Frontiers in Drug, Chemistry and Clinical Research最新文献

Boosting effect of pre-existing immunity on anti-cancer immunotherapies 预先免疫在抗癌免疫治疗中的增强作用

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/fdccr.1000155

M. Conti

引用次数: 3

Alkaline phosphatases, B6 vitamers and Pre-eclampsia 碱性磷酸酶，维生素B6和先兆子痫

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/fdccr.1000122

Medina Ja, D. Rabelo, R. C. B. Alves, D. Maria

引用次数: 0

Which is the best strategy for using diuretics in decompensated chronic heart failure? 在失代偿性慢性心力衰竭中使用利尿剂的最佳策略是什么?

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/fdccr.1000127

B. Vincenzo, D. Martina, De Marco

引用次数: 0

Synthesis and anti-Trypanosoma cruzi profile of the novel 4-thiazolidinone and 1,3-thiazole derivatives 新型4-噻唑烷酮和1,3-噻唑衍生物的合成及抗克氏锥虫谱分析

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/FDCCR.1000120

de Siqueira Lrp, M deOliveiraBarbosa, Oliveira Ar, de Moraes Gomes Pat, de Oliveira Filho Gb, Demcheva Mv, Hernandes Vp, D. Ac, J. Pas, Romanha Aj, Leite Acl

{"title":"Synthesis and anti-Trypanosoma cruzi profile of the novel 4-thiazolidinone and 1,3-thiazole derivatives","authors":"de Siqueira Lrp, M deOliveiraBarbosa, Oliveira Ar, de Moraes Gomes Pat, de Oliveira Filho Gb, Demcheva Mv, Hernandes Vp, D. Ac, J. Pas, Romanha Aj, Leite Acl","doi":"10.15761/FDCCR.1000120","DOIUrl":"https://doi.org/10.15761/FDCCR.1000120","url":null,"abstract":"Chagas disease is a serious public health problem in Brazil and world. Caused by the protozoan Trypanosoma cruzi, it is estimated 6-7 million people infected worldwide. The only drug used to treatment is Benzonidazole, but this drug is only effective in the acute phase of the disease. This paper reports the synthesis and the anti-Trypanosoma cruzi activity of 4-thiazolidinone and 1,3-thiazole derivatives based in thiosemicarbazones previously described as potent trypanocidal agent, planned through the bioisosterism strategy. Therefore, the synthesis of 28 aryl-4-thiazolidinones (2a-r and 3a-j) was achieved, which aryl ring possesses halogens atoms in meta and para positions, and the heterocyclic system had lipophilic substituents. These compounds were thus evaluated as anti-T. cruzi agents against epimastigote, trypomastigote and amastigote forms of T. cruzi. Compounds were also tested its toxicity in L929 fibroblasts. In view to investigate a bioisosteric relationship between 1,3-thiazoles and 4-thiazolidinones, eighteen 1,3thiazoles derived from trifluoromethyl thiosemicarbazone (4a-r) were also tested in the same model. It was possible to show that between the 46 tested compounds, those that possess a bromine (2a-r) atom showed better activity compared to compounds substituted by a trifluoromethyl group (3a-j) and to 1,3-thiazole derivatives (4a-r), which were inactive. In general, the 2a-r series showed low toxic profile in the cell line tested. Besides, compound 2h was the most active of then all when compared to the standard Benznidazole. *Correspondence to: Ana Cristina Lima Leite, Laboratório de Planejamento em Química Medicinal, Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil, E-mail: acllb2003@yahoo.com.br","PeriodicalId":112494,"journal":{"name":"Frontiers in Drug, Chemistry and Clinical Research","volume":"52 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134019512","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 5

Colorectal carcinogenesis, colorectal cancer development and Fusobacterium nucleatum 结直肠癌发生、结直肠癌发展与核梭杆菌

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/fdccr.1000152

T. Ohara

{"title":"Colorectal carcinogenesis, colorectal cancer development and Fusobacterium nucleatum","authors":"T. Ohara","doi":"10.15761/fdccr.1000152","DOIUrl":"https://doi.org/10.15761/fdccr.1000152","url":null,"abstract":"Many studies of colorectal cancer and gut microbiota have been reported since Fusobacterium nucleatum (F. nucleatum) was reported to be involved in carcinogenesis and cancer development. The reports range from inflammation to carcinogenesis / development, avoidance from the immune system, effects on oncogenes / tumor suppressor genes, cell growth promotion, and tumor cell adhesion. There is a report suggesting that F. nucleatum is involved in the development of cancer, which is a poor prognosis due to large amounts of bacteria as the stage progression. In addition, F. nucleatum has been reported to be associated with CIMP-high, microsatellite instability and MLH1 hypermethylation. This is a report suggesting that F. nucleatum may be involved not only in the carcinogenic pathway from adenomas but also in the carcinogenic pathway from serrated adenomas. In addition, F. nucleatum is an indigenous bacterium in the oral cavity and is also a causative bacterium of periodontal disease, but there is a report that the strains of colorectal cancer and F. nucleatum in the oral cavity are the same, and its carcinogenic mechanism is drawing attention. In this review, I will outline the relationship between colorectal carcinogenesis and colorectal cancer development and F. nucleatum, and also address the issues. *Correspondence to: Tadashi Ohara, M.D, Ph.D, Department of Gastroenterology, Kitashinagawa Third Hospital, Kohno Clinical Medicine Research Institute, 3-37 Kitashinagawa, Shinagawa, Tokyo 140-0001, Japan, Tel: +81-3-34741831; Fax: +81-5461-3740; E-mail: t.ohara@kcmi.or.jp Received: May 02, 2021; Accepted: May 12, 2021; Published: May 17, 202","PeriodicalId":112494,"journal":{"name":"Frontiers in Drug, Chemistry and Clinical Research","volume":"329 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134428422","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Flavonoid chemistry and neuroprotection 类黄酮化学与神经保护

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/fdccr.1000140

Douglas Vieira Thomaz

引用次数: 4

Does pomegranate protect against gamma-rays-induced cardiac illnesses in rats? 石榴能防止大鼠患γ射线引起的心脏病吗?

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/FDCCR.1000147

S. Tawfik, A. El-Kady, Heba H. Mansour

{"title":"Does pomegranate protect against gamma-rays-induced cardiac illnesses in rats?","authors":"S. Tawfik, A. El-Kady, Heba H. Mansour","doi":"10.15761/FDCCR.1000147","DOIUrl":"https://doi.org/10.15761/FDCCR.1000147","url":null,"abstract":"Pomegranate is a heart healthy fruit juice. The study aims to evaluate the effectiveness of pomegranate powder extract (Pom) in preventing γ -rays-induced cardiac illnesses in rat model. Rats were randomly divided into four groups of 10. Control group received 0.2ml diluted ethanol (vehicle) for 20days; Irradiated (IR) group received the vehicle for 10days, exposed to 8Gy- γ -rays and then given the vehicle for additional 10days; Pom group received 50mg Pom/kg body weight for 20days, and Pom+IR group received Pom for 10days then, rats were exposed to 8Gy- γ -rays and received Pom for additional 10days. Irradiated rats showed increased lipid peroxidation (LPO) and total nitrate/nitrite (NO(x)), and decreased levels of reduced glutathione (GSH) content, and the relative antioxidant enzyme activity of superoxide dismutase (SOD), glutathione peroxidase (GSHPx) and total antioxidant capacity (TAC) in the heart homogenates. Besides, asymmetric dimethylarginines (ADMA) was augmented in serum. Myocardial necrosis, edema, and inflammation were evident through the light microscope examination. Pre-treated rats with Pom significantly prevented or resisted all these alterations. Oral pre-treatment with Pom was effective in cardio protection in the γ -irradiated rats.","PeriodicalId":112494,"journal":{"name":"Frontiers in Drug, Chemistry and Clinical Research","volume":"12 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115167005","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Alternative therapeutic strategies to fight bacterial infections 对抗细菌感染的替代治疗策略

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/FDCCR.1000115

Leila Mousavifar, R. Roy

引用次数: 5

Tailoring Specialized Scoring Functions For More Efficient Virtual Screening 定制专门的评分功能，更有效的虚拟筛选

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/FDCCR.1000118

Tatiana F. Vieira, Rita P. Magalhães, S. Sousa

引用次数: 9

Exploration of the protein targets and function mechanism of tricetin based on surface plasmon resonance and reverse molecular docking 基于表面等离激元共振和反向分子对接的三曲霉素蛋白靶点及作用机制探索

Frontiers in Drug, Chemistry and Clinical Research Pub Date : 1900-01-01 DOI: 10.15761/fdccr.1000126

Yuan Y, Wang N, Zhu F, Shen M, Chen K

{"title":"Exploration of the protein targets and function mechanism of tricetin based on surface plasmon resonance and reverse molecular docking","authors":"Yuan Y, Wang N, Zhu F, Shen M, Chen K","doi":"10.15761/fdccr.1000126","DOIUrl":"https://doi.org/10.15761/fdccr.1000126","url":null,"abstract":"Tricetin is a type of flavonoid that plays an important role in anti-cancer activity. However, the protein targets and function mechanism of tricetin in HepG2 cells remain unclear, which greatly limits its clinical application. In this paper, tricetin was immobilized by 3D photo cross linking chip and the microfluidic environment was established. The SPR (surface plasmon resonance) technique was used to monitor the protein targets interacting with the tricetin on the surface of the chip. The target proteins captured by tricetin in HepG2 cell were identified by HPLC-MS (high performance liquid chromatography-mass pec trometry) method. Bioinformatics annotation and analysis of the obtained proteins showed that the VDR (vitamin D receptor) and PIM1 (Ser/Thr-protein kinase-1) were significantly enriched in the vitamin D receptor signalling pathway (Rich factor > 0.6), and thirty high affinity proteins mainly involved in pathways in Cancer, MAPK (mitogenactivated protein kinase) signalling pathway, TNF (tumour necrosis factor) signalling pathway, Osteoclast differentiation. Among them, four high score affinity target proteins, CYP1B1 (cytochrome P4501B1), VDR, PIM1 and GAA were screened by reverse molecular docking. Finally, the two target proteins, VDR and PIM1, which provided important theoretical support for tricetin in anti-liver cancer research were fully discussed. *Correspondence to: Keping Chen, Institute of Life Sciences, Jiangsu University, Zhenjiang, Jiangsu, China, E-mail: kpchen@ujs.edu.cn","PeriodicalId":112494,"journal":{"name":"Frontiers in Drug, Chemistry and Clinical Research","volume":"79 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"122456526","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0