Newly sythnesized acridone derivatives targeting lung cancer: A toxicity & xenograft model study
This article talks about the acridone derivatives (AC‐2, AC‐7, and AC‐26) toxicity that can be used in NSCLC treatment via activation of the p‐AKT1 pathway. It did not cause any signs of acute and repeated dose oral toxicity study, for any of the organs in rats. A lung cancer xenograft model study showed that the compounds inhibit p‐AKT1 and reduce the tumor size by about 30‐40% at a dose of 100 mg/kg. The result is very encouraging and can be used for lung cancer treatment after regulatory clinical investigations.
A review of potential heterocycles for the treatment of glioblastoma targeting receptor tyrosine kinases
The paper focuses on the molecular pathways targeted by different heterocycles. The groups attached to the heterocycles, like aromatic or aliphatic and electron donating or electron-withdrawing, differ in the potency of the molecules w.r.t. target. The different kinases present in cells like RTKs, CDKs, LKs, etc. are the most targeted enzymes in cancer. Modify the expression of RTKs, their ligands and related proteins, focused on the MAPK, PI3K/AKT, JAK/STA and NF-κB downstream pathways. Subsequently, all the pathways, including RAS-RAF-MAPK, PI3K and AKT, are activated. The heterocycles that target receptor kinase pathways have been the main focus of this article.
Using nanotechnology to progress the utilization of marine natural products in combating multidrug resistance in cancer: A prospecting strategy
Here we highlighted pharmacological opportunities that offered significant context and insightful information about mainly the undiscovered anticancer leads based on marine flora. The development of intrinsic and acquired drug resistance, continues to be a significant obstacle on the way to effective cancer therapy. Nanomedicine loaded with small molecule chemotherapeutics is a fast-evolving approach which can assist in enhanced biodistribution and pharmacokinetics due to their nanometric size, surface characteristics that allow longer circulation time, passive targeting, and evasion of MDR efflux pumps. Here, we outlined how marine natural products may be used to treat MDR in cancer using cutting‐edge active drug targeting strategies based on nanomedicines.
Gut microbial metabolites of dietary polyphenols and their potential role in human health and diseases
In this paper, we focused on the effect of diet composition on human well-being. Inclusion of several polyphenol-rich fruits, vegetables, and cereals in the daily diet helps in the prevention as well as treatment of some chronic diseases. Pharmacological activities of parent polyphenols can be enhanced by formation of their gut microbial metabolites. Several sets of experiments are being carried out to investigate the potential of metabolites to exert pharmacological actions by themselves or if they act as prodrugs aid in understanding their mechanism of action. Dietary polyphenols from terrestrial sources subjected to colonic metabolism are studied widely. Here, in this paper we overviewed and covered all such studies. We proposed the need of such similar studies considering marine polyphenols.
Virtual Screening of a Marine Natural Product Database for In Silico Identification of a Potential Acetylcholinesterase Inhibitor
This study deals with virtual screening of marine natural products from CMNPD library for their therapeutic application in Alzheimer’s disease (AD) as acetylcholinesterase inhibitors (AChEI). Acetylcholinesterase hydrolyses acetylcholine and induces amyloid-beta aggregation. AChEI inhibits this aggregation by binding to AChE, making it a potential target for the treatment of AD. The docking studies, toxicity profiles, molecular dynamics studies and DFT calculations confirmed molecule 64 (CMNPD 8741, δ-Indomycinone) as a hit compound. Further studies are required to confirm the potential of the hit molecule in the treatment of AD. This study opens a new avenue and suggests the exploratory potential of Indomycinones for their various pharmacological actions.
Exploring the therapeutic potential of steroidal alkaloids in managing Alzheimer’s disease
This article focuses on steroidal alkaloids, as a remarkable class of natural compounds, exhibiting extensive routes of structurally and functionally diverse molecules for the new potential therapeutic use in anti-inflammatory, AChE inhibition etc on Alzheimer’s disease progression. The purpose of this review article was to provide an overview of the mechanism, toxicity and neuroprotective benefits of steroidal alkaloids and to discuss future possibilities to improve the application of steroidal alkaloids as anti-Alzheimer’s disease agents. The therapeutic value and limitations of the steroidal alkaloid are investigated to provide new perspectives for future clinical development studies.
*This article was nominated and selected for a special issue collection of cutting-edge Alzheimer’s articles for Elsevier’s Sustainability and Development Resource Center during the month of September 2024 for Alzheimer’s Awareness Month.
Effect of epigenetic changes in hypoxia-induced (HIF) gene across cancer types.
This article deals with cancer hypoxia, a key characteristic of malignancy, which impacts gene expression, metabolism, and tumor formation mechanisms. It triggers a complex network of cell signaling pathways, including NF-κB, PI3K, mTOR/AKT, MAPK, and HIF. Epigenetic modifications lead to gene mutations, altering the epigenome, and posing a challenge in developing treatment strategies. Advances in omics and multi-view clustering algorithms offer opportunities for subtyping cancers, improving prognosis and treatment outcomes, and understanding pathophysiological mechanisms. Understanding the role of the HIF gene in hypoxic environments is crucial for developing novel treatment options.