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Neurodegenerative diseases (NDs), characterized by progressive degeneration and death of neurons, are strongly related to aging, and the number of people with NDs will continue to rise. Alzheimer's disease (AD) and Parkinson's disease (PD) are the most common NDs, and the current treatments offer no cure. A growing body of research shows that AD and especially PD are intricately related to intestinal health and the gut microbiome and that both diseases can spread retrogradely from the gut to the brain. Zeolites are a large family of minerals built by [SiO4]4− and [AlO4]5− tetrahedrons joined by shared oxygen atoms and forming a three-dimensional microporous structure holding water molecules and ions. The most widespread and used zeolite is clinoptilolite, and additionally, mechanically activated clinoptilolites offer further improved beneficial effects. The current review describes and discusses the numerous positive effects of clinoptilolite and its forms on gut health and the gut microbiome, as well as their detoxifying, antioxidative, immunostimulatory, and anti-inflammatory effects, relevant to the treatment of NDs and especially AD and PD. The direct effects of clinoptilolite and its activated forms on AD pathology in vitro and in vivo are also reviewed, as well as the use of zeolites as biosensors and delivery systems related to PD. [ABSTRACT FROM AUTHOR]

We tested in vivo anti-herpetic effect of castalagin, an ellagitannin compound, extracted from pedunculate oak (Quercus robur). Previous investigations found that castalagin possesses a strong inhibitory effect in vitro against HSV-1/2 equal to acyclovir (ACV). It is also effective against ACV-resistant mutants and shows a synergistic effect with ACV. We study castalagin's activity towards HSV-1 infection in newborn mice. Acute toxicity determination in mice showed LD50 value of 295mg/kg. Prolonged toxicity was also constructed. Castalagin manifested a marked activity against HSV-1 (LD90/0.02 ml) administered in 7-day course at 0.02ml s.c. doses of 7.5 or 10 mg/kg (PI 57-58%). ACV course demonstrated a marked activity at 20 mg/kg. The selectivity ratio LD50/ED50 (295/7.5) could be accepted as ≥ 33. [ABSTRACT FROM AUTHOR]

Pomegranate (Punica granatum L.) is a rich source of polyphenols, including ellagitannins and ellagic acid. The plant is used in traditional medicine, and its purified components can provide anti-inflammatory and antioxidant activity and support of host defenses during viral infection and recovery from disease. Current data show that pomegranate polyphenol extract and its ellagitannin components and metabolites exert their beneficial effects by controlling immune cell infiltration, regulating the cytokine secretion and reactive oxygen and nitrogen species production, and by modulating the activity of the NFκB pathway. In vitro, pomegranate extracts and ellagitannins interact with and inhibit the infectivity of a range of viruses, including SARS-CoV-2. In silico docking studies show that ellagitannins bind to several SARS-CoV-2 and human proteins, including a number of proteases. This warrants further exploration of polyphenol–viral and polyphenol–host interactions in in vitro and in vivo studies. Pomegranate extracts, ellagitannins and ellagic acid are promising agents to target the SARS-CoV-2 virus and to restrict the host inflammatory response to viral infections, as well as to supplement the depleted host antioxidant levels during the stage of recovery from COVID-19. [ABSTRACT FROM AUTHOR]

Peptides and peptidomimetics are a major field of bioorganic chemistry research. We endeavored to describe the current trends in medicinal and bioorganic chemistry regarding the design of drug molecules which are peptide mimetics. To this end, we reviewed the literature regarding peptidomimetics classification, new research data on innovative potential drug molecules, current research, and its perspectives. Potential or current neuropharmacological agents that possess a peptide bond in their molecules and can be used in the treatment of pain or Alzheimer's disease are of particular interest to our study. The inclusion criteria required that the studies explore peptides, peptide mimetics, and peptidomimetics or mimetics of peptides that show biological activity in the central/peripheral nervous system. Electronic search strategies were developed and undertaken, and relevant articles were selected and reviewed. A considerable number of pharmacological agents showing pharmacotherapeutic relevance were identified and reviewed regarding biological activity in the nervous system. The ones more closely reviewed are prospective or proven effective neuropharmacological agents that are analogs of peptides/oligopeptides. The potential for discovery of various peptides and peptidomimetics, which can affect the pathogenesis of pain, neurodegenerative diseases (Alzheimer's disease, Parkinson's disease and others) offers to broaden the scientific horizon; in the end leading to the synthesis of potential alternatives to current pharmacotherapeutics. Translational research can be encouraged after careful consideration of the risk-benefit ratio. [ABSTRACT FROM AUTHOR]

Myrtenal (M) is a natural bicyclic monoterpenoid with poorly studied neuroprotective potential. Our previous results established memory improvement in rats accompanied by significantly increased brain acetylcholine (ACh) levels. Adamantane is used as a pharmacophore for new drugs design based on known pharmacological agents for the development of medicines with stronger effects or with different therapeutic properties. The aim of this study was to evaluate on male Wistar rats the memory-improving potential of two Myrtenal- Adamantane derivatives MDs (MD-197, MD-198), synthesized in Novosibirsk Institute of Organic Chemistry. Both substances (1 mg kg-1 b.wt.) and the referent Myrtenal (40 mg kg-1 b.wt.), were applied as intraperitoneal (i.p.) emulsions for 11 consecutive days. Memory status was evaluated via a Passive avoidance test (at the beginning and at the end of the experiment). Acetylcholine esterase (AChE) activity, noradrenaline (NA), and serotonin (5-HT) content in brain structures related to memory (cortex and hippocampus) were biochemically measured. Results demonstrated significant memory improvement after multiple applications of both MDs. The significant inhibition of hippocampal AChE activity after MD-197 and MD-198 treatment was accompanied by specific changes in monoamine levels in the cerebral cortex and hippocampus. MD-197 significantly increased brain NA and 5-HT content showing potential antidepressant properties. All established effects of the two Myrtenal-Adamantane conjugates were stronger than those of the natural Myrtenal. This research revealed for the first time MDs' improving memory capacity related to their AChE inhibiting activity and neuromodulatory ability. These original data provide a reason for further investigation of these new perspective substances on the experimental model of dementia. [ABSTRACT FROM AUTHOR]

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Apples contain substantial amounts of polyphenols, and diverse phenolics - mainly flavonoids and phenolic acids, have been identified in their flesh and skins. This work aimed to analyze the overall landscape of the research literature published to date on apple phenolic compounds in the context of human and animal health. The Web of Science Core Collection electronic database was queried with (apple* polyphenol*) AND (health* OR illness* OR disease* OR medic* OR pharma*) to identify relevant papers covering these words and their derivatives in the titles, abstracts, and keywords. The resulted 890 papers were bibliometrically analyzed. The VOSviewer software was utilized to produce term maps that illustrate how the frequent phrases fared in terms of publication and citation data. The apple polyphenol papers received global contributions, particularly from China, Italy, the United States, Spain, and Germany. Examples of frequently mentioned chemicals/chemical classes are quercetin, anthocyanin, catechin, epicatechin, and flavonol, while examples of frequently mentioned medical conditions are cardiovascular disease, atherosclerosis, diabetes, Alzheimer's disease, and obesity. The potential health benefits of apple polyphenols on humans and animals are diverse and warrant further study. [ABSTRACT FROM AUTHOR]

Peptidomimetics are a class of chemical compounds, many of which are being developed as potential medications. Social isolation stress is known to negatively affect neurodevelopment and normal neural functions. The purpose of the study was to examine the neuropharmacological effects of M6 peptidomimetic, a derivative of the branched chain amino acid L-Valine and m-pyridinic acid, while focusing on the sexual dimorphism among its effects on memory, balance and exploratory behavior in adolescent male and female rats under social isolation stress. The aim was also to compare the effects observed with those of the peptidomimetic on control (grouped) adolescent male and female rats. The post-weaning social isolation (21st PND) of 12 Wistar male and 12 female rat pups over a period of 6 weeks was used as a method of chronic stress. Half of the animals (grouped and isolated) received M6 150 mg/kg (i. p.) daily for 3 days. Then they participated in a battery of behavioral tests: Rotarod test, Hole board test, and Step-through test. The rats were tested for memory retention 1 h after acquaintance of the animal with the Step through test, and 24 h later. ANOVA (mixed design) was used to compare and analyze the results obtained. It is shown that the rats’ memory and neuro-muscular coordination during their early post-adolescent period are diversely influenced by the chronic stress and the administration of peptidomimetic depending on the animals’ sex and on the isolation stress effect. [ABSTRACT FROM AUTHOR]