Faculty of Pharmaceutical Sciences, Post Graduate Program in Biodiversity and Biotechnology of the Amazon (Bionorte), Federal University of Amazonas, Manaus, Amazonas, Brazil.
Drug Research and Development Center (NPDM), Federal University of Ceará, Fortaleza, Ceará, Brazil.
Toxicol In Vitro. 2020 Aug;66:104879. doi: 10.1016/j.tiv.2020.104879. Epub 2020 Apr 29.
Melanoma is a skin cancer with high invasive potential and high lethality. Considering that quinonemethide triterpenes are described as promising anticancer agents, the aim of this study was to evaluate the effect of 22β-hydroxytingenone (22-HTG) against human melanoma cells. Alamar blue assay was performed in order to evaluate its cytotoxic effect. Thus, subtoxic concentrations (1.0, 2.0, and 2.5 μM) were used to evaluate the effect of this compound on proliferation, migration, metabolism, and invasion. IC value against SK-MEL-28 cell line was 4.35, 3.72, and 3.29 μM after 24, 48, and 72 h of incubation, respectively. 22-HTG reduced proliferation, migration and invasion by melanoma cells, with decreased activity of metalloproteinases (MMP-2 and MMP-9). Futhermore, 22-HTG decreased expression of lactate dehydrogenase (LDHA), an enzyme associated with cell metabolism. Howerver, the small reduction in LDHA enzyme activity must have occurred by the cytotoxic effect of 22-HTG. According to the results, 22-HTG interferes with important characteristics of cancer, with anti-proliferative, and anti-invasive effect against melanoma cells. The data suggest that 22-HTG is an effective substance against melanoma cells and it should be considered as a potential anticancer agent.
黑色素瘤是一种具有高侵袭性和高致命性的皮肤癌。鉴于醌烯甲醚三萜被描述为有前途的抗癌药物，本研究旨在评估 22β-羟基金合欢酮（22-HTG）对人黑色素瘤细胞的作用。通过阿尔玛蓝法评估其细胞毒性作用。因此，使用亚毒性浓度（1.0、2.0 和 2.5μM）来评估该化合物对增殖、迁移、代谢和侵袭的影响。孵育 24、48 和 72 小时后，IC 值对 SK-MEL-28 细胞系分别为 4.35、3.72 和 3.29μM。22-HTG 降低了黑色素瘤细胞的增殖、迁移和侵袭，降低了金属蛋白酶（MMP-2 和 MMP-9）的活性。此外，22-HTG 降低了与细胞代谢相关的乳酸脱氢酶（LDHA）的表达。然而，LDHA 酶活性的微小降低可能是由于 22-HTG 的细胞毒性作用所致。根据结果，22-HTG 干扰了癌症的重要特征，对黑色素瘤细胞具有抗增殖和抗侵袭作用。数据表明，22-HTG 是一种有效的黑色素瘤细胞物质，应被视为一种潜在的抗癌药物。
