20 results on '"Atanasov, Atanas"'
Search Results
2. The germacranolide sesquiterpene lactone neurolenin B of the medicinal plant Neurolaena lobata (L.) R.Br. ex Cass inhibits NPM/ALK-driven cell expansion and NF-κB-driven tumour intravasation
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Unger, Christine, Kiss, Izabella, Vasas, Andrea, Lajter, Ildiko, Kramer, Nina, Atanasov, Atanas Georgiev, Nguyen, Chi Huu, Chatuphonprasert, Waranya, Brenner, Stefan, Krieger, Sigurd, McKinnon, Ruxandra, Peschel, Andrea, Kain, Renate, Saiko, Philipp, Szekeres, Thomas, Kenner, Lukas, Hassler, Melanie R., Diaz, Rene, Frisch, Richard, Dirsch, Verena M., Jager, Walter, de Martin, Rainer, Bochkov, Valery N., Passreiter, Claus M., Peter-Vorosmarty, Barbara, Mader, Robert M., Grusch, Michael, Dolznig, Helmut, Kopp, Brigitte, Zupko, Istvan, Hohmann, Judit, and Krupitza, Georg
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Lactones ,Lymphomas ,Medicine, Botanic ,Medicinal plants ,Medicine, Herbal ,Biological sciences ,Health ,Science and technology - Abstract
ABSTRACT Background: The t(2;5)(p23;q35) chromosomal translocation results in the expression of the fusion protein NPM/ALK that when expressed in T-lymphocytes gives rise to anaplastic large cell lymphomas (ALCL). In search [...]
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- 2015
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3. Editorial: Natural products based management of neurological disorders: Mechanistic insight and translational informatics approach.
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Kumar, Suresh, Gezici, Sevgi, Sekeroglu, Nazim, Atanasov, Atanas G., and Singla, Rajeev K.
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NEUROLOGICAL disorders ,NATURAL products ,PRODUCT management ,ALZHEIMER'S disease ,PARKINSON'S disease ,MEDICAL informatics - Published
- 2023
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4. Role of Diet and Nutrients in SARS-CoV-2 Infection: Incidence on Oxidative Stress, Inflammatory Status and Viral Production.
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Brahmi, Fatiha, Vejux, Anne, Ghzaiel, Imen, Ksila, Mohamed, Zarrouk, Amira, Ghrairi, Taoufik, Essadek, Soukena, Mandard, Stéphane, Leoni, Valerio, Poli, Giuseppe, Vervandier-Fasseur, Dominique, Kharoubi, Omar, El Midaoui, Adil, Atanasov, Atanas G., Meziane, Smail, Latruffe, Norbert, Nasser, Boubker, Bouhaouala-Zahar, Balkiss, Masmoudi-Kouki, Olfa, and Madani, Khodir
- Abstract
Coronavirus illness (COVID-19) is an infectious pathology generated by intense severe respiratory syndrome coronavirus 2 (SARS-CoV-2). This infectious disease has emerged in 2019. The COVID-19-associated pandemic has considerably affected the way of life and the economy in the world. It is consequently crucial to find solutions allowing remedying or alleviating the effects of this infectious disease. Natural products have been in perpetual application from immemorial time given that they are attested to be efficient towards several illnesses without major side effects. Various studies have shown that plant extracts or purified molecules have a promising inhibiting impact towards coronavirus. In addition, it is substantial to understand the characteristics, susceptibility and impact of diet on patients infected with COVID-19. In this review, we recapitulate the influence of extracts or pure molecules from medicinal plants on COVID-19. We approach the possibilities of plant treatment/co-treatment and feeding applied to COVID-19. We also show coronavirus susceptibility and complications associated with nutrient deficiencies and then discuss the major food groups efficient on COVID-19 pathogenesis. Then, we covered emerging technologies using plant-based SARS-CoV-2 vaccine. We conclude by giving nutrient and plants curative therapy recommendations which are of potential interest in the COVID-19 infection and could pave the way for pharmacological treatments or co-treatments of COVID-19. [ABSTRACT FROM AUTHOR]
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- 2022
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5. SYNTHESIS, ISOLATION AND BIOLOGICAL ACTIVITY STUDIES OF GALANTHAMINE DERIVATIVES INCLUDING PEPTIDE MOIETY AND TANNINS FROM MEDICINAL PLANTS.
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Atanasov, Atanas, Karadjova, Veronika, Andonova, Albena, Tsekova, Daniela, Lozanov, Valentin, Parashkevova, Boryana, Mindov, Ivan, Todorova, Roumiana, and Vezenkov, Lyubomir
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TANNINS , *MEDICINAL plants , *GALANTHAMINE , *PEPTIDE derivatives , *QUINCE , *BLOOD platelet aggregation - Abstract
The search of a new chemical substances influencing platelet aggregation is a very important endeavor for medical practice. Among the compounds that have antiaggregating activity are some peptides, tannins, etc. Here we present antiaggregation activity of Arg-Gly-Asp (RGD) peptide derivatives. Synthetic procedures of new peptide-galantamine derivatives including also glucose moiety designed to possess such activity are included. The in vitro effect of water extract from 20 tannins-containing plants from Bulgarian flora on aggregation of modified rat platelet-rich plasma was investigated and seven of them (Corylus avellana L, Cydonia oblonga Mill, Dryopteris filix-mas (L.) Schott, Ephedra distachya L., Geum urbanum L., Primula officinalis (L.) Hill and Punica granatum L.)were able to inhibit platelet aggregation. [ABSTRACT FROM AUTHOR]
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- 2022
6. Characterization of a Structural Leoligin Analog as Farnesoid X Receptor Agonist and Modulator of Cholesterol Transport#.
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Ladurner, Angela, Linder, Thomas, Wang, Limei, Hiebl, Verena, Schuster, Daniela, Schnürch, Michael, Mihovilovic, Marko D., Atanasov, Atanas G., and Dirsch, Verena M.
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CHOLESTEROL metabolism ,CARRIER proteins ,CELL receptors ,GENE expression ,MACROPHAGES ,MEDICINAL plants ,METABOLITES ,MOLECULAR structure ,PLANT extracts ,PEROXISOME proliferator-activated receptors - Abstract
The ligand-activated farnesoid X receptor is an emerging therapeutic target for the development of drugs against metabolic syndrome-related diseases. In this context, selective bile acid receptor modulators represent a novel concept for drug development. Selective bile acid receptor modulators act in a target gene- or tissue-specific way and are therefore considered less likely to elicit unwanted side effects. Based on leoligin, a lignan-type secondary plant metabolite from the alpine plant Leontopodium nivale ssp. alpinum , 168 synthesized structural analogs were screened in a farnesoid X receptor in silico pharmacophore-model. Fifty-six virtual hits were generated. These hits were tested in a cell-based farnesoid X receptor transactivation assay and yielded 7 farnesoid X receptor-activating compounds. The most active one being LT-141A, with an EC
50 of 6 µM and an Emax of 4.1-fold. This analog did not activate the G protein-coupled bile acid receptor, TGR5, and the metabolic nuclear receptors retinoid X receptor α , liver X receptors α / β , and peroxisome proliferator-activated receptors β / γ. Investigation of different farnesoid X receptor target genes characterized LT-141A as selective bile acid receptor modulators. Functional studies revealed that LT-141A increased cholesterol efflux from THP-1-derived macrophages via enhanced ATP-binding cassette transporter 1 expression. Moreover, cholesterol uptake in differentiated Caco-2 cells was significantly decreased upon LT-141A treatment. In conclusion, the leoligin analog LT-141A selectively activates the nuclear receptor farnesoid X receptor and has an influence on cholesterol transport in 2 model systems. [ABSTRACT FROM AUTHOR]- Published
- 2020
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7. Medicinal Plants and Natural Products Used in Cataract Management.
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Tewari, Devesh, Samoilă, Ovidiu, Gocan, Diana, Mocan, Andrei, Moldovan, Cadmiel, Devkota, Hari Prasad, Atanasov, Atanas G., Zengin, Gokhan, Echeverría, Javier, Vodnar, Dan, Szabo, Bianca, and Crişan, Gianina
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INTRAOCULAR lenses ,PLANT products ,NATURAL products ,MEDICINAL plants ,CATARACT ,TRADITIONAL medicine ,PLANTS - Abstract
Cataract is the leading reason of blindness worldwide and is defined by the presence of any lens opacities or loss of transparency. The most common symptoms of cataract are impaired vision, decreased contrast sensitivity, color disturbance, and glare. Oxidative stress is among the main mechanisms involved in the development of age-related cataract. Surgery through phacoemulsification and intraocular lens implantation is the most effective method for cataract treatment, however, there are chances of serious complications and irreversible loss of vision associated with the surgery. Natural compounds consisting of antioxidant or anti-inflammatory secondary metabolites can serve as potential leads for anticataract agents. In this review, we tried to document medicinal plants and plant-based natural products used for cataract treatment worldwide, which are gathered from available ethnopharmacological/ethnobotanical data. We have extensively explored a number of recognized databases like Scifinder, PubMed, Science Direct, Google Scholar, and Scopus by using keywords and phrases such as "cataract", "blindness", "traditional medicine", "ethnopharmacology", "ethnobotany", "herbs", "medicinal plants", or other relevant terms, and summarized the plants/phytoconstituents that are evaluated in different models of cataract and also tabulated 44 plants that are traditionally used in cataract in various folklore medical practices. Moreover, we also categorized the plants according to scientific studies carried out in different cataract models with their mechanisms of action. [ABSTRACT FROM AUTHOR]
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- 2019
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8. Polyacetylenes from Notopterygium incisum–New Selective Partial Agonists of Peroxisome Proliferator-Activated Receptor-Gamma
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Atanasov, Atanas, Blunder, Martina, Fakhrudin, Nanang, Liu, Xin, Noha, Stefan, Malainer, Clemens, Kramer, Matthias, Cocic, Amina, Kunert, Olaf, Schinkovitz, Andreas, Heiss, Elke, Schuster, Daniela, Dirsch, Verena, Bauer, Rudolf, University of Vienna [Vienna], Gadjah Mada University, University of Graz, Department of Pharmacology and Toxicology and Center for Molecular Biosciences Innsbruck (CMBI), Substances d'Origine Naturelle et Analogues Structuraux (SONAS), Université d'Angers (UA), and Karl-Franzens-Universität [Graz, Autriche]
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Transcriptional Activation ,Drugs and Devices ,Drug Research and Development ,[SDV]Life Sciences [q-bio] ,lcsh:Medicine ,Partial agonists ,Deoxyglucose ,Plasmid construction ,Biochemistry ,Intracellular Receptors ,Diynes ,Mice ,Medicinal plants ,Genes, Reporter ,3T3-L1 Cells ,Drug Discovery ,Molecular Cell Biology ,Adipocytes ,Animals ,Humans ,Insulin ,Luciferases ,Protein Interactions ,lcsh:Science ,Biology ,Adipogenesis ,Binding Sites ,Plant Extracts ,Adipocyte differentiation ,lcsh:R ,Polyynes ,Proteins ,Molecular Docking Simulation ,PPAR gamma ,Receptor binding assays ,HEK293 Cells ,Metabolism ,Small Molecules ,Medicine ,lcsh:Q ,Metabolic Pathways ,Fatty Alcohols ,Nuclear Receptor Signaling ,Luciferase ,Apiaceae ,Protein Binding ,Research Article ,Biotechnology ,Signal Transduction - Abstract
International audience; Peroxisome proliferator-activated receptor gamma (PPARγ) is a key regulator of glucose and lipid metabolism and therefore an important pharmacological target to combat metabolic diseases. Since the currently used full PPARγ agonists display serious side effects, identification of novel ligands, particularly partial agonists, is highly relevant. Searching for new active compounds, we investigated extracts of the underground parts ofNotopterygium incisum, a medicinal plant used in traditional Chinese medicine, and observed significant PPARγ activation using a PPARγ-driven luciferase reporter model. Activity-guided fractionation of the dichloromethane extract led to the isolation of six polyacetylenes, which displayed properties of selective partial PPARγ agonists in the luciferase reporter model. Since PPARγ activation by this class of compounds has so far not been reported, we have chosen the prototypical polyacetylene falcarindiol for further investigation. The effect of falcarindiol (10 µM) in the luciferase reporter model was blocked upon co-treatment with the PPARγ antagonist T0070907 (1 µM). Falcarindiol bound to the purified human PPARγ receptor with aKiof 3.07 µM.In silicodocking studies suggested a binding mode within the ligand binding site, where hydrogen bonds to Cys285 and Glu295 are predicted to be formed in addition to extensive hydrophobic interactions. Furthermore, falcarindiol further induced 3T3-L1 preadipocyte differentiation and enhanced the insulin-induced glucose uptake in differentiated 3T3-L1 adipocytes confirming effectiveness in cell models with endogenous PPARγ expression. In conclusion, we identified falcarindiol-type polyacetylenes as a novel class of natural partial PPARγ agonists, having potential to be further explored as pharmaceutical leads or dietary supplements.
- Published
- 2013
9. Ethnopharmacological Approaches for Therapy of Jaundice: Part I.
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Tewari, Devesh, Mocan, Andrei, Parvanov, Emil D., Sah, Archana N., Nabavi, Seyed M., Huminiecki, Lukasz, Zheng Feei Ma, Yeong Yeh Lee, Horbańczuk, Jarosław O., and Atanasov, Atanas G.
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JAUNDICE treatment ,ETHNOPHARMACOLOGY ,MEDICINAL plants - Abstract
Jaundice is a very common symptom especially in the developing countries. It is associated with several hepatic diseases which are still major causes of death. There are many different approaches to jaundice treatment and the growing number of ethnomedicinal studies shows the plant pharmacology as very promising direction. Many medicinal plants are used for the treatment of jaundice, however a comprehensive review on this subject has not been published. The use of medicinal plants in drug discovery is highly emphasized (based on their traditional and safe uses in different folk medicine systems from ancient times). Many sophisticated analytical techniques are emerging in the pharmaceutical field to validate and discover new biologically active chemical entities derived from plants. Here, we aim to classify and categorize medicinal plants relevant for the treatment of jaundice according to their origin, geographical location, and usage. Our search included various databases like Pubmed, ScienceDirect, Google Scholar. Keywords and phrases used for these searches included: "jaundice," "hyperbilirubinemia," "serum glutamate," "bilirubin," "Ayurveda." The first part of the review focuses on the variety of medicinal plant used for the treatment of jaundice (a total of 207medicinal plants). In the second part, possiblemechanisms of action of biologically active secondary metabolites of plants from five families for jaundice treatment are discussed. [ABSTRACT FROM AUTHOR]
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- 2017
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10. Discovery and resupply of pharmacologically active plant-derived natural products: A review.
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Atanasov, Atanas G., Waltenberger, Birgit, Pferschy-Wenzig, Eva-Maria, Linder, Thomas, Wawrosch, Christoph, Uhrin, Pavel, Temml, Veronika, Wang, Limei, Schwaiger, Stefan, Heiss, Elke H., Rollinger, Judith M., Schuster, Daniela, Breuss, Johannes M., Bochkov, Valery, Mihovilovic, Marko D., Kopp, Brigitte, Bauer, Rudolf, Dirsch, Verena M., and Stuppner, Hermann
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PLANT products , *MEDICINAL plants , *PHARMACEUTICAL industry , *HIGH throughput screening (Drug development) , *DRUG marketing - Abstract
Medicinal plants have historically proven their value as a source of molecules with therapeutic potential, and nowadays still represent an important pool for the identification of novel drug leads. In the past decades, pharmaceutical industry focused mainly on libraries of synthetic compounds as drug discovery source. They are comparably easy to produce and resupply, and demonstrate good compatibility with established high throughput screening (HTS) platforms. However, at the same time there has been a declining trend in the number of new drugs reaching the market, raising renewed scientific interest in drug discovery from natural sources, despite of its known challenges. In this survey, a brief outline of historical development is provided together with a comprehensive overview of used approaches and recent developments relevant to plant-derived natural product drug discovery. Associated challenges and major strengths of natural product-based drug discovery are critically discussed. A snapshot of the advanced plant-derived natural products that are currently in actively recruiting clinical trials is also presented. Importantly, the transition of a natural compound from a “screening hit” through a “drug lead” to a “marketed drug” is associated with increasingly challenging demands for compound amount, which often cannot be met by re-isolation from the respective plant sources. In this regard, existing alternatives for resupply are also discussed, including different biotechnology approaches and total organic synthesis. While the intrinsic complexity of natural product-based drug discovery necessitates highly integrated interdisciplinary approaches, the reviewed scientific developments, recent technological advances, and research trends clearly indicate that natural products will be among the most important sources of new drugs also in the future. [ABSTRACT FROM AUTHOR]
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- 2015
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11. Activity-guided isolation of NF-?B inhibitors and PPAR? agonists from the root bark of Lycium chinense Miller.
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Xie, Lian-Wu, Atanasov, Atanas G., Guo, De-An, Malainer, Clemens, Zhang, Jing-Xian, Zehl, Martin, Guan, Shu-Hong, Heiss, Elke H., Urban, Ernst, Dirsch, Verena M., and Kopp, Brigitte
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PROTEIN metabolism , *PHENOL analysis , *ALTERNATIVE medicine , *AMIDES , *ANTI-inflammatory agents , *BARK , *BIOLOGICAL models , *PHYSICAL & theoretical chemistry , *COMPARATIVE studies , *DOSE-effect relationship in pharmacology , *MASS spectrometry , *MEDICINAL plants , *NUCLEAR magnetic resonance spectroscopy , *PROTEINS , *PLANT roots , *TUMOR necrosis factors , *PHYTOCHEMICALS , *PLANT extracts , *IN vitro studies , *CHEMICAL inhibitors - Abstract
Abstract: Ethnopharmacological relevance: The root bark of Lycium chinense Miller, Lycii Radicis Cortex, has been used in traditional Chinese medicine (TCM) to treat different inflammation-related symptoms, such as diabetes mellitus. The pro-inflammatory transcription factor nuclear factor kappa B (NF-?B) is a key regulator of inflammation, while the transcription factor peroxisome proliferator-activated receptor gamma (PPAR?) is a key modulator of genes involved in diabetes development. To identify putative active compound(s) from Lycii Radicis Cortex inhibiting NF-?B or activating PPAR?. Material and methods: Using activity-guided fractionation, six extracts with different polarity, isolated fractions, and purified compounds from Lycii Radicis Cortex were tested for NF-?B inhibition and PPAR? activation in vitro. The structure of the purified compounds was elucidated by NMR and MS techniques. Results: The ethyl acetate extract and the methanol extract of Lycii Radicis Cortex suppressed tumor necrosis factor alpha (TNF-?)-induced activation of NF-?B, while the dichloromethane extract activated PPAR?. Nine phenolic amide analogues, including trans-N-(p-coumaroyl)tyramine (1), trans-N-feruloyltyramine (2), trans-N-caffeoyltyramine (3), dihydro-N-caffeoyltyramine (4), three neolignanamides (5–7), and two lignanamide (8, 9), were isolated and their inhibitory potential on NF-?B was determined (1–4 were also contained in water decoction). Two of the nine isolated phenolic amides inhibited TNF-?-induced NF-?B activation. Trans-N-caffeoyltyramine was verified as the key component responsible for the NF-?B inhibition with an IC50 of 18.4?M in our cell-based test system. Activation of PPAR? was attributed to a palmitic-acid enriched fraction which displayed concentration-dependent effect ablated upon co-treatment with the PPAR? antagonist T0070907. Conclusions: Phenolic amides were confirmed as main components from Lycii Radicis Cortex responsible for NF-?B inhibition. Fatty acids were identified as the major plant constituent responsible for the PPAR? activation. Structure-activity relationship analysis suggests that the NF-?B inhibitory activity of trans-N-caffeoyltyramine may be attributed to its Michael acceptor-type structure (?,?-unsaturated carbonyl group). The data of this study contribute to a better understanding of the molecular mechanism of action of Lycii Radicis Cortex extracts in the context of inflammation. [Copyright &y& Elsevier]
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- 2014
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12. Sanguiins—Promising Molecules with Broad Biological Potential.
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Gesek, Jakub, Jakimiuk, Katarzyna, Atanasov, Atanas G., and Tomczyk, Michał
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BIOMOLECULES ,MOLECULAR dynamics ,MOLECULAR docking ,SARS-CoV-2 ,ROSACEAE ,MEDICINAL plants - Abstract
Compounds of natural origin, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovering new medicines. In this review, we summarize the naturally occurring ellagitannins, sanguiins, which are bioactive constituents of various traditional medicinal plants, especially from the Rosaceae family. In-depth studies of sanguiin H-6 as an antimicrobial, antiviral, anticancer, anti-inflammatory, and osteoclastogenesis inhibitory agent have led to potent drug candidates. In addition, recently, virtual screening studies have suggested that sanguiin H-6 might increase resistance toward SARS-CoV-2 in the early stages of infection. Further experimental investigations on ADMET (absorption, distribution, metabolism, excretion, and toxicity) supplemented with molecular docking and molecular dynamics simulation are still needed to fully understand sanguiins' mechanism of action. In sum, sanguiins appear to be promising compounds for additional studies, especially for their application in therapies for a multitude of common and debilitating ailments. [ABSTRACT FROM AUTHOR]
- Published
- 2021
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13. Antiplatelet Aggregation Activity of a Fraction Isolated from Galega officinalis L.
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Todorov Atanasov, Atanas and Tchorbanov, Bojidar
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GALEGA ,PLANT extracts ,ANTICOAGULANTS ,BLOOD plasma ,BLOOD platelet aggregation ,THROMBIN ,MEDICINAL plants - Abstract
A fraction isolated from a crude aqueous extract of Galega officinalis L. and purified by column chromatography inhibit platelet aggregation in platelet-rich plasma. The active fraction of the extract, molecular weight of 100-140 kDa, appeared to be a polysaccharide-protein complex. Aggregation of platelets initiated by 25 µM ADP was inhibited 50 percent by 11.2 µg/ml of the fraction. Aggregation of platelets initiated by 100 µg/ml collagen and 0.8 U/ml thrombin was completely inhibited by 16 µg/ml and 18.3 µg/ml, respectively. [ABSTRACT FROM PUBLISHER]
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- 2002
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14. Walnut leaf extract inhibits PTP1B and enhances glucose-uptake in vitro.
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Pitschmann, Anna, Zehl, Martin, Atanasov, Atanas G., Dirsch, Verena M., Heiss, Elke, and Glasl, Sabine
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PROTEIN metabolism , *GLUCOSE metabolism , *ALTERNATIVE medicine , *ANIMAL experimentation , *BIOLOGICAL models , *FLAVONOIDS , *GAS chromatography , *HYPOGLYCEMIC agents , *LEAVES , *LIQUID chromatography , *MASS spectrometry , *MEDICINAL plants , *MICE , *PHENOLS , *WALNUT , *PHYTOCHEMICALS , *PLANT extracts , *DESCRIPTIVE statistics , *IN vitro studies , *PHARMACODYNAMICS - Abstract
Abstract: Ethnopharmacological relevance: Walnut, Juglans regia L. (Juglandaceae), is one of the medicinal plants used to treat diabetic symptoms in Austrian folk medicine. The air-dried green leaves are either used as aqueous decoctions or liquor preparations and are consumed on a daily basis. We investigated the hypoglycemic effect of a methanolic Juglans regia leaf extract on glucose uptake, protein tyrosine phosphatase 1B (PTP1B) inhibition and peroxisome proliferator-activated receptor gamma (PPARγ) activation. Material and methods: Hypoglycemic activity was assessed by glucose-uptake in C2C12 myocytes, inhibition of PTP1B and activation of PPARγ. Phytochemical characterization of the extract was carried out by LC–MS and GC–MS. Results: Methanolic Juglans regia leaf extract enhanced the glucose uptake rate in C2C12 myocytes at concentrations of 25µg/mL compared to untreated cells. This activity may partly be explained by the inhibition of PTP1B but not PPARγ agonism. LC–MS analyses revealed chlorogenic acid (1), 3-p-coumaroylquinic acid (2), a trihydroxynaphthalene-hexoside (3), as well as eight flavonoids (4–11) as main phenolic constituents in the active extract. Conclusions: The finding that Juglans regia leaf extract enhances glucose uptake and inhibits PTP1B provides an in vitro-based rationale for the traditional use of walnut leaf preparations against elevated blood-glucose levels. [Copyright &y& Elsevier]
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- 2014
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15. Characterization of a Structural Leoligin Analog as Farnesoid X Receptor Agonist and Modulator of Cholesterol Transport#.
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Ladurner, Angela, Linder, Thomas, Wang, Limei, Hiebl, Verena, Schuster, Daniela, Schnürch, Michael, Mihovilovic, Marko D., Atanasov, Atanas G., and Dirsch, Verena M.
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CHOLESTEROL metabolism , *CARRIER proteins , *CELL receptors , *GENE expression , *MACROPHAGES , *MEDICINAL plants , *METABOLITES , *MOLECULAR structure , *PLANT extracts , *PEROXISOME proliferator-activated receptors - Abstract
The ligand-activated farnesoid X receptor is an emerging therapeutic target for the development of drugs against metabolic syndrome-related diseases. In this context, selective bile acid receptor modulators represent a novel concept for drug development. Selective bile acid receptor modulators act in a target gene- or tissue-specific way and are therefore considered less likely to elicit unwanted side effects. Based on leoligin, a lignan-type secondary plant metabolite from the alpine plant Leontopodium nivale ssp. alpinum , 168 synthesized structural analogs were screened in a farnesoid X receptor in silico pharmacophore-model. Fifty-six virtual hits were generated. These hits were tested in a cell-based farnesoid X receptor transactivation assay and yielded 7 farnesoid X receptor-activating compounds. The most active one being LT-141A, with an EC50 of 6 µM and an Emax of 4.1-fold. This analog did not activate the G protein-coupled bile acid receptor, TGR5, and the metabolic nuclear receptors retinoid X receptor α , liver X receptors α / β , and peroxisome proliferator-activated receptors β / γ. Investigation of different farnesoid X receptor target genes characterized LT-141A as selective bile acid receptor modulators. Functional studies revealed that LT-141A increased cholesterol efflux from THP-1-derived macrophages via enhanced ATP-binding cassette transporter 1 expression. Moreover, cholesterol uptake in differentiated Caco-2 cells was significantly decreased upon LT-141A treatment. In conclusion, the leoligin analog LT-141A selectively activates the nuclear receptor farnesoid X receptor and has an influence on cholesterol transport in 2 model systems. [ABSTRACT FROM AUTHOR]
- Published
- 2020
- Full Text
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16. Lotus aegaeus (Gris.) Boiss and Iberis sempervirens L.: Chemical fingerprints, antioxidant potential, and inhibition activities and docking on key enzymes linked to global health problems.
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Mahomoodally, Mohamad Fawzi, Vlaisavljevic, Sanja, Berezni, Sanja, Abdallah, Hassan H., Zengin, Gokhan, Atanasov, Atanas G., Mollica, Adriano, Lobine, Devina, and Aktumsek, Abdurrahman
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NELUMBO , *ANTIOXIDANTS , *BIOLOGICAL products , *ETHYL acetate , *FLAVONOIDS - Abstract
Natural products are gaining much momentum worldwide because they have a broad spectrum of biological effects and present excellent opportunities for bioproducts development. With this fact, this study has been designed to investigate for the first time the effects of the ethyl acetate (EA), methanolic (MeOH), and water (W) extracts of Lotus aegaeus (La) and Iberis sempervirens (Is) on key enzymes as well as to quantify antioxidant capacities. The total phenolic and flavonoid content were determined using colorimetric methods and the individual phenolic compounds were assessed by LC–MS/MS analysis. Quercetin hexoside was the dominant compound in L. aegaeus , particularly in methanol extract, while the ethyl acetate and methanol extracts of I. sempervirens were characterized by the presence scopoletin and hinic acid. The antioxidant abilities of the investigated extracts were tested using different assays including free radical scavenging, reducing power, phosphomolybdenum, and metal chelating. All the extracts showed strong antioxidant abilities. For both species, the ethyl acetate extracts were more potent against cholinesterases and α-amylase, while the methanol extracts were most active against α-glucosidase. Only the water extract, followed by methanol of I. sempervirens exhibited notable inhibitory activity against tyrosinase. In addition, the dominant compounds were docked against tyrosinase and α-glucosidase to investigate their predicted binding affinity and interactions with the active site. In conclusion, L. aegaeus and I. sempervirens showed potent biological attributes, which advocates for further studies to explore their potential use as phytopharmaceuticals. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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17. Lobatin B inhibits NPM/ALK and NF-κB attenuating anaplastic-large-cell-lymphomagenesis and lymphendothelial tumour intravasation.
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Kiss, Izabella, Unger, Christine, Huu, Chi Nguyen, Atanasov, Atanas Georgiev, Kramer, Nina, Chatruphonprasert, Waranya, Brenner, Stefan, McKinnon, Ruxandra, Peschel, Andrea, Vasas, Andrea, Lajter, Ildiko, Kain, Renate, Saiko, Philipp, Szekeres, Thomas, Kenner, Lukas, Hassler, Melanie R., Diaz, Rene, Frisch, Richard, Dirsch, Verena M., and Jäger, Walter
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LYMPHOMAS , *ENDOTHELIAL cells , *ANAPLASTIC lymphoma kinase , *NUCLEOPHOSMIN , *MEDICINAL plants , *SESQUITERPENES - Abstract
An apolar extract of the traditional medicinal plant Neurolaena lobata inhibited the expression of the NPM/ALK chimera, which is causal for the majority of anaplastic large cell lymphomas (ALCLs). Therefore, an active principle of the extract, the furanoheliangolide sesquiterpene lactone lobatin B, was isolated and tested regarding the inhibition of ALCL expansion and tumour cell intravasation through the lymphendothelium. ALCL cell lines, HL-60 cells and PBMCs were treated with plant compounds and the ALK inhibitor TAE-684 to measure mitochondrial activity, proliferation and cell cycle progression and to correlate the results with protein- and mRNA-expression of selected gene products. Several endpoints indicative for cell death were analysed after lobatin B treatment. Tumour cell intravasation through lymphendothelial monolayers was measured and potential causal mechanisms were investigated analysing NF-κB- and cytochrome P450 activity, and 12(S)-HETE production. Lobatin B inhibited the expression of NPM/ALK, JunB and PDGF-Rβ, and attenuated proliferation of ALCL cells by arresting them in late M phase. Mitochondrial activity remained largely unaffected upon lobatin B treatment. Nevertheless, caspase 3 became activated in ALCL cells. Also HL-60 cell proliferation was attenuated whereas PBMCs of healthy donors were not affected by lobatin B. Additionally, tumour cell intravasation, which partly depends on NF-κB, was significantly suppressed by lobatin B most likely due to its NF-κB-inhibitory property. Lobatin B, which was isolated from a plant used in ethnomedicine, targets malignant cells by at least two properties: I) inhibition of NPM/ALK, thereby providing high specificity in combating this most prevalent fusion protein occurring in ALCL; II) inhibition of NF-κB, thereby not affecting normal cells with low constitutive NF-κB activity. This property also inhibits tumour cell intravasation into the lymphatic system and may provide an option to manage this early step of metastatic progression. [ABSTRACT FROM AUTHOR]
- Published
- 2015
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18. Screening of Vietnamese medicinal plants for NF-κB signaling inhibitors: Assessing the activity of flavonoids from the stem bark of Oroxylum indicum.
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Tran, Thi Van Anh, Malainer, Clemens, Schwaiger, Stefan, Hung, Tran, Atanasov, Atanas G., Heiss, Elke H., Dirsch, Verena M., and Stuppner, Hermann
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MEDICINAL plants , *ALTERNATIVE medicine , *ANTI-inflammatory agents , *BARK , *BIOLOGICAL models , *CHROMATOGRAPHIC analysis , *CONFIDENCE intervals , *DOSE-effect relationship in pharmacology , *FLAVONOIDS , *GLYCOSIDES , *LEAVES , *SPECTRUM analysis , *PLANT stems , *DNA-binding proteins , *PHYTOCHEMICALS , *PLANT extracts , *DESCRIPTIVE statistics , *IN vitro studies , *CHEMICAL inhibitors , *PHARMACODYNAMICS - Abstract
Ethnopharmacological relevance Seventeen plants used in Vietnamese traditional medicine for the treatment of inflammatory disorders were screened for NF-κB inhibitory activity. Oroxylum indicum , which exhibited activity, was investigated in detail. Materials and methods Forty plant extracts from 17 species were prepared by maceration using dichloromethane and methanol and were tested (10 µg/mL) to evaluate their ability to inhibit NF-κB activation using TNF-α-stimulated HEK-293 cells stably transfected with a NF-κB-driven luciferase reporter. The active extract of Oroxylum indicum was subsequently fractionated by different chromatographic techniques. After isolation, all single compounds were identified by spectroscopic methods and assessed for NF-κB inhibitory effects. Results The dichloromethane extracts obtained from Chromolaena odorata leaves and the stem bark of Oroxylum indicum showed distinct inhibitory effects on NF-κB activation at a concentration of 10 µg/mL. The active extract of Oroxylum indicum was subjected to further phytochemical studies resulting in identification of four flavonoid aglyca and six flavonoid glycosides. Pharmacological evaluation of the obtained compounds identified oroxylin A as the most active substance (IC 50 =3.9 µM, 95% CI: 3.5–4.4 µM), while chrysin and hispidulin showed lower activity with IC 50 =7.2 µM (95% CI: 6.0–8.8 µM) and 9.0 µM (95% CI: 7.9–10.2 µM), respectively. Interestingly, in this study the activity of baicalein (IC 50 =28.1 µM, 95% CI: 24.6–32.0 µM) was weak. The isolated glycosides showed no inhibitory activity when tested at a concentration of 30 µM. Quantification of the four active flavonoids in extracts and plant materials suggested that oroxylin A contributes to the NF-κB inhibitory activity of the stem barks of Oroxylum indicum to a greater extent than baicalein which was thought to be responsible for the anti-inflammatory activity of this plant. Conclusions The screening presented in this study identified the dichloromethane extracts of Chromolaena odorata and Oroxylum indicum as promising sources for NF-κB inhibitors. Hispidulin, baicalein, chrysin and oroxylin A, isolated from Oroxylum indicum , were identified as inhibitors of NF- κB activation. [ABSTRACT FROM AUTHOR]
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- 2015
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19. Ethnopharmacological in vitro studies on Austria's folk medicine—An unexplored lore in vitro anti-inflammatory activities of 71 Austrian traditional herbal drugs.
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Vogl, Sylvia, Picker, Paolo, Mihaly-Bison, Judit, Fakhrudin, Nanang, Atanasov, Atanas G., Heiss, Elke H., Wawrosch, Christoph, Reznicek, Gottfried, Dirsch, Verena M., Saukel, Johannes, and Kopp, Brigitte
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ANTI-inflammatory agents , *ENDOTHELIUM physiology , *ALTERNATIVE medicine , *BIOLOGICAL assay , *BIOLOGICAL models , *COMPARATIVE studies , *DATABASES , *INTERLEUKINS , *MEDICINAL plants , *TRADITIONAL medicine , *TUMOR necrosis factors , *DESCRIPTIVE statistics , *IN vitro studies ,THERAPEUTIC use of plant extracts - Abstract
Abstract: Ethnopharmacological relevance: In Austria, like in most Western countries, knowledge about traditional medicinal plants is becoming scarce. Searching the literature concerning Austria's ethnomedicine reveals its scant scientific exploration. Aiming to substantiate the potential of medicinal plants traditionally used in Austria, 63 plant species or genera with claimed anti-inflammatory properties listed in the VOLKSMED database were assessed for their in vitro anti-inflammatory activity. Material and methods: 71 herbal drugs from 63 plant species or genera were extracted using solvents of varying polarities and subsequently depleted from the bulk constituents, chlorophylls and tannins to avoid possible interferences with the assays. The obtained 257 extracts were assessed for their in vitro anti-inflammatory activity. The expression of the inflammatory mediators E-selectin and interleukin-8 (IL-8), induced by the inflammatory stimuli tumor necrosis factor alpha (TNF-α) and the bacterial product lipopolysaccharide (LPS) was measured in endothelial cells. The potential of the extracts to activate the nuclear factors PPARα and PPARγ and to inhibit TNF-α-induced activation of the nuclear factor-kappa B (NF-κB) in HEK293 cells was determined by luciferase reporter gene assays. Results: In total, extracts from 67 of the 71 assessed herbal drugs revealed anti-inflammatory activity in the applied in vitro test systems. Thereby, 30 could downregulate E-selectin or IL-8 gene expression, 28 were strong activators of PPARα or PPARγ (inducing activation of more than 2-fold at a concentration of 10µg/mL) and 21 evoked a strong inhibition of NF-κB (inhibition of more than 80% at 10µg/mL). Conclusion: Our research supports the efficacy of herbal drugs reported in Austrian folk medicine used for ailments associated with inflammatory processes. Hence, an ethnopharmacological screening approach is a useful tool for the discovery of new drug leads. [Copyright &y& Elsevier]
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- 2013
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20. The ethnopharmacological literature: An analysis of the scientific landscape.
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Yeung, Andy Wai Kan, Heinrich, Michael, Kijjoa, Anake, Tzvetkov, Nikolay T., and Atanasov, Atanas G.
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BIBLIOMETRICS , *BIOLOGICAL products , *COMPUTER software , *MEDICINAL plants , *MEDICAL research , *PHARMACOLOGY , *SEMANTICS , *SERIAL publications , *TRADITIONAL medicine , *SYSTEMATIC reviews , *CITATION analysis - Abstract
The research into bioactive natural products originating from medicinal plants, fungi and other organisms has a long history, accumulating abundant and diverse publications. However no quantitative literature analysis has been conducted so far. Here we analyze the bibliometric data of ethnopharmacology literature and relate the semantic content to the publication and citation data so that the major research themes, contributors, and journals of different time periods could be identified and evaluated. Web of Science (WoS) was searched to identify relevant publications. The Analyze function of WoS and bibliometric software (VOSviewer) were utilized to perform the analyses. Until the end of November 2018, 59,576 publications -linked to 'ethnopharmacology' indexed by WoS, published since 1958 in more than 5600 journals, and contributed by over 20,600 institutions located in more than 200 countries/regions, were identified. The papers were published under four dominating WoS categories, namely pharmacology/pharmacy (34.4%), plant sciences (28.6%), medicinal chemistry (25.3%), and integrative complementary medicine (20.6%). India (14.6%) and China (13.2%) were dominating the publication space. The United States and Brazil also had more than 8.0% contribution each. The rest of the top ten countries/regions were mainly from Asia. There were around ten-fold more original articles (84.6%) than reviews (8.4%). Ethnopharmacological research has a consistent focus on food and plant sciences, (bio)chemistry, complementary medicine and pharmacology, with a more limited scientific acceptance in the socio-cultural sciences. Dynamic global contributions have been shifting from developed countries to economically and scientifically emerging countries in Asia, South America and the Middle East. Research on recording medicinal plant species used by traditional medicine continues, but the evaluation of specific properties or treatment effects of extracts and compounds has increased enormously. Moreover increasing attention is paid to some widely distributed natural products, such as curcumin, quercetin, and rutin. Image 1 [ABSTRACT FROM AUTHOR]
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- 2020
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