Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies
Industrial hemp (<i>Cannabis sativa</i>) is traditionally cultivated as a valuable source of fibers and nutrients. Multiple studies also demonstrated antimicrobial, anti-proliferative, phytotoxic and insecticide effects of the essential oil from hemp female inflorescences. On the other s...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-05-01
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| Series: | Antioxidants |
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| Online Access: | https://www.mdpi.com/2076-3921/9/5/437 |
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| author | Giustino Orlando Lucia Recinella Annalisa Chiavaroli Luigi Brunetti Sheila Leone Simone Carradori Simonetta Di Simone Maria Chiara Ciferri Gokhan Zengin Gunes Ak Hassan H. Abdullah Estefanía Cordisco Maximiliano Sortino Laura Svetaz Matteo Politi Paola Angelini Stefano Covino Roberto Venanzoni Stefania Cesa Luigi Menghini Claudio Ferrante |
| author_facet | Giustino Orlando Lucia Recinella Annalisa Chiavaroli Luigi Brunetti Sheila Leone Simone Carradori Simonetta Di Simone Maria Chiara Ciferri Gokhan Zengin Gunes Ak Hassan H. Abdullah Estefanía Cordisco Maximiliano Sortino Laura Svetaz Matteo Politi Paola Angelini Stefano Covino Roberto Venanzoni Stefania Cesa Luigi Menghini Claudio Ferrante |
| author_sort | Giustino Orlando |
| collection | DOAJ |
| description | Industrial hemp (<i>Cannabis sativa</i>) is traditionally cultivated as a valuable source of fibers and nutrients. Multiple studies also demonstrated antimicrobial, anti-proliferative, phytotoxic and insecticide effects of the essential oil from hemp female inflorescences. On the other side, only a few studies explored the potential pharmacological application of polar extracts from inflorescences. In the present study, we investigated the water extract from inflorescences of industrial hemp Futura 75 variety, from phytochemical and pharmacological point of view. The water extract was assayed for phenolic compound content, radical scavenger/reducing, chelating and anti-tyrosinase effects. Through an ex vivo model of toxicity induced by lipopolysaccharide (LPS) on isolated rat colon and liver, we explored the extract effects on serotonin, dopamine and kynurenine pathways and the production of prostaglandin (PG)E<sub>2</sub>. Anti-proliferative effects were also evaluated against human colon cancer HCT116 cell line. Additionally, antimycotic effects were investigated against <i>Trichophyton rubrum, Trichophyton interdigitale, Microsporum gypseum.</i> Finally, in silico studies, including bioinformatics, network pharmacology and docking approaches were conducted in order to predict the putative targets underlying the observed pharmacological and microbiological effects. Futura 75 water extract was able to blunt LPS-induced reduction of serotonin and increase of dopamine and kynurenine turnover, in rat colon. Additionally, the reduction of PGE<sub>2</sub> levels was observed in both colon and liver specimens, as well. The extract inhibited the HCT116 cell viability, the growth of <i>T. rubrum</i> and <i>T. interdigitale</i> and the activity of tyrosinase, in vitro, whereas in silico studies highlighting the inhibitions of cyclooxygenase-1 (induced by carvacrol), carbonic anhydrase IX (induced by chlorogenic acid and gallic acid) and lanosterol 14-α-demethylase (induced by rutin) further support the observed pharmacological and antimycotic effects. The present findings suggest female inflorescences from industrial hemp as high quality by-products, thus representing promising sources of nutraceuticals and cosmeceuticals against inflammatory and infectious diseases. |
| first_indexed | 2024-03-10T19:46:53Z |
| format | Article |
| id | doaj.art-9bae3826fbd243d586ce8ac3c2fcec6b |
| institution | Directory Open Access Journal |
| issn | 2076-3921 |
| language | English |
| last_indexed | 2024-03-10T19:46:53Z |
| publishDate | 2020-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antioxidants |
| spelling | doaj.art-9bae3826fbd243d586ce8ac3c2fcec6b2023-11-20T00:46:54ZengMDPI AGAntioxidants2076-39212020-05-019543710.3390/antiox9050437Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo StudiesGiustino Orlando0Lucia Recinella1Annalisa Chiavaroli2Luigi Brunetti3Sheila Leone4Simone Carradori5Simonetta Di Simone6Maria Chiara Ciferri7Gokhan Zengin8Gunes Ak9Hassan H. Abdullah10Estefanía Cordisco11Maximiliano Sortino12Laura Svetaz13Matteo Politi14Paola Angelini15Stefano Covino16Roberto Venanzoni17Stefania Cesa18Luigi Menghini19Claudio Ferrante20Department of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Biology, Science Faculty, Selcuk Universtiy, Campus, Konya, Konya 42130, TurkeyDepartment of Biology, Science Faculty, Selcuk Universtiy, Campus, Konya, Konya 42130, TurkeyChemistry Department, College of Education, Salahaddin University-Erbil, Erbil 44001, IraqFarmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario 2000, ArgentinaFarmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario 2000, ArgentinaFarmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario 2000, ArgentinaDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Chemistry, Biology and Biotechnology, University of Perugia, 06100 Perugia, ItalyDepartment of Chemistry, Biology and Biotechnology, University of Perugia, 06100 Perugia, ItalyDepartment of Chemistry, Biology and Biotechnology, University of Perugia, 06100 Perugia, ItalyDepartment of Drug Chemistry and Technologies, “Sapienza” University of Rome, 00185 Rome, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyDepartment of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, 66100 Chieti, ItalyIndustrial hemp (<i>Cannabis sativa</i>) is traditionally cultivated as a valuable source of fibers and nutrients. Multiple studies also demonstrated antimicrobial, anti-proliferative, phytotoxic and insecticide effects of the essential oil from hemp female inflorescences. On the other side, only a few studies explored the potential pharmacological application of polar extracts from inflorescences. In the present study, we investigated the water extract from inflorescences of industrial hemp Futura 75 variety, from phytochemical and pharmacological point of view. The water extract was assayed for phenolic compound content, radical scavenger/reducing, chelating and anti-tyrosinase effects. Through an ex vivo model of toxicity induced by lipopolysaccharide (LPS) on isolated rat colon and liver, we explored the extract effects on serotonin, dopamine and kynurenine pathways and the production of prostaglandin (PG)E<sub>2</sub>. Anti-proliferative effects were also evaluated against human colon cancer HCT116 cell line. Additionally, antimycotic effects were investigated against <i>Trichophyton rubrum, Trichophyton interdigitale, Microsporum gypseum.</i> Finally, in silico studies, including bioinformatics, network pharmacology and docking approaches were conducted in order to predict the putative targets underlying the observed pharmacological and microbiological effects. Futura 75 water extract was able to blunt LPS-induced reduction of serotonin and increase of dopamine and kynurenine turnover, in rat colon. Additionally, the reduction of PGE<sub>2</sub> levels was observed in both colon and liver specimens, as well. The extract inhibited the HCT116 cell viability, the growth of <i>T. rubrum</i> and <i>T. interdigitale</i> and the activity of tyrosinase, in vitro, whereas in silico studies highlighting the inhibitions of cyclooxygenase-1 (induced by carvacrol), carbonic anhydrase IX (induced by chlorogenic acid and gallic acid) and lanosterol 14-α-demethylase (induced by rutin) further support the observed pharmacological and antimycotic effects. The present findings suggest female inflorescences from industrial hemp as high quality by-products, thus representing promising sources of nutraceuticals and cosmeceuticals against inflammatory and infectious diseases.https://www.mdpi.com/2076-3921/9/5/437futura 75serotonindopaminekynurenineantimycoticanti-proliferative |
| spellingShingle | Giustino Orlando Lucia Recinella Annalisa Chiavaroli Luigi Brunetti Sheila Leone Simone Carradori Simonetta Di Simone Maria Chiara Ciferri Gokhan Zengin Gunes Ak Hassan H. Abdullah Estefanía Cordisco Maximiliano Sortino Laura Svetaz Matteo Politi Paola Angelini Stefano Covino Roberto Venanzoni Stefania Cesa Luigi Menghini Claudio Ferrante Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies Antioxidants futura 75 serotonin dopamine kynurenine antimycotic anti-proliferative |
| title | Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies |
| title_full | Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies |
| title_fullStr | Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies |
| title_full_unstemmed | Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies |
| title_short | Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies |
| title_sort | water extract from inflorescences of industrial hemp futura 75 variety as a source of anti inflammatory anti proliferative and antimycotic agents results from in silico in vitro and ex vivo studies |
| topic | futura 75 serotonin dopamine kynurenine antimycotic anti-proliferative |
| url | https://www.mdpi.com/2076-3921/9/5/437 |
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