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Novel semicarbazide-sensitive amine oxidase inhibitor screening from anti-obesity drugs using HPLC-MS based technique
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作者 车宝泉 王琳 +2 位作者 张永谦 肖盛元 邓玉林 《Journal of Beijing Institute of Technology》 EI CAS 2013年第1期135-142,共8页
Semicarbazide-sensitive the metabolism of glucose and fat, amine oxidase (SSAO) has been considered to be associated with and elevated SSAO activity was observed in obese patients. In the present study, an in vitro ... Semicarbazide-sensitive the metabolism of glucose and fat, amine oxidase (SSAO) has been considered to be associated with and elevated SSAO activity was observed in obese patients. In the present study, an in vitro SSAO activity-based method was developed to screen inhibitors from 15 an- ti-obesity drugs. Among the fifteen anti-obesity drugs, four drugs including caffeine, fenfluramine, bumetanide and amfebutamone inhibited SSAO activity, and caffeine was the most effective one. When the concentration of caffeine was 1.4 mmol/L, the inhibition ratio was 31.9% and 18.8% in rabbit serum and rat adipose tissue, respectively. Inhibition of SSAO activity by caffeine was also confirmed in the in vivo study, showing the inhibition ratio of 15.6% on serum SSAO. Caffeine pro- vides a natural source of inhibition of SSAO activity and may be a promising inhibitor for the study of SSAO. 展开更多
关键词 anti-obesity drugs CAFFEINE enzyme inhibition HPLC-MS semicarbazide-sensitive a-mine oxidase
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Rise and fall of anti-obesity drugs 被引量:7
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作者 Bernard MY Cheung 《World Journal of Diabetes》 SCIE CAS 2011年第2期19-23,共5页
Although it is not generally a life-threatening disease,obesity is becoming a major health problem worldwide.It can be controlled by means of drugs,and,consequently,these are required to be safe as well as effective.I... Although it is not generally a life-threatening disease,obesity is becoming a major health problem worldwide.It can be controlled by means of drugs,and,consequently,these are required to be safe as well as effective.In this paper,we summarize the fate of various drugs that have been introduced for clinical use in the treatment of obesity.Fenfluramine and dexfenfluramine were withdrawn because of heart valve damage.Sibutramine suppresses appetite and increases heart rate and blood pressure.In the Sibutramine Cardiovascular OUTcomes trial,an increase in major adverse cardiovascular events prompted its withdrawal in Europe and the United States.Rimonabant is an endocannabinoid receptor antagonist that reduces body weight and ameliorates some cardiovascular risk factors.However,adverse psychiatric side effects led to its withdrawal as well.Orlistat is approved in Europe and the United States for the treatment of obesity,but its use is limited by gastrointestinal side-effects.Ephedrine and caffeine are natural ingredients in foods and supplements that may help the person to lose weight.In the light of several failed attempts,there is a clear need to develop drugs that are effective and safe in the long term in order to successfully combat the phenomenon of obesity. 展开更多
关键词 OBESITY anti-obesity drugs SIBUTRAMINE RIMONABANT ORLISTAT
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Anti-obesity drugs currently used and new compounds in clinical development
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作者 Armindo Martins Sandra Morgado Manuel Morgado 《World Journal of Meta-Analysis》 2014年第4期135-153,共19页
Obesity is a chronic disease which requires treatment. As lifestyle interventions alone hardly ever result in long-term weight loss, pharmacotherapy is an impor-tant adjunct to lifestyle measures to improve the induc-... Obesity is a chronic disease which requires treatment. As lifestyle interventions alone hardly ever result in long-term weight loss, pharmacotherapy is an impor-tant adjunct to lifestyle measures to improve the induc-tion and maintenance of weight loss. Owing to the lim-ited options currently available for the pharmacological treatment of obesity, it is imperative to develop new safe compounds. This study aims to review the current medications approved by European Medicines Agency and United States Food and Drug Administration (FDA) for the treatment of obesity, focusing essentially on their benefits and risks, as well as on the new drugs which are presently under clinical trials. Moreover, it lists the anti-obesity agents that have been recently withdrawn from the market. A revision of the scientifc literature was carried out, through a search on Pubmedfor papers published from January 2010 to January2013. Orlistat (Xenical?) is currently the only long-termpharmacotherapy for obesity available in the Europeanmarket, as rimonabant and sibutramine were with-drawn in 2008 and 2010, respectively, due to serious psychiatric and cardiovascular adverse effects. Lorca-serin (Belviq?) and the association of phentermine and topiramate (QsymiaTM) were recently approved by FDA. Orlistat suppresses appetite inhibiting gastrointestinal lipase, being its adverse effects mostly gastrointestinal. Lorcaserin activates 5-HT2C receptors, phentermine is a norepinephrine releasing drug, and topiramate is an anticonvulsivant drug with weight loss properties. 展开更多
关键词 OBESITY Weight loss Pharmacological treatment European Medicines Agency Food and drug Administration Clinical trials
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Recognition and quality mapping of traditional herbal drugs:way forward towards artificial intelligence
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作者 Sanyam Sharma Subh Naman Ashish Baldi 《Traditional Medicine Research》 2025年第1期12-26,共15页
The use of traditional herbal drugs derived from natural sources is on the rise due to their minimal side effects and numerous health benefits.However,a major limitation is the lack of standardized knowledge for ident... The use of traditional herbal drugs derived from natural sources is on the rise due to their minimal side effects and numerous health benefits.However,a major limitation is the lack of standardized knowledge for identifying and mapping the quality of these herbal medicines.This article aims to provide practical insights into the application of artificial intelligence for quality-based commercialization of raw herbal drugs.It focuses on feature extraction methods,image processing techniques,and the preparation of herbal images for compatibility with machine learning models.The article discusses commonly used image processing tools such as normalization,slicing,cropping,and augmentation to prepare images for artificial intelligence-based models.It also provides an overview of global herbal image databases and the models employed for herbal plant/drug identification.Readers will gain a comprehensive understanding of the potential application of various machine learning models,including artificial neural networks and convolutional neural networks.The article delves into suitable validation parameters like true positive rates,accuracy,precision,and more for the development of artificial intelligence-based identification and authentication techniques for herbal drugs.This article offers valuable insights and a conclusive platform for the further exploration of artificial intelligence in the field of herbal drugs,paving the way for smarter identification and authentication methods. 展开更多
关键词 artificial intelligence AYURVEDA machine learning models herbal drugs image pre-processing medicinal plants
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Peptide drugs: a new direction in cancer immunotherapy 被引量:1
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作者 Xinghua Sui Xiaoshuang Niu +1 位作者 Xiuman Zhou Yanfeng Gao 《Cancer Biology & Medicine》 SCIE CAS CSCD 2024年第3期198-203,共6页
Cancer immunotherapy has emerged as a promising approach in cancer treatment and is considered a major advancement after surgical interventions, radiotherapy, chemotherapy, and targeted therapy. The clinical use of im... Cancer immunotherapy has emerged as a promising approach in cancer treatment and is considered a major advancement after surgical interventions, radiotherapy, chemotherapy, and targeted therapy. The clinical use of immunotherapeutic drugs, particularly antibody-based drugs that target immune checkpoints, has notably increased~1. 展开更多
关键词 drugs IMMUNOTHERAPY CANCER
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Prediction of treatment response to antipsychotic drugs for precision medicine approach to schizophrenia:randomized trials and multiomics analysis 被引量:1
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作者 Liang-Kun Guo Yi Su +24 位作者 Yu-Ya-Nan Zhang Hao Yu Zhe Lu Wen-Qiang Li Yong-Feng Yang Xiao Xiao Hao Yan Tian-Lan Lu Jun Li Yun-Dan Liao Zhe-Wei Kang Li-Fang Wang Yue Li Ming Li Bing Liu Hai-Liang Huang Lu-Xian Lv Yin Yao Yun-Long Tan Gerome Breen Ian Everall Hong-Xing Wang Zhuo Huang Dai Zhang Wei-Hua Yue 《Military Medical Research》 SCIE CAS CSCD 2024年第1期19-33,共15页
Background:Choosing the appropriate antipsychotic drug(APD)treatment for patients with schizophrenia(SCZ)can be challenging,as the treatment response to APD is highly variable and difficult to predict due to the lack ... Background:Choosing the appropriate antipsychotic drug(APD)treatment for patients with schizophrenia(SCZ)can be challenging,as the treatment response to APD is highly variable and difficult to predict due to the lack of effective biomarkers.Previous studies have indicated the association between treatment response and genetic and epigenetic factors,but no effective biomarkers have been identified.Hence,further research is imperative to enhance precision medicine in SCZ treatment.Methods:Participants with SCZ were recruited from two randomized trials.The discovery cohort was recruited from the CAPOC trial(n=2307)involved 6 weeks of treatment and equally randomized the participants to the Olanzapine,Risperidone,Quetiapine,Aripiprazole,Ziprasidone,and Haloperidol/Perphenazine(subsequently equally assigned to one or the other)groups.The external validation cohort was recruited from the CAPEC trial(n=1379),which involved 8 weeks of treatment and equally randomized the participants to the Olanzapine,Risperidone,and Aripiprazole groups.Additionally,healthy controls(n=275)from the local community were utilized as a genetic/epigenetic reference.The genetic and epigenetic(DNA methylation)risks of SCZ were assessed using the polygenic risk score(PRS)and polymethylation score,respectively.The study also examined the genetic-epigenetic interactions with treatment response through differential methylation analysis,methylation quantitative trait loci,colocalization,and promoteranchored chromatin interaction.Machine learning was used to develop a prediction model for treatment response,which was evaluated for accuracy and clinical benefit using the area under curve(AUC)for classification,R^(2) for regression,and decision curve analysis.Results:Six risk genes for SCZ(LINC01795,DDHD2,SBNO1,KCNG2,SEMA7A,and RUFY1)involved in cortical morphology were identified as having a genetic-epigenetic interaction associated with treatment response.The developed and externally validated prediction model,which incorporated clinical information,PRS,genetic risk score(GRS),and proxy methylation level(proxyDNAm),demonstrated positive benefits for a wide range of patients receiving different APDs,regardless of sex[discovery cohort:AUC=0.874(95%CI 0.867-0.881),R^(2)=0.478;external validation cohort:AUC=0.851(95%CI 0.841-0.861),R^(2)=0.507].Conclusions:This study presents a promising precision medicine approach to evaluate treatment response,which has the potential to aid clinicians in making informed decisions about APD treatment for patients with SCZ.Trial registration Chinese Clinical Trial Registry(https://www.chictr.org.cn/),18 Aug 2009 retrospectively registered:CAPOC-ChiCTR-RNC-09000521(https://www.chictr.org.cn/showproj.aspx?proj=9014),CAPEC-ChiCTRRNC-09000522(https://www.chictr.org.cn/showproj.aspx?proj=9013). 展开更多
关键词 SCHIZOPHRENIA Antipsychotic drug Treatment response Prediction model GENETICS EPIGENETICS
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Systematic review and network meta-analysis of different nonsteroidal anti-inflammatory drugs for juvenile idiopathic arthritis 被引量:2
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作者 Tao Zeng Jian-Zhong Ye +1 位作者 Hui Qin Qian-Qian Xu 《World Journal of Clinical Cases》 SCIE 2024年第12期2056-2064,共9页
BACKGROUND Various non-steroidal anti-inflammatory drugs(NSAIDs)have been used for juvenile idiopathic arthritis(JIA).However,the optimal method for JIA has not yet been developed.AIM To perform a systematic review an... BACKGROUND Various non-steroidal anti-inflammatory drugs(NSAIDs)have been used for juvenile idiopathic arthritis(JIA).However,the optimal method for JIA has not yet been developed.AIM To perform a systematic review and network meta-analysis to determine the optimal instructions.METHODS We searched for randomized controlled trials(RCTs)from PubMed,EMBASE,Google Scholar,CNKI,and Wanfang without restriction for publication date or language at August,2023.Any RCTs that comparing the effectiveness of NSAIDs with each other or placebo for JIA were included in this network meta-analysis.The surface under the cumulative ranking curve(SUCRA)analysis was used to rank the treatments.P value less than 0.05 was identified as statistically significant.RESULTS We included 8 RCTs(1127 patients)comparing 8 different instructions including meloxicam(0.125 qd and 0.250 qd),Celecoxib(3 mg/kg bid and 6 mg/kg bid),piroxicam,Naproxen(5.0 mg/kg/d,7.5 mg/kg/d and 12.5 mg/kg/d),inuprofen(30-40 mg/kg/d),Aspirin(60-80 mg/kg/d,75 mg/kg/d,and 55 mg/kg/d),Tolmetin(15 mg/kg/d),Rofecoxib,and placebo.There were no significant differences between any two NSAIDs regarding ACR Pedi 30 response.The SUCRA shows that celecoxib(6 mg/kg bid)ranked first(SUCRA,88.9%),rofecoxib ranked second(SUCRA,68.1%),Celecoxib(3 mg/kg bid)ranked third(SUCRA,51.0%).There were no significant differences between any two NSAIDs regarding adverse events.The SUCRA shows that placebo ranked first(SUCRA,88.2%),piroxicam ranked second(SUCRA,60.5%),rofecoxib(0.6 mg/kg qd)ranked third(SUCRA,56.1%),meloxicam(0.125 mg/kg qd)ranked fourth(SUCRA,56.1%),and rofecoxib(0.3 mg/kg qd)ranked fifth(SUCRA,56.1%).CONCLUSION In summary,celecoxib(6 mg/kg bid)was found to be the most effective NSAID for treating JIA.Rofecoxib,piroxicam,and meloxicam may be safer options,but further research is needed to confirm these findings in larger trials with higher quality studies. 展开更多
关键词 Non-steroidal anti-inflammatory drugs Juvenile idiopathic arthritis Network meta-analysis Systematic review
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Recent advances in promising drugs for primary prevention of gastroesophageal variceal bleeding with cirrhotic portal hypertension 被引量:1
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作者 Ji-Yao Sheng Zi-Fan Meng +1 位作者 Qiao Li Yong-Sheng Yang 《Hepatobiliary & Pancreatic Diseases International》 SCIE CAS CSCD 2024年第1期4-13,共10页
Background:Gastroesophageal variceal bleeding is one of the most severe complications of patients with cirrhosis.Although primary prevention drugs,including non-selectiveβ-blockers,have effectively reduced the incide... Background:Gastroesophageal variceal bleeding is one of the most severe complications of patients with cirrhosis.Although primary prevention drugs,including non-selectiveβ-blockers,have effectively reduced the incidence of bleeding,their efficacy is limited due to side effects and related contraindications.With recent advances in precision medicine,precise drug treatment provides better treatment efficacy.Data sources:Literature search was conducted in PubMed,MEDLINE and Web of Science for relevant articles published up to May 2022.Information on clinical trials was obtained from https://clinicaltrials.gov/and http://www.chictr.org.cn/.Results:The in-depth understanding of the pathogenesis and advances of portal hypertension has enabled the discovery of multiple molecular targets for promising drugs.According to the site of action,these drugs could be classified into four classes:intrahepatic,extrahepatic,both intrahepatic and extrahepatic targets and others.All these classes of drugs offer advantages over traditional treatments in prevention of gastroesophageal variceal bleeding in patients with cirrhotic portal hypertension.Conclusions:This review classified and summarized the promising drugs,which prevent gastroesophageal variceal bleeding by targeting specific markers of pathogenesis of portal hypertension,demonstrating the significance of using the precision medicine strategy to discover and develop promising drugs for the primary prevention of gastroesophageal variceal bleeding in patients with cirrhotic portal hypertension. 展开更多
关键词 Cirrhotic portal hypertension Target drug Primary prevention BLEEDING
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Vitamin D,selenium,and antidiabetic drugs in the treatment of type 2 diabetes mellitus with Hashimoto's thyroiditis 被引量:2
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作者 Fen Feng Bin Zhou +3 位作者 Ci-La Zhou Ping Huang Gang Wang Kuang Yao 《World Journal of Diabetes》 SCIE 2024年第2期209-219,共11页
BACKGROUND Diabetes and thyroiditis are closely related.They occur in combination and cause significant damage to the body.There is no clear treatment for type-2 diabetes mellitus(T2DM)with Hashimoto's thyroiditis... BACKGROUND Diabetes and thyroiditis are closely related.They occur in combination and cause significant damage to the body.There is no clear treatment for type-2 diabetes mellitus(T2DM)with Hashimoto's thyroiditis(HT).While single symptomatic drug treatment of the two diseases is less effective,combined drug treatment may improve efficacy.AIM To investigate the effect of a combination of vitamin D,selenium,and hypoglycemic agents in T2DM with HT.METHODS This retrospective study included 150 patients with T2DM and HT treated at The Central Hospital of Shaoyang from March 2020 to February 2023.Fifty patients were assigned to the control group,test group A,and test group B according to different treatment methods.The control group received low-iodine diet guidance and hypoglycemic drug treatment.Test group A received the control treatment plus vitamin D treatment.Test group B received the group A treatment plus selenium.Blood levels of markers of thyroid function[free T3(FT3),thyroid stimulating hormone(TSH),free T4(FT4)],autoantibodies[thyroid peroxidase antibody(TPOAB)and thyroid globulin antibody(TGAB)],blood lipid index[low-density lipoprotein cholesterol(LDL-C),total cholesterol(TC),triacylglycerol(TG)],blood glucose index[fasting blood glucose(FBG),and hemoglobin A1c(HbA1c)]were measured pre-treatment and 3 and 6 months after treatment.The relationships between serum 25-hydroxyvitamin D3[25(OH)D3]level and each of these indices were analyzed.RESULTS The levels of 25(OH)D3,FT3,FT4,and LDL-C increased in the order of the control group,test group A,and test group B(all P<0.05).The TPOAB,TGAB,TC,TG,FBG,HbA1c,and TSH levels increased in the order of test groups B,A,and the control group(all P<0.05).All the above indices were compared after 3 and 6 months of treatment.Pre-treatment,there was no divergence in serum 25(OH)D3 level,thyroid function-related indexes,autoantibodies level,blood glucose,and blood lipid index between the control group,test groups A and B(all P>0.05).The 25(OH)D3 levels in test groups A and B were negatively correlated with FT4 and TGAB(all P<0.05).CONCLUSION The combination drug treatment for T2DM with HT significantly improved thyroid function,autoantibody,and blood glucose and lipid levels. 展开更多
关键词 Type-2 diabetes mellitus Hashimoto's thyroiditis Vitamin D Selenium agent Hypoglycemic drugs Curative effect
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Development of small molecule drugs targeting immune checkpoints 被引量:1
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作者 Luoyi Chen Xinchen Zhao +3 位作者 Xiaowei Liu Yujie Ouyang Chuan Xu Ying Shi 《Cancer Biology & Medicine》 SCIE CAS CSCD 2024年第5期382-399,共18页
Immune checkpoint inhibitors(ICIs)are used to relieve and refuel anti-tumor immunity by blocking the interaction,transcription,and translation of co-inhibitory immune checkpoints or degrading co-inhibitory immune chec... Immune checkpoint inhibitors(ICIs)are used to relieve and refuel anti-tumor immunity by blocking the interaction,transcription,and translation of co-inhibitory immune checkpoints or degrading co-inhibitory immune checkpoints.Thousands of small molecule drugs or biological materials,especially antibody-based ICIs,are actively being studied and antibodies are currently widely used.Limitations,such as anti-tumor efficacy,poor membrane permeability,and unneglected tolerance issues of antibody-based ICIs,remain evident but are thought to be overcome by small molecule drugs.Recent structural studies have broadened the scope of candidate immune checkpoint molecules,as well as innovative chemical inhibitors.By way of comparison,small molecule drug-based ICIs represent superior oral bioavailability and favorable pharmacokinetic features.Several ongoing clinical trials are exploring the synergetic effect of ICIs and other therapeutic strategies based on multiple ICI functions,including immune regulation,anti-angiogenesis,and cell cycle regulation.In this review we summarized the current progression of small molecule ICIs and the mechanism underlying immune checkpoint proteins,which will lay the foundation for further exploration. 展开更多
关键词 Immune checkpoints small molecule drugs programmed death protein 1 CD47 signal-regulatory proteinα
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An Update on the Clinical Pipelines of New Antibacterial Drugs Developed in China 被引量:1
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作者 Xinyi Yang Congran Li +8 位作者 Xiukun Wang Zhonghui Zheng Peiyi Sun Chunjie Xu Luni Chen Jiandong Jiang Staffan Normark Birgitta Henriques-Normark Xuefu You 《Engineering》 SCIE EI CAS CSCD 2024年第7期52-68,共17页
Antibacterial resistance is a global health threat that requires further concrete action on the part of all countries.In this context,one of the biggest concerns is whether enough new antibacterial drugs are being dis... Antibacterial resistance is a global health threat that requires further concrete action on the part of all countries.In this context,one of the biggest concerns is whether enough new antibacterial drugs are being discovered and developed.Although several high-quality reviews on clinical antibacterial drug pipelines from a global perspective were published recently,none provides comprehensive information on original antibacterial drugs at clinical stages in China.In this review,we summarize the latest progress of novel antibacterial drugs approved for marketing and under clinical evaluation in China since 2019.Information was obtained by consulting official websites,searching commercial databases,retrieving literature,asking personnel from institutions or companies,and other means,and a considerable part of the data covered here has not been included in other reviews.As of June 30,2023,a total of 20 antibacterial projects from 17 Chinese pharmaceutical companies or developers were identified and updated.Among them,two new antibacterial drugs that belong to traditional antibiotic classes were approved by the National Medical Products Administration(NMPA)in China in 2019 and 2021,respectively,and 18 antibacterial agents are in clinical development,with one under regulatory evaluation,five in phase-3,six in phase-2,and six in phase-1.Most of the clinical candidates are new analogs or monocomponents of traditional antibacterial pharmacophore types,including two dual-acting hybrid antibiotics and a recombinant antibacterial protein.Overall,despite there being 17 antibacterial clinical candidates,our analysis indicates that there are still relatively few clinically differentiated antibacterial agents in stages of clinical development in China.Hopefully,Chinese pharmaceutical companies and institutions will develop more innovative and clinically differentiated candidates with good market potential in the future research and development(R&D)of original antibacterial drugs. 展开更多
关键词 Antimicrobial resistance New antibiotics Clinical pipelines WHO priority pathogens National Mega-Project for Innovative drugs
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Anti-obesity effects of fucoidan from Sargassum thunbergii in adipocytes and high fat diet induced obese mice through inhibiting adipogenic specific transcription factor
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作者 Hyo-Geun Lee H.H.A.C.K.Jayawardhana +7 位作者 Fengqi Yang D.P.Nagahawaththa N.M.Liyanage Kyung-Mo Song Yun-Sang Choi Seung-Hong Lee You-Jin Jeon Min-Cheol Kang 《Food Science and Human Wellness》 SCIE CSCD 2024年第3期1608-1616,共9页
The prevalence of obesity has increased and is a health concern worldwide.Due to the concerns regarding synthetic anti-obesity treatments,nowadays natural products become a trend.Previous studies proved that there is ... The prevalence of obesity has increased and is a health concern worldwide.Due to the concerns regarding synthetic anti-obesity treatments,nowadays natural products become a trend.Previous studies proved that there is a potential to use marine algae as anti-obesity agents.Therefore,in this study,the lipid inhibitory effect of crude polysaccharide of amyloglucosidase-assisted hydrolysate from Sargassum thunbergii(STAC)and its fucoidan fractions(STAFs)on 3T3-L1 cells and high-fat diet(HFD)-induced obese mice were investigated.According to the results,the STAF3,showed the highest xylose content and exhibited significant inhibitory effects on lipid accumulation by downregulating adipogenic and lipogenic proteins in 3T3-L1 cells.Furthermore,oral supplementation with STAC significantly declined gain in body weight and fat weight,and serum lipid contents in an HFD-induced obesity mouse model.Structural and chemical characterizations demonstrated that puritied STAF3 has consistent surface morphology and small particle size,with similar structural characteristics as commercial fucoidan.Together,these results indicate that STAC and purified STAF3 from Sargassum thunbergia is a potent source to develop as ananti-obesity agents or functional food products to counter obesity. 展开更多
关键词 Sargassum thunbergii FUCOIDAN anti-obesity Anti-steatosis
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Antibody-platinum(IV)prodrugs conjugates for targeted treatment of cutaneous squamous cell carcinoma
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作者 Xiangye Yin Yingjie Zhuang +9 位作者 Haiqin Song Yujian Xu Fan Zhang Jianxin Cui Lei Zhao Yingjie Yu Qixu Zhang Jun Ye Youbai Chen Yan Han 《Journal of Pharmaceutical Analysis》 SCIE CAS CSCD 2024年第3期389-400,共12页
Antibody-drug conjugates(ADCs)are a new type of targeting antibodies that conjugate with highly toxic anticancer drugs via chemical linkers to exert high specificity and efficient killing of tumor cells,thereby attrac... Antibody-drug conjugates(ADCs)are a new type of targeting antibodies that conjugate with highly toxic anticancer drugs via chemical linkers to exert high specificity and efficient killing of tumor cells,thereby attracting considerable attention in precise oncology therapy.Cetuximab(Cet)is a typical antibody that offers the benefits of good targeting and safety for individuals with advanced and inoperable cutaneous squamous cell carcinoma(cSCC);however,its anti-tumor activity is limited to a single use.Cisplatin(CisPt)shows good curative effects;however,its adverse effects and non-tumor-targeting ability are major drawbacks.In this study,we designed and developed a new ADC based on a new cytotoxic platinum(IV)prodrug(C8Pt(IV))and Cet.The so-called antibody-platinum(IV)prodrugs conjugates,named Cet-C8Pt(IV),showed excellent tumor targeting in cSCC.Specifically,it accurately delivered C8Pt(IV)into tumor cells to exert the combined anti-tumor effect of Cet and CisPt.Herein,metabolomic analysis showed that Cet-C8Pt(IV)promoted cellular apoptosis and increased DNA damage in cSCC cells by affecting the vitamin B6 metabolic pathway in tumor cells,thereby further enhancing the tumor-killing ability and providing a new strategy for clinical cancer treatment using antibody-platinum(IV)prodrugs conjugates. 展开更多
关键词 Antibody drug conjugate Cutaneous squamous cell carcinoma DNA damage Platinum drug Targeted therapy
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Bacterial Exofactors Modulate Biofilm Growth and Resistivity to Antimicrobial Drugs
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作者 Van Nguyen# Bea Penaredondo# Girdhari Rijal 《Advances in Microbiology》 CAS 2024年第1期11-24,共14页
Some bacteria have the ability to co-exist, proliferate and survive in a multicellular community, biofilm. Each participating bacteria can form its colonies and encases itself by a self-produced insoluble extracellula... Some bacteria have the ability to co-exist, proliferate and survive in a multicellular community, biofilm. Each participating bacteria can form its colonies and encases itself by a self-produced insoluble extracellular matrix substance (EPS). Microcolonies within biofilm are held together by interactions and bonding of the substances present in the EPS with their separation from the water channels. Similar to insoluble EPS, bacterial microcolonies release soluble exofactors that have direct impacts on the survivability, growth and antibacterial resistivity of other microcolonies made of single- or multi-species bacteria in the same biofilm. How the exofactors of microcolonies of one-type bacteria impact on microcolonies of other-type bacteria is still unclear. We studied about the role of exofactors released from Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, which are common biofilm-forming pathogenic bacteria. Exofactors facilitate to transform the microenvironment where bacteria can acquire alternative lifestyle with a long survival period and resistivity to certain antimicrobial drugs. 展开更多
关键词 BIOFILM Exofactors Antimicrobial drugs GROWTH Extracellular Matrix Substance Microcolonies
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Practice of Perioperative Rational Use of Antibacterial Drugs Based on Drug Pathway
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作者 Changkai ZHOU Fanbo JING +1 位作者 Haijun QU Jing GAO 《Medicinal Plant》 2024年第2期57-60,64,共5页
[Objectives]To establish a new management model for rational use of perioperative antibacterial drugs in surgical departments.[Methods]Based on evidence-based medicine,the department s drug pathway was formulated,and ... [Objectives]To establish a new management model for rational use of perioperative antibacterial drugs in surgical departments.[Methods]Based on evidence-based medicine,the department s drug pathway was formulated,and the new mode of rational drug use control was established by using fine pharmaceutical technology intervention,and the intervention effect was evaluated by the intensity of antibacterial drug use,per capita drug costs and the proportion of drugs.[Results]After adopting drug pathway in departments,the intensity of antibacterial drug use,per capita drug costs and the proportion of drugs decreased significantly,and the effect of rational drug use control was remarkable.[Conclusions]The drug pathway provides a new management and control mode for the rational use of perioperative antibacterial drugs in surgical departments of hospitals.Thus,it is worthy of popularization and application. 展开更多
关键词 Perioperative period Antibacterial drugs drug pathway Rational drug use Management model
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Global hotspots and future directions for drugs to improve the skin flap survival: A bibliometric and visualized review
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作者 Shuangmeng Jia Jieshen Huang +5 位作者 Wuyan Lu Yongen Miao Kehua Huang Chenzhang Shi Shuaijun Li Jiefeng Huang 《Journal of Pharmaceutical Analysis》 SCIE CAS CSCD 2024年第7期972-982,共11页
Skin flaps are frequently employed in plastic and reconstructive surgery to address tissue defects.However,their low survival rates remain a challenge,attributed to vascular crisis and necrosis.Despite numerous studie... Skin flaps are frequently employed in plastic and reconstructive surgery to address tissue defects.However,their low survival rates remain a challenge,attributed to vascular crisis and necrosis.Despite numerous studies investigating drugs to alleviate flap necrosis,a comprehensive analysis of the research trend in this critical area is lacking.To gain a deeper understanding of the current status,research focal points,and future trends in drugs aimed at enhancing flap survival,a thorough retrospective analysis is imperative.This study aims to employ bibliometric methods to scrutinize the evolution,mechanisms,and forthcoming trends of drugs targeting flap survival improvement.Using VOSviewer software,we quantitatively and visually depict 1)annual temporal trends in the number of documents and citations;2)national/regional publications and their collaborations;3)institutional and authors’contribution;4)journal contribution and relevance;and 5)analysis of research hotspots and directions derived from keywords.Ultimately,we discussed the prospects and challenges of future advances and clinical translation of drugs designed to enhance skin flap survival.In conclusion,the field of pharmacology dedicated to improving skin flap survival is expanding,and this study aims to offer a fresh perspective to promote the advancement and clinical application of such drugs. 展开更多
关键词 Skin flap drug therapy Bibliometric analysis Global trends
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Combination Activity of Standard Antituberculosis Drugs and Extracts of Medicinal Plants Commonly Used in Traditional Treatment of Tuberculosis in Uganda
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作者 Moses Mpeirwe Kevin Komakech +2 位作者 Duncan Ssesazi Patrick Engeu Ogwang Joel Bazira 《Advances in Infectious Diseases》 CAS 2024年第3期511-522,共12页
Introduction: Resistance to antituberculosis drugs and adverse drug reactions remain the leading causes of tuberculosis therapeutic failure globally. Despite the increasing acceptance of medicinal plant use in combina... Introduction: Resistance to antituberculosis drugs and adverse drug reactions remain the leading causes of tuberculosis therapeutic failure globally. Despite the increasing acceptance of medicinal plant use in combination with conventional antituberculosis drugs in treatment of tuberculosis (TB) in Uganda, there is paucity of knowledge on their combination effect. Aim: This research aimed to determine combination activity of standard antituberculosis drugs with extracts of Zanthoxylum leprieurii Guill. & Perr. and Rubia cordifolia L., the two common antituberculosis medicinal plants in Uganda, against pansensitive (H37Rv) and multi-drug resistant (MDR) Mycobacterium tuberculosis strains. Materials and Methods: Two reference MTB strains (H37Rv and MDR strain) were inoculated on Middlebrook 7H11 medium containing a combination of standard antituberculosis drugs and methanol extracts of Z. leprieurii and R. cordifolia at varying concentrations. The number of colonies on the plates was observed and counted weekly for up to 8 weeks. In vitro combination activity was determined using proportion method. Mean percentage inhibition was calculated for the reduction of number of colonies on drug-extract combination medium in relation to drug-extract-free control medium. Results: Drug-extract combinations showed good combination activity against Mycobacterium tuberculosis strains when compared with individual standard anti-TB drugs. This was more exhibited against MDR strain. There was however a reduction in percentage inhibition when extracts were combined with ethambutol and streptomycin against H37Rv strain. Conclusions: Zanthoxylum leprieurii and Rubia cordifolia in combination with standard anti-TB drugs exhibited increased in vitro activity against Mycobacterium tuberculosis, especially MDR-TB strain. This justifies the local use of these plants in traditional treatment of tuberculosis especially in resistant cases in Uganda. 展开更多
关键词 Combination Activity Medicinal Plants Zanthoxylum leprieurii Rubia cordifolia Standard Antituberculosis drugs
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Alcohol and illicit drugs:prevalence of alcohol and illicit drug use and their predictors in young people from Argentina,Bulgaria,Chile and Romania
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作者 Daniel Vankov David Jankovszky +2 位作者 Borislav Vankov Martin Galanternik Claudia Rodriguez 《Global Health Journal》 2024年第1期16-23,共8页
Background:Alcohol and illicit drugs(AID)continue to be a major global health concern.Although preventable,AID is linked to millions of deaths annually worldwide.The situation is particularly grave for young people,wi... Background:Alcohol and illicit drugs(AID)continue to be a major global health concern.Although preventable,AID is linked to millions of deaths annually worldwide.The situation is particularly grave for young people,with AID being a major direct risk factor for disability-adjusted youth life-years lost and death.It further contributes to assaults,road crashes,accidental poisoning,and suicide,leading to long-term issues and public health concerns.Objective:This study aimed at disclosing current AID prevalence data for Argentinian,Bulgarian,Chilean and Romanian youth.It shed light on the predictors of AID in young people from those countries.Method:The study used an online survey to gather data from people aged 18 to 25(n=1,297).The survey was underpinned by the theory of planned behaviour(TPB).Predictors were investigated separately for drinking alcohol and using illicit drugs.Results:Our data revealed that across the four target countries,49%to 90%of the participants drank alcohol,and 8%to 35%used illicit drugs in the past three months.Between 20%and 91%of them intended to drink,and between 8%and 31%intended to use illicit drugs in the following three months.Our TPB model predicted statistically significant(P<0.001)amounts of variance in drinking alcohol(between 61%and 72%)and using illicit drugs(between 20.3%and 74.4%).Intention was consistent in significantly predicting both behaviours.Evidence around the predictive validity of self-efficacy,age and gender was mixed across the investigated countries.Conclusion:This research provided an update on the scarce AID epidemiological data.It also supplied evidence about what theoretically-informed measures might be useful targets of interventions in the case of Argentina,Bulgaria,Chile and Romania.This new knowledge of understanding substance abuse determinants and prevalence may help researchers and practitioners better meet young people's health prevention needs. 展开更多
关键词 Young people ALCOHOL Ilicit drugs INTENTION SELF-EFFICACY
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Roles of Community Pharmacists in Screening and Disseminating of Information about Non-Steroidal Anti-Inflammatory Drugs Risks: Implications for Drug Safety Assessment
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作者 Martin Kampamba Progress Mulenga +8 位作者 Steward Mudenda Billy Chabalenge Jenipher Zulu Tadius Chimombe Webrod Mufwambi Mashebe Innocent Ngula Audrey Hamachila Jimmy Hangoma Christabel Nang’andu Hikaambo 《Pharmacology & Pharmacy》 2024年第4期129-145,共17页
Background: The increasing use of non-steroidal anti-inflammatory drugs (NSAIDs) both on prescription and over the counter raises a major global health concern because of the risks associated with their use if no prop... Background: The increasing use of non-steroidal anti-inflammatory drugs (NSAIDs) both on prescription and over the counter raises a major global health concern because of the risks associated with their use if no proper guidance is given by the health care provider. This study assessed the roles of community pharmacists in screening and disseminating information about the risks associated with NSAID use in Zambia. Methodology: This was a national cross-sectional study in which a structured self-administered questionnaire was administered to 245 registered community pharmacists in Zambia. Stata/BE, version 15.1 (Stata Corporation, College Station, Texas, USA) and multivariate logistic regression model was used to determine factors associated with information dissemination about ADRs of NS-NSAIDs. Results: 231 of the 245 distributed questionnaires were returned giving a response rate of 94.3%. All (100%) participating community pharmacists claimed to have practiced dispensing NSAIDs. However, only 26 (11.0%) and 71 (30.8%) regularly screened for risk factor of selective COX-2 NSAIDS (SC2-NSAIDS) and non-selective NSAIDS (NS-NSAIDs) respectively. Information dissemination on adverse drug reactions (ADRs) of SC2-NSAIDS was regularly provided by only 22 (9.5%) of pharmacists while that of NS-NSAIDs was regularly provided by 49 (21.2%). In the multivariate logistic regression model, being the owner of a pharmacy (AOR: 5.4, CI: 1.84 - 16.4) was significantly associated with information dissemination about ADRs of NS-NSAIDs while an hour increase in the working hours per day (AOR: 0.9, CI: 0.64 - 0.95) was associated with less likelihood of information dissemination. Conclusion: Pharmacists working in community pharmacies in Zambia did not regularly screen and disseminate information about the risks associated with NSAID use. Therefore, pharmacists should be able to screen and monitor patients at risk and be aware of the majority of risk factors while dispensing NSAIDs to minimize the associated complications. 展开更多
关键词 Community Pharmacists Non-Steroidal Anti-Inflammatory drug Risk SCREENING
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Nonsteroidal anti-inflammatory drugs before endoscopic ultrasound guided tissue acquisition to reduce the incidence of post procedural pancreatitis
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作者 Mike de Jong Foke van Delft +4 位作者 Christine Roozen Erwin-Jan van Geenen Tanya Bisseling Peter Siersema Marco Bruno 《World Journal of Gastroenterology》 SCIE CAS 2024年第8期811-816,共6页
Endoscopic ultrasound(EUS)with fine needle aspiration or fine needle biopsy is the gold standard for sampling tissue to diagnose pancreatic cancer and auto-immune pancreatitis or to analyze cyst fluid.The most common ... Endoscopic ultrasound(EUS)with fine needle aspiration or fine needle biopsy is the gold standard for sampling tissue to diagnose pancreatic cancer and auto-immune pancreatitis or to analyze cyst fluid.The most common reported adverse event of fine needle aspiration and/or fine needle biopsy is acute pancreatitis,which is likely induced by the same pathophysiological mechanisms as after en-doscopic retrograde cholangiopancreatography(ERCP).According to the current European Society of Gastrointestinal Endoscopy guideline,nonsteroidal anti-inflammatory drugs are administered prior to ERCP as a scientifically proven treatment to reduce post-ERCP pancreatitis incidence rate.A single suppository of diclofenac or indomethacin prior to EUS guided tissue acquisition(TA)is harm-less in healthy adults.Since it is associated with low costs and,most important,may prevent a dreadsome complication,we strongly recommend the adminis-tration of 100 mg diclofenac rectally prior to EUS-TA.We will explain this recom-mendation in more detail in this review as well as the risk and pathophysiology of post-EUS TA pancreatitis. 展开更多
关键词 PANCREATITIS Endoscopic ultrasound Tissue acquisition Nonsteroidal antiinflammatory drugs Pancreatic cancer
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