抗心肌缺血药3-{4-[(2-羟基-3-烷氨基)丙氧基]苯基(苄基)}-取代4(3H)-喹唑酮的合成

In order to search for effective antimyocardial ischemic agents, fourteen new 3 4-[(3-alkylamino-2-hydroxy)propoxy] phenyl(benzyl)]-substituted 4(3H)-quin zolinones (Ⅱ) were synthesized. Substituted o-aminobenzoic acids used as the starting materials were allowed to react with acetic anhydride and then p-aminophenol (method A), or with N- (4- hydroxyphenyl)formamide (method B), or with thionyl chloride and then N - (4 - hydroxybenzyl) formamide (methode C) to form 3-[(4-hydroxyphenyl(benzyl)]-substituted 4(3H)-quinazolinones (Ⅲ). The intermediate Ⅲ reacted with epichiorohydrin to form the epoxides (Ⅳ). The reaction of Ⅳ with an excess of isopropylamine or tert-butylamine in boiling chloroform gave the desired products. Of all the compounds synthesized, Compounds Ⅱ_3～5 and Ⅱ₁₃ were found to increase the tolerance of mice to hypoxia. Further evaluation is in progress.     

中药赤芍中化学成分的研究

Two new monoterpene glycosides were isolated from the ethanolic extract of the root of Paeonia laetiflora Pall. The structure of compound (Ⅰ) has been identified as (Z)-(1S, 5R)-β-pinen-10-yl β-vicianoside; Compound (Ⅱ) is named lactiflorin and tentatively assigned as (Ⅱ).Compound (Ⅰ) is the glycoside of the enol form of an aldehyde. In compound (Ⅱ), the sugar moiety is attached to the aglycone by two ether-like linkages. Both seem to be unprecedented.     

青蒿素类似物的研究 Ⅶ.双(二氢青蒿素)醚和双(二氢脱氧青蒿素)醚类化合物的合成

Some ethers, of bis(dihydroqinghaosu) Ⅲ and bis(dihydrodeoxyqinghaosu) Ⅳ were prepared in order to study the structure-activity relationships and to search for new antimalarials. Compounds Ⅲ were sythesized by condensation of glycol with two moles of dihydroqinghaosu using boron trifluoride etherate as catalyst. Compounds Ⅳ were prepared from ethers of bis (dihydroqinghaosu) by reduction with zinc and acetic acid.The bis-ethers were evaluated against chloroquine-resistant strain of plasmodium berghei in mice. Compounds Ⅲ were less potent than methyl-dihydroqinghaosu (Ⅰ) and compounds Ⅳ were inactive.     

传统植物药和兰花的最新进展(英文)

The main objective of this paper is to review recent advances in plant drug research and developments in orchid study, in an attempt to provide useful references for plant drug studies. Plants have been used as medicine for millennia. Out of estimated 250 000 to 350 000 plant species identified so far, about 35000 are used worldwide for medicinal purposes. It has been confirmed by WHO that herbal medicines serve the health needs of about 80 percent of the world's population; especially for millions of people in the vast rural areas of developing countries.Meanwhile, consumers in developed countries are becoming disillusioned with modem healthcare and are seeking alternatives. The recent resurgence of plant remedies results from several factors: 1) the effectiveness of plant medicines; 2) the side effect of most modem drugs; and 3) the development of science and technology. It has been estimated that in the mid-1990s over 200 companies and research organizations worldwide are screening plant and animal c     

薯蓣属植物化学成分的研究——Ⅹ.蜀葵叶薯蓣中甾体皂甙和皂甙元的分离和鉴定

Four components were isolated from acid-treated rhizome of Dioscorea althaeoides Kunth. Their structures were identified as diosgenin (Ⅰ), β-sitosterol (Ⅱ), diosgenin palmitate (Ⅲ) and △^3,5-deoxytigogenin (Ⅳ) on the basis of physical constants and spectral data.Two sparingly soluble steroid saponins were also isolated from this plant Their physicochemical constants showed that one of them is dioscin (Ⅴ) and the other graeillin (Ⅵ).     

重齿毛当归(独活)中异当归醇、毛当归醇及其它香豆素的分离与鉴定

Nine coumarins were isolated from dichloromethane extract of the roots of Angelica pubescens Maxim. Seven of them were identified as osthol (Ⅰ), columbianetin acetate (Ⅱ), columbianetin (Ⅲ), bergapten (Ⅳ), angelol (Ⅴ),xanthotoxin (Ⅵ) and isoimperatorin (Ⅶ). (Ⅵ) and (Ⅶ) were isolated for the first time from this plant. Two new coumarins were elucidated as isoangelol (Ⅷ), a geometric isomer of angelol C₂₀H₂₄O₇ [α]_D²⁰-133.5 and anpubesol C₂₀H₂₆O₇ [α]_D²⁰ -72.5 on the basis of spectral evidences.     

Pharmacological Research of Tetrandrine and Fangchinoline, the Major Components of Stephania Tetrandrae

Purpose: The root of the Chinese herbal remedy Han Fang Ji ( Radix of Stephania Tetrandrae) has been used since antiquity by Chinese physicians as an ahtihypertenion, antirheumatic, analgesic and antipyretic agent. Tetrandrine (TET) and fangchinoline (FAN), the bisbenzylisoquinolide alkaloids, are the major components of Han Fang Ji. TET has been well known as a natural occurred non - specific calcium channel blocker. However, the effects of TET on the cardiovascular system are not fully understood, and that a few of researches about FAN, an another major constituent of Han Fang Ji, are reported. Thus, we have done these studies to investigate and compare the effects of TET and FAN on cardiovascular system,CNS and multi - drug resistance to anticancer drugs for several years.     

Iridoid Glycosides from Buddleja lindeyana

Aim To study the chemical constituents of Buddleja lindeyana. Methods The constituents were separated and purified by different methods of chromatography, and their structures were elucidated by IR, MS and NMR. Results Three iridoid glycosides and two other compounds were isolated from Buddeja lindeyana. Their structures were elucidated to be 6-O-fendoylajugol (1), erythro-6-oxo-4‘-(3-methoxyl-4-hydroxyphenylglycol-8“)-fendoylaj-ugol (2), threo-6-oxo-4‘-(3-methoxyl-4-hydroxyphenylglycol-8“)-fendoylajugol (3), tetra-cosanoic acid 2,3-dihydroxypropyl ester (4), and galactitol (5). Conclusion All the compounds have been isolated from this plant for the first time. Compounds 1,2 and 3 have protective effect agains MPP^ -induced apoptosis.     

多次标准加入分光光度法同时测定复方药物中各组分含量的研究

A computational analytical method of simultaneous determination of components in compound drug without preliminary separation has been proposed. It is a matrix computation by means of multi-standard addition spectrophotometry on multi-wavelengths. The compound tablets of sulfamethoxazole was used to perform the experiment. In the experiment, the rule of error propagation for matrix computation was taken for the selection of solvent, groups of wavelengths and faction of standard addition, and the suitable concentration of standard addition was decided by test. In the case of determination for the simulated solution compound sulfamethoxazole, the recoveries for SMZ and TMP were 99.26～101.8 and 97.77～102.0%, respectively, with standard deviation of less than 0.51% and 213%, respectively. The method had been applied to the determination for compound tablets of sulfamethoxazole with satisfactory results.     

Peptide-drug conjugates(PDCs): a novel trend of research and development on targeted therapy,hype or hope?

Peptide-drug conjugates(PDCs) are the next generation of targeted therapeutics drug after antibody-drug conjugates(ADCs), with the core benefits of enhanced cellular permeability and improved drug selectivity. Two drugs are now approved for market by US Food and Drug Administration(FDA), and in the last two years, the pharmaceutical companies have been developing PDCs as targeted therapeutic candidates for cancer, coronavirus disease 2019(COVID-19), metabolic diseases, and so on.The therapeutic ...     

水如意化学成分的研究

罂粟科紫堇属植物水如意(Corydalis taliensis Fr.)别名金钩如意草,五味草,云南民间药用全草,对风湿骨痛,牙痛及肝炎,肠炎,结膜炎等症有一定疗效。这个植物的化学研究尚无报道。我们从中得到九个结晶,经光谱及物理、化学常数的测定,鉴定其中七个生物碱分别为乙酰紫堇灵(acetylcorynoline)Ⅰ,消旋紫茧灵(±)corynoline Ⅱ,必枯枯灵     

白喉乌头中生物碱的研究

目的 研究白喉乌头Aconitum leucostomum Worosch.中的生物碱.方法 采用柱色谱法分离纯化得到单体化合物,通过多种波谱方法鉴定其结构.结果 分离得到了10个生物碱,分别为:高乌甲素(I)、dehydroacosanine(Ⅱ)、冉乌碱(Ⅲ)、宋果灵(Ⅳ)、乌头碱(Ⅴ)、新乌头碱(Ⅵ)、去氧刺乌头碱(Ⅶ)、spicatine A(Ⅷ)、印乌碱(Ⅸ)、puberuline C(Ⅹ).结论 化合物Ⅴ～Ⅹ为首次从该植物中分离得到.     

绿舒筋有效成分研究

首次从卫矛科植物宝兴卫矛(Euonymus mupinensis Loes et Rehd)藤茎中分得八个单体化合物,经光谱分析和理化常数测定,分别确定为雷公藤内酯甲(wilforlide A,Ⅰ)、雷公藤内酯乙(wilforlide B,Ⅱ)、齐墩果-12-烯-3,29-二醇(olean-12-en-3,29-diol,Ⅲ)、齐墩果-3-酮-12-烯-29-醇(olean-3-oxo-12-en-29-ol,Ⅳ)、豆甾-3-酮(stigmastan-3-ono,Ⅴ)、豆甾-3,6-二酮(stigmastan-3,6-dione,Ⅳ)、β-谷甾醇(β-sistosterol,Ⅶ)和β-谷甾醇-β-D-吡喃葡萄糖甙(β-sistosterol-3-O-β-D-glucopyranoside,Ⅷ),其中Ⅳ为一新化合物,命名为绿舒筋酮(mupinensisone)。并归属了Ⅴ和Ⅵ的化学位移。     

露蕊乌头的二萜生物碱

从露蕊乌头(Aconitum gymnandrum Maxim)中分离到11个二萜生物碱,利用光谱方法确定结构,证明其中一个为新生物碱,命名为露乌定,其余10个分别鉴定为14-乙酰基-8-O-甲基-塔拉胺(tal-atisamine,Ⅱ)、acoforine(Ⅲ)、非洲防己碱(columbidine,Ⅳ)、乌头碱(aconitine,Ⅴ)、ranaeonitine(Ⅵ)、塔拉定(talatizidine,Ⅶ)、异塔拉定(isotalatizidine.Ⅷ)、露乌碱(gymanaconitine,Ⅸ)、塔拉胺(talatisamine,Ⅹ)和阿替辛盐酸盐(atisine.HCl)。其中碱Ⅱ为首次在自然界中发现,碱Ⅲ～Ⅶ为首次从该植物中分离得到。     

东阳元胡块茎中的生物碱的化学研究

从浙江省东阳元胡(Corydalis turtschaninovii Bess.f.yanhusuo Y.H.Chou et C.C.Hsü)的块茎中分离了15个生物碱。通过理化常数测定,光谱分析及衍生物制备等方法鉴定了结构,其中9个生物碱文献已报道。(+)-紫堇碱(Ⅰ),(±)-四氢巴马亭(Ⅱ),(—)-四氢黄连碱(Ⅲ),(—)-四氢非洲防己胺(Ⅳ),(+)-紫堇球碱(Ⅴ),去氢紫茧碱(Ⅵ),(+)-海罂粟碱(Ⅶ)普鲁托品(Ⅷ),α-别隐品碱(Ⅸ),5个为首次从该植物中得到的已知化合物(—)-四氢小檗碱(Ⅹ)巴马亭(Ⅺ),非洲防己胺(Ⅻ),(+)-N-甲基樟苍碱(ⅩⅢ)去氢海罂粟碱(ⅩⅣ),1个为新生物碱,暂命名为元胡宁(XV yuanhunine).     

知母化学成分的研究

从知母根茎乙醇提取物中分离得到20个化合物，采用光谱法和化学方法鉴定其中15个化合物的结构；分别为二十九烷醇（Ⅰ）、二十八烷酸混合物（Ⅱ）、β-谷甾醇（Ⅲ）、胡萝卜甙（Ⅳ）、菝葜皂甙元（Ⅴ）、马尔可皂甙元（Ⅵ）、知母皂甙AⅢ（Ⅶ）、知母皂甙BⅠ（Ⅷ）、知母皂甙BⅢ（Ⅸ）、2，6，4＇-三羟基-4-甲氧基苯酰酮（Ⅹ）、宝藿甙Ⅰ（Ⅺ）、淫羊藿甙-Ⅰ（Ⅻ）、芒果甙（ⅩⅢ）、7-O-萄葡糖基芒果甙（ⅩⅣ）、知母双糖（ⅩⅤ）．其中化合物Ⅷ为新的天然产物，化合物Ⅰ，Ⅺ，Ⅻ，ⅩⅣ为首次从知母中分得的已知化合物．     

藏药薰倒牛的活性物质研究

从植物藏药薰倒牛(BiebersteiniaheterostemonMaxim.)中首次分离得7个化合物,经化学方法和光谱解析鉴定为:β-谷甾醇(Ⅰ)、胡萝卜甙(Ⅱ)、伞形花内酯(Ⅲ)、5,7,3′-三羟基-8,4′,5′-三甲氧基黄酮(Ⅳ)、木犀草素-7-葡萄糖甙(Ⅴ)、槲皮素-7-葡萄糖甙(Ⅵ)和N-3-甲基-2-丁烯基脲(Ⅶ)。其中Ⅳ和Ⅶ是二个新的天然产物。药理实验表明化合物Ⅶ有镇痛、降压等活性。     

新疆藁本有效成分研究

从新疆藁本(ConiselinumvaginatumThell)的根茎中分到七个化合物,根据理化常数和光谱解析,分别鉴定为coniselin(Ⅰ),(E)-3-methoxy-4,5-methyenedioxycinnamicaldehyde(Ⅱ),(E)-3-methoxy-4,5-methylenedioxycinnamicalcohol(Ⅲ),(E)-3-methoxy-4,5-methylenedoxycinnamicacid(Ⅳ),肉豆劳动蔻酸(myristicicacid,V),阿魏酸(ferulicacid,Ⅵ)和香草醛(vanilin,Ⅶ)。其中Ⅰ为新化合物,其余均为首次从该植物中分到。经药理实验表明化合物Ⅱ～Ⅴ对四氯化碳引起的小鼠转氨酶升高有降低作用,对丙酸杆菌引起的小鼠免疫性肝损伤有保护作用。     

海芒果Cerbera odollam果仁中强心甙的分离鉴定

从海南岛产的海芒果Cerbera odollam果仁中分离到四种强心多糖甙monoacetyl-the-vetinB(Ⅰ)⁽¹⁾ thevetin B(Ⅲ)⁽²⁾及它们的7β,8β环氧衍生物tanghinoside(Ⅱ)⁽³⁾ desacetyl-tanghinoside(Ⅳ)。经果仁中的酶水介获得相应四个单糖甙Cerberin(Ⅴ)⁽⁴⁾ neriifolin(Ⅶ)⁽⁵⁾ tang hinin(Ⅵ)⁽⁶⁾ desacetyl-tanghinin(Ⅷ)⁽⁶⁾ tanghinoside,tanghinin及desacetyl-tanghinin以前未从Cerbera odollam中分到过。甙Ⅳ为一新甙。     

紫丁香有效成分的研究

木樨科植物紫丁香(Syringa oblata Lindl.)在我国分布较广,资源丰富。紫丁香有抗菌作用,民间用叶的水煎液洗眼敷疮治疗暴发火眼及多种疮疡肿痛,黑龙江中医学院等单位用紫丁香叶提取物治疗菌痢,吉林白求恩医科大学用以治疗急性黄疸型肝炎,均收到较好的疗效。有关丁香属植物的化学研究,国内外做了大量工作,先后从洋丁香(Syringa