Department of Biological Science and Technology, China Medical University, Taichung 404, Taiwan.
Phytochemistry. 2013 Oct;94:211-9. doi: 10.1016/j.phytochem.2013.05.022. Epub 2013 Jun 27.
Celastrus paniculatus is a traditional medicinal plant with diverse pharmacological activities. To identify its bioactive constituents, three new β-dihydroagarofuranoid sesquiterpenes were isolated from the whole plant, of which the major constituent is (1α,2α,8β,9β)-1,8-bis(acetyloxy)-2,9-bis(benzoyloxy)-14-hydroxy-β-dihydroagarofuran. It was assessed for its antiproliferative activity, and it suppressed the viability of MCF-7 breast cancer cells with an IC50 of 17±1μM. This growth inhibition was, in part, attributable to apoptosis. Moreover, this drug treatment led to LC3B-II accumulation, indicative of autophagy. Western blot analysis established its ability to target a broad range of signaling effectors related to survival and cell cycle progression, including Akt, NF-κB, p53, and MAP kinases. In addition, flow cytometry analysis indicates increased reactive oxygen species production in response to this compound. Taken together, these findings suggest a pleiotropic mode of mechanism that underlies the antiproliferative activity of this compound in MCF-7 breast cancer cells.
杠柳是一种具有多种药理活性的传统药用植物。为了鉴定其生物活性成分，从全株植物中分离得到了三种新的β-二氢沉香呋喃型倍半萜，其中主要成分是（1α,2α,8β,9β）-1,8-双（乙酰氧基）-2,9-双（苯甲酰氧基）-14-羟基-β-二氢沉香呋喃。评估其对 MCF-7 乳腺癌细胞的增殖活性，其对 MCF-7 乳腺癌细胞的半数抑制浓度（IC50）为 17±1μM。这种生长抑制部分归因于细胞凋亡。此外，这种药物处理导致 LC3B-II 积累，表明自噬。Western blot 分析确定了它能够靶向与存活和细胞周期进展相关的广泛信号效应物，包括 Akt、NF-κB、p53 和 MAP 激酶。此外，流式细胞术分析表明，该化合物能增加活性氧的产生。综上所述，这些发现表明，该化合物在 MCF-7 乳腺癌细胞中具有增殖活性的作用机制具有多效性。
