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Topic Review
Biography
Topic Review
Antibody–Drug Conjugates for Non-Oncological Applications
Typically, antibody–drug conjugates (ADCs) are made up of a humanized antibody and a small-molecule medication connected by a chemical linker. ADCs’ ability to deliver cytotoxic agents to the specific site with reduced side effects showed promising results in oncology. Inspired by these outcomes, scientists explored the potential of antibody–drug conjugates in non-oncological conditions such as arthritis, myasthenia gravis, immunological disorders, and kidney failure.
616
07 Jul 2023
Topic Review
Effects of Rhein on the Kidney
Rhein is a monomeric component of anthraquinone isolated from rhubarb, a traditional Chinese medicine. It has anti-inflflammation, anti-oxidation, anti-apoptosis, anti-bacterial and other pharmacological activities, as well as a renal protective effects. Rhein exerts its nephroprotective effects mainly through decreasing hypoglycemic and hypolipidemic, playing anti-inflflammatory, antioxidant and anti-fifibrotic effects and regulating drug-transporters. However, the latest studies show that rhein also has potential kidney toxicity in case of large dosages and long use times.
613
02 Dec 2022
Topic Review
Insights into the Pharmacological Effects of Flavonoids
Flavonoids are widely occurring secondary metabolites of plants. Currently, there is a trend of article numbers increasing, which focuses on the computer modeling of flavonoid interactions with biological targets. Such studies help to accumulatethe data on lead compounds that can find medicinal implementation, including COVID-19. Flavanonol taxifolin demonstrated wound-healing activity. Luteolin, apigenin, and wogonin, which can be classified as flavones, show induced neutrophil apoptosis and have potential as neutrophil apoptosis-inducing anti-inflammatory, proresolution agents.
610
10 Jun 2022
Topic Review
Peer Reviewed
Biofunctional Peptide FNIII14: Therapeutic Potential
Biofunctional peptide FNIII14, which is derived from the 14th fibronectin (FN) type III-like (FN-III) repeat of FN molecule, is capable of inhibiting cell adhesion to the extracellular matrix (ECM). This functional site is usually buried within the molecular structure of FN, but can be exposed by conformational changes and proteolytic cleavage. Peptide FNIII14 can induce a conformational change in β1-integrin from the active to the inactive form, causing functional inactivation. Based on this anti-adhesive activity, peptide FNIII14 exhibits therapeutic potential for several diseases such as metabolic diseases, organ fibrosis, and malignant tumors. Peptide FNIII14 blocks integrin-mediated signaling by a mechanism entirely distinct from that of conventional antagonisitic peptides, including Arg-Gly-Asp peptides that competitively inhibit the ECM binding of integrin.
583
13 Apr 2022
Topic Review
Aripiprazole Lauroxil
Aripiprazole lauroxil is a prodrug of aripiprazole and is administered as an intramuscular injection. Once administered, aripiprazole lauroxil is first converted to N-hydroxymethyl aripiprazole by enzyme-mediated hydrolysis and is hydrolyzed again to aripiprazole. Aripiprazole was originally reported to be a partial agonist at D2and 5HT1Areceptors, with a combination of antagonistic activity at 5HT2Areceptors.
609
18 Jul 2021
Topic Review
Food Polyphenols and Type II Diabetes Mellitus
Type II diabetes mellitus and its related complications are growing public health problems. Many natural products present in our diet, including polyphenols, can be used in treating and managing type II diabetes mellitus and different diseases, owing to their numerous biological properties. Anthocyanins, flavonols, stilbenes, curcuminoids, hesperidin, hesperetin, naringenin, and phenolic acids are common polyphenols found in blueberries, chokeberries, sea-buckthorn, mulberries, turmeric, citrus fruits, and cereals. These compounds exhibit antidiabetic effects through different pathways.
609
22 May 2023
Topic Review
Hydrodynamic Delivery
The principle of hydrodynamic delivery was initially used to develop a method for delivering plasmids into mouse hepatocytes through tail vein injection and has since been expanded for use in delivering various biologically active materials to cells in different organs of several animal species.
608
18 Apr 2023
Topic Review
Antiarrhythmic Drugs on Antiepileptic Drug Action
Severe cardiac arrhythmias developing in the course of seizures increase the risk of SUDEP (sudden unexpected death in epilepsy). Hence, epilepsy patients with pre-existing arrhythmias should receive appropriate pharmacotherapy. Concomitant treatment with antiarrhythmic and antiseizure medications creates, however, the possibility of drug–drug interactions. This is due, among other reasons, to a similar mechanism of action. Both groups of drugs inhibit the conduction of electrical impulses in excitable tissues.
608
28 Mar 2022
Topic Review
Combination Therapy for Glioblastoma
Aggressive glioblastoma (GBM) has no known treatment as a primary brain tumor. Since the cancer is so heterogeneous, an immunosuppressive tumor microenvironment (TME) exists, and the blood–brain barrier (BBB) prevents chemotherapeutic chemicals from reaching the central nervous system (CNS), therapeutic success for GBM has been restricted. Drug delivery based on nanocarriers and nanotechnology has the potential to be a handy tool in the continuing effort to combat the challenges of treating GBM. Combination therapies may be enhanced by using nanotechnology-based delivery techniques. Nano-chemotherapy, nano-chemotherapy–radiation, nano-chemotherapy–phototherapy, and nano-chemotherapy–immunotherapy for GBM.
607
02 Nov 2022
Topic Review
Anti-Leishmania Drug Delivery Systems
Two series of new hybrid γ/γ-peptides, γ-CC and γ-CT, formed by (1S,2R)-3-amino-2,2-dimethylcyclobutane-1-carboxylic acid joined in alternation to a Nα-functionalized cis- or trans-γ-amino-L-proline derivative, respectively, have been synthesized and evaluated as cell penetrating peptides (CPP) and as selective vectors for anti-Leishmania drug delivery systems (DDS). They lacked cytotoxicity on the tumoral human cell line HeLa with a moderate cell-uptake on these cells. In contrast, both γ-CC and γ-CT tetradecamers were microbicidal on the protozoan parasite Leishmania beyond 25 μM, with significant intracellular accumulation. They were conjugated to fluorescent doxorubicin (Dox) as a standard drug showing toxicity beyond 1 μM, while free Dox was not toxic. Intracellular accumulation was 2.5 higher than with Dox-TAT conjugate (TAT = transactivator of transcription, taken as a standard CPP). The conformational structure of the conjugates was approached both by circular dichroism spectroscopy and molecular dynamics simulations. Altogether, computational calculations predict that the drug-γ-peptide conjugates adopt conformations that bury the Dox moiety into a cavity of the folded peptide, while the positively charged guanidinium groups face the solvent. The favorable charge/hydrophobicity balance in these CPP improves the solubility of Dox in aqueous media, as well as translocation across cell membranes, making them promising candidates for DDS.
605
20 Oct 2020
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