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Topic Review
Aripiprazole Lauroxil
Aripiprazole lauroxil is a prodrug of aripiprazole and is administered as an intramuscular injection. Once administered, aripiprazole lauroxil is first converted to N-hydroxymethyl aripiprazole by enzyme-mediated hydrolysis and is hydrolyzed again to aripiprazole. Aripiprazole was originally reported to be a partial agonist at D2and 5HT1Areceptors, with a combination of antagonistic activity at 5HT2Areceptors.
  • 1.1K
  • 18 Jul 2021
Topic Review
FAAH, MAGL, and DAGL in Obesity Treatment
The endocannabinoid system (ECS) plays an integral role in maintaining metabolic homeostasis and may affect hunger, caloric intake, and nutrient absorption. Obesity has been associated with higher levels of the endogenous cannabinoid transmitters (endocannabinoids). Therefore, the ECS is an important target in obesity treatment. Modulating the enzymes that synthesize and degrade endocannabinoids, namely fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), and diacylglycerol lipase (DAGL), may be a promising strategy to treat obesity.
  • 1.1K
  • 18 Jan 2022
Topic Review
Sustained Antiviral Ocular Drug Delivery
The eyes are the window to the world and the key to communication, but they are vulnerable to multitudes of ailments. More serious than is thought, corneal infection by herpes simplex viruses (HSVs) is a prevalent yet silent cause of blindness in both the paediatric and adult population, especially if immunodeficient. Globally, there are 1.5 million new cases and forty thousand visual impairment cases reported yearly. The Herpetic Eye Disease Study recommends topical antiviral as the front-line therapy for HSV keratitis. Ironically, topical eye solutions undergo rapid nasolacrimal clearance, which necessitates oral drugs but there is a catch of systemic toxicity. The hurdle of antiviral penetration to reach an effective concentration is further complicated by drugs’ poor permeability and complex layers of ocular barriers.
  • 1.1K
  • 02 Feb 2021
Topic Review
Magnetic Molecularly Imprinted Polymers
The combination of molecular imprinting technology with magnetic nanoparticles provides a new class of smart hybrids, i.e., magnetic molecularly imprinted polymers (MMIPs) to overcome limitations in current cancer therapy. The application of these complexes is gaining more interest in therapy, due to their favorable properties, namely, the ability to be guided and to generate slight hyperthermia with an appropriate external magnetic field, alongside the high selectivity and loading capacity of imprinted polymers toward a template molecule. In cancer therapy, using the MMIPs as smart-drug-delivery robots can be a promising alternative to conventional direct administered chemotherapy, aiming to enhance drug accumulation/penetration into the tumors while fewer side effects on the other organs. 
  • 1.1K
  • 23 Sep 2020
Topic Review
Pharmacogenetic Testing
Pharmacogenomics is a study of how the genome background is associated with drug resistance and how therapy strategy can be modified for a certain person to achieve benefit. The pharmacogenomics (PGx) testing becomes of great opportunity for physicians to make the proper decision regarding each non-trivial patient that does not respond to therapy. Although pharmacogenomics has become of growing interest to the healthcare market during the past five to ten years the exact mechanisms linking the genetic polymorphisms and observable responses to drug therapy are not always clear. Therefore, the success of PGx testing depends on the physician’s ability to understand the obtained results in a standardized way for each particular patient. The review aims to lead the reader through the general conception of PGx and related issues of PGx testing efficiency, personal data security, and health safety at a current clinical level.
  • 1.1K
  • 07 Jan 2021
Topic Review
Nanoparticles in the Intestinal Epithelial Cell Membrane
Intestinal epithelial cells are the most abundant epithelial cells in the intestine, accounting for 90–95% of intestinal cells. They are columnar cells with hair-like projections called microvilli on the apical membrane, which greatly increase the surface area available for absorption. The transintestinal cell pathway refers to the process in which nanoparticles pass through apical and basolateral membranes via intercellular transport and then discharge from the basement membrane to the extracellular space. The entire process can be divided into three stages: the uptake of nanoparticles in the apical membrane of intestinal epithelial cells, the transport of endosomes in the cytoplasm and the exocytosis of nanoparticles in the basement membrane.
  • 1.0K
  • 05 Jul 2023
Topic Review
Bone Mass Loss during Menopause
Antiosteoporotic Activity of Genistein Aglycone in Postmenopausal Women: Evidence from a Post-Hoc Analysis of a Multicenter Randomized Controlled Trial. Genistein has a preventive role against bone mass loss during menopause. However, experimental data in animal models of osteoporosis suggest an anti-osteoporotic potential for this isoflavone. We performed a post-hoc analysis of a previously published trial investigating the effects of genistein in postmenopausal women with low bone mineral density. The parent study was a randomized, double-blind, placebo-controlled trial involving postmenopausal women with a femoral neck (FN) density <0.795 g/cm². A cohort of the enrolled women was, in fact, identified at the baseline as osteoporotic (n = 121) on the basis of their T-score and analyzed thereafter for the 24 months' treatment with either 1000 mg of calcium and 800 IU vitamin D3 (placebo; n = 59); or calcium, vitamin D3, and Genistein aglycone (54 mg/day; genistein; n = 62). According to the femoral neck T-scores, 31.3% of the genistein and 30.9% of the placebo recipients were osteoporotic at baseline. In the placebo and genistein groups, the 10-year hip fracture probability risk assessed by Fracture Risk Assessment tool (FRAX) was 4.1 ± 1.9 (SD) and 4.2 ± 2.1 (SD), respectively. Mean bone mineral density (BMD) at the femoral neck increased from 0.62 g/cm² at baseline to 0.68 g/cm² at 1 year and 0.70 g/cm² at 2 years in genistein recipients, and decreased from 0.61 g/cm² at baseline to 0.60 g/cm² at 1 year and 0.57 g/cm² at 2 years in placebo recipients. At the end of the study only 18 postmenopausal women had osteoporosis in the genistein group with a prevalence of 12%, whereas in the placebo group the number of postmenopausal women with osteoporosis was unchanged, after 24 months. This post-hoc analysis is a proof-of concept study suggesting that genistein may be useful not only in postmenopausal osteopenia but also in osteoporosis. However, this proof-of concept study needs to be confirmed by a large, well designed, and appropriately focused randomized clinical trial in a population at high risk of fractures.
  • 1.0K
  • 01 Nov 2020
Topic Review
Unconventional Treatment of Biofilm Infection
Today, researchers are looking at new ways to treat severe infections caused by resistance to standard antibiotic therapy. This is quite challenging due to the complex and interdependent relationships involved: the cause of infection–the patient–antimicrobial agents. The sessile biofilm form is essential in research to reduce resistance to very severe infections (such as ESKAPE pathogens: Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumanni, Pseudomonas aeruginosa, and Enterobacter spp). The purpose of this study is to elucidate the mechanisms of the occurrence, maintenance, and suppression of biofilm infections. One form of biofilm suppression is the efficient action of natural antagonists of bacteria—bacteriophages. Bacteriophages effectively penetrate the biofilm’s causative cells. They infect those bacterial cells and either destroy them or prevent the infection from spreading. In this process, bacteriophages are specific, relatively easy to apply, and harmless to the patient. Antimicrobial peptides (AMPs) support the mechanisms of bacteriophages’ action. AMPs could also attack and destroy infectious agents on their own (even on biofilm). AMPs are simple, universal peptide molecules, mainly cationic peptides. Additional AMP research could help develop even more effective treatments of biofilm (bacteriophages, antibiotics, AMPs, nanoparticles). This is a review of recent unconventional agents, such as bacteriophages and AMPs, used for the eradication of biofilm, providing an overview of potentially new biofilm treatment strategies.
  • 1.0K
  • 20 Oct 2020
Topic Review Peer Reviewed
Biofunctional Peptide FNIII14: Therapeutic Potential
Biofunctional peptide FNIII14, which is derived from the 14th fibronectin (FN) type III-like (FN-III) repeat of FN molecule, is capable of inhibiting cell adhesion to the extracellular matrix (ECM). This functional site is usually buried within the molecular structure of FN, but can be exposed by conformational changes and proteolytic cleavage. Peptide FNIII14 can induce a conformational change in β1-integrin from the active to the inactive form, causing functional inactivation. Based on this anti-adhesive activity, peptide FNIII14 exhibits therapeutic potential for several diseases such as metabolic diseases, organ fibrosis, and malignant tumors. Peptide FNIII14 blocks integrin-mediated signaling by a mechanism entirely distinct from that of conventional antagonisitic peptides, including Arg-Gly-Asp peptides that competitively inhibit the ECM binding of integrin. 
  • 1.0K
  • 13 Apr 2022
Topic Review
Pharmacomicrobiomics and Drug–Infection Interactions
Microorganisms have a close relationship with humans, whether it is commensal, symbiotic, or pathogenic. It has been documented that microorganisms may influence the response to drug therapy. Pharmacomicrobiomics is an emerging field that focuses on the study of how variations in the microbiome affect the disposition, action, and toxicity of drugs. Two additional sciences have been added to complement pharmacomicrobiomics, namely toxicomicrobiomics, which explores how the microbiome influences drug metabolism and toxicity, and pharmacoecology, which refers to modifications in the microbiome as a result of drug administration. Additionally, the concept of "drug-infection interaction" is included to describe the influence of pathogenic microorganisms on drug response. This entry analyzes in detail each of these concepts.
  • 1.0K
  • 05 Jan 2024
Topic Review
Novel Pyridothienopyrimidine Derivatives
The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set of pyridothienopyrimidine derivatives 2a,b–9a,b was synthesized via cyclization reactions of 3-amino-thieno[2,3-b]pyridine-2-carboxamides 1a,b with different reagents. All new compounds were evaluated against five bacterial and five fungal strains. Many of the target compounds showed significant antimicrobial activity. In addition, the new derivatives were further subjected to cytotoxicity evaluation against HepG-2 and MCF-7 cancer cell lines. The most potent cytotoxic candidates (3a, 4a, 5a, 6b, 8b and 9b) were examined as EGFR kinase inhibitors. 
  • 1.0K
  • 10 Feb 2022
Topic Review
Bioactive Phytochemicals from Ruta angustifolia Pers.
The genus Ruta in the family Rutaceae includes about 40 species, such as the well-known plants R. graveolens L. (common rue) or R. chalepensis L. (fringed rue), but also much lesser-known species such as R. angustifolia Pers. (narrow-leaved fringed rue). This rue specie, originating from the Mediterranean region, is well-distributed in Southeast Asia, notably in the Indo-Chinese peninsula and other territories. In some countries, such as Malaysia, the plant is used to treat liver diseases and cancer. Extracts of R. angustifolia display antifungal, antiviral and antiparasitic effects. Diverse bioactive natural products have been isolated from the aerial parts of the plant, notably quinoline alkaloids and furocoumarins, which present noticeable anti-inflammatory, antioxidant and/or antiproliferative properties.
  • 1.0K
  • 23 Feb 2023
Topic Review
Potential Benefits of Herbal Medicines in Lupus Conditions
Systemic lupus erythematosus (SLE) is an autoimmune disease involving multiple organs and clinical manifestations. The Latin word lupus, meaning wolf, was in the medical literature prior to the 1200s to describe skin lesions that devour flesh, and the resources available to physicians to help people were limited. The present text reviews the ethnobotanical and pharmacological aspects of medicinal plants and purified molecules from natural sources with efficacy against lupus conditions. Among these molecules are artemisinin and its derivatives, antroquinonol, baicalin, curcumin, emodin, mangiferin, salvianolic acid A, triptolide, the total glycosides of paeony (TGP), and other supplements such as fatty acids and vitamins. In addition, medicinal plants, herbal remedies, mushrooms, and fungi that have been investigated for their effects on different lupus conditions through clinical trials, in vivo, in vitro, or in silico studies are reviewed. A special emphasis was placed on clinical trials, active phytochemicals, and their mechanisms of action. This discussion can be helpful for researchers in designing new goal-oriented studies. It can also help practitioners gain insight into recent updates on supplements that might help patients suffering from lupus conditions.
  • 1.0K
  • 26 Jul 2023
Topic Review
α-Melanocytic Hormone
The melanocortin system encompasses melanocortin peptides, five receptors, and two endogenous antagonists. Besides pigmentary effects generated by α-Melanocytic Hormone (α-MSH), new physiologic roles in sexual activity, exocrine secretion, energy homeostasis, as well as immunomodulatory actions, exerted by melanocortins, have been described recently. 
  • 1.0K
  • 02 Feb 2021
Topic Review
Chitosan-Based Nano-Smart Drug Delivery System in Breast Cancer
Chitosan nanoparticles (CSNPs) have prospects as a revolutionary delivery system capable of enhancing anticancer drug activity and reducing negative impacts on normal cells. The use of smart drug delivery systems (SDDs) as delivering materials to improve the bioactivity of NPs and to understand the intricacies of breast cancer has garnered significant interest. 
  • 1.0K
  • 16 May 2023
Topic Review
Ferulic Acid in Animal Models of Alzheimer’s Disease
Alzheimer’s disease (AD) is a neurodegenerative disease with a high incidence in the elderly. Many preclinical studies show that a natural product, ferulic acid (FA), displays neuroprotective effects in AD models. 
  • 1.0K
  • 27 Oct 2021
Topic Review
Therapeutic Potential of Myrtenal and Its Derivatives
Myrtenal is a perspective monoterpenoid with therapeutic potential in various fields of medicine. Its chemical modifications often lead to new or more pronounced biological effects. As an example, the conjugation of myrtenal with the established pharmacophore adamantane enables the augmentation of several of its pivotal properties. Myrtenal–adamantane derivatives exhibited a variety of beneficial characteristics, such as antimicrobial, antifungal, antiviral, anticancer, anxiolytic, and neuroprotective properties, which are worth examining in more detail and at length.
  • 1.0K
  • 30 Oct 2023
Topic Review
Oral siRNA Delivery for Inflammatory Bowel Disease Treatments
RNA interference (RNAi) therapies have significant potential for the treatment of inflammatory bowel diseases (IBD). Oral nanomedicines carrying small interfering RNA (siRNA) drugs include the following two: (1) Polyplex or lipoplex. (2) Polyplex or lipoplex embedded in hydrogels or polymeric materials
  • 1.0K
  • 11 Oct 2022
Topic Review
Nitroglycerin (Drug)
Nitroglycerin, also known as glyceryl trinitrate (GTN), is a medication used for heart failure, high blood pressure, and to treat and prevent chest pain from not enough blood flow to the heart (angina) or due to cocaine. This includes chest pain from a heart attack. It is taken by mouth, under the tongue, applied to the skin, or by injection into a vein. Common side effects include headache and low blood pressure. The low blood pressure can be severe. It is unclear if use in pregnancy is safe for the baby. It should not be used together with medications within the sildenafil (PDE5 inhibitor) family due to the risk of low blood pressure. Nitroglycerin is in the nitrate family of medications. While it is not entirely clear how it works, it is believed to function by dilating blood vessels. Nitroglycerin was written about as early as 1846 and came into medical use in 1878. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. The wholesale cost in the developing world as of 2014, was US$0.06–0.22 per dose by mouth. The drug nitroglycerin (GTN) is a dilute form of the same chemical used as the explosive, nitroglycerin. Dilution makes it non-explosive.
  • 1.0K
  • 25 Oct 2022
Topic Review
κ-Opioid Receptor Agonists
The κ-opioid receptor (KOR) belongs to the class of inhibitory G protein-coupled receptors (GPCRs), widely expressed throughout the central nervous system and peripheral tissues. Due to the implications of KOR activation, KOR agonists have attracted recent attention for their ability to produce analgesia without the harmful side effects typically associated with MOR activation. In addition, KOR agonists show the potential for the treatment of pruritis, multiple sclerosis, Alzheimer’s disease, immune mediated diseases such as osteoarthritis, atopic dermatitis, food allergy, gastrointestinal diseases, cancer, hypoxia and ischemia.
  • 1.0K
  • 20 Feb 2023
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