Department of Chemistry, Università degli Studi di Milano, 20133 Milan, Italy.
Ann Romney Center for Neurologic Diseases, Department of Neurology, Brigham and Women's Hospital and Harvard Medical School, Boston, MA 02115, USA.
Molecules. 2022 Dec 23;28(1):112. doi: 10.3390/molecules28010112.
Cannabidiol (CBD) is a biologically active compound present in the plants of the family, used as anticonvulsant, anti-inflammatory, anti-anxiety, and more recently, anticancer drug. In this work, its use as a new self-assembly inducer in the formation of nanoparticles is validated. The target conjugates are characterized by the presence of different anticancer drugs (namely -desacetyl thiocolchicine, podophyllotoxin, and paclitaxel) connected to CBD through a linker able to improve drug release. These nanoparticles are formed via solvent displacement method, resulting in monodisperse and stable structures having hydrodynamic diameters ranging from 160 to 400 nm. Their biological activity is evaluated on three human tumor cell lines (MSTO-211H, HT-29, and HepG2), obtaining GI values in the low micromolar range. Further biological assays were carried out on MSTO-211H cells for the most effective NP , confirming the involvement of paclitaxel in cytotoxicity and cell death mechanism.
大麻二酚(CBD)是一种存在于大麻科植物中的生物活性化合物,可用作抗惊厥药、抗炎药、抗焦虑药,最近还可用作抗癌药物。在这项工作中,验证了其作为形成纳米粒子的新自组装诱导剂的用途。目标缀合物的特征在于通过连接子连接有不同的抗癌药物(即去乙酰基硫代秋水仙碱、鬼臼毒素和紫杉醇),该连接子能够改善药物释放。这些纳米粒子通过溶剂置换法形成,得到单分散且稳定的结构,其水动力直径范围为 160 至 400nm。它们的生物活性在三种人类肿瘤细胞系(MSTO-211H、HT-29 和 HepG2)上进行评估,获得了低微摩尔范围内的 GI 值。针对最有效的 NP ,在 MSTO-211H 细胞上进行了进一步的生物学检测,证实紫杉醇参与了细胞毒性和细胞死亡机制。