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Biography
Gottfried Heinisch
On 19 September 2019, the Pharmaceutical Science community in Austria lost a distinguished luminary, O. Univ.-Prof.i.R. Dr. Dr.h.c. Mag. pharm. Gottfried Heinisch, at the age of eighty after a long, severe illness. Born in 1938 to a Lower-Austrian Pharmacist’s family, Gottfried Heinisch studied pharmaceutical sciences at the University of Vienna, initially with the perspective of becoming a P
  • 674
  • 13 Sep 2022
Topic Review
Orally Fast Disintegrating Tablets for Infants and Children
A significant number of current drug formulations are not suitable for children of different age groups because of heterogeneity of the pediatric population, immature Absorption, Distribution, Metabolism and Elimination (ADME) processes, rapid developmental changes, palatability issues, low drug adherence and ethical concerns. Improvements in flexibility of dose administration, tablet size, taste masking, bioavailability, excipient safety and acceptability, stability, manufacturing and affordability represent multiple opportunities at various scales of child-friendly formulations design to overcome clinical and technological challenges in pediatric drug development. Orally Dispersible Tablets (ODTs) are a promising child-friendly drug delivery strategy, offering a potential solution to address unique medical needs in infants and children while maintaining a favorable excipient safety and acceptability profile in these vulnerable patient populations.
  • 671
  • 05 May 2023
Topic Review
Polydynamic Biological Activity of Quercetin
Quercetin is one of those natural products. It belongs to the family of flavonoids and, more specifically, flavonols. Quercetin is an organic compound that belongs to the family of flavonoids, with a wide range of medical properties. Some of these include anti-allergy, anti-inflammatory, anticancer, anti-tumor, and antiviral properties as well as cardiovascular protection. It has also been found that quercetin plays a vital role in plants. Specifically, quercetin has antioxidant and antimicrobial activities, and as a result, it contributes to photosynthesis, growth, and seed germination. Moreover, the presence of quercetin in various regions of the brain contributes to combatting against various neurological diseases such as Alzheimer’s and Parkinson’s.
  • 666
  • 20 Dec 2023
Topic Review
The Challenging Treatment of Cisplatin-Resistant Tumors
Cancer is one of the most lethal diseases, causing millions of deaths worldwide. In particular, carcinogenesis, the process responsible for healthy cells’ transformation into tumoral cells, is characterized by multi-stage evolution: initiation, promotion, and the malignant transformation of cells and progression. During this process, some DNA mutations occur, providing the cancer with different distinctive features, such as uncontrolled cell proliferation, replicative cell immortality, the circumvention of growth suppressors, the induction of angiogenesis, resistance to cell death, activation to invasion, and metastasis. The principal cancer treatments rely on surgical resection, radiotherapy, chemotherapy, immunotherapy, and targeted therapy, but usually combined therapy is the preferred choice. Indeed, after surgery, the patient often undergoes radio- or chemotherapy. 
  • 659
  • 21 Apr 2023
Topic Review
Small Schiff Base Molecules
Microorganisms participating in the development of biofilms exhibit heightened resistance to antibiotic treatment, therefore infections involving biofilms have become a problem in recent years as they are more difficult to treat. Consequently, research efforts are directed towards identifying novel molecules that not only possess antimicrobial properties but also demonstrate efficacy against biofilms. While numerous investigations have focused on antimicrobial capabilities of Schiff bases, their potential as antibiofilm agents remains largely unexplored.
  • 647
  • 01 Mar 2024
Topic Review
2-Substituted Benzimidazoles as Photo-Protective Agents
The modern trend in sunscreen products is towards the development of UV filters with multi-functional properties, to provide a broad shielding against ultraviolet radiation, antioxidant activity, and the prevention of skin cancer. Additionally, they should also be safe for humans as well as the environment. The benzimidazole heterocycle is a suitable platform for the development of such multifunctional molecules with potential application in cosmetic formulations, due to their ability to act as both UV protectors and reactive pharmacophores. 
  • 645
  • 16 Dec 2023
Topic Review
Functionalized Peptides in Nanomedicine for Effective Cancer Therapy
Peptide-functionalized nanomedicine, which addresses the challenges of specificity and efficacy in drug delivery, is emerging as a pivotal approach for cancer therapy. Globally, cancer remains a leading cause of mortality, and conventional treatments, such as chemotherapy, often lack precision and cause adverse effects. The integration of peptides into nanomedicine offers a promising solution for enhancing the targeting and delivery of therapeutic agents.
  • 645
  • 23 Jan 2024
Topic Review
Anti-Cancer Effect of Gypsogenin and Gypsogenic Acid
Gypsogenin possesses a versatile and unique aldehyde group that can be utilized to create covalent interactions with undruggable targets. Gypsogenin carboxamides have demonstrated high cytotoxic activity against breast and lung cancer. The bisamides of gypsogenic acid possess prominent activity as well; however, their anti-leukemic activity is yet to be explored.
  • 630
  • 08 Aug 2023
Topic Review
Pharmacological Activities of Diterpenoid Alkaloids
Diterpenoid alkaloids (DAs) are characteristic components of some genera of the Ranunculaceae family, the occurrence of which is extraordinarily high in the genera Aconitum, Delphinium, and Consolida. To affect the central nervous system, primarily, the drug should pass the blood–brain barrier (BBB). Transmembrane diffusion is the most common route of drugs to pass the BBB and, in contrast to the transport system, shows a non-saturable kinetic. Physiochemical features of the drug mainly determine the amounts of this passage. Molecular weight (400–600 Da is optimum), lipid solubility, molecular charge, and tertiary structure are the most important factors necessary for transmembrane diffusion through BBB. The diterpenic backbone of DAs provides their suitable lipid solubility, but the presence of tertiary nitrogen makes them different from normal diterpenoids. The tertiary nitrogen with the highest proton affinity in the molecule (in water) rearranges the electronic structure of DA by its protonation. Moreover, computational modeling showed that the function of nitrogen besides ester sidechains causes DAs to interact with the active sites as well as their toxicity.
  • 627
  • 22 May 2023
Topic Review
Optical Imaging for Nature of Cytosolic Iron Pools
The chemical nature of intracellular labile iron pools (LIPs) is described. By virtue of the kinetic lability of these pools, it is suggested that the isolation of such species by chromatography methods will not be possible, but rather mass spectrometric techniques should be adopted. Iron-sensitive fluorescent probes, which have been developed for the detection and quantification of LIP, are described, including those specifically designed to monitor cytosolic, mitochondrial, and lysosomal LIPs. The potential of near-infrared (NIR) probes for in vivo monitoring of LIP is discussed.
  • 623
  • 19 Sep 2023
Topic Review
Biological Activity of the 3-Heteroaryl Fluoroquinolone Hybrids
There are promising studies in the area of 3-heteroaryl hybrids. The latter can be synthesized via different convinient methods with the formation of new derivatives with five-membered and fused heterocycles or creation of bis-fluoroquinolones with variable linking moieties. These novel compounds revealed not only good antimicrobial properties compared to the parent molecules but were also widely investigated as anticancer agents with promising activity.
  • 610
  • 19 Jun 2023
Topic Review
5-Arylidenerhodanines as P-gp Modulators
Multidrug resistance (MDR) is considered one of the major mechanisms responsible for the failure of numerous anticancer and antiviral chemotherapies. Various strategies to overcome the MDR phenomenon have been developed, and one of the most attractive research directions is focused on the inhibition of MDR transporters, membrane proteins that extrude cytotoxic drugs from living cells. 
  • 596
  • 14 Apr 2023
Topic Review
Electrospun Fibers for Skin Burn Treatment
Burns are a major threat to public health and the economy due to their costly and laborious treatment and high susceptibility to infection. Efforts have been made recently to investigate natural bioactive compounds with potential use in wound healing.
  • 588
  • 30 Jun 2023
Topic Review
Polypeptides for Anticancer Drug Delivery
Even though polypeptide drug delivery systems have already achieved good results in preclinical studies, there is still a significant lack of clinical trials using these systems. Obviously, there is a large gap between preclinical studies and their translation to the clinic. The lack of consistency in reporting preclinical studies using drug delivery systems has prevented a systematic assessment of these studies. For the effective application of nanotechnology in the clinical environment, researchers should be able to compare new data with previously published results in a reliable and meaningful way. This requires a standard of specific information that needs to be reported, including material characterization, biological characterization, and so on, so that quantitative comparisons, meta-analyses and in silico modeling can be conducted and facilitated.
  • 584
  • 12 May 2022
Topic Review
Functionalized Calixarenes as Promising Antibacterial Drugs
Since the discovery of polyphenolic resins 150 years ago, the study of polymeric compounds named calix[n]arene has continued to progress, and those skilled in the art perfectly know now how to modulate this phenolic ring. Consequently, calix[n]arenes are now used in a large range of applications and notably in therapeutic fields. In particular, the calix[4]arene exhibits multiple possibilities for regioselective polyfunctionalization on both of its rims and offers researchers the possibility of precisely tuning the geometry of their structures. Thus, in the crucial research of new antibacterial active ingredients, the design of calixarenes finds its place perfectly. Out of all the work of the community, there are some excellent activities emerging that could potentially place these original structures in a very good position for the development of new active ingredients.
  • 576
  • 29 Dec 2023
Topic Review
Polyphenols against Adverse Effects of Antitumor Therapies
Polyphenolic compounds, encompassing flavonoids (e.g., quercetin, rutin, and cyanidin) and non-flavonoids (e.g., gallic acid, resveratrol, and curcumin), show several health-related beneficial effects, which include antioxidant, anti-inflammatory, hepatoprotective, antiviral, and anticarcinogenic properties, as well as the prevention of coronary heart diseases. Polyphenols have also been investigated for their counteraction against the adverse effects of common anticancer chemotherapeutics.
  • 565
  • 04 Feb 2024
Topic Review Peer Reviewed
Polyhydroxyalkanoates (PHAs): Mechanistic Insights and Contributions to Sustainable Practices
A polymer is a long-chain molecule formed by linking numerous simpler repeating chemical units, known as monomers, with identical structures. Over the past two centuries, there has been a significant increase in the global production and use of petrochemical-based plastics. This surge has led to widespread ecological imbalances, affecting air quality, terrestrial and marine ecosystems, food chains, and plant life. Consequently, the excessive use of such polymers has created challenges in solid waste management, with methods like bio- or photo-degradation, incineration, landfilling, and recycling proving to be time-consuming and laborious. Therefore, there is a growing urgency for biodegradable polymers due to increasing demand. Biodegradable polymers consist of interconnected monomers with unstable links in the backbone, facilitated by various functional groups. Throughout the degradation process of these polymers, numerous biologically acceptable molecules are produced. This study examines the significance of biopolymers over petroleum-based counterparts, offering a detailed analysis. It is noteworthy that within the spectrum of biodegradable polymers, polyhydroxyalkanoates (PHAs) emerge as exceptionally promising candidates for substituting petroleum-derived polymers, owing to their remarkable physical attributes. Therefore, this study provides a systematic overview of PHAs, including their classification, historical background, methods of production, potential challenges to commercialization, and diverse applications.
  • 538
  • 06 Jan 2025
Topic Review
Five-Membered Heterocycles in Human Histone Deacetylase Inhibitors
Five-membered heteroaromatic rings, in particular, have gained prominence in medicinal chemistry as they offer enhanced metabolic stability, solubility and bioavailability, crucial factors in developing effective drugs. The unique physicochemical properties and biological effects of five-membered heterocycles have positioned them as key structural motifs in numerous clinically effective drugs. 
  • 533
  • 08 Sep 2023
Topic Review
The Mammalian Thioredoxin Reductase Probes
The cardinal component of the thioredoxin system, mammalian thioredoxin reductase (TrxR) plays a vital role in supporting various physiological functions; however, its malfunction, disrupting redox balance, is intimately associated with the pathogenesis of multiple diseases. Fluorescent probes offer several advantages for in situ imaging and the quantification of biological targets, such as non-destructiveness, real-time analysis, and high spatiotemporal resolution. These benefits facilitate the transition from a poise to a flux understanding of cellular targets, further advancing scientific studies in related fields. The TrxR fluorescent probes have contributed significantly to the investigation of TrxR’s biological functions and have been valuable tools in TrxR-related research.
  • 513
  • 24 Aug 2023
Topic Review
Radiolabeled Peptoids and Peptoid/Peptide Hybrids for Cancer-Targeted Imaging
Peptoids (N-substituted glycine oligomers) are a relatively new class of peptidomimetics, being highly versatile and capable of mimicking the architectures and the activities of the peptides but with a marked resistance to proteases and a propensity to cross the cellular membranes over the peptides themselves. For these properties, they have gained an ever greater interest in applications in bioengineering and biomedical fields.
  • 504
  • 30 Nov 2023
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