14 results on '"Donatella Cicia"'
Search Results
2. Adding New Scientific Evidences on the Pharmaceutical Properties of Pelargonium quercetorum Agnew Extracts by Using In Vitro and In Silico Approaches
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Annalisa Chiavaroli, Maria Loreta Libero, Simonetta Cristina Di Simone, Alessandra Acquaviva, Nilofar, Lucia Recinella, Sheila Leone, Luigi Brunetti, Donatella Cicia, Angelo Antonio Izzo, Giustino Orlando, Gokhan Zengin, Abdullahi Ibrahim Uba, Ugur Cakilcioğlu, Muzaffer Mukemre, Omer Elkiran, Luigi Menghini, and Claudio Ferrante
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Pelargonium quercetorum ,phenolic compounds ,antioxidant ,enzyme inhibition ,colon inflammation ,TRPM8 ,Botany ,QK1-989 - Abstract
Pelargonium quercetorum is a medicinal plant traditionally used for treating intestinal worms. In the present study, the chemical composition and bio-pharmacological properties of P. quercetorum extracts were investigated. Enzyme inhibition and scavenging/reducing properties of water, methanol, and ethyl acetate extracts were assayed. The extracts were also studied in an ex vivo experimental model of colon inflammation, and in this context the gene expression of cyclooxygenase-2 (COX-2) and tumor necrosis factor α (TNFα) were assayed. Additionally, in colon cancer HCT116 cells, the gene expression of transient receptor potential cation channel subfamily M (melastatin) member 8 (TRPM8), possibly involved in colon carcinogenesis, was conducted as well. The extracts showed a different qualitative and quantitative content of phytochemicals, with water and methanol extracts being richer in total phenols and flavonoids, among which are flavonol glycosides and hydroxycinnamic acids. This could explain, at least in part, the higher antioxidant effects shown by methanol and water extracts, compared with ethyl acetate extract. By contrast, the ethyl acetate was more effective as cytotoxic agent against colon cancer cells, and this could be related, albeit partially, to the content of thymol and to its putative ability to downregulate TRPM8 gene expression. Additionally, the ethyl acetate extract was effective in inhibiting the gene expression of COX-2 and TNFα in isolated colon tissue exposed to LPS. Overall, the present results support future studies for investigating protective effects against gut inflammatory diseases.
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- 2023
- Full Text
- View/download PDF
3. Involvement of Opioid System and TRPM8/TRPA1 Channels in the Antinociceptive Effect of Spirulina platensis
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Mariana A. Freitas, Amanda Vasconcelos, Elaine C. D. Gonçalves, Eduarda G. Ferrarini, Gabriela B. Vieira, Donatella Cicia, Maíra Cola, Raffaele Capasso, and Rafael C. Dutra
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Spirulina platensis ,pain ,opioid system ,ionic channel ,functional food ,analgesic ,Microbiology ,QR1-502 - Abstract
Spirulina platensis is a “super-food” and has attracted researchers’ attention due to its anti-inflammatory, antioxidant, and analgesic properties. Herein, we investigated the antinociceptive effects of Spirulina in different rodent behavior models of inflammatory pain. Male Swiss mice were treated with Spirulina (3–300 mg/kg, p.o.), indomethacin (10 mg/kg, p.o.), or vehicle (0.9% NaCl 10 mL/kg). Behavioral tests were performed with administration of acetic acid (0.6%, i.p.), formalin 2.7% (formaldehyde 1%, i.pl.), menthol (1.2 µmol/paw, i.pl.), cinnamaldehyde (10 nmol/paw, i.pl.), capsaicin (1.6 µg/paw, i.pl.), glutamate (20 µmol/paw, i.pl.), or naloxone (1 mg/kg, i.p.). The animals were also exposed to the rotarod and open field test to determine possible effects of Spirulina on locomotion and motor coordination. The quantitative phytochemical assays exhibited that Spirulina contains significant concentrations of total phenols and flavonoid contents, as well as it showed a powerful antioxidant effect with the highest scavenging activity. Oral administration of Spirulina completely inhibited the abdominal contortions induced by acetic acid (ED50 = 20.51 mg/kg). Spirulina treatment showed significant inhibition of formalin-induced nociceptive behavior during the inflammatory phase, and the opioid-selective antagonist markedly blocked this effect. Furthermore, our data indicate that the mechanisms underlying Spirulina analgesia appear to be related to its ability to modulate TRMP8 and TRPA1, but not by TRPV1 or glutamatergic system. Spirulina represents an orally active and safe natural analgesic that exhibits great therapeutic potential for managing inflammatory pain disorders.
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- 2021
- Full Text
- View/download PDF
4. Bromelain a Potential Bioactive Compound: A Comprehensive Overview from a Pharmacological Perspective
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Arka Jyoti Chakraborty, Saikat Mitra, Trina E. Tallei, Abu Montakim Tareq, Firzan Nainu, Donatella Cicia, Kuldeep Dhama, Talha Bin Emran, Jesus Simal-Gandara, and Raffaele Capasso
- Subjects
bromelain ,Ananas comosus ,pineapple ,nanoparticles ,proteolytic enzymes ,Science - Abstract
Bromelain is an effective chemoresponsive proteolytic enzyme derived from pineapple stems. It contains several thiol endopeptidases and is extracted and purified via several methods. It is most commonly used as an anti-inflammatory agent, though scientists have also discovered its potential as an anticancer and antimicrobial agent. It has been reported as having positive effects on the respiratory, digestive, and circulatory systems, and potentially on the immune system. It is a natural remedy for easing arthritis symptoms, including joint pain and stiffness. This review details bromelain’s varied uses in healthcare, its low toxicity, and its relationship to nanoparticles. The door of infinite possibilities will be opened up if further extensive research is carried out on this pineapple-derived enzyme.
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- 2021
- Full Text
- View/download PDF
5. Pharmacological Studies on Traditional Plant-Based Remedies
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Giuseppe Lucariello, Donatella Cicia, and Raffaele Capasso
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n/a ,Biology (General) ,QH301-705.5 - Abstract
For years, plant-based remedies have been used as a traditional practice to treat and prevent a broad range of diseases [...]
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- 2021
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6. Isomadecassoside, a New Ursane-Type Triterpene Glycoside from Centella asiatica Leaves, Reduces Nitrite Levels in LPS-Stimulated Macrophages
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Giuseppina Chianese, Francesca Masi, Donatella Cicia, Daniele Ciceri, Sabrina Arpini, Mario Falzoni, Ester Pagano, and Orazio Taglialatela-Scafati
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Centella asiatica ,triterpenoid saponins ,phytochemicals ,anti-inflammatory activity ,Microbiology ,QR1-502 - Abstract
A madecassoside-rich fraction obtained from the industrial purification of Centella asiatica leaves afforded a new triterpene glycoside, named isomadecassoside (4), characterized by an ursane-type skeleton and migration of the double bond at Δ20(21) in ring E. The structure of isomadecassoside was established by means of HR-ESIMS and detailed analysis of 1D and 2D NMR spectra, which allowed a complete NMR assignment. Studies on isolated J774A.1 macrophages stimulated by LPS revealed that isomadecassoside (4) inhibited nitrite production at non-cytotoxic concentrations, thus indicating an anti-inflammatory effect similar to that of madecassoside.
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- 2021
- Full Text
- View/download PDF
7. N-Acylethanolamine acid amidase (NAAA) inhibition rescues intestinal fibrosis through IL-23 pathway
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MariaFrancesca Nanì, Giuseppe Lucariello, Ester Pagano, Fabio Cattaneo, Donatella Cicia, Federica Raucci, FrancescaPaola Tropeano, Stefania Petrosino, PaolaDe Cicco, Francesca Borrelli, AngeloA. Izzo, and Barbara Romano
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- 2023
8. TRPM8 indicates poor prognosis in colorectal cancer patients and its pharmacological targeting reduces tumour growth in mice by inhibiting Wnt/β-catenin signalling
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Ester Pagano, Barbara Romano, Donatella Cicia, Fabio A. Iannotti, Tommaso Venneri, Giuseppe Lucariello, Maria Francesca Nanì, Fabio Cattaneo, Paola De Cicco, Maria D'Armiento, Marcello De Luca, Ruggiero Lionetti, Stefania Lama, Paola Stiuso, Pietro Zoppoli, Geppino Falco, Silvia Marchianò, Stefano Fiorucci, Raffaele Capasso, Vincenzo Di Marzo, Francesca Borrelli, Angelo A. Izzo, Pagano, E., Romano, B., Cicia, D., Iannotti, F. A., Venneri, T., Lucariello, G., Nani, M. F., Cattaneo, F., De Cicco, P., D'Armiento, M., De Luca, M., Lionetti, R., Lama, S., Stiuso, P., Zoppoli, P., Falco, G., Marchiano, S., Fiorucci, S., Capasso, R., Di Marzo, V., Borrelli, F., and Izzo, A. A.
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TRPM8 ,Wnt/β-catenin ,transient receptor potential channel ,TRPM Cation Channels ,Membrane Proteins ,Prognosis ,Gene Expression Regulation, Neoplastic ,Mice ,colon cancer ,transient receptor potential channels ,Cell Line, Tumor ,Colonic Neoplasms ,Humans ,Animals ,pharmacology ,Colorectal Neoplasms ,Wnt Signaling Pathway ,beta Catenin ,Cell Proliferation - Abstract
Background and Purpose: Transient receptor potential melastatin type-8 (TRPM8) is a cold-sensitive cation channel protein belonging to the TRP superfamily of ion channels. Here, we reveal the molecular mechanism of TRPM8 and its clinical relevance in colorectal cancer (CRC). Experimental Approach: TRPM8 expression and its correlation with the survival rate of CRC patients was analysed. To identify the key pathways and genes related to TRPM8 high expression, Kyoto Encyclopedia of Genes and Genomes pathway enrichment analyses were conducted in CRC patients. TRPM8 functional role was assessed by using Trpm8−/− mice in models of sporadic and colitis-associated colon cancer. TRPM8 pharmacological targeting by WS12 was evaluated in murine models of CRC. Key Results: TRPM8 is overexpressed in colon primary tumours and in CD326+ tumour cell fraction. TRPM8 high expression was related to lower survival rate of CRC patients, Wnt–Frizzled signalling hyperactivation and adenomatous polyposis coli down-regulation. In sporadic and colitis-associated models of colon cancer, either absence or pharmacological desensitization of TRPM8 reduced tumour development via inhibition of the oncogenic Wnt/β-catenin signalling. TRPM8 pharmacological blockade reduced tumour growth in CRC xenograft mice by reducing the transcription of Wnt signalling regulators and the activation of β-catenin and its target oncogenes such as C-Myc and Cyclin D1. Conclusion and Implications: Human data provide valuable insights to propose TRPM8 as a prognostic marker with a negative predictive value for CRC patient survival. Animal experiments demonstrate TRPM8 involvement in colon cancer pathophysiology and its potential as a drug target for CRC.
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- 2022
9. N-Acylethanolamine acid amidase (NAAA) is dysregulated in colorectal cancer patients and its inhibition reduces experimental cancer growth
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Donatella Cicia, Maria D'Armiento, Alexandros Makriyannis, Tommaso Venneri, Fabio Arturo Iannotti, Michael S. Malamas, Federica Di Tella, Giovanna Vanacore, Ester Pagano, Raffaele Capasso, Barbara Romano, Fabiana Piscitelli, Angelo A. Izzo, Giovanni Aprea, Giuseppe Lucariello, Vincenzo Brancaleone, Francesca Borrelli, Bernardo Sbarro, Marcello De Luca, Vincenzo Di Marzo, Ruggero Lionetti, Maria Francesca Nanì, Ferdinando Fiorino, Rosa Sparaco, Romano, B., Pagano, E., Iannotti, F. A., Piscitelli, F., Brancaleone, V., Lucariello, G., Nani, M. F., Fiorino, F., Sparaco, R., Vanacore, G., Di Tella, F., Cicia, D., Lionetti, R., Makriyannis, A., Malamas, M., De Luca, M., Aprea, G., D'Armiento, M., Capasso, R., Sbarro, B., Venneri, T., Di Marzo, V., Borrelli, F., and Izzo, A. A.
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Pharmacology ,Cell cycle checkpoint ,Colorectal cancer ,Azoxymethane ,business.industry ,Cancer ,Cell cycle ,medicine.disease ,acylethanolamide ,Amidohydrolases ,chemistry.chemical_compound ,colon cancer ,chemistry ,Downregulation and upregulation ,Epidermal growth factor ,Ethanolamines ,medicine ,Cancer research ,Humans ,endocannabinoid system ,business ,Colorectal Neoplasms ,Cyclin A2 - Abstract
Background and purpose N-acylethanolamine acid amidase (NAAA) is a lysosomal enzyme accountable for the breakdown of N-acylethanolamides (NAEs) and its pharmacological inhibition determines beneficial effects in inflammatory conditions. The knowledge of NAAA in cancer is fragmentary with an unclarified mechanism whereas its contribution to colorectal cancer (CRC) is unknown to date. Experimental approach CRC xenograft and azoxymethane models assessed the in vivo pharmacological effect of NAAA inhibition; tumor secretome was evaluated by an oncogenic array; CRC cell lines were used for in vitro studies; cell cycle was analyzed by cytofluorimetry; NAAA was knocked down with siRNA; human biopsies were obtained from surgically resected CRC patients; gene expression was revealed by RT-PCR; NAEs were measured by LC-MS. Key results The NAAA inhibitor AM9053 reduced CRC xenograft tumor growth and counteracted tumor development in the azoxymethane model. NAAA inhibition impacted the composition of the tumor secretome that negatively affected the expression of epidermal growth factor family members. In CRC cells, AM9053 reduced proliferation with a mechanism mediated by PPAR-α and TRPV1 and induced cell cycle arrest in the S phase with cyclin A2/CDK2 downregulation. NAAA knock-down mirrored the effects of NAAA pharmacological inhibition. NAAA expression was downregulated in human CRC tissues, with a consequential augmentation of NAEs levels and dysregulation of some of their targets. Conclusions and implications Our results provide unprecedented data on the functional importance of NAAA in CRC progression and its mechanism. We propose this enzyme as a valid drug target for the treatment of CRC growth and development.
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- 2021
10. Involvement of Opioid System and TRPM8/TRPA1 Channels in the Antinociceptive Effect of Spirulina platensis
- Author
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Eduarda Gomes Ferrarini, Donatella Cicia, Amanda Vasconcelos, Rafael C. Dutra, Maíra Cola, Raffaele Capasso, Gabriela Bonfanti Vieira, Mariana A. Freitas, Elaine C. D. Gonçalves, Freitas, M. A., Vasconcelos, A., Goncalves, E. C. D., Ferrarini, E. G., Vieira, G. B., Cicia, D., Cola, M., Capasso, R., and Dutra, R. C.
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Male ,Nociception ,0301 basic medicine ,Antioxidant ,Narcotic Antagonists ,medicine.medical_treatment ,Analgesic ,TRPV1 ,TRPM Cation Channels ,Spirulina platensis ,(+)-Naloxone ,Pharmacology ,Microbiology ,Biochemistry ,Article ,Plant Extract ,Nociceptive Pain ,functional food ,Mice ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,opioid system ,ionic channel ,Oral administration ,Spirulina ,medicine ,Animals ,pain ,TRPA1 Cation Channel ,Molecular Biology ,Spirulina (genus) ,Analgesics ,biology ,Animal ,Naloxone ,Plant Extracts ,Chemistry ,analgesic ,biology.organism_classification ,QR1-502 ,030104 developmental biology ,Capsaicin ,Menthol ,Spirulina platensi ,Narcotic Antagonist ,030217 neurology & neurosurgery - Abstract
Spirulina platensis is a “super-food” and has attracted researchers’ attention due toits anti-inflammatory, antioxidant, and analgesic properties. Herein, we investigated the antinociceptive effects of Spirulina in different rodent behavior models of inflammatory pain. Male Swiss mice were treated with Spirulina (3–300 mg/kg, p.o.), indomethacin (10 mg/kg, p.o.), or vehicle (0.9% NaCl 10 mL/kg). Behavioral tests were performed with administration of acetic acid (0.6%, i.p.), formalin 2.7% (formaldehyde 1%, i.pl.), menthol (1.2 µmol/paw, i.pl.), cinnamaldehyde (10 nmol/paw, i.pl.), capsaicin (1.6 µg/paw, i.pl.), glutamate (20 µmol/paw, i.pl.), or naloxone (1 mg/kg, i.p.).The animals were also exposed to the rotarod and open field test to determine possible effects of Spirulina on locomotion and motor coordination. The quantitative phytochemical assays exhibited thatSpirulina contains significant concentrations of total phenols and flavonoid contents, as well as it showed a powerful antioxidant effect with the highest scavenging activity.Oral administration of Spirulina completely inhibited the abdominal contortions induced by acetic acid (ED50 = 20.51 mg/kg). Spirulinatreatment showed significant inhibition of formalin-induced nociceptive behavior during the inflammatory phase, and the opioid-selective antagonist markedly blocked this effect. Furthermore, our data indicate that the mechanisms underlying Spirulina analgesia appear to be related to its ability to modulate TRMP8 and TRPA1, but not by TRPV1 or glutamatergic system. Spirulina represents an orally active and safe natural analgesic that exhibits great therapeutic potential for managing inflammatory pain disorders.
- Published
- 2021
- Full Text
- View/download PDF
11. Palmitoylethanolamide Reduces Colon Cancer Cell Proliferation and Migration, Influences Tumor Cell Cycle and Exerts In Vivo Chemopreventive Effects
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Barbara Romano, Vincenzo Brancaleone, Francesca Borrelli, M Francesca Nanì, Ester Pagano, Giuseppe Lucariello, Donatella Cicia, Angelo A. Izzo, Tommaso Venneri, Raffaele Capasso, Nunzio Antonio Cacciola, Pagano, E., Venneri, T., Lucariello, G., Cicia, D., Brancaleone, V., Nani, M. F., Cacciola, N. A., Capasso, R., Izzo, A. A., Borrelli, F., and Romano, B.
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0301 basic medicine ,Cancer Research ,Cell cycle checkpoint ,Colorectal cancer ,Article ,acylethanolamides ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Downregulation and upregulation ,medicine ,endocannabinoid system ,RC254-282 ,Cyclin-dependent kinase 1 ,Palmitoylethanolamide ,Acylethanolamide ,Chemistry ,Azoxymethane ,food and beverages ,Neoplasms. Tumors. Oncology. Including cancer and carcinogens ,Cell cycle ,medicine.disease ,Endocannabinoid system ,030104 developmental biology ,Oncology ,colon cancer ,030220 oncology & carcinogenesis ,Cancer research - Abstract
Simple Summary Treatment of colon cancer remains a significant unmet need. Palmitoylethanolamide (PEA) is an endogenous fatty acid amide also present in food sources. PEA exerts intestinal anti-inflammatory effects, but knowledge of its role in colon carcinogenesis is still largely fragmentary. Here, we found that ultramicronized PEA inhibited tumor cell proliferation mediated by PPAR-α and GPR55, induced cell cycle arrest in the G2/M phase and DNA fragmentation, reduced cell migration and exerted beneficial effects in the azoxymethane model of colonic tumors. Collectively, these data provide evidence on the beneficial effects of PEA in colon carcinogenesis. Abstract Palmitoylethanolamide (PEA) is an endogenous fatty acid amide related to the endocannabinoid anandamide. PEA exerts intestinal anti-inflammatory effects, but knowledge of its role in colon carcinogenesis is still largely fragmentary. We deepened this aspect by studying the effects of PEA (ultramicronized PEA, um-PEA) on colon cancer cell proliferation, migration and cell cycle as well as its effects in a murine model of colon cancer. Results showed that um-PEA inhibited tumor cell proliferation via peroxisome proliferator-activated receptor α and G protein-coupled receptor 55, induced cell cycle arrest in the G2/M phase, possibly through cyclin B1/CDK1 upregulation, and induced DNA fragmentation. Furthermore, um-PEA reduced tumor cell migration by reducing MMP2 and TIMP1 expression. In vivo administration of um-PEA exerted beneficial effects in the azoxymethane model of colonic tumors, by reducing the number of preneoplastic lesions and tumors. Collectively, our findings provide novel proofs on the effects of um-PEA in colon carcinogenesis.
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- 2021
12. Bromelain a Potential Bioactive Compound: A Comprehensive Overview from a Pharmacological Perspective
- Author
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Trina Ekawati Tallei, Firzan Nainu, Abu Montakim Tareq, Jesus Simal-Gandara, Talha Bin Emran, Kuldeep Dhama, Saikat Mitra, Arka Jyoti Chakraborty, Donatella Cicia, Raffaele Capasso, Chakraborty, A. J., Mitra, S., Tallei, T. E., Tareq, A. M., Nainu, F., Cicia, D., Dhama, K., Emran, T. B., Simal-Gandara, J., and Capasso, R.
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0301 basic medicine ,Bromelain (pharmacology) ,3309 Tecnología de Los Alimentos ,3209.04 Medicamentos Naturales ,Review ,Pharmacology ,General Biochemistry, Genetics and Molecular Biology ,03 medical and health sciences ,chemistry.chemical_compound ,Ananas comosu ,0302 clinical medicine ,Nanoparticle ,Medicine ,Ananas comosus ,lcsh:Science ,Ecology, Evolution, Behavior and Systematics ,Proteolytic enzymes ,Low toxicity ,Arthritis symptoms ,business.industry ,Pineapple ,Natural remedy ,Paleontology ,Antimicrobial ,Bioactive compound ,030104 developmental biology ,chemistry ,Space and Planetary Science ,030220 oncology & carcinogenesis ,lcsh:Q ,nanoparticles ,Bromelain ,business ,2302.09 Enzimología - Abstract
Bromelain is an effective chemoresponsive proteolytic enzyme derived from pineapple stems. It contains several thiol endopeptidases and is extracted and purified via several methods. It is most commonly used as an anti-inflammatory agent, though scientists have also discovered its potential as an anticancer and antimicrobial agent. It has been reported as having positive effects on the respiratory, digestive, and circulatory systems, and potentially on the immune system. It is a natural remedy for easing arthritis symptoms, including joint pain and stiffness. This review details bromelain’s varied uses in healthcare, its low toxicity, and its relationship to nanoparticles. The door of infinite possibilities will be opened up if further extensive research is carried out on this pineapple-derived enzyme.
- Published
- 2021
13. NAAA is dysregulated in colorectal cancer patients and its inhibition reduces experimental cancer growth
- Author
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Barbara Romano 1 2, Ester Pagano 1 2, Fabio A Iannotti 3 2, Fabiana Piscitelli 3 2, Vincenzo Brancaleone 4, Giuseppe Lucariello 1, Maria Francesca Nanì 1 2, Ferdinando Fiorino 1, Rosa Sparaco 1, Giovanna Vanacore 1, Federica Di Tella 1, Donatella Cicia 1, Ruggero Lionetti 5, Alexandros Makriyannis 6, Michael Malamas 6, Marcello De Luca 5, Giovanni Aprea 7, Maria D'Armiento 8, Raffaele Capasso 9 2, Bernardo Sbarro 1, Tommaso Venneri 1 2, Vincenzo Di Marzo 3 10 11 2, Francesca Borrelli 1 2, and Angelo A Izzo 1 2
- Subjects
acylethanolamides ,colon cancer ,endocannabinoid system - Abstract
Background and purpose: N-acylethanolamine acid amidase (NAAA) is a lysosomal enzyme accountable for the breakdown of N-acylethanolamides (NAEs) and its pharmacological inhibition determines beneficial effects in inflammatory conditions. The knowledge of NAAA in cancer is fragmentary with an unclarified mechanism whereas its contribution to colorectal cancer (CRC) is unknown to date. Experimental approach: CRC xenograft and azoxymethane models assessed the in vivo pharmacological effect of NAAA inhibition; tumor secretome was evaluated by an oncogenic array; CRC cell lines were used for in vitro studies; cell cycle was analyzed by cytofluorimetry; NAAA was knocked down with siRNA; human biopsies were obtained from surgically resected CRC patients; gene expression was revealed by RT-PCR; NAEs were measured by LC-MS. Key results: The NAAA inhibitor AM9053 reduced CRC xenograft tumor growth and counteracted tumor development in the azoxymethane model. NAAA inhibition impacted the composition of the tumor secretome that negatively affected the expression of epidermal growth factor family members. In CRC cells, AM9053 reduced proliferation with a mechanism mediated by PPAR-? and TRPV1 and induced cell cycle arrest in the S phase with cyclin A2/CDK2 downregulation. NAAA knock-down mirrored the effects of NAAA pharmacological inhibition. NAAA expression was downregulated in human CRC tissues, with a consequential augmentation of NAEs levels and dysregulation of some of their targets. Conclusions and implications: Our results provide unprecedented data on the functional importance of NAAA in CRC progression and its mechanism. We propose this enzyme as a valid drug target for the treatment of CRC growth and development.
- Published
- 2021
14. Isomadecassoside, a New Ursane-Type Triterpene Glycoside from Centella asiatica Leaves, Reduces Nitrite Levels in LPS-Stimulated Macrophages
- Author
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Donatella Cicia, Giuseppina Chianese, Daniele Ciceri, Orazio Taglialatela-Scafati, Sabrina Arpini, Francesca Masi, Mario Falzoni, Ester Pagano, Chianese, Giuseppina, Masi, Francesca, Cicia, Donatella, Ciceri, Daniele, Arpini, Sabrina, Falzoni, Mario, Pagano, Ester, and Taglialatela-Scafati, Orazio
- Subjects
chemistry.chemical_classification ,Centella ,biology ,Double bond ,010405 organic chemistry ,Chemistry ,Stereochemistry ,lcsh:QR1-502 ,Glycoside ,Centella asiatica, triterpenoid saponins, phytochemicals, anti-inflammatory activity ,biology.organism_classification ,phytochemicals ,01 natural sciences ,Biochemistry ,lcsh:Microbiology ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,triterpenoid saponins ,Centella asiatica ,Triterpene ,Nitrite ,anti-inflammatory activity ,Molecular Biology ,Two-dimensional nuclear magnetic resonance spectroscopy - Abstract
A madecassoside-rich fraction obtained from the industrial purification of Centella asiatica leaves afforded a new triterpene glycoside, named isomadecassoside (4), characterized by an ursane-type skeleton and migration of the double bond at Δ20(21) in ring E. The structure of isomadecassoside was established by means of HR-ESIMS and detailed analysis of 1D and 2D NMR spectra, which allowed a complete NMR assignment. Studies on isolated J774A.1 macrophages stimulated by LPS revealed that isomadecassoside (4) inhibited nitrite production at non-cytotoxic concentrations, thus indicating an anti-inflammatory effect similar to that of madecassoside.
- Published
- 2021
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