College of Pharmacy, Yeungnam University, Gyeongbuk, South Korea.
Phytother Res. 2010 Jun;24 Suppl 2:S225-8. doi: 10.1002/ptr.3149.
Inhibition of fatty acid synthase (FAS) has been proposed to be a new therapeutic target for the treatment of cancer and obesity. In our preliminary screening study on the FAS inhibitory activity, a n-hexane soluble fraction prepared from the fruit of Schisandra chinensis (Schisandraceae) was found to inhibit FAS activity at 100 microg/mL. Nine dibenzocyclooctadiene lignans were isolated from the active fraction and were evaluated for their inhibitory effect on FAS for the first time. The compounds possessing a benzoyl or tigloyl group in the dibenzocyclooctadiene skeleton entirely inhibited the FAS activity in a dose dependent manner. The findings may be partially related to the anticancer effect of the medicinal plant, suggesting a further study on the anticancer potential of dibenzocyclooctadiene derivatives.
脂肪酸合酶（FAS）的抑制作用被认为是治疗癌症和肥胖的新的治疗靶点。在我们对 FAS 抑制活性的初步筛选研究中，从五味子（五味子科）的果实中制备的正己烷可溶部分在 100μg/ml 时就显示出抑制 FAS 活性的作用。从活性部分分离出 9 种二苯并环辛二烯木脂素，并首次对它们抑制 FAS 的作用进行了评价。具有苯甲酰基或丁烯二酰基的二苯并环辛二烯骨架的化合物完全地以剂量依赖的方式抑制 FAS 活性。这一发现可能与药用植物的抗癌作用部分相关，提示对二苯并环辛二烯衍生物的抗癌潜力进行进一步的研究。
