Evaluation of Antitumor,Immunomodulatory and Free Radical Scavenging Effects of A New Herbal Prescription Seaweed Complex Preparation

Seaweed Complex Preparation(SCP) is a clinical traditional Chinese medicine preparation which is composed of seven traditional Chinese herbs,and it has been used for treatment of lung cancer,liver cancer and digestive cancer.However,little information is available about the pharmacodynamic basis.The antitumor,immunomodulatory and free radical scavenging effects of SCP were evaluated in this study.Transplanted tumor in vivo method was used to determine the antitumor effect.The effects on splenocyte proliferation and phagocytosis of macrophages in tumor-bearing mice were measured by the MTT method and the phagocytizing cock red blood cell(CRBC) method respectively.The scavenging activities of SCP on DPPH and hydroxyl radicals in vitro were investigated.It was found that the medium-dose and high-dose of SCP could significantly inhibit the growth of transplanted hepatic tumor of murine hepatocarcinoma cell line H22,and promote proliferation of splenocytes and phagocytosis of macrophages.SCP possessed noticeable scavenging activities on DPPH and hydroxyl radicals.The antitumor effects of SCP might be achieved by improving immune system and scavenging free radicals,which is in accordance with the viewpoint of traditional Chinese medicine in promoting the body resistance and eliminating pathogenic factors for cancer treatment.

海洋来源(+)-sclerotiorin衍生物的半合成、抗结核活性与初步构效关系研究

目的结核病仍然是世界范围内一个重要的公共卫生问题,因此迫切需要寻找新型抗结核分子。以海洋天然产物(+)-sclerotiorin为原料半合成一系列衍生物,其中包含18个新化合物,通过考察它们的抗结核等活性,探究其初步构效关系。方法利用Mycobacterium marinum和Mycobacterium tuberculosis菌株对衍生物的生物活性进行测定。结果衍生物4、5、8~10和12的抗海分枝杆菌活性与阳性药相当,最低抑菌浓度(MIC90)在16.1~18.9μmol/L之间。此外,衍生物9、11、12和15也显示出中等的抗结核活性。初步构效关系表明喹啉、异喹啉、联苯和联苯醚等基团有利于提升(+)-sclerotiorin衍生物的抗结核活性。衍生物12在结核杆菌蛋白酪氨酸磷酸酶B抑制试验中显示出最强的活性,分子对接的结果表明,它与蛋白的Phe98残基之间存在苯环与苯环间的π-π相互作用。该研究证实了(+)-sclerotiorin衍生物作为抗结核候选药物的潜力。

1株红树来源真菌Penicillium sp.次级代谢产物及其生物活性研究

目的研究1株红树来源真菌Penicillium sp.中的次级代谢产物及生物活性。方法综合运用硅胶柱层析(CC)和半制备型高效液相色谱(HPLC)等方法分离纯化次级代谢产物,利用核磁共振(NMR)及质谱(MS)等现代波谱分析方法鉴定化合物结构,以斑马鱼血管抑制模型对其进行活性评价。结果在细胞毒活性的指导下,从Penicillium sp.中分离出抗肿瘤活性化合物brefeldin A,同时还分离出5个天然产物,分别是(+)-semivioxanthin(1)、(-)-st r iatisporolideA(2)、dibut ylphthalate(3)、bisdethiobis(methylthio)-acetylapoaranotin(4)和alternarosin A(5)。其中化合物1和3分别在1和10μg/mL浓度下显示出斑马鱼血管抑制活性,但同时会导致一定的脊柱弯曲。化合物3还具有抑制硅藻附着的潜在防污活性。结论化合物4和5为首次从真菌Penicillium sp.中分离获得。化合物1和3具有潜在的生物活性。