Carbon-based quantum dots (CBQDs), sulfur-doped carbon-based quantum dots (S-CBQDs), and nitrogen-doped carbon-based quantum dots (N-CBQDs) have strong potential for drug delivery platforms. They ...were conjugated with andrographolide, a well-known hydrophobic drug, to study the concomitant changes in hydrophilicity. The interactions between these nanomaterials and the drug were studied by characterizing the optical and structural properties of the nanoparticles before and after coupling with the drug. It was found that the interaction of the drug with these nanomaterials produced noticeable changes in their optical and structural properties. Moreover, the partition coefficient for the nanocomposites was determined by NMR. The results indicate that conjugating the drug with the nanoparticles significantly enhanced its affinity for the aqueous phase, from 2.632 to 0.1117, thereby opening the possibility of using this approach for developing an effective drug delivery platform for this hydrophobic drug.
The Caribbean region is a hotspot of biodiversity (i.e., algae, sponges, corals, mollusks, microorganisms, cyanobacteria, and dinoflagellates) that produces secondary metabolites such as polyketides ...and polypropionates. Polyketides are a diverse class of natural products synthesized by organisms through a biosynthetic pathway catalyzed by polyketide synthase (PKS). This group of compounds is subdivided into fatty acids, aromatics, and polypropionates such as macrolides, and linear and cyclic polyethers. Researchers have studied the Caribbean region to find natural products and focused on isolation, purification, structural characterization, synthesis, and conducting biological assays against parasites, cancer, fungi, and bacteria. These studies have been summarized in this review, including research from 1981 to 2020. This review includes about 90 compounds isolated in the Caribbean that meet the structural properties of polyketides. Out of 90 compounds presented, 73 have the absolute stereochemical configuration, and 82 have shown biological activity. We expect to motivate the researchers to continue exploring the Caribbean region's marine environments to discover and investigate new polyketide and polypropionate natural products.
Classical antibacterial drugs were designed to target specific bacterial properties distinct from host human cells to maximize potency and selectivity. These designs were quite effective as they ...could be easily derivatized to bear next-generation drugs. However, the rapid mutation of bacteria and their associated acquired drug resistance have led to the rise of highly pathogenic superbug bacterial strains for which treatment with first line drugs is no match. More than ever, there is a dire need for antibacterial drug design that goes beyond conventional standards. Taking inspiration by the body’s innate immune response to employ its own supply of labile copper ions in a toxic attack against pathogenic bacteria, which have a very low Cu tolerance, this review article examines the feasibility of Cu-centric strategies for antibacterial preventative and therapeutic applications. Promising results are shown for the use of Cu-containing materials in the hospital setting to minimize patient bacterial infections. Studies directed at disrupting bacterial Cu regulatory pathways elucidate new drug targets that can enable toxic increase of Cu levels and perturb bacterial dependence on iron. Likewise, Cu intracellular chelation/prochelation strategies effectively induce bacterial Cu toxicity. Cu-based small molecules and nanoparticles demonstrate the importance of the Cu ions in their mechanism and display potential synergism with classical drugs.
Abstract Cancer continues to be a global health challenge, with millions suffering from its various forms. Prostate cancer, in particular, emerges as a significant health risk for men. Originating in ...the prostate gland—a small organ nestled in the male pelvis—this type of cancer the second most common cause of cancer-related deaths among men in the U.S. Despite numerous medical breakthroughs over the years, finding an effective treatment for prostate cancer remains a challenge. Our research is venturing into a new frontier in the fight against prostate cancer, focusing on an innovative method, it explores the potential of nanoparticles for targeted drug delivery. This targeted approach promises to not only intensify the therapeutic effect, but also minimize adverse side effects on healthy cells, ensuring a more balanced and effective treatment regimen. A key in this study is the drug Andrographolide (ADG), which has been previously recognized for its robust anti-cancer properties. However, one of its limitations is its hydrophobicity, which makes it challenging to administer due to solubility concerns. To navigate this challenge, we are pioneering the synthesis of AuAg (gold and silver) graphene quantum dots (GQDs) alloy nanoparticles. AuAg particles, in have been the subject of numerous studies due to their profound impact on cellular processes. By integrating a protective layer of GQDs, we aim to boost the nanoparticles' stability, all while preventing any potential release of harmful metallic ions. The primary objective of this advanced approach is to augment the solubility of andrographolide, paving the way for its targeted and efficient delivery to PC-3 cells. An integral part of our research involves determining the IC50 value, which is pivotal in indicating the concentration at which the drug can inhibit the growth of 50% of prostate cancer cells. Once the IC50 value for the AuAgGQDs is firmly established, our focus will shift to evaluating its effects on the morphology of Red Blood Cells (RBCs). By encapsulating andrographolide within the designed nanoparticles, such as AuAgGQDs and their derivatives, we aim to observe changes in morphology. If there is a change in morphology, it indicates successful drug encapsulation. Through this research, we are not just seeking a viable treatment method, but also aiming to expand the horizons of drug delivery systems. The insights gained from this study could very well revolutionize our understanding of therapeutic potential and underscore the importance of nanoparticles in the realm of biomedical applications. Citation Format: Alondra Del Mar Veloz Bonilla, Brad Weiner, Gerardo Morell, Nataniel Medina-Berríos. Graphene quantum dots-covered AuAg alloy nanoparticles as drug delivery platforms for anticancer applications abstract. In: Proceedings of the American Association for Cancer Research Annual Meeting 2024; Part 1 (Regular Abstracts); 2024 Apr 5-10; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2024;84(6_Suppl):Abstract nr 5757.
Abstract Prostate cancer, along with various other types of cancer, has been a prominent focus in medical and clinical discussions for many years due to its high fatality rates and significant health ...risks. To enhance oncological healthcare, various methods and technologies, such as drug delivery systems (DDS), have been extensively studied. Developing an effective DDS offers distinct advantages compared to other approaches to anticancer drug treatment. Some anticancer drug molecules possess unfavorable properties that directly impact metabolism and solubility, issues that DDS aims to address. Recent progress in nanomaterial synthesis has introduced innovative and efficient drug systems, providing a new perspective on cancer treatments. Gold nanoparticles, particularly in conjunction with semiconductor graphene quantum dots (GQDs), play a role in creating a unified carrier system applicable to multiple therapeutic methods. The choice of graphene quantum dots is based on their widespread applications and diverse benefits, ranging from compatible size and core-shell chemistry richness to substantial progress in achieving signal homogeneity by reducing the distance between molecules and substrate. The selected model for the DDS is the hydrophobic alkaloid Tetrandrine. Despite its use in treating conditions such as hypertension, and arthritis, and exhibiting anti-cancer activities, Tetrandrine is highly insoluble as an anti-cancer drug, with a solubility of 24.1 μmol/L 15 μg/mL in water and only 5mM in ethanol and DMSO. This research aims to enhance the solubility of hydrophobic Tetrandrine by incorporating it into gold graphene quantum dot nanocomposites, serving as a potential drug delivery system for combating prostate cancer. The synthesis of nanocomposites (Au-GQD, Au-NGQD, Au-SGQD) and Tetrandrine-loaded products (AuGQD-T, AuNGQD-T, AuSGQD-T) will be examined. Additionally, the properties of Tetrandrine loaded onto the nanoparticles will be scrutinized and characterized using NMR spectroscopy, UV-Vis, and fluorescence spectrum analyses. Citation Format: MiaSara Perez Salvá, Nataniel Medina-Berrios, Brad Weiner, Gerardo Morell Marrero. Design of Au-graphene quantum dot nanocomposite as a potential drug delivery system to solubilize Tetrandrine abstract. In: Proceedings of the American Association for Cancer Research Annual Meeting 2024; Part 1 (Regular Abstracts); 2024 Apr 5-10; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2024;84(6_Suppl):Abstract nr 5759.
