keyword
https://read.qxmd.com/read/38534687/navigating-the-chemical-space-of-enr-inhibitors-a-comprehensive-analysis
#21
JOURNAL ARTICLE
Vid Kuralt, Rok Frlan
Antimicrobial resistance is a global health threat that requires innovative strategies against drug-resistant bacteria. Our study focuses on enoyl-acyl carrier protein reductases (ENRs), in particular FabI, FabK, FabV, and InhA, as potential antimicrobial agents. Despite their promising potential, the lack of clinical approvals for inhibitors such as triclosan and isoniazid underscores the challenges in achieving preclinical success. In our study, we curated and analyzed a dataset of 1412 small molecules recognized as ENR inhibitors, investigating different structural variants...
March 11, 2024: Antibiotics
https://read.qxmd.com/read/38534663/polylactic-glycolic-acid-mediated-delivery-of-plectasin-derivative-nz2114-in-staphylococcus-epidermidis-biofilms
#22
JOURNAL ARTICLE
Xuanxuan Ma, Na Yang, Ruoyu Mao, Ya Hao, Da Teng, Yinhua Huang, Jianhua Wang
Antimicrobial peptides (AMPs) are antibiotic candidates; however, their instability and protease susceptibility limit clinical applications. In this study, the polylactic acid-glycolic acid (PLGA)-polyvinyl alcohol (PVA) drug delivery system was screened by orthogonal design using the double emulsion-solvent evaporation method. NZ2114 nanoparticles (NZ2114-NPs) displayed favorable physicochemical properties with a particle size of 178.11 ± 5.23 nm, polydispersity index (PDI) of 0.108 ± 0.10, ζ potential of 4...
February 29, 2024: Antibiotics
https://read.qxmd.com/read/38534656/antisense-and-functional-nucleic-acids-in-rational-drug-development
#23
REVIEW
Robert Penchovsky, Antoniya V Georgieva, Vanya Dyakova, Martina Traykovska, Nikolet Pavlova
This review is focused on antisense and functional nucleic acid used for completely rational drug design and drug target assessment, aiming to reduce the time and money spent and increase the successful rate of drug development. Nucleic acids have unique properties that play two essential roles in drug development as drug targets and as drugs. Drug targets can be messenger, ribosomal, non-coding RNAs, ribozymes, riboswitches, and other RNAs. Furthermore, various antisense and functional nucleic acids can be valuable tools in drug discovery...
February 27, 2024: Antibiotics
https://read.qxmd.com/read/38534647/synthesis-and-characterization-of-new-n-acyl-hydrazone-derivatives-of-carprofen-as-potential-tuberculostatic-agents
#24
JOURNAL ARTICLE
Ilinca Margareta Vlad, Diana Camelia Nuță, Miron Theodor Căproiu, Florea Dumitrașcu, Eleonóra Kapronczai, Georgiana Ramona Mük, Speranta Avram, Adelina Gabriela Niculescu, Irina Zarafu, Vanesa Alexandra Ciorobescu, Ana Maria Brezeanu, Carmen Limban
N-acyl hydrazone (NAH) is recognized as a promising framework in drug design due to its versatility, straightforward synthesis, and attractive range of biological activities, including antimicrobial, antitumoral, analgesic, and anti-inflammatory properties. In the global context of increasing resistance of pathogenic bacteria to antibiotics, NAHs represent potential solutions for developing improved treatment alternatives. Therefore, this research introduces six novel derivatives of ( EZ )-N'-benzylidene-2-(6-chloro-9 H -carbazol-2-yl)propanehydrazide, synthesized using a microwave-assisted method...
February 23, 2024: Antibiotics
https://read.qxmd.com/read/38534603/the-controlled-release-of-abscisic-acid-aba-utilizing-alginate-chitosan-gel-blends-a-synergistic-approach-for-an-enhanced-small-molecule-delivery-controller
#25
JOURNAL ARTICLE
Oscar Valdes, Daniel Bustos, Luis Guzmán, Marcelo Muñoz-Vera, Gabriela Urra, Ricardo I Castro, Luis Morales-Quintana
The integration of abscisic acid (ABA) into a chitosan-alginate gel blend unveils crucial insights into the formation and stability of these two substances. ABA, a key phytohormone in plant growth and stress responses, is strategically targeted for controlled release within these complexes. This study investigates the design and characterization of this novel controlled-release system, showcasing the potential of alginate-chitosan gel blends in ABA delivery. Computational methods, including molecular dynamics simulations, are employed to analyze the structural effects of microencapsulation, offering valuable insights into complex behavior under varying conditions...
March 8, 2024: Gels
https://read.qxmd.com/read/38534533/three-dimensional-printing-of-drug-eluting-implantable-plga-scaffolds-for-bone-regeneration
#26
JOURNAL ARTICLE
Manjusha Annaji, Nur Mita, Ishwor Poudel, Sai H S Boddu, Oladiran Fasina, R Jayachandra Babu
Despite rapid progress in tissue engineering, the repair and regeneration of bone defects remains challenging, especially for non-homogenous and complicated defects. We have developed and characterized biodegradable drug-eluting scaffolds for bone regeneration utilizing direct powder extrusion-based three-dimensional (3D) printing techniques. The PLGA scaffolds were fabricated using poly (lactic-co-glycolic acid) (PLGA) with inherent viscosities of 0.2 dl/g and 0.4 dl/g and ketoprofen. The effect of parameters such as the infill, geometry, and wall thickness of the drug carrier on the release kinetics of ketoprofen was studied...
March 6, 2024: Bioengineering
https://read.qxmd.com/read/38534519/molecular-dynamics-and-in-vitro-studies-elucidating-the-tunable-features-of-reconfigurable-nanodiscs-for-guiding-the-optimal-design-of-curcumin-formulation
#27
JOURNAL ARTICLE
Yongxiao Li, Wanting Xu, Xinpei Wang, Ruizhi Lai, Xiaohui Qiu, Zekai Zeng, Zhe Wang, Junqing Wang
In this study, we advance our exploration of Apolipoprotein A-I (apoA-I) peptide analogs (APAs) for their application in nanodisc (ND) assembly, focusing on the dynamic conformational characteristics and the potential for drug delivery. We explore APA-ND interactions with an emphasis on curcumin encapsulation, utilizing molecular dynamic simulations and in vitro assessments to evaluate the efficacy of various APA-ND formulations as drug carriers. The methodological approach involved the generation of three unique apoA-I α-11/3 helical mimics, resulting in fifteen distinct APAs...
February 29, 2024: Bioengineering
https://read.qxmd.com/read/38534380/fluvastatin-converts-human-macrophages-into-foam-cells-with-increased-inflammatory-response-to-inactivated-mycobacterium-tuberculosis-h37ra
#28
JOURNAL ARTICLE
María Teresa Montero-Vega, Joaquín Matilla, Eulalia Bazán, Diana Reimers, Ana De Andrés-Martín, Rafael Gonzalo-Gobernado, Carlos Correa, Francisco Urbano, Diego Gómez-Coronado
Cholesterol biosynthesis inhibitors (statins) protect hypercholesterolemic patients against developing active tuberculosis, suggesting that these drugs could help the host to control the pathogen at the initial stages of the disease. This work studies the effect of fluvastatin on the early response of healthy peripheral blood mononuclear cells (PBMCs) to inactivated Mycobacterium tuberculosis (Mtb) H37Ra . We found that in fluvastatin-treated PBMCs, most monocytes/macrophages became foamy cells that overproduced NLRP3 inflammasome components in the absence of immune stimulation, evidencing important cholesterol metabolism/immunity connections...
March 18, 2024: Cells
https://read.qxmd.com/read/38534362/repurposing-drugs-for-senotherapeutic-effect-potential-senomorphic-effects-of-female-synthetic-hormones
#29
JOURNAL ARTICLE
Laura R Bramwell, Ryan Frankum, Lorna W Harries
Repurposing previously approved drugs may fast track the route to the clinic for potential senotherapeutics and improves the inefficiency of the clinical drug development pipeline. We performed a repurposing screen of 240 clinically approved molecules in human primary dermal fibroblasts for their effects on CDKN2A expression. Molecules demonstrating effects on CDKN2A expression underwent secondary screening for senescence-associated beta galactosidase (SAB) activity, based on effect size, direction, and/or molecule identity...
March 15, 2024: Cells
https://read.qxmd.com/read/38533994/mobile-phone-text-messaging-for-medication-adherence-in-secondary-prevention-of-cardiovascular-disease
#30
REVIEW
Julie Redfern, Qiang Tu, Karice Hyun, Matthew A Hollings, Nashid Hafiz, Clara Zwack, Caroline Free, Pablo Perel, Clara K Chow
BACKGROUND: Cardiovascular diseases (CVDs) are the leading cause of death globally, accounting for almost 18 million deaths annually. People with CVDs have a five times greater chance of suffering a recurrent cardiovascular event than people without known CVDs. Although drug interventions have been shown to be cost-effective in reducing the risk of recurrent cardiovascular events, adherence to medication remains suboptimal. As a scalable and cost-effective approach, mobile phone text messaging presents an opportunity to convey health information, deliver electronic reminders, and encourage behaviour change...
March 27, 2024: Cochrane Database of Systematic Reviews
https://read.qxmd.com/read/38533902/new-n-1-3-4-thiadiazole-2-yl-acetamide-derivatives-as-human-carbonic-anhydrase-i-and-ii-and-acetylcholinesterase-inhibitors
#31
JOURNAL ARTICLE
Sam Dawbaa, Cüneyt Türkeş, Demokrat Nuha, Yeliz Demir, Asaf Evrim Evren, Leyla Yurttaş, Şükrü Beydemir
Various carbonic anhydrase (CA) enzyme isoforms are known today. In addition to the use of CA inhibitors as diuretics, antiepileptics and antiglaucoma agents, the inhibition of other specific isoforms of CA was reported to have clinical benefits in cancers. In this study, two groups of 1,3,4-thiadiazole derivatives were designed and synthesized to act as human CA I and II ( h CA I and h CA II) inhibitors. The activities of these compounds were tested in vitro and evaluated in silico studies. The activity of the synthesized compounds was also tested against acetylcholinesterase (AChE) to evaluate the relation of the newly designed structures to the activity against AChE...
March 27, 2024: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38533896/synthesis-of-novel-hydrazide-schiff-bases-with-anti-diabetic-and-anti-hyperlipidemic-effects-in-vitro-in-vivo-and-in-silico-approaches
#32
JOURNAL ARTICLE
Waseem Ul Islam, Abad Khan, Faizullah Khan, Saeed Ullah, Muhammad Waqas, Hammad Khan, Momin Khan, Shaikh Mizanoor Rahman, Shaukat Ali, Abdul Mateen, Asaad Khalid, Ajmal Khan, Ahmed Al-Harrasi
The increasing global incidence of non-insulin-dependent diabetes mellitus (NIDDM) necessitates innovative therapeutic solutions. This study focuses on the design, synthesis and biological evaluation of Schiff base derivatives from 2-bromo-2-(2-chlorophenyl) acetic acid, particularly hydrazone compounds 4a and 4b . Both in-vitro and in-vivo assays demonstrate these derivatives' strong antidiabetic and anti-hyperlipidemic properties. In a 15-d experiment, we administered 4a and 4b at doses of 2.5 and 5 mg/kg body weight, which effectively improved symptoms of alloxan-induced diabetes in mice...
March 27, 2024: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38533688/-in-vitro-evaluation-of-physicochemical-dependent-effects-of-polymeric-nanoparticles-on-their-cellular-uptake-and-co-localization-using-pulmonary-calu-3-cell-lines
#33
JOURNAL ARTICLE
Nashwa Osman, Paul Curley, Helen Box, Neill Liptrott, Darren Sexton, Imran Saleem
OBJECTIVE: The study evaluated physicochemical properties of eight different polymeric nanoparticles (NPs) and their interaction with lung barrier and their suitability for pulmonary drug delivery. METHODS: Eight physiochemically different NPs were fabricated from Poly lactic-co-glycolic acid (PLGA, PL) and Poly glycerol adipate-co-ω-pentadecalactone (PGA-co-PDL, PG) via emulsification-solvent evaporation. Pulmonary barrier integrity was investigated in vitro using Calu-3 under air-liquid interface...
March 27, 2024: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/38533582/a-short-term-economic-evaluation-of-early-insulin-therapy-compared-to-oral-anti-diabetic-drugs-in-order-to-reduce-the-major-adverse-events-in-type-2-diabetes-patients-in-iran
#34
JOURNAL ARTICLE
Ramin Heshmat, Ali Darvishi, Ramin Abdi Dezfouli, Adeleh Nikkhah, Ramin Radmanesh, Elham Moslemi
OBJECTIVE: While there are some recommendations about early insulin therapy in newly diagnosed Type 2 Diabetes Mellitus (T2DM) patients, there is not sufficient evidence on this strategy's cost-effectiveness. This study compared early insulin therapy versus oral anti-diabetic drugs (OADs) for managing T2DMusing a cost-effectiveness analysis approach in Iran. METHODS: In this economic evaluation, a decision analytic model was designed. The target population was newly diagnosed type 2 diabetic patients, and the study was carried out from the perspective of Iran's healthcare system with a one-year time horizon...
March 27, 2024: Current Medical Research and Opinion
https://read.qxmd.com/read/38533552/taar1-agonist-ulotaront-delays-gastric-emptying-of-solids-in-patients-with-schizophrenia-and-concurrent-metabolic-syndrome-with-prediabetes
#35
JOURNAL ARTICLE
Snežana Milanović, Nina Dedic, Robert Lew, Duane Burton, Kenneth S Koblan, Michael Camilleri, Seth C Hopkins
BACKGROUND: Metabolic syndrome (MetS), which can be induced or exacerbated by the current class of antipsychotic drugs, is highly prevalent in patients with schizophrenia and presents significant challenges to lifetime disease management. Supported by initial clinical results, trace amine-associated receptor 1 (TAAR1) agonists have emerged as potential novel treatments for schizophrenia. Notably, non-clinical studies have also shown weight-lowering and glucoregulatory effects of TAAR1 agonists, including the investigational agent ulotaront...
March 27, 2024: Diabetes, Obesity & Metabolism
https://read.qxmd.com/read/38533490/barriers-to-medication-adherence-among-patients-with-non-communicable-disease-in-north-wollo-zone-public-hospitals-socio-ecologic-perspective-2023
#36
JOURNAL ARTICLE
Eneyew Talie Fenta, Birtukan Gizachew Ayal, Atitegeb Abera Kidie, Tadele Fentabil Anagaw, Tesfaye Shumet Mekonnen, Eyob Ketema Bogale, Sileshi Berihun, Tilahun Degu Tsega, Chernet Mengistie Munie, Tizazu Talie Fenta, Nigus Kassie Worku, Sintayehu Shiferaw Gelaw, Misganaw Guadie Tiruneh
BACKGROUND: The practice of taking medication as directed by a healthcare provider is known as medication adherence. Therefore, the application of a socio-ecological model to this study identifies multilevel factors on barriers of medication adherence on chronic non-communicable disease and provides information to develop scientific health communication interventional strategies to improve medication adherence. OBJECTIVE: This study aimed to explore barriers of medication adherence on non-communicable disease prevention and care among patients in North Wollo Zone public hospitals, northeast Ethiopia...
2024: Patient Preference and Adherence
https://read.qxmd.com/read/38533429/harmonising-iv-oxycodone-with-paediatric-perioperative-medications-a-compatibility-study-through-y-type-connectors
#37
JOURNAL ARTICLE
Souha H Youssef, Alka Garg, Yunmei Song, Nicole E Wylie, Sanjay Garg
PURPOSE: Co-administering multiple intravenous (IV) agents via Y-connectors is a common practice in hospitalised and fasting surgical patients. However, there is a lack of reliable data confirming the physical compatibility of some combinations including IV oxycodone, a drug that is gaining increasing popularity in the perioperative period. Concern regarding physical drug incompatibilities precludes concurrent coadministration with other common drugs through a single lumen. This can result in the cessation of infusions to allow the administration of other medications, resulting in exacerbation of acute pain...
2024: Drug Design, Development and Therapy
https://read.qxmd.com/read/38533051/therapeutic-potential-of-clinically-proven-natural-products-in-the-management-of-dementia
#38
REVIEW
Farzana Ansari, Md Sohel, Md Mahfujul Haque Haidary, Md Saqline Mostaq, Shamima Akter, Asrafun Nahar, Fatematuz Zohora Labony, Arman Ahmed, Mohammed Shamim Hasan, Mohammad Hasem Babu, Mohammad Nurul Amin
Dementia is a common neurodegenerative disorder connected to damage to nerve cells in the brain. Although some conventional drugs are available for dementia treatments and are still sanctified for dementia patients, their short- and long-term side effects and other limitations make treating patients more challenging. The authors aimed to explain novel options for treating dementia with natural products and unravel some clinically proven natural products. This article systematically reviewed recent studies that have investigated the role of natural products and their bioactive compounds for dementia...
March 30, 2024: Heliyon
https://read.qxmd.com/read/38533040/comprehensive-single-cell-analysis-reveals-heterogeneity-of-fibroblast-subpopulations-in-ovarian-cancer-tissue-microenvironment
#39
JOURNAL ARTICLE
Bo Ding, Zheng Ye, Han Yin, Xin-Yi Hong, Song-Wei Feng, Jing-Yun Xu, Yang Shen
BACKGROUND: Ovarian cancer, as a highly malignant tumor, features the critical involvement of tumor-associated fibroblasts in the ovarian cancer tissue microenvironment. However, due to the apparent heterogeneity within fibroblast subpopulations, the specific functions of these subpopulations in the ovarian cancer tissue microenvironment remain insufficiently elucidated. METHODS: In this study, we integrated single-cell sequencing data from 32 ovarian cancer samples derived from four distinct cohorts and 3226 bulk RNA-seq data from GEO and TCGA-OV cohorts...
March 30, 2024: Heliyon
https://read.qxmd.com/read/38533033/elucidating-the-anti-cancer-potential-of-cinnamomum-tamala-essential-oil-against-non-small-cell-lung-cancer-a-multifaceted-approach-involving-gc-ms-profiling-network-pharmacology-and-molecular-dynamics-simulations
#40
JOURNAL ARTICLE
Debajani Mohanty, Sucheesmita Padhee, Arpita Priyadarshini, Bibhuti Bhusan Champati, Prabhat Kumar Das, Sudipta Jena, Ambika Sahoo, Pratap Chandra Panda, Sanghamitra Nayak, Asit Ray
Cinnamomum tamala (Buch.-Ham.) T.Nees & Eberm., or Indian Bay Leaf, is a well-known traditional ayurvedic medicine used to treat various ailments. However, the molecular mechanism of action of Cinnamomum tamala essential oil (CTEO) against non-small cell lung cancer (NSCLC) remains elusive. The present study aims to decipher the molecular targets and mechanism of CTEO in treating NSCLC. GC-MS analysis detected 49 constituents; 44 successfully passed the drug-likeness screening and were identified as active compounds...
March 30, 2024: Heliyon
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