Synthesis,Anticancer Activity,Structure-Activity Relationship and Mechanistic Investigations of Falcarindiol Analogues

Forty samples of optically active falcarindiol analogues are synthesized by using the easily available C2 symmetric (R)- and (S)-1,1’-binaphth-2-ol (BINOL) in combination with Ti(OⁱPr)₄, Zn powder and EtI. Their anticancer activities on Hccc-9810, HepG2, MDA-MB-231, Hela, MG-63 and H460 cells are assayed to elucidate their structure-activity relationships. These results showed that the falcarindiol analogue (3R,8S)- 2 i with the terminal double bond has the most potent anti-proliferation effect on Hccc-9810 cells with IC₅₀ value of 0.46 μM. The falcarindiol analogue (3R,8S)- 2 i can induce obvious Hccc-9810 cell apoptosis in a concentration-dependent manner by Hoechst staining and flow cytometry analysis. The proposed mechanism suggests that the falcarindiol analogue (3R,8S)- 2 i increases LDH release and MDA content, and reduces the levels of SOD activity, which lead to the accumulation of oxidative stress and induce apoptosis in Hccc-9810 cells.     

石油降解菌ZS1对典型抗生素毒害作用的应激响应机制

为了解抗生素对石油降解菌的生态效应及微生物对典型抗生素毒害作用的应激响应机制，通过开展不同浓度典型抗生素对高效石油降解菌铜绿假单胞菌（ZS1）的毒性试验，研究了菌体细胞在3种不同种类抗生素（土霉素、红霉素、磺胺嘧啶）作用下的生长及毒理指标。结果表明，3种抗生素对ZS1有不同的抑菌效果，其中土霉素对ZS1活性的抑制程度最强，抑制率随着土霉素浓度的增大而明显上升，有显著的浓度-效应关系。研究了ZS1抗氧化酶（过氧化氢酶、过氧化物酶、超氧化物歧化酶）对抗生素的响应机制，结果表明ZS1受到污染时会通过产生抗氧化酶抵抗外界污染并维持细胞功能。     

Germination improves the functional properties of soybean and enhances soymilk quality

The effects of soybean variety and germination time on structural changes, antinutritional factor content, antioxidant activity of germinated soybean, and on the functional properties of soymilk were comprehensively investigated. The results showed that the antioxidant activity increased with increasing germination time. The content of antinutritional factors decreased with increasing germination time. Soybean varieties with the lowest tannin and trypsin inhibitor content were DN690 and HJ1. Lipoxygenase activity and phytic acid content showed no significant differences among soybean varieties. The content of α-helices and β-turns in soybean protein decreased with increasing germination time, while the content of β-sheets was increased. Soybean protein was progressively broken down into smaller molecular peptides during the germination process. The digestion and content of soluble protein in soymilk increased with germination. In summary, we show that germination is an effective, cheap, and green method that improves the functional properties of soybean and soymilk.     

贵长猕猴桃皮HPLC指纹图谱及抗氧化谱效关系研究

目的:研究贵长猕猴桃皮HPLC指纹图谱与抗氧化活性的关系。方法:采用高效液相色谱法建立10批不同来源地贵长猕猴桃皮的指纹图谱,采用SPSS 13.0进行样品聚类分析和主成分分析;并通过DPPH和ABTS法测定其抗氧化活性,以EC50与共有峰峰面积数据为基础,应用皮尔逊相关分析法和逐步回归分析法研究谱效关系。结果:建立了10批贵长猕猴桃皮HPLC指纹图谱,确定了14个共有峰,相似度均>0.90。采用对照品比对方法指认了其中6个峰:2号峰没食子酸,5号峰原儿茶酸,9号峰表儿茶素,10号峰二氢槲皮素,11号峰4-香豆酸,12号峰落新妇苷,样本可聚为3类。皮尔逊相关分析与逐步回归分析结果显示:5号峰(原儿茶酸)和9号峰(表儿茶素)峰面积变化与贵长猕猴桃皮抗氧化活性呈显著正相关,对其抗氧化活性贡献度较大。结论:贵长猕猴桃皮具有较高的体外抗氧化活性,抗氧化活性的物质基础初步确定为贵长猕猴桃皮开发利用、质量评价提供依据。     

Loliolide,a New Therapeutic Option for Neurological Diseases? In Vitro Neuroprotective and Anti-Inflammatory Activities of a Monoterpenoid Lactone Isolated from Codium tomentosum

Parkinsons Disease (PD) is the second most common neurodegenerative disease worldwide, and is characterized by a progressive degeneration of dopaminergic neurons. Without an effective treatment, it is crucial to find new therapeutic options to fight the neurodegenerative process, which may arise from marine resources. Accordingly, the goal of the present work was to evaluate the ability of the monoterpenoid lactone Loliolide, isolated from the green seaweed Codium tomentosum, to prevent neurological cell death mediated by the neurotoxin 6-hydroxydopamine (6-OHDA) on SH-SY5Y cells and their anti-inflammatory effects in RAW 264.7 macrophages. Loliolide was obtained from the diethyl ether extract, purified through column chromatography and identified by NMR spectroscopy. The neuroprotective effects were evaluated by the MTT method. Cells’ exposure to 6-OHDA in the presence of Loliolide led to an increase of cells’ viability in 40%, and this effect was mediated by mitochondrial protection, reduction of oxidative stress condition and apoptosis, and inhibition of the NF-kB pathway. Additionally, Loliolide also suppressed nitric oxide production and inhibited the production of TNF-α and IL-6 pro-inflammatory cytokines. The results suggest that Loliolide can inspire the development of new neuroprotective therapeutic agents and thus, more detailed studies should be considered to validate its pharmacological potential.