Caroli Clarissa, Brighenti Virginia, Cattivelli Alice, Salamone Stefano, Pollastro Federica, Tagliazucchi Davide, Pellati Federica
Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 103, 41125 Modena, Italy; Clinical and Experimental Medicine PhD Program, University of Modena and Reggio, Via Giuseppe Campi 287, 41125 Modena, Italy.
Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 103, 41125 Modena, Italy.
J Pharm Biomed Anal. 2023 Nov 30;236:115723. doi: 10.1016/j.jpba.2023.115723. Epub 2023 Sep 14.
Phenolic compounds from Cannabis sativa L. (Cannabaceae family), in particular cannflavins, are known to possess several biological properties. However, their antiproliferative activity, being of great interest from a medicinal chemistry point of view, has not been deeply investigated so far in the literature. In the light of this, the aim of this study was to obtain an enriched fraction of polyphenols (namely PEF) from inflorescences of a non-psychoactive C. sativa (hemp) variety and to evaluate its antiproliferative activity against cancer cells, capitalizing on a new and selective extraction method for hemp polyphenols, followed by preparative flash column chromatography. Untargeted metabolomics, using a new method based on ultra-high-performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC-HRMS), was applied here for the first time to fully characterize PEF. Then, the main phenolic compounds were quantified by HPLC-UV. The antiproliferative activity of PEF and of the isolated compounds was assessed in vitro for the first time against Caco-2 and SW480 human colon adenocarcinoma cell lines providing promising IC values, in comparison with the reference drug used in therapy for this cancer type. Based on these results, PEF can be considered as a new highly potential therapeutic product to be further investigated against colorectal cancer, thanks to the possible synergistic interaction of its compounds.
来自大麻（大麻科）的酚类化合物，特别是大麻黄酮，已知具有多种生物学特性。然而，从药物化学的角度来看，它们的抗增殖活性虽然备受关注，但迄今为止在文献中尚未得到深入研究。鉴于此，本研究的目的是从一种无精神活性的大麻（工业大麻）品种的花序中获得富含多酚的组分（即PEF），并利用一种新的、选择性的大麻多酚提取方法，随后进行制备型快速柱色谱，评估其对癌细胞的抗增殖活性。本研究首次采用基于超高效液相色谱与高分辨率质谱联用（UHPLC-HRMS）的新方法进行非靶向代谢组学分析，以全面表征PEF。然后，通过HPLC-UV对主要酚类化合物进行定量。首次在体外评估了PEF和分离出的化合物对Caco-2和SW480人结肠腺癌细胞系的抗增殖活性，与该癌症类型治疗中使用的参考药物相比，提供了有前景的IC值。基于这些结果，由于其化合物可能存在协同相互作用，PEF可被视为一种新的极具潜力的治疗产品，有待进一步针对结直肠癌进行研究。
