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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.
  • 631
  • 20 Feb 2023
Topic Review
Novel Antituberculosis Agents
Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), is a curable airborne disease currently treated using a drug regimen consisting of four drugs.
  • 630
  • 21 May 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.
  • 630
  • 04 Nov 2022
Topic Review
Non-Steroidal Anti-Inflammatory Drugs
The non-steroidal anti-inflammatory drugs (NSAIDs) are the most used drugs in knee OA (osteoarthritis) treatment. Despite their efficiency in pain and inflammation alleviation, NSAIDs accumulate in the environment as chemical pollutants and have numerous genetic, morphologic, and functional negative effects on plants and animals. Ultrasound (US) therapy can improve pain, inflammation, and function in knee OA, without impact on environment, and with supplementary metabolic beneficial effects on cartilage compared to NSAIDs. These features recommend US therapy as alternative for NSAIDs use in knee OA treatment. 
  • 628
  • 01 Jun 2021
Topic Review
Target antigens for Approved ADCs
Biologically-based therapies increasingly rely on the endocytic cycle of internalization and exocytosis of target receptors for cancer therapies. However, receptor trafficking pathways (endosomal sorting (recycling, lysosome localization) and lateral membrane movement) are often dysfunctional in cancer. Antibody-drug conjugates (ADCs) have revitalized the concept of targeted chemotherapy by coupling inhibitory antibodies to cytotoxic payloads. Significant advances in ADC technology and format, and target biology have hastened the FDA approval of nine ADCs (four since 2019). Although the links between aberrant endocytic machinery and cancer are emerging, the impact of dysregulated internalization processes of ADC targets and response rates or resistance have not been well studied. This is despite the reliance on ADC uptake and trafficking to lysosomes for linker cleavage and payload release. 
  • 628
  • 21 Jul 2021
Topic Review
Bowman-Birk Inhibitors
Bowman-Birk inhibitors (BBIs) are found primarily in seeds of legumes and in cereal grains. These canonical inhibitors share a highly conserved nine-amino acids binding loop motif CTP1SXPPXC (where P1 is the inhibitory active site, while X stands for various amino acids). They are natural controllers of plants’ endogenous proteases, but they are also inhibitors of exogenous proteases present in microbials and insects. They are considered as plants’ protective agents, as their elevated levels are observed during injury, presence of pathogens, or abiotic stress, i.a. Similar properties are observed for peptides isolated from amphibians’ skin containing 11-amino acids disulfide-bridged loop CWTP1SXPPXPC. They are classified as Bowman-Birk like trypsin inhibitors (BBLTIs). These inhibitors are resistant to proteolysis and not toxic, and they are reported to be beneficial in the treatment of various pathological states.
  • 627
  • 22 Dec 2020
Topic Review
UPLC Technique in Pharmacy
In recent years, ultra-efficient liquid chromatography (UPLC) has gained particular popularity due to the possibility of faster separation of small molecules. This technique, used to separate the ingredients present in multi-component mixtures, has found application in many fields, such as chemistry, pharmacy, food, and biochemistry. It is an important tool in both research and production. UPLC created new possibilities for analytical separation without reducing the quality of the obtained results. This technique is therefore a milestone in liquid chromatography. Thanks to the increased resolution, new analytical procedures, in many cases, based on existing methods, are being developed, eliminating the need for re-analysis. Researchers are trying to modify and transfer the analytical conditions from the commonly used HPLC method to UPLC. This topic may be of strategic importance in the analysis of medicinal substances.
  • 626
  • 07 Dec 2022
Topic Review Video
Allosteric Antagonism of the Pregnane X Receptor
The pregnane X receptor (PXR, NR1I2) is a xenobiotic-activated transcription factor with high levels of expression in the liver. It not only plays a key role in drug metabolism and elimination, but also promotes tumor growth, drug resistance, and metabolic diseases. It has been proposed as a therapeutic target for type II diabetes, metabolic syndrome, and inflammatory bowel disease, and PXR antagonists have recently been considered as a therapy for colon cancer. The identified allosteric sites of the PXR provide new insights into the development of safe and efficient allosteric modulators of the PXR receptor. Researchers therefore propose that novel PXR allosteric sites might be promising targets for treating chronic metabolic diseases and some cancers. 
  • 626
  • 13 Oct 2022
Topic Review
Development of Peptide Biopharmaceuticals
Peptides are low-molecular-weight substances that participate in numerous important physiological functions, such as human growth and development, stress, regulation of the emotional state, sexual behavior, and immune responses. Their mechanisms of action are based on receptor–ligand interactions, which result in highly selective effects. These properties and low toxicity enable them to be considered potent drugs. Peptide preparations became possible at the beginning of the 20th century after a method was developed for selectively synthesizing peptides; however, after synthesis of the first peptide drugs, several issues related to increasing the stability, bioavailability, half-life, and ability to move across cell membranes remain unresolved. 
  • 625
  • 07 Apr 2022
Topic Review
New Therapeutical Approaches for COVID-19
The pandemic of coronavirus disease (COVID-19) stimulated an unprecedented international collaborative effort for rapid diagnosis, epidemiologic surveillance, clinical management, prevention, and treatment. Since the beginning of the COVID-19 pandemic, treatment of the SARS-CoV-2 infection was a real challenge. An overview of the viral structure and life cycle of SARS-CoV-2 is given and future therapeutical options are discussed.
  • 624
  • 08 Jun 2022
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
  • 624
  • 11 Oct 2022
Topic Review
Treatment Options of Helicobacter pylori
Helicobacter pylori is among the most common infections worldwide, and it can lead to burdensome sequela for the patient and the healthcare system, without appropriate treatment. Due to constantly fluctuating resistance rates, regimens must be constantly assessed to ensure effectiveness. 
  • 624
  • 21 Dec 2022
Topic Review
Pharmacological Activities of E. ferox
Euryale ferox Salisb. (prickly water lily) is the only extent of the genus Euryale that has been widely distributed in China, India, Korea, and Japan. The seeds of E. ferox (EFS) have been categorized as superior food for 2000 years in China, based on their abundant nutrients including polysaccharides, polyphenols, sesquineolignans, tocopherols, cyclic dipeptides, glucosylsterols, cerebrosides, and triterpenoids. These constituents exert multiple pharmacological effects, such as antioxidant, hypoglycemic, cardioprotective, antibacterial, anticancer, antidepression, and hepatoprotective properties. 
  • 624
  • 01 Jun 2023
Topic Review
Lopinavir/Ritonavir
Lopinavir-ritonavir (LPV/RTV) is a human immunodeficiency virus (HIV) antiviral combination that has been considered for the treatment of COVID-19 disease.
  • 623
  • 07 Dec 2020
Topic Review
NO in Viral Infections
Nitric oxide is a ubiquitous signaling radical that influences critical body functions. Its importance in the cardiovascular system and the innate immune response to bacterial and viral infections has been extensively investigated. The overproduction of NO is an early component of viral infections, including those affecting the respiratory tract. The production of high levels of NO is due to the overexpression of NO biosynthesis by inducible NO synthase (iNOS), which is involved in viral clearance. The development of NO-based antiviral therapies, particularly gaseous NO inhalation and NO-donors, has proven to be an excellent antiviral therapeutic strategy. 
  • 623
  • 20 Apr 2022
Topic Review
Inhibiting Angiogenesis by Anti-Cancer Saponins
Saponins are one of the broadest classes of high-molecular-weight natural compounds, consisting mainly of a non-polar moiety with 27 to 30 carbons and a polar moiety containing sugars attached to the sapogenin structure. Saponins are found in more than 100 plant families as well as found in marine organisms. Saponins have several therapeutic effects, including their administration in the treatment of various cancers. These compounds also reveal noteworthy anti-angiogenesis effects as one of the critical strategies for inhibiting cancer growth and metastasis.
  • 623
  • 24 Mar 2023
Topic Review
Postpartum Depression and Brexanolone
Brexanolone is being hailed as a ‘breakthrough’ medication for the treatment of PPD. As highlighted in this review, the positive outcomes with regard to the clinical use of the drug obtained from the three RCTs gave extensive evidence in favor of the safety, tolerability, and efficacy of brexanolone. Consequently, it prompted the FDA to give brexanolone a ‘priority review’ and ‘breakthrough therapy’ classification, which ultimately led to its approval.
  • 621
  • 22 Jul 2021
Topic Review
Fabrication Methods for Composite Films/Coatings
Chitin is made by joining N-acetyl glucosamine residues through β (1–4) glycosidic linkages and is the second-most prevalent natural polysaccharide after cellulose. Chitosan and its derivatives exhibit anti-hypoxic, adaptogenic, immunostimulant, antiviral, antibacterial, radioprotective, and hemostatic properties. In addition, they are nontoxic, biocompatible, and biodegradable.
  • 619
  • 02 Aug 2023
Topic Review
Selective Cytotoxicity of Ethiopian Plants
Few studies have reported the in vitro anticancer activities of medicinal plants that are collected from different agro‐ecological zones of Ethiopia. Hence, the main aim of this study was to screen the cytotoxic activities of 80% methanol extracts of 22 plants against human peripheral blood mononuclear cells (PBMCs), as well as human breast (MCF‐7), lung (A427), bladder (RT‐4), and cervical (SiSo) cancer cell lines. Active extracts were further screened against human large cell lung carcinoma (LCLC‐103H), pancreatic cancer (DAN‐G), ovarian cancer (A2780), and squamous cell carcinoma of the esophagus (KYSE‐70) by using the crystal violet cell proliferation assay, while the vitality of the acute myeloid leukemia (HL‐60) and histiocytic lymphoma (U‐937) cell lines was monitored in the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl‐2H‐tetrazolium bromide (MTT) microtiter assay. Euphorbia schimperiana, Acokanthera schimperi, Kniphofia foliosa, and Kalanchoe petitiana exhibited potent antiproliferative activity against A427, RT‐4, MCF‐7, and SiSo cell lines, with IC50 values ranging from 1.85 ± 0.44 to 17.8 ± 2.31μg/mL. Hence, further studies focusing on bio‐assay‐guided isolation and structural elucidation of active cytotoxic compounds from these plants are warranted.
  • 618
  • 25 Jun 2021
Topic Review
Lipophilic Polyamines
Gene therapy requires an effective and safe delivery vehicle for nucleic acids. Non-viral vehicles, including cationic liposomes, are intensively developed now. The structure of compounds composing them determines the delivery efficiency a lot. This review focuses on polycationic amphiphiles as prospective compounds for liposomal formulations and includes a discussion of the mutual influence of structural components. 
  • 618
  • 11 Aug 2021
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