13-Hydroxy-9Z,11E,15E-octadecatrienoic acid from the leaves of Cucurbita moschata

A new unsaturated hydroxy fatty acid was isolated from the leaves of Cucurbita moschata through repeated silica gel column chromatography and chemical methods. The structure of the new fatty acid was determined as 13-hydroxy-9,11,15-octadecatrienoic acid on the basis of several spectral data including 2D-NMR. The stererostructures of double bonds were determined to be 9Z, 11E and 15E by coupling patterns of related proton signals in the 1H-NMR and NOESY experiments.     

北马兜铃的化学成分研究——Ⅱ、马兜铃酸E的化学结构

From the root of Aristolochia contorta Bunge six chemical constituents were isolated; one of them is a new phenanthrene compound containing nitro group for which the name aristolochic acid E is suggested. By means of spectral methods combined with chemical analysis the chemical structure of aristolochic acid E was determined to be 7-methoxy-8-hydroxy-aristolochic acid. The other components were identified as allantoin, aristolochic acid A, magnoflorine, β-sitosterol and daucosterol respectively.     

A new cytotoxic acyclic diterpene fromCarpesium divaricatum

A new acyclic diterpene (1) and a known acyclic diterpene, 12(S)-hydroxygeranylgeraniol (2) were isolated from the aerial parts of Carpesium divaricatum. The structure of 1 was determined to be (2E,10E)-1,12-dihydroxy-18-acetoxy-3,7,15-trimethylhexadeca- 2,10,14-triene (1) on the basis of spectroscopic studies. Compounds 1 and 2 exhibited cytotoxicity against cultured human tumor cell lines, A549, SK-OV-3, SK-MEL-2, XF498, and HCT15, with ED50 values ranging from 4.3-10.2 micrograms/ml and 4.1-8.3 micrograms/ml, respectively.     

N2-芳基三嗪青霉素和N2-苯基-N4-烷基(芳基)三嗪青霉素的合成及其抗菌活性

设计合成了十个N²-芳基三嗪青霉素和六个N²-苯基-N⁴-烷基(芳基)三嗪青霉素,这十六个化合物均为未见文献报道的新化合物,元素分析数据和光谱数据证实了它们的结构。初步体外抑菌试验表明,十六个化合物对G(+)菌和G(-)菌均有一定的活性,其中的五个化合物具有一定程度的广谱特征。     

A new homoisoflavan from Caesalpinia sappan

A new homoisoflavan, 7,3′,4′-trihydroxy-3-benzyl-2H-chromene (1), was isolated from the dried heartwood of Caesalpinia sappan L., together with seven known phenolic compounds. The structure of the new compound (1) was determined on the basis of spectroscopic analysis.     

Structural studies on minor enniatins from Fusarium sp. VI 03441: Novel N-methyl-threonine containing enniatins

A strain of a yet unidentified Fusarium sp. produced in addition to enniatins A1, B and B1 a number of minor enniatins. The strain formed a well supported clade with strains identified as Fusarium acuminatum (Gibberella acuminata) in phylogenetic analyses using the TEF-1α gene sequences. Two of the minor enniatins were easily recognised as hydroxylated species on the basis of their fragment ion spectra. The hydroxylation could be traced to one of the amino acid moieties using multiple-stage ion trap mass spectrometry. Different approaches for acetylation of the isolated compounds and complete hydrolysis supported the elucidation of the amino acid moiety as 3-hydroxy-2-methylamino-butyric acid, which is equivalent with N-methyl-threonine. The primary structures of the two enniatins were tentatively determined to be cyclo[Hiv-N-Me-Val-Hiv-N-Me-Val-Hiv-N-Me-Thr] and cyclo[Hiv-N-Me-Leu-Hiv-N-Me-Val-Hiv-N-Me-Thr]. The two depsipeptides represent new analogues and were named enniatin P1 and P2, respectively.     

New butyrylcholinesterase inhibitory steroid and peroxy acid from Leucas urticifolia

A new steroid leucisterol (1) and a new peroxy acid urticic acid (2) along with methoxybenzyl benzoate (3), 4-hydroxy benzoic acid (4), beta-sitosterol (5), and ursolic acid (6), have been isolated from the chloroform soluble fraction of the whole plant of Leucas urticifolia. Their structures were elucidated on the basis of nuclear magnetic resonance (1D and 2D NMR) spectral data. Leucisterol showed potent inhibitory activity against butyrylcholinesterase enzyme.     

A quinic acid ester from Strychnos lucida

A new quinic acid ester, 4-O-(3,5-dimethoxy-4-hydroxybenzoyl)quinic acid (1) was isolated, together with 22 known compounds, from the barks and woods of Strychnos lucida. The structure of the new compound was determined by spectroscopic (NMR, MS) and chemical means.     

雪松松针中莽草酸的分离及其纯度检查

目的从雪松松针中提取分离莽草酸并进行纯度检查。方法采用水提、萃取、柱层析、重结晶等步骤分离纯化莽草酸,用NMR和理化性质鉴定其结构,再采用TLC和HPLC对其纯度进行检查。结果分离得到的莽草酸纯度达95％以上,得率为0．72％。结论该法简便经济、合理可行,可用于雪松松针中莽草酸的提取分离。     

刺梨酸的分离与结构研究

从刺梨中分离出一种新的五环三萜酸,命名为刺梨酸。通过光谱分析和衍生物的制备,确定其化学结构为2β,3α,7β,19α-四羟基乌苏-12-烯-28-羧酸。     

dl-扁桃酸对人精子与阴道黏膜上皮VK2/E6E7细胞的毒性研究

目的探讨dl-扁桃酸对人阴道黏膜上皮细胞(VK2/E6E7)与精子的细胞毒性损伤。方法不同浓度的dl-扁桃酸处理高活力精子20 s,计算机辅助精子分析仪测定精子活率,扫描电子显微镜检测精子受损情况。1.25,2.5 g·L?1 dl-扁桃酸和4.0 g·L?1壬苯醇醚(nonoxynol-9,N-9)处理VK2/E6E7细胞,MTT法检测细胞活性,ELISA试剂盒检测乳酸脱氢酶(LDH)释放率,并用流式细胞法检测细胞凋亡率。结果 dl-扁桃酸抑制精子活率的半数有效浓度约为1.25 g·L?1,最低有效浓度约为2.5 g·L?1。扫描电镜结果显示,dl-扁桃酸处理组精子表面结构与对照组形态相似,无明显受损特征,N-9组精子严重受损。MTT实验结果表明,1.25 g·L?1 dl-扁桃酸组细胞存活率>95%,2.5 g·L?1 dl-扁桃酸组细胞存活率约为50%。1.25,2.5 g·L?1 dl-扁桃酸处理组LDH释放量只有微量检出,远低于N-9组。流式细胞检测表明,1.25,2.5 g·L?1 dl-扁桃酸处理组中活细胞和晚期凋亡比例与对照组相近,早期凋亡细胞略少于对照组,死亡细胞稍多于对照组,N-9组大量细胞死亡。结论 dl-扁桃酸对VK2/E6E7细胞毒性远低于N-9,其对精子的抑制作用不是通过破坏精子质膜与鞭毛来实现。     

Studies on the chemical constituents of green leaves of <Emphasis Type="Italic">Eucommia ulmoide</Emphasis>s Oliv.

From the green leaves of Eucommia ulmoides Oliv., 12 compounds were isolated: asperuloside, asperulosidic acid, scandoside 10-O-acetate, deacetyl asperulosidic acid, geniposidic acid, aucubin, isoquercetin, quercetin 3-O-sambubioside, rutin, astragalin, kaempherol 3-O-rutinoside and chlorogenic acid. The structures were determined on the basis of spectral data.     

Tungtungmadic acid, a novel antioxidant, fromSalicornia herbacea

Tungtungmadic acid (3-caffeoyl-4-dihydrocaffeoyl quinic acid) is a new chlorogenic acid derivative that was isolated from the Salicornia herbacea. The structure of tungtungmadic acid was determined using chemical and spectral analysis. The antioxidant activity of tungtungmadic acid was evaluated using various antioxidant assays, including free radical scavenging, lipid peroxidation and hydroxyl radical-induced DNA strand breaks assays. Tungtungmadic acid (IC50 = 5.1 microM and 9.3 microM) was found to have higher antioxidant activity in the DPPH scavenging assay as well as in the iron-induced liver microsomal lipid peroxidation system. In addition, the tungtungmadic acid was also effective in protecting the plasmid DNA against strand breakage induced by hydroxyl radicals.     

岩筋菜中三萜的研究

从岩筋菜(Bemevxia thibetica Decne)地上部分的乙醇提取物中分得四个三萜,经光谱解析鉴定了一个新化合物,16α,21β,22α,28-四羟基齐墩果-12-烯-3-酮,命名为岩筋菜素(bemeuxin,Ⅰ)。其余三个是已知物,即21-惕各酰基玉蕊皂甙元C(Ⅱ),2α,3α-二羟基乌苏酸(Ⅲ)和2α,3β-二羟基乌苏酸(Ⅳ)。     

Acetylsalicylic acid—inducer of cytochrome P-450 2E1?

Pretreatment of rats with acetylsalicylic acid or sodium salicylate stimulates the metabolism of dichloromethane to carbon monoxide as measured by the carboxyhemoglobin level in blood. Simultaneous administration of dichloromethane and acetylsalicylic acid or sodium salicylate, respectively, was accompanied by reduced carboxyhemoglobin formation. In liver microsomes of rats pretreated with acetylsalicylic acid thep-nitrophenol hydroxylase activity was increased. It is concluded that (i) cytochrome P-450 2E1 is involved in the metabolic conversion of both dichloromethane and salicylic acid, and (ii) salicylic acid may be an inducer of cytochrome P-450 2E1.     

蒙药材飞廉的定性及定量研究

目的建立飞廉药材的定性及定量方法。方法分别采用化学法和薄层色谱法对飞廉药材中的黄酮类成分和绿原酸进行定性鉴别,并采用高效液相色谱法测定绿原酸的含量。色谱柱为Hypersil ODS2柱（4．6mm×250mm,5μm）;流动相为甲醇．0．5％醋酸（15：85）;流速为1．0mL·min-1;柱温为25℃;检测波长为32513131。结果定性鉴别试验特征明显,绿原酸在0．088～1．76μg内呈良好的线性关系,平均回收率为100．3％（RSD为1．52％）。结论该方法简便、快速,重复性好,准确度高,可有效控制飞廉药材的质量。     

Isocoumarin derivatives from the sea squirt-derived fungus penicillium stoloniferum QY2-10 and the halotolerant fungus penicillium notatum B-52

Two isocoumarin derivatives, stoloniferol A (1) and B (2), a known 5alpha, 8alpha-epidioxy-23-methyl-(22E, 24R)-ergosta-6, 22-dien-3beta-ol (3), and a known dihydrocitrinone (4) were isolated from the ethyl acetate extract of the sea squirt-derived fungus, Penicillium stoloniferum QY2-10, and a halophilic fungus, Penicillium notatum B-52, respectively. Their structures were elucidated by spectroscopic methods and optical rotation. The stereochemistry of 2 was determined on the basis of different NOE experiments and chemical transformation. Compound 3 showed cytotoxicity against P388 cells, with an IC50 value of 4.07 microM.     

Antioxidant flavonoids and chlorogenic acid from the leaves ofEriobotrya japonica

The antioxidant activity of Eriobotrya japonica was determined by measuring the radical scavenging effect on DPPH (1,1-diphenyl-2-picrylhydrazyl) radical and lipid peroxidation produced when mouse liver homogenate was exposed to the air at 37 degrees C, using 2-thiobarbituric acid (TBA). The methanol extract and its fractions of Eriobotrya japonica leaves showed strong antioxidant activity. The antioxidant activity of EtOAc and n-BuOH soluble fractions were stronger than the others, and were further purified by repeated silica gel, MCl gel CHP-20P, and Sephadex LH-20 column chromatography. Antioxidant chlorogenic acid, quercetin-3-sambubioside from n-BuOH fraction, and methyl chlorogenate, kaempferol- and quercetin-3-rhamnosides, together with the inactive ursolic acid and 2 alpha-hydroxyursolic acid from EtOAc fraction were isolated. Antioxidant flavonoids and chlorogenic acid also showed prominent inhibitory activity against free radical generation in dichlorofluorescein (DCF) method.     

桔梗中远志酸型皂苷的化学研究

目的分离、鉴定桔梗［Platycodon grandiflorum (Jacq.)A.DC］根中的远志酸型皂苷类化学成分。方法 采用乙醇提取、乙酸乙酯萃取，大孔树脂柱色谱、硅胶柱色谱及高效液相色谱等方法进行分离，得到3个化学成分，运用IR，MS，¹H NMR和¹³C NMR等光谱法鉴定化合物的结构。结果分离鉴定了3种三萜皂苷：3-O-β-D-laminaribiosyl polygalacic acid (I)，3-O-β-D-glucopyranosyl polygalacic acid (II)及polygalacin D (III)。结论化合物I是新化合物，II，III为已知化合物。化合物II为首次从该植物中分得，化合物I和II也是首次从桔梗中分离得到的单糖链糖苷。     

多舌飞蓬甙的分离和结构

从多舌飞蓬[Erigeron multiradiatus(Wal.)Benth.]全草中分离得到12个化合物,其中5个经理化性质和光谱分析鉴定为:焦袂康酸(I)、东莨菪素(II)、对羟基苯甲酸(II)、香草酸(IV)、γ-吡喃酮-3-氧-[6″-(3′,4′-二羟基桂皮酰)]-β-D-葡萄糖甙(V)。其中II,II,IV为首次从该属植物中获得,V为一新化合物,命名为多舌飞蓬甙(6′-O-cafeylerigeroside)。