate dimmer and trimer a composition of oligomers of N-acetyl-β-D-glucosamine (NAG) into monomer. Prawn (P. vannamei) NAGase is involved in digestion and molting processes. Some pollutants in seawater affect the enzyme activity causing loss of the biological function of the enzyme, which affects the exuviating shell and threatens the survival of the animal. The effect of formaldehyde on prawn (P. vannamei) β-N-acetyl-D-glucosaminidase activity for the hydrolysis of pNP-NAG has been studied. The results show that formaldehyde, at appropriate concentrations, can lead to reversible inactivation of the enzyme, and the IC50 is estimated to be 1.05mol· L^-1. The inactivation mechanism obtained from Lineweaver-Burk plots shows that the inactivation of the enzyme by formaldehyde belongs to the competitive type. The inactivation kinetics of the enzyme by formaldehyde has been studied using the progress-of-substrate-reaction method described by Tsou, and the rate constants have been determined. The results show that k+0 is much larger than k-0, indicating the free enzyme molecule is fragile in the formaldehyde solution.展开更多
Objective To screen forα-glucosidase inhibitor active compounds in the total saponins of Baibiandou(Lablab Semen Album)based on UHPLC-Q-Exactive Orbitrap MS technology and to evaluate its hypoglycemic activity in viv...Objective To screen forα-glucosidase inhibitor active compounds in the total saponins of Baibiandou(Lablab Semen Album)based on UHPLC-Q-Exactive Orbitrap MS technology and to evaluate its hypoglycemic activity in vivo.Methods Acarbose was used as the positive control,and the median inhibitory concentration(IC50)was used as the evaluation index ofα-glucosidase inhibitory activity to establish an in vitroα-glucosidase inhibition model.Further,UHPLC-Q-Exactive Orbitrap MS technology was used to screen and identify the active compounds ofα-glucosidase inhibitors in the total saponins of Baibiandou(Lablab Semen Album)in order to further verify the activity of the main active monomer and to perform homologous modeling and molecular docking of yeast-derivedα-glucosidase and human-derivedα-glucosidase,while the hypoglycemic activity was evaluated in diabetic mice.Results This study successfully identified 15 compounds with potentialα-glucosidase inhibitory activity,including Chikusetsusaponin IVa,from the total saponins of Baibiandou(Lablab Semen Album).Simultaneously,we verified the activity of the main active monomer Chikusetsusaponin IVa,and showed that it has strongα-glucosidase inhibitory activity.Theα-glucosidase inhibitory concentration IC50 was(565.2±1.026)μg/m L,and the IC50 of acarbose,which was lower than the positive control,was(706.6±1.058)μg/m L.The docking energies of Chikusetsusaponin IVa were–6.1 and–7.7 kcal/mol with yeast-derivedα-glucosidase and human-derivedα-glucosidase molecules,respectively.Both showed strong binding activity,and the levels of alanine aminotransaminase(ALT),aspartate aminotransaminase(AST),UREA,Creatinine(CREA),and cholesterol(CHO)were significantly decreased by Chikusetsusaponin IVa(P<0.05).In addition,it could repair damaged liver and pancreas cells of diabetic mice to some extent.Conclusion This study provides a basis for screeningα-glucosidase inhibitors and structural modifications of the total saponins of Baibiandou(Lablab Semen Album).展开更多
Poly(p-phenylenediamine)/chitosan (PPPDA/Chi) composite was prepared by in situ chemical oxidative polymerization of p-phenylenediamine (PPPDA) into chitosan (Chi) using ammonium persulphate (APS) as an oxidant. PPPDA...Poly(p-phenylenediamine)/chitosan (PPPDA/Chi) composite was prepared by in situ chemical oxidative polymerization of p-phenylenediamine (PPPDA) into chitosan (Chi) using ammonium persulphate (APS) as an oxidant. PPPDA and PPPDA/Chi composite were characterized by FT-IR spectra and SEM before and after copper loading. In batch adsorption method, the maximum removal of copper was experienced when 1 g/L of PPPDA and PPPDA/Chi composite dosages were used at pH 5.0 for PPPDA and 6.0 for PPPDA/Chi composite for 360 min for both sorbents. PPPDA showed adsorption capacity q<sub>e</sub><sup>max</sup> of 650 mg/g whereas its composite achieved q<sub>e</sub><sup>max</sup> of 573 mg/g. The experimental data correlate well with the Freundlich isotherm equation and the pseudo-second order kinetic model. The Cu(II), loaded PPPDA and its composite can be efficiently reused for as many as four cycles. The Cu(II)-loaded sorbents showed high antibacterial efficiency against Gram-positive and Gram-negative bacteria than their unloaded forms.展开更多
In order to improve the wettability and biocompatibility of the poly (butylene terephthalate) non-woven (PBTNW), the method of surface modification is used to graft copolymerization of chitosan (CS) onto the PBT...In order to improve the wettability and biocompatibility of the poly (butylene terephthalate) non-woven (PBTNW), the method of surface modification is used to graft copolymerization of chitosan (CS) onto the PBTNW under alkylpolyglycoside (APG) inducing. The product is thoroughly characterized with the Fourier transform infrared spectroscopy (FrIR), the electron spectroscopy for chemical analysis (ESCA), the thermogravimetric (TG) and the scanning electron microscopy (SEM). It is found that chitosan is successfully grafted onto PBTNW. In addition, the water contact angles, hemolysis tests and cytotoxicity evaluation tests show an improvement in wettability and biocompatihility as a result of graft copolymerization of chitosan. So the CS-grafted PBTNW exhibits greater superiority than the original PBTNW. The CS-grafted PBTNW can be a candidate for blood filter materials and other medical applications.展开更多
Metformin is a kind of biguanide hypoglycemic agent that has been widely used in patients with diabetes mellitus. In clinical practice, whether metformin should be stopped before Fundus fluorescein angiography (FFA)...Metformin is a kind of biguanide hypoglycemic agent that has been widely used in patients with diabetes mellitus. In clinical practice, whether metformin should be stopped before Fundus fluorescein angiography (FFA) remains largely unclear. Some endocrinologists suggest stop metformin before FFA. However, ophthalmologists do not always adopt this opinion in their practice. This situation may lead to disputes between physicians and patients. This article analyzed contrast-induced nephropathy(CIN) and the related contrast agent, as well as the adverse reactions of fluorescein angiography. It pointed out that the discrepancy may be caused by misunderstanding of contrast agents used in FFA. For angiography using iodine contrast agent, metformin must be stopped because of the increased possibility of CIN, while for FFA using fluorescein sodium, no CIN has been reported yet. Therefore, the authors believe FFA is safe for diabetic patients with oral metformin and it is unnecessary to stop metformin before the examination.展开更多
Objective Our objective was to analyze the traditional Chinese medicine(TCM)syndrome and treatment laws of diabetic kidney disease(DKD)and the action mechanism of high-frequency Chinese herbs in the treatment of DKD b...Objective Our objective was to analyze the traditional Chinese medicine(TCM)syndrome and treatment laws of diabetic kidney disease(DKD)and the action mechanism of high-frequency Chinese herbs in the treatment of DKD based on realworldstudy.MethodsThe data of patients with DKD who had been treated in the First Hospital Affiliated to Henan Universityof ChineseMedicine from January1,2014to December 31,2021 were retrospectively analyzed through the hospital information management system.The contents of the cases were statistically analyzed using IBM SPsS Statistics 25 software,and the laws of DKDtreatment were summarized.Network pharmacology and molecular docking were used to analyze the action mechanism of high-frequency Chinese herbs in the treatment of DKD.ResultsThe data of a total of 1,201 patients with DKD were included,involving 72 kinds of TCM syndromes.Nine disease nature elements and six disease location elements were extracted,involving 405 Chinese herbs.The top five high-frequency Chinese herbs were Baizhu(Atractylodis Macrocephalae Rhizoma),Fuling(Poria),Huangqi(Astragali Radix),Chuanxiong(Chuanxiong Rhizoma),and Danshen(Salviae Miltiorrhizae Radix et Rhizoma).Thirty kinds of Chinese herbs with the frequency of≥100 were mainly deficiency-tonifying herbs and blood-activating and stasis-eliminating herbs.The medicinal properties were mainly warm and mild,and the medicinal flavors were sweet and bitter mostly.For the meridian tropism,the main meridian tropism of these herbs is spleen meridian and lung meridian.The clustering method.展开更多
A six-week growth trial was conducted to compare the effects of different feeding strate- gies of dietary immunostimulants on the growth and immunity of white shrimp Litopenaeus vannamei (4.70 ±0.20g). Shrimps ...A six-week growth trial was conducted to compare the effects of different feeding strate- gies of dietary immunostimulants on the growth and immunity of white shrimp Litopenaeus vannamei (4.70 ±0.20g). Shrimps were fed with diet containing glycyrrhizin continuously, containing β -glucan continuously, discontinuously (seven days with diet containing β -gluseven days with diet without -glucan; two days with diet containing β-glucan following five days with diet without -glucan),展开更多
Objective To explore the pharmacological mechanism of active saponin compounds of Tuchao Baibiandouren(Lablab Semen Album fried with earth,TCBBDR)in treating type 2 diabetes(T2DM)using UHPLC-Q-Exactive Orbitrap MS and...Objective To explore the pharmacological mechanism of active saponin compounds of Tuchao Baibiandouren(Lablab Semen Album fried with earth,TCBBDR)in treating type 2 diabetes(T2DM)using UHPLC-Q-Exactive Orbitrap MS and network pharmacology.Methods UHPLC-Q-Exactive Orbitrap MS was used for a qualitative analysis of saponin compounds in TCBBDR.PharmMapper and CTD were used to screen drug active compounds and disease targets,and an active compound-target network was constructed via Cytoscape 3.8.0.Molecular docking was applied with the drug active compounds and key targets using AutoDock Vina 1.1.2,and a trajectory for the molecular dynamics simulation was completed by GROMACS 2019-3.Results Sixteen saponin compounds were identified from TCBBDR,along with 292 saponin compoud targets and 792 T2DM targets.Through Venn analysis of target saponin constituents and T2DM related targets,a total of 91 intersection targets were screened out in the treatment of T2DM with saponin.The mean values of degree,betweenness centrality and closeness centrality were taken as the thresholds to screen out 22 key genes,among which 4 key proteins namely MAPK1,IGF1 EGFR,PIK3R1 were selected in the top 10 key genes.On this basis,the saponin active constituent-target-signaling pathway network was established.The Gene Ontology(GO)enrichment analysis showed that the related biological modules included activity of steroid hormone receptor,steroid binding,and insulin receptor binding,etc.;the related signaling pathways were EGFR,PI3K-Akt and MAPK,etc.;regulating signaling pathways like MAPK could induce the proliferation,inhibition and apoptosis of pancreaticβcells,increase the quantity of pancreaticβcells,improve the functions of pancreaticβcells and stimulate the insulin secretion.Docking experiment analysis showed that all selected saponin compounds could enter the active sites of targets and form 3–14 hydrogen bonds with residues of the active sites.Moreover,van der Waals forces were present between chemical compounds and active sites.By combining the docking binding energy,we determined that the chemical compounds showed strong binding energy to the targets.Conclusion TCBBDR exerts therapeutic effects on diabetes through multi-compound and multi-target collaboration.Specifically,saponin components mediate pathways including inflammatory reaction and signal transduction to treat T2DM by regulating several key proteins that interact with EGFR and a series of signaling pathways related to disease development.展开更多
Convection-enhanced delivery (CED) is a promising technique leveraging pressure-driven flow to increase penetration of infused drugs into interstitial spaces. We have developed a fiberoptic microneedle device for in...Convection-enhanced delivery (CED) is a promising technique leveraging pressure-driven flow to increase penetration of infused drugs into interstitial spaces. We have developed a fiberoptic microneedle device for inducing local sub-lethal hyperthermia to further improve CED drug distribution volumes, and this study seeks to quantitatively characterize this approach in agarose tissue phantoms. Infusions of dye were conducted in 0.6% (w/w) agarose tissue phantoms with isothermal conditions at 15 ℃, 20℃, 25 ℃, and 30 ℃. Infusion metrics were quantified using a custom shadowgraphy setup and image- processing algorithm. These data were used to build an empirical predictive temporal model of distribution volume as a function of phantom temperature. A second set of proof- of-concept experiments was conducted to evaluate a novel fiberoptic device capable of generating local photothermal heating during fluid infusion. The isothermal infusions showed a positive correlation between temperature and distribution volume, with the volume at 30℃ showing a 7-fold increase at 100 min over the 15 ℃ isothermal case. Infusions during photothermal heating (1064 nm at 500 mW) showed a similar effect with a 3.5-fold increase at 4 h over the control (0 mW). These results and analyses serve to provide insight into and characterization of heat-mediated enhancement of volumetric dispersal.展开更多
Chinese shrimp (Fenneropenaeus chinensis) is an economically important aquaculture species in China. However, cytogenetic and genomic data is limited in the organism partly because the chromosomes are difficult to i...Chinese shrimp (Fenneropenaeus chinensis) is an economically important aquaculture species in China. However, cytogenetic and genomic data is limited in the organism partly because the chromosomes are difficult to isolate and analyze. In this study, fluorescence in-situ hybridization (FISH) was used to identify the chromosomes of F. chinensis. The 5S ribosomal RNA gene (rDNA) of F. chinensis was isolated, cloned and then used as a hybridization probe. The results show that the 5S rDNA was located on one pair of homologous chromosomes in F chinensis. In addition, triploid shrimp were used to evaluate the feasibility of chromosome identification using FISH and to validate the method. It was confirmed that 5S rDNA can be used as a chromosome-specific probe for chromosome identification in E chinensis. The successful application ofFISH in E chinensis shows that chromosome-specific probes can be developed and this finding will facilitate further research on the chromosomes ofpenaeid shrimps.展开更多
Effective enantioseparation of Naftopidil and its derivatives by HPLC was accomplished using several different polysaccharide-based chiral stationary phases(CSPs).In normal-phase mode,the compounds were eluted on fo...Effective enantioseparation of Naftopidil and its derivatives by HPLC was accomplished using several different polysaccharide-based chiral stationary phases(CSPs).In normal-phase mode,the compounds were eluted on four coated-and two immobilized-columns with the mixture of n-hexane,isopropanol and diethylamine(DEA).Polysaccharide tris(3,5- dimethylphenyl carbamate) was shown to be the best enantiomer selector.In addition,the immobilized column packed with Chiralpak IA or IB was applied under polar-organic and reversed-phase conditions,both of which exhibited excellent enantioselectivity for Naftopidil and its derivatives.Furthermore,the underlying possible chiral recognition mechanisms were discussed.展开更多
A new procedure for the highly diastereoselective synthesis of (1S)-trans-cyclopropane derivatives using a fructose derivative as the chiral auxiliary was developed. Chloroacetylated 1,2;4,5-di-O-isopropylidene-D-fr...A new procedure for the highly diastereoselective synthesis of (1S)-trans-cyclopropane derivatives using a fructose derivative as the chiral auxiliary was developed. Chloroacetylated 1,2;4,5-di-O-isopropylidene-D-fructopyranose was reacted with a tertiary amine to form the ammonium salt, which was treated with cesium carbonate to give the cyclopropane derivative through ylide intermediate. The described procedure provides an efficient method to synthesize optically pure dior poly-substituded cyclopropanes.展开更多
Six newly synthesized racemic 1-(substituted phenyl)-4-[3-(indole-4-yl-oxy)-2-hydroxypropyl]-piperazine 1-6 were successfully resolved by carbon dioxide supercritical fluid chromatography (SFC) on an analytical ...Six newly synthesized racemic 1-(substituted phenyl)-4-[3-(indole-4-yl-oxy)-2-hydroxypropyl]-piperazine 1-6 were successfully resolved by carbon dioxide supercritical fluid chromatography (SFC) on an analytical scale column packed with immobilized polysaccharide-based chiral stationary phases (CSPs). We found that separation on the Chiralpak IA CSP was superior to the other two immobilized CSPs (Chiralpak IB and Chiralpak IC), and isopropanol (IPA) was a superior modifier compared to the other five solvents including ethanol, methanol, tetrahydrofuran, acetonitrile and dichloromethane. The effects of organic modifier composition, back pressure, and column temperature for enantioseparation of all six compounds were studied. Of the physical parameters studied, modifier composition had the greatest impact on retention. Changing temperature generally had less impact on retention but produced the greatest selectivity changes. The optimum condition was found as follows: Chiralpak IA column, column temperature 35 ~C, back pressure 120 bar, 35% IPA containing 0.1% diethylamine (v/v) in mobile phase, flow rate of mobile phase 3.0 mL/min, UV detection 283 nm. Separation of all six racemic compounds was completed within 10 rain and excellent resolution was obtained. Thus, SFC was found to be the methodology of choice for resolving the enantiomers of this class of compounds.展开更多
OBJECTIVE: To assess the renal protective effects of curcumin administration ondiabetic rats/mice.METHODS: Databases were searched electronically and conference papers searched manually for search terms to find releva...OBJECTIVE: To assess the renal protective effects of curcumin administration ondiabetic rats/mice.METHODS: Databases were searched electronically and conference papers searched manually for search terms to find relevant studies. Articles were assessed independently by two reviewers. Review Manager 5.1 was used fordata analysis.RESULTS: Fourteen randomized controlled experiments were included. Meta-analysis demonstrated that blood sugar levels and kidney weight to body weight ratios in the model group were higher than those in the normal group, and the curcumin group had significantly lower mesangial area to glomerular area ratios compared with the model group, and also lower levels of urinary protein,blood urea nitrogen and serum creatinine.CONCLUSION: Curcumin shows protective effects on the kidneys of rats/mice with diabetes.展开更多
文摘目的观察祝氏降糖对药方对社区慢性阻塞性肺疾病(COPD)合并糖尿病患者血糖水平及呼吸功能影响。方法研究纳入社区收治的114例慢性阻塞性肺疾病合并糖尿病患者(2022年3月—2023年2月收治)作为本次研究对象,以随机数字表法将患者分为观察组与对照组,各组57例,对照组患者给予社区常规疗法,观察组患者在社区常规疗法治疗基础上给予患者祝氏降糖对药方治疗,各组数据观察:治疗前后患者空腹血糖(FPG)及餐后2h血糖(2 h PG)、糖化血红蛋白(HbA1c)指标变化,用力肺活量(FVC)及一秒用力呼气容积(FEV_(1))、FEV_(1)/FVC等呼吸功能指标、6 min步行距离变化及慢性阻塞性肺疾病评估测试(CAT)评分变化、改良英国医学研究委员会呼吸困难指数(mMRC)变化、患者治疗前后生活质量(SF-36)评分变化、治疗满意率。结果治疗前,各组患者FPG、2 h PG、HbA1c、FVC、FEV_(1)、FEV_(1)/FVC、6 min步行距离、CAT及mMRC评分、SF-36评分比较,P>0.05,治疗后各组患者FPG、2 h PG、HbA1c、FVC、FEV_(1)、FEV_(1)/FVC、6 min步行距离、CAT及mMRC评分、SF-36评分等指标均改善,观察组患者治疗后FPG、2 h PG、HbA1c、FVC、FEV_(1)、FEV_(1)/FVC、6 min步行距离、CAT及mMRC评分、SF-36评分等指标优于对照组,P<0.05;观察组患者治疗满意率(98.25%)均高于对照组患者(85.96%),P<0.05。结论祝氏降糖对药方有助于稳定COPD合并糖尿病患者病情,患者血糖水平降低,呼吸功能改善,生活质量提升,患者较为认可与满意,值得应用。
基金Supported by National Key Technology R&D Program of China(2008BADC0B00)Natural Innovation Experiment Program for University students (081035917)International Cooperation Program of Anhui (08080703002)~~
文摘[Objective]The aim was to study cold-resistant indexes and physiological characters of three different cold-resisitant tomato strains selected under natural conditions. [Method]With 3-4 weeks tomato seedlings as tested materials,through simulating external environment conditions by the cold treatment in lab,the survival ratio and growth status of seedlings were identified; by studying the morphological change of in vitro leaves after cold treatment and determining the relative conductivity,the cold-resistant degree of different tomato strains was identified and the correlation between conductivity and survival rate was analyzed; the variation of soluble sugar and praline content in plant of tomato was determined under the condition of cold stress. [Result]The results showed that leaf morphological changes,size of conductivity and growth status of different tomato strains after cold treatment have significant differences; the variation of soluble sugar contents in plant has significant differences,while the variation of proline content has no significant differences. [Conclusion]There is a certain correlation between conductivity and survival rate under cold treatment conditions,and plant cold tolerance is related to accumulation of soluble sugar content.
文摘β-N-Acetyl-D-glucosaminidase (NAGase, EC.3.2.1.52) is chitinolytic enzymes and disintegrate dimmer and trimer a composition of oligomers of N-acetyl-β-D-glucosamine (NAG) into monomer. Prawn (P. vannamei) NAGase is involved in digestion and molting processes. Some pollutants in seawater affect the enzyme activity causing loss of the biological function of the enzyme, which affects the exuviating shell and threatens the survival of the animal. The effect of formaldehyde on prawn (P. vannamei) β-N-acetyl-D-glucosaminidase activity for the hydrolysis of pNP-NAG has been studied. The results show that formaldehyde, at appropriate concentrations, can lead to reversible inactivation of the enzyme, and the IC50 is estimated to be 1.05mol· L^-1. The inactivation mechanism obtained from Lineweaver-Burk plots shows that the inactivation of the enzyme by formaldehyde belongs to the competitive type. The inactivation kinetics of the enzyme by formaldehyde has been studied using the progress-of-substrate-reaction method described by Tsou, and the rate constants have been determined. The results show that k+0 is much larger than k-0, indicating the free enzyme molecule is fragile in the formaldehyde solution.
基金funding support from the Program of the Educational Commission of Hunan Province of China(No.20B418)。
文摘Objective To screen forα-glucosidase inhibitor active compounds in the total saponins of Baibiandou(Lablab Semen Album)based on UHPLC-Q-Exactive Orbitrap MS technology and to evaluate its hypoglycemic activity in vivo.Methods Acarbose was used as the positive control,and the median inhibitory concentration(IC50)was used as the evaluation index ofα-glucosidase inhibitory activity to establish an in vitroα-glucosidase inhibition model.Further,UHPLC-Q-Exactive Orbitrap MS technology was used to screen and identify the active compounds ofα-glucosidase inhibitors in the total saponins of Baibiandou(Lablab Semen Album)in order to further verify the activity of the main active monomer and to perform homologous modeling and molecular docking of yeast-derivedα-glucosidase and human-derivedα-glucosidase,while the hypoglycemic activity was evaluated in diabetic mice.Results This study successfully identified 15 compounds with potentialα-glucosidase inhibitory activity,including Chikusetsusaponin IVa,from the total saponins of Baibiandou(Lablab Semen Album).Simultaneously,we verified the activity of the main active monomer Chikusetsusaponin IVa,and showed that it has strongα-glucosidase inhibitory activity.Theα-glucosidase inhibitory concentration IC50 was(565.2±1.026)μg/m L,and the IC50 of acarbose,which was lower than the positive control,was(706.6±1.058)μg/m L.The docking energies of Chikusetsusaponin IVa were–6.1 and–7.7 kcal/mol with yeast-derivedα-glucosidase and human-derivedα-glucosidase molecules,respectively.Both showed strong binding activity,and the levels of alanine aminotransaminase(ALT),aspartate aminotransaminase(AST),UREA,Creatinine(CREA),and cholesterol(CHO)were significantly decreased by Chikusetsusaponin IVa(P<0.05).In addition,it could repair damaged liver and pancreas cells of diabetic mice to some extent.Conclusion This study provides a basis for screeningα-glucosidase inhibitors and structural modifications of the total saponins of Baibiandou(Lablab Semen Album).
文摘Poly(p-phenylenediamine)/chitosan (PPPDA/Chi) composite was prepared by in situ chemical oxidative polymerization of p-phenylenediamine (PPPDA) into chitosan (Chi) using ammonium persulphate (APS) as an oxidant. PPPDA and PPPDA/Chi composite were characterized by FT-IR spectra and SEM before and after copper loading. In batch adsorption method, the maximum removal of copper was experienced when 1 g/L of PPPDA and PPPDA/Chi composite dosages were used at pH 5.0 for PPPDA and 6.0 for PPPDA/Chi composite for 360 min for both sorbents. PPPDA showed adsorption capacity q<sub>e</sub><sup>max</sup> of 650 mg/g whereas its composite achieved q<sub>e</sub><sup>max</sup> of 573 mg/g. The experimental data correlate well with the Freundlich isotherm equation and the pseudo-second order kinetic model. The Cu(II), loaded PPPDA and its composite can be efficiently reused for as many as four cycles. The Cu(II)-loaded sorbents showed high antibacterial efficiency against Gram-positive and Gram-negative bacteria than their unloaded forms.
文摘In order to improve the wettability and biocompatibility of the poly (butylene terephthalate) non-woven (PBTNW), the method of surface modification is used to graft copolymerization of chitosan (CS) onto the PBTNW under alkylpolyglycoside (APG) inducing. The product is thoroughly characterized with the Fourier transform infrared spectroscopy (FrIR), the electron spectroscopy for chemical analysis (ESCA), the thermogravimetric (TG) and the scanning electron microscopy (SEM). It is found that chitosan is successfully grafted onto PBTNW. In addition, the water contact angles, hemolysis tests and cytotoxicity evaluation tests show an improvement in wettability and biocompatihility as a result of graft copolymerization of chitosan. So the CS-grafted PBTNW exhibits greater superiority than the original PBTNW. The CS-grafted PBTNW can be a candidate for blood filter materials and other medical applications.
基金Supported by the Science Foundation of Xi'an Bureau of PublicHealth (No.2013020) and the Natural Science Foundation of Xi'anScience Technology Bureau (No.SF1508-3).
文摘Metformin is a kind of biguanide hypoglycemic agent that has been widely used in patients with diabetes mellitus. In clinical practice, whether metformin should be stopped before Fundus fluorescein angiography (FFA) remains largely unclear. Some endocrinologists suggest stop metformin before FFA. However, ophthalmologists do not always adopt this opinion in their practice. This situation may lead to disputes between physicians and patients. This article analyzed contrast-induced nephropathy(CIN) and the related contrast agent, as well as the adverse reactions of fluorescein angiography. It pointed out that the discrepancy may be caused by misunderstanding of contrast agents used in FFA. For angiography using iodine contrast agent, metformin must be stopped because of the increased possibility of CIN, while for FFA using fluorescein sodium, no CIN has been reported yet. Therefore, the authors believe FFA is safe for diabetic patients with oral metformin and it is unnecessary to stop metformin before the examination.
基金supported by the National Key Research Project(2020YFE0201800)Henan Province Science and Technology Program for Tackling Key Problems(21210230347)2021 Postgraduate Scientifc Re-search Innovation Progrpm of Henan Universityof Chinese Medicine(2021KYCX008).
文摘Objective Our objective was to analyze the traditional Chinese medicine(TCM)syndrome and treatment laws of diabetic kidney disease(DKD)and the action mechanism of high-frequency Chinese herbs in the treatment of DKD based on realworldstudy.MethodsThe data of patients with DKD who had been treated in the First Hospital Affiliated to Henan Universityof ChineseMedicine from January1,2014to December 31,2021 were retrospectively analyzed through the hospital information management system.The contents of the cases were statistically analyzed using IBM SPsS Statistics 25 software,and the laws of DKDtreatment were summarized.Network pharmacology and molecular docking were used to analyze the action mechanism of high-frequency Chinese herbs in the treatment of DKD.ResultsThe data of a total of 1,201 patients with DKD were included,involving 72 kinds of TCM syndromes.Nine disease nature elements and six disease location elements were extracted,involving 405 Chinese herbs.The top five high-frequency Chinese herbs were Baizhu(Atractylodis Macrocephalae Rhizoma),Fuling(Poria),Huangqi(Astragali Radix),Chuanxiong(Chuanxiong Rhizoma),and Danshen(Salviae Miltiorrhizae Radix et Rhizoma).Thirty kinds of Chinese herbs with the frequency of≥100 were mainly deficiency-tonifying herbs and blood-activating and stasis-eliminating herbs.The medicinal properties were mainly warm and mild,and the medicinal flavors were sweet and bitter mostly.For the meridian tropism,the main meridian tropism of these herbs is spleen meridian and lung meridian.The clustering method.
文摘A six-week growth trial was conducted to compare the effects of different feeding strate- gies of dietary immunostimulants on the growth and immunity of white shrimp Litopenaeus vannamei (4.70 ±0.20g). Shrimps were fed with diet containing glycyrrhizin continuously, containing β -glucan continuously, discontinuously (seven days with diet containing β -gluseven days with diet without -glucan; two days with diet containing β-glucan following five days with diet without -glucan),
基金We thank for the funding support from the Program of Survey of Chinese Medicines of China(No.[2017]66).
文摘Objective To explore the pharmacological mechanism of active saponin compounds of Tuchao Baibiandouren(Lablab Semen Album fried with earth,TCBBDR)in treating type 2 diabetes(T2DM)using UHPLC-Q-Exactive Orbitrap MS and network pharmacology.Methods UHPLC-Q-Exactive Orbitrap MS was used for a qualitative analysis of saponin compounds in TCBBDR.PharmMapper and CTD were used to screen drug active compounds and disease targets,and an active compound-target network was constructed via Cytoscape 3.8.0.Molecular docking was applied with the drug active compounds and key targets using AutoDock Vina 1.1.2,and a trajectory for the molecular dynamics simulation was completed by GROMACS 2019-3.Results Sixteen saponin compounds were identified from TCBBDR,along with 292 saponin compoud targets and 792 T2DM targets.Through Venn analysis of target saponin constituents and T2DM related targets,a total of 91 intersection targets were screened out in the treatment of T2DM with saponin.The mean values of degree,betweenness centrality and closeness centrality were taken as the thresholds to screen out 22 key genes,among which 4 key proteins namely MAPK1,IGF1 EGFR,PIK3R1 were selected in the top 10 key genes.On this basis,the saponin active constituent-target-signaling pathway network was established.The Gene Ontology(GO)enrichment analysis showed that the related biological modules included activity of steroid hormone receptor,steroid binding,and insulin receptor binding,etc.;the related signaling pathways were EGFR,PI3K-Akt and MAPK,etc.;regulating signaling pathways like MAPK could induce the proliferation,inhibition and apoptosis of pancreaticβcells,increase the quantity of pancreaticβcells,improve the functions of pancreaticβcells and stimulate the insulin secretion.Docking experiment analysis showed that all selected saponin compounds could enter the active sites of targets and form 3–14 hydrogen bonds with residues of the active sites.Moreover,van der Waals forces were present between chemical compounds and active sites.By combining the docking binding energy,we determined that the chemical compounds showed strong binding energy to the targets.Conclusion TCBBDR exerts therapeutic effects on diabetes through multi-compound and multi-target collaboration.Specifically,saponin components mediate pathways including inflammatory reaction and signal transduction to treat T2DM by regulating several key proteins that interact with EGFR and a series of signaling pathways related to disease development.
基金the Coulter Foundation and NIH (NIH/NCI 1R21CA156078) for their funding of this project
文摘Convection-enhanced delivery (CED) is a promising technique leveraging pressure-driven flow to increase penetration of infused drugs into interstitial spaces. We have developed a fiberoptic microneedle device for inducing local sub-lethal hyperthermia to further improve CED drug distribution volumes, and this study seeks to quantitatively characterize this approach in agarose tissue phantoms. Infusions of dye were conducted in 0.6% (w/w) agarose tissue phantoms with isothermal conditions at 15 ℃, 20℃, 25 ℃, and 30 ℃. Infusion metrics were quantified using a custom shadowgraphy setup and image- processing algorithm. These data were used to build an empirical predictive temporal model of distribution volume as a function of phantom temperature. A second set of proof- of-concept experiments was conducted to evaluate a novel fiberoptic device capable of generating local photothermal heating during fluid infusion. The isothermal infusions showed a positive correlation between temperature and distribution volume, with the volume at 30℃ showing a 7-fold increase at 100 min over the 15 ℃ isothermal case. Infusions during photothermal heating (1064 nm at 500 mW) showed a similar effect with a 3.5-fold increase at 4 h over the control (0 mW). These results and analyses serve to provide insight into and characterization of heat-mediated enhancement of volumetric dispersal.
基金Supported by the Key Program of the National Natural ScienceFoundation of China(No.30730071)the National High-Tech Researchand Development Program of China(863 program)(No.2007AA09Z430)the General Program of National Natural Science Foundation of China(Nos.30471347&40706048)
文摘Chinese shrimp (Fenneropenaeus chinensis) is an economically important aquaculture species in China. However, cytogenetic and genomic data is limited in the organism partly because the chromosomes are difficult to isolate and analyze. In this study, fluorescence in-situ hybridization (FISH) was used to identify the chromosomes of F. chinensis. The 5S ribosomal RNA gene (rDNA) of F. chinensis was isolated, cloned and then used as a hybridization probe. The results show that the 5S rDNA was located on one pair of homologous chromosomes in F chinensis. In addition, triploid shrimp were used to evaluate the feasibility of chromosome identification using FISH and to validate the method. It was confirmed that 5S rDNA can be used as a chromosome-specific probe for chromosome identification in E chinensis. The successful application ofFISH in E chinensis shows that chromosome-specific probes can be developed and this finding will facilitate further research on the chromosomes ofpenaeid shrimps.
基金Guangzhou mega Projects of Science Research in 2009(Grant No.2009A1-E011-7)
文摘Effective enantioseparation of Naftopidil and its derivatives by HPLC was accomplished using several different polysaccharide-based chiral stationary phases(CSPs).In normal-phase mode,the compounds were eluted on four coated-and two immobilized-columns with the mixture of n-hexane,isopropanol and diethylamine(DEA).Polysaccharide tris(3,5- dimethylphenyl carbamate) was shown to be the best enantiomer selector.In addition,the immobilized column packed with Chiralpak IA or IB was applied under polar-organic and reversed-phase conditions,both of which exhibited excellent enantioselectivity for Naftopidil and its derivatives.Furthermore,the underlying possible chiral recognition mechanisms were discussed.
基金National Natural Science Foundation of China (Grant No. 20602001)
文摘A new procedure for the highly diastereoselective synthesis of (1S)-trans-cyclopropane derivatives using a fructose derivative as the chiral auxiliary was developed. Chloroacetylated 1,2;4,5-di-O-isopropylidene-D-fructopyranose was reacted with a tertiary amine to form the ammonium salt, which was treated with cesium carbonate to give the cyclopropane derivative through ylide intermediate. The described procedure provides an efficient method to synthesize optically pure dior poly-substituded cyclopropanes.
基金Science and Technology Program of Guangzhou City(Grant No.2010U1-E0531-2)
文摘Six newly synthesized racemic 1-(substituted phenyl)-4-[3-(indole-4-yl-oxy)-2-hydroxypropyl]-piperazine 1-6 were successfully resolved by carbon dioxide supercritical fluid chromatography (SFC) on an analytical scale column packed with immobilized polysaccharide-based chiral stationary phases (CSPs). We found that separation on the Chiralpak IA CSP was superior to the other two immobilized CSPs (Chiralpak IB and Chiralpak IC), and isopropanol (IPA) was a superior modifier compared to the other five solvents including ethanol, methanol, tetrahydrofuran, acetonitrile and dichloromethane. The effects of organic modifier composition, back pressure, and column temperature for enantioseparation of all six compounds were studied. Of the physical parameters studied, modifier composition had the greatest impact on retention. Changing temperature generally had less impact on retention but produced the greatest selectivity changes. The optimum condition was found as follows: Chiralpak IA column, column temperature 35 ~C, back pressure 120 bar, 35% IPA containing 0.1% diethylamine (v/v) in mobile phase, flow rate of mobile phase 3.0 mL/min, UV detection 283 nm. Separation of all six racemic compounds was completed within 10 rain and excellent resolution was obtained. Thus, SFC was found to be the methodology of choice for resolving the enantiomers of this class of compounds.
文摘OBJECTIVE: To assess the renal protective effects of curcumin administration ondiabetic rats/mice.METHODS: Databases were searched electronically and conference papers searched manually for search terms to find relevant studies. Articles were assessed independently by two reviewers. Review Manager 5.1 was used fordata analysis.RESULTS: Fourteen randomized controlled experiments were included. Meta-analysis demonstrated that blood sugar levels and kidney weight to body weight ratios in the model group were higher than those in the normal group, and the curcumin group had significantly lower mesangial area to glomerular area ratios compared with the model group, and also lower levels of urinary protein,blood urea nitrogen and serum creatinine.CONCLUSION: Curcumin shows protective effects on the kidneys of rats/mice with diabetes.