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Topic Review
Thymoquinone and Cancer
Thymoquinone (TQ) is a bioactive molecule with anticancer as well as anti-inflammatory activities via the downregulation of several chemokines and cytokines. Administering it as a nanoformulation increases its therapeutic value.
  • 1.2K
  • 22 Sep 2021
Topic Review
Novel 1,2,4-Oxadiazole Derivatives
Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently accessible drugs containing 1,2,4-oxadiazole unit. It is worth noting that the interest in a 1,2,4-oxadiazoles’ biological application has been doubled in the last fifteen years. Herein, after a concise historical introduction, we present a comprehensive overview of the recent achievements in the synthesis of 1,2,4-oxadiazole-based compounds and the major advances in their biological applications in the period of the last five years as well as brief remarks on prospects for further development.
  • 1.2K
  • 03 Jun 2021
Topic Review
Doxorubicin
The antibiotic doxorubicin is often used as an anti-neoplastic drug; however, many patients showed very unpleasant side-effects. Previous studies have demonstrated that dietary substances such as Aloe arborescens, Annona muricata, Morinda citrifolia, Beta rubra, Scutellaria baicalensis, and Vaccinium myrtillus may have anti-oxidant, anti-proliferative, and anti-inflammatory effects. The purpose of this study was to investigate the protective effects of a mixture of these components in an experimental model of doxorubicin toxicity. Rats (n = 30) received doxorubicin (5 mg/kg/day) for 4 weeks and were randomized to receive the dietary mixture 2 hours following the first doxorubicin injection and until the end of the experiment. Animals were killed following 4 weeks, and blood, liver, and heart were collected for further analysis. The dietary supplement improved the depressed body weight and food consumption induced by DOX. In addition, the nutraceutical mixture reduced oxidative stress, ameliorated the morphological score, and preserved liver and heart structure, demonstrating a protective effect. These data show for the first time that the mixture of Aloe arborescens, Annona muricata, Morinda citrifolia, Beta rubra, Scutellaria baicalensis, and Vaccinium myrtillus may be useful to reduce the side effects following treatment with doxorubicin, and might ameliorate the quality of life of patients following chemotherapy.
  • 1.2K
  • 06 Nov 2020
Topic Review
The Coming of Age of Biosimilars
The first biosimilar, Sandoz’s Omnitrope  (human growth hormone), was approved in 2006 by both the FDA and EMA; it was approved by the FDA under the 505(b)(2) generic product legislation and by the EU as a biosimilar. Later, Sandoz received the first licensing of Zarzio/Zarxio (filgrastim) in 2015; this was the first biosimilar product approved under the 351(k) BLA legislation in the US. Biosimilars have come of age from 2005 to the present, with 84 approvals in the EU and 35 in the US, representing almost 90% of the world market. While the acceptance of biosimilars in the US is catching up with that in the EU, the cost benefits remain elusive due to the high development barrier and complex distribution system involved, mainly in the US. In the EU, the cost of biosimilars has already dropped 70% or more, and interchangeability is a routine in some European jurisdictions, unlike in the US, where a separate regulatory approval is required.
  • 1.2K
  • 27 Apr 2022
Topic Review
Transporters Expressed at the BBB
The blood–brain barrier (BBB) is a highly selective and restrictive semipermeable network of cells and blood vessel constituents. All components of the neurovascular unit give to the BBB its crucial and protective function, i.e., to regulate homeostasis in the central nervous system (CNS) by removing substances from the endothelial compartment and supplying the brain with nutrients and other endogenous compounds. Many transporters have been identified that play a role in maintaining BBB integrity and homeostasis. The restrictive nature of the BBB provides an obstacle for drug delivery to the CNS. Drug transporters functionally expressed on various compartments of the BBB involve numerous proteins from either the ATP-binding cassette (ABC) or the solute carrier (SLC) superfamilies. 
  • 1.2K
  • 26 May 2021
Topic Review
Plectranthus neochilus Schltr
Plectranthus neochilus Schltr. (Lamiaceae) is a plant recently introduced in Cuba. Worldwide, it is an ethnomedicinal alternative for its use against microbial infections, but the Cuban population use the extracts to treat sleep disorders. To address this apparent incongruity, four collections (from different seasonal conditions in the year) of Cuban P. neochilus cultivars were analyzed in terms of their pharmacognostic characteristics. 
  • 1.2K
  • 18 Jan 2022
Topic Review
SARS-CoV-2 Main Protease
The main protease (Mpro) of the newly emerged severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was subjected to hyphenated pharmacophoric-based and structural-based virtual screenings using a library of microbial natural products (>24,000 compounds). Subsequent filtering of the resulted hits according to Lipinski’s rules was applied to select only the drug-like molecules. Top-scoring hits were further filtered out depending on their ability to show constant good binding affinities towards the molecular dynamic simulation (MDS)-derived enzyme’s conformers. Final MDS experiments were performed on the ligand-protein complexes to verify their binding modes and calculate their binding free energy. Consequently, a final selection of six compounds of microbial origin was proposed to possess high potential as anti-SARS-CoV-2 drug candidates. Our study provides insight into the role of the Mpro structural flexibility during interactions with the possible inhibitors and sheds light on the structure-based design of anti-coronavirus disease 2019 (COVID-19) therapeutics targeting SARS-CoV-2
  • 1.2K
  • 26 Oct 2020
Topic Review
Intrinsic and Acquired Chemotherapy Resistance
Drug resistance is a commonly unavoidable consequence of cancer treatment that results in therapy failure and disease relapse. Intrinsic (pre-existing) or acquired resistance mechanisms can be drug-specific or be applicable to multiple drugs, resulting in multidrug resistance.
  • 1.2K
  • 23 Feb 2021
Topic Review
GABAAR-Mediated Currents
Propofol or barbiturate application at low concentrations increases desensitization and slows deactivation of GABA-induced current and propofol/barbiturate at high concentrations directly elicits after-responses upon their washout in hippocampal or sensory neurons. It is postulated that the generation of such after-responses is caused by removal of the blockade by anesthetic agents as partial antagonists. However, the increased desensitization was invariably followed by slowdown of deactivation of GABA-induced current, and the after-response may arise as a consequence of extreme slowdown of deactivation following strong desensitization. It is thus possible that propofol and barbiturate can facilitate resensitization of GABA responses. Propofol and barbiturate are useful to treat the alcohol/benzodiazepine withdrawal syndrome. Considering that the slowdown of deactivation following desensitization and the after-response induced by propofol or barbiturate application, the regulatory mechanisms of desensitization/resensitization of GABAAR-mediated currents might be important for understanding the treatment of the alcohol/benzodiazepine withdrawal syndrome.
  • 1.2K
  • 29 Oct 2020
Topic Review
Astaxanthin as Potential Neurotherapeutic Agent
ASX, a member of the xanthophyll group, was found to be a promising therapeutic anti-inflammatory agent for many neurological disorders, including cerebral ischemia, Parkinson’s disease, Alzheimer’s disease, autism, and neuropathic pain.
  • 1.2K
  • 15 Apr 2021
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