Orlando Giustino, Recinella Lucia, Chiavaroli Annalisa, Brunetti Luigi, Leone Sheila, Carradori Simone, Di Simone Simonetta, Ciferri Maria Chiara, Zengin Gokhan, Ak Gunes, Abdullah Hassan H, Cordisco Estefanía, Sortino Maximiliano, Svetaz Laura, Politi Matteo, Angelini Paola, Covino Stefano, Venanzoni Roberto, Cesa Stefania, Menghini Luigi, Ferrante Claudio
Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, 66100 Chieti, Italy.
Department of Biology, Science Faculty, Selcuk Universtiy, Campus, Konya, Konya 42130, Turkey.
Antioxidants (Basel). 2020 May 17;9(5):437. doi: 10.3390/antiox9050437.
Industrial hemp () 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. Anti-proliferative effects were also evaluated against human colon cancer HCT116 cell line. Additionally, antimycotic effects were investigated against 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 levels was observed in both colon and liver specimens, as well. The extract inhibited the HCT116 cell viability, the growth of and 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.
工业大麻传统上作为一种有价值的纤维和营养来源进行种植。多项研究还证明了大麻雌花序精油的抗菌、抗增殖、植物毒性和杀虫作用。另一方面，只有少数研究探索了花序极性提取物的潜在药理学应用。在本研究中，我们从植物化学和药理学角度研究了工业大麻Futura 75品种花序的水提取物。对水提取物进行了酚类化合物含量、自由基清除/还原、螯合和抗酪氨酸酶作用的测定。通过脂多糖（LPS）诱导的离体大鼠结肠和肝脏毒性的体外模型，我们探索了提取物对血清素、多巴胺和犬尿氨酸途径以及前列腺素（PG）E产生的影响。还评估了其对人结肠癌HCT116细胞系的抗增殖作用。此外，研究了其对……的抗真菌作用。最后，进行了包括生物信息学、网络药理学和对接方法在内的计算机模拟研究，以预测所观察到的药理和微生物学效应背后的假定靶点。Futura 75水提取物能够减轻LPS诱导的大鼠结肠中血清素的降低以及多巴胺和犬尿氨酸周转率的增加。此外，在结肠和肝脏标本中也观察到了PGE水平的降低。该提取物在体外抑制了HCT116细胞活力、……的生长以及酪氨酸酶的活性，而计算机模拟研究突出了对环氧化酶-1（由香芹酚诱导）、碳酸酐酶IX（由绿原酸和没食子酸诱导）和羊毛甾醇14-α-去甲基酶（由芦丁诱导）的抑制，进一步支持了所观察到的药理和抗真菌作用。本研究结果表明，工业大麻的雌花序是高质量的副产品，因此是对抗炎症和传染病的营养保健品和药妆品的有前景的来源。
