猴头菌丝体多糖的化学研究

目的:对猴头菌丝体的多糖类成分进行化学组成及结构研究。方法:DEAE 纤维素、DEAE-Sephadex 柱分离,葡聚糖凝胶柱层析测定纯度,凝胶过滤法测定分子量,酶解、气相色谱及光谱分析等测定化学组成及结构。结果和结论:从猴头菌丝体中分离得到5 个多糖均一体,其主要成分HEPA₁ 分子量6 .2 ×10⁴ ,为以葡萄糖为主的杂多糖,单糖组成摩尔比为葡萄糖∶阿拉伯糖∶木糖= 33 .1∶1 .7∶1 .0 ;HEPA₄ 分子量2 .6 ×10⁴ ,为杂多糖肽,肽部分由17 种氨基酸组成,占糖肽的3 .8 % ;HEPB2 分子量1 .2×10⁴ ,为以葡萄糖为主的杂多糖,单糖组成摩尔比为葡萄糖∶阿拉伯糖∶木糖∶甘露糖= 50 .7∶2 .1∶1 .0∶2 .4 。各均一体单糖间的甙键构型均以α-甙键为主。     

灵芝免疫活性多糖的化学研究

从灵芝中分离得到免疫活性多糖BN₃B,进一步分离纯化得到4个多糖均一体,对其中主要成分BN₃B₁及BN₃B₃进行化学研究证明,BN₃B₁为含β-(1→6)及(1→3)甙键的葡聚糖,BN₃B₃为含β-(1→6)及(1→3)甙键的阿拉伯半乳聚糖。     

单色云芝多糖的结构研究

 目的研究单色云芝多糖(CUP)的化学结构,并与云芝多糖进行比较。方法气相色谱分析糖组成,红外光谱(IR)、高碘酸氧化、甲基化、核磁共振(NMR)等方法确定多糖的结构。结果CUP单糖组成为葡萄糖,相对分子质量约1.3×10⁴,主要连接方式为β-(1→3)连接,此外包括α-(1→3),β-(1→6),α-(1→4),(1→3,6)和(1→4,6)连接。结论CUP的单糖组成和结构与云芝多糖相似,在相对分子质量、蛋白含量等方面有区别。     

徐长卿多糖的分离纯化与化学结构研究Ⅰ

 目的:研究中药徐长卿中一种葡聚糖的化学结构。方法:采用柱层析进行分离纯化,并用甲基化分析和¹³C-NMR等方法阐明多糖CPB-2IG的化学结构。结果:该多糖分子量为17×10⁴,由单一葡萄糖组成,比旋度为+1592°,构型为α型,单糖的连接方式为1,6连接。结论:CPB-2IG的化学结构为直链α-D--(1→6)葡聚糖。     

黑石耳多糖的初步化学研究

 目的：测定黑石耳(Dermatocarpon miniatum,DEM)多糖的组成、分子量及苷键的连接方式。方法：利用气相色谱法测定多糖的组成，凝胶过滤法测定分子量，Smith降解及高碘酸氧化确定苷键的连接方式。红外光谱测定苷键类型。结果：DEM多糖由葡萄糖聚合而成，平均分子量为1.8×10⁶。高碘酸氧化，Smith降解有甲酸、丙三醇、丁四醇生成。结论：DEM多糖主要由〖WTBX〗α(1→4)、α(1→6)苷键连接而成的葡聚糖。     

17β-雌二醇对骨髓基质细胞成骨、成脂分化和成骨细胞成脂横向分化的影响

 目的研究17β-雌二醇对小鼠原代骨髓基质细胞成骨、成脂分化以及小鼠原代成骨细胞成脂横向分化的影响。方法四甲基偶氮唑盐法(MTT)检测17β-雌二醇对骨髓基质细胞和成骨细胞增殖的影响,碱性磷酸酶(ALP)活性测定法检测17β-雌二醇对骨髓基质细胞成骨分化的影响,油红O染色形态学及定量测定法检测17β-雌二醇对骨髓基质细胞成脂分化和成骨细胞成脂横向分化的影响。结果1×10^-8,1×10^-7,5×10^-7,1×10^-6,5×10^-6和1×10^-5mol·L^-1的17β-雌二醇可以促进小鼠原代骨髓基质细胞和成骨细胞增殖(P<0.05);5×10^-7,1×10^-6,5×10^-6和1×10^-5mol·L^-1的17β-雌二醇促进骨髓基质细胞的成骨分化、抑制成脂分化,但是浓度为1×10^-7mol·L^-1的17β-雌二醇抑制骨髓基质细胞的成骨分化、促进成脂分化(P<0.05);浓度为1×10^-8,5×10^-7,1×10^-6,和1×10^-5mol·L^-1的17β-雌二醇抑制成骨细胞的成脂分化(P<0.05)。结论17β-雌二醇可以调节骨髓基质细胞向成骨细胞分化而减少其向脂肪细胞分化,并且可以抑制成骨细胞向脂肪细胞的横向分化。     

党参果聚糖的化学结构

目的:对中药党参中多糖进行研究。方法:DE-52纤维素和Sephadex G-200凝胶柱色谱分离纯化一多糖CPP-1。凝胶色谱法测定其纯度和分子质量。酸全水解,甲基化反应,高碘酸盐氧化及降解,IR,¹H-NMR和¹³C-NMR分析其结构。结果:CPP-1分子质量约为7.5×10⁴,化学结构为呋喃果糖以-β(2→1)连接而成的果聚糖。结论:该多糖为一中性的均一多糖。     

丹参多糖的提取分离及结构鉴定

目的：对中药丹参中多糖进行研究。方法：丹参药材经过水提醇沉得到丹参粗多糖,以DEAE-Sepharose Fast Flow 纯化后,以H₂O₂脱色,流水透析,冷冻干燥后得到2个浅黄色均一多糖SMP 1,SMP 0.5,经¹3C-NMR,DEPT,IR谱,单糖组分分析、部分酸水解等方法鉴定其结构。结果：SMP 1,SMP 0.5相对分子质量分别约为1.39×10⁶,4.03×10⁵,SMP 1主要以α-(1→6)D-Glc聚合而成,有少量的α-(1→2)D-Glc聚合；SMP 0.5主要由α-(1→6)D-Glc聚合而成。结论：SMP 1,SMP 0.5为从丹参中首次分离得到的中性均一多糖。     

灵芝孢子粉水溶性多糖SGL-Ⅲ的结构研究

 目的对从灵芝孢子粉中提取出来的纯多糖SGL-Ⅲ进行结构分析。方法多糖SGL-Ⅲ经比旋光、高效液相色谱法、苯酚-硫酸法确定物理性状后,再经部分酸水解、高碘酸氧化、Smith降解、甲基化分析及IR,GC,GC-MS和¹³C-NMR等方法确定其结构。结果SGL-Ⅲ相对分子质量为1.41×10⁴,由葡萄糖(Glc)和半乳糖(Gal)组成,摩尔比为4.46∶1,为少分支结构,其基本结构中主链由(1→3)Glc和(1→6)Gal构成,分支点分别在6-O,2-O及4-O处,(1→4)Gal或(1→6)Glc位于侧链,分支末端残基为Glc。结论多糖SGL-Ⅲ具有天然活性多糖的特征,可以对其进行药理活性的研究开发。     

雷公藤内酯醇抑制脂多糖诱导的PC-12细胞COX-2的表达

 目的　了解雷公藤内酯醇(TP)对PC-12细胞增殖和表达环氧化酶-2(COX-2)及合成前列腺素E₂ (PGE₂ )的影响 ,探讨TP应用于痴呆治疗的可能机制。方法　采用神经生长因子 (NGF)诱导培养PC-12细胞 ,用不同浓度的TP(0,0.28×10^-6,2.8×10^-6,2.8×10^-6mol·L^-1)预处理后 ,加或不加脂多糖(LPS),分别用氚-胸腺嘧啶核苷(³H-TdR)掺入法、竞争酶联免疫吸附试验(ELISA)、半定量逆转录-聚合酶联反应(RT-PCR)法、细胞酶联免疫法及蛋白免疫印迹 (Western-blot)法检测PC-12细胞的增殖活性、细胞培养上清液中PGE² 的水平、细胞COX-2mRNA及蛋白表达水平。同时提取各组细胞蛋白 ,测定其核转录因子 (NF-κB)活性。结果　TP对LPS诱导的PC-12细胞的COX-2mRNA ,蛋白表达 [空白对照与不同浓度下分别为[(0.34±0.12 )×10^-6,(1.92±0.26)×10^-6,(1.78±0.32)×10^-6,(1.14±0.22)×10^-6,(0.48±0.14 )×10^-6mol·L^-1,P <0.01]及PGE₂ 的合成 [分别为(2.28±0.32)×10^-6,(32.86±6.23)×10^-6,(31.28±5.44)×10^-6,(18.43±3.92)×10^-6,(4.18±1.79)×10^-6mol·L^-1,P<0.01]具有不同程度的抑制作用,与TP浓度(0～28×10^-6mol·L^-1)呈明显正相关性(分别为r=0.94和r=0.92),且对LPS激活的PC-12细胞的核转录因子NF-κB活性有明显的抑制作用[分别为(0.16±0.08)×10^-6,(1.39±0.18)×10^-6,(1.09±0.14)×10^-6,(0.52±0.15)×10^-6,(0.28±0.09)×10^-6mol·L^-1,P<1.01]。实验未观察到TP对PC-12细胞增殖的影响。结论TP可显著抑制LPS诱导的PC-12细胞COX-2细胞COX-2的表达及其产物PGE₂的合成,这种作用可能通过TP抑制PC-12细胞核转录因子NF-κB活性而实现。     

Hemolytic steroid disulfates from the far eastern starfish Pteraster pulvillus

Six steroidal ophiuroid-type disulfates, namely, disodium salts of (20R)-cholest-5-ene-3alpha,4beta,21-triol 3, 21-disulfate (1), (20R)-5alpha-cholestane-3alpha,4beta,21-triol 3,21-disulfate (2), (20R)-5alpha-cholestane-2beta,3alpha,21-triol 3,21-disulfate (3), and (20R)-5alpha-cholestane-3alpha,21-diol 3,21-disulfate (4), the dityrammonium salt of (20R)-5alpha-cholestane-3alpha,21-diol 3,21-disulfate (5), and a mixture of sodium and tyrammonium salts (1:1) of (20R)-cholest-5-ene-3alpha,21-diol 3,21-disulfate (6), have been isolated from the ethanolic extracts of Far Eastern starfish Pteraster pulvillus. Steroids 2 and 3 are new compounds. Steroids 1, 2, and 4-6 showed hemolytic activity to mouse erythrocytes with HC(50) values of 8.0 x 10(-5), 4.5 x 10(-5), 1.0 x 10(-5), 1.8 x 10(-5), and 3.3 x 10(-5) M, respectively.     

Furanosesquiterpenoids of Commiphora myrrha.

An investigation on the gum exudates of Commiphora myrrha has led to the isolation of six sesquiterpenoids. On the basis of spectroscopic data interpretation, they were determined as two new furanosesquiterpenoids, rel-1S,2S-epoxy-4R-furanogermacr-10(15)-en-6-one (1) and rel-2R-methyl-5S-acetoxy-4R-furanogermacr-1(10)Z-en-6-one (2), and four known furanosesquiterpenoids, rel-3R-methoxy-4S-furanogermacra-1E,10(15)-dien-6-one (3), rel-2R-methoxy-4R-furanogermacr-1(10)E-en-6-one (4), furanogermacra-1(10)Z,4Z-dien-6-one, and curzerenone [6,7-dihydro-5beta-isopropenyl-3,6beta-dimethyl-6-vinylbenzofuran-4(5H)-one]. This is the first report of the relative stereochemistry for the known compounds 3 and 4. Compound 1 exhibited weak cytotoxic activity against a MCF-7 breast tumor cell line in a clonogenic assay, while the other five compounds were inactive in this assay.     

红藻扇形叉枝藻中的降碳倍半萜及其衍生物

目的：对红藻扇形叉枝藻Gymnogongrus flabelliformis进行化学成分研究。方法：利用正相和反相硅胶柱色谱、Sephadex LH-20凝胶柱色谱和反相HPLC等手段进行分离纯化,借助MS,1D和2D NMR等波谱方法鉴定化合物结构；通过MTT法对分离鉴定的单体化合物在人肺癌细胞株(A549)、人肝癌细胞株(Bel 7402)、人胃癌细胞株(BGC 823)、人结肠癌细胞株(HCT-8)和人卵巢癌细胞株(A2780)上进行肿瘤细胞毒活性筛选。结果：从红藻扇形叉枝藻中分离得到5个降碳倍半萜类化合物,分别鉴定为(3S,6R,7E)-(+)-3-hydroxyl-4,7-megastigmadien-9-one(1),(3S,5R,6S,7E)-(-)-3-hydroxy-5,6-epoxy-7-megastig-mene-9-one(2),(3S,5S,6R,7E)-(+)3-hydroxy-5,6-epoxy-7-megastigmene-9-one(3),dehydrovomifoliol(4)和(3R)-(-)-4-［(2R,4S)-4-acetoxy-2-hydroxy-2,6,6-trimethylcyclohexylidene］-3-buten-2-one(5)。结论：以上化合物均为首次从该属海藻中分离得到,其中化合物1为新天然产物。细胞毒活性试验结果显示所有化合物在10 μg·mL^-1均无明显细胞毒活性。     

Iridoid glycosides of Leonurus persicus.

Two new iridoid glucosides, 6-O-acetylajugol (1) and 7, 8-epoxy-8-epi-loganic acid (2), together with five known iridoid glucosides, galiridoside (3), ajugoside (4), 10-deoxygeniposidic acid (5), 7-deoxy-8-epi-loganic acid (6), and 8-O-acetylharpagide (7), have been isolated from the aerial parts of Leonurus persicus. Leucosceptoside A (8), eugenyl beta-rutinoside (9), and kaempferol 3-O-glucoside (10) were also isolated. The structures of 1 and 2 were elucidated by extensive 1D- and 2D-NMR spectroscopy and molecular modeling. The structure of 3 was confirmed by single-crystal X-ray diffraction. Antimicrobial activity of compounds (1-10) was also evaluated against a panel of gram-positive and gram-negative bacteria and two strains of fungi.     

Eremophilane-type sesquiterpene derivatives from Senecio aegyptius var. discoideus

Investigation of a CH(2)Cl(2) extract of the aerial parts of Senecio aegyptius var. discoideus afforded nine eremophilane compounds, of which six are new (1-6), namely, 1beta-hydroxy-8alphaH-eremophil-7(11),9-dien-8beta,12-olide (1), 1beta,8alpha-dihydroxyeremophil-7(11),9-dien-8beta,12-olide (2), 1beta-hydroxy-8alpha-methoxyeremophil-7(11),9-dien-8beta,12-olide (3), 1-oxo-8alpha-methoxy-10alphaH-eremophil-7(11)-en-8beta,12-lactam (4), 1beta,10beta-epoxy-8alpha-hydroxyeremophil-7(11)-en-8beta,12-olide (5), and 1beta,10beta-epoxy-8alpha-methoxyeremophil-7(11)-en-8beta,12-olide (6). The structures of 1-6 were elucidated by spectroscopic methods and by comparison with literature data. The antibacterial activity of the isolated compounds was tested against Bacillus cereus and a Serratia sp.     

百两金根的化学成分研究

目的 百两金为传统苗药,其化学成分的有关研究报道较少,本研究目的在于研究百两金的化学成分。方法 将百两金干燥根体积分数70%乙醇提取物利用硅胶、重结晶、ODS及制备/半制备HPLC进行分离纯化,根据理化性质及波谱数据对所得化合物结构进行鉴定。结果 从百两金根中得到了20个化合物。分别为岩白菜素 (1)、甲基岩白菜素 (2)、11-O-没食子酰岩白菜素 (3)、 syringin (4)、(+)-syringaresinol-O-β-D-glucopyranoside (5)、(-)-(7R,8S,7′R,8′S)-4,9,4′,9′-tetrahydroxy-3,3′-dimethoxy-7,7′-epoxylignan-9-O-β-D-xylopyranoside (6)、saracoside (7)、isolariciresinol-4-O-β-D-glucopyranoside (8)、(7S,8R)-urolignoside (9)、staphylionoside D (10)、蚱蜢酮 (11)、l-borneol 6-O-β-D-aiosyl-β-D-glucoside (12)、(+)-angelicoidenol 2-O-β-D-glucopyranoside (13)、牡荆素-2″-O-鼠李糖苷 (14)、根皮苷 (15)、phenethyl alcohol β-D-(2′-O-β-D-glucopyranosyl)glucopyranoside (16)、phenylethyl-β-D-glucopyranoside (17)、菖蒲碱C (18)、己内酰胺 (19)、蔗糖 (20)。结论 其中化合物5~19为首次从紫金牛科植物中分离得到,化合物4为首次从紫金牛属植物中分离得到,化合物2和3为首次从该植物中分离得到。其中化合物6是自国内学者2013年从岭南杜鹃分离得到以来第二次被分离得到。     

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??OBJECTIVE To study the chemical constituents of Citrus aurantium L. METHODS Chromatographic techniques were employed for isolation and purification of the constituents and their structures were determined by spectral analysis and chemical evidence. RESULTS Sixteen compounds were obtained and identified as pyrrolezanthine-6-methyl ether (1), methyl 3-hydroxy-4-methoxybenzoate (2), 3-hydroxy-4-methoxybenzoic acid (3), methyl 3,4-dihydroxybenzoate (4), methyl 3-(4-acetoxyphenyl)propanoate (5), 4-hydroxybenzoic acid (6), scopoletin (7), 5-(hydroxymethyl)furan-2-carbaldehyde (8), hesperidin (9), naringin (10), gossypetin-8,3'-dimethylether-3-O-??-D-galactoside (11), 2-homoeriodictyol-7-O-??-D-glucopyranoside (12), 6-demethoxytangeretin (13), naringenin (14), 5,6,7,8,4'-pentamethoxyflavone (tangeretin) (15), and 5-O-desmethylnobiletin (16). CONCLUSION Compounds 1??2??4??8??11-13 are for the first time obtained from Citrus.     

The relaxant activity of the methanolic extract of Acanthus montanus on intestinal smooth muscles

The effects of the methanolic extract of Acanthus montanus on different smooth muscle preparations have been investigated. The extract (6.25-100 microg/ml) produced a concentration-dependent relaxation and inhibition of the spontaneous contraction of the rabbit jejunum which was reversed by CaCl2 (0.1-1mM). This effect of the extract was not blocked by propranolol (3 x 10(-7) M) but partially antagonised by phentolamine (10(-6)-3 x 10(-6) M), procaine (10(-3) M) and methylene blue (10(-5) M). The extract also caused a concentration-dependent relaxation of the KCl-precontracted taenia coli of the guinea-pig which was partially blocked by propranolol (3 x 10(-5) M) that completely blocked isoprenaline (10(-8)-3 x 10(-4) M) relaxation of the tissue. Methylene blue (10(-5) M) and procaine (10(-3) M) completely blocked the direct relaxant effects of the extract and isoprenaline on the guinea-pig taenia coli. The extract (0.1-1mg/ml) shifted the concentration-response curves of CaCl2 to the right in a concentration-dependent manner on the guinea-pig taenia coli. These effects of the extract suggest a non specific smooth muscle relaxant activity.     

Lucidenic acids P and Q, methyl lucidenate P, and other triterpenoids from the fungus Ganoderma lucidum and their inhibitory effects on Epstein-Barr virus activation

A new triterpene acid, lucidenic acid P (1a), and two new triterpene acid methyl esters, methyl lucidenates P (1b) and Q (2b), were isolated and characterized from the fruiting body of the fungus Ganoderma lucidum. Their structures were elucidated on the basis of spectroscopic methods. In addition, eight known triterpene acids, lucidenic acids A (3a), C (4a), D(2) (5a), E(2) (6a), and F (7a) and ganoderic acids E (9a), F (10a), and T-Q (11a), and six known triterpene acid methyl esters, methyl lucidenates A (3b), D(2) (5b), E(2) (6b), F (7b), and L (8b) and methyl ganoderate F (10b), were isolated and identified from the fungus. All of the triterpenoids, with the exception of 7a, were evaluated with respect to their inhibitory effects on the induction of Epstein-Barr virus early antigen (EBV-EA) by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells, which is known to be a primary screening test for antitumor promoters. All of the compounds tested showed potent inhibitory effects on EBV-EA induction (96-100% inhibition at 1 x 10(3) mol ratio/TPA).     

New naphthopyranone glycosides from Paepalanthus vellozioides and Paepalanthus latipes.

Three new compounds-3, 4-dihydro-10-hydroxy-7-methoxy-3-(R)-methyl-1H-3,4-dihydronaphtho- ]2, 3c]-pyran-1-one-9-O-beta-D-glucopyranoside (1), 3, 4-dihydro-10-hydroxy-7-methoxy-3-(R)-methyl-1H-3,4-dihydronaphtho- [2, 3c]-pyran-1-one-9-O-beta-D-glucopyranosyl-(1-->6)-glucopyranoside (2), and 3,4-dihydro-10-dihydroxy-7-methoxy-3-(R)-methyl-1H-3, 4-dihydronaphtho-[2,3c]-pyran-1-one-9-O-beta-D-allopyranosyl (1-->6)glucopyranoside (3)-were isolated from the leaves of Paepalanthus vellozioides and Paepalanthus latipes and characterized by spectrometric methods, mainly electrospray mass spectrometry and 1D and 2D NMR experiments. These unusual glycosylated dihydronaphthopyranones may serve as taxonomic markers of the genus Paepalanthus, since these compounds were not detected in other genera belonging to the Eriocaulaceae family.