苦红菇化学成分的研究

从野生真菌苦红菇(Russula rosacea(Bull)Grrayem,Fr.)子实体酸性部分得到两个新的四环三萜酸化合物,经光谱(IR,¹HNMR,¹³CNMR,MS)、尤其是二维核磁共振(¹³C-¹HCOSY,COLOC,NOEDIFF)谱解析,确定其结构分别如Ⅰ和Ⅱ所示,Ⅰ命名为苦红菇酸A(rosaceaacidA),Ⅱ为苦红菇酸B(rosaceaacidB)。     

大花哥纳香碱Ⅰ的结构鉴定

目的：研究云南西双版纳的大花哥纳香(Goniothalamus griffithii Hook.f.et Thoms)茎皮的化学成分。方法：采用各种色谱技术进行分离,用IR,UV,MS,¹HNMR,¹³CNMR光谱鉴定化合物。 结果：得到2个化合物,分析鉴定为:10-氨基-4-羟基-3,8-二甲氧基菲-1-羧酸内酰胺(Ⅰ),命名为大花哥纳香碱Ⅰ;3,4,5-三甲氧基苯-1-O-β-D-葡吡喃糖苷(Ⅱ)。结论：Ⅰ为新化合物,Ⅱ为首次从该植物中分离得到。     

祁州漏芦蜕皮甾酮类化学成分的研究

从祁州漏芦[Rhaponticum uniflorum(L.)DC.]的根中,分离出三个蜕皮甾酮类化合物Ⅰ,Ⅱ,Ⅲ,其中Ⅱ根据UV,IR,MS,¹³CNMR,¹HNMR,¹H-¹HCOSY,¹H-¹HNOESY,¹H-¹³C COSY,及CD谱确定其结构为(20R,22R,24S)-2β,3β,11α,14α,20,22,24-heptahydroxy-5β-cholest-7-en-6-one,为一新化合物,命名为漏芦甾酮(rhaponfisterone)。化合物Ⅰ和Ⅲ分别鉴定为蜕皮甾酮(ecdysterone)和土克甾酮(turkesterone)。     

赤芝孢子粉三萜化学成分研究

自赤芝(Ganoderma lucidum Karst)孢子粉酸性部分分离得到一个新的四环三萜化合物,命名为ganosporeric acid A(1),根据光谱(IR,¹HNMR,¹³CNMR和MS)分析确定其结构为Ⅰ所示。同时还分到四个已知化合物:ganoderic acid B(Ⅱ),ganodefic acid C(Ⅲ),ganoderic acidE(Ⅳ),和ganodermanontriol(Ⅴ)。这些化合物均为首次从赤芝孢子粉中得到。     

何首乌乙酸乙酯不溶部分化学成分的研究

从四川何首乌(polygonu mnultiflorum Thunb)块根乙醇提取物的乙酸乙酯不溶部分分离得到五个单体,经理化常数测定,光谱(IR,UV,FAB-MS,¹HNMR,¹³CNMR,¹H-¹³CCOSY和NOE差谱)分析及衍生物制备,确定了两个化合物的结构为新化合物。化合物Ⅰ1,3-二羟基-6,7-二甲基酮-1-O-β-D-葡萄糖甙,命名为何首乌乙素,化合物Ⅱ为2,3,5,4′-四羟基-二苯乙烯-2,3-二-O-β-D葡萄糖甙,命名为何首乌丙素。其余三个结晶因量少有待进一步分离、鉴定。     

华北白前中的新三萜成分

从华北白前(Cynanchum hancockianum)中分离到4个新三萜类化合物,通过光谱分析(¹HNMR,¹³CNMR,2DNMR,MS,X-Ray)及化学相关等分别鉴定为华北白前醇(hancockinal,Ⅰa).新自前醇(hancolupenoI,Ⅱd),新白前酮(hancolupenone,Ⅱc)及新白前醇二十八烷酸酯(hancolupenol octacosanate,Ⅱd),均为新型骨架的化合物。     

狭叶香蒲花粉(蒲黄)黄酮类成分的研究

自香蒲科(Typhaceae)植物狭叶香蒲(Typha augustifolia L.)的干燥花粉中分离到五个黄酮醇甙,包括两个黄酮醇-3-三糖甙(Ⅰ,Ⅱ)和三个黄酮醇-3-双糖甙(Ⅲ,Ⅳ,Ⅴ)。其中,化合物Ⅰ是一个新的黄酮醇甙,为本植物的主要成分,经光谱分析(UV,IR.MS;¹HNMR和¹³CNMR)和水解试验确定为异鼠李素-3-0-(2_G-α-L-鼠李糖基)-α-L-鼠李糖(1→6)-β-D-葡萄糖甙,命名为香蒲新甙(typhaneoside,Ⅰ)。其它四种为已知成分。Ⅱ从本属植物中首次发现。     

川产九节龙皂甙的化学研究

从川产九节龙(Ardisea pusilla A. DC)的正丁醇提取物中分离到两个三萜皂甙。经化学和光谱(IR,MS,¹HNRM,¹³CNMR和两种新的核磁技术)分析,两个化合物的结构分别鉴定为3-O-[α-L-吡喃鼠李糖(1→2)-β-D-吡喃葡萄糖(1→3)][B-D-吡喃葡萄糖(1→2)]-α-L-阿拉伯糖-西克拉敏A(Ⅰ)和3-O-[β-D-吡喃木糖(1→2)-B-D-吡喃葡萄糖-(1→4)][B-D-吡喃葡萄糖-(1→2)-β-D-吡喃葡萄糖(1→2)]-α-L-吡喃阿拉伯糖-西克拉敏A(Ⅱ)。二者均为新皂甙,依次命名为九节龙皂甙Ⅰ(ardipusilloside Ⅰ)和九节龙皂甙Ⅱ(ardipusillosidc Ⅱ)。     

金不换(口山)酮成分的研究Ⅰ.金不换甙及甙元的结构

从民间草药金不换(Veratrilla baillonii Franch.)根中提取分离得三种咄酮类化合物,经化学方法及光谱法分析(UV,IR,MS,¹HNMR.¹³CNMR)证明,一种为1-羟基2,3,4,7-四甲氧基(口山)酮(Ⅲ)。其它两种为新化合物1,7-二羟基3,4-二甲氧基咄酮(Ⅰ);1-羟基7-0-β-D-吡喃葡萄糖基3,4-二甲氧基(口山)酮(Ⅱ)。     

叶下珠化学成分的研究

从叶下珠(Phyllantlais urinaria L.)的干燥全草中分得11个化合物。经光谱分析(UV,IR,¹HNMR,¹³C-NMR,¹H-¹H COSY,¹³C-¹H COSY,long range ¹³-¹H COSY,DEPT and MS)和化学反应等,鉴定了其中10个化合物,分别为正十八烷(Ⅰ),β-谷甾醇(Ⅲ),鞣花酸(Ⅳ),胡萝卜甙(Ⅴ),短叶苏木酚酸甲酯(methyl brevifolincarboxylate,Ⅵ),山萘素(Ⅶ),槲皮素(Ⅷ),去氢诃子次酸三甲酯(trimethyl ester dehydrochebulic acid,Ⅸ),没食子酸(Ⅹ),芸香甙(Ⅺ)。晶Ⅱ为一醛类化合物,结构正在鉴定中,晶Ⅵ和Ⅸ为新化合物。     

云南红豆杉抗肿瘤活性成分的研究

云南红豆杉(Taxus yunnanensis Cheng et L.K.Fu)树皮的乙醇提取物显示较强的抗肿瘤活性,从中分离得到8个紫杉烷类二萜及其生物碱。经光谱分析和化学反应鉴定7个已知物为taxinine E(1),taxinine J(2),1-acetoxy-5-deacetvl baccatin Ⅰ(4),baccatin Ⅲ(5),taxol(6),cephalomannine(7)和7-xylosyl-10-deacetyl taxol(8)。化合物3命名为云南红豆杉甲素(ymlnanxane),为一新的紫杉烷二萜化合物,其结构为taxa-4(20),11-diene-2α,5α,10β,14β-tetraol-2α,5α,10β-triacetate-14β-αmethyl-β-hydroxyl butyrate,并通过X-射线单晶衍射予以证实.经体外筛迭化合物3具有抗肿瘤活性。     

用二维核磁共振技术研究野菊花三醇的结构

从野菊花(Chrysanthemum indicum L.)亲脂性极性较大的部分,分离得到一个新的倍半萜成分,命名为野菊花三醇。通过¹H-¹H COSY,¹H-¹³C COSY及远程¹H-¹³C COSY二维核磁共振谱研究,确定其属于(牛龙)牛儿烷衍生物,并确定其结构和相对立体构型。     

豨莶脂溶性成分的研究

从豨莶(Siegesbeckia orientalis L.)的地上部分,分离出八个化合物,其中I和I根据理化性质和光谱数据确定其结构为ent-17-acetoxy-18-isobutyryloxy-16(α)-kauran-19-oicacid(I)和ent-17-ethoxy-16(α)-kauran-19-oicacid(II),均为新化合物,分别被命为豨莶酯酸(siegesesteric acid,I)和豨莶醚酸(siegesetheric acid,I)。其余化合物分别鉴定为腺梗豨莶萜醇酸(ent-16β,17-dihydroxy-kauran-19-oicacid,II),奇任醇(kirenol,IV,β-谷甾醇葡萄糖甙(β-sitosterolglucoside,V),二十一醇(heneicosanol,VI),花生酸甲酯(methyl arachidate,VII)和β-谷甾醇(β-sitosterol,VII)。除奇任醇和β-谷甾醇外,均为首次从该植物中分得。     

苦山柰化学成分的研究

目的　研究中药山柰的混杂品种苦山柰Kaempferia marginata Carey的化学成分。方法　利用色谱技术进行分离纯化, 根据化合物的理化性质和光谱数据进行结构鉴定。结果　从苦山柰的根茎分得苦山柰萜醇(1)、8(14),15-sanderacopimaradiene-1α,9α-diol (2)、8(14),15-sanderacopimaradiene-1α,6β,9α-triol (3)、吉马酮(4)、对-甲氧基-肉桂酸乙酯(5)和正-十五烷(6)。结论　苦山柰萜醇(1)为新二萜醇, 化学结构为8(14),15-isopimaradiene-6α-ol。2, 3和4是首次从该植物中分得。     

秦岭珠子参叶的达玛烷型皂甙的进一步研究

前已报道秦岭产珠子参(Panax japonicus var.mojor (Burk.) Wu et Feng)叶的九个达玛烷型皂甙成分。本文继续报告得自珠子参叶的另外两个新的同类皂甙成分。珠子参甙F_σ(Ⅰ) 由甲醇中得白色粉末,分子式:C_(48)H_(82)O_(19);正、反相薄层层析示为单一斑点;PPC检查Ⅰ的酸水解物中有葡萄糖和鼠李糖存在:FAB-MS给出分子离子峰m/z 985 (M Na)~ 及碎片峰716(M-162-2H_2O 2H)~ ,619(M-162-146-2H_2O H)~ ,439(M-2×162-146-3H_2O 2H)~ ,说明Ⅰ中含有二个葡萄糖和一个鼠李糖。     

Three major urinary metabolites of sinomenine in rats

Urinary metabolites of sinomenine were investigated in rats after intragastric administration. Three major metabolites were obtained and characterised as 4-hydroxy-3,7,7-trimethoxy-17-methyl-(9alpha,13alpha,14alpha)-morphinan-6-one (1), 7,8-didehydro-4-hydroxy-3,7-dimethoxy-17-methyl-N-oxide-(9alpha,13alpha,14alpha)-morphinan-6-one (2), and 7,8-didehydro-4-hydroxy-3,7-dimethoxy-(9alpha,13alpha,14alpha)-morphinan-6-one (3). Their structures have been elucidated on the base of spectral analysis, among which 1 and 2 were new compounds.     

Preclinical studies with IL-13PE38QQR for therapy of malignant glioma

To develop novel therapeutic agents for the treatment of brain tumors, we have been investigating the expression of unique tumor-associated receptors or antigens on the tumor cell surface. About six years ago, we discovered that human solid tumor cell lines, including human malignant glioma, express high- to intermediate-affinity receptors (R) for a Th2 cell-derived cytokine, interleukin-13 (IL-13). Analysis of the subunit composition of IL-13R in primary explants of malignant glioma cells has demonstrated that IL-13R is composed of three different chains (IL-13R alpha 1, IL-13R alpha 2 and IL-4R alpha, also known as IL-13R alpha', alpha and IL-4R beta, respectively) and that IL-13R alpha 2 chain is overexpressed on these cells. Normal brain tissues express IL-13R alpha 1 and IL-4R alpha chains, but show only marginal expression of IL-13R alpha 2 chain. Thus IL-13R alpha 2 chain appears to be overexpressed on glioma cells and may serve as a novel tumor biomarker or a target for receptor-directed therapeutic agents for brain tumors. To target IL-13 receptors, we have produced a recombinant fusion protein composed of IL-13 and a mutated form of Pseudomonas exotoxin (PE). This cytotoxin, termed IL-13PE38QQR or IL-13 cytotoxin, is highly and specifically cytotoxic to a spectrum of human glioma cell lines. In preclinical models of human glioblastoma tumors growing subcutaneously in immunodeficient mice, IL-13 cytotoxin has been found to have remarkable antitumor activity. The data that emerged from these studies reveal that localized or systemic administration of IL-13 cytotoxin can produce nontoxic drug levels and that IL-13 cytotoxin is potently effective against established glioblastoma tumors. On the basis of these and other preclinical studies, we have begun a phase I clinical trial using IL-13PE38QQR for therapy of recurrent malignant glioma.     

New cytotoxic sesquiterpene lactones from Warionia saharae

Cytotoxicity-guided fractionation of the methanol soluble part of the dichloromethane extract of the leaves of Warionia saharae led to the isolation of the two new guaianolide-type sesquiterpene lactones, 5 alpha H-3 beta,4 beta-epoxy-14-oxo-guaia-1(10),11(13)-dien-6 alpha,12-olide (1), 5 alpha H-2 beta,4 beta-epoxy-3 alpha-hydroxy-guaia-1(10),11(13)-dien-6 alpha,12-olide (6), and the new eudesmane type sesquiterpene 1 beta,6 alpha-dihydroxycostic acid ( 4). In addition, the known sesquiterpene lactones 5 alpha H-2 beta-hydroxyguaia-3(4),10(14),11(13)-trien-6 alpha,12-olide (2), reynosin (3), 5 alpha H-1 alpha,10 alpha:3 alpha,4 alpha-diepoxyguaia-11(13)-en-6 alpha,12-olide (5), and dehydroleucodin (7) were isolated together with the known flavone hispidulin. Cytotoxicity testing of the sesquiterpene lactones against the KB cancer cell line (ATCC CCL17) revealed IC50 values of 3.5 (1), 2.6 ( 2), 2.7 ( 3), 4.3 ( 5), 3.6 ( 6), and 1.3 (7) microg/mL. Compound 4 was not active up to 20 microg/mL.     

中药路路通化学成分的研究

目的研究中药路路通(Fructus liquidambaris)的化学成分。方法用色谱法分离路路通的化学成分,根据理化性质和波谱数据鉴定其结构。结果分离得到11个化合物,分别鉴定为:β-谷甾醇(1),3-oxo-11α,12α-epoxyoleanan-28,13β-olide (2),3-oxo-12α-hydroxy-oleanan-28,13β-olide (3),3α-acetoxyl-25-hydroxyolean-12-en-28-oic acid (4),齐墩果酸(5),熊果酸(6),胡萝卜苷(7)桦木酮酸(8),没食子酸(9),正二十九烷(10),正三十烷酸(11)。结论4为新化合物,3为首次从天然产物中分离得到,5,6,7,9,10和11为首次从路路通中分离得到。