The development of 5-aminosalicylic acid (5-ASA) therapy as a life long treatment for ulcerative colitis is reviewed from its origins in the 1940s to the present day. The drug was designed to treat rheumatoid arthriti...The development of 5-aminosalicylic acid (5-ASA) therapy as a life long treatment for ulcerative colitis is reviewed from its origins in the 1940s to the present day. The drug was designed to treat rheumatoid arthritis,but was found helpful in the management of nine patients with ulcerative colitis. This discovery preceded the emergence of the clinical trial as a tool for assessing a new drug's efficacy; as a result it lacked scientific rigour and was selective in its presentation of results. Nevertheless it identified the future cornerstone of therapy in ulcerative colitis. In 1962,the first double blind controlled trial of sulphasalazine was conducted on 40 patients. Outcome measures were subjective and included symptoms and an assessment of the rectal mucosa. In 1973,the first two papers on the role of sulphasalazine in maintenance of remission were published. Both used placebo controls and had a stratified design. Outcomes were measured using "an intention to treat" approach. The British study of 64 patients used both subjective and objective criteria to assess outcomes. Patients on placebo had a relapse rate four times patients on active treatment and this founded the basis for a life long approach to therapy with 5-ASA compounds in ulcerative colitis. However,in 1985,a small "on demand" study of 32 patients suggested this approach might be as effective as continuous treatment. Some support for this view came from an Italian study which showed no benefit to continued treatment for those in remission for two years or more. The central problem these studies identify is that of adherence to treatment in the long-term. Few studies have considered patients' attitudes to continuous therapy and it is an area that needs further investigation.展开更多
A simple and efficient method for the iodination of aromatic compounds has been achieved in the presence of iodine and 1,4- bis（triphenylphosphonium）-2-butene peroxodisulfate.
Objective:To assess the efficacy of compound Bai Yu San(CBYS)as a new treatment option,in healing diabetic skin ulcer.Materials and Methods:A total of 64 diabetic patients with skin ulcer were enrolled and randomly as...Objective:To assess the efficacy of compound Bai Yu San(CBYS)as a new treatment option,in healing diabetic skin ulcer.Materials and Methods:A total of 64 diabetic patients with skin ulcer were enrolled and randomly assigned to experimental group(n=33)and control group(n=31).In the control group,normal saline(NS)was used to cleanse the wound.After debridement,the wound was dressed with modern materials.In the experimental group,the NS‑cleansed wound was dressed with CBYS.The infection rate,healing rate,treatment cost,and patient satisfaction between the two groups were compared.Results:On the 35th day after treatment,the infection rate and healing rate showed no between‑group difference(P>0.05);the experimental group showed lower treatment cost and higher satisfaction than the control group(P<0.05).Conclusion:As a new treatment option for diabetes‑induced skin ulcer,CBYS can effectively control the infection,promote the healing,reduce treatment cost,and increase patient satisfaction.Dressing with CBYS can be clinically replicated in the treatment of diabetic skin ulcer.展开更多
AIM： To investigate EP4-selective agonist effect on indomethacin-induced gastric lesions and on the spontaneous healing of chronic gastric ulcers. METHODS： In a mouse model of gastric bleeding with high dose of indo...AIM： To investigate EP4-selective agonist effect on indomethacin-induced gastric lesions and on the spontaneous healing of chronic gastric ulcers. METHODS： In a mouse model of gastric bleeding with high dose of indomethacin （20 mg/kg）, an EP4-selective agonist was administered orally. Stomach lesions and gastric mucous regeneration were monitored. In a mouse model of chronic gastric ulcer induced by acetic acid, EP4 agonist effect on the healing of chronic gastric ulcer was evaluated in the presence or absence of low dose indomethadn （3 mg/kg）. In cultured human gastric mucous cells, EP4 agonist effect on indomethacin- induced apoptosis was assessed by flow cytometry. RESULTS： The EP4-selective agonist reduced high dose indomethacin-induced acute hemorrhagic damage and promoted mucous epithelial regeneration. Low-dose indomethacin aggravated ulcer bleeding and inflammation, and delayed the healing of the established chronic gastric ulcer. The EP4 agonist, when applied locally, not only offset indomethacin-induced gastric bleeding and inflammation, but also accelerated ulcer healing. In the absence of indomethacin, the EP4 agonist even accelerated chronic gastric ulcer healing and suppressed inflammatory cell infiltration in the granulation tissue. In vitro, the EP4 agonist protected human gastric mucous cells from indomethacin-induced apoptosis.CONCLUSION： EP4-selective agonist may prevent indomethacin-induced gastric lesions and promote healing of existing and i ulcers, via promoting mucous epithelial cells. proliferation and survival of mucous epithelial cells.展开更多
Substituting effects of Nd for La in La 0.5 Ba 0.5 CoO 3 compounds were studied systematically. The results show that Nd doping does not change the itinerant properties of the Co3d electrons. The molecular ma...Substituting effects of Nd for La in La 0.5 Ba 0.5 CoO 3 compounds were studied systematically. The results show that Nd doping does not change the itinerant properties of the Co3d electrons. The molecular magnetic moment of the materials decreases monotonically with increasing Nd dopant. When Nd content x ≥0.45, a magnetic phase separation appears in the materials. When x ≤0.45, the Curie temperature decreases monotonically with increasing Nd dopant. This is due to the size effects of the rare earth ions. The electric resistance measurements show that in the studied temperature range, the conduction of the materials belongs to the thermo diffusion conduction below the Curie temperature, while it belongs to the variable range hopping conduction of polarons over the Curie temperature.展开更多
A novel supramolecular compound,{[2-（2-pyridyl）benzimidazoleH2]2·[BiCl6]·Cl},was synthesized by the hydrothermal reaction of o-phenylenediamine and α-pyridinecarboxylic acid with BiCl3 in 6.0 mol·L-1...A novel supramolecular compound,{[2-（2-pyridyl）benzimidazoleH2]2·[BiCl6]·Cl},was synthesized by the hydrothermal reaction of o-phenylenediamine and α-pyridinecarboxylic acid with BiCl3 in 6.0 mol·L-1 HCl solution,and characterized by elemental analysis,IR,X-ray single-crystal diffraction and photoluminescence spectroscopy.The crystal （C24H22N6Cl7Bi,Mr= 851.61） belongs to the triclinic system,space group P1 with a =7.2887（18）,b =9.548（2）,c= 12.469（3）,α=85.306（4）,β=82.814（4）,γ=71.349（4）°,Z=1,V=814.9（3）3,Dc=1.735 g/cm3,μ（MoKα）=6.007 mm-1,F（000）=410,R=0.0307 and wR=0.0787.The bismuth ion and six chlorine ions construct a distorted octahedral configuration.The three-dimensional supramolecular network is built from electrostatic attractions,hydrogen bonds and π-π interaction between the BiCl6 anion,Cl anion and [2-（2-pyridyl）benzimidazoleH2] cation.The photoluminescence spectroscopy study shows that the title compound has a blue fluorescent emission at 450 nm in the solid state.展开更多
目的 基于现代科学技术对四妙勇安汤进行改良,验证其促进糖尿病足伤口愈合的效果。方法 采用乙氧二羟丁酮辅助的单链DNA测序(kethoxal-assisted single stranded DNA sequencing, KAS-seq)技术检测糖尿病足患者创面组织和正常创面组织,...目的 基于现代科学技术对四妙勇安汤进行改良,验证其促进糖尿病足伤口愈合的效果。方法 采用乙氧二羟丁酮辅助的单链DNA测序(kethoxal-assisted single stranded DNA sequencing, KAS-seq)技术检测糖尿病足患者创面组织和正常创面组织,筛选糖尿病足相关的关键基因,并结合网络药理学,根据这些关键基因寻找有针对性的中药从而对四妙勇安汤进行改良,最后通过糖尿病足动物模型验证改良方的治疗效果。结果 通过临床样本测序分析得到CREB1、GRID2、PIK3R3、DRD2、ADORA1、TNFSF11、EDNRB、HTR1B 8个关键基因,靶向到黄柏、苍术、地黄和半夏4味中药配伍入原方。在灌胃干预第7天时改良方组(S+)小鼠伤口愈合效率显著高于对照组(Control)(P<0.05),第12天时S+组伤口愈合率显著高于原方组(S)(P<0.05)。改良方中药靶点在原方基础上更多富集到了神经系统、缺氧和血液循环调节相关通路中。结论 改良方与经方相比具有更好地促进糖尿病足伤口愈合的效果,相关机制可能与调节炎性反应、改善周围神经病变和促进伤口愈合等通路有关,同时也为中药方剂的临床加减应用提供了一种新方法和现代科学理论依据。展开更多
Intestinal macrophages are essential players in intestinal inflammation and intestinal immune homeostasis.Intestinal macrophages have the ability to polarize into two distinct phenotypes based on various environmental...Intestinal macrophages are essential players in intestinal inflammation and intestinal immune homeostasis.Intestinal macrophages have the ability to polarize into two distinct phenotypes based on various environmental signals.These phenotypes include the typically activated pro-inflammatory M1 phenotype and the alternatively activated anti-inflammatory M2 phenotype.Under normal circumstances,intestinal macrophages prevent inflammatory damage to the gut.However,when genetic and environmental factors influence the polarization of intestinal macrophages,it can lead to an imbalance in M1/M2 macrophage activation and subsequently an imbalance in the control of intestinal inflammation.It transforms physiological inflammation into pathological intestinal damage.In patients with ulcerative colitis-associated cancer(UC-CRC),intestinal inflammatory disorders are closely associated with intestinal M1/M2 macrophage polarization imbalance.Consequently,restoring the polarization equilibrium of M1/M2 macrophages might be an evidence of traditional Chinese medicine in the treatment of UC-CRC,the pivotal role o effective measure to prevent and treat UC-CRC.This paper aims to examine the clinicalf macrophage polarization in UC-CRC pathogenesis,and the potential mechanisms of traditional Chinese medicine in regulating macrophage polarization to treat UC-CRC.Our goal is to provide novel insights into the clinical practice,basic research,and drug development of UC-CRC.展开更多
The quantitative structure-activity relationship （QSAR） of 16 pyrazole compounds was studied by ab initio method at the HF/3-21G level using Guassian03 soft. The optimized structures together with some characteristi...The quantitative structure-activity relationship （QSAR） of 16 pyrazole compounds was studied by ab initio method at the HF/3-21G level using Guassian03 soft. The optimized structures together with some characteristic and electric parameters of the title compounds were obtained; some stereo-parameters were calculated by HyperChem software. Stepwise multiple regression method was adopted to establish bi- and tri-parametric models between biological activity and some parameters. The lager △E and logP, the higher biological activity; and the biological activity would be promoted with the smaller μ, QN and QPYRA. It provided a theory direction to synthesize some compounds with high activity.展开更多
Objective:To systematically evaluate the efficacy and safety of Compound Stomachache Capsule(复方胃痛胶囊)in the treatment of digestive ulcer and inflammation Helicobacter pylori-Peptic Ulcer(Hp-PU)caused by Helicobac...Objective:To systematically evaluate the efficacy and safety of Compound Stomachache Capsule(复方胃痛胶囊)in the treatment of digestive ulcer and inflammation Helicobacter pylori-Peptic Ulcer(Hp-PU)caused by Helicobacter pylori(Hp).Methods:Randomized controlled trials(RCTs)of Compound Stomachache Capsule(复方胃痛胶囊)in the treatment of Hp-PU were screened out by searching CNKI,VIP,Wanfang,China Biomedical Literature Service System,Cochrane Library,Pub Med,EMbase,Web of Science and Clinical Trials.gov.Meta-analysis was performed with Rev Man 5.4 software.Results:Three RCTs were included,including 331 patients of 166 patients in the experimental group(Compound Stomachache Capsule(复方胃痛胶囊)+conventional western medicine treatment)and 165 patients in the control group(conventional western medicine treatment).Meta-analysis data showed that Hp eradication rate(RR=1.10,95%CI[1.01-1.19],P=0.03)was significantly higher in the experimental group than in the control group.The experimental group was superior to the control group in improving clinical symptoms(RR=1.59,95%CI[1.22-2.06],P=0.0006).Conclusion:According to the current evidence,the Compound Stomachache Capsule(复方胃痛胶囊)combined with conventional Western medicine treatment can improve the Hp eradication rate of Hp-PU,relieve symptoms,and do not increase the incidence of adverse reactions.However,the number of included studies is small and the sample size is small,so its effectiveness and safety need further verification.展开更多
文摘The development of 5-aminosalicylic acid (5-ASA) therapy as a life long treatment for ulcerative colitis is reviewed from its origins in the 1940s to the present day. The drug was designed to treat rheumatoid arthritis,but was found helpful in the management of nine patients with ulcerative colitis. This discovery preceded the emergence of the clinical trial as a tool for assessing a new drug's efficacy; as a result it lacked scientific rigour and was selective in its presentation of results. Nevertheless it identified the future cornerstone of therapy in ulcerative colitis. In 1962,the first double blind controlled trial of sulphasalazine was conducted on 40 patients. Outcome measures were subjective and included symptoms and an assessment of the rectal mucosa. In 1973,the first two papers on the role of sulphasalazine in maintenance of remission were published. Both used placebo controls and had a stratified design. Outcomes were measured using "an intention to treat" approach. The British study of 64 patients used both subjective and objective criteria to assess outcomes. Patients on placebo had a relapse rate four times patients on active treatment and this founded the basis for a life long approach to therapy with 5-ASA compounds in ulcerative colitis. However,in 1985,a small "on demand" study of 32 patients suggested this approach might be as effective as continuous treatment. Some support for this view came from an Italian study which showed no benefit to continued treatment for those in remission for two years or more. The central problem these studies identify is that of adherence to treatment in the long-term. Few studies have considered patients' attitudes to continuous therapy and it is an area that needs further investigation.
文摘A simple and efficient method for the iodination of aromatic compounds has been achieved in the presence of iodine and 1,4- bis（triphenylphosphonium）-2-butene peroxodisulfate.
基金Jiangsu TCM Bureau Project(YB2015043)Jiangsu Science and Technology Department Project(BK20161606).
文摘Objective:To assess the efficacy of compound Bai Yu San(CBYS)as a new treatment option,in healing diabetic skin ulcer.Materials and Methods:A total of 64 diabetic patients with skin ulcer were enrolled and randomly assigned to experimental group(n=33)and control group(n=31).In the control group,normal saline(NS)was used to cleanse the wound.After debridement,the wound was dressed with modern materials.In the experimental group,the NS‑cleansed wound was dressed with CBYS.The infection rate,healing rate,treatment cost,and patient satisfaction between the two groups were compared.Results:On the 35th day after treatment,the infection rate and healing rate showed no between‑group difference(P>0.05);the experimental group showed lower treatment cost and higher satisfaction than the control group(P<0.05).Conclusion:As a new treatment option for diabetes‑induced skin ulcer,CBYS can effectively control the infection,promote the healing,reduce treatment cost,and increase patient satisfaction.Dressing with CBYS can be clinically replicated in the treatment of diabetic skin ulcer.
文摘AIM： To investigate EP4-selective agonist effect on indomethacin-induced gastric lesions and on the spontaneous healing of chronic gastric ulcers. METHODS： In a mouse model of gastric bleeding with high dose of indomethacin （20 mg/kg）, an EP4-selective agonist was administered orally. Stomach lesions and gastric mucous regeneration were monitored. In a mouse model of chronic gastric ulcer induced by acetic acid, EP4 agonist effect on the healing of chronic gastric ulcer was evaluated in the presence or absence of low dose indomethadn （3 mg/kg）. In cultured human gastric mucous cells, EP4 agonist effect on indomethacin- induced apoptosis was assessed by flow cytometry. RESULTS： The EP4-selective agonist reduced high dose indomethacin-induced acute hemorrhagic damage and promoted mucous epithelial regeneration. Low-dose indomethacin aggravated ulcer bleeding and inflammation, and delayed the healing of the established chronic gastric ulcer. The EP4 agonist, when applied locally, not only offset indomethacin-induced gastric bleeding and inflammation, but also accelerated ulcer healing. In the absence of indomethacin, the EP4 agonist even accelerated chronic gastric ulcer healing and suppressed inflammatory cell infiltration in the granulation tissue. In vitro, the EP4 agonist protected human gastric mucous cells from indomethacin-induced apoptosis.CONCLUSION： EP4-selective agonist may prevent indomethacin-induced gastric lesions and promote healing of existing and i ulcers, via promoting mucous epithelial cells. proliferation and survival of mucous epithelial cells.
文摘Substituting effects of Nd for La in La 0.5 Ba 0.5 CoO 3 compounds were studied systematically. The results show that Nd doping does not change the itinerant properties of the Co3d electrons. The molecular magnetic moment of the materials decreases monotonically with increasing Nd dopant. When Nd content x ≥0.45, a magnetic phase separation appears in the materials. When x ≤0.45, the Curie temperature decreases monotonically with increasing Nd dopant. This is due to the size effects of the rare earth ions. The electric resistance measurements show that in the studied temperature range, the conduction of the materials belongs to the thermo diffusion conduction below the Curie temperature, while it belongs to the variable range hopping conduction of polarons over the Curie temperature.
基金Supported by the Natural Science Foundation of Henan Province (No. 0611023700)
文摘A novel supramolecular compound,{[2-（2-pyridyl）benzimidazoleH2]2·[BiCl6]·Cl},was synthesized by the hydrothermal reaction of o-phenylenediamine and α-pyridinecarboxylic acid with BiCl3 in 6.0 mol·L-1 HCl solution,and characterized by elemental analysis,IR,X-ray single-crystal diffraction and photoluminescence spectroscopy.The crystal （C24H22N6Cl7Bi,Mr= 851.61） belongs to the triclinic system,space group P1 with a =7.2887（18）,b =9.548（2）,c= 12.469（3）,α=85.306（4）,β=82.814（4）,γ=71.349（4）°,Z=1,V=814.9（3）3,Dc=1.735 g/cm3,μ（MoKα）=6.007 mm-1,F（000）=410,R=0.0307 and wR=0.0787.The bismuth ion and six chlorine ions construct a distorted octahedral configuration.The three-dimensional supramolecular network is built from electrostatic attractions,hydrogen bonds and π-π interaction between the BiCl6 anion,Cl anion and [2-（2-pyridyl）benzimidazoleH2] cation.The photoluminescence spectroscopy study shows that the title compound has a blue fluorescent emission at 450 nm in the solid state.
基金This work was supported by the National Natural Science Foundation of China(No.82274600,No.81774451 and No.82104501)the Natural Science Foundation of Guangdong Province(No.2017A030313827)+1 种基金The Basic and Applied Basic Research Project of Guangzhou Municipal Science and Technology Bureau(No.202102080485)Science and Technology Innovation Special Topic of Maoming City(No.2022S014).
文摘Intestinal macrophages are essential players in intestinal inflammation and intestinal immune homeostasis.Intestinal macrophages have the ability to polarize into two distinct phenotypes based on various environmental signals.These phenotypes include the typically activated pro-inflammatory M1 phenotype and the alternatively activated anti-inflammatory M2 phenotype.Under normal circumstances,intestinal macrophages prevent inflammatory damage to the gut.However,when genetic and environmental factors influence the polarization of intestinal macrophages,it can lead to an imbalance in M1/M2 macrophage activation and subsequently an imbalance in the control of intestinal inflammation.It transforms physiological inflammation into pathological intestinal damage.In patients with ulcerative colitis-associated cancer(UC-CRC),intestinal inflammatory disorders are closely associated with intestinal M1/M2 macrophage polarization imbalance.Consequently,restoring the polarization equilibrium of M1/M2 macrophages might be an evidence of traditional Chinese medicine in the treatment of UC-CRC,the pivotal role o effective measure to prevent and treat UC-CRC.This paper aims to examine the clinicalf macrophage polarization in UC-CRC pathogenesis,and the potential mechanisms of traditional Chinese medicine in regulating macrophage polarization to treat UC-CRC.Our goal is to provide novel insights into the clinical practice,basic research,and drug development of UC-CRC.
基金talents in University (NCET-04-0649)the Natural Science Foundation of Shandong Province (Y2006B07, Z2006B01)
文摘The quantitative structure-activity relationship （QSAR） of 16 pyrazole compounds was studied by ab initio method at the HF/3-21G level using Guassian03 soft. The optimized structures together with some characteristic and electric parameters of the title compounds were obtained; some stereo-parameters were calculated by HyperChem software. Stepwise multiple regression method was adopted to establish bi- and tri-parametric models between biological activity and some parameters. The lager △E and logP, the higher biological activity; and the biological activity would be promoted with the smaller μ, QN and QPYRA. It provided a theory direction to synthesize some compounds with high activity.
基金National Key R&D Plan"Research on Modernization of Traditional Chinese Medicine"(2018YFC1707400)。
文摘Objective:To systematically evaluate the efficacy and safety of Compound Stomachache Capsule(复方胃痛胶囊)in the treatment of digestive ulcer and inflammation Helicobacter pylori-Peptic Ulcer(Hp-PU)caused by Helicobacter pylori(Hp).Methods:Randomized controlled trials(RCTs)of Compound Stomachache Capsule(复方胃痛胶囊)in the treatment of Hp-PU were screened out by searching CNKI,VIP,Wanfang,China Biomedical Literature Service System,Cochrane Library,Pub Med,EMbase,Web of Science and Clinical Trials.gov.Meta-analysis was performed with Rev Man 5.4 software.Results:Three RCTs were included,including 331 patients of 166 patients in the experimental group(Compound Stomachache Capsule(复方胃痛胶囊)+conventional western medicine treatment)and 165 patients in the control group(conventional western medicine treatment).Meta-analysis data showed that Hp eradication rate(RR=1.10,95%CI[1.01-1.19],P=0.03)was significantly higher in the experimental group than in the control group.The experimental group was superior to the control group in improving clinical symptoms(RR=1.59,95%CI[1.22-2.06],P=0.0006).Conclusion:According to the current evidence,the Compound Stomachache Capsule(复方胃痛胶囊)combined with conventional Western medicine treatment can improve the Hp eradication rate of Hp-PU,relieve symptoms,and do not increase the incidence of adverse reactions.However,the number of included studies is small and the sample size is small,so its effectiveness and safety need further verification.
