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Aqueous extract of Glycyrrhiza inflata inhibits aggregation by upregulating PPARGC1A and NFE2L2-ARE pathways in cell models of spinocerebellar ataxia 3.

Spinocerebellar ataxia (SCA) types 1, 2, 3, 6, 7, and 17 and dentatorubropallidoluysian atrophy, as well as Huntington disease, are a group of neurodegenerative disorders caused by a CAG triplet-repeat expansion encoding a long polyglutamine (polyQ) tract in the respective mutant proteins. The cytoplasmic and nuclear aggregate formation, a pathological hallmark of polyQ diseases, is probably the initial process triggering the subsequent pathological events. Compromised oxidative stress defense capacity and mitochondrial dysfunction have emerged as contributing factors to the pathogenesis of po

Development of Newly Synthesized Chromone Derivatives with High Tumor Specificity against Human Oral Squamous Cell Carcinoma.

Since many anticancer drugs show severe adverse effects such as mucositis, peripheral neurotoxicity, and extravasation, it was crucial to explore new compounds with much reduced adverse effects. Comprehensive investigation with human malignant and nonmalignant cells demonstrated that derivatives of chromone, back-bone structure of flavonoid, showed much higher tumor specificity as compared with three major polyphenols in the natural kingdom, such as lignin-carbohydrate complex, tannin, and flavonoid. A total 291 newly synthesized compounds of 17 groups (consisting of 12 chromones, 2 esters, an

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… Chalcones ( L ) were synthesized by base-catalyzed condensation of the corresponding acetophenones with various benzaldehyde derivatives [ 31 ] ( Figure 5 ). … Quantitative Structure-Cytotoxicity Relationship of Chalcones Anticancer Res. 2017 37 1091 1098 10.21873/anticanres.11421 28314269 48. Uesawa Y. Sakagami H. Okudaira N. Toda K. Takao K. Kagaya H. Sugita Y. …

Isoliquiritigenin from licorice root suppressed neovascularisation in experimental ocular angiogenesis models.

AIM: To explore the antiangiogenic property of isoliquiritigenin (ISL) on in vivo and in vitro models. DESIGN: Laboratory investigation. METHODS: The effect of ISL on angiogenesis development was investigated using ex ovo chick chorioallantoic membrane model. Its effect on pathological angiogenesis was examined by (1) silver nitrate cauterisation-induced corneal neovascularisation in BALB/c mice, followed by topical ISL (0.2-50 μM) and CD31 immunofluorescence of corneal blood vessels; (2) argon laser photocoagulation-induced choroidal neovascularisation in C57BL/6 mice, followed by intravitr

Deciphering the Potentials of Cardamom in Cancer Prevention and Therapy: From Kitchen to Clinic.

Cardamom (cardamum) is a spice produced from the seeds of several Elettaria and Amomum plants of the Zingiberaceae family. Cardamom has been demonstrated to offer numerous benefits, including its antioxidant, antimicrobial, anti-inflammatory, and other metabolic (anti-diabetic) properties, and its potential to reduce cancer risk. Recently, researchers have extracted and tested multiple phytochemicals from cardamom to assess their potential effectiveness against various types of human malignancy. These studies have indicated that cardamom can help overcome drug resistance to standard chemothera

MDM2/X Inhibitors as Radiosensitizers for Glioblastoma Targeted Therapy.

Inhibition of the MDM2/X-p53 interaction is recognized as a potential anti-cancer strategy, including the treatment of glioblastoma (GB). In response to cellular stressors, such as DNA damage, the tumor suppression protein p53 is activated and responds by mediating cellular damage through DNA repair, cell cycle arrest and apoptosis. Hence, p53 activation plays a central role in cell survival and the effectiveness of cancer therapies. Alterations and reduced activity of p53 occur in 25-30% of primary GB tumors, but this number increases drastically to 60-70% in secondary GB. As a result, reacti

Polyphenols: Chemoprevention and therapeutic potentials in hematological malignancies.

Polyphenols are one of the largest plant-derived natural product and they play an important role in plants' defense as well as in human health and disease. A number of them are pleiotropic molecules and have been shown to regulate signaling pathways, immune response and cell growth and proliferation which all play a role in cancer development. Hematological malignancies on the other hand, are cancers of the blood. While current therapies are efficacious, they are usually expensive and with unwanted side effects. Thus, the search for newer less toxic agents. Polyphenols have been reported to po

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… Hydroxycinnamic acids share a similar pathway of production with the likes of lignins, 89 coumarins, lignans, stilbenes, chalcones, anthocyanins and flavonoids ( 77 ). They are well-distributed in most plants including many species that are consumed as food or processed into beverages. … The chalcone butein has also been shown to markedly downregulate the protein expression levels of CDK4, CDK6, cyclin D1, cyclin D2, cyclin E and phospho-pRb in HTLV-1-infected T cells, both in vitro and in vivo suggesting its therapeutic potentials in ATLL ( 217 ). …

Medicinal Plants with Anti-Leukemic Effects: A Review.

Leukemia is a leukocyte cancer that is characterized by anarchic growth of immature immune cells in the bone marrow, blood and spleen. There are many forms of leukemia, and the best course of therapy and the chance of a patient's survival depend on the type of leukemic disease. Different forms of drugs have been used to treat leukemia. Due to the adverse effects associated with such therapies and drug resistance, the search for safer and more effective drugs remains one of the most challenging areas of research. Thus, new therapeutic approaches are important to improving outcomes. Almost half

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… . | Mitotic inhibitor and Arrests the cell division which causes the death of the cells | [ 84 ] Coreopsis lanceolata | Asteraceae | Flavonoids: flavanone, chalcones, and aurones 4 Methoxylanceoletin. | Leukemia HL-60 cells | Antiproliferation and Apoptosis induction | [ 85 , 86 , 87 ] Ferulago angulata … C. lanceolata flowers are also an excellent natural source of rare flavonoids, including flavanone, chalcones and aurones ( Figure 11 ), and they show strong antileukemic properties [ 86 ]. …

Oxyphenbutazone ameliorates carfilzomib induced cardiotoxicity in rats via inhibition of oxidative free radical burst and NF-κB/IκB-α pathway.

Carfilzomib (CFZ), a chemotherapeutic agent used for multiple myeloma treatments reported to cause high incidence of cardiac events either new onset and/or exacerbate formerly diagnosed heart failure with ventricular and myocardial dysfunction. Purpose: Current research designed to explore and examine the preventive effect of oxyphenbutazone in the CFZ -instigated cardiotoxicity. Methodology: Female Wistar Rats weighing 200-250 g selected randomly and grouped as follows: Group 1 designated as the Normal control and receive normal saline only. Group 2 served toxic control and exposed to CFZ (4

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… Synthesis of novel pyrazolic analogues of chalcones and their 3-aryl-4-(3-aryl-4,5-dihydro-1H-pyrazol-5-yl)-1- phenyl-1H-pyrazole derivatives as potential antitumor agents Bioorg. Med. Chem. 18 2010 4965 4974 20594863 10.1016/j.bmc.2010.06.013 Jones W.K. Brown M. Ren X. …

Advancing Brain Health Naturally: β-Caryophyllene and Xanthohumol as Neuroprotective Agents.

Neurodegenerative diseases (NDDs) represent a class of incurable and progressive disorders characterized by the gradual degeneration of the structure and function of the nervous system, particularly the brain and spinal cord. A range of innovative therapeutic approaches is currently under investigation, such as stem cell-based therapies, gene-editing platforms such as CRISPR, and immunotherapies directed at pathogenic proteins. Moreover, phytochemicals such as β-caryophyllene and xanthohumol have demonstrated significant neuroprotective potential in preclinical models. These natural agents exe

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… In recent years, XAN and other prenylated chalcones have drawn considerable scientific interest for their potential role in cancer prevention. … Xanthohumol, a Polyphenol Chalcone Present in Hops, Activating Nrf2 Enzymes To Confer Protection against Oxidative Damage in PC12 Cells. J. Agric. Food Chem. 2015;63:1521–1531. doi: 10.1021/jf505075n. 46. …

Protective Effects of Flavonoids Against Mitochondriopathies and Associated Pathologies: Focus on the Predictive Approach and Personalized Prevention.

Multi-factorial mitochondrial damage exhibits a "vicious circle" that leads to a progression of mitochondrial dysfunction and multi-organ adverse effects. Mitochondrial impairments (mitochondriopathies) are associated with severe pathologies including but not restricted to cancers, cardiovascular diseases, and neurodegeneration. However, the type and level of cascading pathologies are highly individual. Consequently, patient stratification, risk assessment, and mitigating measures are instrumental for cost-effective individualized protection. Therefore, the paradigm shift from reactive to pred

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… Additional minor classes of flavonoids include chalcones, dihydrochalcones, and aurones are categorized into minor flavonoids [ 85 , 86 ]. … Minor Flavonoids (Chalcones, Flavanones, Dihydrochalcones, and Aurones) Nat. Prod. 2013 1867 1900 86. Liskova A. Koklesova L. Samec M. Smejkal K. Samuel S.M. Varghese E. Abotaleb M. Biringer K. Kudela E. Danko J. …

Role of phytoconstituents in the management of COVID-19.

BackgroundCOVID-19, a severe global pandemic caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has emerged as one of the most threatening transmissible disease. As a great threat to global public health, the development of treatment options has become vital, and a rush to find a cure has mobilized researchers globally from all areas.Scope and approachThis review focuses on deciphering the potential of different secondary metabolites from medicinal plants as therapeutic options either as inhibitors of therapeutic targets of SARS-CoV-2 or as blockers of viral particles entry

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… B2 ( Bupleurum sp. ) Image 53 HCoV-229E Targets viral replication [ 110 ] β-Sitosterol ( Isatis indigotica ) Image 54 SARS CoV Against 3CL Pro [ 107 ] Flavaglines Silvestrol ( Algaria sp. ) Image 55 MERS-CoV Targets RNA helicase [ 111 ] Glucosides Sinigrin Image 56 SARS CoV Against 3CL Pro [ 107 ] Chalcones … Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV J. Enzym. Inhib. Med. Chem. 31 1 2016 23 30 10.3109/14756366.2014.1003215 25683083 113 Park J.Y. Jeong H.J. Kim J.H. Kim Y.M. Park S.J. Kim D. Park K.H. Lee W.S. Ryu Y.B. …

Интерферонские регулятивные факторы как потенциальная терапевтическая цель для нейроинфламмации: фокус на болезни Альцгеймера.

Регулирующие факторы интерферона (ИРФ) являются важнейшими модуляторами иммунной и подстрекательской реакции, однако их роль в болезни Альцгеймера (AD) и других нейродегенеративных расстройствах остается неполной. В то время как IRF признаются за их регулирующие функции в нейроинфламмации, микроглиальной активации и выживании нейронов, их двойная роль как факторов патологического воспаления и посредников нейрозащитных путей подчеркивает сложный нормативный парадокс в нейродегенеративных расстройствах. Цель этого обзора заключается в обобщении текущих данных о нейрофламмации в области АД и связ

A review of chemotherapeutic drugs-induced arrhythmia and potential intervention with traditional Chinese medicines.

Significant advances in chemotherapy drugs have reduced mortality in patients with malignant tumors. However, chemotherapy-related cardiotoxicity increases the morbidity and mortality of patients, and has become the second leading cause of death after tumor recurrence, which has received more and more attention in recent years. Arrhythmia is one of the common types of chemotherapy-induced cardiotoxicity, and has become a new risk related to chemotherapy treatment, which seriously affects the therapeutic outcome in patients. Traditional Chinese medicine has experienced thousands of years of cli

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… Hybrid flavan-chalcones, aromatase and lipoxygenase inhibitors, from Desmos cochinchinensis. Phytochemistry 72 (16), 2062–2067. 10.1016/j.phytochem.2011.07.002 Bao X. Y., Zheng. Q., Tong Q., Zhu P. C., Zhuang Z., Zheng G. Q., et al. (2018). … Blockade of nuclear factor-kappaB signaling pathway and anti-inflammatory activity of cardamomin, a chalcone analog from Alpinia conchigera. J. Pharmacol. Exp. Ther. 316 (1), 271–278. 10.1124/jpet.105.092486 Lee M. Y., Seo C. S., Lee J. A., Shin I. S., Kim S. J., Ha H., et al. (2012). …

Корреляция физико-химических свойств с антиоксидантной активностью в фенолах и тиофенолах.

Окисляющий стресс, связанный с чрезмерным производством реактивных видов кислорода и азота (ROS, RNS), способствует развитию и развитию многих заболеваний, таких, как старение, сердечно-сосудистые заболевания, болезнь Альцгеймера, болезнь Паркинсона, диабет, рак, предэклампсия или множественный склероз. В то время как фенолы и полифенолы являются наиболее изученными структурно схожими соединениями антиоксидантов, такими, как анилины или тиофенолины, периодически анализируются, несмотря на их радикальный потенциал сбора. В ходе этой работы проводится оценка воздействия структурных особенностей

Capsaicin: Current Understanding of Its Mechanisms and Therapy of Pain and Other Pre-Clinical and Clinical Uses.

In this review, we discuss the importance of capsaicin to the current understanding of neuronal modulation of pain and explore the mechanisms of capsaicin-induced pain. We will focus on the analgesic effects of capsaicin and its clinical applicability in treating pain. Furthermore, we will draw attention to the rationale for other clinical therapeutic uses and implications of capsaicin in diseases such as obesity, diabetes, cardiovascular conditions, cancer, airway diseases, itch, gastric, and urological disorders.

Pleiotropic Effects of Modified Citrus Pectin.

Modified citrus pectin (MCP) has a low-molecular-weight degree of esterification to allow absorption from the small intestinal epithelium into the circulation. MCP produces pleiotropic effects, including but not limited to its antagonism of galectin-3, which have shown benefit in preclinical and clinical models. Regarding cancer, MCP modulates several rate-limiting steps of the metastatic cascade. MCP can also affect cancer cell resistance to chemotherapy. Regarding fibrotic diseases, MCP modulates many of the steps involved in the pathogenesis of aortic stenosis. MCP also reduces fibrosis to

A Novel Hydroxamic Acid-Based Curcumin Derivative as Potent Histone Deacetylase Inhibitor for the Treatment of Glioblastoma.

Glioblastoma (GBM) is one of the most common primary and deadliest malignant brain tumor with chemoresistance and poor prognosis. There is a lack of effective chemotherapeutic drug for the treatment of GBM. In this work, we reported the preparation of a histone deacetylase (HDAC) inhibitor, DMC-HA, from the structural modification of natural product curcumin. DMC-HAs were tested in an HDAC inhibition assay and an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay for cytotoxicity. It showed potent inhibition of HDAC1-2 and HDAC6 with IC50 values in the submicromolar conce

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… Indeed, several natural products have been found to exhibit anticancer activities by affecting HDACs, like resveratrol, heliomycin chalcones, and curcumin ( 20 ). Curcumin is a polyphenol extracted from turmeric, which exhibits diverse and broad pharmacological activities ( 21 ). …

Exploration of the Use of Natural Compounds in Combination with Chemotherapy Drugs for Tumor Treatment.

Currently, chemotherapy is the main treatment for tumors, but there are still problems such as unsatisfactory chemotherapy results, susceptibility to drug resistance, and serious adverse effects. Natural compounds have numerous pharmacological activities which are important sources of drug discovery for tumor treatment. The combination of chemotherapeutic drugs and natural compounds is gradually becoming an important strategy and development direction for tumor treatment. In this paper, we described the role of natural compounds in combination with chemotherapeutic drugs in synergizing, reduci

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… Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance Eur. J. Med. Chem. 2019 180 350 366 10.1016/j.ejmech.2019.05.053 31325783 49. Sabatino M.A. Marabese M. Ganzinelli M. Caiola E. Geroni C. Broggini M. …

Exploring The Role of TOP2A in the Intersection of Pathogenic Mechanisms Between Rheumatoid Arthritis and Idiopathic Pulmonary Fibrosis Based on Bioinformatics.

BackgroundRheumatoid arthritis (RA) and idiopathic pulmonary fibrosis (IPF) share a common pathogenic mechanism, but the underlying mechanisms remain ambiguous. Our study aims at exploring the genetic-level pathogenic mechanism of these two diseases.MethodsWe carried out bioinformatics analysis on the GSE55235 and GSE213001 datasets. Machine learning was employed to identify candidate genes, which were further verified using the GSE92592 and GSE89408 datasets, as well as quantitative real-time PCR (qRT-PCR). The expression levels of TOP2A in RA and IPF in vitro models were confirmed using West

Identification and validation of CKAP2 as a novel biomarker in the development and progression of rheumatoid arthritis.

BACKGROUND: Rheumatoid arthritis (RA) is a common chronic joint disease. However, many patients exhibit inadequate responses to treatment due to disease heterogeneity. Identifying novel biomarkers for RA is crucial for advancing molecular diagnosis and identifying potential therapeutic targets. METHODS: Synovial tissue transcriptome data from RA patients and healthy controls were obtained from the GEO database. Differentially expressed gene (DEG) analysis, functional enrichment analysis, and weighted gene co-expression network analysis (WGCNA) identified key gene modules in RA. Machine learni