Yang Heejung, Choi Mina, Lee Dong Young, Sung Sang Hyun
College of Pharmacy, Kangwon National University, Chuncheon, Republic of Korea.
College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University, Seoul, Republic of Korea.
Pharmacogn Mag. 2017 Apr-Jun;13(50):293-299. doi: 10.4103/0973-1296.204549. Epub 2017 Apr 18.
Obesity is a pathological state caused by abnormal or excessive accumulation of fat. JACQ., known as West Indian mahogany, is a medium-sized semi-evergreen tree belonging to Meliaceae. Their seeds are used in Indonesian folk medicine as a treatment for hypertension, diabetes, malaria, and it also has anti-feedant activities. The major components of are B, D-seco limonoids, a type of irregular triterpenes are well known.
We tried to find the bioactive components, which have the inhibitory activity on adipocyte differentiation from the seeds of .
3T3-L1 cells, derived from mouse preadipocyte, are widely used in studying adipogenesis process. In this study, we used 3T3-L1 cells to find natural products with the inhibitory activity on adipocyte differentiation. seeds were dried and extracted with 100% MeOH.
The methanolic extract was fractionated by bioassay-guided method to give nine B, D-seco limonoids (1-9) with slight structural modifications. Among nine compounds, compounds 4, 6 and 8 exhibited significant inhibitory effects of cell differentiation on 3T3-L1 cells. Those compounds have tigloyl residue at C-3 in common. Besides, compounds with no tigloyl residue at C-3 showed insignificant effect. Nevertheless, not all compounds with tigloyl residue at C-3 exerted significant inhibitory effect.
These results suggested that tigloyl residue at C-3 may play a role in the anti-proliferative activity on a dipogenesis and the refined extract of may have a potential to be developed as a therapeutic agent to treat obesity.
Nine irregular seco-limonoids were isolated from .Total extract and CHCl3 fraction of showed the significant inhibitory activities on 3T3-L1 cell differentiation.A tigloyl residue at C-3 in an aglycone may play a role in the anti-proliferative activity on adipogenesis.
肥胖是一种由脂肪异常或过度积累引起的病理状态。JACQ.，即西印度桃花心木，是一种属于楝科的中型半常绿乔木。其种子在印度尼西亚民间医学中用于治疗高血压、糖尿病、疟疾，并且还具有拒食活性。其主要成分是B、D-裂环柠檬苦素类化合物，这是一类众所周知的不规则三萜。
我们试图从JACQ.种子中找到对脂肪细胞分化具有抑制活性的生物活性成分。
源自小鼠前脂肪细胞的3T3-L1细胞被广泛用于研究脂肪生成过程。在本研究中，我们使用3T3-L1细胞来寻找对脂肪细胞分化具有抑制活性的天然产物。将JACQ.种子干燥并用100%甲醇提取。
通过生物测定导向法对甲醇提取物进行分离，得到9种结构略有修饰的B、D-裂环柠檬苦素类化合物（1-9）。在这9种化合物中，化合物4、6和8对3T3-L1细胞的细胞分化表现出显著的抑制作用。这些化合物在C-3位均具有惕各酰基残基。此外，在C-3位没有惕各酰基残基的化合物显示出不显著的效果。然而，并非所有在C-3位具有惕各酰基残基的化合物都具有显著的抑制作用。
这些结果表明，C-3位的惕各酰基残基可能在对脂肪生成的抗增殖活性中起作用，并且JACQ.的精制提取物可能有潜力被开发为治疗肥胖的治疗剂。
从JACQ.中分离出9种不规则裂环柠檬苦素类化合物。JACQ.的总提取物和CHCl3馏分对3T3-L1细胞分化显示出显著的抑制活性。苷元中C-3位的惕各酰基残基可能在对脂肪生成的抗增殖活性中起作用。
