草药牛筋果中牛筋果酸的分离和结构测定

本文报道从苦木科牛筋果属植物牛筋果(Harrisonia perforate(Blanco)Merr.)根中再分得一种新的色原酮化合物,命名为牛筋果酸(perforatic acid),其水溶液对³H-TdR体外渗入小鼠肝癌腹水细胞有较高的抑制率。     

马银花的化学成分研究

目的研究马银花的化学成分。方法利用硅胶色谱分离纯化马银花根的化学成分，根据化合物的理化性质和光谱数据鉴定化合物的结构。结果分离并鉴定了7个化合物，其结构分别为3，5，7-三羟基色原酮-3-O-β-D-吡喃木糖苷(I)，蒲公英赛醇(II)，β-谷甾醇(III)，白桦酸(IV)，槲皮素(V)，槲皮素-3-O-α-L-鼠李糖苷(VI)和葡萄糖(VII)。结论化合物I为新化合物，化合物II-VII为首次从该植物中分离得到。     

刺果甘草化学成分的研究

从刺果甘草(Glycyrrhiza pallidiflora Maxim)的根和根茎中分离到五种化合物,经理化性质和光谱方法鉴定,化合物P-2为4-羟基-2,4’-二甲氧基查尔酮,为一新的化合物,命名为刺果甘草查尔酮(glypallichalcone,P-2)。其它分别为4'-O-methyl-coumestrol(P-1),谷氨酸乙酰化物(N-acetylglutamicacid,P-3)和芒柄花素(formononetin,P-4),均为首次从该植物中获得。此外还得到β-谷甾醇(β-sitos-terol,P-5)     

茵陈色原酮对小鼠急性乙醇性肝损伤的保护作用研究

目的:探讨茵陈色原酮对小鼠急性乙醇性肝损伤的保护作用及其机制。方法:实验小鼠随机分为5组:模型组、茵陈色原酮(高、中、低剂量)组和正常对照组,每组各6只。给予茵陈色原酮组小鼠相应剂量的茵陈色原酮灌胃7d,第7天时将模型组、茵陈色原酮组小鼠采用50%乙醇12mL/(kg·d)灌胃,禁食12h,致小鼠急性乙醇性肝损伤;观察小鼠肝脏组织形态,计算肝脏指数(LI),ELISA法测定小鼠血清丙氨酸转氨酶(ALT)、天门冬氨酸转氨酶(AST)、总蛋白(TP)、肝胞浆乙醛脱氢酶(ALDH)、谷胱甘肽过氧化物酶(GSH-Px)水平。结果:茵陈色原酮(高、中剂量)组均明显降低急性乙醇性肝损伤小鼠肝脏指数(P<0.01);高剂量组可减轻肝组织脂肪变性(P<0.05),明显降低血清ALT、AST水平(P<0.01),升高肝胞浆ALDH、GSH-Px水平(P<0.01)与血清TP水平(P<0.01)。结论:茵陈色原酮对小鼠急性乙醇性肝损伤具有保护作用,其机制与增强肝脏清除乙醛和抗氧化能力有关。     

防风化学成分的分离与结构鉴定

防风乙醇提取物经大孔树脂富集后，采用各种柱色谱法进行分离纯化，从中得到14个化合物，根据理化性质和光谱数据鉴定结构为：防风嘧啶(1)，clemiscosin A (2)，5-羟基-8-甲氧基补骨脂素(3)，亥茅酚苷(4)，亥茅酚(5)，紫花前胡苷元(6)，升麻素苷(7)，升麻素(8)，5-O-甲基维斯阿米醇苷(9)，5-O-甲基维斯阿米醇(10)，异紫花前胡苷(11)，腺苷(12)，胡萝卜苷(13)和β-谷甾醇(14)。其中化合物1为新化合物，化合物2为首次从伞形科植物中分离得到，化合物3为首次从防风中分离得到。     

库拉索芦荟化学成分的研究

目的：从中药库拉索芦荟(Aloe vera L.)中寻找新的降糖及抗炎活性成分。方法：利用多种柱色谱方法进行分离纯化,根据光谱数据和化学方法进行结构鉴定。结果：从库拉索芦荟乙醇浸膏的乙酸乙酯部分分离鉴定了11个化合物,分别为：芦荟色苷G(aloeresin G, 1),异芦荟色苷D（isoaloeresin D, 2),芦荟大黄素(aloe-emodin, 3),芦荟苷A(babarloin A, 4),8-O-甲基-7-羟基芦荟苷B(8-O-methyl-7-hydroxyaloin B, 5),elgonica-dimer A(6),elgonica-dimer B(7), feralolide(8),何伯烷-3-醇(hopan-3-ol,9), β-谷甾醇(β-sitosterol, 10)及胡萝卜苷(daucosterol, 11)。结论：化合物1为新化合物,命名为芦荟色苷G。     

国产沉香化学成分研究 Ⅳ.2-(2-苯乙基)色酮类化合物的分离与鉴定

自国产沉香(Lignum Aquilariae sinensis)[属瑞香科(Thymeleaceae)植物]的乙醇提取物的乙醚溶解部分中分离得到六个2-(2-苯乙基)色酮类化合物。经光谱(UV,IR,¹HNMR ¹³CNMR和MS)分析及化学合成,确定其中一个为新化合物,即6-羟基-2-[2-(4-甲氧基苯)乙基]色酮(Ⅴ)。其余五个为已知化合物,即2-(2-苯乙基)色酮,6-氧基-2-(2-苯乙基)色酮,6,7-二甲氧基-2-(2-苯乙基)色酮,6-甲氧基-2-[2-(3′-甲氧基苯)乙基]色酮和6-羟基-2-(2-苯乙基)色酮,这些化合物均是首次从该植物中分离得到。     

拐芹根化学成分研究

从拐芹Angelica polymorpha Maxim根及根茎的酯溶性部位分得两个化合物I和II。经光谱解析(UV,IR,MS,¹H-NMR,¹³CNMR,¹H-¹HCOSY,¹³C-1HCOSY和DEPT等),确定1为一个新成分,命名为拐芹色原酮A(angeliticinA),II为saxalin。     

佩特曲霉菌中1个新的色原酮类化合物△*

目的 研究盐碱地来源的佩特曲霉菌在静置发酵条件下的次级代谢产物。方法 用正反相硅胶柱、Sephadex LH-20、高效液相等色谱技术对目标菌株的次生代谢产物进行分离纯化,经核磁共振谱、质谱、单晶X衍射等光谱方法和理化性质确定化合物的结构。结果 从佩特曲霉菌的静置发酵物中分离得到6个单体化合物,分别鉴定为：5-甲基-2-乙酰基-7-羟基色原酮 (1),2,5-二甲基-7-羟基色原酮 (2),avellanine A (3),avellanine B (4),(E)-N-[2-(4-羟基苯基)]乙烯基甲酰胺 (5),(Z)-N-[2-(4-羟基苯基)]乙烯基甲酰胺 (6)。结论 化合物1为新化合物,化合物2-6均为首次从佩特曲霉菌中获得。化合物1-6均没有明显的抗肿瘤活性。     

色原酮及其苷在植物中的分布和生物活性研究进展

目前,对色原酮及其苷类化合物在植物中的分布还无人统计过,其在植物中分布广泛,多种科属中都存在该类化合物。近年来,国内外许多学者对色原酮及其苷的生物学功能研究越来越多,结果表明其具有抗肿瘤、抗炎、镇痛、降血压等很多有益于人类健康的生物活性,因此受到生物医学界的重视。为促进开发和利用,本文对色原酮及其苷在植物中的分布及其生物活性研究进展作一概述。     

改进雌甾-3-甲醚的合成方法

目的改进雌激素类化合物3位酚羟基的甲醚化工艺。方法以含3-酚羟基的雌激素类化合物为原料，丙酮为溶剂，在碳酸钾存在下与硫酸二甲酯反应。结果以高收率合成了目的化合物。结论该工艺操作简便、试剂价廉易得、产率高，实现了对原有工艺的改进。     

巴戟天抗衰老活性成分研究

目的研究巴戟天(Morinda officinalis)活性部位的化学成分。方法用色谱法分离,用波谱法对化合物结构进行鉴定。结果从巴戟天活性部位中分出5个化合物,分别为甲基异茜草-1-甲醚(Ⅰ)、2-羟基-1-甲氧基蒽醌(Ⅱ)、7-羟基-6-甲氧基香豆素(Ⅲ)、异嗪皮啶(Ⅳ)、2-醛基蒽醌(Ⅴ)。结论化合物Ⅳ为首次从该属植物分离得到,化合物Ⅴ为首次从该种植物分离得到。     

茜素型蒽醌基因突变风险评价

目的 使用毒性预测软件及细菌回复突变（Ames）试验评价茜素型蒽醌的基因突变风险。方法 通过毒性软件Toxtree、Derek Nexus和Sarah Nexus对茜素型蒽醌：茜草素、异茜草素、甲基异茜草素、甲基异茜草素-1-甲醚、茜素-1-甲醚、羟基茜草素、光泽汀进行致突变风险预测;每个受试物设置5个给药浓度,分别在有或无S9代谢活化条件下,使用5种鼠伤寒沙门氏菌TA97、TA100、TA102、TA1535和TA1537开展基于6孔板培养的Ames试验,判断该类化合物苯环上不同取代基对致突变性的影响。结果 软件基于蒽醌环的存在预测该类化合物均具有致突变风险。在非S9代谢活化下,异茜草素和羟基茜草素可导致TA1537回复突变菌落数增加;光泽汀可诱导TA97、TA100和TA1537回复突变菌落数增加。在S9代谢活化下,异茜草素可导致TA97、TA100和TA1537回复突变菌落数增加;羟基茜草素可导致TA1537回复突变菌落数增加;光泽汀可导致TA97、TA100和TA1537回复突变菌落数增加;甲基异茜草素可导致TA97、TA100、TA102和TA1537回复突变菌落数大幅增加;甲基异茜草素-1-甲醚可导致TA100回复突变菌落数增加。结论 茜素型蒽醌受试物在有或无S9代谢条件下表现出不同程度、不同菌株的回复突变,开展相关研究评价其毒性风险对该类化合物合理监管具有重要价值。     

Neuraminidase Inhibitors from<Emphasis Type="Italic">Reynoutria elliptica</Emphasis>

In the course of screening neuraminidase inhibitors from herbal medicines, Reynoutria elliptica exhibited high inhibitory activity. Four active compounds were isolated from the ethyl acetate soluble fraction by consecutive purification using sillica gel, Sephadex LH-20 chromatography, and recrystallization. The chemical structures of these compounds were identified as 1,3,8-trihydroxy-6-methylanthraquinone (emodin) 1,8-dihydroxy-3-methoxy-6-methylanthraquinone (emodin 3-methyl ether; physcion), 1,3,8-trihydroxy-6-hydoxymethylanthraquinone (omega-hydroxyemodin), and 3,5,4'-trihydroxystilbene (trans-resvertrol) by spectral data including MS, 1H-, and 13C-NMR. The IC50 values of emodin, emodin 3-methyl ether, omega-hydroxyemodin, and trans-resvertrol were 2.81, 74.07, 10.49, and 8.77 microM, respectively. They did not inhibit other glycosidase such as glucosidase, mannosidase, and galactosidase, indicating that they were relatively specific inhibitors of neuraminidase.     

交链孢醇和交链孢醇单甲醚的制备

按Ｓｏｔｉ等的方法制备交链孢醇和交链孢醇单甲醚，发现当完全按照他们的实验条件操作时，不能每步反应都获得所报道的产率，而且相差颇大，为此改变反应条件以使产率较为满意。本文详细报道这一实验结果。     

Constituents of the stems and fruits of<Emphasis Type="Italic">Opuntia ficus-indica</Emphasis> var.<Emphasis Type="Italic">saboten</Emphasis>

From the stems and fruits of Opuntia ficus-indica var. saboten, eight flavonoids, kaempferol (1), quercetin (2), kaempferol 3-methyl ether (3), quercetin 3-methyl ether (4), narcissin (5), (+)-dihydrokaempferol (aromadendrin, 6), (+)-dihydroquercetin (taxifolin, 7), eriodictyol (8), and two terpenoids, (6S,9S)-3-oxo-alpha-ionol-beta-D-glucopyranoside (9) and corchoionoside C (10) were isolated and identified by means of chemical and spectroscopic. Among these isolates, compounds 3-5 and 8-10 were reported for the first time from the stems and fruits of O. ficus-indica var. saboten.     

Determination of 8,2′-diprenylquercetin 3-methyl ether in plasma by UPLC-MS-MS and its pharmacokinetic application in rats

8,2′-Diprenylquercetin 3-methyl ether with significant anti-breast cancer activityis the main constituent of Tibetan medicine Sinopodophylli Fructus. In the present study, we developed and validated a rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the determination of 8,2′-diprenylquercetin 3-methyl etherin rat plasma. 8-Prenylkaempferol was used as the internal standard. The separation was carried out using Waters ACQUITY UPLC BEH C₁₈ column (2.1 mm×100 mm, 1.7 µm) with a mobile phase consisting of acetonitrile and 0.1% formic acid in water on a gradient program at a flow rate of 0.4 mL·min^–1 and temperature of 30 ºC. Triple quadrupole mass spectrometric detection in negative ion mode was used for multiple-reaction monitoring of the transitions at m/z 451.30→177.25 and m/z 353.25→298.15 for 8,2′-diprenylquercetin 3-methyl ether and 8-prenylkaempferol, respectively. The calibration curves were linear within the concentration range 0.1–2000 ng/mL (r = 0.9954). The recoveries were 103%–115%, and the results were consistent across low, middle and high concentration levels. The intra- and inter-day precisions were within 15%, and the bias was between –6%~15%. This method was simple, rapid and sensitive, which could be applied to the determination of 8,2′-diprenylquercetin 3-methyl ether in plasma and pharmacokinetic study in rats. Pharmacokinetic test indicated that the peak plasma concentration occurred in 2 h after the female rats were intragastrically administered with 8,2′-diprenylquercetin 3-methyl ether at the dose of 100 mg/kg, and the biological half-life was 6.79 h. The blood drug concentration maintained equal amount for 20 h, which was conducive to the in vivo effects of drugs.     

4-甲基-(3''S, 4''S)-凯林硫代内酯衍生物的合成及其体外抗血小板聚集活性研究

目的设计并合成凯林硫代内酯衍生物,并测定其体外血小板聚集抑制活性。方法以7-羟基-4-甲基香豆素为原料,经亲核取代、克莱森重排、硫化反应、sharpless不对称羟基化、酯化反应制备目标化合物5a~5h;采用微量反应板酶标仪比浊法评价目标化合物的抗血小板聚集活性。结果合成了8个新化合物,其结构经1H-NMR、13C-NMR及MS确证。活性测试结果表明,化合物5h、5b的活性强于阳性对照药奥扎格雷钠,具有抗血小板聚集活性。结论 4-甲基-(3'S,4'S)-凯林硫代内酯衍生物具有良好的抗血小板聚集活性,值得进一步研究。     

Chromon-Derivate aus Mannichbasen

Chromone Derivatives from Mannich Bases The 3-substituted chromones 5a--f have been obtained by the reaction of 3-(dimethylaminomethyl)chromone ( 3 ) with CH-acidic compounds or from the substituted o-hydroxybutyrophenone derivatives 7a--c and 7f and dimethylformamide dimethylacetal.     

Metabolic studies of four soy isoflavones in rats by HPLC–HR-MS

In this paper, the metabolites of four soy isoflavones, daidzein, daidzin, genistein, and genistin, on perfused rat intestine–liver model were investigated by high-performance liquid chromatography coupled with high-resolution mass spectrometer/tandem mass spectrometer. Totally 16 metabolites were detected and identified based on accurate mass, fragmentation patterns, and multiple-stage mass data (MSⁿ). The metabolic site of dadzein-7-methyl ether (D-7-M) was further confirmed by nuclear magnetic resonance. Methylation, glucuronide conjugation, and sulfate conjugation were the primary metabolic processes. Among them, six metabolites, daidzin-4′,7-diglucoside, genistein-4′-glucoside, D-7-M, dadzein-4′,7-dimethyl ether, genistein-4′-methyl ether, and genistein-7-methyl ether were detected in rats for the first time and not reported in humans. The metabolic pathways of daidzein, daidzin genistein, and genistin in rats were postulated. The biological effects of these metabolites are worthy of further investigation.