Mini Reviews in Medicinal Chemistry - Volume 22, Issue 10, 2022

Background: Alzheimer's disease (AD) is a multifactorial disorder coupled with an array of neuropathological mechanisms, including tau phosphorylation, Aβ aggregation, metal ion deregulation, and oxidative stress, along with neuro-inflammation. The clinically available drugs for the management of AD include four acetylcholinesterase inhibitors and one glutamatergic antagonist. These agents provide only temporary relief from the symptoms by altering the neurotransmitter level in the brain. Objective: Keeping in view the focus on research, the numerous pharmacological activities associated with the aromatic diazole heterocyclic nucleus, imidazole, triggered the medicinal chemist to develop a large number of novel anti-AD compounds targeting multiple pathological mechanisms associated with AD. These prepared analogs represent a higher potential against neurological disorders, including AD. This review article aims an ornately pronounce the therapeutic voyage of imidazole and its analogs as anti-AD. Methods: It emphasizes the synthesized imidazole derivatives as anti-AD with multiple targets reviewed from the data available on Pubmed. Results: These compounds diminish the pathophysiological aspects of AD; still, further studies are required to prove the safety and efficacy of these compounds in humans. Conclusion: The review aims to provide knowledge and highlight the status of this moiety in the design and development of novel drug candidates against Alzheimer’s disease conditions. Thus, it paves the way for further work.

Background: Long non-coding RNA rhabdomyosarcoma 2-associated transcript (LncRNA RMST) can affect every aspect of tumor progressions, such as proliferation, translocation, and apoptosis. As a result, RMST can be used as an attractive biomarker for early diagnosis and clinical therapies of different disease states. This article aims to review pathophysiological functions, molecular mechanisms as well as promising biotherapies of RMST in multiple tumors. Methods: Through the systematic induction and summary of 46 papers published in PubMed concerning this study, the molecular mechanisms of RMST in all kinds of tumors have been reviewed. Results: LncRNA RMST is a tumor-related regulatory mediator, aberrantly expressed in diverse tumors, including medullary thyroid cancer, hepatocellular carcinoma, endometrial carcinoma, colon cancer, pancreatic cancer, glioma, Wilm’s tumor, and breast cancer. Furthermore, as a mechanismbased player, RMST probably guides the translation and post-translation modification, containing DNA methylation and SUMOylation. It is capable of regulating distinct tumor cells and stem cells of biological behaviors via various molecular pathways. Conclusion: LncRNA RMST, potentially as an original therapeutic target, is valuable in the occurrence, development, and apoptosis of different tumors.

The existence of multidrug–resistant (MDR) E. coli (superbugs) is a global health issue confronting humans, livestock, food processing units, and pharmaceutical industries. The quorum sensing (QS) controlling ability of the E. coli to form biofilms has become one of the important reasons for the emergence of multidrug-resistant pathogens. Quorum signaling activation and formation of biofilm lead to the emergence of antimicrobial resistance of the pathogens increasing the therapy difficult for treating bacterial diseases. There is a crucial need, therefore, to reinforce newer therapeutic designs to overcome this resistance. As the infections caused by E. coli are attributed via the QSregulated biofilm formation, easing this system by QS inhibitors is a possible strategy for treating bacterial diseases. Plant based natural products have been reported to bind to QS receptors and interrupt the QS systems of pathogens by inhibiting biofilm formation and disrupting the formed biofilms, thus minimizing the chances to develop a resistance mechanism. The present report reviews critically the QS capability of E. coli to form biofilms leading to multidrug resistant pathogens and the investigations that have been carried out so far on plant acquired natural products as QS inhibitors.

The beneficial effect of plants in treating diabetes is not only well-known in traditional medicine but also confirmed in numerous scientific studies. The basic platform for testing the potential antidiabetic activity of traditionally known plants and their bioactive compounds is a set of in vitro, in vivo experiments, clinical trials, and molecular docking studies. Basic assays usually measure enzyme inhibitory activity (α-amylase and α-glucosidase) and other aspects related to diabetes mellitus disease. Recently, the use of plant-derived compounds has proven useful in treating diabetes and reducing complications resulting from high blood sugar levels. The main goal is to establish an action mechanism of plant extracts or active compounds to find new antidiabetic drugs with less toxicological properties. This work aims to collect data and discuss the newest results in the area of plant extracts, compounds, and antidiabetic effects using in vitro, in vivo, and in silico models. The data covered in this review include plant extracts, polyphenols, terpenoids, saponins, phytosterols, and other bioactive compounds, with some of the investigated plants being less known. Isolation of new compounds might be a plentiful source for treatment and prevention of diabetes mellitus. Clinical trials with adequate monitoring give the best results of plants' product efficacy and safety. Many studies have confirmed the importance of patent and use of medicinal herbs in the treatment of diabetes.

The field of Free Radical Chemistry has gained considerable interest in the current scenario. The formation of free radicals is attributable to different physiochemical factors, radiation exposure, pathological conditions, environmental contaminants, and as by-products of metabolized drugs. The concentration of free radicals is regulated strongly under normal conditions by physiological antioxidants. Free radicals may cause oxidative damage to proteins, lipids, sugars, and DNA when abundantly produced or when antioxidants are depleted. This imbalance of reduction-oxidation, referred to as oxidative stress, can change the body's physiological conditions and ultimately lead to tissue injury, further contributing to various disease pathologies. A proper balance between free radicals and antioxidants is required for an effective physiological process. The oxidation mechanism is chemically hindered by antioxidants; these are often called free radical scavengers. The application of an external antioxidant source is crucial in addressing the issue of oxidative stress. Plenty of naturally occurring, semi-synthetic, and synthetic antioxidants are used, and the search for an efficient, non-toxic, and safe antioxidant is stepped up over time. As an influential scaffold, thiophene and its derivatives have become a significant source of interest for researchers due to its substantial variety of biological activities. The versatility of thiophene moiety has been identified by an affluent unveiling of its derivatives with anti-inflammatory, antioxidant, anti-cancer, and antimicrobial behaviors. Thiophene activity has been influenced greatly by the nature and orientation of the substitutions. The current study aims at addressing various synthetic compounds with thiophene or condensed thiophene as a fundamental moiety or substituent as radical scavengers.

The present article reviews the effects of the textile in the wound healing process, as well as the availability of these products in the market. A brief description of applications is given based on the literature obtained from searching the scientific databases, besides the data obtained from secondary sources, like books and congress proceedings. The historical context of the textiles used in wounds, their general characteristics, particularities in the healing process, and incorporation of new technologies are discussed. It was evidenced that the textiles and associated technologies might influence directly or indirectly the stimulation of collagen, cell migration, angiogenesis, and reduction of pro-inflammatory factors and fibroblasts. However, the mechanisms by which the textiles act in the healing process are not well established in the literature. The interaction among textile engineering, biotechnology, medicine, and pharmacology is essential for the improvement and development of new products with better efficiency and accessibility.

Diabetes mellitus is the most common chronic metabolic disorder and is considered one of the leading causes of morbidity and mortality. The improperly-treated chronic hyperglycemia of diabetes has been related to several long-term complications and multiple organ failures, including nephropathy, which can lead to kidney failure, retinopathy with the potential loss of vision, and cardiovascular symptoms. Current commercially available synthetic glucose-lowering agents have been reported to have several adverse effects. Therefore, the search for alternative remedies such as medicinal plants and their active compounds have attracted attention. Chrysin is an active flavonoid that exists widely in various plants and diets and has been reported to possess pharmacological properties, including antidiabetic activity. Many studies have been conducted to characterize the antidiabetic of chrysin, as well as its potential pathways, in in vitro and in vivo experiments. Chrysin has shown promise as an antidiabetic agent in animal studies, thus, demonstrating its potential to be developed as an antidiabetic drug. This review discussed the antidiabetic action of chrysin and its mechanisms, including targeting different mechanisms such as stimulation of insulin signaling, blockage of endoplasmic reticulum stress and oxidative damage, promotion of skeletal glucose uptake, as well as modulation of apoptosis and autophagy signaling. Additionally, this review would be useful for further studies regarding the mechanism of work of plant derived-compound as a potential antidiabetic agent.