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Topic Review
Anticancer Small-Molecule Agents Targeting Eukaryotic Elongation Factor 1A
Eukaryotic elongation factor 1A (eEF1A) canonically delivers amino acyl tRNA to the ribosomal A site during the elongation stage of protein biosynthesis. Yet paradoxically, the oncogenic nature of this instrumental protein has long been recognized. Consistently, eEF1A has proven to be targeted by a wide assortment of small molecules with excellent anticancer activity, among which plitidepsin has been granted approval for the treatment of multiple myeloma. Meanwhile, metarrestin is under clinical development for metastatic cancers.
  • 409
  • 15 Mar 2023
Topic Review
Functionalized Peptides in Nanomedicine for Effective Cancer Therapy
Peptide-functionalized nanomedicine, which addresses the challenges of specificity and efficacy in drug delivery, is emerging as a pivotal approach for cancer therapy. Globally, cancer remains a leading cause of mortality, and conventional treatments, such as chemotherapy, often lack precision and cause adverse effects. The integration of peptides into nanomedicine offers a promising solution for enhancing the targeting and delivery of therapeutic agents.
  • 407
  • 23 Jan 2024
Topic Review
Targeting Nrf2 and NF-κB Signaling Pathways in Cancer
Plant secondary metabolites, known as phytochemicals, have gained much attention in light of the “circular economy”, to reutilize waste products deriving from agriculture and food industry. Phytochemicals are known for their onco-preventive and chemoprotective effects, among several other beneficial properties. Apple phytochemicals have been extensively studied for their effectiveness in a wide range of diseases, cancer included.
  • 406
  • 15 Feb 2023
Topic Review
Bioactivity of Bisindolylmaleimides and Derivatives
Bisindolylmaleimide (BIM)-type compounds arise from natural sources such as arcyriarubin and are biosynthetically related to indolocarbazoles. BIMs are commonly the immediate synthetic precursors of indolocarbazoles, lacking a central bond between the two aromatic units and making them more flexible and drug-like. Synthetic endeavours within this class of compounds are broad and have led to the development of both remarkably potent and selective protein kinase inhibitors. Clinical BIM examples include ruboxistaurin and enzastaurin, which are highly active inhibitors of protein kinase C-β. While BIMs are widely recognised as protein kinase inhibitors, other modes of activity have been reported, including the inhibition of calcium signalling and antimicrobial activity. BIMs can be highly functionalised or chemically manipulated, which provides the opportunity to generate new derivatives with unique biological profiles. Critically, structural differences can be used to exploit new bioactivity and therefore it is imperative to discover new chemical entities to address new targets. 
  • 404
  • 13 Sep 2023
Topic Review
Deep Eutectic Solvents in Pharmaceutical Industry
Neoteric solvents emerged as an alternative to organic solvents and are commonly called green solvents, since they have low toxicity, are biodegradable, are made with accessible and low-cost materials, and are quite easy to produce. Deep eutectic solvents (DESs) are defined as a mixture of two or more pure compounds, which, when combined in an appropriate ratio, give rise to a eutectic mixture that deviates from the ideal thermodynamic behaviour. This deviation is due to strong interactions between the initial components that act as hydrogen bond donors (HBDs) and hydrogen bond acceptors (HBAs). The HBDs and HBAs interact in the DESs to form a dense network of molecules that give them remarkably interesting physical and chemical properties. 
  • 403
  • 23 Jan 2024
Topic Review
Health Effects of European Elderberry and American Elderberry
Elderberry is highly reputed for its health-improving effects. Multiple pieces of evidence indicate that the consumption of berries is linked to enhancing human health and preventing or delaying the onset of chronic medical conditions. Compared with other fruit, elderberry is a very rich source of anthocyanins (approximately 80% of the polyphenol content). These polyphenols are the principals that essentially contribute to the high antioxidant and anti-inflammatory capacities and the health benefits of elderberry fruit extract. These health effects include attenuation of cardiovascular, neurodegenerative, and inflammatory disorders, as well as anti-diabetic, anticancer, antiviral, and immuno-stimulatory effects.
  • 402
  • 06 Apr 2023
Topic Review
5-Arylidenerhodanines as P-gp Modulators
Multidrug resistance (MDR) is considered one of the major mechanisms responsible for the failure of numerous anticancer and antiviral chemotherapies. Various strategies to overcome the MDR phenomenon have been developed, and one of the most attractive research directions is focused on the inhibition of MDR transporters, membrane proteins that extrude cytotoxic drugs from living cells. 
  • 401
  • 14 Apr 2023
Topic Review
N-Phenylquinoneimine
The N-phenylquinoneimine scaffold is a versatile synthetic platform that has gained significant attention in the field of drug discovery due to its structural diversity and capacity to interact with biologically relevant targets. 
  • 390
  • 10 Jan 2024
Topic Review
Marine-Derived Bisindoles for Potent Selective Cancer Drug Discovery
Indole is a multifunctional active pharmacophore and a heterocyclic compound widely present in natural and synthetic compounds with biological activity. Indole alkaloids from natural sources display diverse mechanisms and structures and exert anticancer potential through various antiproliferation mechanisms. Thus, indole alkaloids play a significant role in the discovery of new anticancer drugs. Scientists have subsequently isolated various new bisindole alkaloids from marine organisms, especially deep-water sponges. They are usually extracted with organic solvents (e.g., methanol, ethyl acetate). And the extracts were concentrated and partitioned between organic and aqueous phases. The organic phase is separated with chromatography separation technology, including silica gel column chromatography, high-performance liquid chromatography, etc. Most marine-derived bisindoles exist in solid form, which makes it convenient for us to determine their absolute configuration by single crystal. A number of marine-derived bisindoles exhibit strong and varied biological activities. Due to their unique biological activities and chemical structures, they have become a research focal point in pharmaceutical chemistry as lead compounds for new drug development. It is noteworthy that many drugs based on marine-derived bisindoles have been approved or are currently in clinical research, such as midostaurin, lestaurtinib, and enzastaurin. These drug molecules have shown potent selective anti-tumor effects.
  • 381
  • 06 Mar 2024
Topic Review
Amidoalkyl Naphthols: Bioactive Substances and Building Blocks
1-amidoalkyl-2-naphthol derivatives are of increasing interest due to their biological activities and further use in the preparation of other important bioactive molecules, such as aminoalkyl naphthols and oxazines.
  • 380
  • 16 Jun 2023
Topic Review
Pharmacological Activities of Betulin
Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It reduces postprandial hyperglycemia by inhibiting α-amylase and α-glucosidase activity, combats tumor cells by inducing apoptosis and inhibiting metastatic proteins, and modulates chronic inflammation by blocking the expression of proinflammatory cytokines via modulation of the NFκB and MAPKs pathways.
  • 379
  • 25 Jul 2023
Topic Review
Pharmacological Properties Improvement by Engineering of Nisin
Nisin is a readily available and cheap lanthipeptide and thus serves as a good model in the search for the tools to engineer lantibiotics with improved pharmacological properties. There are basically two general means to obtain nisin analogs—protein engineering and chemical functionalization of this antibiotic. Although bioengineering techniques have been well developed and enable the creation of nisin mutants of variable structures and properties, they are lacking spectacular effects so far. Chemical modifications of nisin based on utilization of the reactivity of its free amino and carboxylic moieties, as well as reactivity of the double bonds of its dehydroamino acids, are in their infancy.
  • 368
  • 08 Sep 2023
Topic Review
First-Line Anti-Hepatocellular Carcinoma Drugs
Following the most recent guidelines of the European Association for the Study of Liver/European Institute for Cancer Research and Treatment research organization, liver cancer is the sixth most frequent cancer and the third leading cause of cancer-related mortality. Among the most frequently occurring forms of primary liver cancer, hepatocellular carcinoma (HCC) is responsible for more than 90% of the global health burden due to liver cancer. Males appear to be more susceptible to HCC than females. Hepatocellular carcinoma is most frequently reported in people with chronic liver disorders, such as cirrhosis caused by hepatitis B or C infection or a genetic disorder (e.g., hemochromatosis). Additionally, HCC is more prevalent in those who use a considerable amount of alcohol and have a fatty liver. Generally, HCC treatment has been classified as curative or palliative. Curative procedures such as percutaneous ablation, liver transplantation, and resection all result in complete remission in many cases and are likely to enhance survival. While palliative treatments are not intended to cure, they can enhance response rates and even survival in some patients. When treating patients with liver cancer, it is common to use a combination of multidisciplinary approaches that take into account the patient’s specific condition, including the severity of their liver disease and overall health. Liver cancers are treated differently in different specialties and in different parts of the world. Additionally, most people with HCC have an incurable illness. Traditionally, these individuals have had few therapy choices because HCC displays resistance to currently available systemic treatments. 
  • 358
  • 31 Mar 2023
Topic Review
Nano/Micromotors for Cancer Diagnosis and Therapy
Nano/micromotors are artificial robots at the nano/microscale that are capable of transforming energy into mechanical movement. In cancer diagnosis or therapy, such “tiny robots” show great promise for targeted drug delivery, cell removal/killing, and even related biomarker sensing. 
  • 358
  • 12 Jan 2024
Topic Review
Classification, Toxicity and Bioactivity of Natural Diterpenoid Alkaloids
Diterpenoid alkaloids are natural compounds having complex structural features with many stereo-centres originating from the amination of natural tetracyclic diterpenes and produced primarily from plants in the Aconitum, Delphinium, Consolida genera. Corals, Xenia, Okinawan/Clavularia, Alcyonacea (soft corals) and marine sponges are rich sources of diterpenoids, despite the difficulty to access them and the lack of availability. Researchers have long been concerned with the potential beneficial or harmful effects of diterpenoid alkaloids due to their structural complexity, which accounts for their use as pharmaceuticals as well as their lousy reputation as toxic substances. Compounds belonging to this unique and fascinating family of natural products exhibit a broad spectrum of biological activities. Some of these compounds are on the list of clinical drugs, while others act as incredibly potent neurotoxins. Despite numerous attempts to prepare synthetic products, this review only introduces the natural diterpenoid alkaloids, describing ‘compounds’ structures and classifications and their toxicity and bioactivity. The purpose of the review is to highlight some existing relationships between the presence of substituents in the structure of such molecules and their recognised bioactivity.
  • 357
  • 27 Sep 2023
Topic Review
Structural Characteristics, Classification, and Nomenclature of Glycosphingolipids
Glycosphingolipids (GSLs) are a glycolipid subtype which plays vital roles in numerous biological processes, cell–cell interactions, as well as oncogenesis and ontogenesis. They are ubiquitous molecules found mostly in cell membranes.
  • 348
  • 11 Sep 2023
Topic Review
Pharmacological Activities of Diterpenoid Alkaloids
Diterpenoid alkaloids (DAs) are characteristic components of some genera of the Ranunculaceae family, the occurrence of which is extraordinarily high in the genera Aconitum, Delphinium, and Consolida. To affect the central nervous system, primarily, the drug should pass the blood–brain barrier (BBB). Transmembrane diffusion is the most common route of drugs to pass the BBB and, in contrast to the transport system, shows a non-saturable kinetic. Physiochemical features of the drug mainly determine the amounts of this passage. Molecular weight (400–600 Da is optimum), lipid solubility, molecular charge, and tertiary structure are the most important factors necessary for transmembrane diffusion through BBB. The diterpenic backbone of DAs provides their suitable lipid solubility, but the presence of tertiary nitrogen makes them different from normal diterpenoids. The tertiary nitrogen with the highest proton affinity in the molecule (in water) rearranges the electronic structure of DA by its protonation. Moreover, computational modeling showed that the function of nitrogen besides ester sidechains causes DAs to interact with the active sites as well as their toxicity.
  • 347
  • 22 May 2023
Topic Review
Ruthenium(II)
The two Ru(III) and Ru(II) complexes, namely, BOLD-100 and RAPTA-C, are presently being studied in a clinical trial and preclinical studies evaluation, respectively, as anticancer agents. Ruthenium N-heterocyclic carbene (Ru-NHC) complexes show interesting properties in medicinal chemistry, exhibiting multiple biological activities, among them anticancer, antimicrobial, antioxidant, and anti-inflammatory. Among the newly synthesized complexes, RANHC-V and RANHC-VI are the most active against triple-negative human breast cancer cell lines MDA-MB-231. These compounds were selective in vitro inhibitors of the human topoisomerase I activity and triggered cell death by apoptosis. Furthermore, the Ru-NHC complexes’ antimicrobial activity was studied against Gram-positive and -negative bacteria, revealing that all the complexes possessed the best antibacterial activity against the Gram-positive Staphylococcus aureus, at a concentration of 0,025 mg/mL. Finally, the antioxidant effect was assessed by DPPH and ABTS radicals scavenging assays, resulting in a higher ability for inhibiting the ABTS+, with respect to the well-known antioxidant Trolox. Thus, this work provides encouraging insights for further development of novel Ru-NHC complexes as potent chemotherapeutic agents endowed with multiple biological properties.
  • 347
  • 07 Mar 2024
Topic Review
Antifungal Azoles by Transition Metal Coordination
Coordination compounds featuring one or more antifungal azole (AA) ligands constitute an interesting family of candidate molecules, given their medicinal polyvalence and the viability of drug complexation as a strategy to improve and repurpose available medications.
  • 329
  • 11 Dec 2023
Topic Review
Electrospun Fibers for Skin Burn Treatment
Burns are a major threat to public health and the economy due to their costly and laborious treatment and high susceptibility to infection. Efforts have been made recently to investigate natural bioactive compounds with potential use in wound healing.
  • 326
  • 30 Jun 2023
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