The crystal structure of fac-tricarbonyl(2-pyridin-2-yl-quinoline-κ2 N,N′)-(pyrazole-κN)rhenium(I)nitrate, C20H14N4O3ReNO3

Please read the abstract in the article.National Research Foundation of South Africa, Tshwane University of Technology, and the University of Pretoria.https://www.degruyter.com/view/j/ncrsChemistr

The crystal structure of fac-tricarbonyl((pyridin2-yl)methanamino-κ2 N,N′)-((pyridin-2-yl) methanamino-κN)rhenium(I) nitrate, C15H16O3N4Re

Please read abstract in the article.NRFhttps://www.degruyter.com/view/j/ncrsChemistr

The crystal structure of (bromido, chlorido)-tricarbonyl-(5,5′-dimethyl-2,2′-bipyridine)-rhenium(I), C15H12Br0.2Cl0.8N2O3Re1

Please read abstract in the article.National Research Foundation of South Africa, Tshwane University of Technology, University of Pretoria, University of the Free State.https://www.degruyter.com/view/j/ncrsChemistr

The crystal structure of fac-tricarbonyl(N-benzoylN,N-cyclohexylmethylcarbamimidothioato-k(2)S,O)(pyridine-kN)rhenium(I), C23H24N3O4ReS

Please read abstract in the article.The National Research Foundation of South Africa, Tshwane University of Technology and the University of Pretoria.https://www.degruyter.com/view/j/ncrsChemistr

Nanocarriers for methotrexate delivery/codelivery in the frame of cancer diagnostics and treatment: a review

Cancer is one of the most life-threatening family of diseases that cause death worldwide. As a highly researched and successful therapeutic agent, methotrexate (MTX) treats many solid tumours, hematologic malignancies, and autoimmune illnesses. Despite many benefits, methotrexate induces drug resistance and limits plasma half-life due to its poor pharmacokinetics. The variable biological availability have prompted researchers to investigate innovative delivery strategies for enhancing its therapeutic qualities. To develop more suitable methotrexate formulations, nanoparticles (NPs) have recently gained a significant interest. A wide range of nanoparticles, including polymer-based nanoparticles, carbon-based nanoparticles, lipid-based nanoparticles, as well as inorganic nanoparticles, can be deliver cancer chemotherapeutics such as methotrexate. Loading methotrexate into NPs can provide a delivery system that has shown great promise to carcinoma therapy. In this review, we will describe the feasibility of NP-based strategies to deliver methotrexate in cancer therapy, outlining the current state of the art and the challenges/promises for the future

Nanoparticles Functionalised with Re(I) Tricarbonyl Complexes for Cancer Theranostics

Globally, cancer is the second (to cardiovascular diseases) leading cause of death. Regardless of various efforts (i.e., finance, research, and workforce) to advance novel cancer theranostics (diagnosis and therapy), there have been few successful attempts towards ongoing clinical treatment options as a result of the complications posed by cancerous tumors. In recent years, the application of magnetic nanomedicine as theranostic devices has garnered enormous attention in cancer treatment research. Magnetic nanoparticles (MNPs) are capable of tuning the magnetic field in their environment, which positively impacts theranostic applications in nanomedicine significantly. MNPs are utilized as contrasting agents for cancer diagnosis, molecular imaging, hyperfusion region visualization, and T cell-based radiotherapy because of their interesting features of small size, high reactive surface area, target ability to cells, and functionalization capability. Radiolabelling of NPs is a powerful diagnostic approach in nuclear medicine imaging and therapy. The use of luminescent radioactive rhenium(I), 188/186Re, tricarbonyl complexes functionalised with magnetite Fe3O4 NPs in nanomedicine has improved the diagnosis and therapy of cancer tumors. This is because the combination of Re(I) with MNPs can improve low distribution and cell penetration into deeper tissues

Steric and electronic influence of Re(I) tricarbonyl complexes with various coordinated β-diketones

Please read abstract in the article.The National Research Foundation and Tshwane University of Technology, University of the Free State, South Africa.http://www.elsevier.com/locate/molstr2023-05-18hj2023Chemistr

Nano-immunotherapeutic strategies for targeted RNA delivery: Emphasizing the role of monocyte/macrophages as nanovehicles to treat glioblastoma multiforme

Glioblastoma multiforme (GBM) is considered the most aggressive and heterogeneous type of brain malignancy. The substantial invasion of the central nervous system parenchyma is a typical hallmark of all grades of glioma. To improve tumor localization and prevent unanticipated toxicity, anti-tumor drug delivery mechanisms must be upgraded in parallel with pharmacotherapeutics. Monocytes can easily pass the blood-brain barrier, and thus, drugs with difficulty entering the brain can be loaded into monocytes, resulting in the treatment of brain cancers. RNA as a natural and biocompatible polymer has many advantages for biomedical applications, and RNA-based therapies can provide regulated biological functions by highly selective and controlling means. In this context, macrophages are excellent carriers for distributing RNA-based treatments. However, developing an efficient macrophage-targeted RNA delivery has remained challenging. Several approaches have been introduced in the last decade to efficiently deliver RNA-based therapy via macrophages to treat GBM and inflammatory conditions. This review summarizes the most suitable nano-carrier systems to deliver RNA into immunocytes; also, different methods of synthesizing RNA-loaded nanopArticles and their application, with an emphasis on targeting GBM, are discussed. Furthermore, it focuses specifically on the stability of such nanoformulations and the effect of targeting moieties and adjuvants in determining the worth of the aroused immune response. Finally, the critical aspects of delivering RNA-lipid hybrid nanopArticles (LNPs) via oral, systemic, and local routes are highlighted. We hope that these findings will pave the way for more effective treatment of solid tumors, such as GBM, in the future

Nano-scale drug delivery systems for carboplatin: A comprehensive review

Carboplatin (CRBP) is a chemotherapeutic agent based on platinum that has applications in the effective management of ovarian, testis, cervical, neck, head, and small cell lung cancer. CRBP prevents duplication and transcription by binding to the DNA of tumor cells to inhibit the growth and division of cancer cells. CRBP has some limitations such as destroying normal cells alongside cancer cells and being poor at uptake by the cells, leading to the need for high doses, which has prompted significant attention to develop a targeted and localized delivery system that is effective for this anticancer drug. It is common to use CRBP in drug combination therapy. However, there are some disadvantages that could be overcome with nanoparticulate systems. Nano-engineered delivery systems can be an efficient approach to enhancing the cellular uptake and accumulation of CRBP, leading to improving the therapeutic potential with negligible toxicity. CRBP has been encapsulated into various nano-delivery systems, including polymer-based nanocarriers and micelles, protein nanoparticles, lipid-based nanoparticles (liposomes and solid lipid nanoparticles), silica-based nanostructures, carbon nanoparticles and etc. Moreover, there is growing interest in stimuli-responsive delivery systems for cancer-targeted delivery using modes such as induced temperature changes, electric/magnetic fields, pH, ultrasound waves, light, and laser. Cancer targeting by drug delivery systems, owing to their selective targeting, efficacy, biocompatibility and high drug payload, provides an attractive alternative treatment; however, there are technical, therapeutic, manufacturing and clinical barriers that limit their use. In this regard, the need for robust analytical methods to determine biodistribution, PK and PD profile of liposomes was highlighted in addition to a critical gap between efficient preclinical to clinical efficacy predictive modeling. Systems with the ability of co-delivery also could be useful to decrease drug toxicity on healthy tissues and improve the bioavailability of CRBP

In vitro cytotoxic effect of stigmasterol derivatives against breast cancer cells

Abstract Background Stigmasterol is an unsaturated phytosterol that belong to the class of tetracyclic steroids abundant in Rhoicissus tridentata. Stigmasterol is an important constituent since it has shown impressive pharmacological effects such as anti-osteoarthritis, anticancer, anti-diabetic, anti-inflammatory, antiparasitic, immunomodulatory, antifungal, antioxidant, antibacterial, and neuroprotective activities. Furthermore, due to the presence of π system and hydroxyl group, stigmasterol is readily derivatized through substitution and addition reactions, allowing for the synthesis of a wide variety of stigmasterol derivatives. Methods Stigmasterol (1) isolated from Rhoicissus tridentata was used as starting material to yield eight bio-active derivatives (2–9) through acetylation, epoxidation, epoxide ring opening, oxidation, and dihydroxylation reactions. The structures of all the compounds were established using spectroscopic techniques, NMR, IR, MS, and melting points. The synthesized stigmasterol derivatives were screened for cytotoxicity against the hormone receptor-positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12 A) cell lines using the resazurin assay. Results Eight stigmasterol derivatives were successfully synthesized namely; Stigmasterol acetate (2), Stigmasta-5,22-dien-3,7-dione (3), 5,6-Epoxystigmast-22-en-3β-ol (4), 5,6-Epoxystigmasta-3β,22,23-triol (5), Stigmastane-3β,5,6,22,23-pentol (6), Stigmasta-5-en-3,7-dion-22,23-diol (7), Stigmasta-3,7-dion-5,6,22,23-ol (8) and Stigmast-5-ene-3β,22,23-triol (9). This is the first report of Stigmasta-5-en-3,7-dion-22,23-diol (7) and Stigmasta-3,7-dion-5,6,22,23-ol (8). The synthesized stigmasterol analogues showed improved cytotoxic activity overall compared to the stigmasterol (1), which was not toxic to the three cell lines tested (EC50 ˃ 250 µM). In particular, 5,6-Epoxystigmast-22-en-3β-ol (4) and stigmast-5-ene-3β,22,23-triol (9) displayed improved cytotoxicity and selectivity against MCF-7 breast cancer cells (EC50 values of 21.92 and 22.94 µM, respectively), while stigmastane-3β,5,6,22,23-pentol (6) showed improved cytotoxic activity against the HCC70 cell line (EC50: 16.82 µM). Conclusion Natural products from Rhoicissus tridentata and their derivatives exhibit a wide range of pharmacological activities, including anticancer activity. The results obtained from this study indicate that molecular modification of stigmasterol functional groups can generate structural analogues with improved anticancer activity. Stigmasterol derivatives have potential as candidates for novel anticancer drugs