Marine Drugs Research Center, College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.
College of Pharmacy and Advanced Institute for Medical Sciences, Dalian Medical University, Dalian 116044, China.
Mar Drugs. 2018 Dec 6;16(12):488. doi: 10.3390/md16120488.
Ten new triterpenoid compounds with structure diversity of the C-17 side-chain, including nine tirucallanes, named xylocarpols A⁻E (⁻) and agallochols A⁻D (⁻), and an apotirucallane, named 25-dehydroxy protoxylogranatin B (), were isolated from the mangrove plants , , and . The structures of these compounds were established by HR-ESIMS and extensive one-dimensional (1D) and two-dimensional (2D) NMR investigations. The absolute configurations of and were unequivocally determined by single-crystal X-ray diffraction analyses, conducted with Cu K radiation; whereas those of , ⁻ were assigned by a modified Mosher's method and the comparison of experimental electronic circular dichroism (ECD) spectra. Most notably, , , , and displayed potent activation effects on farnesoid⁻X⁻receptor (FXR) at the concentration of 10.0 μM; exhibited very significant agonistic effects on pregnane⁻X⁻receptor (PXR) at the concentration of 10.0 nM.
从红树林植物 和 中分离得到了 10 种具有 C-17 侧链结构多样性的新三萜类化合物，包括 9 种桐甾烷，分别命名为木卡波醇 A⁻E（⁻）和 agallocols A⁻D（⁻），以及一种 apotirucallane，命名为 25-去羟基原桐烷 B（）。这些化合物的结构通过高分辨电喷雾电离质谱（HR-ESIMS）和广泛的一维（1D）和二维（2D）NMR 研究确定。通过单晶 X 射线衍射分析，使用 Cu K 辐射，明确确定了 和 的绝对构型；而 、 ⁻的绝对构型则通过改进的 Mosher 法和实验电子圆二色谱（ECD）光谱的比较来确定。值得注意的是，化合物 、 、 、和 在 10.0 μM 的浓度下对法尼醇 X 受体（FXR）表现出强烈的激活作用；在 10.0 nM 的浓度下，化合物 对孕烷 X 受体（PXR）表现出非常显著的激动作用。
