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Topic Review
Roxadustat
Roxadustat is the first oral drug in the class of new erythropoiesis drugs and a potent HIF-PHD inhibitor, exerted to treat anemia in patients with CKD. In phase 1, 2 and 3 studies with CKD-affected patients, roxadustat was more effective to stimulate erythropoiesis for anemia correction than previously used drugs. Roxadustat can be orally given, unlike other erythropoiesis drugs with parenteral administration only, which grants roxadustat a considerable advantage.
  • 1.4K
  • 16 Mar 2021
Topic Review
Formulation Strategies to Improve Pharmacokinetics Profile
The oral route is the most common and practical means of drug administration, particularly from a patient’s perspective. However, the pharmacokinetic profile of oral drugs depends on the rate of drug absorption through the intestinal wall before entering the systemic circulation. However, the enteric epithelium represents one of the major limiting steps for drug absorption, due to the presence of efflux transporters on the intestinal membrane, mucous layer, enzymatic degradation, and the existence of tight junctions along the intestinal linings. These challenges are more noticeable for hydrophilic drugs, high molecular weight drugs, and drugs that are substrates of the efflux transporters. Another challenge faced by oral drug delivery is the presence of first-pass hepatic metabolism that can result in reduced drug bioavailability. Over the years, a wide range of compounds have been investigated for their permeation-enhancing effect in order to circumvent these challenges. There is also a growing interest in developing nanocarrier-based formulation strategies to enhance the drug absorption.
  • 1.4K
  • 26 Aug 2022
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
Topic Review
The Coming of Age of Biosimilars: Perspective
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 Many firsts were to follow in the US: the first mAb (bevacizumab), the first pegylated cytokine (pegfilgrastim), the first ophthalmic biosimilar (ranibizumab), and the first two interchangeable biosimilars (insulin glargine and adalimumab). The US also approved the first biosimilars without clinical efficacy testing (filgrastim, pegfilgrastim, and erythropoietin alfa).
  • 1.4K
  • 02 Jun 2022
Topic Review
Beta-Blockers
Beta-blockers are a class of drugs with important benefits in cardiovascular pathology. The neuropsychiatric and cognitive effects of beta-blockers were proven many years ago.
  • 1.4K
  • 03 Mar 2021
Topic Review
Gender Differences and NPS
Sex and gender deeply affect the subjective effects and the pharmaco-toxicological responses to drugs. Men are more likely than women to use almost all types of illicit drugs and to present to emergency departments for serious or fatal intoxications. However, women are just as likely as men to develop substance use disorders, and may be more susceptible to craving and relapse.
  • 1.4K
  • 26 Oct 2020
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
Ion Channels of Nociception
Acute pain plays the vital role protecting our health whereas chronic and pathological pain are debilitating conditions.  However molecular mechanisms of pain which are the keys for pain relief remain largely unaddressed. Nevertheless, new molecular actors with important roles in pain mechanisms are being characterized, such as the mechanosensitive Piezo ion channels. This study presents modern trends and promising advances in the field of molecular mechanisms of pain. 
  • 1.4K
  • 24 Mar 2021
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
Engineering Drug Delivery Systems
Engineering drug delivery systems (DDS) aim to release bioactive cargo to a specific site within the human body safely and efficiently. Hydrogels have been used as delivery matrices in different studies due to their biocompatibility, biodegradability, and versatility in biomedical purposes. Microparticles have also been used as drug delivery systems for similar reasons. The combination of microparticles and hydrogels in a composite system has been the topic of many research works. These composite systems can be injected in loco as DDS. The hydrogel will serve as a barrier to protect the particles and retard the release of any bioactive cargo within the particles. Additionally, these systems allow different release profiles, where different loads can be released sequentially, thus allowing a synergistic treatment. The reported advantages from several studies of these systems can be of great use in biomedicine for the development of more effective DDS.
  • 1.4K
  • 04 Oct 2021
Topic Review
Ivermectin for the Treatment and/or Prophylaxis of COVID-19
The pathogenesis of Coronavirus Disease 2019 (COVID-19) is initiated by viral entry through the angiotensin-converting enzyme 2 (ACE-2) receptor in the host cell. After entry, RNA is translated into viral proteins upon its release in the cytoplasm. The resulting symptoms and clinical manifestations include fever, headache, myalgia, and respiratory symptoms. Several drugs have been and continue to be repurposed for the prophylaxis and treatment of COVID-19. Ivermectin (IVM) belongs to the naturally occurring family of avermectins produced by the bacterium Streptomyces avermitilis. Its broad antiparasitic spectrum is achieved through the hyperpolarization of the invertebrate’s cell membrane, with subsequent parasite paralysis. It was tested and confirmed for its in vitro antiviral activity against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). Trials have put IVM to test for both the treatment and prophylaxis of COVID-19, as well as its potential role in combination therapy. Additionally, the targeted delivery of IVM was studied in animals and COVID-19 patients.
  • 1.4K
  • 31 Oct 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
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
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
Natural Peptides and Their Beneficial Effects on Skin
Peptides, functional nutrients with a size between those of large proteins and small amino acids, are easily absorbed by the human body. Therefore, they are seeing increasing use in clinical medicine and have revealed immunomodulatory and anti-inflammatory properties which could make them effective in healing skin wounds.
  • 1.4K
  • 17 Feb 2023
Topic Review
Anthocyanin Bioactivity in Obesity
Obesity and type-2 diabetes trends continue to worsen in the United States. Dietary anthocyanins (typically provided by berries and other fruits) are reported to have protective effects against both conditions using a variety of experimental research models including animal and human feeding studies. This review highlights studies that explore the biochemical pathways in both tissue and rodent models which could explain clinical improvements noted with anthocyanin consumption. First, the primary mode of intestinal absorption of anthocyanins is through both sGLT1 and GLUT2 glucose transporters. Stronger binding affinities may allow anthocyanins to be more inhibitive to glucose absorption compared to the reverse, where GLUT2 expression may also be affected. Genetic or chemical inhibition of sGLT1 or GLUT2 demonstrate their essential function in anthocyanin absorption across the enterocyte, where the former interacts with a greater variety of anthocyanins but the latter is the major transporter for specific anthocyanin-glycosides. Once absorbed, anthocyanins positively modulate GLUT4 density and function in both skeletal muscle and adipose tissues via the upregulation of AMPK and restoration of insulin sensitivity. Antioxidant properties and phosphodiesterase inhibition by anthocyanins promote both mitochondrial function and density which could be novel targets for dietary management of obesity and its complications.
  • 1.4K
  • 01 Dec 2020
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
Adiponectin System (Rescue Hormone)
The adipose tissue, regardless of its role in generating and storing energy, acts as a key player as an endocrine tissue, producing a wide scale of cytokines/hormones called adipokines. Adipokines such as leptin, resistin, visfatin and osteopontin own pro-inflammatory effects on the cardiovascular system in some cases. In contrast, some adipokines have cardioprotective and anti-inflammatory impacts including adiponectin, omentin, and apelin.
  • 1.4K
  • 12 Jul 2022
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
RONS and Myokines in Skeletal Muscle Glucose Uptake
The skeletal muscle is the largest organ in the body that performs different functions, including those related to the movement of the body such as stability, equilibrium, and locomotion; vital functions such as breathing; and those associated with the maintenance of metabolic homeostasis, in which the generation and expenditure of energy and heat production are critical. The adequate interplay of these functions leads to the maintenance of life in organisms. Glucose is essential in metabolism since it is one of the main substrates that produces ATP, the key molecule that transfers energy during chemical reactions in organisms. To produce ATP, glucose needs to be transported from the extracellular space into the cytosol of the cell. This process is called glucose uptake, and it is critical in skeletal muscle since it provides enough glucose to the cell to produce ATP and satisfy the high demand for energy of the skeletal muscle. Glucose uptake in skeletal muscle tissue is a process mainly regulated by insulin, which is a hormone synthesized in the pancreas and released into the blood stream, where it is transported until it binds to specific insulin receptors that are anchored at the plasma membrane of skeletal muscle cells.
  • 1.4K
  • 23 Dec 2022
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