三叶青石油醚萃取部位的化学成分研究

目的研究三叶青石油醚萃取部位的化学成分。方法运用硅胶柱色谱、凝胶柱色谱和制备HPLC等色谱分离方法对三叶青石油醚萃取部位化学成分进行分离纯化,用质谱法和核磁共振波谱法等波谱学方法鉴定化合物的结构。结果从三叶青石油醚萃取部位分离得到5个化合物,分别鉴定为:9-羟基-10,12-十八碳二烯酸(1),(4R,5R)-4-羟基-5-异丙基-2-甲基环己-2-烯酮(2),(4S,5R)-4-羟基-5-异丙基-2-甲基环己-2-烯酮(3),(3R,4R,6S)-3,6-二羟基-1-薄荷烯(4),肉桂酸(5)。结论化合物1~5均为首次从崖爬藤属植物中分离得到。     

两面针中苯丙素类成分研究

目的：对两面针根的化学成分进行研究。方法：采用硅胶柱色谱及重结晶等方法进行成分分离及精制，并利用^1HNMR、^13C—NMR、MS等光谱技术和理化性质鉴定其化学结构。结果：从两面针根乙醇提取液的石油醚萃取物中分离得到4个苯丙索类化合物，分别鉴定为l-芝麻脂素（1-sesamin，化合物1）、d-表芝麻脂素（d—episesamin，化合物2）、horsfieldin（化合物3）、5，6，7-三甲氧基香豆素（5，6，7-trimethoxycoumarin，化合物4）。结论：化合物2、3和4为首次从两面针中分离得到。     

葱子化学成分的研究

目的：研究百合科葱属植物葱Allium fistulosum L．的干燥成熟种子的化学成分。方法：采用大孔树脂柱色谱、硅胶柱色谱、凝胶柱色谱和反相硅胶柱色谱进行分离纯化,通过理化常数和^1H—NMR、^13C-NMR、ESI—MS等波谱技术进行化合物的结构鉴定。结果：从葱子水提取物的50％乙醇大孔树脂洗脱部位中分离得到了7个化合物,分别鉴定为腺苷（Ⅰ）,2,3,4,5,6．五羟基己酸（Ⅱ）,1,4-二羟基-2-甲氧基苯（Ⅲ）,S-顺式-烯丙基-L-半胱氨酸（Ⅳ）,S-反式-烯丙基-L-半胱氨酸（Ⅴ）,反-异扁柏脂素（Ⅵ）,β-谷甾醇（Ⅶ）。结论：以上化合物均为首次从葱子中分离得到,其中化合物Ⅵ为首次从葱属植物中分离得到。     

紫藤瘤化学成分研究

目的研究紫藤瘤(Wisteria sinensis Sweet Caulis)化学成分。方法紫藤瘤(15 kg)95%乙醇渗漉液的石油醚萃取部位,经过硅胶、Sephadex LH-20等多种材料进行分离纯化,通过波谱技术进行结构鉴定。结果从95%乙醇提取物的石油醚萃取部位中分离鉴定了6个化合物,分别为蒲公英赛醇(1),蒲公英赛酮(2),木栓酮(3),表木栓醇(4),β-谷甾醇(5),β-胡萝卜苷(6)。结论化合物1～6均为首次从该种中分得。     

基于斑马鱼模型三棱抗血栓活性部位筛选及其化学成分研究

目的：筛选中药三棱抗血栓活性部位并对其化学成分进行研究。方法：采用斑马鱼血栓模型对中药三棱80%乙醇提取物的石油醚部位、乙酸乙酯部位、正丁醇部位和水部位的抗血栓作用进行测试。以硅胶柱色谱等方法对抗血栓作用显著的部位进行分离纯化，通过NMR，MS等方法并结合文献数据鉴定化合物结构。结果：乙酸乙酯萃取物能显著增加斑马鱼血栓模型的心脏染色强度（P<0.01），其余各部位抗血栓作用不明显。在该部位分离得到11个化合物，分别鉴定为对羟基苯甲酸（1）、5-羟甲基糠醛（2）、对甲氧基苯甲醛（3）、对羟基苯甲醛（4）、对香豆酸（5）、阿魏酸（6）、香草酸（7）、原儿茶酸（8）、香兰素（9）、Methyl-3，6-dihydroxy-2-[2-（2-hydroxyphenyl）-ethynyl]benzoate （10）及1，3-O-二阿魏酰基甘油（11）。结论：三棱提取物的乙酸乙酯萃取部位具有显著的抗血栓作用，其主要化学成分为酚酸类化合物。     

紫藤瘤化学成分研究

目的 研究紫藤瘤(Wisteria sinensis Sweet Caulis)化学成分.方法 紫藤瘤(15 kg)95%乙醇渗漉液的石油醚萃取部位,经过硅胶、Sephadex LH-20等多种材料进行分离纯化,通过波谱技术进行结构鉴定.结果 从95%乙醇提取物的石油醚萃取部位中分离鉴定了6个化合物,分别为蒲公英赛醇(1),蒲公英赛酮(2),木栓酮(3),表木栓醇(4),β-谷甾醇(5),β-胡萝卜苷(6).结论 化合物1～6均为首次从该种中分得.     

鸡冠花子的化学成分研究

目的:分离鉴定鸡冠花子的化学成分。方法:采用硅胶柱色谱、Sephadex-20柱色谱、重结晶及制备高效液相色谱等技术提取分离鸡冠花子的化学成分,用UV、IR、EI-MS、ES-MS、1H-NMR、13 C-NMR、HMQC及HMBC等光谱方法鉴定化合物结构。结果:从鸡冠花子乙醇提取物的石油醚部位分离得到3个化合物,分别鉴定为棕榈酸(1)、对羟基苯甲醛(2)、齐墩果酸(3);从二氯甲烷部位分离得到6个化合物,分别鉴定为stigmast-5-en-3-ol,oleate(4)、4-羟基-3-甲氧基苯甲酸(5)、胡萝卜苷(6)、芹菜素(7)、木樨草素(8)、鸡冠花苷(9)。结论:化合物4～6首次从鸡冠花子中分离得到,化合物9是新化合物。     

锦灯笼中酸浆苦素类化学成分的研究

目的 研究锦灯笼95％乙醇提取物的石油醚、氯仿、醋酸乙酯萃取部位中化学成分.方法 利用硅胶柱色谱、反相ODS柱色谱、制备液相色谱等方法进行分离、纯化,根据化合物的理化性质和光谱数据鉴定其结构.结果 分离得到了7个化合物,经结构鉴定分别为酸浆苦素A(1)、酸浆苦素D(2)、酸浆苦素L(3)、酸浆苦素O(4)、木犀草素(5...     

山莓化学成分研究

目的对山莓的化学成分进行研究。方法采用硅胶柱色谱、Sephadex-20柱色谱、重结晶,并经高效液相色谱等技术提取分离山莓的化学成分,用UV、IR、EI-MS、ES-MS及NMR等光谱方法鉴定化合物结构。结果从山莓乙醇提取物的石油醚部位分离得到化合物1～6,分别鉴定为豆甾醇(1)、β-谷甾醇(2)、胡萝卜苷(3)、Homofukinolide(4)、Bakkenolide-B(5)、Bakkenolide-D(6);从二氯甲烷部位分离得到化合物7～10,分别鉴定为4-羟基-3-甲氧基苯甲酸(7)、芹菜素(8)、木樨草素(9)、山莓素(10)。结论化合物4、5、6、7、8、9首次从山莓子中分离得到,化合物10是新化合物。     

马蹄莲中水溶性化合物的分离与鉴定

目的研究马蹄莲中水溶性化合物。方法将乙醇提取物依次用石油醚、苯、氯仿、正丁醇、乙酸乙酯萃取后的水溶液,经硅胶色谱分离,分离得到的化合物,经UV、IR、^1H—NMR、^13C-NMR及C-C-MS渡谱分析,对其进行结构鉴定。结果从马蹄莲中分离得到3种水溶性化合物：三胺嗪、5-羟甲基糠醛及脱水内醚糖。结论3种水溶性化合物均系首次从马蹄莲中分离得到。     

New sesquiterpenoids from Ainsliaea macrocephala and their nitric oxide inhibitory activity

Investigation of the ethanol extract of the whole plant of Ainsliaea macrocephala led to the isolation of five new sesquiterpenoids, namely ainsliadimer C (1), ainsliadimer D (2), ainsliaolide B (3), ainsliatone B (4), and ainsliaolide C (5), together with seventeen known sesquiterpenes and sesquiterpene glycosides (6- 22). Their structures were elucidated by spectroscopic methods. The relative stereochemistry of ainsliadimers C (1) and D (2) were further confirmed by single crystal X-ray diffraction analysis. Total extract of A. macrocephala and compounds 1- 22 were tested for inhibitory activity against the production of nitric oxide in RAW 264.7 cells stimulated by LPS, as well as for cytotoxicity against RAW 264.7 macrophages. Of all samples tested, purified compounds 4, 7, and 12 strongly inhibited the production of nitric oxide with IC50 values of 8.78, 2.50, and 7.11?μM, and simultaneously showed low cytotoxicity against RAW 264.7 macrophages.     

杏香兔耳风化学成分的分离与鉴定

目的研究杏香兔耳风(Ainsliaea fragransChamp.)的化学成分,为活性测试及制定质量标准提供依据。方法利用多种色谱方法进行分离纯化,并根据理化性质和波谱数据确定化合物结构。结果分离并鉴定了9个化合物,其中1个倍半萜:(-)-clovane-2β,9α-diol(1);2个三萜:降香萜醇乙酸酯(bauerenyl acetate,2)、熊果酸(ursolic acid,3);1个寡肽:橙黄胡椒酰胺乙酸酯(aurantiamideacetate,4);5个有机酸类化合物:丁香酸(syringic acid,5)、香草酸(vanillic acid,6)、琥珀酸(succin-ic acid,7)、辛二酸(octanedioic acid,8)、二十六酸(hexacosanic acid,9)。结论上述化合物均为首次从兔儿风属植物中分离得到。     

牛蒡根乙酸乙酯部位的化学成分研究

摘 要 目的：研究牛蒡根乙酸乙酯部位的化学成分。方法: 采用柱色谱和制备液相等方法对牛蒡根乙酸乙酯部位化学成分进行分离纯化,运用波谱学方法鉴定化合物结构。结果: 从牛蒡根乙酸乙酯部位共分离得到了7个化合物,分别鉴定为: 邻苯二甲酸二丁酯（1）、咖啡酸甲酯（2）、8- 甲氧羰甲基-对羟基肉桂酸（3）、3-O-咖啡酰奎宁酸甲酯（4）、咖啡酸（5）、3,4-O-双咖啡酰奎宁酸甲酯（6-a）和3,5-O-双咖啡酰奎宁酸甲酯（6-b）、乙二醇（7）。结论:确定其中8- 甲氧羰甲基-对羟基肉桂酸（3）为首次从菊科植物中分离获得;3-O-咖啡酰奎宁酸甲酯（4）、3,4-O-双咖啡酰奎宁酸甲酯（6-a）和3,5-O-双咖啡酰奎宁酸甲酯（6-b）为首次从牛蒡属植物中分离得到。     

Two novel sesquiterpenoids from Ainsliaea fragrans Champ.

A new sesquiterpene lactone, 3β-O-β-d-glucopyranosyl-8α-hydroxy-11α,13-dihydrozaluzanin C (1), and a novel trinorguaiane-type sesquiterpene, 4β,10α-dimethyl-1β,5α-bicycle[3,5,0]dec-6-en-4α,10β-diol (2), together with three known compounds, glucozaluzanin C (3), 11α,13-dihydrozaluzanin C (4), and 8α-hydroxy-11α,13-dihydrozaluzanin C (5), were isolated from the whole plant of Ainsliaea fragrans Champ. The structures of 1 and 2 were elucidated on the basis of detailed spectral analysis. Structures of the known compounds were identified by comparison of its spectral data with those values in the literature.     

冬凌草的化学成分研究

目的 研究冬凌草的化学成分。方法 利用硅胶柱色谱、中压液相色谱、高效液相色谱等色谱技术对冬凌草甲醇提取物进行分离纯化,通过波谱数据分析,鉴定了化合物的结构,利用噻唑蓝(MTT)法测试化合物抗肿瘤活性。结果 从冬凌草中共分离鉴定6个化合物,分别为：rabdosianin A（1）、parvifoline G（2）、rabdoternin C（3）、betulin（4）、betulinic acid（5）、古柯二醇（6）。结论 化合物6为首次从香茶菜属中分离得到,化合物1、2、4、5为首次从冬凌草中分离得到。化合物5对人白血病细胞K562有较强的抑制作用,IC₅₀值为1.45 µmol·L^-1。     

Investigating glucosyltransferase inhibitory activities of polyphenols from kapur (<Emphasis Type="Italic">Dryobalanops</Emphasis> sp.) heartwood extracts

The inhibitory effects of 50% aqueous ethanol extracts obtained from 36 tropical woody plants species on glucosyltransferase (GTase) activity were studied. Out of the 36 species examined, those obtained from kapur (Dryobalanops sp.), a species growing in Kalimantan (Indonesia), showed the highest level of GTase inhibition. Kapur extracts were further subjected to fractionation using column chromatography (LH-20 gel, cellulose and C-18 silica gel column). LH-20 gel provided the most successful method of fractionation. The separated fractions showed positive with Folin-Ciocalteau’s reagent and negative with vanillin-HCl reagent, indicating that the main constituents of the active fractions were polyphenols but not proanthocyanidin (condensed tannins). Results of the assay for protein precipitating ability with bovine serum albumin (BSA) solution suggested these polyphenols have strong protein-precipitating ability. The predominant compound produced after acid hydrolysis was ellagic acid, indicating that the GTase-inhibitory components were mainly ellagitannins. Two polyphenolic compounds referred to as compounds 1 and 2 were isolated from the water eluate fraction with LH-20 gel column, and these compounds showed comparatively strong GTase-inhibitory activities and relatively low molecular weight. Using a combination of two-dimensional, ¹H and ¹³C nuclear magnetic resonance analysis, compound 1 was identified as 4-methoxy-2-[tetrahydro-3,4,5-trihydroxy-6-(hydroxymethyl)pyran-2-yl]-α-resorcylic acid δ–lactone (bergenin), and 2 was identified as 4-O-(α-rhamnopyranosyl) ellagic acid (eschweilenol C). Bergenin has been previously isolated from the roots of Bergenia crassifolia, and eschweilenol C has been isolated from the bark of Eschweilera coriacea. Both compounds were found in kapur for the first time.     

Synthesis of new 1,2,4-triazoles as anti-inflammatory and anti-nociceptive agents

A series of fifteen new substituted 1,2,4-triazoles (6a – 6o) have been synthesized in order to obtain new agents with potential anti-inflammatory and anti-nociceptive activity. The title compounds were synthesized using 4-methylbenzoic acid as a starting reactant. The synthesized compounds were characterized by spectroscopic methods (IR, ¹H NMR, ¹³ C NMR, FAB⁺ − MS) and elemental analysis (nitrogen analysis). The title compounds were evaluated for anti-inflammatory activity by the carrageenan induced paw edema method, and some compounds were evaluated for anti-nociceptive activity by the hot plate method and tail immersion method. Compounds N-[3-mercapto-5-(4-methylphenyl)-4H-1,2,4-triazol-4-yl]-2-piperidin-1-ylacetamide (6f), 2-(4-benzylpiperazin-1-yl)-N-[3-mercapto-5-(4-methylphenyl)-4H-1,2,4-triazol-4-yl]acetamide (6i) and N-[3-mercapto-5-(4-methylphenyl)-4H-1,2,4-triazol-4-yl]-2-morpholin-4-ylacetamide (6 k) showed significant anti-inflammatory activity compared to other synthesized compounds, and N-[3-mercapto-5-(4-methylphenyl)-4H-1,2,4-triazol-4-yl]-2-morpholin-4-ylacetamide (6 k) exhibited superior anti-nociceptive activity.     

Asterosaponins and glycosylated polyhydroxysteroids from the starfish Culcita novaeguineae and their cytotoxic activities

Using combined chromatographic methods, two asterosaponins (compounds 1 and 2), including a new compound novaeguinoside E (compound 1), and six glycosylated polyhydroxysteroids (compounds 3–8) were isolated from a methanol extract of the starfish Culcita novaeguineae. Their structures were determined on the basis of spectroscopic data (¹H and ¹³C NMR, HSQC, HMBC, ¹H–¹H COSY, ROESY, and HRESI-MS) and by comparison with the literature values. The new compound 1 represents the third example of asterosaponins containing the 5α-cholesta-9(1l)-en-3β,6α,20,22-tetraol aglycone. Among isolated compounds, 4–7 exhibited moderate to weak cytotoxic activities against five human cancer cell lines such as Hep-G2 (hepatoma), KB (epidermoid carcinoma), LNCaP (prostate cancer), MCF7 (breast cancer), and SK-Mel2 (melanoma).     

Ozocardic A: a new alkylanacardic acid from Ozoroa pulcherrima

One new alkylanacardic acid, ozocardic A (1), along with the known and related metabolites 6-tridecyl anacardic acid (2) and β-sitosterol (3) was isolated from Ozoroa pulcherrima. The structure of the new compound was elucidated by detailed spectroscopic analysis such as ¹H, ¹³C NMR, COSY, HMQC, HMBC, and HREIMS. The structures of known compounds (6-tridecyl anacardic acid (2) and β-sitosterol (3)) were identified by the comparison of their spectral data with those published in the literature.     

Bioassay-guided isolation,identification of compounds from Origanum rotundifolium and investigation of their antiproliferative and antioxidant activities

Context: Origanum (Lamiaceae) has been used in food and pharmaceutical industries.

Objective: Isolation and identification of bioactive compounds from Origanum rotundifolium Boiss. and investigation of their antiproliferative and antioxidant activities.

Materials and methods: The aerial part of O. rotundifolium was dried and powdered (1.0?kg ±2.0?g) then extracted with hexane, ethyl acetate, methanol and water. Solvent (3?×?1?L) was used for each extraction for a week at room temperature. The aqueous extract was partitioned with ethyl acetate (3?×?1?L) to yield the water/EtOAc extract subjected to chromatography to isolate the active compounds. The structures of isolated compounds were elucidated by 1?D, 2?D NMR and LC-TOF/MS.

Results: Apigenin (1), ferulic acid (2), vitexin (3), caprolactam (4), rosmarinic acid (5), and globoidnan A (6) were isolated and identified. Globoidnan A (6), vitexin (3), and rosmarinic acid (5) revealed the excellent DPPH^? scavenging effect with IC₅₀ values of 22.4, 31.4, 47.2?μM, respectively. Vitexin (3) (IC₅₀ 3.6), globoidnan A (6) (IC₅₀ 4.6), apigenin (1) (IC₅₀ 8.9) and ferulic acid (2) exhibited more ABTS^?+ activity than standard Trolox (IC₅₀ 13.8?μg/mL). Vitexin (3) revealed the most antiproliferative activity against HeLa, HT29, C6 and Vero cells lines with IC₅₀ values of 35.6, 32.5, 41.6, 46.7 (μM), respectively.

Discussion and conclusion: Globoidnan A (6) has the most antioxidant effects on all assays. This has to do with the chemical structure of the compound bearing the acidic protons. Vitexin (3) could be a promising anticancer agent.