红树林真菌草酸青霉(092007)的环二肽类成分

目的研究海南文昌红树林真菌草酸青霉(Penicillium oxalicum)的代谢产物,寻找新的抗肿瘤活性化合物。方法利用硅胶、Sephadex LH-20、ODS柱色谱及制备型高效液相色谱等方法进行分离,通过化合物的理化性质及各种波谱技术鉴定它们的结构,采用MTT法评价化合物体外细胞毒活性。结果从真菌菌丝体的丙酮提取物中分离得到6个环二肽类化合物,鉴定其结构分别为:环(苯丙-异亮)二肽cyclo-(Phe-Ile)](1)、环(苯丙-缬)二肽cyclo-(Phe-Val)](2)、环(异亮-亮)二肽cyclo-(Ile-Leu)](3)、环(缬-缬)二肽cyclo-(Val-Val)](4)、环(脯-缬)二肽cyclo-(Pro-Val)](5)、环(脯-甘)二肽cyclo-(Pro-Gly)](6)。体外活性表明:化合物1、3和5在50μg.mL-1下对肝癌细胞HepG-Ⅱ的抑制率分别为31%、32%、17%,对前列腺癌细胞LNCaP抑制率分别为50%、43%、53%。结论这些化合物均为首次从该属真菌的代谢产物中分离得到,其中化合物2、3和5具有一定的细胞毒活性。

Cyclic dipeptide constituents from the mangrove fungus Penicillium oxalicum (No. 092007)

Objective To study the metabolites of mangrove fungus Penicillium oxalicum from the south China sea and search for new anti-tumor compounds.Methods Compounds were isolated by silica gel,ODS column chromatography,Sephadex LH-20 column chromatography and reversed-phase HPLC purification.Structural elucidation was achieved by physico-chemical constants and spectroscopic analysis.MTT assay was used to evaluate the bioactivities in vitro.Results Six cyclic dipeptides were isolated from the acetone extracts of mycelium of fungus and elucidated as cyclo-(Phe-Ile)(1),cyclo-(Phe-Val)(3),cyclo-(Ile-Leu)(3),cyclo-(Val-Val)(4),cyclo-(Pro-Val)(5),cyclo-(Pro-Gly)(6).Coumpouds 2,3 and 5 could evidently inhibit the growth of cancer cell lines HepG Ⅱ and LNCaP at the concentration of 50 μg·mL-1.Conclusions All of Compounds are obtained from the marine fungus for the fist time.Compounds 2,3 and 5 show cytotoxic activity in vitro.