Constant exposure to harmful substances from both inside and outside the body can mess up the body’s natural ways of keeping itself in balance. This can cause severe skin damage, including basal cell carcinoma (BCC), squamous cell carcinoma (SCC), and melanoma. However, plant-derived compounds found in fruits and vegetables have been shown to protect against skin cancer-causing free radicals and other harmful substances. It has been determined that these dietary phytochemicals are effective in preventing skin cancer and are widely available, inexpensive, and well-tolerated. Studies have shown that these phytochemicals possess anti-inflammatory, antioxidant, and antiangiogenic properties that can aid in the prevention of skin cancers. In addition, they influence crucial cellular processes such as angiogenesis and cell cycle control, which can halt the progression of skin cancer. The present paper discusses the benefits of specific dietary phytochemicals found in fruits and vegetables, as well as the signaling pathways they regulate, the molecular mechanisms involved in the prevention of skin cancer, and their drawbacks.
Increasing cases of sunburn is one of the serious problems across the globe. In this connection, there is an urgent requirement for some effective sun screening agents. In the search for the same, nanoemulsions of some new synthesized and characterized chalcone derivatives were prepared and evaluated in vitro and in vivo. In order to meet the said objective, in the first step, vanillin was reacted with 4-aminoacetophenone in the presence of 15% sodium hydroxide and ethanol to synthesize the target compounds (C-1 to C-5). Progress of reaction was monitored using thin-layer chromatography (TLC). The crystals of purified compounds were characterized using spectroscopic techniques such as Infrared (IR) spectroscopy, 1H-NMR spectroscopy, 13C-NMR, and mass spectrometry. We prepared the nanoemulsions of the final compounds (C-1 to C-5) and subsequently evaluated them for in vitro sun protection factor activity. The concentration of the nanoemulsions, consistently ranging from 0.88 to 0.91 mg/mL across all formulations, demonstrated a high degree of consistency. The range of particle size varied from approximately 172 to 183 nm, with low polydispersity index values (approximately 0.11 to 0.15). The negative zeta potentials recorded for all the formulations (ranging from −35.87 mV to −39.30 mV) showed that the nanoemulsions are electrostatically stable enough to keep them from sticking together. The pH values of the nanoemulsions ranged narrowly from approximately 5.00 to 5.16, which indicated the compatibility of emulsion with biological systems and the potential to reduce irritation or instability during administration. The viscosity of the nanoemulsions varied between 2.00 and 2.12 cP. In silico studies were performed using MMP-I and MMP-2 as target receptors. For in vitro SPF evaluation, the Mansur equation was employed. COLIPA guidelines were compiled for in vivo SPF evaluation. The nanoemulsions derived from compounds C-3 and C-4, designated as C-3NE and C-4NE, were more effective as anti-aging agents. Findings suggested the possible scope of further synthesis of newer synthetic derivatives of chalcones for furfur development nanoemulsions for better SPF activity.
The present work was aimed to synthesize eight new diphenylamine derivatives by the reactions of 2-chloro-N-(4-(diphenyl amino) thiazol-2-yl)acetamide with substituted phenols in the chloroform along with anhydrous potassium carbonate and potassium iodide. The structures of newly synthesized compounds were characterized by IR, NMR, Mass and elemental analysis techniques. Toxicity profile (acute and subacute oral toxicity) and biological activity (analgesic and anti-inflammatory activity) of the synthesized derivatives was performed. Findings of the present work suggested that the synthesized compounds may be one of the excellent potent compounds to treat pain and inflammation. Therefore compounds of this group especially AK-4 (N-(4-(diphenylamino)thiazol-2-yl)-2-(2- nitrophenoxy)acetamide) could be an excellent starting point to build up new lead compounds in the management of pain and inflammation.
Ferroptosis, an iron-dependent form of regulated cell death driven by phospholipid peroxidation, has emerged as a potential contributor to neuronal dysfunction and degeneration in Alzheimer’s disease (AD). This review critically examines the biochemical basis, AD-specific evidence, chemical modulators, and therapeutic prospects of ferroptosis, emphasizing the distinction between mechanistic compatibility and causal demonstration. Ferroptotic susceptibility is governed by the balance among polyunsaturated phospholipid substrates, redox-active iron, lipid-peroxyl radical propagation, and enzymatic or chemical termination systems, including glutathione peroxidase 4 (GPX4), FSP1, and radical-trapping antioxidants. Human and experimental AD studies show brain iron accumulation, enhanced lipid peroxidation, impaired glutathione/GPX4 defenses, and disrupted iron export, but none establishes neuronal ferroptosis as the predominant mode of cell death. Two randomized trials of brain-penetrant iron chelation lowered the bulk brain iron signal and worsened clinical outcomes, which refutes the proposition that depleting bulk brain iron is therapeutic; because neither trial measured the kinetically labile iron pool, the mechanism of that harm remains undetermined. Among emerging strategies, membrane-active radical-trapping antioxidants and substrate-directed approaches offer mechanistically rational alternatives, whereas many natural products and multitarget agents remain difficult to interpret pharmacologically. Future studies should integrate cell-type-resolved redox lipidomics, direct target engagement, and rigorous causal intervention to determine whether ferroptosis or chronic sublethal lipid peroxidation is therapeutically actionable in AD.
Oriental Journal of Chemistry is a peer reviewed quarterly research journal of pure and applied chemistry. It publishes standard research papers in almost all thrust areas of current chemistry of academic and commercial importance. It provides a platform for rapid publication of quality research papers, reviews and chemistry letters. Oriental Journal of Chemistry is abstracted and indexed in almost all reputed National and International agencies.
Novel multifunctional medication candidates are needed to treat Alzheimer’s disease (AD), a neurodegenerative illness with few treatments. A nitrogen-containing heterocycle, piperidine, is a popular medicinal chemistry scaffold with broad therapeutic potential. We synthesized a series of novel piperidin-1-yl-phenyl-acetamide derivatives (AS-1 to AS-5) by reacting piperidine with 4-chloroaniline and characterizing them by IR, 1 H NMR, 13 C NMR, and mass spectrometry. All compounds meet Lipinski’s rule of five for drug-likeness and oral bioavailability. AutoDockVina molecular docking demonstrated that compounds AS-5 and AS-2 bind acetylcholinesterase (AChE) with affinities comparable to or higher than donepezil, suggesting they may inhibit AChE. AS-5 was the most potent free radical scavenger in DPPH and FRAP studies. Further behavioral evaluation utilizing Y-maze and Morris water maze tests showed that AS-5 was more effective against Alzheimer’s than AS-1. Piperidin-1-yl-phenyl-acetamide derivatives, particularly the 2,5-dimethyl-substituted counterpart (AS-5), have multifunctional properties due to acetylcholinesterase inhibition and antioxidant activity. These findings suggest AS-5 as a lead chemical for optimizing and developing Alzheimer’s disease treatments. The piperidin-1-yl-phenyl-acetamide derivative (AS-5)’s significant acetylcholinesterase inhibition, robust antioxidant action, and in vivo cognitive enhancement comparable to Donepezil make it important. Structure–activity relationship insight highlights the 2,5-dimethyl substitution as a significant driver of increased anti-Alzheimer action, providing a target for next-generation drug design.