Department of Oriental Pharmacy and Wonkwang-Oriental Medicines Research Institute, Wonkwang University, Iksan 570-749, Korea.
Department of Pharmacy, College of Pharmacy, Wonkwang University, Iksan 570-749, Korea.
Molecules. 2022 Jan 20;27(3):676. doi: 10.3390/molecules27030676.
Ponciri Fructus, a crude drug consisting of the dried immature fruits of (L.) Raf., is a popular folk medicine used for the treatment of allergy and gastrointestinal disorders in Korea and China. In this study, the anti-adipogenic activity of extracts and isolated compounds were evaluated using 3T3-L1 preadipocytes.
Dried immature fruits were extracted and fractionated into -hexane, ethyl acetate (EtOAc), -butanol and water-soluble fractions. The ethanol extract and fractions were tested for anti-adipogenic activity in the 3T3-L1 cell line. The active fractions (-hexane and EtOAc fractions) were further subjected to chromatographic techniques to isolate and identify active compounds. Furthermore, the isolated compounds were evaluated for their anti-adipogenic activity.
Altogether, seven compounds, including two flavonoids, one phytosteroid and four coumarin derivatives, were isolated. Ethanol extract, -hexane fraction, EtOAc fraction and three isolated compounds (phellopterin, oxypeucedanin and poncirin) showed significant anti-adipogenic activity as observed by reduced lipid deposition in differentiated 3T3-L1 cells. Further, oxypeucedanin downregulated the key adipogenic markers, such as peroxisome proliferator-activated receptors proteins (PPAR-), sterol response element binding proteins-1 (SREBP-1), CCAAT/enhancer binding proteins- (C/EBP-), adipocyte-specific lipid binding proteins (FABP-4), adipocyte fatty acid binding proteins (aP2), lipoprotein lipase (LPL) and leptin.
This study indicated that the ethanol extract, hexane fraction and ethyl acetate fraction of fruits possess strong anti-adipogenic activity, containing the active compounds such as phellopterin, oxypeucedanin and poncirin. Further research is recommended to explore their efficacy and safety in animal and clinical models.
枳实为芸香科酸橙（Citrus aurantium L.）的未成熟干燥果实，是一种民间药物，在韩国和中国被用于治疗过敏和胃肠道疾病。本研究采用 3T3-L1 前脂肪细胞评价其提取物及单体化合物的抗脂肪生成活性。
干燥的未成熟果实经提取和溶剂分配，得到正己烷、乙酸乙酯（EtOAc）、正丁醇和水溶性部位。用 3T3-L1 细胞系检测乙醇提取物和各部位的抗脂肪生成活性。对具有活性的部位（正己烷和 EtOAc 部位）进行进一步的色谱分离，以鉴定活性化合物。此外，对分离得到的化合物进行抗脂肪生成活性评价。
共分离鉴定了 7 种化合物，包括 2 种黄酮类化合物、1 种植物甾醇和 4 种香豆素衍生物。乙醇提取物、正己烷部位、EtOAc 部位和 3 种分离得到的化合物（补骨脂素、氧化前胡素和枳实苷）显著抑制 3T3-L1 细胞分化过程中的脂滴形成，表现出抗脂肪生成活性。进一步研究表明，氧化前胡素下调过氧化物酶体增殖物激活受体蛋白（PPAR-γ）、固醇调节元件结合蛋白-1（SREBP-1）、CCAAT/增强子结合蛋白（C/EBP-α）、脂肪细胞特异性脂结合蛋白（FABP-4）、脂肪细胞脂肪酸结合蛋白（aP2）、脂蛋白脂肪酶（LPL）和瘦素等关键脂肪生成标志物的表达。
本研究表明，枳实的乙醇提取物、正己烷部位和 EtOAc 部位具有较强的抗脂肪生成活性，其中含有补骨脂素、氧化前胡素和枳实苷等活性成分。建议进一步研究其在动物和临床模型中的疗效和安全性。
