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Topic Review
Heteronuclear Metal Complexes with Anticancer Activity
Transition metal complexes have been deeply studied for different applications, such as catalysis, antimicrobial, and also antitumoral drugs. Platinum complexes are probably the most well-known and studied in the field of anticancer compounds, also thanks to the omnipresence of cisplatin and its derivatives as a starting point. Two promising new strategies to increase the efficacy of transition metal-based complexes have been described. First, the possibility of assembling two biologically active fragments containing different metal centres into the same molecule were considered, thus obtaining a heterobimetallic complex. Secondly, the conjugation of metal-based complexes to a targeting moiety was discussed.
  • 603
  • 09 Jan 2023
Topic Review
NPECs for Rheumatoid Arthritis Therapy
Natural plant extracts and compounds (NPECs), which originate from herbs or plants, have been used in the clinical treatment of rheumatoid arthritis (RA) for many years. 
  • 601
  • 25 Jun 2021
Topic Review
Non-Alkaloid Cholinesterase Inhibitory Compounds
The classes of cholinesterase inhibitors discussed here are mainly terpenoids, phenolic compounds, and coumarins, and some of these compounds have shown high potency. In order to consider which classes are most suitable, based on the benefits and drawbacks, certain structural features of each class will be of great importance. Using chalcones as an example, it is believed that besides economical and cost-effective production, small molecular size and flexibility for modifications to improve lipophilicity necessary for blood-brain barrier permeability are important to consider for a preferred potential therapeutic candidate for AD.
  • 598
  • 29 Sep 2021
Topic Review
Medicinal Potential of Isoflavonoids
In recent years, there is emerging evidence that isoflavonoids could play an important role in the management of type 2 diabetes mellitus (T2DM) due to their reported pronounced biological effects in relation to multiple metabolic factors associated with diabetes. Hence, in this regard, we have comprehensively reviewed the potential biological effects of isoflavonoids, particularly biochanin A, genistein, daidzein, glycitein, and formononetin on metabolic disorders and long-term complications induced by T2DM in order to understand whether they can be future candidates as a safe antidiabetic agent. Based on in-depth in vitro and in vivo studies evaluations, isoflavonoids have been found to activate gene expression through the stimulation of peroxisome proliferator-activated receptors (PPARs) (α, γ), modulate carbohydrate metabolism, regulate hyperglycemia, induce dyslipidemia, lessen insulin resistance, and modify adipocyte differentiation and tissue metabolism. Moreover, these natural compounds have also been found to attenuate oxidative stress through the oxidative signaling process and inflammatory mechanism. Hence, isoflavonoids have been envisioned to be able to prevent and slow down the progression of long-term diabetes complications including cardiovascular disease, nephropathy, neuropathy, and retinopathy. 
  • 595
  • 28 Sep 2021
Topic Review
Synthetic Imidazopyridine-Based Derivatives
Fused pyridines are reported to display various pharmacological activities, such as antipyretic, analgesic, antiprotozoal, antibacterial, antitumor, antifungal, anti-inflammatory, and antiapoptotic. They are widely used in the field of medicinal chemistry. Imidazopyridines (IZPs) are crucial classes of fused heterocycles that are expansively reported on in the literature. Evidence suggests that IZPs, as fused scaffolds, possess more diverse profiles than individual imidazole and pyridine moieties. Bacterial infections and antibacterial resistance are ever-growing risks in the 21st century. Only one IZP, i.e., rifaximin, is available on the market as an antibiotic
  • 595
  • 02 Feb 2023
Topic Review
Bisphosphonate-Based Conjugates and Derivatives
Metastatic bone cancer occurs in every type of cancer but is prevalent in lung, breast, and prostate cancers. These metastases can cause extensive morbidity, including a range of skeletal-related events, often painful and linked with substantial hospital resource usage. The treatment used is a combination of chemotherapy and surgery. However, anticancer drugs are still limited because of severe side effects, drug resistance, poor blood supply, and non-specific drug uptake, necessitating high toxic doses. Bisphosphonates are the dominant class of drugs used to inhibit metastatic bone cancer. It is also used to treat osteoporosis and other bone diseases. However, bisphosphonate also suffers from serious side effects. Thus, there is a serious need to develop bisphosphonate conjugates with promising therapeutic outcomes for treating metastatic bone cancer and osteoporosis. This review article focuses on the biological outcomes of designed bisphosphonate-based conjugates for the treatment of metastatic bone cancer and osteoporosis. 
  • 594
  • 09 Jul 2021
Topic Review
New Antimicrobial Oleanonic Acid Polyamine Conjugates
The series of 21 oleanolic acid derivatives containing di- and polyamine fragments at position C3 and C28 was synthesized and evaluated for their antimicrobial activities against both Gram-positive and Gram-negative bacterial. Almost all series presented good to moderate Minimum Inhibitory Concentrations (MIC) against Gram-positive S. aureus, S. faecalis and B. cereus bacteria, moreover compounds possess important antimicrobial activities against Gram-negative E. coli, P. aeruginosa, S. enterica, and EA289 bacteria with MICs ranging from 6.25 to 200 µg/mL. The SAR data showed that the nature of the polyamine fragment, as well as differences in the structure of oleanolic acid plays an important role in the potential activities of tested compounds. The testing of the ability to restore the antibiotic activity of doxycycline and erythromycin at a 2 µg/mL concentration in a synergistic assay showed that only Mannich base with spermine fragment 6 lead to a moderate improvement in terms of antimicrobial activities of the different selected combinations against both P. aeruginosa and E. coli. The study of the mechanism of action of the most important compound in this series (amide 2i derived from N-methyl-norspermidine) showed the effect of disruption of the outer bacterial membrane of P. aeruginosa PA01 cells. Computational ADMET profiling renders compound 2i as a suitable starting point for pharmacokinetic optimization.
  • 594
  • 19 Jan 2022
Topic Review
Volatilomics in Prostate Cancer
The lack of highly specific and sensitive biomarkers for the early detection of prostate cancer (PCa) is a major barrier to its management. Volatilomics emerged as a non-invasive, simple, inexpensive, and easy-to-use approach for cancer screening, characterization of disease progression, and follow-up of the treatment’s success.
  • 594
  • 24 Aug 2022
Topic Review
Vanadium and Melanoma
Melanoma is the most aggressive type of skin cancer, the incidence of which has been increasing annually worldwide.
  • 593
  • 08 Jun 2021
Topic Review
Taccalonolides
Taccalonolides are a new class of microtube-stabilizing agents isolated from plants of the genus Tacca demonstrating effectiveness against drug-resistant tumors in cellular and animal models.
  • 592
  • 16 Sep 2021
Topic Review
Pioglitazone-Loaded PLGA Nanoparticles
Albeit, the relationship between diabetes drugs and the progression of atherosclerosis is still elusive, Pioglitazone (PGZ; 5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]–1,3- thiazolidine-2,4-diona), one of the most frequently prescribed anti-diabetic medication in the United States, slows the progression of atherosclerosis.
  • 590
  • 14 Mar 2022
Topic Review
Microbubbles Based Drug Delivery Systems
The blood-brain barrier (BBB) is one of the most selective endothelial barriers that protect the brain and maintains homeostasis in neural microenvironments. This barrier restricts the passage of molecules into the brain, except for gaseous or extremely small hydrophobic molecules. Thus, the BBB hinders the delivery of drugs with large molecular weights for the treatment of brain cancers. Various methods have been used to deliver drugs to the brain by circumventing the BBB; however, they have limitations such as drug diversity and low delivery efficiency. To overcome this challenge, microbubbles (MBs)-based drug delivery systems have garnered a lot of interest in recent years. MBs are widely used as contrast agents and are recently being researched as a vehicle for delivering drugs, proteins, and gene complexes. The MBs are 1–10 μm in size and consist of a gas core and an organic shell, which cause physical changes, such as bubble expansion, contraction, vibration, and collapse, in response to ultrasound.
  • 590
  • 20 Apr 2023
Topic Review
Health-Promoting Effects of Bioactive Compounds from Endophytic Fungi
The study examines the intricate relationship between plants and the endophytic fungi inhabiting their tissues. These fungi harmoniously coexist with plants, forming a distinct symbiotic connection that has caught scientific attention due to its potential implications for plant health and growth. The diverse range of bioactive compounds produced by these fungi holds significant promise for human health.
  • 588
  • 09 Oct 2023
Topic Review
Peptidomimetics and Their Applications for Opioid Peptide Drug
Peptidomimetics are synthetically altered peptides with adjusted molecular properties for specific biological or therapeutic applications and have been an important class of drug molecules due to their potential features, high potency, and low toxicity since the term was created first in the late 1970s.
  • 585
  • 30 Nov 2022
Topic Review
Molecular Hybridization of Alkaloids Using 1,2,3-Triazole-Based Click Chemistry
Alkaloids found in multiple species, known as ‘driver species’, are more likely to be included in early-stage drug development due to their high biodiversity compared to rare alkaloids. Many synthetic approaches have been employed to hybridize the natural alkaloids in drug development. Click chemistry is a highly efficient and versatile reaction targeting specific areas, making it a valuable tool for creating complex natural products and diverse molecular structures. It has been used to create hybrid alkaloids that address their limitations and serve as potential drugs that mimic natural products.
  • 584
  • 22 Nov 2023
Topic Review
Influenza Antiviral Drugs
Influenza virus is a highly contagious zoonotic respiratory disease that causes seasonal outbreaks each year and unpredictable pandemics occasionally with high morbidity and mortality rates, posing a great threat to public health worldwide. Besides the limited effect of vaccines, the prob-lem is exacerbated by the lack of drugs with strong antiviral activity against all flu strains. Cur-rently, there are two classes of antiviral drugs available that are chemosynthetic and approved against influenza A virus for prophylactic and therapeutic treatment, but the appearance of drug-resistant virus strains is a serious issue that strikes at the core of influenza control. There is therefore an urgent need to develop new antiviral drugs. Many reports have shown that the de-velopment of novel bioactive plant extracts and microbial extracts has significant advantages in influenza treatment.
  • 583
  • 01 Mar 2021
Topic Review
Tumor Polyamine-Suppressing Strategy
Several tumor polyamine-suppressing strategies have been developed, as follows. (1) Ornithine decarboxylase (ODC) and S-adenosylmethionine decarboxylase 1 (AMD1) are important for polyamine synthesis. The α-difluoromethylornithine (DFMO), which acts as an irreversible suicide inhibitor of ODC, has been used to prevent and treat multiple cancers, such as pancreatic cancer, gastric cancer, lung carcinoma, neuroblastoma, endometrial cancer, and osteosarcoma. (2) Highly regulated catabolic pathways are utilized to control the intracellular polyamine pool. The modulation of the polyamine catabolic enzyme produces decreasing polyamine content and induces the generation of toxic compounds. (3) Some inhibitors targeting the polyamine transport system (PTS) can hinder polyamine import and antagonize polyamine uptake. (4) Synthetic polyamines, including polyamine analogs and polyamine conjugates, possess anticancer activity against tumor cells.
  • 581
  • 01 Sep 2022
Topic Review
Electrochemical Aptasensors for Detection of Neurodegenerative Diseases Biomarkers
Neurodegenerative diseases (NDs) are becoming a major global health problem. They constitute an incurable diverse group of disorders characterized by the progressive degeneration of the structure and function of the central or peripheral nervous system. There is an enormous unmet demand worldwide for methods for the early detection of ND biomarkers. Among the various approaches reported so far, biosensors are powerful analytical implements that have been applied to detect biomarkers of NDs. Electrochemical aptasensors have been at the forefront of this development not only thanks to their low cost and simple design but also due to advances in nanomaterials modifying the surface of the transducers involved.
  • 579
  • 13 Feb 2023
Topic Review
Nitrogen Heterocycles and NRF2 Activation
Several nitrogen heterocyclic analogues have been applied to clinical practice, and about 75% of drugs approved by the FDA contain at least a heterocyclic moiety. Thus, nitrogen heterocycles are beneficial scaffolds that occupy a central position in the development of new drugs. The fact that certain nitrogen heterocyclic compounds significantly activate the NRF2/ARE signaling pathway and upregulate the expression of NRF2-dependent genes, especially HO-1 and NQO1, underscores the need to study the roles and pharmacological effects of N-based heterocyclic moieties in NRF2 activation. Furthermore, nitrogen heterocycles exhibit significant antioxidant and anti-inflammatory activities. NRF2-activating molecules have been of tremendous research interest due to their therapeutic roles in neuroinflammation and oxidative stress-mediated diseases. 
  • 577
  • 28 Apr 2023
Topic Review
Endogenous Hydrogen Sulfide
Hydrogen sulfide (H2S) is an endogenously produced gaseous signaling molecule and is critical for the regulation of cardiovascular homeostasis.
  • 576
  • 14 Apr 2021
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