Dendrobeaniamine A,a new alkaloid from the Arctic marine bryozoan Dendrobeania murrayana

Abstract

The new guanidine alkaloid Dendrobeaniamine A (1) was isolated from the organic extract of the Arctic marine bryozoan Dendrobeania murrayana. The chemical structure of 1 was elucidated by spectroscopic experiments, including 1D and 2D NMR and HRESIMS analysis. Compound 1 is a lipoamino acid, consisting of a C₁₂ fatty acid anchored to the amino acid arginine. The bioactivity of 1 was evaluated using cellular and biochemical assays, but the compound did not show cytotoxic, antimicrobial, anti-inflammatory or antioxidant activities     

Complex Polypropionates from a South China Sea Photosynthetic Mollusk: Isolation and Biomimetic Synthesis Highlighting Novel Rearrangements

Placobranchus ocellatus is well known to produce diverse and complex γ‐pyrone polypropionates. In this study, the chemical investigation of P. ocellatus from the South China Sea led to the discovery and identification of ocellatusones A–D, a series of racemic non‐γ‐pyrone polyketides with novel skeletons, characterized by a bicyclo[3.2.1]octane ( 1 , 2 ), a bicyclo[3.3.1]nonane ( 3 ) or a mesitylene‐substituted dimethylfuran‐3(2H)‐one core ( 4 ). Extensive spectroscopic analysis, quantum chemical computation, chemical synthesis, and/or X‐ray diffraction analysis were used to determine the structure and absolute configuration of the new compounds, including each enantiomer of racemic compounds 1 – 4 after chiral HPLC resolution. An array of new and diversity‐generating rearrangements is proposed to explain the biosynthesis of these unusual compounds based on careful structural analysis and comparison with six known co‐occurring γ‐pyrones ( 5 – 10 ). Furthermore, the successful biomimetic semisynthesis of ocellatusone A ( 1 ) confirmed the proposed rearrangement through an unprecedented acid induced cascade reaction.     

β-secretase 1 inhibitory activity and AMP-activated protein kinase activation of Callyspongia samarensis extracts

Abstract

The methanolic extract of Callyspongia samarensis (MCS) significantly inhibited β-secretase 1 (IC₅₀ 99.82?µg/mL) in a dose-dependent manner and demonstrated a noncompetitive type of inhibition. Furthermore, it exhibited the highest AMPK activation (EC₅₀ 14.47?μg/mL) as compared with the standard, Aspirin (EC₅₀ >100?μg/mL). HPLC/ESI-MS analysis of MCS extract revealed 15 peaks, in which nine peaks demonstrated similar fragmentation pattern with the known compounds in literature and in database library: 5-aminopentanoic acid (1), 4-aminobutanoic acid (3), Luotonin A (4), (E)-3-(1H-imidazol-5-yl) prop-2-enoic acid (8), Galactosphingosine (10), D-sphingosine (11), 5,7,4′-trihydroxy-3′,5′-dimethoxyflavone (12), hydroxydihydrovolide (13), and 3,5-dibromo-4-methoxyphenylpyruvic acid (14); and 6 peaks are not identified (2, 5–7, 9, and 15). Acute oral toxicity test of MCS extract revealed that it is nontoxic, with an LD₅₀ of >2000?mg/kg. Assessment of BBB permeability of MCS extract showed that compound 15 was able to cross the BBB making it a suitable candidate for developing CNS drugs.     

GWC6066船用齿轮箱振动噪声分析及试验

采用弹簧单元模拟轮齿啮合刚度,杆单元模拟箱体间的联结螺栓,弹簧阻尼单元模拟滑动轴承和滚动轴承,建立由齿轮、传动轴、轴承和箱体等组成的GWC6066船用齿轮箱动态有限元分析模型及声学边界元模型;分析了齿轮箱在内部动态激励下的动态响应,预估了齿轮箱的振动烈度、结构噪声及空气噪声,并对齿轮箱进行实验模态分析及振动噪声测试,与仿真结果对比分析,二者吻合良好。     

Anti-Inflammatory Dysidazirine Carboxylic Acid from the Marine Cyanobacterium Caldora sp. Collected from the Reefs of Fort Lauderdale,Florida

Dysidazirine carboxylic acid (1) was isolated from the lipophilic extract of a collection of the benthic marine cyanobacterium Caldora sp. from reefs near Fort Lauderdale, Florida. The planar structure of this new compound was determined by spectroscopic methods and comparisons between HRMS and NMR data with its reported methyl ester. The absolute configuration of the single chiral center was determined by the conversion of 1 to the methyl ester and the comparison of its specific rotation data with the two known methyl ester isomers, 2 and 3. Molecular sequencing with 16S rDNA indicated that this cyanobacterium differs from Caldora penicillata (Oscillatoriales) and represents a previously undocumented and novel Caldora species. Dysidazirine (2) showed weak cytotoxicity against HCT116 colorectal cancer cells (IC₅₀ 9.1 µM), while dysidazirine carboxylic acid (1) was non-cytotoxic. Similar cell viability patterns were observed in RAW264.7 cells with dysidazirine only (2), displaying cytotoxicity at the highest concentration tested (50 µM). The non-cytotoxic dysidazirine carboxylic acid (1) demonstrated anti-inflammatory activity in RAW264.7 cells stimulated with LPS. After 24 h, 1 inhibited the production of NO by almost 50% at 50 µM, without inducing cytotoxicity. Compound 1 rapidly decreased gene expression of the pro-inflammatory gene iNOS after 3 h post-LPS treatment and in a dose-dependent manner (IC₅₀ ~1 µM); the downregulation of iNOS persisted at least until 12 h.     

Biotechnological Innovations from Ocean: Transpiring Role of Marine Drugs in Management of Chronic Disorders

Marine drugs are abundant in number, comprise of a diverse range of structures with corresponding mechanisms of action, and hold promise for the discovery of new and better treatment approaches for the management of several chronic diseases. There are huge reserves of natural marine biological compounds, as 70 percent of the Earth is covered with oceans, indicating a diversity of chemical entities on the planet. The marine ecosystems are a rich source of bioactive products and have been explored for lead drug molecules that have proven to be novel therapeutic targets. Over the last 70 years, many structurally diverse drug products and their secondary metabolites have been isolated from marine sources. The drugs obtained from marine sources have displayed an exceptional potential in the management of a wide array of diseases, ranging from acute to chronic conditions. A beneficial role of marine drugs in human health has been recently proposed. The current review highlights various marine drugs and their compounds and role in the management of chronic diseases such as cancer, diabetes, neurodegenerative diseases, and cardiovascular disorders, which has led to the development of new drug treatment approaches.     

智能PID控制器在船舶发电机电压控制中的应用

解决船舶发电机在负荷突变尤其是大负荷突变时能够稳定发电机端电压是控制系统需要解决的基本问题.为此提出和使用一种新型智能PID控制系统,其中PID控制器由三层前馈神经网络组成.利用神经网络的自学习能力,PID控制器的参数能够根据系统动态特性通过神经网络权系数进行自行调整,其特点是结构简单、工作稳定.仿真结果表明,该智能PID控制器比传统的PID控制器具有对扰动响应速度快和具有更好的控制效果和更好的鲁棒性,能更好地稳定船舶发电机端电压.该智能PID控制器已用于船舶发电机控制系统中,并取得满意的效果.     

码头岸壁的凹凸贴图绘制

介绍凹凸贴图的几种方法,详细分析了点乘凹凸贴图,特别是从物体空间到切线空间的变换过程.基于GPU顶点着色及像素着色,应用点乘凹凸贴图绘制码头岸壁,岸壁表面看上去凹凸不平,取得了逼真效果.为基于GPU进行船舶操纵模拟器的开发做了有益尝试.     

南大洋冰山特征初步分析

基于中国第19次南极科学考察从2002年12月至2003年1月在南大洋航行期间利用船舶雷达对航线两侧冰山的观测,给出了从雷达图像中获取冰山尺寸及其运动速度、方向的方法,获得了航线周围冰山的运动速度和尺寸分布.通过比较分析发现R oss海和W edde ll海冰山长度主要集中在880 m和1 180 m左右,冰山运动主要呈东北或西北向,运动速度与北极冰山的速度接近;P rydz湾的最大冰山尺寸则在65.4°S~68.2°S内随着接近Am ery冰架先增大后减小,符合一般物体崩塌的力学规律.另外,通过多元回归分析建立了冰山运动速度和同步测量的风速、流速间的关系,发现在当地典型情况下,风速对冰山运动的贡献是流速贡献的一半.     

CuPCr钢显微组织对全浸海水腐蚀行为的影响

为考察CuPCr型耐海水腐蚀钢不同显微组织的腐蚀行为,采用热轧后不同冷却方式分别获得贝氏体和铁素体+珠光体组织,进行模拟海水腐蚀的全浸加速腐蚀实验,并利用失重法测量腐蚀速率,采用SEM,XRD和电化学方法评价钢的腐蚀行为.结果表明:贝氏体组织能够在更短时间内形成比较致密的锈层,其耐蚀性能明显优于铁素体和珠光体组织.碳元素在贝氏体中的均匀分布减少了微电池数量,因而能够降低钢的腐蚀电流密度.