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Topic Review
Antibacterial Prodrugs to Overcome Bacterial Resistance
Prodrugs are pharmacologically inactive entities of active drugs that undergo biotransformation before eliciting their pharmacological effects. A prodrug strategy can be used to revive drugs discarded due to a lack of appropriate pharmacokinetic and drug-like properties, or high host toxicity. A special advantage of the use of the prodrug approach in the era of bacterial resistance is targeting resistant bacteria by developing prodrugs that require bacterium-specific enzymes to release the active drug. 
  • 1.4K
  • 29 Feb 2024
Topic Review
Cyclo- and Polyphosphazenes for Biomedical Applications
Cyclic and polyphosphazenes are extremely interesting and versatile substrates characterized by the presence of -P=N- repeating units. The chlorine atoms on the P atoms in the starting materials can be easily substituted with a variety of organic substituents, thus giving rise to a huge number of new materials for industrial applications. A wide variety of new phosphazene systems, either trimeric or polymeric, have been developed as biomaterials in view of different applications. The materials to apply in biomedical applications should be biocompatible.
  • 1.4K
  • 09 Dec 2022
Topic Review
Drug Carriers for Arthritis Therapy
Drug carriers are used to penetrate the biological barriers and deliver the requisite active pharmaceutical ingredients (API). This has greater significance for medication in arthritis therapies because the inflammatory progression of rheumatoid arthritis (RA) and osteoarthritis (OA) is complex, intertwined, and influenced by one another. For this purpose, the drug delivery systems (DDS) of this carrier are currently being investigated with exogenous triggers and endogenous stimuli. This flexible-release invention will solve the problems of multiple implantations and local toxic accumulation at the lesion sites.
  • 1.4K
  • 10 Nov 2022
Topic Review
Effects of Hydroxytyrosol in Endothelial Functioning
Pharmacologists have been emphasizing and applying plant and herbal-based treatments in vascular diseases. Olives, for example, are a traditional symbol of the Mediterranean diet. Hydroxytyrosol is an olive-derived compound known for its antioxidant and cardioprotective effects. Acknowledging the merit of antioxidants in maintaining endothelial function warrants the application of hydroxytyrosol in endothelial dysfunction salvage and recovery. Endothelial dysfunction (ED) is an impairment of endothelial cells that adversely affects vascular homeostasis. Disturbance in endothelial functioning is a known precursor for atherosclerosis and, subsequently, coronary and peripheral artery disease.
  • 1.4K
  • 10 Mar 2023
Topic Review
Soluble Guanylyl Cyclase Activators
The guanylyl cyclase (sGC) is heme-containing enzyme, which causes an increase in the level of cyclic 3′-5′-guanosine monophosphate (cGMP) in smooth muscle and subsequent vascular relaxation.
  • 1.4K
  • 10 May 2023
Topic Review
Lectin Protein
Lectins are natural proteins with the ability to bind specific carbohydrates related to various microorganisms, including viruses, bacteria, fungi and parasites. Lectins have the ability to agglutinate and neutralize these pathogeneses. The delivery of the encapsulated antiviral agents or vaccines across the cell membrane can be possible by functionalized micellar and liposomal formulations. 
  • 1.4K
  • 14 Apr 2022
Topic Review
Nod-Like Receptors
The nucleotide-binding domain and leucine-rich-repeat-containing family (NLRs) (sometimes called the NOD-like receptors, though the family contains few bona fide receptors) are a superfamily of multidomain-containing proteins that detect cellular stress and microbial infection.
  • 1.4K
  • 29 Jun 2021
Topic Review
Glycemic Control
Experimental evidence suggests that cadmium (Cd) boosts oxidative stress that may result in toxicity on the endocrine system also in humans. The aim of this study was to investigate the glycemic control and oxidative stress markers in male adolescents with increased urinary levels of cadmium. We investigated 111 males, aged 12–14 years, living in a polluted area of Sicily and a control age-matched population (n = 60) living 28–45 km far from the polluted site. Malondialdehyde (MDA), total antioxidant activity (TAC), metallothionein-1A (MT-1A) gene expression, insulin resistance by the homeostatic model assessment (HOMA-IR), and urinary cadmium were investigated. Cd levels were significantly higher in adolescents living in the polluted area than in control age-matched subjects. Adolescents with elevated Cd levels had a significant increase in MDA, MT-1A, and HOMA-IR and reduced TAC compared to the control group. A robust correlation was found between urinary cadmium and MT-1A, HOMA-IR, and MDA whereas an inverse correlation was identified between urinary cadmium and TAC. This study indicates that cadmium burden alters glycemic control in adolescents and suggests that oxidative stress plays a key role in cadmium-induced insulin resistance, increasing the risk of developing metabolic disorders.
  • 1.4K
  • 01 Nov 2020
Topic Review
Oral Bioavailability and Regulatory Aspects
Oral bioavailability refers to the extent a substance or drug becomes completely available to systemic circulation or to its intended biological destination(s) via the oral route. High oral bioavailability reduces the amount of a drug necessary to achieve a desired pharmacological effect, therefore reducing the risk of side-effects and toxicity. Low oral bioavailability results in low efficacy and is a major reason for drug candidates failing to reach the market. Hence, oral bioavailability is one of the most important properties in drug design and development.
  • 1.4K
  • 11 Oct 2021
Topic Review
Sex Differences in Dopamine Receptors
Dopamine is an important neurotransmitter that plays a key role in neuropsychiatric illness.
  • 1.4K
  • 28 Sep 2021
Topic Review
The Pharmacological Activities of Siraitia grosvenorii 
Siraitia grosvenorii (Swingle) C. Jeffrey ex Lu et Z. Y. Zhang is a unique economic and medicinal plant of Cucurbitaceae in Southern China. For hundreds of years, Chinese people have used the fruit of S. grosvenorii as an excellent natural sweetener and traditional medicine for lung congestion, sore throat, and constipation. It is one of the first species in China to be classified as a medicinal food homology, which has received considerable attention as a natural product with high development potential. Various natural products, such as triterpenoids, flavonoids, amino acids, and lignans, have been released from this plant by previous phytochemical studies. Pharmacological research of the fruits of S. grosvenorii has attracted extensive attention, and an increasing number of extracts and compounds have been demonstrated to have antitussive, expectorant, antiasthmatic, antioxidant, hypoglycemic, immunologic, hepatoprotective, antibacterial, and other activities.
  • 1.4K
  • 04 Nov 2022
Topic Review
Application of Probiotics for Acne Vulgaris Topical Therapies
The skin microbiome is an essential barrier for preventing the invasion of pathogens and regulating the immune responses. When this barrier is disrupted, several dermatoses, including acne vulgaris, may arise. Probiotics have proven to be an alternative to the use of antibiotics, often associated with undesirable effects, in the treatment and prevention of dermatological disorders such as acne. 
  • 1.4K
  • 30 May 2023
Topic Review
CCL-11 or Eotaxin-1
CCL-11 (eotaxin) is a chemokine with an important role in allergic conditions. Recent evidence indicates that CCL-11 plays a role in brain disorders as well. CCL-11 is rapidly transported from the blood to the brain through the blood-brain barrier. Age-related increases in CCL-11 are associated with cognitive impairments in executive functions and episodic and semantic memory, and therefore, this chemokine has been described as an “Endogenous Cognition Deteriorating Chemokine” (ECDC) or “Accelerated Brain-Aging Chemokine” (ABAC).
  • 1.4K
  • 16 Apr 2021
Topic Review
Lipopolysaccharide, Inflammation and Mitochondria-Targeted Antioxidants
Lipopolysaccharide (LPS), the major component of the outer membrane of Gram-negative bacteria, is the most abundant proinflammatory agent. Considerable evidence indicates that LPS challenge inescapably causes oxidative stress and mitochondrial dysfunction, leading to cell and tissue damage. Increased mitochondrial reactive oxygen species (mtROS) generation triggered by LPS is known to play a key role in the progression of the inflammatory response. mtROS at excessive levels impair electron transport chain functioning, reduce the mitochondrial membrane potential, and initiate lipid peroxidation and oxidative damage of mitochondrial proteins and mtDNA. Over the past 20 years, a large number of mitochondria-targeted antioxidants (mito-AOX) of different structures that can accumulate inside mitochondria and scavenge free radicals have been synthesized. Their protective role based on the prevention of oxidative stress and the restoration of mitochondrial function has been demonstrated in a variety of common diseases and pathological states.
  • 1.4K
  • 16 Apr 2021
Topic Review
Toxin Genes of Bacillus cereus
Bacillus cereus is a ubiquitous soil bacterium responsible for two types of food-associated gastrointestinal diseases. While the emetic syndrome is caused by the cyclic depsipeptide cereulide, proteinaceous enterotoxins provoke the diarrheal disease. Here, an overview on the distribution of the main toxin genes/operons ces (encoding cereulide), hbl (encoding the tripartite hemolysin BL), nhe (encoding the tripartite non-hemolytic enterotoxin), and cytK (encoding the single protein cytotoxin K) within the B. cereus group is given.
  • 1.4K
  • 18 Feb 2021
Topic Review
Advanced Drug Delivery for Treating Sjögren’s Dry Eye
Sjögren’s syndrome is a chronic and insidious autoimmune disease characterized by lymphocyte infiltration of exocrine glands. Patients typically present with dry eye (keratoconjunctivitis sicca), dry mouth (xerostomia), and other systemic manifestations. The current management for Sjögren's syndrome dry eye (SSDE) has been ineffective as it only targets ocular surface inflammation and dryness without addressing the specific disease process. Ophthalmologists often adopt a trial-and-error approach, which allows the cycle of dry eye disease (DED) to progress and potentially cause permanent damage to the lacrimal functional unit. Topical treatments also depend on patients' ability to administer eye drops and their compliance. These limitations emphasize the need for personalized, targeted treatments that address the underlying pathophysiology of SSDE. This article aims to present new advances in ocular drug delivery for more effective treatment.
  • 1.4K
  • 10 Feb 2023
Topic Review
Factors Affecting Vitamin C Pharmacokinetics
The pharmacokinetics of vitamin C (vitC) is highly complex. Regulated primarily by a family of saturable sodium dependent vitC transporters (SVCTs), both the absorption and elimination phases display high dose-dependency. Also, tissue specific expression of SVCT subtypes result in a diverse distribution pattern with organ concentrations of vitC at homeostasis ranging from about 0.2 mM up to 10 mM. Unfortunately, the complex pharmacokinetics of vitC has often been overlooked in the design of human intervention studies, giving rise to misinterpretations and erroneous conclusions.
  • 1.4K
  • 23 Sep 2022
Topic Review
Differential Inhibitors of Aldose Reductase
Aldose reductase, classified within the aldo-keto reductase family as AKR1B1, is an NADPH dependent enzyme that catalyzes the reduction of hydrophilic as well as hydrophobic aldehydes. AKR1B1 is the first enzyme of the so-called polyol pathway that allows the conversion of glucose into sorbitol, which in turn is oxidized to fructose by sorbitol dehydrogenase. The activation of the polyol pathway in hyperglycemic conditions is generally accepted as the event that is responsible for a series of long-term complications of diabetes such as retinopathy, cataract, nephropathy and neuropathy. The role of AKR1B1 in the onset of diabetic complications has made this enzyme the target for the development of molecules capable of inhibiting its activity.
  • 1.4K
  • 11 Apr 2022
Topic Review
Nintedanib
Nintedanib is a synthetic orally active tyrosine kinase inhibitor, whose main action is to inhibit the receptors of the platelet-derived growth factor, fibroblast growth factor and vascular endothelial growth factor families.
  • 1.4K
  • 30 Sep 2021
Topic Review
Traditional Medicinal Uses of Yingzhao
The medicinal plant Artabotrys hexapetalus (synonyms: A.uncinatus and A. odoratissimus) is known as yingzhao in Chinese. Extracts of the plant have long been used in Asian folk medicine to treat various symptoms and diseases, including fevers, microbial infections, ulcers, hepatic disorders and other health problems. In particular, extracts from the roots and fruits of the plant are used for treating malaria. Numerous bioactive natural products have been isolated from the plant, mainly aporphine (artabonatines, artacinatine) and benzylisoquinoline (hexapetalines) alkaloids, terpenoids (artaboterpenoids), flavonoids (artabotrysides), butanolides (uncinine, artapetalins) and a small series of endoperoxides known as yingzhaosu A-to-D. These natural products confer antioxidant, anti-inflammatory and antiproliferative properties to the plant extracts. The lead compound yingzhaosu A displays marked activities against the malaria parasites Plasmodium falciparum and P. berghei.
  • 1.4K
  • 27 Sep 2022
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