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Topic Review
Copper-Coordinated Thiazoles and Benzothiazoles as Antimicrobial Agents
Thiazole and benzothiazole are present in different structures with interesting biological effects and are used to develop new effective antimicrobial agents. Moreover, nitrogen atoms that are present in this heterocycle allow for coordination with various metals, forming metal complexes that enhance the biological activity of organic ligands that are often used as commercial drugs.
  • 1.1K
  • 09 May 2023
Topic Review
Cannabis sativa Bioactive Compounds in Colorectal Cancer
Cannabis sativa is a multipurpose plant that has been used in medicine for centuries. Considerable research has focused on the bioactive compounds of this plant, particularly cannabinoids and terpenes. Among other properties, these compounds exhibit antitumor effects in several cancer types, including colorectal cancer (CRC). Cannabinoids show positive effects in the treatment of CRC by inducing apoptosis, proliferation, metastasis, inflammation, angiogenesis, oxidative stress, and autophagy. Terpenes, such as β-caryophyllene, limonene, and myrcene, have also been reported to have potential antitumor effects on CRC through the induction of apoptosis, the inhibition of cell proliferation, and angiogenesis. In addition, synergy effects between cannabinoids and terpenes are believed to be important factors in the treatment of CRC. 
  • 1.1K
  • 18 May 2023
Topic Review
Taccalonolides
Taccalonolides are a new class of microtube-stabilizing agents isolated from plants of the genus Tacca demonstrating effectiveness against drug-resistant tumors in cellular and animal models.
  • 1.1K
  • 16 Sep 2021
Topic Review
Isolated Marine Compounds with Antifungal Activity
The oceans represent the largest ecosystem on earth, with a high diversity of organisms. Oceans have received some attention, and promising compounds with antimicrobial activities were isolated from marine organisms such as bacteria, fungi, algae, sea cucumbers, sea sponges, etc. 
  • 1.1K
  • 02 Aug 2023
Topic Review Peer Reviewed
Cyclodextrin-Based Nanosponges and Proteins
Cyclodextrin-based nanosponges (CD-NSs) have gained importance in drug delivery in the last years due to their easy synthesis and versatility. However, their use as carriers for the delivery of macromolecules such as proteins is less known and sometimes difficult to consider. In this entry, the authors summarize and highlight the multiple possibilities of CD-NSs to deliver active proteins, improving their activity or stability. Starting with a brief description of CD-NSs and their characteristics, the entry will be focused on several proteins, such as (1) Lipase, (2) Insulin and (3) Nisin, for chemical or pharmaceutical applications. The revised results demonstrated that CD-NSs can generate different and interesting applications with proteins. These results could be added to their uses with small drugs, being an interesting alternative for protein delivery and applicability. 
  • 1.1K
  • 14 Apr 2022
Topic Review
The Genus Tulbaghia
Amaryllidaceae is a significant source of bioactive phytochemicals with a strong propensity to develop new drugs. The genera Allium, Tulbaghia, Cyrtanthus and Crinum biosynthesize novel alkaloids and other phytochemicals with traditional and pharmacological uses. Amaryllidaceae biomolecules exhibit multiple pharmacological activities such as antioxidant, antimicrobial, and immunomodulatory effects.
  • 1.1K
  • 29 Jul 2022
Topic Review
Regenerative Medicine Bioconjugated Hydrogel Scaffolds
Materials used for regenerative medicine purposes pose a series of challenges in terms of biocompatibility, adaptability and functionality. A way to design functional and compatible materials that mimic soft tissue is to exploit synthetic hydrogels. To widen their activity scope, hydrogels can be coupled with molecular cues to promote tissue regeneration or trigger regeneration processes. Within this entry we asses the criteria to choose the design of a bioconjugated for regenerative medicine purposes, giving relevant examples from the current literature.
  • 1.1K
  • 21 Oct 2020
Topic Review
Extremophilic Fungi from Marine Environments
Marine environments are underexplored terrains containing fungi that produce a diversity of natural products given unique environmental pressures and nutrients. While bacteria are commonly the most studied microorganism for natural products in the marine world, marine fungi are also abundant but remain an untapped source of bioactive metabolites. Given that their terrestrial counterparts have been a source of many blockbuster antitumor agents and anti-infectives, including camptothecin, the penicillins, and cyclosporin A, marine fungi also have the potential to produce new chemical scaffolds as leads to potential drugs. Fungi are more phylogenetically diverse than bacteria and have larger genomes that contain many silent biosynthetic gene clusters involved in making bioactive compounds. However, less than 5% of all known fungi have been cultivated under standard laboratory conditions. While the number of reported natural products from marine fungi is steadily increasing, their number is still significantly lower compared to those reported from their bacterial counterparts.
  • 1.1K
  • 29 Mar 2022
Topic Review
Surface Functionalization of Magnetic Nanoparticles
The surface functionalization of magnetic nanoparticles (MNPs) has witnessed significant progress recently, revolutionizing their utility in multimodal imaging, drug delivery, and catalysis. This progression, spanning over the last decade, has unfolded in discernible phases, each marked by distinct advancements and paradigm shifts. In the early stage, emphasis was placed on foundational techniques, such as ligand exchange and organic coatings, establishing the groundwork for innovations to come.
  • 1.1K
  • 18 Oct 2023
Topic Review
Health-Promoting Effects of Bioactive Compounds from Endophytic Fungi
The study examines the intricate relationship between plants and the endophytic fungi inhabiting their tissues. These fungi harmoniously coexist with plants, forming a distinct symbiotic connection that has caught scientific attention due to its potential implications for plant health and growth. The diverse range of bioactive compounds produced by these fungi holds significant promise for human health.
  • 1.1K
  • 09 Oct 2023
Topic Review
Botanicals in Postmenopausal Osteoporosis
Osteoporosis is a systemic bone disease characterized by reduced bone mass and the deterioration of bone microarchitecture leading to bone fragility and an increased risk of fractures. Conventional anti-osteoporotic pharmaceutics are effective in the treatment and prophylaxis of osteoporosis, however they are associated with various side effects that push many women into seeking botanicals as an alternative therapy. 
  • 1.1K
  • 02 Jun 2021
Topic Review
Proteasome Structure and Function in Multiple Myeloma
Multiple myeloma (MM) is an aggressive and incurable disease for most patients, characterized by periods of treatment, remission and relapse. The introduction of new classes of drugs, such as proteasome inhibitors (PIs), has improved survival outcomes in these patient populations. The proteasome is the core of the ubiquitin–proteasome system (UPS), a complex and conserved pathway involved in the control of multiple cellular processes, including cell cycle control, transcription, DNA damage repair, protein quality control and antigen presentation. 
  • 1.1K
  • 23 Feb 2023
Topic Review
Metal-Based Chemotherapeutic Treatments
Herein we provides an overview of the various research approaches we have explored in recent years to improve metal-based agents for cancer or infection treatments. Although cisplatin, carboplatin, and oxaliplatin remain the cornerstones in tumor chemotherapy, the discovery and approval of novel inorganic anticancer drugs is a very slow process. Analogously, although a few promising inorganic drugs have found clinical application against parasitic or bacterial infections, their use remains relatively limited. Moreover, the discovery process is often affected by small therapeutic enhancements that are not attractive for the pharmaceutical industry. However, the availability of increasing mechanistic information for the modes of action of established inorganic drugs is fueling the exploration of various approaches for developing effective inorganic chemotherapy agents. Through a series of examples, some from our own research experience, we focus our attention on a number of promising strategies, including (1) drug repurposing, (2) the simple modification of the chemical structures of approved metal-based drugs, (3) testing novel drug combinations, and (4) newly synthesized complexes coupling different anticancer drugs. Accordingly, we aim to suggest and summarize a series of reliable approaches that are exploitable for the development of improved and innovative treatments.
  • 1.1K
  • 25 May 2021
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. 
  • 1.1K
  • 13 Sep 2023
Topic Review
Fundamentals of Rhenium-188 Radiopharmaceutical Chemistry
The β− emitter, rhenium-188 (188Re), has long been recognized as an attractive candidate for targeted cancer radionuclide therapy (TRNT). This transition metal shares chemical similarities with its congener element technetium, whose nuclear isomer technetium-99m (99mTc) is the current workhorse of diagnostic nuclear medicine. This pair of elements forms a characteristic matched pair for chemical and medical research and applications.
  • 1.1K
  • 21 Apr 2023
Topic Review
Royleanones
Plants have been used for centuries to treat several illnesses. The Plectranthus genus has a vast variety of species that has allowed the isolation of cytotoxic compounds with notable activities.The abietane diterpenes 6,7-dehydroroyleanone (DeRoy), 7alfa-acetoxy-6 -hydroxyroyleanone (Roy), and Parvifloron D (ParvD) were obtained from Plectranthus spp. and showed promising biological activities, such as cytotoxicity on several cancer cell lines, including cancer stem cell inducing sphere cells. In silico studies comparied the possible binding modes of active compounds and derivatives against different PKC isoforms alpha/beta/delta/iota/lambda/theta/zeta.
  • 1.1K
  • 27 Oct 2020
Topic Review
G-Quadruplex Structures in Plants
G-quadruplex (G4) oligonucleotides are higher-order DNA and RNA secondary structures of enormous relevance due to their implication in several biological processes and pathological states in different organisms.  Plants offer a cornucopia of phytocompounds that, in many cases, are effective in binding and modulating the thermal stability of G4s and, on the other hand, contain almost unexplored G4 motifs in their genome that could inspire new biotechnological strategies.
  • 1.1K
  • 10 Nov 2022
Topic Review
Peptidomimetics and Their Applications for Opioid Peptide Drug
Peptidomimetics are synthetically altered peptides with adjusted molecular properties for specific biological or therapeutic applications and have been an important class of drug molecules due to their potential features, high potency, and low toxicity since the term was created first in the late 1970s.
  • 1.1K
  • 30 Nov 2022
Topic Review
Pioglitazone-Loaded PLGA Nanoparticles
Albeit, the relationship between diabetes drugs and the progression of atherosclerosis is still elusive, Pioglitazone (PGZ; 5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]–1,3- thiazolidine-2,4-diona), one of the most frequently prescribed anti-diabetic medication in the United States, slows the progression of atherosclerosis.
  • 1.1K
  • 14 Mar 2022
Topic Review
Dimeric/Multimeric Anticoagulant DNA Aptamers
Multivalent interactions frequently occur in biological systems and typically provide higher binding affinity and selectivity in target recognition than when only monovalent interactions are operative. Thus, taking inspiration by nature, bivalent or multivalent nucleic acid aptamers recognizing a specific biological target have been extensively studied in the last decades. Indeed, oligonucleotide-based aptamers are suitable building blocks for the development of highly efficient multivalent systems since they can be easily modified and assembled exploiting proper connecting linkers of different nature. Thus, substantial research efforts have been put in the construction of dimeric/multimeric versions of effective aptamers with various degrees of success in target binding affinity or therapeutic activity enhancement. Several dimeric and multimeric DNA-based aptamers, including those forming G-quadruplex (G4) structures, were designed as anti-inflammatory, antiviral, anticoagulant, and anticancer agents and their number is certainly bound to grow in the near future. In this content, we here focus on dimeric/multimeric constructs designed as anticoagulant agents.
  • 1.1K
  • 01 Dec 2020
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