Fujian Provincial Key Laboratory of Innovative Drug Target, School of Pharmaceutical Sciences, Xiamen University, Xiamen, People's Republic of China.
Nat Prod Res. 2021 Nov;35(22):4534-4541. doi: 10.1080/14786419.2020.1739044. Epub 2020 Mar 12.
Descaudatine A (), an undescribed phenolic glycoside, along with a known analogue () and ten flavonoids (), were isolated from the whole plant of . Compounds and exhibited potent antioxidant activities with the IC of 58.59 μM and 31.31 μM, respectively, which were approached to that of the positive control Vitamin C (IC = 46.32 μM). Meanwhile, showed moderate antioxidant activity with the IC of 173.9 μM. Besides, compounds and inhibited the proliferation of HeLa cells with IC values of 56.14 μM and 69.04 μM, respectively. Further studies indicated that and could dose-dependently induce PARP cleavage and might trigger caspase-3, 8, 9 activation to induce apoptosis. RXRα is an ideal anticancer target of nuclear receptor. The reporter gene assay of RXRα indicated that and could inhibited the 9--RA induced RXRα transcription in a concentration-dependent manner.
Descaudatine A (), 一种未被描述的酚糖苷,以及一个已知的类似物 () 和十个黄酮类化合物 (),从 的全植物中分离得到。化合物 和 表现出很强的抗氧化活性,IC 分别为 58.59 μM 和 31.31 μM,接近阳性对照维生素 C (IC = 46.32 μM)。同时, 表现出中等强度的抗氧化活性,IC 为 173.9 μM。此外,化合物 和 对 HeLa 细胞的增殖具有抑制作用,IC 值分别为 56.14 μM 和 69.04 μM。进一步的研究表明, 和 可以剂量依赖性地诱导 PARP 切割,并可能触发 caspase-3、8、9 的激活诱导细胞凋亡。RXRα 是核受体理想的抗癌靶点。RXRα 的报告基因试验表明, 和 可以浓度依赖方式抑制 9--RA 诱导的 RXRα 转录。