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Topic Review
Mannose Ligands for Mannose Receptor Targeting
The mannose receptor (MR, CD 206) is an endocytic receptor primarily expressed by macrophages and dendritic cells, which plays a critical role in both endocytosis and antigen processing and presentation. MR carbohydrate recognition domains (CRDs) exhibit a high binding affinity for branched and linear oligosaccharides. Furthermore, multivalent mannose presentation on the various templates like peptides, proteins, polymers, micelles, and dendrimers was proven to be a valuable approach for the selective and efficient delivery of various therapeutically active agents to MR. 
  • 1.5K
  • 20 Feb 2024
Topic Review
Smart Contrast Agents in MRI
Zinc and copper are essential cations involved in numerous biological processes; and variations in their concentrations can cause diseases; such as neurodegenerative diseases; diabetes and cancers. Hence, the detection and quantification of these cations is of utmost importance for the early diagnosis of disease. MRI responsive contrast agents (mainly Lanthanide 3+ complexes), relying on a change in state of the MRI active part upon interaction with the cation of interest e.g. switch ON/OFF or vice versa, have been successfully utilized to detect zinc and are now being developed to detect Copper(II). These paramagnetic probes mainly exploit the relaxation-based properties (T1-based contrast agents), but also the paramagnetic induced hyperfine shift properties (paraCEST and parashift probes) of the contrast agents. The challenges encountered going from zinc to copper(II) detection are discussed. Depending on the response mechanism, the use of fast-field cycling MRI seems promising to increase the detection field while keeping a good response. In vivo applications of cation responsive MRI probes are only at their infancy and the recent developments are described, along with the associated quantification problems.
  • 1.4K
  • 08 Jan 2021
Topic Review
Hydrogels Combined with Silver Nanoparticles against Antimicrobial Resistance
The development of multidrug-resistant (MDR) microorganisms has increased dramatically as a natural consequence of the misuse and overuse of antimicrobials. The World Health Organization (WHO) recognizes that this is one of the top ten global public health threats facing humanity today, demanding urgent multisectoral action. In this sense, metallic nanoparticles (such as silver nanoparticles) have emerged as promising alternatives due to their outstanding antibacterial and antibiofilm properties. The efficient delivery of the nanoparticles (NPs) is also a matter of concern, and studies have demonstrated that hydrogels present an excellent ability to perform this task.
  • 1.4K
  • 03 Feb 2023
Topic Review
3-Phenylcoumarins as a Privileged Scaffold in Medicinal Chemistry
3-Phenylcoumarins are a family of heterocyclic molecules that are widely used in both organic and medicinal chemistry. 3-Phenylcoumarins have been used by several research groups in the search for new chemical entities with potential in the discovery of new therapeutic solutions for several diseases. The versatility and chemical properties of this scaffold have been attracting the attention of researchers all over the world.
  • 1.4K
  • 25 Nov 2021
Topic Review
Applying CADD for Neurodegenerative Diseases
Neurodegenerative diseases (NDs) including Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, and Huntington’s disease are incurable and affect millions of people worldwide. The development of treatments for this unmet clinical need is a major global research challenge. Computer-aided drug design (CADD) methods minimize the huge number of ligands that could be screened in biological assays, reducing the cost, time, and effort required to develop new drugs. 
  • 1.4K
  • 07 May 2021
Topic Review
Composition and Industrial Applications of Phytochemical
Phytochemicals are versatile plant secondary metabolites with therapeutic properties. Lemongrass is well-known for its antioxidant, anti-microbial, anti-inflammatory, anti-hypertensive, anti-diabetic, anti-mutagenicity, anxiolytic properties, and for its hypoglycemic and hypolipidemic activities. Therefore, it is widely used in pharmaceuticals, food, feed, and the cosmetics industry. Lemongrass contains phenolic metabolites (including phenolic acids, flavonoids, stilbenes, and lignans), terpenoids, and alkaloids, which are potent bioactive ingredients. Lemongrass is a precious medicinal plant. 
  • 1.4K
  • 06 Feb 2023
Topic Review
Dendrimers in Biomedicine
Biomedicine represents one of the main study areas for dendrimers, which have proven to be valuable both in diagnostics and therapy, due to their capacity for improving solubility, absorption, bioavailability and targeted distribution. Molecular cytotoxicity constitutes a limiting characteristic, especially for cationic and higher-generation dendrimers. Antineoplastic research of dendrimers has been widely developed, and several types of poly(amidoamine) and poly(propylene imine) dendrimer complexes with doxorubicin, paclitaxel, imatinib, sunitinib, cisplatin, melphalan and methotrexate have shown an improvement in comparison with the drug molecule alone. The anti-inflammatory therapy focused on dendrimer complexes of ibuprofen, indomethacin, piroxicam, ketoprofen and diflunisal. In the context of the development of antibiotic-resistant bacterial strains, dendrimer complexes of fluoroquinolones, macrolides, beta-lactamines and aminoglycosides have shown promising effects. Regarding antiviral therapy, studies have been performed to develop dendrimer conjugates with tenofovir, maraviroc, zidovudine, oseltamivir and acyclovir, among others. Furthermore, cardiovascular therapy has strongly addressed dendrimers. Employed in imaging diagnostics, dendrimers reduce the dosage required to obtain images, thus improving the efficiency of radioisotopes. Dendrimers are macromolecular structures with multiple advantages that can suffer modifications depending on the chemical nature of the drug that has to be transported. The results obtained so far encourage the pursuit of new studies.
  • 1.4K
  • 11 Sep 2020
Topic Review
Hovenia dulcis Thumberg
Hovenia dulcis Thunberg is an herbal plant, belonging to the Rhamnaceae family, widespread in west Asia, USA, Australia and New Zealand, but still almost unknown in Western countries. H. dulcis has been described to possess several pharmacological properties, such as antidiabetic, anticancer, antioxidant, anti-inflammatory and hepatoprotective, especially in the hangover treatment, validating its use as an herbal remedy in the Chinese Traditional Medicine. These biological properties are related to a variety of secondary metabolites synthesized by the different plant parts. Root, bark and leaves are rich of dammarane-type triterpene saponins; dihydrokaempferol, quercetin, 3,3′,5′,5,7-pentahydroflavone and dihydromyricetin are flavonoids isolated from the seeds; fruits contain mainly dihydroflavonols, such as dihydromyricetin (or ampelopsin) and hovenodulinol, and flavonols such as myricetin and gallocatechin; alkaloids were found in root, barks (frangulanin) and seeds (perlolyrin), and organic acids (vanillic and ferulic) in hot water extract from seeds. Finally, peduncles have plenty of polysaccharides which justify the use as a food supplement.
  • 1.4K
  • 02 Mar 2021
Topic Review
Steroid Oximes
Steroids and their derivatives have been the subject of extensive research among investigators due to their wide range of pharmacological properties, in which steroidal oximes are included. Oximes are a chemical group with the general formula R1R2C=N−OH and they exist as colorless crystals and are poorly soluble in water. Oximes can be easily obtained through the condensation of aldehydes or ketones with various amine derivatives, making them a very interesting chemical group in medicinal chemistry for the design of drugs as potential treatments for several diseases. A large number of steroid oximes exhibit important biological activities, such as anticancer, anti-inflammatory, antibacterial, antifungal and antiviral, among others, through different mechanisms of action. Several steroid oximes are used clinically as drugs and many others are in clinical trials.
  • 1.4K
  • 20 Feb 2023
Topic Review
Potential Photodynamic Diagnosis Targets
Photodynamic diagnosis and therapy (PDD and PDT) are emerging, non/minimally invasive techniques for cancer diagnosis and treatment. Both techniques require a photosensitizer and light to visualize or destroy cancer cells. However, a limitation of conventional, non-targeted PDT is poor selectivity, causing side effects. The bioconjugation of a photosensitizer to a tumor-targeting molecule, such as an antibody or a ligand peptide, is a way to improve selectivity. The bioconjugation strategy can generate a tumor-targeting photosensitizer conjugate specific for cancer cells, or ideally, for multiple tumor compartments to improve selectivity and efficacy, such as cancer stem cells and tumor neovasculature within the tumor microenvironment. If successful, such targeted photosensitizer conjugates can also be used for specific visualization and detection of cancer cells and/or tumor angiogenesis (an early event in tumorigenesis) with the hope of an early diagnosis of cancer.
  • 1.4K
  • 03 Dec 2020
Topic Review
Sources and Absorption of Resveratrol
Polyphenols are secondary metabolites produced by plants and also found in many natural products, such as fruit and vegetables, and their derivatives, such as tea, coffee, olive oil, and wine. Polyphenols are well known for their antioxidant properties, which confer to them health-beneficial effects. Among them, resveratrol is probably one of the most investigated molecules. It was first described in 1940 by Michio Takaoka, a Japanese student who was investigating extracts from traditional medicinal plants and called it “resveratrol” because the molecule had been extracted from the roots of Veratrum grandiflorum (white hellebore) and presented the skeleton of resorcinol in its molecular structure. The extract from this plant was exploited for treating several allergic and inflammatory diseases, among others. However, this molecule did not attract much interest until 1997, when Jang and colleagues published an article regarding its cancer chemopreventive activity. Resveratrol is the common name for 3,5,4′-trihydroxy-trans-stilbene, a natural phytoalexin derived from phenylpropanoids, that is synthesized in plants under stress conditions, such as infections or UV exposure. 
  • 1.4K
  • 14 Dec 2021
Topic Review
Quinazoline Based HDAC Dual Inhibitors
Quinazolines are the most versatile, ubiquitous and privileged nitrogen bearing heterocyclic compounds with a wide array of biological and pharmacological applications. Most of the anti-cancer agents featuring quinazoline pharmacophore have shown promising therapeutic activity. Histone deacetylases (HDACs) have emerged as an important anti-cancer target in the recent years given its role in cellular growth, gene regulation, and metabolism.
  • 1.4K
  • 20 Jun 2022
Topic Review
Tu Youyou
Tu Youyou (屠呦呦), born in 1930 in Ningbo, Zhejiang, China, is a Chinese pharmaceutical chemist and malariologist best known for discovering artemisinin (Qinghaosu), a groundbreaking antimalarial compound derived from traditional Chinese medicine. Her work has saved millions of lives and earned her global recognition, including the 2015 Nobel Prize in Physiology or Medicine.
  • 1.4K
  • 22 May 2025
Topic Review
Deep eutectic solvents in pharmaceutical synthesis
DES are mixtures of two or more compounds, able to form liquids upon mixing, with lower freezing points when compared to the individual constituents (eutectic mixtures). DES have been utilized in organic synthesis as green media thanks to the high potential to replace the classical solvents. In fact, since the DES are characterized by a network of hydrogen bonds, they have the possibility to dissolve solutes that can form hydrogen bonds and stabilize transition states. Furthermore, during the purification procedures, the addition of water to a DES (very soluble in water) causes the precipitation of organic products, facilitating the workup and avoiding the use of solvents for the extraction. 
  • 1.4K
  • 04 Nov 2021
Topic Review
Screening of Medicinal Plants
Secondary metabolites, used as a single compound or as a mixture, are medicines that can be effective and safe even when synthetic drugs fail. They may even potentiate or synergize the effects of other compounds in the medicine. To meet the positive demands, heterologous expression of the genes involved in the biosynthesis of the potent compound will help in the production on the required scale. Further modifications to enhance the ADME properties of the compounds will have a significant advantage in the drug’s biological activities and bioavailability.
  • 1.4K
  • 30 Oct 2020
Topic Review
Nanomaterial-Modified Electrodes for Electrochemical Biosensors
Electrochemical biosensors are superior technologies that are used to detect or sense biologically and environmentally significant analytes in a laboratory environment, or even in the form of portable handheld or wearable electronics. 
  • 1.4K
  • 16 Jun 2023
Topic Review
Novel Agent with the Terminal Phenoxy Group
The terminal phenoxy group is a moiety of many drugs in use today. Numerous literature reports indicated its crucial importance for biological activity; thus, it is a privileged scaffold in medicinal chemistry. Most often, the presence of the phenoxy moiety provided the chances for the compound to match the target, ensuring selectivity, the π–π interaction, or increase the ability to form the hydrogen bonds by the oxygen ether atom.
  • 1.4K
  • 01 Sep 2022
Topic Review
Proteolysis-targeting Chimeras for Drug Targeted Protein Research
Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically, PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and the specific ligand of E3 ubiquitin ligase, respectively, via a suitable linker. PROTAC degradation of the target protein is performed through the ubiquitin–proteasome system (UPS).
  • 1.4K
  • 26 Sep 2022
Topic Review
Consumer Behavior, Sunscreens, and Tools for Photoprotection
Sunscreens and photoprotection tools along with consumer habits and behaviors, can mitigate the skin damage caused by excessive solar radiation. For example, protecting oneself in the shade, avoiding inadequate sun exposure at times of higher incidence of UVB radiation (between 10:00 a.m. and 4:00 p.m.), wearing clothes with sun protection factors, applying sunscreens at the correct amounts and intervals, and wearing glasses with anti-UVA and UVB lenses are effective measures for protecting an individual.
  • 1.4K
  • 03 Apr 2023
Topic Review
Phytochemicals of the Genus Maytenus
The genus Maytenus is a member of the Celastraceae family, of which several species have long been used in traditional medicine. Between 1976 and 2021, nearly 270 new compounds have been isolated and elucidated from the genus Maytenus. Among these, maytansine and its homologues are extremely rare in nature. Owing to its unique skeleton and remarkable bioactivities, maytansine has attracted many synthetic endeavors in order to construct its core structure.
  • 1.4K
  • 09 Aug 2021
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