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Topic Review
Biography
Topic Review
Classification of Allosteric G-Protein-Coupled Receptors Regulators
Allosteric regulation is critical for the functioning of G-protein-coupled receptors (GPCRs) and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions, various biomolecules (lipids, amino acids, polypeptides, hormonal agents, etc.), and the peptide components of GPCR signaling. According to the ability to influence the basal and orthosteric/allosteric agonist-stimulated activity, the ligands of GPCR allosteric sites can be divided into the positive (PAM), negative (NAM), and silent (SAM) allosteric modulators, the allosteric full agonists, inverse agonists and neutral antagonists, as well as the allosteric regulators with the combined activity (ago-PAM, ago-NAM).
324
19 Apr 2023
Topic Review
Classes of Translational Readthrough-Inducing Drugs
Translational Readthrough-Inducing Drugs (TRIDs) can affect various biomolecular targets, leading to different types of readthrough.
560
11 Jan 2022
Topic Review
Circadian Clock to Skin /Cancer
Over the years, the circadian regulation of drug metabolism and processing has been employed in the treatment of a range of disease states, including diabetes, hypertension, peptic ulcers, and allergic rhinitis . There is also interest in using chronotherapeutic approaches for skin disease, including psoriasis and atopic dermatitis . Although time-dictated drug administration had been demonstrated many decades ago, its application in cancer treatment was limited due to insufficient mechanistic data supporting experimental results and inconsistency among clinical trials.
547
21 Jun 2021
Topic Review
Ciguatoxins in Fish
Ciguatoxins are very potent marine neurotoxins, that accumulate to toxic levels in edible fish in certain circumtropical areas, and are associated with ciguatera fish poisoning worldwide. Ciguatoxins are produced by specific benthic dinoflagellates, enter the marine food chain via herbivorous fish and invertebrates, and eventual are biotransformed in herbivorous, omnivorous, and carnivorous fishes to more poisonous forms. Ciguatoxins cause risks to human health at very low concentrations. To decrease the risk of ciguatera fish poisoning, it is important to know fishing areas with low concentrations of ciguatoxins, as well as to test fish tissue for toxins before consumption. Modern laboratories use several detection techniques, such as mouse bioassay, cell-based assays, receptor-binding assays, antibody-based immunoassays, electrochemical methods, and analytical techniques, to obtain information about the total toxicity of fish tissue samples, as well as to identify toxins and to determine the toxin profile. State-of-the-art ciguatoxin detection involves the combination of a cell-based assay or receptor-binding assay to screen total toxicity, and liquid chromatography coupled with mass spectrometry to confirm toxins and provide toxin profiles.
1.4K
25 Aug 2020
Topic Review
Chrysin
Pharmacological profile of phytochemicals has attracted much attention to their use in disease therapy. Since cancer is a major problem for public health with high mortality and morbidity worldwide, experiments have focused on revealing the anti-tumor activity of natural products. Flavonoids comprise a large family of natural products with different categories. Chrysin is a hydroxylated flavonoid belonging to the flavone category. Chrysin has demonstrated great potential in treating different disorders, due to possessing biological and therapeutic activities, such as antioxidant, anti-inflammatory, hepatoprotective, neuroprotective, etc. Over recent years, the anti-tumor activity of chrysin has been investigated, and in the present review, we provide a mechanistic discussion of the inhibitory effect of chrysin on proliferation and invasion of different cancer cells. Molecular pathways, such as Notch1, microRNAs, signal transducer and activator of transcription 3 (STAT3), nuclear factor-kappaB (NF-κB), PI3K/Akt, MAPK, etc., as targets of chrysin are discussed. The efficiency of chrysin in promoting anti-tumor activity of chemotherapeutic agents and suppressing drug resistance is described. Moreover, poor bioavailability, as one of the drawbacks of chrysin, is improved using various nanocarriers, such as micelles, polymeric nanoparticles, etc. This updated review will provide a direction for further studies in evaluating the anti-tumor activity of chrysin.
1.9K
13 Oct 2020
Topic Review
Chronicles of Nanoerythrosomes
Nanoerythrosomes (NERs) are the carrier erythrocytes (C-ERs) which are recognized as modern day, novel, and smart drug delivery systems associated with increased bioavailability, improved pharmacokinetics, and low toxicity.
662
30 Apr 2021
Topic Review
Chronic Oral Methylphenidate Behavioral, Neurochemical and Developmental Effects
The majority of animal studies on methylphenidate (MP) use intraperitoneal (IP) injections, subcutaneous (SC) injections, or the oral gavage route of administration. While all these methods allow for delivery of MP, it is the oral route that is clinically relevant. IP injections commonly deliver an immediate and maximum dose of MP due to their quick absorption. This quick-localized effect can give timely results but will only display a small window of the psychostimulant’s effects on the animal model. On the opposite side of the spectrum, a SC injection does not accurately represent the pathophysiology of an oral exposure because the metabolic rate of the drug would be much slower. The oral-gavage method, while providing an oral route, possesses some adverse effects such as potential animal injury and can be stressful to the animal compared to voluntary drinking. It is thus important to allow the animal to have free consumption of MP, and drinking it to more accurately mirror human treatment. The use of a two-bottle drinking method allows for this. Rodents typically have a faster metabolism than humans, which means this needs to be considered when administering MP orally while reaching target pharmacokinetic levels in plasma.
267
31 Mar 2023
Topic Review
Chronic Obstructive Pulmonary Disease (COPD)
Chronic obstructive pulmonary disease (COPD) is a lung disease primarily characterized by the presence of airflow limitation and inflammation, due to elevated inflammatory cells, especially neutrophils, in the lungs.
553
26 May 2021
Topic Review
Chromium
Chromium (Cr) is a common element in the Earth’s crust. It may exist in different oxidation states, Cr(0), Cr(III) and Cr(VI), with Cr(III) and Cr(VI) being relatively stable and largely predominant. Chromium’s peculiarity is that its behavior relies on its valence state. Cr(III) is a trace element in humans and plays a major role in glucose and fat metabolism. The beneficial effects of Cr(III) in obesity and types 2 diabetes are known. It has been long considered an essential element, but now it has been reclassified as a nutritional supplement. On the other hand, Cr(VI) is a human carcinogen and exposure to it occurs both in occupational and environmental contexts. It induces also epigenetic effects on DNA, histone tails and microRNA; its toxicity seems to be related to its higher mobility in soil and swifter penetration through cell membranes than Cr(III). The microorganisms Acinetobacter sp. Cr1 and Pseudomonas sp. Cr13 have been suggested as a promising agent for bioremediation of Cr(VI).
1.7K
22 Feb 2021
Topic Review
Chromatographic Techniques in Pharmaceutical Analysis
High-performance liquid chromatography (HPLC) is an incredibly universal tool, especially when combined with different detectors, such as UV-Visible spectroscopy, mass spectrometry (MS), and fluorescence detection for numerous active ingredients in different pharmaceutical formulations without interferences from other excipients. TLC, in combination with densitometry, is a very efficient tool for the determination of biologically active substances present in pharmaceutical preparations. In addition, TLC coupled to densitometry and mass spectrometry could be suitable for preliminary screening and determination of the biological activity (e.g., antioxidant properties, thin layer chromatography (TLC) by 2,2-diphenyl-1-picrylhydrazyl (DPPH) method) of plant materials. Gas chromatography, coupled with a mass spectrometer (GC-MS, GC-MS/MS), is of particular importance in the testing of any volatile substances, such as essential oils. LC, coupled to NMR and MS, is the best solution for identifying and studying the structure of unknown components from plant extracts, as well as degradation products (DPs). Thanks to size-exclusion chromatography, coupled to multi-angle light scattering, the quality control of biological pharmaceuticals is possible.
3.1K
26 Apr 2022
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