狭苞橐吾中几种倍半萜类化合物的活性筛选

本文对山西狭苞橐吾中倍半萜类化合物的生物学活性进行了筛选。用不同浓度的4种艾里莫芬烷型倍半萜干预携带有P53和SV40肿瘤病毒大T抗原基因的AH109菌液,采用酵母双杂交系统的β-半乳糖苷酶活力测定方法,分析了4种倍半萜对P53蛋白与SV40大T抗原之间相互作用力的影响。发现8β-methoxyeremophil-7(11)-ene-12,8α(4β,6α)-diolide(1)和8β-hydroxyl-6β-angloxyeremophil-7(11)-ene-12,8α-olide-15-oic acid(2)对P53蛋白及SV40-大T抗原相互作用没有显著影响,但是中、高浓度的furanoeremophilan-4β,6α-olide(3)和低、中、高浓度的8β-hydroxyeremophil-7(11)-ene-12,8α(4β,6α)-diolide(4)对P53蛋白与SV40大T抗原之间相互作用有抑制效应。说明从山西狭苞橐吾中提取出的化合物3和4对酵母双杂交系统中的P53和SV40-大T抗原的相互作用有生物学抑制活性。     

蒙药土木香的化学成分研究CSCD

研究蒙药土木香的化学成分,采用RP-HPLC、硝酸银硅胶色谱等方法分离纯化,应用NMR、MS等波谱技术鉴定化合物结构,共分离鉴定了22个单体化合物,分别为5α,6α-dihydroxy-eudesma-11(13)-dien-12,8β-olide(1)、4α-hydroxy-5-methoxy-5,8α-dimethyl-3-methylenedecahydronaphtho[2,3-b]furan-2-one(2)、木香烯内酯(3)、土木香内酯(4)、异土木香内酯(5)、11,13-二氢土木香内酯(6)、alloalantolactone(7)、4α,5β-环氧-1(10),11(13)-吉玛烷-12,8α-交酯(8)、septuplinolide(9)、8-epi-ivangustin(10)、santamarine(11)、racemosalactone A(12)、3-oxo-eudesma-4(11)-dien-12,8β-olide(13)、telekin(14)、igalane(15)、macrophyllilactone E(16)、4α,15-环氧异土木香内酯(17)、11,13-dihydroxy-alantolactone(18)、1(2),4(15),11(3)-eudesma-trien-12,8β-olide(19)、亚麻酸(20)、亚油酸(21)、油酸(22)。化合物1是新倍半萜内酯类化合物,化合物2、3、9~14、17、19~22为首次从该属植物中分离得到,化合物4~8、15、16、18为土木香药材中已报道的化合物。     

肋果茶中的萜类化学成分研究

从肋果茶(Sladenia celastrifolia)95％乙醇提取物的乙酸乙酯部位中分离得到15个萜类化合物,经波谱学方法分别鉴定为sladeniafolin A(1),grasshopper ketone (2),(3S,5R,6S,7E,9R) -7-megastigmene-3,6,9-triol (3),hedytriol (4),(3S,5R,6R,7E,9R) -3,5,6,9-tetrahydroxy-7-megastigmene(5),1′S*,4′R*-8-(4′-hydroxy-2′,6′,6′-trimethylcyclohex-2-enyl)-6-methyloct-3E,5E,7E-trien -2-one (6),2α,3α,19α,23-tetrahydroxyurs-12-en-28-oic acid (7),2α,3β,19α,23-tetrahydroxyurs-12-en-28-oic acid(8),pomolic acid(9),3-O-acetyl pomolic acid(10),ursaldehyde (11),camarolide (12),3β-hydroxyurs-11-en-13β(28) -olide (13),3β-hydroxy -11α,12α-epoxy-urs-13β,28-olide (14)和28-0-β-D-glucopyranosyl euscaphic acid (15).以上化合物均首次从该植物中分离得到,其中1为新的C9裂环烯醚萜.     

棉毛橐吾根茎中化学成分研究

采用硅胶、Sephadex LH-20凝胶、Toyopearl HW-40凝胶及Diaion HP-20树脂等色谱方法从云南丽江棉毛橐吾中分离得到化合物18个,通过理化手段及波谱技术分别鉴定为:呋喃艾里莫芬-14β,6α-内酯(1)、β-谷甾醇(2)、惕格酸(3)、棕榈酸(4)、十九烷酸甲酯(5)、艾里莫芬-7(11)-烯-12,8α(14β,6α)-二内酯(6)、8β-甲氧基艾里莫芬-7(11)-烯-12,8α(14β,6α)-二内酯(7)、1-O-十六烷酰基甘油酯(8)、8β-羟基艾里莫芬-7(11)-烯-12,8α(14β,6α)-二内酯(9)、对羟基桂皮酸甲酯(10)、对羟基苯乙酮(11)、伞形花内酯(12)、3,4-二羟基苯乙酮(13)、胡萝卜苷(14)、1,5-二咖啡酰奎宁酸(15)、对羟基桂皮酸(16)、咖啡酸(17)及七叶内酯(18),其中化合物4~5,8,10,13,15及17,18为首次从该植物中分离得到。     

海南红树植物角果木的二萜类化学成分研究

研究海南红树植物角果木的二萜类化学成分。通过硅胶、Sephadex LH-20柱色谱以及高效液相色谱等分离纯化手段,从角果木醇提物中共分离得到10个二萜类化合物,运用现代波谱技术鉴定了它们的结构,分别为:(5S*,8S*,9S*,10R*,13S*)-2,16-dihydroxydolabr-4R*,18-epoxy-3,15-dione(1)、tagalsin B(2)、ent-5α,2-oxodolabr-3-ene-3,15,16-triol(3)、(5S*,8S*,9S*,10R*)-3,13S*-dihydroxy-15,16-dinorlabr-3-en-2-one(4)、(5S*,8S*,9S*,10R*,13S*)-3-hydroxy-16-nor-2-oxodolar-3-ene-15-oic acid(5)、(5S*,8S*,9S*,10R*)-13S*,18-dihydroxy-15,16-dinordolabr-4(18)-ene-3-one(6)、(5S*,8S*,9S*,10R*,13S*)-18-hydroxy-16-nor-3-oxodolabr-4(18)-en-15-oic acid(7)、(5S*,8S*,9S*,10R*)-13S*-hydroxy-4S*,18-epoxy-15,16-dinordolabr-1-en-3-one(8)、ent-8(14)-pimarane-16,18-dihydroxy-15-one(9)、ent-8(14)-pimarane-15,18-diol(10)。其中化合物1为新化合物,化合物3和5为首次从角果木中分离得到。     

麻疯树种子二萜类化学成分的研究

为深入了解麻疯树种子的化学成分,有必要对其具有生物活性的二萜类成分进行研究。该研究利用正相硅胶、ODS、制备液相等色谱分离方法,从麻疯树种子的乙醇提取物中共分离得到了6个二萜类化合物,并采用荧光偏振技术对化合物进行蛋白激酶C (PKC)抑制活性的测定。结果表明:根据化合物的理化性质、MS和NMR,并参考相关文献,这6个二萜类化合物分别鉴定为3β-acetoxy-12-methoxy-13-methylpodocarpa-8,11,13-trien-7-one (1)、4-epi-dehydroabietic acid (2)、3β-hydroxy-19-O-acetyl-pimara-8 (9),15-dien-7-one (3)、Jatrophodione A (4)、14-O-acetyl-5,6-epoxy-(14E)-jatrogrossidentadion (5)、2-Hydroxy jatrophone (6)。其中,化合物2、3、6均为首次从该植物中分离得到,且化合物2对PKCβ具有一定的抑制作用。     

草珊瑚化学成分的研究

采用硅胶、SephadexLH-20、MCI等方法从草珊瑚(Sarcandra glabra)全草乙酸乙酯萃取部位分离得到10个化合物,经波谱学方法鉴定为Chlorajapolide C(1),Shizukanolide H(2),Chloranthalactone E(3),Istanbulin B(4),Istanbulin A(5),4-Hydroxy-4,7-dimethyl-1-tetralone(6),4α,7α-Epoxyguaiane-10α,11-diol(7),(+)-Hydroxydihydroneocurueol(8),3β-Hydroxystigmast-5-en-7-one(9),3β-Hydroxystigmast-5,22-dien-7-one(10)。其中6~10这5个化合物均为首次从该科植物中得到,1、2为首次从该植物中得到。     

南海疏枝刺柳珊瑚中甾醇类化合物的研究

本文对采自海南三亚海域的疏枝刺柳珊瑚(Echinogorgia pseudossapo)化学成分进行研究,分离到11个甾醇类化合物。经波谱数据分析,分别鉴定为cholest-5-en-3β-ol(1),24-methylene-cholest-4-ene-3β,6β-diol(2),24-norcholesta-22-en-3β-ol(3),acanthovagasteroid A(4),calicoferol E(5),calicoferol F(6),6-hydroxy-cholest-4-ene-3-one(7),echinoflorasterol(8),echissaposterol(9),24-methylcholest-5-en-3β,7α-diol(10)和24-methylcholest-5,22(E)-dien-3β,7α-diol(11)。除化合物8外,其余化合物均首次从该种海洋动物中分离得到。     

柯拉斯那沉香的化学成分研究

对柬埔寨野生柯拉斯那(Aquilaria crassna)沉香的化学成分和生物活性进行研究。实验采用多种柱色谱法对该沉香进行分离纯化;通过现代波普技术结合化合物理化性质对所得单体化合物进行结构鉴定,从柬埔寨野生柯拉斯那沉香共分离出12个化合物,分别鉴定为7α-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(1)、7β-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(2)、neopetasane (eremophila-9,11-dien-8-one)(3)、jinkoh-eremol(4)、(rel)-4β,5β,7β-eremophil-9-en-12,8β-olide(5)、诺卡酮(6)、11-hydroxy-valenc-1(10)-en-2-one(7)、(7S, 9S, 10S)-(+)-9-hydroxy-selina-4,11-dien-14-al(8)、5-羟基-2-[2-(4-甲氧基苯)乙烯基]色酮(9)、5-羟基-6甲氧基-2-(2-苯乙基)色酮(10)、6-甲氧基-2-(2-苯乙基)色酮(11)、5-羟基-6甲氧基-2-[2-(4-甲氧基苯)乙基]色酮(12)。其中化合物1～8为倍半萜类化合物,化合物9为2-(2-苯乙烯基)色酮类化合物,化合物10～12为2-(2-苯乙基)色酮类化合物。且化合物2～11均是首次从柯拉斯那沉香分离。采用Ellman比色法对单体化合物进行乙酰胆碱酯酶抑制活性的测定,活性测定结果表明化合物1～3和12具有乙酰胆碱酯酶抑制活性。     

云南割舌树的化学成分

从云南割舌树（Walsura yunnanensis C.Y.Wu.)树皮的乙醇提取物中分离鉴定了12个化合物,它们分别是walsurol(1),tocopherol(2),sitoindoside Ⅰ（3）,3β-stigmast-5-en-3-yl-β-D-xylopyranoside(4),stigmast-4-en-6β-ol-3-one(5),7-oxositosterol(6),3β-hydroxy-5α,8α-epidioxyergosta-6,22-diene(7),(-)epicatechin(8),3,5-dihydroxy-4-methoxylphenylethanol(9),间三甲氧基苯,（β－谷甾醇和胡萝卜甙,新化合物1命名为割舌醇（walsurol)。     

Two new sesquiterpenes from Ligularia dictyoneura

The detailed investigation of the whole plant of Ligularia dictyoneura was performed during a search for unique chemical skeletons. One novel noreremophilane-type sesquiterpene, (4S, 5R, 8R, 10S)-1-nor-10-hydroxy-8-methoxyeremophil-7(11)-en-12,8-olide (1) and one new highly oxygenated eremophilane, 1β-angeloyloxy-6α, 10β-dihydroxyeremophil-7(11), 8-dien-12, 8-olide (2), were obtained. Their structures, including the absolute configuration, were elucidated by spectroscopic data and CD analysis.     

中华小苦荬萜类化学成分的研究(英文)

从中华小苦荬全草的乙酸乙酯提取物中分离得到8个萜类化合物,通过波谱方法及文献对照分别鉴定为β-香树脂素(1),3β-羟基-20(30)-蒲公英甾烯(2),熊果-12-烯-3β-醇(3),羽扇豆醇(4),10-羟基艾里莫芬-7(11)-烯-12,8α-内酯(5),乌苏-12,20(30)-二烯-3β,28-二醇(6),3β,8α-二羟基-6β-当归酰基艾里莫芬-7(11)-烯-12,8β-内酯(7)和乌苏酸(8),化合物1～8均首次从该植物中分离得到。     

Eremophilenolides from petasites japonicus

Chemical investigation of the young flower stalks of Petasites japonicus afforded some eremophilenolides, including a mixture of the two new compounds 6β-angeloyloxy-3β,8α-dihydroxyeremophil-7(11)-en-12,8β- olide and 6β-angeloyloxy-3β,8β-dihydroxyeremophil-7(11)-en-12,8α- olide. Their structures were elucidated by chemical and spectroscopic methods. The ¹³C NMR signals for the carbon atoms of the eremophilenolides were assigned with the help of Beierbeck's parameters. The CD spectra of the compounds are briefly discussed.     

Sesquiterpenoids from Curcuma wenyujin with anti-influenza viral activities

Five sesquiterpenoids, 1α,8α-epidioxy-4α-hydroxy- 5αH-guai-7(11),9-dien- 12,8-olide. (1), 8,9-seco-4β-hydroxy-1α,5βH-7(11)-guaen-8,10-olide (2), 8α-hydroxy-1α, 4β,7βH-guai-10(15)-en- 5β,8β-endoxide(3), 7β,8α-dihydroxy-1α,4αH-guai-10(15)-en-5β,8β-endoxide(4) and 7-hydroxy-5(10),6,8-cadinatriene-4-one(5), together with seven known analogs were isolated from the rhizomes of Curcuma wenyujin. Their structures and relative configurations were determined on the basis of spectroscopic methods including 2D NMR techniques, and the structures of 1 and 2 were confirmed by single-crystal X-ray diffraction experiment. Compounds 1–10 and 12 showed significant in vitro antiviral activity against the influenza virus A with IC₅₀ values ranged from 6.80 to 39.97 μM, and SI values ranged from 6.35 to 37.25.     

Terpenoids from Tripterygium doianum (Celastraceae)

The extract of Tripterygium doianum (Celastraceae) afforded three triterpenoids [3beta-acetoxy-11-ursen-13alpha,30-olide, 25-chloro-24-hydroxytirucall-7-en-3-one and tirucall-7-en-3,24-dione], two sesquiterpenoids [5alpha-acetoxy-1beta,8alpha-bis-cinnamoyl-4alpha-hydroxydihydroagarofuran and 5alpha-acetoxy-1beta-benzoyl-8alpha-cinnamoyl-4alpha-hydroxydihydroagarofuran] and nine known triterpenoids. Their structures were established based on spectroscopic studies.     

Chemotaxonomic significance of lindenane sesquiterpenoid dimers and eudesmane sesquiterpenoids from Chloranthus henryi Hemsl. var. hupehensis (Pamp.) K. F. Wu

Seventeen known compounds were isolated from the 95% alcohol extract of the aerial parts of Chloranthus henryi Hemsl. var. hupehensis (Pamp.) K. F. Wu, including five lindenane sesquiterpenoid dimers (1–5) and twelve eudesmane sesquiterpenoids (6–17). In the present research, compounds 3 sarcaglabrin C, 6 neolitacumone C, 7 ent-Atractylenolide III and 8 dehydrocarissone were reported from the Chloranthus genus for the first time, and compounds 1 spicachlorantin B, 2 chloramultilide C, 4 shizukaol B, 5 japonicone C, 9 6α-hydroxyeudesma-4(15),7(11),8(9)-triene-12,8-olide, 10 ent-(3R)-3-hydroxyatractylenolide III, 11 8βH-hydroxyeudesma-4(14),7(11)-dien-12,8-olide, 12 lasianthuslactone A, 13 (5S,6R,8S,10R)-6-hydroxyeudesma-4(15),7(11)-diene-12,8-olide, 14 4β-hydroxy5α,8β(H)-eudesm-7(11)-en-8,12-olide, 15 4β,8β-dihydroxy-5α(H)-eudesm-7(11)-en-8,12-olide, 16 curcolonol and 17 1β, 8β-dihydroxyeudesm - 3,7(11)-dien-8α,12-olide were firstly isolated from the plant. Their structures were elucidated on the basis of extensive spectroscopic and chemical analyses. Moreover, the chemotaxonomic significance of the isolated compounds is discussed.     

广东紫珠中的萜类化合物及其抗炎活性

对岭南药材广东紫珠(Callicarpa kwangtungensis)地上部分进行化学成分研究,得到11个萜类化合物,分别鉴定为sambucunlin A(1)、2α-羟基羽扇豆醇(2)、swinhoeic acid(3)、3β-羟基-乌苏烷-11-烯-13β,28-内酯(4)、蔷薇酸(5)、2α,3β,6β,18β,23-pentahydroxy-olean-12-en-28-oic acid(6)、rel-5-(3S,8S-dihydroxy-1R,5S-dimethyl-7-oxa-6-oxobicyclo-oct-8-yl)-3-methyl-2Z,4E-pentadienoic acid(7)、salvionoside B(8)、齐墩果酸(9)、白桦脂酸(10)和α-香树脂醇(11)。其中,化合物1～4和6～8为首次从该属植物中分离得到。在化学成分分离基础上,进一步选择脂多糖(LPS)诱导的RAW 264.7小鼠巨噬细胞炎症模型进行萜类化合物抗炎活性测试。结果表明:化合物3和9具有显著的抗炎活性,对比结构发现,三萜类化合物(3～6、9和11)抗炎活性优于倍半萜类化合物(7和...     

New eudesmane sesquiterpenes from Alpinia oxyphylla and determination of their inhibitory effects on microglia

The fruits of Alpinia oxyphylla are used as healthcare products for the protection on neurons and prevention of dementia. Two new noreudesmane sesquiterpenoids, (5R,7S,10S)-5-hydroxy-13-noreudesma-3-en-2,11-dione (1) and (10R)-13-noreudesma-4,6-dien-3,11-dione (2), and a new eudesmane sesquiterpenoid, (5S,8R,10R)-2-oxoeudesma-3,7(11)-dien-12,8-olide (3), as well as 12 known sesquiterpenoids, were isolated from the fruits of A. oxyphylla. The structures of the new compounds (1–3) were elucidated on the basis of spectroscopic data and circular dichroism experiments. All isolates were evaluated their neuroprotective potential by inhibitory assay on nitric oxide (NO) and tumor necrosis factor-α (TNF-α) production in lipopolysaccharide (LPS)-induced mouse microglia BV-2 cells.     

马尾伸筋草化学成分及抗骨质疏松活性研究

为研究马尾伸筋草(Lycopodium fargesii Hert.)的化学成分及其抗骨质疏松活性,采用硅胶、MCI、RP-18、Sephadex LH-20柱色谱及半制备高效液相色谱对马尾伸筋草的乙醇提取物进行系统分离,从乙酸乙酯部位中得到18个化合物,综合利用NMR、HR-ESI-MS等技术,分析鉴定化合物的结构,分别鉴定为α-芒柄蜡素(1)、26-去甲-8-氧化-α-芒柄蜡素(2)、serrat-14-en-3β,21α,24-triol(3)、serrat-14-en-3β,21β,24-triol(4)、1,20-eicosanediol(5)、二十三烷(6)、glycerolmonolinoleate(7)、glyceryl linolentate(8)、3-(4′-formylphenoxy)-4-methoxybenzaldehyde(9)、芹菜素(10)、对羟基苯甲醛(11)、香草酸(12)、3-羟基-4-甲氧基苯甲酸(13)、2-羟基-1-(4-羟基-3-甲氧基-苯基)-丙基-1-酮(14)、3-甲氧基-4-羟基桂皮醛(15)、8-acetoxy-5-hydroxyumbelliprenin(16)、trans-4-hydroxy-2-nonenoic acid(17)和正十烷硫醇(18)。化合物1~18均为首次从马尾伸筋草中分离得到,其中化合物16对破骨细胞活性具有显著的抑制作用,其IC₅₀为1.98μM。