DBT-AIST International Laboratory for Advanced Biomedicine (DAILAB), National Institute of Advanced Industrial Science and Technology (AIST), Tsukuba, Ibaraki 305 8565, Japan.
School of Biotechnology, Jawaharlal Nehru University, New Delhi 110 067, India.
Int J Oncol. 2018 Mar;52(3):925-932. doi: 10.3892/ijo.2018.4249. Epub 2018 Jan 22.
Propolis, a resinous substance collected by honeybees by mixing their saliva with plant sources, including tree bark and leaves and then mixed with secreted beeswax, possesses a variety of bioactivities. Whereas caffeic acid phenethyl ester (CAPE) has been recognized as a major bioactive ingredient in New Zealand propolis, Brazilian green propolis, on the other hand, possesses artepillin C (ARC). In this study, we report that, similar to CAPE, ARC docks into and abrogates mortalin-p53 complexes, causing the activation of p53 and the growth arrest of cancer cells. Cell viability assays using ARC and green propolis-supercritical extract (GPSE) revealed higher cytotoxicity in the latter, supported by nuclear translocation and the activation of p53. Furthermore, in vivo tumor suppression assays using nude mice, we found that GPSE and its conjugate with γ cyclodextrin (γCD) possessed more potent anticancer activity than purified ARC. GPSE‑γCD may thus be recommended as a natural, effective and economic anticancer amalgam.
蜂胶是蜜蜂通过将其唾液与植物来源(包括树皮和树叶)混合,然后与分泌的蜂蜡混合而收集的一种树脂状物质,具有多种生物活性。咖啡酸苯乙酯 (CAPE) 已被确认为新西兰蜂胶和巴西绿蜂胶的主要生物活性成分,而另一方面,巴西绿蜂胶含有 artepillin C (ARC)。在这项研究中,我们报告说,与 CAPE 相似,ARC 与 mortalin-p53 复合物结合并使其失活,导致 p53 激活和癌细胞生长停滞。使用 ARC 和绿蜂胶超临界提取物 (GPSE) 的细胞活力测定显示后者具有更高的细胞毒性,这得到了 p53 核转位和激活的支持。此外,在裸鼠体内肿瘤抑制试验中,我们发现 GPSE 及其与 γ 环糊精 (γCD) 的缀合物比纯化的 ARC 具有更强的抗癌活性。因此,GPSE-γCD 可被推荐为一种天然、有效且经济的抗癌混合物。