scholarly journals AZP2006, a new promising treatment for Alzheimer’s and related diseases

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
N. Callizot ◽  
C. Estrella ◽  
S. Burlet ◽  
A. Henriques ◽  
C. Brantis ◽  
...  
Keyword(s):  
Therapeutic Application ◽  
Neuroprotective Effects ◽  
Beneficial Effects ◽  
Potential Therapeutic Application ◽  
Promising Treatment ◽  
Central Synapses ◽  
First Time ◽  
Pgrn Level

AbstractProgranulin (PGRN) is a protein with multiple functions including the regulation of neuroinflammation, neuronal survival, neurite and synapsis growth. Although the mechanisms of action of PGRN are currently unknown, its potential therapeutic application in treating neurodegenerative diseases is huge. Thus, strategies to increase PGRN levels in patients could provide an effective treatment. In the present study, we investigated the effects of AZP2006, a lysotropic molecule now in phase 2a clinical trial in Progressive Supranuclear Palsy patients, for its ability to increase PGRN level and promote neuroprotection. We showed for the first time the in vitro and in vivo neuroprotective effects of AZP2006 in neurons injured with Aβ1–42 and in two different pathological animal models of Alzheimer’s disease (AD) and aging. Thus, the chronic treatment with AZP2006 was shown to reduce the loss of central synapses and neurons but also to dramatically decrease the massive neuroinflammation associated with the animal pathology. A deeper investigation showed that the beneficial effects of AZP2006 were associated with PGRN production. Also, AZP2006 binds to PSAP (the cofactor of PGRN) and inhibits TLR9 receptors normally responsible for proinflammation when activated. Altogether, these results showed the high potential of AZP2006 as a new putative treatment for AD and related diseases.

scholarly journals Antioxidant and Anti-Inflammatory Effects of Citrus Flavonoid Hesperetin: Special Focus on Neurological Disorders

Antioxidants ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 609 ◽  
Author(s):  
Amjad Khan ◽  
Muhammad Ikram ◽  
Jong Ryeal Hahm ◽  
Myeong Ok Kim
Keyword(s):  
Neurodegenerative Disorders ◽  
In Vitro Models ◽  
Experimental Models ◽  
Special Focus ◽  
Neuroprotective Effects ◽  
Beneficial Effects ◽  
Wide Range ◽  
Underlying Mechanisms

Neurodegenerative disorders have emerged as a serious health issue in the current era. The most common neurodegenerative disorders are Alzheimer’s disease (AD), Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis (ALS). These diseases involve progressive impairment of neurodegeneration and memory impairment. A wide range of compounds have been identified as potential neuroprotective agents against different models of neurodegeneration both in vivo and in vitro. Hesperetin, a flavanone class of citrus flavonoid, is a derivative of hesperidin found in citrus fruits such as oranges, grapes, and lemons. It has been extensively reported that hesperetin exerts neuroprotective effects in experimental models of neurodegenerative diseases. In this systematic review, we have compiled all the studies conducted on hesperetin in both in vivo and in vitro models of neurodegeneration. Here, we have used an approach to lessen the bias in each study, providing a least biased, broad understanding of findings and impartial conclusions of the strength of evidence and the reliability of findings. In this review, we collected different papers from a wide range of journals describing the beneficial effects of hesperetin on animal models of neurodegeneration. Our results demonstrated consistent neuroprotective effects of hesperetin against different models of neurodegeneration. In addition, we have summarized its underlying mechanisms. This study provides the foundations for future studies and recommendations of further mechanistic approaches to conduct preclinical studies on hesperetin in different models.

scholarly journals Bioconversion of Corticosterone into Corticosterone-Glucoside by Glucosyltransferase

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1783 ◽  
Author(s):  
Tokutaro Yamaguchi ◽  
Joo-Ho Lee ◽  
A-Rang Lim ◽  
Joon-Soo Sim ◽  
Eun-Ji Yu ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Hydroxyl Group ◽  
Oxygen Species ◽  
Neuroprotective Agents ◽  
Neuroprotective Effects ◽  
The Difference ◽  
First Time ◽  
Resolution Mass

Glucosylation of the 21-hydroxyl group of glucocorticoid changes its solubility into hydrophilicity from hydrophobicity and, as with glucocorticoid glucuronides as a moving object in vivo, it is conceivable that it exhibits the same behavior. Therefore, glucosylation to the 21-hydroxyl group while maintaining the 11β-hydroxyl group is particularly important, and glucosylation of corticosterone was confirmed by high-resolution mass spectrometry and 1D (1H and 13C) and 2D (COSY, ROESY, HSQC-DEPT and HMBC) NMR. Moreover, the difference in bioactivity between corticosterone and corticosterone 21-glucoside was investigated in vitro. Corticosterone 21-glucoside showed greater neuroprotective effects against H2O2-induced cell death and reactive oxygen species (ROS) compared with corticosterone. These results for the first time demonstrate that bioconversion of corticosterone through the region-selective glucosylation of a novel compound can present structural potential for developing new neuroprotective agents.

scholarly journals A Study on the Quality and Identity of Brazilian Pampa Biome Honey: Evidences for Its Beneficial Effects against Oxidative Stress and Hyperglycemia

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
L. C. Cruz ◽  
J. E. S. Batista ◽  
A. P. P. Zemolin ◽  
M. E. M. Nunes ◽  
D. B. Lippert ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
High Concentration ◽  
Beneficial Effects ◽  
Pampa Biome ◽  
First Time

We characterized, for the first time, the quality and identity of Brazilian Pampa biome honey and its antioxidant propertiesin vitro(FRAP, DDPH and ABTS). The potential protective effect of honey against oxidative stress induced by iron (Fe) and paraquat, (PQ) in aDrosophila melanogastermodel (in vivo) was also tested. The results indicated that all honey samples tested showed antioxidant activityin vitro. Flies treated with honey showed increased lifespan and were protected against oxidative stress induced by Fe and PQ. Despite the high concentration of sugars in honey (approximately 70–80%), our results demonstrate a hypoglycemic-like effect of honey inDrosophila. Thus, this study demonstrates the high quality of Brazilian Pampa biome honey as well as its significant antioxidant activityin vitroandin vivo, pointing to the potential use of this natural product as an alternative in the therapy of oxidative stress-associated diseases.

scholarly journals Protective Effects and Mechanism of Radix Polygalae Against Neurological Diseases as Well as Effective Substance

2021 ◽  
Vol 12 ◽  
Author(s):  
Ning Jiang ◽  
Shanshan Wei ◽  
Yiwen Zhang ◽  
Wenlu He ◽  
Haiyue Pei ◽  
...  
Keyword(s):  
Neurological Diseases ◽  
Chinese Herb ◽  
Receptor Activation ◽  
Mechanisms Of Action ◽  
Protective Effects ◽  
Neuroprotective Effects ◽  
Beneficial Effects ◽  
Apoptotic Effects

Radix Polygalae (also known as Yuanzhi in China) is the dried rhizome of Polygala tenuifolia Willd. or Polygala sibirica L., which is a famous Chinese herb and has been widely used for centuries in traditional medicines including expectorants, tonics, tranquilizers, antipsychotic, and so on. This article reviews the neuroprotective effects of Radix Polygalae in preclinical models of central nervous system (CNS) disorders, especially anxiety, depression, declining cognition, Alzheimer's disease (AD), and Parkinson's disease (PD). The chemical composition of Radix Polygalae as well as the underlying mechanisms of action were also reviewed. We found that Radix Polygalae possesses a broad range of beneficial effects on the abovementioned conditions. The multifold mechanisms of action include several properties such as antioxidant and associated apoptotic effects; anti-inflammatory and associated apoptotic effects; neurogenesis, regeneration, differentiation, and neuronal plasticity improvement; hypothalamic–pituitary–adrenal axis (HPA) regulation; neurotransmitter release; and receptor activation (A2AR, NMDA-R, and GluR). Nevertheless, the detailed mechanisms underlying this array of pharmacological effects observed in vitro and in vivo still need further investigation to attain a coherent neuroprotective profile.

scholarly journals Essential Oils and Bioactive Components against Arthritis: A Novel Perspective on Their Therapeutic Potential

Plants ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 1252
Author(s):  
Mariangela Marrelli ◽  
Valentina Amodeo ◽  
Maria Rosaria Perri ◽  
Filomena Conforti ◽  
Giancarlo Statti
Keyword(s):  
Essential Oils ◽  
Therapeutic Potential ◽  
Current Knowledge ◽  
Point Of View ◽  
Beneficial Effects ◽  
Negative Results ◽  
Potential Therapeutic Application ◽  
In Vitro Effects

Essential oils (EOs) are known to possess a number of beneficial properties. Their antimicrobial, anti-inflammatory, antioxidant, antidiabetic, and cancer-preventing activities have been extensively reported. Due to their wide use as food preservers and additives, as well as their use in agriculture, perfumes, and make-up products, these complex mixtures of volatile compounds have gained importance from a commercial point of view, not only in the pharmaceutical industry, but also in agronomic, food, cosmetic, and perfume industries. An analysis of the recent scientific literature allowed us to highlight the presence of an increasing number of studies on the potential antiarthritic properties of EOs and their main constituents, which seems to suggest a new interesting potential therapeutic application. The aim of this review is to examine the current knowledge on the beneficial effects of essential oils in the treatment of arthritic diseases, providing an overview of the reports on the in vivo and in vitro effects of EOs. Furthermore, this review critically examines the recent findings on the potential roles of the main components of EOs in the exerted beneficial effects. Obtained negative results are also reported.

scholarly journals Ursolic and Oleanolic Acids: Plant Metabolites with Neuroprotective Potential

2021 ◽  
Vol 22 (9) ◽  
pp. 4599
Author(s):  
Evelina Gudoityte ◽  
Odeta Arandarcikaite ◽  
Ingrida Mazeikiene ◽  
Vidmantas Bendokas ◽  
Julius Liobikas
Keyword(s):  
Plant Defence ◽  
Model Systems ◽  
Animal Origin ◽  
Antioxidant Systems ◽  
Plant Metabolites ◽  
Neuroprotective Effects ◽  
Secondary Plant Metabolites ◽  
Beneficial Effects

Ursolic and oleanolic acids are secondary plant metabolites that are known to be involved in the plant defence system against water loss and pathogens. Nowadays these triterpenoids are also regarded as potential pharmaceutical compounds and there is mounting experimental data that either purified compounds or triterpenoid-enriched plant extracts exert various beneficial effects, including anti-oxidative, anti-inflammatory and anticancer, on model systems of both human or animal origin. Some of those effects have been linked to the ability of ursolic and oleanolic acids to modulate intracellular antioxidant systems and also inflammation and cell death-related pathways. Therefore, our aim was to review current studies on the distribution of ursolic and oleanolic acids in plants, bioavailability and pharmacokinetic properties of these triterpenoids and their derivatives, and to discuss their neuroprotective effects in vitro and in vivo.

scholarly journals Osthole enhances the bone mass of senile osteoporosis and stimulates the expression of osteoprotegerin by activating β-catenin signaling

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Zhen-Xiong Jin ◽  
Xin-Yuan Liao ◽  
Wei-Wei Da ◽  
Yong-Jian Zhao ◽  
Xiao-Feng Li ◽  
...  
Keyword(s):  
Bone Mass ◽  
Osteoclast Formation ◽  
Dependent Manner ◽  
Therapeutic Application ◽  
Senile Osteoporosis ◽  
Protein Levels ◽  
Potential Therapeutic Application ◽  
Dose Dependent

Abstract Introduction Osthole has a potential therapeutic application for anti-osteoporosis. The present study verified whether osthole downregulates osteoclastogenesis via targeting OPG. Methods In vivo, 12-month-old male mice were utilized to evaluate the effect of osthole on bone mass. In vitro, bone marrow stem cells (BMSCs) were isolated and extracted from 3-month-old OPG−/− mice and the littermates of OPG+/+ mice. Calvaria osteoblasts were extracted from 3-day-old C57BL/6J mice or 3-day-old OPG−/− mice and the littermates of OPG+/+ mice. Results Osthole significantly increased the gene and protein levels of OPG in primary BMSCs in a dose-dependent manner. The deletion of the OPG gene did not affect β-catenin expression. The deletion of the β-catenin gene inhibited OPG expression in BMSCs, indicating that osthole stimulates the expression of OPG via activation of β-catenin signaling. Conclusion Osthole attenuates osteoclast formation by stimulating the activation of β-catenin-OPG signaling and could be a potential drug for the senile osteoporosis.

scholarly journals Sulforaphane as a Potential Protective Phytochemical against Neurodegenerative Diseases

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Andrea Tarozzi ◽  
Cristina Angeloni ◽  
Marco Malaguti ◽  
Fabiana Morroni ◽  
Silvana Hrelia ◽  
...  
Keyword(s):  
Neurodegenerative Diseases ◽  
Neurological Disorders ◽  
Neuronal Loss ◽  
In Vivo Studies ◽  
Alternative Form ◽  
Neuroprotective Effects ◽  
Beneficial Effects ◽  
Hydrolysis Of

A wide variety of acute and chronic neurodegenerative diseases, including ischemic/traumatic brain injury, Alzheimer’s disease, and Parkinson's disease, share common characteristics such as oxidative stress, misfolded proteins, excitotoxicity, inflammation, and neuronal loss. As no drugs are available to prevent the progression of these neurological disorders, intervention strategies using phytochemicals have been proposed as an alternative form of treatment. Among phytochemicals, isothiocyanate sulforaphane, derived from the hydrolysis of the glucosinolate glucoraphanin mainly present inBrassicavegetables, has demonstrated neuroprotective effects in several in vitro and in vivo studies. In particular, evidence suggests that sulforaphane beneficial effects could be mainly ascribed to its peculiar ability to activate the Nrf2/ARE pathway. Therefore, sulforaphane appears to be a promising compound with neuroprotective properties that may play an important role in preventing neurodegeneration.

scholarly journals Osthole enhances the bone mass of senile osteoporosis and stimulates the expression of osteoprotegerin by activating β-catenin signaling

2021 ◽  
Author(s):  
Zhen-Xiong Jin ◽  
Xin-Yuan Liao ◽  
Wei-Wei Da ◽  
Yong-Jian Zhao ◽  
Xiao-Feng Li ◽  
...  
Keyword(s):  
Bone Mass ◽  
Osteoclast Formation ◽  
Dependent Manner ◽  
Therapeutic Application ◽  
Senile Osteoporosis ◽  
Protein Levels ◽  
Potential Therapeutic Application ◽  
Dose Dependent

Abstract Introduction Osthole has a potential therapeutic application for anti-osteoporosis. The present study verified whether osthole downregulates osteoclastogenesis via targeting OPG. Methods In vivo, 12-month-old male mice were utilized to evaluate the effect of osthole on bone mass. In vitro, bone marrow stem cells (BMSCs) were isolated and extracted from 3-month-old OPG-/- mice and the littermates of OPG+/+ mice. calvaria osteoblasts were extracted from 3-day-old C57BL/6J mice or 3-day-old OPG-/- mice and the littermates of OPG+/+ mice.Results Osthole significantly increased the gene and protein levels of OPG in primary BMSCs in a dose-dependent manner. The deletion of the OPG gene did not affect β-catenin expression. The deletion of the β-catenin gene inhibited OPG expression in BMSCs, indicating that osthole stimulates the expression of OPG via activation of β-catenin signaling.Conclusion Osthole attenuates osteoclast formation by stimulating the activation of β-catenin-OPG signaling and could be a potential drug for the senile osteoporosis.

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