来自山竹果提取物的具有生物活性的多异戊烯基化二苯甲酮衍生物。
Bioactive polyprenylated benzophenone derivatives from the fruits extracts of Garcinia xanthochymus.
作者信息
Youn Ui Joung, Sripisut Tawanun, Miklossy Gabriella, Turkson James, Laphookhieo Surat, Chang Leng Chee
机构信息
Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, Hilo, HI 96720, United States; Division of Life Sciences, Korea Polar Research Institute, KIOST, Incheon 21990, Republic of Korea.
Natural Products Research Laboratory, School of Science, Mae Fah Luang University, Tasud, Muang, Chiang Rai 57100, Thailand.
出版信息
Bioorg Med Chem Lett. 2017 Aug 15;27(16):3760-3765. doi: 10.1016/j.bmcl.2017.06.073. Epub 2017 Jul 1.
Two new polycyclic prenylated xanthones (1 and 2) and a new phenylpropanoid glycoside (3), along with seven known compounds (4-10) were isolated from the fruits of Garcinia xanthochymus. The structures were elucidated by 1D- and 2D-NMR, and HRMS experiments. The isolates were evaluated for their inhibitory effects against the viability of U251MG glioblastoma and MDA-MB-231 breast cancer cells that harbor an aberrantly active signal transducer and exhibit activation of transcription 3 (STAT3), and compared to normal NIH3T3 mouse fibroblasts. Among the isolates, compounds 1, 2, 5, and 6-9 inhibited the viability of glioma cancer cells with IC values in the range of 1.6-6.5μM. Furthermore, treatment of U251MG with 6 and 7 inhibited intracellular STAT3 tyrosine phosphorylation and glioma cell migration in vitro, respectively.
从山竹子果实中分离出两种新的多环异戊烯基呫吨酮（1和2）、一种新的苯丙素苷（3）以及七种已知化合物（4 - 10）。通过一维和二维核磁共振以及高分辨质谱实验对其结构进行了阐明。评估了这些分离物对U251MG胶质母细胞瘤和MDA - MB - 231乳腺癌细胞活力的抑制作用，这两种癌细胞具有异常活跃的信号转导子并表现出转录激活因子3（STAT3）的激活，同时与正常的NIH3T3小鼠成纤维细胞进行了比较。在这些分离物中，化合物1、2、5以及6 - 9对胶质瘤癌细胞活力具有抑制作用，IC值在1.6 - 6.5μM范围内。此外，用化合物6和7处理U251MG细胞分别抑制了细胞内STAT3酪氨酸磷酸化和体外胶质瘤细胞迁移。
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