المؤلفون: Din, Shajrath, Hamid, Saima, Yaseen, Aadil, Yatoo, Ali Mohd, Ali, Shafat, Shamim, Kashif, Mahdi, Wael A., Alshehri, Sultan, Rehman, Muneeb U., Shah, Wajaht A.

المصدر: Plants (2223-7747); Dec2022, Vol. 11 Issue 24, p3588, 16p

مصطلحات موضوعية: FLAVONOIDS, METABOLITES, PLANT metabolites, NARINGENIN, LACTATE dehydrogenase, ALKALOIDS, PLANT polyphenols, PHYTOCHEMICALS, GLYCOSIDES

مستخلص: Despite its limited exploration, Nymphaea mexicana Zucc. can be beneficial if pharmacology, isolation, and biological evaluation are given attention. It is an aquatic species that belongs to the family Nymphaeaceae. The thrust area of the work was the extraction, isolation, and biological evaluation of different extracts of the N. mexicana Zucc. plant. The primary goal of this research was to assess the antimicrobial, antioxidant, and anticancer activities of the extracts and to isolate the target naringenin compound. Comparative FT IR analysis of different extracts of this plant revealed the presence of functional groups of plant secondary metabolites, including polyphenols, flavonoids, terpenoids, esters, amines, glycosides, alkanes, alkaloids, fatty acids, and alcohols. Moderate free radical scavenging potential has been achieved for the various extracts via reducing power and DPPH assays. While cytotoxic activity was evaluated by colorimetric and lactate dehydrogenase cell viability tests on potent cancer cell lines. Lung adenocarcinoma epithelial cells (A-549), and breast cells (MC-7) were treated with MeOH extract. The antimicrobial activity against bacterial strains was evaluated using Gram-positive and -negative cultures, where maximum and minimum inhibition zones were recorded for different strains, including 1.6–25.6 μg/mL for Streptococcus aureus, using the agar well diffusion method. In addition, the anti-inflammatory activity of different extracts of N. mexicana Zucc. was evaluated in a nitrite radical scavenging assay with high concentrations of secondary metabolites, which are important against human pathogens and other diseases. [ABSTRACT FROM AUTHOR]

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المؤلفون: Karel Šmejkal, Kiavash Hushmandi, Milad Ashrafizadeh, Sandra Mersakova, Mehdi Shakibaei, Sepideh Mirzaei, Aranka Brockmueller, Peter Kubatka, Martin Péč, Luciano Saso, Lenka Koklesova, Alena Liskova, Jan Strnadel, Marek Samec, Kevin Zhai, Karol Kajo, Dietrich Büsselberg

المصدر: Cancers, Vol 13, Iss 130, p 130 (2021)
Cancers

مصطلحات موضوعية: 0301 basic medicine, Cancer Research, Pyruvate dehydrogenase kinase, Review, PKM2, lcsh:RC254-282, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Lactate dehydrogenase, cancer, Glycolysis, Tumor hypoxia, HIF-1, lcsh:Neoplasms. Tumors. Oncology. Including cancer and carcinogens, Warburg effect, 3. Good health, 030104 developmental biology, Oncology, chemistry, 030220 oncology & carcinogenesis, Cancer cell, flavonoids, Cancer research, flavonoids, pharmacology, pharmacology, Pyruvate kinase

الوصف: Simple Summary This comprehensive review discusses the anticancer effects of plant phenolic compounds, known as flavonoids, through the targeting of HIF-1 and critical enzymes contributing to the Warburg effect. Connections between HIF-1 and metabolic reprogramming seem to play a crucial role in cancer progression. The core of presented paper summarizes the current knowledge about the in vitro and in vivo efficacy of flavonoids against aerobic glycolysis and HIF-1 activity. Despite the lack of clinical evidence, we emphasize the possibility of introducing flavonoids (targeting HIF-1) to the clinical research considering predictive, preventive, and/or personalized medical approach. Abstract Tumor hypoxia is described as an oxygen deprivation in malignant tissue. The hypoxic condition is a consequence of an imbalance between rapidly proliferating cells and a vascularization that leads to lower oxygen levels in tumors. Hypoxia-inducible factor 1 (HIF-1) is an essential transcription factor contributing to the regulation of hypoxia-associated genes. Some of these genes modulate molecular cascades associated with the Warburg effect and its accompanying pathways and, therefore, represent promising targets for cancer treatment. Current progress in the development of therapeutic approaches brings several promising inhibitors of HIF-1. Flavonoids, widely occurring in various plants, exert a broad spectrum of beneficial effects on human health, and are potentially powerful therapeutic tools against cancer. Recent evidences identified numerous natural flavonoids and their derivatives as inhibitors of HIF-1, associated with the regulation of critical glycolytic components in cancer cells, including pyruvate kinase M2(PKM2), lactate dehydrogenase (LDHA), glucose transporters (GLUTs), hexokinase II (HKII), phosphofructokinase-1 (PFK-1), and pyruvate dehydrogenase kinase (PDK). Here, we discuss the results of most recent studies evaluating the impact of flavonoids on HIF-1 accompanied by the regulation of critical enzymes contributing to the Warburg phenotype. Besides, flavonoid effects on glucose metabolism via regulation of HIF-1 activity represent a promising avenue in cancer-related research. At the same time, only more-in depth investigations can further elucidate the mechanistic and clinical connections between HIF-1 and cancer metabolism.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ac8d02358d55a9f3ffcc02480bc8b0bTest
http://hdl.handle.net/11573/1472439Test

المؤلفون: Matthieu Dallons, Manuel Podrecca, Jean-Marie Colet, Manon Delcourt, Corentin Schepkens

المصدر: Biology
Volume 9
Issue 5
Biology, Vol 9, Iss 98, p 98 (2020)

مصطلحات موضوعية: 0301 basic medicine, Taurine, 030204 cardiovascular system & hematology, Biology, Pharmacology, Creatine, QT interval, General Biochemistry, Genetics and Molecular Biology, Article, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Clarithromycin, Lactate dehydrogenase, medicine, metabonomics, lcsh:QH301-705.5, Creatinine, Cardiotoxicity, General Immunology and Microbiology, isoproterenol, 1H-NMR, clarithromycin, urine, 030104 developmental biology, chemistry, lcsh:Biology (General), Toxicity, biomarker, General Agricultural and Biological Sciences, medicine.drug

الوصف: Cardiotoxicity remains a challenging concern both in drug development and in the management of various clinical situations. There are a lot of examples of drugs withdrawn from the market or stopped during clinical trials due to unpredicted cardiac adverse events. Obviously, current conventional methods for cardiotoxicity assessment suffer from a lack of predictivity and sensitivity. Therefore, there is a need for developing new tools to better identify and characterize any cardiotoxicity that can occur during the pre-clinical and clinical phases of drug development as well as after marketing in exposed patients. In this study, isoproterenol and clarithromycin were used as prototypical cardiotoxic agents in rats in order to evaluate potential biomarkers of heart toxicity at very early stages using 1H-NMR-based metabonomics. While isoproterenol is known to cause heart necrosis, clarithromycin may induce QT interval prolongation. Heart necrosis and QT prolongation were validated by histological analysis, serum measurement of lactate dehydrogenase/creatine phosphate kinase and QTc measurement by electrocardiogram (ECG). Urine samples were collected before and repeatedly during daily exposure to the drugs for 1H-NMR based-metabonomics investigations. Specific metabolic signatures, characteristic of each tested drug, were obtained from which potential predictive biomarkers for drug-induced heart necrosis and drug-induced QT prolongation were retrieved. Isoproterenol-induced heart necrosis was characterized by higher levels of taurine, creatine, glucose and by lower levels of Krebs cycle intermediates, creatinine, betaine/trimethylamine N-oxide (TMAO), dimethylamine (DMA)/sarcosine. Clarithromycin-induced QT prolongation was characterized by higher levels of creatinine, taurine, betaine/TMAO and DMA/sarcosine and by lower levels of Krebs cycle intermediates, glucose and hippurate.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fecfd7212c3b3950c5486730c7c68f7fTest
http://europepmc.org/articles/PMC7284797Test

المؤلفون: Byung-Yong Park, Weishun Tian, Jing Zhao, Rashedunnabi Akanda, Jeong-Hwi Cho, Jeong-Ho Lee, Yu-Jin Choi, Sang-Ki Kim

المصدر: Antioxidants
Antioxidants, Vol 9, Iss 1, p 27 (2019)
Volume 9
Issue 1

مصطلحات موضوعية: 0301 basic medicine, immobilization stress, Antioxidant, Physiology, medicine.medical_treatment, H2O2, Clinical Biochemistry, cornus officinalis, Pharmacology, medicine.disease_cause, Biochemistry, Neuroprotection, Article, Superoxide dismutase, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Lactate dehydrogenase, medicine, oxidative stress, Molecular Biology, chemistry.chemical_classification, Reactive oxygen species, biology, Chemistry, lcsh:RM1-950, Neurotoxicity, MAPK pathway, Cell Biology, Cornus officinalis, medicine.disease, h2o2, 030104 developmental biology, lcsh:Therapeutics. Pharmacology, Catalase, biology.protein, 030217 neurology & neurosurgery, Oxidative stress

الوصف: Oxidative stress plays a vital role in neurodegenerative diseases. Cornus officinalis (CC) has a wide range of pharmacological activities (e.g., antioxidant, neuroprotective, and anti-inflammatory). The present study was undertaken to elucidate the neuroprotective mechanism of CC and fermented CC (FCC) on stress and H2O2-induced oxidative stress damage in rats and SH-SY5Y cells. A dose of 100 mg/kg CC or FCC was orally administered to rats 1 h prior to immobilization 2 h per day for 14 days. CC, especially FCC administration decreased immobility time in forced swim test (FST), effectively alleviated the oxidative stress, and remarkably decreased corticosterone, &beta
endorphin and increased serotonin levels, respectively. In cells, CC and FCC significantly inhibited reactive oxygen species (ROS) generation, lactate dehydrogenase (LDH) release and significantly increased the genes expression of antioxidant and neuronal markers, such as superoxide dismutase (SOD), catalase (CAT), and brain-derived neurotrophic factor (BDNF). Moreover, the pro-apoptotic factor Bax and anti-apoptotic factor Bcl-2 (Bax/Bcl-2) ratio was regulated by CC and FCC pretreatment. Both in rats and cells, CC and FCC downregulated mitogen-activated protein kinase (MAPK) phosphorylation. Taken together, these results demonstrated that CC and particularly FCC ameliorated oxidative stress and may be used on the neuroprotection.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec3d6fcf6bfac23920276642c6ac5cc9Test
http://europepmc.org/articles/PMC7023136Test

المؤلفون: Mohamed Abdo Nassan, Khaled Ben Issa, Abdelkarim Sasi, Adil Aldhahrani, Gamal A. Salem, Yasmina M. Abd-Elhakim, Amany Abdel-Rahman Mohamed

المصدر: Toxins
Toxins, Vol 11, Iss 11, p 642 (2019)
Volume 11
Issue 11

مصطلحات موضوعية: Male, Cell Survival, Health, Toxicology and Mutagenesis, Aspartate transaminase, lcsh:Medicine, Pharmacology, Toxicology, Creatine, anticancer, Kidney, Article, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Euphorbia peplus, In vivo, Euphorbia, Lactate dehydrogenase, medicine, Animals, Computer Simulation, Rats, Wistar, Linolenate, 030304 developmental biology, 0303 health sciences, Creatinine, biology, euphorbia peplus, Plant Extracts, Myocardium, lcsh:R, apoptosis, di-(2-ethylhexyl) phthalate, MDM2-p53, Heart, Proto-Oncogene Proteins c-mdm2, Rats, Molecular Docking Simulation, medicine.anatomical_structure, chemistry, 030220 oncology & carcinogenesis, biology.protein, Creatine kinase, Tumor Suppressor Protein p53, Biomarkers

الوصف: This study explored the probable in vivo cardiac and renal toxicities together with in silico approaches for predicting the apoptogenic potential of Euphorbia peplus methanolic extract (EPME) in rats. Cardiac and renal injury biomarkers were estimated with histopathological and immunohistochemical evaluations of both kidney and heart. The probable underlying mechanism of E. peplus compounds to potentiate p53 activity is examined using Molecular Operating Environment (MOE) docking software and validated experimentally by immunohistochemical localization of p53 protein in the kidney and heart tissues. The gas chromatography/mass spectrometry analysis of E. peplus revealed the presence of nine different compounds dominated by di-(2-ethylhexyl) phthalate (DEHP). Significant elevations of troponin, creatine phosphokinase, creatine kinase&ndash
myocardium bound, lactate dehydrogenase, aspartate transaminase, alkaline phosphatase, urea, creatinine, and uric acid were evident in the EPME treated rats. The EPME treated rats showed strong renal and cardiac p53 expression and moderate cardiac TNF-&alpha
expression. Further, our in silico results predicted the higher affinity and good inhibition of DEHP, glyceryl linolenate, and lucenin 2 to the MDM2-p53 interface compared to the standard reference 15 a compound. Conclusively, EPME long-term exposure could adversely affect the cardiac and renal tissues probably due to their inflammatory and apoptotic activity. Moreover, the in silico study hypothesizes that EPME inhibits MDM2-mediated degradation of p53 suggesting possible anticancer potentials which confirmed experimental by strong p53 expression in renal and cardiac tissues.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3eba02fc325f735540460f0919dbf9b5Test
http://europepmc.org/articles/PMC6891376Test

المؤلفون: Claudio Ferrante

المصدر: Proceedings of 5th International Electronic Conference on Medicinal Chemistry.

مصطلحات موضوعية: Neurotoxicity, Biology, Pharmacology, medicine.disease, biology.organism_classification, Neuroprotection, Parthenium, chemistry.chemical_compound, Nutraceutical, chemistry, Phytochemical, Lactate dehydrogenase, Tanacetum parthenium, medicine, Gallic acid

الوصف: Migraine is one of the most common neurological disorder, which has long been related to brain serotonin (5-HT) depletion and neuro-inflammation. Despite many treatment options are available, the frequent occurrence of unacceptable adverse effects further supports the research toward nutraceuticals and herbal preparations, among which Tanacetum parthenium and Salix alba showed promising anti-inflammatory and neuro-modulatory activities. The impact of extract treatment on astrocyte viability, spontaneous migration and apoptosis was evaluated. Anti-inflammatory/anti-oxidant effects were investigated on isolated rat cortexes exposed to a neurotoxic stimulus. The lactate dehydrogenase (LDH) release, nitrite levels and 5-HT turnover were evaluated, as well. A proteomic analysis was focused on specific neuronal proteins and a fingerprint analysis was carried out on selected phenolic compounds. Both extracts appeared able to exert in vitro anti-oxidant and anti-apoptotic effects. S. alba and T. parthenium extracts reduced LDH release, nitrite levels and 5-HT turnover induced by neurotoxicity stimulus. The downregulation of selected proteins suggest a neurotoxic, which could be ascribed to an elevate content of gallic acid in both S. alba and T. parthenium extracts. Concluding, both extracts exert neuroprotective effects, although the downregulation of key proteins involved in neuron physiology suggest caution in their use as food supplements.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_________::56b16399a9263a7975730511f5a08c34Test
https://doi.org/10.3390/ecmc2019-06282Test

المؤلفون: Satyan Lakshminrusimha, Sara K. Berkelhamer, Maciej L. Goniewicz, Sylvia F. Gugino, Noel J. Leigh, Justin Helman

المصدر: International Journal of Environmental Research and Public Health
International Journal of Environmental Research and Public Health, Vol 16, Iss 19, p 3635 (2019)
International journal of environmental research and public health, vol 16, iss 19
Volume 16
Issue 19

مصطلحات موضوعية: Health, Toxicology and Mutagenesis, lcsh:Medicine, Pharmacology, Electronic Nicotine Delivery Systems, Toxicology, Fetal Development, chemistry.chemical_compound, 0302 clinical medicine, Smooth Muscle, 2.2 Factors relating to the physical environment, immature lung, 030212 general & internal medicine, Aetiology, Lung, Pediatric, 0303 health sciences, Chemistry, food and beverages, electronic cigarette flavorings, Menthol, medicine.anatomical_structure, electronic cigarettes, Toxicity, Respiratory, Programmed cell death, Myocytes, Smooth Muscle, In Vitro Techniques, Pulmonary Artery, Article, 03 medical and health sciences, Lactate dehydrogenase, medicine.artery, Tobacco, Toxicity Tests, medicine, Animals, 030304 developmental biology, lung development, Fetus, Myocytes, Sheep, Tobacco Smoke and Health, lcsh:R, Public Health, Environmental and Occupational Health, toxicity, Newborn, In vitro, Flavoring Agents, Good Health and Well Being, Animals, Newborn, Pulmonary artery

الوصف: Background: The developing lung is uniquely susceptible and may be at increased risk of injury with exposure to e-cigarette constituents. We hypothesize that cellular toxicity and airway and vascular responses with exposure to flavored refill solutions may be altered in the immature lung. Methods: Fetal, neonatal, and adult ovine pulmonary artery smooth muscle cells (PASMC) were exposed to popular flavored nicotine-free e-cigarette refill solutions (menthol, strawberry, tobacco, and vanilla) and unflavored solvents: propylene glycol (PG) or vegetable glycerin (VG). Viability was assessed by lactate dehydrogenase assay. Brochodilation and vasoreactivity were determined on isolated ovine bronchial rings (BR) and pulmonary arteries (PA). Results: Neither PG or VG impacted viability of immature or adult cells
however, exposure to menthol and strawberry flavored solutions increased cell death. Neonatal cells were uniquely susceptible to menthol flavoring-induced toxicity, and all four flavorings demonstrated lower lethal doses (LD50) in immature PASMC. Exposure to flavored solutions induced bronchodilation of neonatal BR, while only menthol induced airway relaxation in adults. In contrast, PG/VG and flavored solutions did not impact vasoreactivity with the exception of menthol-induced relaxation of adult PAs. Conclusion: The immature lung is uniquely susceptible to cellular toxicity and altered airway responses with exposure to common flavored e-cigarette solutions.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07bb69c7e7531dac6fde3b4d7be3a865Test
http://europepmc.org/articles/PMC6801380Test

المؤلفون: Kong Xiaojun, Ya-Jun Yang, Qin Zhe, Ning Ma, Jianyong Li, Dong-Shuai Shen, Jiao Zenghua, Li Shihong, Liu Xiwang

المصدر: Molecules
Molecules, Vol 24, Iss 13, p 2380 (2019)
Volume 24
Issue 13

مصطلحات موضوعية: Platelet Aggregation, Blood viscosity, Pharmaceutical Science, Prostaglandin, UPLC-Q-TOF/MS, Blood stasis, Pharmacology, Article, Analytical Chemistry, lcsh:QD241-441, 03 medical and health sciences, chemistry.chemical_compound, Thromboxane A2, 0302 clinical medicine, lcsh:Organic chemistry, Lactate dehydrogenase, Drug Discovery, Eugenol, medicine, Animals, Platelet, Physical and Theoretical Chemistry, AEE, Blood Coagulation, Chromatography, High Pressure Liquid, 030304 developmental biology, chemistry.chemical_classification, 0303 health sciences, Aspirin, Organic Chemistry, Fatty acid, Blood Viscosity, metabolomics, Epoprostenol, Hematologic Diseases, Rats, Disease Models, Animal, blood stasis, Blood, chemistry, Chemistry (miscellaneous), 030220 oncology & carcinogenesis, Molecular Medicine, Female, Blood Chemical Analysis, medicine.drug

الوصف: Aspirin eugenol ester (AEE) is a novel compound that is formed from the esterification of aspirin (acetylsalicylic acid (ASA)) and eugenol. This study aimed to investigate the effects of AEE on blood stasis in rats and to characterize the underlying mechanisms using a plasma metabolomic study. The results indicate that AEE and ASA could modulate whole blood viscosity (WBV), plasma viscosity (PV), blood coagulation parameters, platelet count, platelet aggregation, lactate dehydrogenase (LDH), creatinine (CR) and the levels of thromboxane A2 (TXA2) and 6-keto prostaglandin F1&alpha
(6-keto-PGF1&alpha
). The metabolic profiles of the plasma samples from all groups were clearly separated in the score plots. Nineteen potential metabolites were selected and identified, and disordered levels of these metabolites could be regulated by AEE and ASA. Pathway analysis showed that the mechanism of action of AEE on blood stasis might be principally related to the metabolism of amino acid, fatty acid, energy and glycerophospholipid. The above results indicate that AEE protected the rats against blood stasis, and that this effect might have been caused by the anticoagulation activity of AEE and its abilities to maintain a balance between TXA2 and PGI2, reduce blood viscosity, inhibit platelet aggregation and normalize the plasma metabolic profile.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea7f7b301927d4e986395d79104b227eTest
http://europepmc.org/articles/PMC6651160Test

المؤلفون: Jeffrey Pradeep Raj, Pavani Nathala, Sajid Melvin George, Anantha R Vellipuram, Prashanth Rawla

المصدر: Diseases
Diseases, Vol 7, Iss 2, p 38 (2019)

مصطلحات موضوعية: entresto, adverse drug reaction, lcsh:Medicine, Case Report, 030204 cardiovascular system & hematology, Pharmacology, Sacubitril, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Lactate dehydrogenase, Medicine, Adverse effect, biology, business.industry, lcsh:R, medicine.disease, Valsartan, chemistry, sacubitril/valsartan, biology.protein, rhabdomyolysis, Creatine kinase, business, Rhabdomyolysis, 030217 neurology & neurosurgery, Adverse drug reaction, Sacubitril, Valsartan, medicine.drug

الوصف: Rhabdomyolysis is caused by extensive damage to skeletal muscles resulting in elevated creatine phosphokinase (CPK), Lactate dehydrogenase (LDH), and aspartate aminotransferase (AST), leading to life-threatening consequences like acute renal failure, cardiac arrhythmias, and hyperthermia. A variety of causes for muscle damage are known, and one of the most common is drug-induced. Statins and many other agents are known to induce muscle damage, but here we report Entresto™ (Sacubitril/Valsartan) induced rhabdomyolysis which has not been previously reported as solely responsible in the literature.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b0796578c599ba0cc241c5900ebbc02Test
http://europepmc.org/articles/PMC6631059Test

المؤلفون: Azahara Rodríguez-Luna, Antonio M. Rabasco, Elena Talero, M.L. González-Rodríguez, María José Cózar, Javier Ávila-Román, Virginia Motilva

المساهمون: Universidad de Sevilla. Departamento de Farmacología, Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica

المصدر: idUS. Depósito de Investigación de la Universidad de Sevilla
instname
Marine Drugs
Volume 16
Issue 10
Marine Drugs, Vol 16, Iss 10, p 378 (2018)

مصطلحات موضوعية: 0301 basic medicine, Keratinocytes, Skin erythema, Erythema, Anti-Inflammatory Agents, Pharmaceutical Science, Nitric Oxide Synthase Type II, Pharmacology, Xanthophylls, fucoxanthin, Ointments, chemistry.chemical_compound, Mice, 0302 clinical medicine, Drug Discovery, Fucoxanthin, skin and connective tissue diseases, Pharmacology, Toxicology and Pharmaceutics (miscellaneous), lcsh:QH301-705.5, Skin, integumentary system, Chemistry, Hyperplasia, epidermal hyperplasia, Up-Regulation, 030220 oncology & carcinogenesis, Female, medicine.symptom, UVB, Ultraviolet Rays, Down-Regulation, Article, Cell Line, 03 medical and health sciences, In vivo, medicine, Animals, Humans, Mice, Hairless, L-Lactate Dehydrogenase, Interleukin-6, Tumor Necrosis Factor-alpha, Macrophages, medicine.disease, Hairless, HaCaT, photoprotection, 030104 developmental biology, lcsh:Biology (General), Cyclooxygenase 2, inflammation, Reactive Oxygen Species, Ex vivo

الوصف: Microalgae represent a source of bio-active compounds such as carotenoids with potent anti-inflammatory and antioxidant properties. We aimed to investigate the effects of fucoxanthin (FX) in both in vitro and in vivo skin models. Firstly, its anti-inflammatory activity was evaluated in LPS-stimulated THP-1 macrophages and TNF-&alpha
stimulated HaCaT keratinocytes, and its antioxidant activity in UVB-irradiated HaCaT cells. Next, in vitro and ex vivo permeation studies were developed to determine the most suitable formulation for in vivo FX topical application. Then, we evaluated the effects of a FX-containing cream on TPA-induced epidermal hyperplasia in mice, as well as on UVB-induced acute erythema in hairless mice. Our results confirmed the in vitro reduction of TNF-&alpha
IL-6, ROS and LDH production. Since the permeation results showed that cream was the most favourable vehicle, FX-cream was elaborated. This formulation effectively ameliorated TPA-induced hyperplasia, by reducing skin edema, epidermal thickness, MPO activity and COX-2 expression. Moreover, FX-cream reduced UVB-induced erythema through down-regulation of COX-2 and iNOS as well as up-regulation of HO-1 protein via Nrf-2 pathway. In conclusion, FX, administered in a topical formulation, could be a novel natural adjuvant for preventing exacerbations associated with skin inflammatory pathologies as well as protecting skin against UV radiation.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5493be963654918368e4cacc384f5e91Test