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Topic Review
Antitumour Activity of Natural Products Containing Isoxazole/Isoxazoline Moiety
Isoxazoles and isoxazolines are five-membered heterocyclic molecules containing nitrogen and oxygen. Isoxazole and isoxazoline are the most popular heterocyclic compounds for developing novel drug candidates. As biosynthetic technology has advanced, A growing number of natural products are being developed for cancer therapy as clinical candidates. As a result, scientists have created several isoxazole and isoxazoline derivatives with anti-cancer properties based on natural products.
  • 721
  • 09 Feb 2023
Topic Review
Nanosystems for Brain Drug Delivery
Antipsychotic drugs have numerous disabling side effects, and many are lipophilic, making them hard to formulate at high strength. Incorporating them into nanometric emulsions can increase their solubility, protect them from degradation, and increase their brain delivery, being a promising strategy to overcome the current treatment gap.
  • 719
  • 09 Nov 2022
Topic Review
Lipopolysaccharide, Inflammation and Mitochondria-Targeted Antioxidants
Lipopolysaccharide (LPS), the major component of the outer membrane of Gram-negative bacteria, is the most abundant proinflammatory agent. Considerable evidence indicates that LPS challenge inescapably causes oxidative stress and mitochondrial dysfunction, leading to cell and tissue damage. Increased mitochondrial reactive oxygen species (mtROS) generation triggered by LPS is known to play a key role in the progression of the inflammatory response. mtROS at excessive levels impair electron transport chain functioning, reduce the mitochondrial membrane potential, and initiate lipid peroxidation and oxidative damage of mitochondrial proteins and mtDNA. Over the past 20 years, a large number of mitochondria-targeted antioxidants (mito-AOX) of different structures that can accumulate inside mitochondria and scavenge free radicals have been synthesized. Their protective role based on the prevention of oxidative stress and the restoration of mitochondrial function has been demonstrated in a variety of common diseases and pathological states.
  • 718
  • 16 Apr 2021
Topic Review
Microfluidic for Cutaneous Wound Healing
Cutaneous wound healing is a complex, multi-stage process involving direct and indirect cell communication events with the aim of efficiently restoring the barrier function of the skin. One key aspect in cutaneous wound healing is associated with cell movement and migration into the physically, chemically, and biologically injured area, resulting in wound closure. Understanding the conditions under which cell migration is impaired and elucidating the cellular and molecular mechanisms that improve healing dynamics are therefore crucial in devising novel therapeutic strategies to elevate patient suffering, reduce scaring, and eliminate chronic wounds. Following the global trend towards the automation, miniaturization, and integration of cell-based assays into microphysiological systems, conventional wound healing assays such as the scratch assay and cell exclusion assay have recently been translated and improved using microfluidics and lab-on-a-chip technologies. These miniaturized cell analysis systems allow for precise spatial and temporal control over a range of dynamic microenvironmental factors including shear stress, biochemical and oxygen gradients to create more reliable in vitro models that resemble the in vivo microenvironment of a wound more closely on a molecular, cellular, and tissue level. 
  • 718
  • 08 Jun 2021
Topic Review
Pharmacological Interventions in Epilepsy
Epilepsy is a non-communicable disease of the brain that affects people of all ages. It is characterized by episodes of spontaneous and abnormal electrical activity in the brain. It is often accompanied by depression, anxiety, and substantially increased morbidity and mortality. A large number of third-generation antiepileptic drugs are available, but they have multiple side effects causing a decline in the quality of life. The inheritance and etiology of epilepsy are complex with multiple underlying genetic and epigenetic mechanisms. Different neurotransmitters play intricate functions to maintain the normal physiology of various neurons. 
  • 718
  • 06 Jul 2021
Topic Review
Nanoparticulate Drug Delivery Systems
Research into the application of nanocarriers in the delivery of cancer-fighting drugs has been a promising research area for decades. On the other hand, their cytotoxic effects on cells, low uptake efficiency, and therapeutic resistance have limited their therapeutic use. However, the urgency of pressing healthcare needs has resulted in the functionalization of nanoparticles’ (NPs) physicochemical properties to improve clinical outcomes of new, old, and repurposed drugs.
  • 717
  • 14 Jun 2022
Topic Review
Immunopotentiating Activity of Fucoidans
Fucoidans, discovered in 1913, are fucose-rich sulfated polysaccharides extracted mainly from brown seaweed. These versatile and nontoxic marine-origin heteropolysaccharides have a wide range of favorable biological activities, including antitumor, immunomodulatory, antiviral, antithrombotic, anticoagulant, antithrombotic, antioxidant, and lipid-lowering activities. In the early 1980s, fucoidans were first recognized for their role in supporting the immune response and later, in the 1990s, their effects on immune potentiation began to emerge. The understanding of the immunomodulatory effects of fucoidan has expanded significantly. The ability of fucoidan(s) to activate CTL-mediated cytotoxicity against cancer cells, strong antitumor property, and robust safety profile make fucoidans desirable for effective cancer immunotherapy.
  • 717
  • 06 May 2023
Topic Review
Animal Lectins
Animal lectins are proteins with carbohydrate recognition activity. Galectins, the β-galactoside binding lectins, are expressed in various cells and have been reported to regulate several immunological and physiological responses. Recently, some galectins have been reported to regulate some viral infections, including influenza A virus (IAV); however, the mechanism is still not fully understood.
  • 715
  • 31 May 2021
Topic Review
Resveratrol from Dietary Supplement to a Drug Candidate
Resveratrol (RVT) is a well known phyto-chemical and is widely used in dietary supplements and botanical products. It shows a wide range of pharmacological/beneficial effects. it can be a potential candidate to be developed as phyto-pharmaceutical. Multiple diseases are reported to be treated by the therapeutic effect of RVT since it has antioxidant, anti-cancer activity and anti-inflammatory activities. It also has a major role in diabetes, arthritis, cardiac disorder and platelet aggregation etc. The major requirements are establishments regarding safety, efficacy profile and physicochemical characterization. 
  • 715
  • 29 Aug 2022
Topic Review
Traditional Medicinal Uses of Yingzhao
The medicinal plant Artabotrys hexapetalus (synonyms: A.uncinatus and A. odoratissimus) is known as yingzhao in Chinese. Extracts of the plant have long been used in Asian folk medicine to treat various symptoms and diseases, including fevers, microbial infections, ulcers, hepatic disorders and other health problems. In particular, extracts from the roots and fruits of the plant are used for treating malaria. Numerous bioactive natural products have been isolated from the plant, mainly aporphine (artabonatines, artacinatine) and benzylisoquinoline (hexapetalines) alkaloids, terpenoids (artaboterpenoids), flavonoids (artabotrysides), butanolides (uncinine, artapetalins) and a small series of endoperoxides known as yingzhaosu A-to-D. These natural products confer antioxidant, anti-inflammatory and antiproliferative properties to the plant extracts. The lead compound yingzhaosu A displays marked activities against the malaria parasites Plasmodium falciparum and P. berghei.
  • 715
  • 27 Sep 2022
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.
  • 714
  • 28 Mar 2022
Topic Review
Dihydropyrimidine Dehydrogenase (DPD) Pharmacogenetics
The dihydropyrimidine dehydrogenase (DPD), encoded by the DPYD gene, is the enzyme mainly involved in the catabolism of fluoropyrimidines (FP). DPYD polymorphisms increase the risk of severe FP-related toxicity and DPYD-pharmacogenetics (DPYD-PGx) is recommended before starting the FP-based chemotherapy. Other factors influence FP safety, therefore phenotyping methods, such as measurement of plasmatic 5-fluorouracil (5-FU) clearance and DPD activity, could complement the DPYD-PGx. Here, authors reported eleven clinical cases in whom a combined genotyping/phenotyping approach, together with careful clinical monitoring was used to optimise the FP-based treatment.  In addition, authors performed a systematic review of the literature concerning the use of DPYD-PGx, together with phenotyping methods to personalise such a chemotherapy.
  • 714
  • 23 Mar 2021
Topic Review
DDS Based on Polysaccharides
Polysaccharides are polymeric carbohydrates composed of repeating monomeric units of monosaccharides that are covalently linked to each other through glucosidic linkage. Polysaccharides are biocompatible, biodegradable biopolymers, and the presence of various functional groups, such as hydroxyl, carboxyl, and amino groups, allow their easy chemical modification in order to increase their intrinsic properties (solubility, chemical stability, etc.). Due to these improved properties, polysaccharides are largely used as biomaterials in food, biomedical, pharmaceutical, cosmetic industry, and also as micellar drug-loaded systems. 
  • 713
  • 12 Apr 2021
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. 
  • 713
  • 02 Dec 2022
Topic Review
Sex Differences in Dopamine Receptors
Dopamine is an important neurotransmitter that plays a key role in neuropsychiatric illness.
  • 712
  • 28 Sep 2021
Topic Review
Development of Trichosanthin
Tian Hua Fen, a herbal powder extract that contains trichosanthin (TCS), was used as an abortifacient in traditional Chinese medicine. In 1972, TCS was purified to alleviate the side effects. Because of its clinical applications, TCS became one of the most active research areas in the 1960s to the 1980s in China. These include obtaining the sequence information in the 1980s and the crystal structure in 1995. The replication block of TCS on human immunodeficiency virus in lymphocytes and macrophages was found in 1989 and started a new chapter of its development.
  • 712
  • 21 Mar 2022
Biography
Carlos M. Villalón
Carlos M. Villalón was born in Mexico City on November 2, 1959. He completed his studies in Chemistry & Pharmacy (Pharmacist) in 1983 at the National School of Biological Sciences (IPN), and his postgraduate studies at the Department of Pharmacology and Toxicology of Cinvestav (M.Sc. in 1986 and Ph.D. in 1988). Between 1988 and 1991 he did a postdoctoral stay at the Erasmus Universiteit Rotterd
  • 712
  • 18 Jul 2023
Topic Review
Ascorbic Acid against Chronic Diseases
Ascorbic acid (ASC) is a key nutrient that serves as an antioxidant and a cofactor for numerous enzymatic reactions. However, humans, unlike most mammals, are unable to synthesize it. Consequently, ASC must be obtained through dietary sources, especially fresh fruit and vegetables. The value of administering exogenous micronutrients, to reestablish antioxidant concentrations in patients with severe disease, has been recognized for decades. Despite the suggestion that ASC supplementation may reduce oxidative stress and prevent several chronic conditions, few large, randomized clinical trials have tested it in patients with severe illness. This article reviews the recent literature on the pharmacological profile of ASC and the role of its supplementation in critically ill patients.
  • 710
  • 11 Dec 2020
Topic Review
Organic Germanium Compounds
Germanium is an essential microelement, and its deficiency can result in numerous diseases, particularly oncogenic conditions. Consequently, water-soluble germanium compounds, including inorganic and coordination compounds, have attracted significant attention due to their biological activity. 
  • 709
  • 01 Jun 2023
Topic Review
Immunoproteasome
Proteasome inhibition is a promising strategy for the treatment of multiple myeloma; unfortunately, this disease is often associated with an increasing chemoresistance. One novel approach may be to target the immunoproteasome, a proteasomal isoform mainly present in cells of hematopoietic origin. We investigated the activity of a panel of amides against immunoproteasome core particles as potential agents for the treatment of multiple myeloma (MM). Amide 6 showed an ideal profile since it was able to inhibit both the chymotrypsin-like activities of the immunoproteasome with Ki values of 4.90 µM and 4.39 µM for β1i and β5i, respectively, coupled with an EC50 =17.8 µM against MM.1R cells. Compound 6 inhibited also ubiquitinated protein degradation and was able to act on different phases of MM cell cycle reducing the levels of cyclin A/CDK1, cyclin B/CDK1 and cyclin D/CDK4/6 complexes, which turns in cell cycle arrest.
  • 708
  • 03 Nov 2020
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