215,513 results match your criteria agents evaluated

Monitoring of pathogenic Borrelia burgdorferi sensu lato in the Almaty oblast, Kazakhstan.

Ticks Tick Borne Dis 2021 Apr 9;12(4):101725. Epub 2021 Apr 9.

Almaty Branch of the National Center for Biotechnology, 14 Zhahanger St., Almaty, 050054, Kazakhstan; M.A. Aitkhozhin's Institute of Molecular Biology and Biochemistry, 86 Dosmukhamedov St., Almaty, 050012, Kazakhstan. Electronic address:

Lyme borreliosis (LB) is one of the most common vector-borne diseases transmitted by ticks. It is caused by the Borrelia burgdorferi sensu lato (s.l. Read More

View Article and Full-Text PDF

Diversity-oriented synthesis of cembranoid derivatives as potential anti-inflammatory agents.

Bioorg Chem 2021 Apr 6;111:104887. Epub 2021 Apr 6.

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China; Open Studio for Druggability Research of Marine Natural Products, Pilot National Laboratory for Marine Science and Technology (Qingdao), 1 Wenhai Road, Aoshanwei, Jimo, Qingdao, 266237, China. Electronic address:

Eleven novel cembranoid derivatives were designed, synthesized, and evaluated for their inflammation related activities on the basis of our isolated and previously reported anti-inflammatory marine cembranoids. In bioassay, compound 11 displayed the most promising inhibitory effects with IC value of 1.1 μM for the TNF-α inhibitory activity. Read More

View Article and Full-Text PDF

Establishment of The Tandem Mass Spectrometric Fingerprints of Taxane-Based Anticancer Compounds.

Rapid Commun Mass Spectrom 2021 Apr 17:e9107. Epub 2021 Apr 17.

College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, SK, Canada.

Compounds in the taxane drug family are among the most successful and effective chemotherapeutic agents used for the treatment of solid tumors, such as breast, ovarian, and prostate cancers. The tandem mass spectrometric (MS/MS) fragmentation behavior of these compounds are described in detail and a generalized MS/MS fingerprint is established for the first time. Five compounds were evaluated, namely paclitaxel, docetaxel, cabazitaxel, cephalomannine, and Baccatin III. Read More

View Article and Full-Text PDF

Targeted antitumor comparison study between dopamine self-polymerization and traditional synthesis for nanoparticle surface modification in drug delivery.

Nanotechnology 2021 Apr 16. Epub 2021 Apr 16.

Chinese Academy of Medical Sciences and Peking Union Medical College Institute of Medicinal Plant Development, Beijing, CHINA.

To improve the therapeutic efficacy of anticancer agents and extend their application, mussel-inspired chemical modifications have attracted considerable attention. Surface modification based on polydopamine (PDA) has been a facile and versatile method to immobilize biomolecules on substrates for targeted drug delivery. To better analyze pharmaceutical differences between PDA-based surface modification and traditional synthesis methods, we prepared two kinds of folate (FA)-targeted nanoparticles (NPs) loaded with paclitaxel (PTX). Read More

View Article and Full-Text PDF

Synthesis and in vivo screening of isosteviol derivatives as new cardioprotective agents.

Eur J Med Chem 2021 Mar 28;219:113396. Epub 2021 Mar 28.

School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou, 510006, China. Electronic address:

Isosteviol, an ent-beyerane diterpenoid, has been repeatedly reported to possess potent cardioprotective activity. With the aim of discovering new cardioprotective derivatives from isosteviol, 47 compounds, including 40 new ones, were synthesized and evaluated in vivo using the easy-handling and efficient zebrafish model. The structure-activity relationship of this type of compounds was thus discussed. Read More

View Article and Full-Text PDF

Cerium oxide nanoparticles acts as a novel therapeutic agent for ulcerative colitis through anti-oxidative mechanism.

Life Sci 2021 Apr 13:119500. Epub 2021 Apr 13.

Department of Physiology, Faculty of Medicine, Mashhad University of Medical Sciences, Mashhad, Iran; Metabolic Syndrome Research Center, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:

Background: Cerium (IV) oxide (CeO) exhibit anti-inflammatory activity via scavenge free radicals and decreasing the oxygen species (ROS) production. Here we aimed to exhibit the therapeutic effect of this nanoparticle in experimental colitis models.

Methods: Cerium oxide nanoparticles (CeONPs) were synthesized via using UiO-66 as a precursor. Read More

View Article and Full-Text PDF

Design, synthesis, and molecular docking of some novel tacrine based cyclopentapyranopyridin- and tetrahydropyranoquinolin-kojic acid derivatives as anti-acetylcholinesterase agents.

Chem Biodivers 2021 Apr 16. Epub 2021 Apr 16.

Hamadan University of Medical Sciences Medical Sciences, Medicinal Chemistry, Shahid fahmideh, 081, hamedan, IRAN (ISLAMIC REPUBLIC OF).

A novel series of tacrine based cyclopentapyranopyridin- and tetrahydropyranoquinolin-kojic acid derivatives were designed, synthesized, and evaluated as anti-cholinesterase agents. The chemical structures of all target compounds were characterized by 1H-NMR, 13C-NMR, and elemental analyses. The synthesized compounds mostly inhibited acetylcholinesterase enzyme (AChE) with IC50 values of 4. Read More

View Article and Full-Text PDF

Antifungal Activities of Curcuminoids and Difluorinated Curcumin Against Clinical Dermatophyte Isolates.

Adv Exp Med Biol 2021 ;1308:101-107

Applied Biomedical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Dermatophytes are a group of fungal agents that can invade humans' keratinized tissues such as skin, nail, and hair, thereby causing dermatophyte infection (dermatophytosis) or ringworm. Some natural products have been reported to possess fungicidal effects. Hence, the present study investigated the effect of curcuminoids (CUR) and difluorinated curcumin (CDF) against clinical isolates of dermatophytes. Read More

View Article and Full-Text PDF
January 2021

Discovery of Anti-TNBC Agents Targeting PTP1B: Total Synthesis, Structure-Activity Relationship, and Investigations of Jamunones.

J Med Chem 2021 Apr 16. Epub 2021 Apr 16.

Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, China.

Twenty-three natural jamunone analogues along with a series of jamunone-based derivatives were synthesized and evaluated for their inhibitory effects against breast cancer (BC) MDA-MB-231 and MCF-7 cells. The preliminary structure-activity relationship revealed that the length of aliphatic side chain and free phenolic hydroxyl group at the scaffold played a vital role in anti-BC activities and the methyl group on chromanone affected the selectivity of molecules against MDA-MB-231 and MCF-7 cells. Among them, jamunone M (JM) was screened as the most effective anti-triple-negative breast cancer (anti-TNBC) candidate with a high selectivity against BC cells over normal human cells. Read More

View Article and Full-Text PDF

Antioxidant Nanomedicine Significantly Enhances the Survival Benefit of Radiation Cancer Therapy by Mitigating Oxidative Stress-Induced Side Effects.

Small 2021 Apr 15:e2008210. Epub 2021 Apr 15.

Department of Materials Science, Graduate School of Pure and Applied Sciences, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki, 305-8573, Japan.

Oxidative stress-induced off-target effects limit the therapeutic window of radiation therapy. Although many antioxidants have been evaluated as radioprotective agents, none of them are in widespread clinical use, owing to the side effects of the antioxidants themselves and the lack of apparent benefit. Aiming for a truly effective radioprotective agent in radiation cancer therapy, the performance of a self-assembling antioxidant nanoparticle (herein denoted as redox nanoparticle; RNP) is evaluated in the local irradiation of a subcutaneous tumor-bearing mouse model. Read More

View Article and Full-Text PDF

Performance of entomopathogenic nematodes on the mealybug, (Hemiptera: Pseudococcidae) and the compatibility of control agents with nematodes.

J Nematol 2021 25;53. Epub 2021 Feb 25.

Universidade Estadual do Norte do Paraná, Laboratório de Entomologia e Controle Microbiano (LECOM), Cornélio Procópio, Paraná, Brazil.

The performance of nine isolates of and one of on the mealybug (Hemiptera: Pseudococcidae), were evaluated. The most virulent isolates were evaluated for nematode vertical and horizontal dispersal, and for efficiency at concentrations of 0 (control), 25, 50, 75, and 100 infective juveniles (IJs)/cm on adult females of the insect. A compatibility assessment was also carried out with commercial products, registered or in the process of registration, for use in the cassava culture. Read More

View Article and Full-Text PDF
February 2021

Exosomes derived from plasma: promising immunomodulatory agents for promoting angiogenesis to treat radiation-induced vascular dysfunction.

PeerJ 2021 2;9:e11147. Epub 2021 Apr 2.

State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu, Sichuan, China.

Ionizing radiation (IR)-induced vascular disorders slow down tissue regeneration. Exosomes derived from plasma exhibit potential to promote angiogenesis; meanwhile, the immune microenvironment plays a significant role in the process. This study aimed to test the hypothesis that plasma exosomes promote angiogenesis in irradiated tissue by mediating the immune microenvironment. Read More

View Article and Full-Text PDF

16S amplicon sequencing of microbial communities in enriched and non-enriched sediments of non-volcanic hot spring with temperature gradients.

PeerJ 2021 2;9:e10995. Epub 2021 Apr 2.

Special Infectious Agents Unit, King Fahd Medical Research Center, King Abdulaziz University, Jeddah, Saudi Arabia.

Microorganisms in geothermal springs can offer insights into the fundamental and applied study of extremophiles. However, low microbial abundance and culturing requirements limit the ability to analyze microbial diversity in these ecosystems. In this study, culture-dependent and culture-independent techniques were used to analyze sediment samples from the non-volcanic Tatta Pani hot springs in district Poonch of Azad Kashmir. Read More

View Article and Full-Text PDF

Gingivitis Effectiveness of Emulgel Containing 2% Resveratrol in Orthodontic Patients: An 8-Week Randomized Clinical Trial.

Int J Dent 2021 29;2021:6615900. Epub 2021 Mar 29.

Department of Orthodontic, School of Dentistry, Kermanshah University of Medical Sciences, Kermanshah, Iran.

Background: Treatment of gingivitis in patients undergoing orthodontic treatment is done through different methods. Anti-inflammatory agents present in toothpaste or mouthwash are applied spontaneously by patients or used as professional treatment protocols. The present study aimed to investigate the gingivitis effectiveness of Emulgel containing 2% resveratrol in orthodontic patients. Read More

View Article and Full-Text PDF

Emerging and Experimental Agents for Anal Cancer: What is New?

J Exp Pharmacol 2021 9;13:433-440. Epub 2021 Apr 9.

Department of Gastrointestinal Medical Oncology, Oncoclínicas, Belo Horizonte, Brazil.

Squamous cell carcinoma of the anal canal (SCCA) is an HPV-related malignancy with rising incidence in the past few decades in the US, characterized by high rates of complete response to chemoradiotherapy with curative intent. However, in a long-term follow-up, a meaningful subgroup of patients with locally advanced disease presents disease recurrence, which demands treatments with high morbidity and important impact in the quality of life. In metastatic or unresectable disease, palliative chemotherapy is the standard of care, but it is still associated with a dismal prognosis. Read More

View Article and Full-Text PDF

N-acetyl cysteine induces quiescent-like pancreatic stellate cells from an active state and attenuates cancer-stroma interactions.

J Exp Clin Cancer Res 2021 Apr 15;40(1):133. Epub 2021 Apr 15.

Department of Surgery and Oncology, Graduate School of Medical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka, 812-8582, Japan.

Background: Pancreatic stellate cells (PSCs) occupy the majority of the pancreatic cancer microenvironment, contributing to aggressive behavior of pancreatic cancer cells (PCCs). Recently, anti-fibrotic agents have proven to be an effective strategy against cancer, but clinical trials have shown little efficacy, and the driving mechanism remains unknown. N-acetyl-cysteine (NAC) is often used for pulmonary cystic fibrosis. Read More

View Article and Full-Text PDF

Evaluation of Benzamide-chalcone Derivatives as EGFR/CDK2 inhibitor: Synthesis, in-vitro Inhibition, and Molecular Modeling Studies.

Anticancer Agents Med Chem 2021 Apr 14. Epub 2021 Apr 14.

Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, Mumbai 400005. India.

Background: EGFR (Epidermal Growth Factor Receptor) and CDK2 (Cyclin Dependent Kinase 2) are important targets in the treatment of many solid tumors and different ligands of these receptors share many common structural features.

Objective: The study involved synthesis of benzamide-substituted chalcones and determination of their antiproliferative activity as well as preliminary evaluation of EGFR and CDK2 inhibitory potential using both receptor binding and computational methods.

Methods: We synthesized 13 benzamide-substituted chalcone derivatives and tested their antiproliferative activity against MCF-7, HT-29 and U373MG cell-lines using Sulforhodamine B Assay. Read More

View Article and Full-Text PDF

Revealing Insights into Natural Products Against mcr-1-Producing Bacteria.

Curr Drug Targets 2021 Apr 14. Epub 2021 Apr 14.

Institute of Chemistry and Biotechnology, Federal University of Alagoas, AC. Simões campus, Lourival Melo Mota Avenue, 57072-970. Brazil.

Bacterial resistance has become a major global concern, affecting about 500,000 individuals in 22 countries. Thus, it is clear that Gram-negative bacteria have been receiving more attention in this scenario. These bacteria perform several resistance mechanisms, such as modifying lipid A from lipopolysaccharides as a product of the mcr-1 gene expression. Read More

View Article and Full-Text PDF

Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome.

Bioorg Med Chem 2021 Apr 2;38:116138. Epub 2021 Apr 2.

Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou 510642, China; Guangdong Laboratory for Lingnan Modern Agriculture, Guangzhou 510642, China. Electronic address:

A series of novel pleuromutilin derivatives were designed and synthesized with 1,2,4-triazole as the linker connected to benzoyl chloride analogues under mild conditions. The in vitro antibacterial activities of the synthesized derivatives against four strains of Staphylococcus aureus (MRSA ATCC 43300, ATCC 29213, AD3 and 144) were tested by the broth dilution method. Most of the synthesized derivatives displayed potent activities, and 22-(3-amino-2-(4-methyl-benzoyl)-1,2,4-triazole-5-yl)-thioacetyl)-22-deoxypleuromutilin (compound 12) was found to be the most active antibacterial derivative against MRSA (MIC = 0. Read More

View Article and Full-Text PDF

Tedizolid Activity against a Multi-center Worldwide Collection of Staphylococcus aureus and Streptococcus pneumoniae Recovered from Patients with Pneumonia (2017-2019).

Int J Infect Dis 2021 Apr 12. Epub 2021 Apr 12.

JMI Laboratories, North Liberty, Iowa, USA.

Objectives: The antimicrobial activity of tedizolid and comparators was evaluated against a large worldwide collection of Staphylococcus aureus and Streptococcus pneumoniae isolates recovered from patients with pneumonia.

Methods: Clinical isolates were collected from patients in 96 medical centers in the Asia-Pacific, Europe, Latin America, and United States during 2017-2019 and tested for susceptibility by reference broth microdilution.

Results: The most active agents against S. Read More

View Article and Full-Text PDF

6-Methyl-7-Aryl-7-Deazapurine Nucleosides as Anti-Trypanosoma cruzi Agents: Structure-Activity Relationship and in Vivo Efficacy.

ChemMedChem 2021 Apr 15. Epub 2021 Apr 15.

Faculty of Pharmaceutical Sciences Ghent University, Laboratory for Medicinal Chemistry, Ottergemsesteenweg 460, 9000, Gent, BELGIUM.

Chagas disease is a tropical infectious disease resulting in progressive organ-damage and currently lacks efficient treatment and vaccine options. The causative pathogen, Trypanosoma cruzi , requires uptake and processing of preformed purines from the host because it cannot synthesize these de novo , instigating the evaluation of modified purine nucleosides as potential trypanocides. By modifying the pyrimidine part of a previously identified 7-aryl-7-deazapurine nucleoside, we found that substitution of a 6-methyl for a 6-amino group allows retaining T. Read More

View Article and Full-Text PDF

A pilot study comparing daily teriparatide with monthly cycles of teriparatide and raloxifene.

Arch Osteoporos 2021 Apr 15;16(1):70. Epub 2021 Apr 15.

Osteoporosis Clinical Research Program, University of Wisconsin-Madison, 2870 University Ave, Suite 100, Madison, WI, 53705, USA.

This 6-month pilot study in osteoporotic postmenopausal women evaluated cyclic TPD/RLX compared to daily subcutaneous TPD with the concept of optimizing bone formation. Compared to daily subcutaneous TPD, cyclic therapy showed comparable increase in spine BMD and favorable effects on total proximal femur BMD and cortical thickness.

Purpose: There is no cure for osteoporosis; better medications or different approaches with current agents are needed. Read More

View Article and Full-Text PDF

Investigating new CT contrast agents: a phantom study exploring quantification and differentiation methods for high-Z elements using dual-energy CT.

Eur Radiol 2021 Apr 15. Epub 2021 Apr 15.

Department of Radiology, University of Texas Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX, 75390-9061, USA.

Objectives: To develop a dual-energy CT method for differentiating and quantifying high-Z contrast elements and to evaluate the limitations based on element concentration and atomic number by using an anthropomorphic phantom study.

Methods: Mass spectrometry standards for iodine, barium, gadolinium, ytterbium, tantalum, gold, and bismuth were diluted from 10.0 to 0. Read More

View Article and Full-Text PDF

Assessing locoregional treatment response to Hepatocellular Carcinoma: comparison of hepatobiliary contrast agents to extracellular contrast agents.

Abdom Radiol (NY) 2021 Apr 15. Epub 2021 Apr 15.

Department of Diagnostic, Molecular and Interventional Radiology, BioMedical Engineering and Imaging Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.

Cross-sectional imaging with contrast-enhanced magnetic resonance imaging (MRI) is routinely performed in patients with hepatocellular carcinoma (HCC) to assess tumor response to locoregional therapy (LRT). Current response assessment algorithms, such as the Liver Imaging Reporting and Data System (LI-RADS) treatment response algorithm (TRA), allow assessment using conventional gadolinium-based extracellular contrast agents (ECA) for accurate tumor response assessment following LRT. MRI with hepatobiliary agents (HBA) allows an acquisition of hepatobiliary phase (HBP), which is proven to increase sensitivity for detection of observations in at-risk patients, particularly for findings < 2 cm. Read More

View Article and Full-Text PDF

Cardiovascular Adverse Events With Intravitreal Anti-Vascular Endothelial Growth Factor Drugs: A Systematic Review and Meta-analysis of Randomized Clinical Trials.

JAMA Ophthalmol 2021 Apr 15. Epub 2021 Apr 15.

EA 4245, T2I (Transplantation, Immunity & Inflammation), Université de Tours, Tours, France.

Importance: Systemic safety of intravitreal anti-vascular endothelial growth factor (anti-VEGF) is a matter of debate and regular updates are necessary.

Objective: To evaluate systemic adverse events (SAEs) associated with intravitreal anti-VEGF drugs compared with non-anti-VEGF treatments in patients with ocular diseases.

Data Sources: Electronic searches were conducted in MEDLINE, Embase, and Cochrane Central Register of Controlled Trials databases from inception to July 7, 2020. Read More

View Article and Full-Text PDF

Assessment of Antiviral Effect of Natural Compounds on Porcine Epidemic Diarrhea Coronavirus.

Front Vet Sci 2021 29;8:652000. Epub 2021 Mar 29.

Department of Animal Health, Faculty of Veterinary Medicine, Universidad de León, León, Spain.

Organic acid and essential oils (EOs), well-known antimicrobials, could also possess antiviral activity, a characteristic which has not been completely addressed up to now. In this study, the effect of two organic acids (formic acid and sodium salt of coconut fatty acid distillates) and two single EO compounds (thymol and cinnamaldehye) was evaluated against porcine epidemic diarrhea virus (PEDV). The concentration used for each compound was established by cytotoxicity assays in Vero cells. Read More

View Article and Full-Text PDF

A randomized controlled trial to compare the efficacy of regenerated and non-regenerated oxidized cellulose gauze for the secondary treatment of local bleeding in patients undergoing hepatic resection.

Ann Surg Treat Res 2021 Apr 30;100(4):193-199. Epub 2021 Mar 30.

Department of Hepatobiliary Surgery, The First Hospital of China Medical University, Shenyang, China.

Purpose: Oxidized cellulose is available in many forms, but manufactured using either a regenerated or non-regenerated process. In this study, we evaluated the effects of 2 different hemostatic agents for the treatment of local bleeding in patients undergoing hepatic resection.

Methods: This was a monocentric, parallel-group, randomized, and controlled clinical trial to compare oxidized regenerated cellulose gauze (ORCG) with oxidized non-regenerated cellulose gauze (ONRCG) in patients undergoing hepatectomy. Read More

View Article and Full-Text PDF

Sodium-glucose cotransporter-2 inhibitors and risk for genitourinary infections in older adults with type 2 diabetes.

Ther Adv Drug Saf 2021 29;12:2042098621997703. Epub 2021 Mar 29.

University of Colorado Skaggs School of Pharmacy and Pharmaceutical Sciences, 12850 E. Montview Blvd., Campus Box C238, Room V20-1127A, Aurora, CO 80045, USA.

Background And Aims: Although landmark clinical trials have demonstrated an increased risk for genitourinary infection (GUI) after initiation of sodium-glucose cotransporter-2 inhibitor (SGLT2i) therapy that led to an FDA label warning, real world findings have been inconsistent and evidence specifically in older adults is lacking. The objective of the study was to examine the incidence of GUI in patients aged 65 years or older initiated on SGLT2i compared with glucagon-like peptide-1 receptor agonist (GLP1-RA) therapy at a large academic health system.

Methods: A retrospective population-based cohort study was conducted using electronic health records of patients aged 65 years and older with a diagnosis of type 2 diabetes mellitus. Read More

View Article and Full-Text PDF

Antimicrobial activities of a small molecule compound II-6s against oral streptococci.

J Oral Microbiol 2021 Mar 30;13(1):1909917. Epub 2021 Mar 30.

State Key Laboratory of Oral Diseases, National Clinical Research Center for Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu, China.

: The side effects of present antimicrobials like chlorhexidine (CHX) and the emergence of drug resistance necessitate the development of alternative agents to control dental caries. : This study developed a novel small molecule, namely II-6s, and investigated its antimicrobial activities against common oral streptococci associated with dental caries. : The susceptibility of streptococci to II-6s was evaluated by the microdilution method, time-kill assay and scanning electron microscopy. Read More

View Article and Full-Text PDF

Heat-cured poly(methyl methacrylate) resin incorporated with different food preservatives as an anti-microbial denture base material.

J Dent Sci 2021 Mar 26;16(2):706-712. Epub 2020 Sep 26.

The Siam Cement Public Company Limited (SCG), Bangkok, Thailand.

Background/purpose: The colonization of microorganisms onto denture bases is one common problem that can contribute to oral diseases. Herein, three food preservatives, including zinc oxide, potassium sorbate, and sodium metabisulfite were introduced as anti-microbial additives into a heat-polymerized poly(methyl methacrylate) (PMMA).

Materials And Methods: Relative microbial reductions of the modified PMMA resins against , , and were evaluated. Read More

View Article and Full-Text PDF