Department of Biomedical and Biotechnological Sciences, Section of Physiology, University of Catania, Via S. Sofia, 89, 95123, Catania, Italy.
Department of Drug Sciences, University of Catania, Via S. Sofia 64, 95125, Catania, Italy.
Chem Biol Interact. 2020 May 25;323:109075. doi: 10.1016/j.cbi.2020.109075. Epub 2020 Mar 27.
The use of orchids in herbal medicine has a very long history. Dendrobium species are known to produce a variety of secondary metabolites such as phenanthrens, bibenzyls, fluorenones and sesquiterpenes, and alkaloids and are responsible for their wide variety of medicinal properties. For decades, bibenzyls, which are the main bioactive components derived from Dendrobium species, have been subjected to extensive investigation as likely candidates for cancer treatment. The present study was undertaken to investigate the effect of moscatilin, a bibenzyl derivative from the orchid Dendrobium loddigesii on human melanoma cells. In A375 cells compound moscatilin showed a clear dose-response relationship in the range of 6.25-50 μM concentrations. In addition, we demonstrated an apoptotic response after treatment of cancer cells with this bibenzyl compound at 6.25 and 12.5 μM concentrations that probably involves PTEN activity, inhibition of Hsp70 expression and reactive oxygen species production. Alternatively, the inhibition of the caspase cascade at higher concentrations, 25 and 50 μM, correlated with additional reactive oxygen species increase, probably switched the mode of moscatilin-induced cell death from apoptosis to necrosis.
兰花在草药中的应用有着非常悠久的历史。已知石斛属植物能产生多种次生代谢产物,如菲类、联苄类、二苯并呋喃酮和倍半萜类以及生物碱,这些物质赋予了它们广泛的药用特性。几十年来,从石斛属植物中提取的主要生物活性成分联苄类化合物一直被广泛研究,作为癌症治疗的候选药物。本研究旨在探讨从兰花石斛中提取的联苄衍生物莫斯卡汀对人黑色素瘤细胞的影响。在 A375 细胞中,该化合物在 6.25-50 μM 浓度范围内表现出明显的剂量反应关系。此外,我们还证明了在 6.25 和 12.5 μM 浓度下用这种联苄化合物处理癌细胞后会产生凋亡反应,这可能涉及到 PTEN 活性、Hsp70 表达抑制和活性氧物质的产生。相反,在更高浓度(25 和 50 μM)下,半胱天冬酶级联的抑制与活性氧物质的进一步增加相关,这可能使莫斯卡汀诱导的细胞死亡模式从凋亡转变为坏死。