Cheng Ju-Hsin, Wu Ho-Cheng, Yen Chia-Hung, Hwang Tsong-Long, Ko Horng-Huey, Chang Hsun-Shuo
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
Plants (Basel). 2023 Aug 14;12(16):2943. doi: 10.3390/plants12162943.
Non-alcoholic fatty liver disease (NAFLD) is a type of steatosis caused by excess lipids accumulating in the liver. The prevalence of NAFLD has increased annually due to modern lifestyles and a lack of adequate medical treatment. Thus, we were motivated to investigate the bioactive components of Formosan plants that could attenuate lipid droplet (LD) accumulation. In a series of screenings of 3000 methanolic extracts from the Formosan plant extract bank for anti-LD accumulation activity, the methanolic extract of aerial parts of Thunb. showed excellent anti-LD accumulation activity. is an evergreen shrub on which only a few phytochemical and biological studies have been conducted. Here, one new flavonoid (), two new triterpenoids ( and ), and 35 known compounds (-) were isolated from the ethyl acetate layer of aerial parts of via a bioassay-guided fractionation process. Their structures were characterized by 1D and 2D NMR, UV, IR, and MS data. Among the isolated compounds, methyl pheophorbide a () efficiently reduced the normalized LD content to 0.3% with a concentration of 20 μM in AML12 cell lines without significant cytotoxic effects. 3--()-Caffeoyloleanolic acid () and methyl pheophorbide a () showed inhibitory effects on superoxide anion generation or elastase release in fMLP/CB-treated human neutrophils (IC < 3.0 μM); they displayed effects similar to those of the positive control, namely, LY294002. These findings indicate that can be used for developing a new botanical drug for managing LD accumulation and against inflammation-related diseases.
非酒精性脂肪性肝病（NAFLD）是一种由肝脏中脂质过度积累引起的脂肪变性。由于现代生活方式和缺乏足够的医学治疗，NAFLD的患病率逐年上升。因此，我们有动力去研究台湾植物中能够减轻脂滴（LD）积累的生物活性成分。在对来自台湾植物提取物库的3000种甲醇提取物进行的一系列抗LD积累活性筛选中，Thunb.地上部分的甲醇提取物表现出优异的抗LD积累活性。Thunb.是一种常绿灌木，目前仅对其进行了少量的植物化学和生物学研究。在此，通过生物活性导向的分级分离过程，从Thunb.地上部分的乙酸乙酯层中分离出一种新的黄酮类化合物（）、两种新的三萜类化合物（和）以及35种已知化合物（-）。它们的结构通过一维和二维核磁共振、紫外、红外和质谱数据进行了表征。在分离出的化合物中，脱镁叶绿酸a甲酯（）在AML12细胞系中以20 μM的浓度有效地将标准化LD含量降低至0.3%，且无明显细胞毒性作用。3--（）-咖啡酰齐墩果酸（）和脱镁叶绿酸a甲酯（）对fMLP/CB处理的人中性粒细胞中超氧阴离子的产生或弹性蛋白酶的释放具有抑制作用（IC<3.0 μM）；它们表现出与阳性对照LY294002相似的作用。这些发现表明，Thunb.可用于开发一种新的植物药，用于管理LD积累和对抗炎症相关疾病。
