羟基

The cytotoxicity of these compounds were valuated by MTT and SRB methods using three cancer cell lines: HL-60, A-549, P-388. Cyclo-shikonin, and cyclo-alkannin have high cytotoxicity against HL-60.The chiral center of side chain has no effect on their activity. 2- 1-(Acetyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (105) has strong inhibition effect on P-388 cells. 2- 1-(isooctyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (108) and 2- 1-(2-furoyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (112) have high inhibition on A-549.Shikonin (1), alkannin (2), and their derivatives have the structural features of a planar chromophores and short side chain. We examined the ability to inhibit the telomerase.

抗肿瘤活性初步筛选测试采用小鼠白血病P-388肿瘤细胞和人肺癌A-549肿瘤细胞进行，结果表明侧链羟基的手性对抗肿瘤活性无明显影响；有数个化合物具有很好的体外抑制活性，特别是化合物2-（1-异辛酰氧基-4-甲基-3-戊烯基）-5，8-二羟基-1，4-萘醌（108）和2-[1-（2-呋喃甲酰氧基）-4-甲基-3-戊烯基]-5，8-二羟基-1，4-萘醌（112）体外显示对人肺癌A-549肿瘤细胞有强效；2-（1-乙酰氧基-4-甲基-3-戊烯基）-5，8-二羟基-1，4-萘醌（105）对小鼠白血病P-388肿瘤细胞有强效；环紫草素和环异紫草素对人白血病HL-60细胞有强烈抑制作用。

Our chief products include as follows: 5-Nitro-8-hydroxy Quinoline, 8-Aminoquinaldine, 8-Hydroxyquinoline Sulfate, 5,7-Dichloro-8-hydroxyquinaldine, 5-Nitro-0-cresol, 6-Nitro-m-cresol, 2'-Chloroacetophenone, 4-Methyl-5-thiazole ethanol, 4-Aminophenethyl alsohol.

主要产品有：硝羟喹啉，8-氨基喹啉，8-羟基喹啉硫酸盐，8-羟基喹哪啶，5，7-二氯-8-羟基喹哪啶，5-硝基邻甲酚，6-硝基间甲酚，邻氯笨乙酮，4-氨基笨乙醇，4-甲基-5-噻唑乙醇，3-羟基吡啶等。

The preparation of polymer is required for high purity of glycolic acid, if not, low-weight polymer is obtained, therefore, high purity glycolic acid is scarce in the market. So, the research for the synthesis of glycolic acid is essential. In domestic and overseas, there are many methods for preparation of glycolic acid, including glycin oxidation, cyanogenesis, aldehyde oxidation, coupling of maldehyde and methyl formate, oxalic acid electrolysis, chloroactic acid hydrolysis and so on.

制备羟基乙酸的聚合物时，对羟基乙酸单体的纯度要求较高，否则得到的聚合物分子量较低，导致高纯度羟基乙酸的需求量逐年增长，目前在国内，高纯度的羟基乙酸还没有形成工业化规模生产，对羟基乙酸的合成进行研究是非常有意义的。

Constituting dicycle; 2. region selectively reducing six-membered ring ketocarbonyl radical; 3. introducing 7alpha-hydroxy group; 4. Aldol reaction to introduce side chain and obtain 8alpha-hydroxy group; 5. oxidizing the position 7 hydroxy group into ketone; 6. turning the configuration of the position 7 hydroxy group; 7. glycosidating the position 7 hydroxy group; and 8. eliminating protecting group to obtain the target compound.

该方法包括如下步骤：(1)双环的构建；(2)区域选择性还原六元环酮羰基；(3)7α-羟基的引入；(4)Aldol反应引入侧链，同时得到8α-羟基；(5)7位羟基氧化为酮；(6)7位羟基构型的翻转；(7)7位羟基的糖苷化；(8)脱除保护基得到目标化合物。

They are 4-(2- hydroxy-3-butynlenoxy) benzoic acid (1, WA), 5-chloro-7, 8-dihydroxy-7-methyl- 6-oxo-3- [ -3, 4-dihydroxy-3, 5-dimethyl-l-heptylene] -1H-8, 8a-dihydrobenzo [2, 3-c] pyran (2, WB),-2-(2-methyl-2-dibutene diamido)-2-butenoic acid (3, B5262), 3, 4-dihydro-9, 10-dihydroxy-7-methoxy-3-methyl-1H-naphtho [2, 3- c] pyran-1-one (4, A73 semi-Vioxanthin), 8, 8'-bis (6, 9-dioxo-3,4-dihydro-10- hydroxy-7-methoxy-3-methyl-1H-naphtho [2, 3-c] pyran-1-one)(5, A122 Xanthomegnin), 2, 5-dioxo-3a-hydroxymethyl-3, 3a, 6, 6a-tetrahydro-furo [2, 3-b] furan (6, 1003-2), 7-acety1-5-chloro-6, 8-dioxo-7-methyl-3- [ -3, 5-dimethyl-1, 3- diheptylene] -4aH-benzo [2, 3-c] pyran (7, M2-2 sclerotiorin), respectively.

它们分别被命名为4-（2-羟基-3-丁炔氧基）苯甲酸（1，WA）、5-氯-7，8-二羟基-7-甲基-6-氧代-3-[-3，4-二羟基-3，5-二甲基-1-庚烯基]-1H-8，8a-二氢苯并[2，3-c]吡喃（2，WB）、-2-（2-甲基-2-丁烯二酰亚胺基）-2-丁烯酸（3，B5262）、3，4-氢-9，10-二羟基-7-甲氧基-3-甲基-1H-萘并［2，3-c］吡喃-1-酮（semi-Vioxanthin，4，A73）、8，8'-双（6，9-二氧代-3，4-二氢-10-羟基-7-甲氧基-3-甲基-1H-萘并［2，3-c］吡喃-1-酮）（Xanthomegnin，5，A122）、2，5-二氧代-3a-羟甲基-3，3a，6，6a-四氢-呋喃并［2，3-b］呋喃（6，1003-2），7-乙酰基-5-氯-6，8-二氧代-7-甲基-3-［-3，5-二甲基-1，3-庚二烯基］-4aH-苯并2，3-c］吡喃（Sclerotiorin，7，M2-2）。

Methods Seven probe drugs were incubated with or without methyl protodioscin respectively in human microsomes. The specific substrates used in this study were caffeine (CYP1A2), dextromethorphan (CYP2D6), tolbutamide (CYP2C9),-mephenytoin (CYP2C19), chlorzoxazone (CYP2E1), coumarin (CYP2A6) and midazolam (CYP3A4). The concentrations of the substrate metabolites (paraxanthine, dextrorphan, 4-hydroxytolbutamide, 4-hydroxymephenytoin, 6-hydroxychlor-zoxazone, 7-hydroxycoumarin and 1-hydroxymidazolam) were determined by HPLC and LC-MS/MS. Results MPD 1-10 μmolL^(-1 had no significant inhibition on the activities of the seven cytochrome P450 enzymes.

将MPD和CYP450酶7种亚型的特异性探针底物咖啡因(CYP1A2)、右美沙芬(CYP2D6)、甲苯磺丁脲(CYP2C9)、s-美芬妥因(CYP2C19)、氯唑沙宗(CYP2E1)、香豆素(CYP2A6)及咪达唑仑(CYP3A4)与人肝微粒体进行孵化反应，采用HPLC和LC-MS/MS法测定对应的7种代谢产物（1，7-二甲基黄嘌呤、去甲右美沙芬、4-羟基甲苯磺丁脲、4-羟基美芬妥因、6-羟基氯唑沙宗、7-羟基香豆素和1-羟基咪达唑仑）的浓度，通过与对照组比较，确定MPD对以上7种酶活性的影响。

In this thesis,the AM1,MNDO,MINDO/3(mainly AM1)and INDO/S-CI semiempirical MO methods were used toinvestigate the excited-state intramolecular protontransfer reactions of salicylic acid derivatives—salicylic acid,methyl salicylate,salicylaldehyde,o-hydroxyaceto-phenone,salicylamide and 3-hydroxy-picolinamide (6 conformers and 2-3 anion species);2-(2'-hydroxy-5' methylphenyl) benzotriazole(4 conformers),2-(2' hydroxyphenyl) benzimidazole (3 conformers and 3anion species),Bis-2,5-(2-benzoxazolyl)hydroquinone(3 conformers),2-(2'-hydroxyphenyl)benzothiazole(2conformers) and 7-azaindole dimer (2 conformers).Theinvestigations were described as follows.Geometry optimization,relative stability andhydrogen bonding energy First,for sylicylic acid derivative molecules,the AM1,MNDO and MINDO/3 methods were used toinvestigate ground-state geometry optimization,energies,relative stabilities and hydrogen-bondingenergies on the five kinds of the molecules(designing 6 conformers and 2-3 anion species).Comparing with experimental data,the optimizedgeometry,the order of stability,the hydrogen-bonding energies and the distances between O-O in O-H..O hydrogen bonds by AM1 method were in agreementwith the experimental data,however,the C-C bondlengths optimized by MNDO and MINDO/3 were longer,C-O and O-H bond lengths were shorter;for C-N bondlengths,the results opitimized by MNDO method werethe same as those by AM1 method,nevertheless the C-Nbond lengths given by MINDO/3 method were muchshorter.For some sylicylic acid derivatives(e.g.methyl salicylate,salicylamide),the order ofstabilities on the conformers given by MNDO andMINDO/3 methods were not in agreement with theexisting conformers deduced by experimental methods,and the hydrogen bonding energies calculated by MNDO.and MINDO/3 methods were smaller.Second,the studyon the other systems found that the optimizedgeometry of the proton-transfered product with INDOmethod could not be obtained,only could theoptimized geometry of reactant be obtained,and thecalculated hydrogen bonding energies were greater.Many results of calculation indicated that the studyon the excited-state intramolecular proton transferreaction system using AM1 method was suitable andreliable.

本论文用AM1、MNDO、MINDO/3（主要是AM1）和INDO/S-CI半经验分子轨道方法对水杨酸衍生物系列——水杨酸、水杨酸甲酯、水杨醛、O-羟基乙酰苯酮、水杨酰胺和3-羟基吡啶酰胺（6种异构体和2-3种阴离子）；2-（2'-羟基-5'-甲基苯基）苯并三〓唑（4种异构体）；2-（2'-羟基苯基）苯并咪唑（3种异构体和3种阴离子）；2，5-二间氮杂氧茚氢醌（3种异构体）；2-（2'-羟基苯基）间〓杂硫茚（2种异构体）和7-〓吲哚二体（2种异构体）的激发态分子内质子转移反应在以下几个方面进行了较系统的理论研究：几何构型优化和相对稳定性及氢键能首先以水杨酸衍生物系列分子为例，用AM1、MNDO和MINDO/3方法考察了5种分子（每种分子设计6种异构体和2-3种阴离子）的基态几何构型优化，能量、相对稳定性和氢键能计算，通过和实验数据进行比较，AM1方法给出的优化几何构型、稳定性次序、氢键能和O—H。。。O氢键的0—0距离与实验数据吻合最好，MNDO和MINDO/3方法优化的C-C键长偏长，C-O键和O-H键长偏短；对于C-N键长，MNDO和AM1优化结果差别不大，而MINDO/3给出了过短的C-N键长，MNDO和MINDO/3方法给出的有些水杨酸衍生物分子（如水杨酸甲酯和水杨酰胺）异构体的稳定性次序和实验上推测的可存在异构体结果不一致，MNDO和MINDO/3方法给出的氢键能偏低，对其他体系的研究发现INDO方法常常不能得到质子转移产物的优化几何构型，只能得到反应物的优化构型，并且估算的氢键能偏高，大量的计算结果表明AM1方法对本论文研究的激发态分子内质子转移反应体系是适宜和可靠的。

A new flavanone from Dryopteris sublaeta;2. Isolation and Structure Identification of a New Flavanone from Dryopteris sublaeta;3. RESULTS Five compounds are isolated from the ether fraction of 70% acetone-extracts,and their structures were identified as(2S)5,7-dihydroxy-6,8-dimethyl flavanone desmethoxymatt.

结果浅裂鳞毛蕨地上部分用体积分数为70%丙酮提取液乙醚萃取部位分离得到了5个化合物，分别鉴定为：(2S)5，7-二羟基-6，8-二甲基二氢黄酮，(2S)5，7-二羟基-6，8-二甲基-4′-甲氧基二氢黄酮，(2S)5，7，2′-三羟基-6，8-二甲基-二氢黄酮，(2S)5，7，4′-三羟基-3′-甲氧基-6，8-二甲基二氢黄酮，(2S)5-羟基-4′-甲氧基-6，8-二甲基二氢黄酮-7-O--βD-葡萄糖苷。

And the ability of antioxidant of polyhydroxy benzamides don't have too many differences with Trolox (IC50 =13.90 μg/ml), the substition of hydroxy group at amino benzene ring doesn't affect the whole ability of antioxidant apparently, but while the single hydroxy group at carboxylic acid benzene ring, they are apparently decrease to scavenge the ability of free radical, as a result, the hydroxy at amino benzene ring substitutes its function, without the hydroxy group, the ability of antioxidant is worst, but it upgrades its function while the hydroxy and amino are in the ortho-position or para-position.

而当多酚醯胺化合物其抗氧化能力与Trolox差不多时(IC50 =13.90 μg/ml)，胺基苯环上之羟基取代对整体抗氧化能力影响不明显，但在羧酸苯环上具单羟基时，其清除自由基能力明显下降，使得胺基苯环上羟基取代发挥了影响力，无羟基取代时，抗氧化能力最差，而羟基与胺基互为邻位或是对位时较间位有提升效果。

The important role of hydroxycinnamic acids,i.e.,caffeic acid, chlorogenic acid,sinapic acid,ferulic acid,3-hydroxycinnamic acid (3-HCA) and 4-hydroxycinnamic acid(4-HCA) as the pBR322 plasmid DNA-Cleaving agents in the presence of Cu ions was investigated.

我们研究了羟基肉桂酸衍生物即咖啡酸、绿原酸、芥子酸、阿魏酸、3-羟基肉桂酸(3-HCA)和4-羟基肉桂酸(4-HCA)在Cu存在下诱导pBR322质粒DNA链断裂损伤情况，结果发现HCAs的促氧化活性与它们的分子结构有密切的关系，具有邻二羟基结构和邻二甲氧基羟基结构的化合物表现出了更高的促氧化活性，其中CaA的活性最高。

This one mode pays close attention to network credence foundation of the businessman very much.

这一模式非常关注商人的网络信用基础。

Cell morphology of bacterial ghost of Pasteurella multocida was observed by scanning electron microscopy and inactivation ratio was estimated by CFU analysi.

扫描电镜观察多杀性巴氏杆菌细菌幽灵和菌落形成单位评价遗传灭活率。