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中国化学会第十二届全国天然有机化学学术会议

作者： Xiang Gao zhan-lin Li Hui-Ming Hua Da-Hong Li Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education Shenyang Pharmaceutical University

Natural products have long been a constant source for both novel molecular skeleton and superior therapeutic *** light of recent discoveries,ent-kaurane diterpenoids which exhibit a broad range of biological effects including anticancer and anti-inflammatory activities,pose enormous potential to serve as a promising candidate for drug *** them,enmein-type6,7-seco-ent-kaurane diterpenoids have unique chemical structures and display significant biological *** order to further enhance the anti-cancer efficacy and improve drug properties of enmein,combination principle is applied with a group of established DNA alkylating agents,through ester linker to afford a series of novel *** this strategy of chemical modifications,several novel compounds were acquired with enhanced anticancer activity,reduced systemic toxicity,and high selectivity for chemotherapy of cancer.

关键词： Enmein-type Diterpenoid Anticancer

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Effects of flavonolignans from Silybun marianum on diabetes

Effects of flavonolignans from Silybun marianum on diabetes

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中国化学会第十二届全国天然有机化学学术会议

作者： Jia Li zhan-lin Li Hui-Ming Hua Da-Hong Li Key Laboratory of Structure-Based Drug Design ＆ Discovery of Ministry of Education Shenyang Pharmaceutical University

Diabetes mellitus is a common metabolic disease characterized by *** there are several treatments for it,such as insulin,insulin secretagogues,insulin sensitizers,and oral hypoglycemic agents, many efforts are still needed to discover new drugs for diabetes treatment,especially medicinal plant *** regulate a variety of cell-signaling pathways as well as inhibiting metabolism of arachidonic acid,thereby reducing the formation of pro-inflammatory *** expected to isolate flavonolignans from Silybun marianum and study the effects on *** seeds of Silybum marianum（L.） *** extracted with 95% *** then we used various chromatographic methods such as silica gel,Sephadex LH-20,opening ODS column chromatography,and semi-preparative HPLC to isolate *** isolates were evaluated for their antidiabetic *** have obtained 8 flavonolignans from Silybun marianum and found flavonolignans exhibited significant α-glucosidase inhibitory activities and PTP1 B inhibitory *** research on Silybun marianum was limited to its hepato-protective effects.A new direction is provided for the treatment of diabetes.

关键词： Silybun marianum Diabetes Flavonolignan

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Synthesis and biological evaluation of brefeldin A derivatives as potential anticancer agents

Synthesis and biological evaluation of brefeldin A derivativ...

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中国化学会第十二届全国天然有机化学学术会议

作者： Tong Han Da-Hong Li zhan-lin Li Hui-Ming Hua Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education Shenyang Pharmaceutical University

Brefeldin A is a 16-membered macrolide antibiotic which was first isolated from Penicillium *** shows a wide variety of biological properties,including antitumor,antifungal,antimitotic and antiviral *** aim of this study was to synthesis brefeldin A derivatives and investigate their antitumor activity.A series of conjugates of brefeldin A were obtained by introducing a variety of active small molecular fragments at 4-OH or 7-OH *** cytotoxic activities of target hybrids against three human cancer cell lines(HL-60 human leukemic cell line,PC-3 human prostatic cancer cell line and Bel-7402 hepatocellular carcinoma cell line),the multidrug resistant cell line Bel-7402/5-FU and the human normal hepatic cell line(L-O2) were screened and compared with lead compound BFA and positive control 5-FU in each *** all the target compounds showed cytotoxic activities against one or more cell ***,one compound displayed the most potent cytotoxic activity among all the ***,it displayed lower toxicity than brefeldin A(IC <0.001 μM) against normal human liver L-O2 cells,showing good selectivity between normal and malignant liver *** summary,novel derivatives of BFA were obtained by introducing molecular fragments at 4-OH and/or *** deserved further investigation as potential chemotherapeutic agents for cancer.

关键词： Brefeldin A Antiproliferative activity Selectivity

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Coexistence of natural gas hydrate,free gas and water in the gas hydrate system in the Shenhu Area,South China Sea

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China Geology 2020年第2期3卷 210-220页

作者： Xu-wen Qin Jing-an Lu Hai-long Lu Hai-jun Qiu Jin-qiang Liang Dong-ju Kang lin-sen zhan Hong-feng Lu Zeng-gui Kuang China Geological Survey Ministry of Natural ResourcesBeijing 100037China Guangzhou Marine Geological Survey China Geological SurveyMinistry of Natural ResourcesGuangzhou 510075China Beijing International Center for Gas Hydrate Peking UniversityBeijing 100871China Southern Marine Science and Engineering Guangdong Laboratory(Guangzhou) Guangzhou 510000China

Shenhu Area is located in the Baiyun Sag of Pearl River Mouth Basin,which is on the northern continental slope of the South China *** hydrates in this area have been intensively investigated,achieving a wide coverage of the three-dimensional seismic survey,a large number of boreholes,and detailed data of the seismic survey,logging,and core *** the beginning of 2020,China has successfully conducted the second offshore production test of gas hydrates in this *** this paper,studies were made on the structure of the hydrate system for the production test,based on detailed logging data and core analysis of this *** to the results of nuclear magnetic resonance(NMR)logging and sonic logging of Well GMGS6-SH02 drilled during the GMGS6 Expedition,the hydrate system on which the production well located can be divided into three layers:(1)207.8–253.4 mbsf,45.6 m thick,gas hydrate layer,with gas hydrate saturation of 0–54.5%(31%av.);(2)253.4–278 mbsf,24.6 m thick,mixing layer consisting of gas hydrates,free gas,and water,with gas hydrate saturation of 0–22%(10%av.)and free gas saturation of 0–32%(13%av.);(3)278–297 mbsf,19 m thick,with free gas saturation of less than 7%.Moreover,the pore water freshening identified in the sediment cores,taken from the depth below the theoretically calculated base of methane hydrate stability zone,indicates the occurrence of gas *** these data reveal that gas hydrates,free gas,and water coexist in the mixing layer from different aspects.

关键词： Mixing layer Gas hydrate NMR logging Sonic logging Core analysis Oil gas exploration engineering Shenhu Area South China Sea China

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Synthesis and biological evaluation of scutellarin-nitric oxide donor hybrids as potential antitumor agents

Synthesis and biological evaluation of scutellarin-nitric ox...

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中国化学会第十一届全国天然有机化学学术会议

作者： Tong Han Da-Hong Li zhan-lin Li Hui-Ming Hua Key Laboratory of Structure-Based Drug Design＆Discovery Ministry of Educationand School of Traditional Chinese Materia MedicaShenyang Pharmaceutical University

＜正＞Scutellarin is a main effective flavonoid component of breviscapine,which is an extract from the dried whole plant of Erigeron breviscapus（Vant.）*** exhibits a variety of biological effects,such as free radica...

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Synthesis of evodiamine derivatives as potential anticancer agents

Synthesis of evodiamine derivatives as potential anticancer ...

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中国化学会第十二届全国天然有机化学学术会议

作者： Xu Hu zhan-lin Li Da-Hong Li Hui-Ming Hua Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education Shenyang Pharmaceutical University

Hydrogen sulfide(H2 S) has been recognized as an important cellular signaling molecule with a wide range of physiological functions.H S donors have reported antiangiogenic effects with phosphorylation of the protein kinase Akt being implicated in the treatment of ***,a quinolone alkaloid is isolated from the fruits of traditional Chinese herb Evodiae fructus,which is widely used for treating diverse human *** evodiamine exhibited safe and broad antitumor activity,the development of evodiamine for cancer therapy was stunted by its relatively moderate ***,it is very necessary to develop novel evodiamine derivatives with improved anti cancer profile by *** to the combinational principle,we designed two series of evodiamine derivatives at N-13 based on two kinds of exogenous H2 S release donors ADTOH and α-thioctic *** synthesized sixteen novel H2 S-releasing derivatives of *** the antitumor activity was *** results showed that evodiamine/H2 S donor hybrids could exhibit potent anticancer effect,leading to a higher antiproliferative efficacy,a broader therapeutic scope,and a lower systemic ***,the potent anti-proliferative activities in vitro and mechanistic studies warranted further preclinical investigations for potential novel anticancer *** vivo study is now carrying out.

关键词： Evodiamine Hydrogen sulfide Anticancer In vivo study

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膨胀土裂隙的工程特性研究

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岩土力学 2014年第7期35卷 1825-1830,1836页

作者：龚壁卫程展林胡波赵亮长江科学院水利部岩土力学与工程重点实验室武汉430010

裂隙是膨胀土的重要特征之一,长期以来,人们常常把分布于膨胀土大气影响深度范围内受干湿循环影响而产生的干缩裂隙与膨胀土地层中特有的原生裂隙混为一谈。在对膨胀土边坡失稳机制的研究中,也忽视了原生裂隙对边坡稳定的重要影响。为... 详细信息

裂隙是膨胀土的重要特征之一,长期以来,人们常常把分布于膨胀土大气影响深度范围内受干湿循环影响而产生的干缩裂隙与膨胀土地层中特有的原生裂隙混为一谈。在对膨胀土边坡失稳机制的研究中,也忽视了原生裂隙对边坡稳定的重要影响。为研究南水北调中线工程膨胀土地段渠道破坏机制,在河南省南阳市郊建设了一条长为2.05 km试验渠道,通过渠道开挖期间的地质勘察、现场观测和取样试验,以及对现场滑坡体的取样分析,研究了膨胀土裂隙及周边土体的物质成分、密度、含水率和强度特性,结合现场观测资料分析了裂隙与渠道滑坡的关系。研究表明,膨胀土地层中的原生裂隙有两种类型:光滑蜡状裂隙和有一定厚度充填黏土的裂隙。裂隙面上的物质成分与两侧土略有不同,且天然密度低、含水率高,强度远低于相邻土体的强度,一旦地层与边坡倾向一致,将产生沿裂隙面的滑动。

关键词：南水北调中线工程膨胀土裂隙强度特性破坏机制

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土石坝工程领域的若干创新与发展

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长江科学院院报 2021年第5期38卷 1-10,16页

作者：程展林潘家军长江科学院武汉430010 长江科学院水利部岩土力学与工程重点实验室武汉430010

我国高土石坝数量居世界之首,保证高坝大库建设与长期运行安全是国家经济和公共安全保障的重大需求。系统总结了长江科学院近年来在土石坝工程领域的若干创新与发展。提出了基于“旁压模量当量密度法”的粗粒料级配相似理论试验方法;介... 详细信息

我国高土石坝数量居世界之首,保证高坝大库建设与长期运行安全是国家经济和公共安全保障的重大需求。系统总结了长江科学院近年来在土石坝工程领域的若干创新与发展。提出了基于“旁压模量当量密度法”的粗粒料级配相似理论试验方法;介绍了研发的系列CT三轴仪,实现了粗粒料组构要素的定量测量;提出了三轴试验中加载板与试样之间由滑动摩擦变为滚动摩擦、整体式接触变为分散式接触的减摩新方法,研发了相关减摩装置;研制了大尺寸、高压力、微摩擦、刚柔复合加载的土工真三轴仪;揭示了粗粒料真实三维应力条件下的强度与变形变化规律、湿化与蠕变变形特性;构建了粗粒料三参量非线性K-K-G剪胀模型、六参数湿化模型、九参数蠕变数学模型及相应的参数确定方法;基于当量密度法的原创思想,提出了利用旁压试验间接确定超百米级深厚覆盖层现场密度的试验方法。上述研究成果可为高土石坝工程建设提供重要科技支撑。

关键词：土石坝粗粒料旁压模量当量密度法 CT三轴仪微摩擦刚柔复合加载湿化变形 K-K-G剪胀模型

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