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About 43,688 results

Two for the price of one: itaconate and its derivatives as an anti-infective and anti-i...
https://doi.org/10.1016/j.coi.2022.102268
Current Opinion in Immunology; McGettrick AF, O'Neill LA

Nov 30th, 2022 - The metabolite itaconate (ITA) and its derivatives, both chemically synthesized and endogenous, have emerged as immunoregulators, with roles in limiting inflammation but also having effects on bacterial and viral infection. Some members of the ITA family have been shown to target and inhibit multiple processes in macrophages with recently identified targets, including NLRP3, JAK1, ten-eleven tr...

Pregnancy outcomes after first-trimester treatment with artemisinin derivatives versus ...
https://doi.org/10.1016/S0140-6736(22)01881-5
Lancet (London, England); Saito M, McGready R et. al.

Nov 29th, 2022 - Malaria in the first trimester of pregnancy is associated with adverse pregnancy outcomes. Artemisinin-based combination therapies (ACTs) are a highly effective, first-line treatment for uncomplicated Plasmodium falciparum malaria, except in the first trimester of pregnancy, when quinine with clindamycin is recommended due to concerns about the potential embryotoxicity of artemisinins. We compa...

Potential SARS-CoV-2 RdRp inhibitors of cytidine derivatives: Molecular docking, molecu...
https://doi.org/10.1371/journal.pone.0273256
PloS One; M A Kawsar S, Hosen MA et. al.

Nov 29th, 2022 - The RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 is one of the optimum targets for antiviral drug design and development. The hydroxyl groups of cytidine structures were modified with different aliphatic and aromatic groups to obtain 5´-O-acyl and 2´,3´-di-O-acyl derivatives, and then, these derivatives were employed in molecular modeling, antiviral prediction, molecular docking, molecular...

Metabolite profiling, antifungal, biofilm formation prevention and disruption of mature...
https://doi.org/10.1371/journal.pone.0278096
PloS One; Harley BK, Quagraine AM et. al.

Nov 29th, 2022 - The antifungal activity of the 70% ethanol stem bark extract of Erythrina senegalensis (ESB) against different strains and drug resistant clinical isolates of Candida albicans and Candida glabrata were evaluated in the study. The effect of ESB on biofilms as well as its activity in combination with fluconazole, nystatin or caspofungin against the Candida strains were also evaluated. We then eva...

Riluzole and novel naphthalenyl substituted aminothiazole derivatives prevent acute neu...
https://doi.org/10.1016/j.neuropharm.2022.109349
Neuropharmacology Kyllo T, Singh V et. al.

Nov 28th, 2022 - Epileptogenic seizures, or status epilepticus (SE), leads to excitotoxic injury in hippocampal and limbic neurons in the kainic acid (KA) animal model of temporal lobe epilepsy (TLE). Here, we have further characterized neural activity regulated methylaminoisobutryic acid (MeAIB)/glutamine transport activity in mature rat hippocampal neurons in vitro that is inhibited by riluzole (IC50 = 1μM), ...

Impatiens balsamina: An updated review on the ethnobotanical uses, phytochemistry, and ...
https://doi.org/10.1016/j.jep.2022.115956
Journal of Ethnopharmacology; Qian HQ, Wang B et. al.

Nov 28th, 2022 - Impatiens balsamina is an annual herb of the Balsaminaceae family, which is cultivated extensively in Asia as an ornamental plant. Notably, as a folk medicine, I. balsamina has been long prescribed for the treatment of rheumatism, isthmus, generalized pain, fractures, inflammation of the nails, scurvy, carbuncles, dysentery, bruises, foot diseases, etc. AIM OF THE STUDY: The paper overviews com...

Evaluation of developmental toxicity in zebrafish embryos and antiproliferative potenti...
https://doi.org/10.1016/j.taap.2022.116325
Toxicology and Applied Pharmacology; Szopa A, Herbet M et. al.

Nov 28th, 2022 - The aim of the studies was to evaluate the antiproliferative potential against human tumor cell lines of newly synthetized derivatives containing 4-nitrophenyl group, as well as its impact on developmental toxicity in zebrafish model. We selected 1-(4-nitrobenzoyl)-4-ethylsemicarbazide (APS-1) and 1-[(4-nitrophenyl)acetyl]-4-hexyl-thiosemicarbazide (APS-18) for research. The antiproliferative p...

Lactobacillus reuteri tryptophan metabolism promotes host susceptibility to CNS autoimm...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9685921
Microbiome Montgomery TL, Eckstrom K et. al.

Nov 25th, 2022 - Dysregulation of gut microbiota-associated tryptophan metabolism has been observed in patients with multiple sclerosis. However, defining direct mechanistic links between this apparent metabolic rewiring and individual constituents of the gut microbiota remains challenging. We and others have previously shown that colonization with the gut commensal and putative probiotic species, Lactobacillus...

JAK-STAT signaling in inflammatory breast cancer enables chemotherapy-resistant cell st...
https://doi.org/10.1158/0008-5472.CAN-22-0423
Cancer Research; Stevens LE, Peluffo G et. al.

Nov 22nd, 2022 - Inflammatory breast cancer (IBC) is a difficult-to-treat disease with poor clinical outcomes due to high risk of metastasis and resistance to treatment. In breast cancer, CD44+CD24- cells possess stem cell-like features and contribute to disease progression, and we previously described a CD44+CD24-pSTAT3+ breast cancer cell subpopulation that is dependent on JAK2/STAT3 signaling. Here we report...

Identification of novel F508del-CFTR traffic correctors among triazole derivatives.
https://doi.org/10.1016/j.ejphar.2022.175396
European Journal of Pharmacology; Bacalhau M, Ferreira FC et. al.

Nov 22nd, 2022 - The most prevalent cystic fibrosis (CF)-causing mutation - F508del - impairs the folding of CFTR protein, resulting in its defective trafficking and premature degradation. Small molecules termed correctors may rescue F508del-CFTR and therefore constitute promising pharmacotherapies acting on the fundamental cause of the disease. Here, we screened a collection of triazole compounds to identify n...

Selective and reversible disruption of mitochondrial inner membrane protein complexes b...
https://doi.org/10.1016/j.mito.2022.11.006
Mitochondrion Kafkova A, Tilokani L et. al.

Nov 20th, 2022 - Triphenylphosphonium (TPP) derivatives are commonly used to target chemical into mitochondria. We show that alkyl-TPP cause reversible, dose- and hydrophobicity-dependent alterations of mitochondrial morphology and function and a selective decrease of mitochondrial inner membrane proteins including subunits of the respiratory chain complexes, as well as components of the mitochondrial calcium u...

Label-free affinity screening, design and synthesis of inhibitors targeting the Mycobac...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9671377
PloS One; Kim HB, Bacik JP et. al.

Nov 18th, 2022 - The ability of Mycobacterium tuberculosis (Mtb) to persist in its host may enable an evolutionary advantage for drug resistant variants to emerge. A potential strategy to prevent persistence and gain drug efficacy is to directly target the activity of enzymes that are crucial for persistence. We present a method for expedited discovery and structure-based design of lead compounds by targeting t...

Many or too many progesterone membrane receptors? Clinical implications.
https://doi.org/10.1016/j.tem.2022.10.001
Trends in Endocrinology and Metabolism: TEM; Wendler A, Wehling M

Nov 18th, 2022 - Several receptors for nongenomically initiated actions of progesterone (P4) exist, namely membrane-associated P4 receptors (MAPRs), membrane progestin receptors (mPRs), receptors for neurosteroids [GABAA receptor (GABAAR), NMDA receptor, sigma-1 and -2 receptors (S1R/S2R)], the classical genomic P4 receptor (PGR), and α/β hydrolase domain-containing protein 2 (ABHD2). Two drugs related to this ...

The cure rate after different treatments for mucosal leishmaniasis in the Americas: A s...
https://doi.org/10.1371/journal.pntd.0010931
PLoS Neglected Tropical Diseases; Carvalho JP, Silva SN et. al.

Nov 18th, 2022 - Mucosal or mucocutaneous leishmaniasis is the most severe form of tegumentary leishmaniasis due to its destructive character and potential damage to respiratory and digestive tracts. The current treatment recommendations are based on low or very low-quality evidence, and pentavalent antimonial derivatives remain strongly recommended. The aim of this review was to update the evidence and estimat...

Phytonadione - phytonadione injection, emulsion-Henry Schein, Inc.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1cf90be3-a744-4db5-999d-a84c67372304

Nov 14th, 2022 - Phytonadione injectable emulsion, USP is indicated in the following coagulation disorders which are due to faulty formation of factors II, VII, IX and X when caused by Vitamin K deficiency or interference with Vitamin K activity. Phytonadione injectable emulsion is indicated in­­  anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives; prophylaxis and therapy...

Midazolam hydrochloride - midazolam hydrochloride injection, solution-Gland Pharma Limited
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=23f4df96-1151-4815-8f01-4d79e5aa2145

Nov 11th, 2022 - Boxed Warning Section Personnel and Equipment for Monitoring and Resuscitation Adults and Pediatrics: Intravenous midazolam hydrochloride has been associated with respiratory depression and respiratory arrest, especially when used for sedation in noncritical care settings. In some cases, where this was not recognized promptly and treated effectively, death or hypoxic encephalopathy has resulted...

Cyclodextrins applied to the treatment of lysosomal storage disorders.
https://doi.org/10.1016/j.addr.2022.114617
Advanced Drug Delivery Reviews; Ishitsuka Y, Irie T et. al.

Nov 11th, 2022 - Cyclodextrin (CD), a cyclic oligosaccharide, is a pharmaceutical additive that improves the solubility of hydrophobic compounds. Recent research has focused on the potential active pharmaceutical abilities of CD. Lysosomal storage diseases are inherited metabolic diseases characterized by lysosomal dysfunction and abnormal lipid storage. Niemann-Pick disease type C (NPC) is caused by mutations ...

The in silico and in vitro analysis of donepezil derivatives for Anopheles acetylcholin...
https://doi.org/10.1371/journal.pone.0277363
PloS One; Rants'o TA, van Greunen DG et. al.

Nov 10th, 2022 - Current studies on Anopheles anticholinesterase insecticides are focusing on identifying agents with high selectivity towards Anopheles over mammalian targets. Acetylcholinesterase (AChE) from electric eel is often used as the bioequivalent enzyme to study ligands designed for activity and inhibition in human. In this study, previously identified derivatives of a potent AChE, donepezil, that ha...

A mini-review: environmental and metabolic factors affecting aminoglycoside efficacy.
https://doi.org/10.1007/s11274-022-03445-8
World Journal of Microbiology & Biotechnology; Webster CM, Shepherd M

Nov 10th, 2022 - Following the discovery of streptomycin from Streptomyces griseus in the 1940s by Selman Waksman and colleagues, aminoglycosides were first used to treat tuberculosis and then numerous derivatives have since been used to combat a wide variety of bacterial infections. These bactericidal antibiotics were used as first-line treatments for several decades but were largely replaced by ß-lactams and ...

Risperidone - risperidone tablet-Aphena Pharma Solutions - Tennessee, LLC
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=bda104ac-1eea-4a1a-836a-24bcc034b90f

Nov 9th, 2022 - RECENT MAJOR CHANGES SECTION Warnings and Precautions (5.4) 07/2018 Boxed Warning Section Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Risperidone tablets are not approved for the treatment of patients with dementia-related psychosis. [see Warnings and Precautions (5.1)] WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WI...