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Topic Review
HIV-1
The HIV-1 integrase enzyme (IN) plays a critical role in the viral life cycle by integrating the reverse-transcribed viral DNA into the host chromosome. This function of IN has been well studied, and the knowledge gained has informed the design of small molecule inhibitors that now form key components of antiretroviral therapy regimens. Recent discoveries unveiled that IN has an under-studied yet equally vital second function in HIV-1 replication. This involves IN binding to the viral RNA genome in virions, which is necessary for proper virion maturation and morphogenesis. Herein we describe these two functions of IN within the context of the HIV-1 life cycle, how IN binding to the viral genome is coordinated by the major structural protein, Gag, and discuss the value of targeting the second role of IN in virion morphogenesis.
  • 1.6K
  • 17 Sep 2020
Topic Review
Thymoquinone
Thymoquinone (TQ), the chief active constituent of Nigella sativa (NS), shows very valuable biomedical properties such as antioxidant, antimicrobial, anticancer, anti-inflammatory, antihypertensive, hypoglycemic, antiparasitic and anti-asthmatic effects. Several studies have examined the pharmacological actions of TQ in the treatment of oral diseases but its potential role in periodontal therapy and regeneration is not yet fully defined.
  • 1.6K
  • 17 Dec 2020
Topic Review
Exosomes for Drug Delivery
Particular interest among the scientific community is focused on exploring the use of exosomes for several pharmaceutical and biomedical applications. This is due to the identification of the role of exosomes as an excellent intercellular communicator by delivering the requisite cargo comprising of functional proteins, metabolites and nucleic acids. Exosomes are the smallest extracellular vesicles (EV) with sizes ranging from 30–100 nm and are derived from endosomes. Exosomes have similar surface morphology to cells and act as a signal transduction channel between cells. They encompass different biomolecules, such as proteins, nucleic acids and lipids, thus rendering them naturally as an attractive drug delivery vehicle. Like the other advanced drug delivery systems, such as polymeric nanoparticles and liposomes to encapsulate drug substances, exosomes also gained much attention in enhancing therapeutic activity. Exosomes present many advantages, such as compatibility with living tissues, low toxicity, extended blood circulation, capability to pass contents from one cell to another, non-immunogenic and special targeting of various cells, making them an excellent therapeutic carrier. Exosome-based molecules for drug delivery are still in the early stages of research and clinical trials. The problems and clinical transition issues related to exosome-based drugs need to be overcome using advanced tools for better understanding and systemic evaluation of exosomes.
  • 1.6K
  • 21 Nov 2022
Topic Review
De Novo Synthesized Estradiol
The estrogen estradiol is a potent neuroactive steroid that may regulate brain structure and function. Although the eff ects of estradiol have been historically associated with gonadal secretion, the discovery that this steroid may be synthesized within the brain has expanded this traditional concept. Indeed, it is accepted that de novo synthesized estradiol in the nervous system (nE2) may modulate several aspects of neuronal physiology, including synaptic transmission and plasticity, thereby influencing a variety of behaviors. These modulations may be on a time scale of minutes via non-classical and often membrane-initiated mechanisms or hours and days by classical actions on gene transcription. Besides the high level, recent investigations in the cerebellum indicate that even a low aromatase expression can be related to the fast nE2 eff ect on brain functioning. These pieces of evidence point to the importance of an on-demand and localized nE2 synthesis to rapidly contribute to regulating synaptic transmission. This review is geared at exploring a new scenario for the impact of estradiol on brain processes as it emerges from the nE2 action on cerebellar neurotransmission and cerebellum-dependent learning.
  • 1.6K
  • 30 Oct 2020
Topic Review
Irinotecan
Irinotecan has been used in the treatment of various malignancies for many years. Still, the knowledge regarding this drug is expanding. The pharmacogenetics of the drug is the crucial component of response to irinotecan. Furthermore, new formulations of the drug are introduced for it enhanced delivery. Novel formulations of drugs (e.g., liposomal formulations, dendrimers, and nanoparticles) have a huge potential to avoid potentially life-threatening side effects of the iriniotecan. 
  • 1.6K
  • 14 Jul 2020
Topic Review
Bone Products Bioequivalence Study
An FDA-regulated, prescription medical food (Fosteum; 27 mg natural genistein, 200 IU cholecalciferol, 20 mg citrated zinc bisglycinate (4 mg elemental zinc) per capsule) and an over-the-counter (OTC) supplement (Citracal Plus Bone Density Builder; 27 mg synthetic genistein, 600 mg elemental calcium (calcium citrate), 400 IU vitamin D3, 50 mg magnesium, 7.5 mg zinc, 1 mg copper, 75 μg molybdenum, 250 μg boron per two tablets) were compared to a clinically proven bone formulation (27 mg natural genistein, 400 IU cholecalciferol, 500 mg elemental calcium (calcium carbonate) per tablet; the Squadrito formulation) in an 8-day steady-state pharmacokinetic (PK) study of healthy postmenopausal women (n = 30) randomized to receive 54 mg of genistein per day. Trough serum samples were obtained before the final dose on the morning of the ninth day followed by sampling at 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hrs. Total serum genistein, after β-glucuronidase/sulfatase digestion, was measured by time-resolved fluorometric assay. Maximal time (T max), concentration (C max), half-life (T 1/2), and area under the curve (AUC) were determined for genistein in each formulation. Fosteum and the Squadrito study formulation were equivalent for genistein T max (2 hrs), C max (0.7 μM), T 1/2 (18 ± 6.9 versus 21 ± 4.9 hrs), and AUC (9221 ± 413 versus 9818 ± 1370 ng·hr/mL). The OTC supplement's synthetically derived genistein, however, showed altered T max (6 hrs), C max (0.57 μM), T 1/2 (8.3 ± 1.9 hrs), and AUC (6474 ± 287 ng·hr/mL). Differences in uptake may be due to multiple ingredients in the OTC supplement which interfere with genistein absorption.
  • 1.6K
  • 01 Nov 2020
Topic Review
Allosteric Modulation of Adenosine A2A Receptors
Adenosine is a naturally occurring purine nucleoside that regulates various physiologic functions, including inflammation and wound healing, cardiac contraction, blood vessel formation, vasodilation, learning, memory, sleep, and arousal. Adenosine is released by neurons and glial cells. Extracellular adenosine modulates neuronal excitability, synaptic plasticity, and the release and reuptake of several neurotransmitters. The effects of extracellular adenosine are modulated via four subtypes of G-protein coupled adenosine receptors (GPCRs), denoted A1, A2A, A2B, and A3. Adenosine A2A receptors (A2ARs) are broadly expressed in the brain, cardiovascular system, blood vessels, spleen, thymus, leukocytes, and lung, making them an important drug target. The therapeutic potential of targeting adenosine A2ARs is immense due to their broad expression in the body and central nervous system. The role of A2ARs in cardiovascular function, inflammation, sleep/wake behaviors, cognition, and other primary nervous system functions has been extensively studied. 
  • 1.6K
  • 29 Mar 2022
Topic Review
Advanced Mass Spectrometry in Service of Forensic Analysis
Mass spectrometry has been used to assist forensic investigation. Due to its unique capabilities, mainly high-resolution mass data and structural information, high sensitivity, and cooperation with separation techniques, this method provides access to many tools streamlining and accelerating sample analysis. Low analyte consumption, advanced derivatization procedures and availability of isotopically labeled standards offer opportunities to study materials previously not considered viable evidence, opening new avenues in forensic investigations.
  • 1.6K
  • 25 Aug 2022
Topic Review
MGluRI and ErbB Receptors
It is well-appreciated that phosphorylation is an essential post-translational mechanism of regulation for several proteins, including group 1 metabotropic glutamate receptors (mGluRI), mGluR1 and mGluR5 subtypes. While contributions of various serine/threonine protein kinases on mGluRI modulation have been recognized, the functional role of tyrosine kinases (TKs) is less acknowledged. Here, we describe current evidence on the modulatory roles of the ErbB tyrosine kinases receptors - activated by the neurotrophic factors neuregulins (NRGs) - on mGluRI function. Available evidence suggests that mGluRI activity is tightly dependent on ErbB signaling, and that ErbB's modulation profoundly influences mGluRI-dependent effects on neurotransmission, neuronal excitability, synaptic plasticity, and learning and memory processes. 
  • 1.6K
  • 13 Nov 2020
Topic Review
Bacterial Ghosts-Based Vaccine
Bacterial ghosts (BGs) are empty bacterial envelopes of Gram-negative bacteria produced by controlled expressions of cloned gene E, forming a lysis tunnel structure within the envelope of the living bacteria.
  • 1.6K
  • 22 Dec 2021
Topic Review
Edible Flowers
Edible flowers have been widely consumed for ages until now. The attractive colors and shapes, exotic aroma, and delightful taste make edible flowers very easy to attain. Moreover, they also provide health benefits for consumers due to the unique composition and concentration of antioxidant compounds in the matrices. Knowing the bioactive compounds and their functional properties from edible flowers is necessary to diversify the usage and reach broader consumers.
  • 1.6K
  • 01 Jun 2021
Topic Review
Protease-Activated Receptors
Protease-activated receptors (PARs) are a class of G protein-coupled receptors (GPCRs) with a unique mechanism of activation, prompted by a proteolytic cleavage in their N-terminal domain that uncovers a tethered ligand, which binds and stimulates the same receptor.
  • 1.6K
  • 20 Feb 2021
Topic Review
The Pharmaceutical Industry in 2021
2021 will be remembered for the COVID-19 pandemic. Although five vaccines have been approved by the two most important drug regulatory agencies, namely the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA), the pandemic has still not been brought under control. However, despite the context of a global pandemic, 2021 has been an excellent year with respect to drug approvals by the FDA. In 2021, 50 drugs have been authorized, making it the fourth-best year after 2018 (59 drugs) and 1996 and 2020 (53 each). Regarding biologics, 2021 has been the third-best year to date, with 14 approvals, and it has also witnessed the authorization of 36 small molecules.
  • 1.6K
  • 21 Mar 2022
Topic Review
Honey in Reversing Metabolic Syndrome
Honey is a natural by-product from the flower nectar and aerodigestive tract of honey bees, which contains various complex biochemical components. Fructose (36%) and glucose (31%) are the main carbohydrate constituents of honey.
  • 1.6K
  • 18 Mar 2021
Topic Review
Gut Microbiota in Anxiety and Depression
The gut microbiota is critical for maintaining human health and the immunological system. Several neuroscientific studies have shown the significance of microbiota in developing brain systems. The gut microbiota and the brain are interconnected in a bidirectional relationship, as research on the microbiome–gut–brain axis shows. Significant evidence links anxiety and depression disorders to the community of microbes that live in the gastrointestinal system. Modified diet, fish and omega-3 fatty acid intake, macro- and micro-nutrient intake, prebiotics, probiotics, synbiotics, postbiotics, fecal microbiota transplantation, and 5-HTP regulation may all be utilized to alter the gut microbiota as a treatment approach. 
  • 1.6K
  • 13 Apr 2023
Topic Review
Eucalyptus globulus Leaves in Alzheimer’s Disease
Alzheimer’s disease (AD) is the most common neurodegenerative disorder affecting elderly people worldwide. Currently, there are no effective treatments for AD able to prevent disease progression, highlighting the urgency of finding new therapeutic strategies to stop or delay this pathology. Several plants exhibit potential as source of safe and multi-target new therapeutic molecules for AD treatment. Meanwhile, Eucalyptus globulus extracts revealed important pharmacological activities, namely antioxidant and anti-inflammatory properties, which can contribute to the reported neuroprotective effects.
  • 1.6K
  • 17 Aug 2022
Topic Review
Endocannabinoid System Present in the Glioblastoma Tumour Microenvironment
The highly aggressive and invasive glioblastoma (GBM) tumour is the most malignant lesion among adult-type diffuse gliomas, representing the most common primary brain tumour in the neuro-oncology practice of adults. With a poor overall prognosis and strong resistance to treatment, this nervous system tumour requires new, innovative treatment. GBM is a polymorphic tumour consisting of an array of stromal cells and various malignant cells contributing to tumour initiation, progression, and treatment response. Cannabinoids possess anti-cancer potencies against glioma cell lines and in animal models. To improve existing treatment, cannabinoids as functionalised ligands on nanocarriers were investigated as potential anti-cancer agents. The GBM tumour microenvironment is a multifaceted system consisting of resident or recruited immune cells, extracellular matrix components, tissue-resident cells, and soluble factors. 
  • 1.6K
  • 31 Jan 2024
Topic Review
Nanotechnology-Based Drug Delivery System for Phytochemical Compounds
According to the literature, 70% of the active ingredients obtained from plants are hydrophobic. New technology has been used as a strategy to increase the bioavailability/bioactivity of phytochemical compounds. In order to develop new nanotechnology-based therapies, the ability to design suitable formulations for drug delivery is of the utmost importance. Phytochemical delivery is essential for effective disease prevention and treatment. These delivery systems include lipid-based delivery systems and polymer-based delivery systems, which have the potential to increase the bioactivity of phytochemical compounds.
  • 1.6K
  • 07 Dec 2022
Topic Review
Flecainide in Ventricular Arrhythmias
Flecainide is an IC antiarrhythmic drug (AAD) that received in 1984 Food and Drug Administration approval for the treatment of sustained ventricular tachycardia (VT) and subsequently for rhythm control of atrial fibrillation (AF). Currently, flecainide is mainly employed for sinus rhythm maintenance in AF and the treatment of idiopathic ventricular arrhythmias (IVA) in absence of ischaemic and structural heart disease on the basis of CAST data. Recent studies enrolling patients with different structural heart diseases demonstrated good effectiveness and safety profile of flecainide.
  • 1.6K
  • 10 Sep 2021
Topic Review
CO2 Pneumoperitoneum
Laparoscopy (LS) has been shown to decrease the inflammatory sequelae of endotoxemia. β-arrestin 2 plays an important function in signal transduction pathway of TLR4. High mobility group box-1 (HMGB-1) is involved in the delayed systemic inflammatory response. We investigated the effects of CO2 insufflation on liver, lung, and kidney expression of both β-arrestin 2 and HMGB-1 during sepsis. Cecal ligation and puncture (CLP) was performed in male rats and 6 h later the animals were randomly assigned to receive a CO2 pneumoperitoneum or laparotomy. Animals were euthanized; liver, lung, and kidney were removed for the evaluation of β-arrestin 2 and HMGB-1 expression. Immunohistochemical detection of myeloperoxidase (MPO) was investigated in lung and liver and bacterial load was determined in the peritoneal fluid. CO2 pneumoperitoneum reduced peritoneal bacterial load, increased the expression of β-arrestin 2, and blunted the expression of the potent proinflammatory HMGB-1 in liver, lung, and kidney compared with laparotomy. Liver and lung MPO was markedly reduced in rats subjected to LS compared with laparotomy. We believe that CO2 exerts an early protective effect by reducing bacterial load and likely toll-like receptor activation which in turn leads to a preserved β-arrestin 2 expression and a reduced HMGB-1 expression.
  • 1.6K
  • 02 Nov 2020
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