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Topic Review
Synthesis of Metal Complexes of 2-Thiouracil and Derivatives
The thionamide antithyroid agents were discovered largely through observations carried out by various researchers in the 1940s that found that sulfhydryl-containing substances were goitrogenic in animals. Prof. Edwin B. Astwood started using these drugs to treat hyperthyroidism. The development background of these agents, the coordination possibility of 2-thiouracil and its derivatives are presented herein.
  • 1.7K
  • 12 Apr 2024
Topic Review
Anthocyanins and Hepatoprotection
Anthocyanins are water-soluble, colored compounds of the flavonoid class, abundantly found in the fruits, leaves, roots, and other parts of the plants. The fruit berries are prime sources and exhibit different colors. The anthocyanins utility as traditional medicament for liver protection and cure, and importance as strongest plants-based anti-oxidants have conferred these plants products different biological activities. These activities include anti-inflammation, liver protective, analgesic, and anti-cancers, which have provided the anthocyanins an immense commercial value, and has impelled their chemistry, biological activity, isolation, and quality investigations as prime focus. 
  • 1.7K
  • 11 Mar 2022
Topic Review
Heteronuclear Metal Complexes with Anticancer Activity
Transition metal complexes have been deeply studied for different applications, such as catalysis, antimicrobial, and also antitumoral drugs. Platinum complexes are probably the most well-known and studied in the field of anticancer compounds, also thanks to the omnipresence of cisplatin and its derivatives as a starting point. Two promising new strategies to increase the efficacy of transition metal-based complexes have been described. First, the possibility of assembling two biologically active fragments containing different metal centres into the same molecule were considered, thus obtaining a heterobimetallic complex. Secondly, the conjugation of metal-based complexes to a targeting moiety was discussed.
  • 1.6K
  • 09 Jan 2023
Topic Review
Polymeric Nanoparticles in Cardiovascular Diseases
Nanoparticles, including biodegradable polymeric nanoparticles, are able to increase the efficiency and reduce the degradability of natural polyphenols, thus increasing their beneficial abilities in the target tissues. Resveratrol-, quercetin-, or curcumin-loaded polymeric nanoparticles have been shown to markedly reduce reactive oxygen species formation, the inflammatory process, apoptosis, lipid peroxidation, cardiac hypertrophy, and even to delay myocardium injury due to ischemia/reperfusion. Thus, polymeric nanoparticles represent a promising tool for the delivery of natural polyphenols to target tissues and enhance their desirable effects in the cardiovascular system.
  • 1.6K
  • 27 Oct 2020
Topic Review
Bioavailability of Lingonberry Polyphenols
Lingonberry (Vaccinium vitis-idaea) is less prevalent in the daily human diet because they are collected from the wild, and plant breeding of lingonberry is still on a small scale. Lingonberries are classed as “superfruits” with the highest content of antioxidants among berries and a broad range of health-promoting effects. Many studies showed various beneficial effects of lingonberries, such as anti-inflammatory, antioxidant, and anticancer activities. Lingonberries have been shown to prevent low-grade inflammation and diet-induced obesity in diabetic animals. Moreover, lingonberry intake has been associated with a beneficial effect on preventing and treating brain aging and neurodegenerative disorders.
  • 1.6K
  • 03 Jun 2021
Topic Review
Gold Nanoparticles Functionalized with Natural Compounds from Plants
Biosynthesis of gold nanoparticles (AuNPs) has been widely studied and described. In the age of bacterial drug resistance, an intensive search for new agents with antibacterial properties or a new form of antibiotics with effective action is necessary.
  • 1.6K
  • 12 Dec 2022
Topic Review
Deep Eutectic Systems as Alternative Solvents
Chemists in the medicinal chemistry field are constantly searching for alternatives towards more sustainable and eco-friendly processes for the design and synthesis of drug candidates. The pharmaceutical industry is one of the most polluting industries, having a high E-factor, which is driving the adoption of more sustainable processes not only for new drug candidates, but also in the production of well-established active pharmaceutical ingredients. Deep eutectic systems (DESs) have emerged as a greener alternative to ionic liquids, and their potential to substitute traditional organic solvents in drug discovery has raised interest among scientists. 
  • 1.6K
  • 28 Feb 2024
Topic Review
Molecular Hybrids Targeting Tubulin Polymerization
Microtubules are cylindrical protein polymers formed from αβ-tubulin heterodimers in the cytoplasm of eukaryotic cells. Microtubule disturbance may cause cell cycle arrest in the G2/M phase, and anomalous mitotic spindles will form. Microtubules are an important target for cancer drug action because of their critical role in mitosis. Several microtubule-targeting agents with vast therapeutic advantages have been developed, but they often lead to multidrug resistance and adverse side effects. Thus, single-target therapy has drawbacks in the effective control of tubulin polymerization. Molecular hybridization, based on the amalgamation of two or more pharmacophores of bioactive conjugates to engender a single molecular structure with enhanced pharmacokinetics and biological activity, compared to their parent molecules, has recently become a promising approach in drug development. The practical application of combined active scaffolds targeting tubulin polymerization inhibitors has been corroborated in the past few years
  • 1.6K
  • 12 Apr 2022
Topic Review
Classification and Chemistry of Elephant Apple
Elephant apple (Dillenia indica L.) grows wild in Southeast Asia’s forests, including in China, India, Nepal, Bangladesh, and Sri Lanka. Elephant apples are considered essential fruit crops because of their high nutritional value, which includes high levels of vitamin C, carbohydrates, fats, fibre, protein, minerals, and fatty acids. It is important to understand the nutritional value and health benefits of elephant apples in order to increase fruit intake in people’s daily diets.
  • 1.6K
  • 17 Aug 2023
Topic Review
Skin Photoprotection by Polyphenols
Polyphenols are phytochemicals with proven antioxidant and antiinflammatory properties. Premature aging and UV-induced skin conditions could be better overcome by topical polyphenols nanoformulations. Further, polyphenols nanoformulations can be of great interest for the cosmetic industries and any individuals who want to improve their skin appearance. Examples in this regard are provided and the potential toxicity issues related to the use of nanomaterials are highlighted.
  • 1.6K
  • 26 Nov 2020
Topic Review
Macrolides
Macrolides are a diverse class of hydrophobic compounds characterized by a macrocyclic lactone ring and distinguished by variable side chains/groups. Some of the most well characterized macrolides are toxins produced by marine bacteria, sea sponges, and other species. Many marine macrolide toxins act as biomimetic molecules to natural actin-binding proteins, affecting actin polymerization, while other toxins act on different cytoskeletal components. The disruption of natural cytoskeletal processes affects cell motility and cytokinesis, and can result in cellular death. While many macrolides are toxic in nature, others have been shown to display therapeutic properties. Indeed, some of the most well known antibiotic compounds, including erythromycin, are macrolides. In addition to antibiotic properties, macrolides have been shown to display antiviral, antiparasitic, antifungal, and immunosuppressive actions.
  • 1.6K
  • 03 Jun 2021
Topic Review
Proteasome Inhibitors
Proteasome inhibitors have shown relevant clinical activity in several hematological malignancies, namely in multiple myeloma and mantle cell lymphoma, improving patient outcomes such as survival and quality of life, when compared with other therapies. However, initial response to the therapy is a challenge as most patients show an innate resistance to proteasome inhibitors, and those that respond to the therapy usually develop late relapses suggesting the development of acquired resistance. The mechanisms of resistance to proteasome inhibition are still controversial and scarce in the literature.
  • 1.6K
  • 18 Apr 2022
Topic Review
Supramolecular Hydrogels for Protein Delivery
Therapeutic proteins, such as growth factors (GFs), have been used in tissue engineering (TE) approaches for their ability to provide signals to cells and orchestrate the formation of functional tissue. However, to be effective and minimize off-target effects, GFs should be delivered at the target site with temporal control. In addition, protein drugs are typically sensitive water soluble macromolecules with delicate structure. As such, hydrogels, containing large amounts of water, provide a compatible environment for the direct incorporation of proteins within the hydrogel network, while their release rate can be tuned by engineering the network chemistry and density. Being formed by transient crosslinks, afforded by non-covalent interactions, supramolecular hydrogels offer important advantages for protein delivery applications.
  • 1.6K
  • 04 Mar 2021
Topic Review
Ethiopian Anticancer Plants
This entry provides an overview on the active phytochemical constituents of twenty-seven medicinal plants that are traditionally used to manage cancer in Ethiopia. It is compiled and discusses the potential anticancer, antiproliferative, and cytotoxic agents based on the types of secondary metabolites, such as terpenoids, phenolic compounds, alkaloids, steroids, and lignans. Among the anticancer secondary metabolites reported in this review, only few have been isolated from plants that are originated and collected in Ethiopia, and the majority of compounds are reported from plants belonging to different areas of the world. Thus, based on the available bioactivity reports, extensive and more elaborate ethnopharmacology-based bioassay-guided studies have to be conducted on selected traditionally claimed Ethiopian anticancer plants, which inherited from a unique and diverse landscape, with the aim of opening a way forward to conduct anticancer drug discovery program.
  • 1.6K
  • 21 Oct 2020
Topic Review
Cholinergic Signaling and Epilepsy
Epilepsy is a common brain disorder characterized by recurrent epileptic seizures with neuronal hyperexcitability. Apart from the classical imbalance between excitatory glutamatergic transmission and inhibitory γ-aminobutyric acidergic transmission, cumulative evidence suggest that cholinergic signaling is crucially involved in the modulation of neural excitability and epilepsy.
  • 1.6K
  • 07 May 2021
Topic Review
Ligands for Alzheimer’s Disease therapy
Despite tremendous research efforts at every level, globally, there is still a lack of effectivedrugs for the treatment of Alzheimer's disease (AD). The biochemical mechanisms of this devastatingneurodegenerative disease are not yet clearly understood. This review analyses the relevance ofmultiple ligands in drug discovery for AD as a versatile toolbox for a polypharmacological approachto AD. Herein, we highlight major targets associated with AD, ranging from acetylcholine esterase(AChE), beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1), glycogen synthase kinase3 beta ( GSK-3β), N-methyl-D-aspartate (NMDA) receptor, monoamine oxidases (MAOs), metal ions inthe brain, 5-hydroxytryptamine (5-HT) receptors, the third subtype of histamine receptor (H3 receptor),to phosphodiesterases (PDEs), along with a summary of their respective relationship to the diseasenetwork. In addition, a multitarget strategy for AD is presented, based on reported milestones in thisarea and the recent progress that has been achieved with multitargeted-directed ligands (MTDLs).Finally, the latest publications referencing the enlarged panel of new biological targets for AD relatedto the microglia are highlighted. However, the question of how to find meaningful combinations oftargets for an MTDLs approach remains unanswered.
  • 1.6K
  • 04 Aug 2020
Topic Review
Molecular Hybridization of Alkaloids Using 1,2,3-Triazole-Based Click Chemistry
Alkaloids found in multiple species, known as ‘driver species’, are more likely to be included in early-stage drug development due to their high biodiversity compared to rare alkaloids. Many synthetic approaches have been employed to hybridize the natural alkaloids in drug development. Click chemistry is a highly efficient and versatile reaction targeting specific areas, making it a valuable tool for creating complex natural products and diverse molecular structures. It has been used to create hybrid alkaloids that address their limitations and serve as potential drugs that mimic natural products.
  • 1.6K
  • 22 Nov 2023
Topic Review
CNSL as a Source of Alzheimer's Drug Leads
Cashew nut shell liquid (CNSL), a natural oil and a byproduct of cashew nut food processing, with a high content of phenolic lipids. The rational modification of their structures has emerged as a successful medicinal chemistry approach to the development of novel anti-AD lead candidates. The biological profile of the newly developed CNSL derivatives towards validated AD targets will be discussed together with the role of these molecular targets in the context of AD pathogenesis.
  • 1.6K
  • 26 Oct 2021
Topic Review
Ecuadorian Medicinal Plants
The use of plants as therapeutic agents is part of the traditional medicine that is practiced by many indigenous communities in Ecuador.
  • 1.6K
  • 29 Mar 2022
Topic Review
Biological Effects of Natural Acylated Flavonoids
Acylated flavonoids are widely distributed natural metabolites in medicinal plants and foods with several health attributes. Flavonoids are secondary metabolites that are widely distributed in planta, and they are well recognized for their health benefits, viz., anticancer, antioxidant, anti-inflammatory, antiviral, and as neuro- and cardio-protective effects. Flavonoids are phytochemicals comprising a benzopyrone ring bearing a phenolic or poly-phenolic group at different positions, classified based on their chemical structure, degree of unsaturation, and oxidation of carbon ring, viz., anthoxanthins (flavanone and flavanol), flavanones, flavanonols, flavans, chalcones, anthocyanidins, and isoflavonoids.
  • 1.6K
  • 14 Sep 2022
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