深海芽孢杆菌E401B03 次生代谢产物分离和结构鉴定

利用硅胶柱、凝胶柱及高效液相(HPLC)等色谱方法,对采自中国南海的深海芽孢杆菌 E401B03发酵液的乙酸乙酯相浸膏进行了分离,通过1H-NMR、13C-NMR、EIMS 等方法鉴定了7个化合物: N-苯乙基乙酰胺、3-(羟基乙酰基)-吲哚、3-(2-羟基乙基)-吲哚、环(缬-缬)二肽、尿嘧啶、胸腺嘧啶、对羟基苯甲醛     

Effects of alga polysaccharide capsule shells on in-vivo bioavailability and disintegration

Gelatin has been used in hard capsule shells for more than a century, and some shortcomings have appeared, such as high moisture content and risk of transmitting diseases of animal origin to people. Based on available studies regarding gelatin and vegetable shells, we developed a new type of algal polysaccharide capsule (APPC) shells. To test whether our products can replace commercial gelatin shells, we measured in-vivo plasma concentration of 12 selected volunteers with a model drug, ibuprofen, using high performance liquid chromatography (HPLC), by calculating the relative bioavailability of APPC and Qualicaps referenced to gelatin capsules and assessing bioequivalence of the three types of shells, and calculated pharmacokinetic parameters with the software DAS 2.0 (China). The results show that APPC shells possess bioequivalence with Qualicaps and gelatin shells. Moreover, the disintegration behavior of four types of shells (APPC, Vegcaps , Qualicaps and gelatin shells) with the content of lactose and radioactive element (99mTc) was observed via gamma-scintigraphic images. The bioavailability and gamma-scintigraphic studies showed that APPC was not statistically different from other vegetable and gelatin capsule shells with respect to in-vivo behavior. Hence, it can be concluded that APPCs are exchangeable with other vegetable and gelatin shells.     

Antithrombotic effects of bromophenol,an alga-derived thrombin inhibitor

Thrombin,the ultimate proteinase of the coagulation cascade,is an attractive target for the treatment of a variety of cardiovascular diseases.A bromophenol derivative named (+)-3-(2,3-dibromo-4,5-dihydroxy-phenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroiso-benzofuran 1,isolated from the brown alga Leathesia nana exhibited significant thrombin inhibitory activity.In this study,we investigated the inhibition of human thrombin in vitro with this bromophenol derivative,and its antithrombotic efficacy in vivo using th...     

Antithrombotic effects of bromophenol, an alga-derived thrombin inhibitor

Thrombin, the ultimate proteinase of the coagulation cascade, is an attractive target for the treatment of a variety of cardiovascular diseases. A bromophenol derivative named (+)-3-(2,3-dibromo-4, 5-dihydroxy-phenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroiso-benzofuran 1, isolated from the brown alga Leathesia nana exhibited significant thrombin inhibitory activity. In this study, we investigated the inhibition of human thrombin in vitro with this bromophenol derivative, and its antithrombotic efficacy in vivo using the arteriovenous shunt model and the ferric chloride-induced arterial thrombosis model in rats. The results show that the bromophenol derivative is a potential inhibitor of thrombin (IC₅₀=1.03 nmol/L). In antithrombotic experiments in vivo, the bromophenol derivative also shows good effect comparing with the control group. These data indicate that the bromophenol derivative is a potential drug for prophylaxis and the treatment of thrombotic diseases.