Bustos-Salgado Paola, Andrade-Carrera Berenice, Domínguez-Villegas Valeri, Noé Véronique, Mallandrich Mireia, Colom Helena, Calpena-Campmany Ana, Garduño-Ramírez María Luisa
Departament de Farmàcia i Tecnologia Farmacèutica, i Fisicoquímica, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona (UB), Av. Joan XXIII 29-31, 08028 Barcelona, Spain.
Centro de Investigaciones Químicas, Instituto de Investigación en Ciencias Básicas y Aplicadas, Universidad Autónoma del Estado de Morelos, Av. Universidad 1001, Cuernavaca 62209, Morelos, Mexico.
Pharmaceutics. 2023 May 31;15(6):1632. doi: 10.3390/pharmaceutics15061632.
The increasing number of skin cancer cases worldwide and the adverse side effects of current treatments have led to the search for new anticancer agents. In this present work, the anticancer potential of the natural flavanone 1, extracted from , and four flavanone derivatives 1a-d obtained by different reactions from 1 was investigated by an in silico study and through cytotoxicity assays in melanoma (M21), cervical cancer (HeLa) cell lines and in a non-tumor cell line (HEK-293). The free compounds and compounds loaded in biopolymeric nanoparticles (PLGA NPs 1, 1a-d) were assayed. A structure-activity study (SAR) was performed to establish the main physicochemical characteristics that most contribute to cytotoxicity. Finally, ex vivo permeation studies were performed to assess the suitability of the flavanones for topical administration. Results revealed that most of the studied flavanones and their respective PLGA NPs inhibited cell growth depending on the concentration; 1b should be highlighted. The descriptors of the energetic factor were those that played a more important role in cellular activity. PLGA NPs demonstrated their ability to penetrate ( of 17.84-118.29 µg) and be retained ( of 0.01-1.44 g/g/cm) in the skin and to exert their action for longer. The results of the study suggest that flavanones could offer many opportunities as a future anticancer topical adjuvant treatment.
全球皮肤癌病例数量不断增加，以及当前治疗方法的不良副作用，促使人们寻找新的抗癌药物。在本研究中，通过计算机模拟研究以及在黑色素瘤（M21）、子宫颈癌（HeLa）细胞系和非肿瘤细胞系（HEK - 293）中进行细胞毒性试验，研究了从[具体来源未给出]提取的天然黄烷酮1以及通过1经不同反应得到的四种黄烷酮衍生物1a - d的抗癌潜力。对游离化合物以及负载在生物聚合物纳米颗粒（PLGA NPs 1、1a - d）中的化合物进行了检测。进行了构效关系研究（SAR）以确定对细胞毒性贡献最大的主要物理化学特征。最后，进行了体外渗透研究以评估黄烷酮用于局部给药的适用性。结果表明，大多数研究的黄烷酮及其各自的PLGA NPs根据浓度抑制细胞生长；应特别强调1b。能量因子的描述符在细胞活性中起更重要的作用。PLGA NPs显示出它们能够渗透（渗透量为17.84 - 118.29 µg）并保留在皮肤中（保留量为0.01 - 1.44 g/g/cm），并能发挥更长时间的作用。研究结果表明，黄烷酮作为未来抗癌局部辅助治疗可能提供很多机会。
