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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.
30 Oct 2020
Hsp90 C-Terminal Inhibitors
Hsp90 is a molecular chaperone with over 300 client proteins that act in the cell cycle and in signalling processes. Disruption of Hsp90 chaperone activity by inhibitors induces simultaneous proteasomal degradation of many deregulated oncoproteins that are critical for all fundamental hallmarks of cancers. To date, mainly Hsp90 N-terminal domain inhibitors have been developed for cancer treatments; however, several of these have not been successful in clinical trials, often due to toxicity. One of the major drawbacks associated with Hsp90 N-terminal domain inhibition is induction of the pro-survival heat-shock response. This response results in increased levels of Hsp90 and anti-apoptotic proteins, such as heat shock factor 1 (HSF-1), Hsp27 and Hsp70, which initiate anti-apoptotic cascades and promote drug resistance, a highly problematic property of any anticancer drug. In contrast, Hsp90 C-terminal inhibitors do not induce the heat shock response, and are therefore promising novel agents for treatment of different cancers.
09 Nov 2020
Antimicrobial photodynamic therapy (aPDT)
Photodynamic inactivation is known as a new antimicrobial photodynamic therapy (aPDT). It is based on the administration of a photosensitizer located in the bacterial/viral cell followed by exposure to light radiations (with a proper wavelength corresponding with the maximum value of absorption of the photosensitizer) that generate singlet oxygen or reactive oxygen species, which lead to the death of different microorganisms. This review will present an overview beyond the state-of-the-art of the photosensitizer types (based on tetra-p-sulphonated-phenyl porphyrin—TSPP, which is able to form cationic and J-aggregates forms at different pH values ((1–4) and concentrations around 10−5 M) and their applications of PDT for viruses, especially.
30 Sep 2021
Rhenium(I) Tricarbonyl Complexes As Photosensitisers
Photodynamic therapy (PDT) is emerging as a significant complementary or alternative approach for cancer treatment. Re(I) tricarbonyl complexes is a new generation of metal-based photosensitisers for PDT that are of great interest in multidisciplinary research.
27 Oct 2020
Curcumin: Biochemistry and Antitumoral Action
Curcumin is a pigment with a strong yellow colour found and the main active component of Curcuma longa, a perennial Zingiberaceae plant native to southwest India, but now grown across the South and Southeast Asia, especially in China and India. It is used for centuries as a spice and currently it is viewed as a nutraceutical due to the increasing number of scientific studies demonstrating its anti-oxidant, anti-inflammatory, anti-tumoral and cancer preventive properties. Its chemical structure comprises two aromatic ring systems with o-methoxy phenol groups connected by a seven-carbon linker consisting of an α,β-unsaturated β-diketone with tautomerism when in solution.
07 Feb 2021
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.
21 Oct 2020
Benchmarking Data Sets
Developing realistic data sets for evaluating virtual screening methods is a task that has been tackled by the cheminformatics community for many years. Numerous artificially constructed data collections were developed, such as DUD, DUD-E, or DEKOIS. However, they all suffer from multiple drawbacks, one of which is the absence of experimental results confirming the impotence of presumably inactive molecules, leading to possible false negatives in the ligand sets. In light of this problem, the PubChem BioAssay database, an open-access repository providing the bioactivity information of compounds that were already tested on a biological target, is now a recommended source for data set construction. Nevertheless, there exist several issues with the use of such data that need to be properly addressed. In this article, an overview of benchmarking data collections built upon experimental PubChem BioAssay input is provided, along with a thorough discussion of noteworthy issues that one must consider during the design of new ligand sets from this database. The points raised in this review are expected to guide future developments in this regard, in hopes of offering better evaluation tools for novel in silico screening procedures.
26 Oct 2020
Nanotechnology for Eye Topical Drug Delivery
Topical drug delivery is one of the most challenging aspects of eye therapy. Eye drops are the most prevalent drug form because they are convenient and easy to apply by patients. However, conventional drug formulations are usually characterized by short retention time in the tear film, insufficient contact with epithelium, fast elimination, and difficulties in overcoming ocular tissue barriers. Not more than 5% of the total drug dose administered in eye drops reaches the interior ocular tissues. Drug-loaded nanoparticles/hydrogels do not enter cells via diffusion. The endocytosis pathway is related to the penetration of drug-loaded nanoparticles/hydrogels into the cell. The interactions between the nanoparticles and the cell membrane generate forces of different origins and lead to the membrane wrapping of the nanoparticles followed by cellular uptake.
24 Dec 2021
Porphyrins/Chlorins for Viruses Inactivation
The problem of treating viral infections is extremely important both in connection with the emergence of new viral diseases and in connection with the low efficiency of existing approaches to the treatment of known viral infections. This entry is devoted to the use of porphyrins, chlorins, and phthalocyanines for the fight against viral infections using chemical and photochemical inactivation methods. The purpose of this work is to summarize the main approaches developed to date to chemical and photodynamic inactivation of human and animal viruses using porphyrins and their analogs, as well as to analyze and discuss information on viral targets and antiviral activity of porphyrins, chlorins and their derivatives obtained in the last 10-15 years, in order to identify the most promising areas.
23 Jun 2021
Gemcitabine Peptide-Based Conjugates
Gemcitabine is an anticancer drug used to treat a wide range of solid tumors and is a first-line treatment for pancreatic cancer. The effect of gemcitabine is significantly weakened by its rapid plasma degradation. In addition, the systemic toxicity and drug resistance significantly reduce its chemotherapeutic efficacy. Up to now, many approaches have been made to improve the therapeutic index of gemcitabine. One of the recently developed approaches to improve conventional chemotherapy is based on the direct targeting of chemotherapeutics to cancer cells using the peptide-drug conjugates (PDCs).
24 Feb 2021
Featured Entry Collections
Encyclopedia of Social Sciences
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