蜘蛛香炮制品的化学成分和抗炎活性研究

目的 研究蜘蛛香炮制品的化学成分及其抗炎活性。方法 采用正相硅胶柱色谱、羟丙基葡聚糖凝胶(Sephadex LH-20)、ODS和高效液相色谱(HPLC)等多种分离材料和方法进行分离纯化,通过理化性质及波谱数据鉴定化合物结构,采用脂多糖(LPS)诱导的RAW264.7细胞体外炎症模型,以总一氧化氮合成酶抑制剂(L-NMMA)作为阳性对照,对化合物进行体外抗炎活性评价。结果 从蜘蛛香炮制品的乙酸乙酯相共分离鉴定了25个化合物,分别为(3S,4R,5S,7S,8S,9S)-3,8-环氧-7-羟基-4,8-二甲基全氢环戊基[c]吡喃(1)、(3S,4S,5S,7S,8S,9S)-3,8-环氧-7-羟基-4,8-二甲基全氢环戊基[c]吡喃(2)、去酰基缬草醛(3)、缬草醛(4)、8-羟基-7′-表松脂醇(5)、(+)-表松脂醇(6)、青刺尖木脂醇(7)、 (7R,8S,7′R,8′S)-5-甲氧基青刺尖木脂醇(8)、(-)-松脂醇(9)、绿原酸(10)、橙皮素(11)、3,8-二羟基-2-甲基色原酮(12)、penicisochroman J(13)、2,5-二(4-羟基-3-甲氧基苯基)-1,4-二烷(14)、4,4′-二羟基-3,3′-二甲氧基-反式-1,2-二苯乙烯(15)、对苯二酚(16)、4-羟基-3-甲氧基苯甲醛(17)、乙酰香草酮(18)、4-羟基-3-甲氧基桂皮醛(19)、2,3-二羟基-1-甲氧基苯(20)、5-羟甲基-2-呋喃甲醛(21)、5-乙酰糠醇(22)、5-[(5-(hydroxymethyl)furan-2-yl)methoxymethoxymethyl]furan-2-carbaldehyde(23)、5-({5-[(5-(hydroxy methyl)furan-2-yl)methoxy(methoxymethyl)]-furan-2-yl} methoxy(methoxymethyl)) furan-2-carbaldehyde(24)和6-羟基-2H-吡喃-3-醛(25)。其中,化合物3,15,16和19均能够显著抑制RAW264.7细胞中脂多糖诱导的一氧化氮生成,且呈显著的剂量依赖性,表现出潜在的抗炎活性。结论 炮制后的蜘蛛香化合物结构类型涉及环烯醚萜及其降解产物、苯丙素、黄酮、色原酮、芳香衍生物和糠醛衍生物等。在炮制过程中,主要是环烯醚萜和单糖的结构发生了变化;化合物 5、6、9~25均为首次从蜘蛛香中分离得到,其中,化合物3,15,16和19具有抗炎活性,半数抑制浓度(IC₅₀)值分别为29.04、10.77、6.37和10.98 μmol·L^-1。     

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。     

泰国大风子化学成分研究北大核心CSCD

研究泰国大风子Hydnocarpus anthelminthica干燥成熟种仁中的化学成分。通过正相硅胶、Sephadex LH-20以及反相HPLC等柱色谱对泰国大风子的化学成分进行分离纯化,应用谱学技术鉴定化合物的结构。并采用MTT法检测化合物的体外细胞毒活性。从泰国大风子的干燥成熟种仁中分离鉴定了10个化合物,分别为2-(4-hydroxy-3,5-dimethoxyphenyl)-3-(2-hydroxy-5-methoxyphenyl)-3-oxo-1-propanol(1)、threo-1,2-bis-(4-hydroxy-3-methoxyphenyl)-propane-1,3-diol(2)、erythro-1,2-bis-(4-hydroxy-3-methoxyphenyl)-propane-1,3-diol(3)、2-(4-hydroxy-3-methoxyphenyl)-3-(2-hydroxy-5-methoxyphenyl)-3-oxo-1-propanol(4)、3-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-propan-1-one(5)、3′-甲氧基木犀草素(6)、楝叶吴萸素B(7)、芹菜素-3′-甲氧基-7-O-芸香糖苷(8)、木犀草素(9)、牡荆素(10)。其中化合物1为新化合物。化合物4、5为首次从该属植物中分离得到。所有化合物均无明显的细胞毒活性。     

狼毒大戟化学成分及其生物活性研究

目的 研究狼毒大戟(Euphorbia fischeriana Steud)根部的抗肿瘤化学成分。方法 运用硅胶柱、ODS、Sephadex LH-20柱色谱以及制备HPLC等多种方法对狼毒大戟根部的体积分数95%乙醇提取物进行分离纯化,并利用HR-ESI-MS、NMR等波谱技术对分离得到的化合物进行结构鉴定。运用CCK-8检测法测定分离得到的化合物对人肝癌细胞Hep-G2、人乳腺癌细胞MCF-7和人肺癌细胞A549的细胞毒活性。结果 从狼毒大戟中共分离得到12个化合物,分别鉴定为7-oxocallitrisic acid(1)、ent-12-hydroxy-12[R]-abieta-8(14),13(15)-dien-16,12-olide(2)、13β-hydroxy-7-oxoabiet-8(14)-en-19,6β-olide(3)、decandrol A(4)、daphneaine B(5)、二氢红花菜豆酸(6)、phenethyl-6-O-α-L-arabinofuranosyl-β-D-glucoside(7)、2-(4-hydroxyphenyl)ethyl-O-α-L-arabinofuranosyl-(1→6)-O-β-D-glucopyranoside(8)、γ-pyrone-2-O-β-D-(6-galloyl)-glucopyranoside(9)、6-hydroxy-2-methoxy-4-O-α-L-arabinofurano-syl(1→6)-β-D-glucopyranoside(10)、(2,3-trans,4E)-2,3-methano-4-decen-1-ol)(11)和3, 4′-O-dimethylellagic acid(12)。结论 化合物1,4,5,7～9和11为首次从大戟属植物中分离得到,化合物1,2,4～9,11和12为首次从狼毒大戟中分离得到。化合物2对人肝癌细胞Hep-G2表现出较好的细胞毒活性,其半数抑制浓度(half maximal inhibitory concentration,IC₅₀)值为32.81 μmol·L^-1,提示该类二萜化合物可能与狼毒大戟的抗肿瘤活性相关。     

檵木水溶性化学成分研究

目的 研究檵木水溶性化学成分。方法 采用大孔树脂、硅胶、凝胶、制备高效液相等色谱技术进行分离,根据波谱数据对化合物进行结构鉴定。结果 从檵木叶中分离得到10个化合物,分别鉴定为(6S,9R)-roseoside(1),rhododendrin(2),epirhododendrin(3),(1S,2R,4S,5S)(-)-Angelicoidenol 2-O-β-D-glucopyranoside(4),dihydroalangionoside A(5),(Z)-3-hexenyl β-primeveroside(6),benzyl β-primeveroside(7),(Z)-3-hexenyl O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside(8),rhododendrol 4'-O-β-D-glucopyranoside(9),3-(4-hydroxyphenol)propyl β-D-glucopyranoside(10)。结论 化合物1~7,9,10均首次从该属植物中分离得到。     

耳叶杜鹃化学成分研究

目的对耳叶杜鹃化学成分进行研究。方法采用正相硅胶柱层析、制备薄层层析及制备型HPLC等方法分离纯化,利用NMR、MS等波谱学方法鉴定化合物结构。结果从耳叶杜鹃中分离并鉴定了7个化合物(化合物1~7),分别为蒲公英赛醇(1)、白桦酯酸(2)、东莨菪素(3)、苯甲酸(4)、(+)-(7R,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7,9-diol-7'-aldehyde(5)、threo-2,3-bis(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-ol(6)、(+)-丁香脂素(7)。结论其中所有化合物均是首次从耳叶杜鹃中分离得到,化合物5、6是首次从杜鹃花中分离得到。     

泰国大风子的化学成分研究

目的 研究泰国大风子的化学成分.方法 采用柱色谱手段,结合波谱方法(MS、ID NMR)分离鉴定泰国大风子的化学成分.结果 从泰国大风子的石油醚和醋酸乙酯部分分离纯化了15个化合物.分别鉴定为对羟基苯甲醛(1)、4-羟基-3-甲氧基苯甲醛(2)、5-羟基-3-醛基吲哚(3)、蔗糖(4)、3-羟基-1-(4-羟基-3-甲氧基苯)-1-丙酮(5)、楝叶吴萸素B (6)、erythro-l,2-bis-(4-hydroxy-3-methoxyphenyl)-propane-1,3-diol (7)、threo-1,2-bis-(4-hydroxy-3-methoxyphenyl)-propane-l,3-diol (8)、erythro-1-(4-hydroxy-3-methoxyphenyl)-2-｛4-[2-formyl-(E)-vinyl]-2-methoxyphenoxy｝-propane-1,3-diol (9)、threo-1-(4-hydroxy-3-methoxyphenyl)-2- ｛4-[2-formyl-(E)-vinyl]-2-methoxyphenoxy ｝-propane-1,3-diol (10)、胡萝卜苷(11)、齐墩果酸(12)、3′-甲氧基木犀草素(13)、5,4′-二羟基-7-甲氧基黄酮(14)、木犀草素(15).结论 所有化合物均为首次从该植物中分离得到.     

狭叶薰衣草中木脂素类化合物的研究

目的对狭叶薰衣草Lavandulaangustifolia中的木脂素类化合物进行研究。方法运用RP-HPLC、TLC、硅胶、凝胶、MCI-gel树脂等方法进行分离纯化,并根据理化性质和波谱数据鉴定化合物的结构。结果从狭叶薰衣草中分离得到11个木脂素类化合物,分别鉴定为松脂醇(1)、丁香树脂醇(2)、fraxiresinol-4′-O-β-D-glucopyranoside(3)、syringaresinol-4′-O-β-D-glucopyranoside(4)、8-hydroxypinoresinol-4-O-β-D-glucopyranoside(5)、rel-(2α,3β)-7-O-methylcedrusin(6)、落叶松脂醇-4′-O-β-D-葡萄糖苷(7)、(2S,3R)-2,3-dihydro-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxybenzofuran-5-(trans)propen-1-ol-3-O-β-glucoside(8)、(7S,8R)-dihydrodehydrodiconiferylalcohol-9-β-D-glucopyranoside(9)、(7R,8R)-7,8-dihydro-9′-hydroxyl-3′-methoxyl-8-hydroxymethyl-7-(4-hydroxy-3-methoxyphenyl)-1′-benzofuranpropanol-9′-O-β-D-glucopyranoside(10)、(E)-3-((2S,3S)-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-2,3-dihydrobenzofuran-5-yl)allyl-2-hydroxyacetate(11)。结论 11个化合物均首次从狭叶薰衣草中分离得到。     

党参的化学成分研究

目的:研究云南高海拔地区产党参(臭参)的化学成分。方法:采用正反相硅胶柱层析、Sephadex LH-20柱等色谱法从党参中分离得到11个化合物,采用核磁共振、质谱等波谱学方法解析化合物结构。结果:从党参乙酸乙酯部位中分离得到11个化合物,分别鉴定为:trandirin(1)、绿原酸(2)、pilosulyne C(3)、tetradeca-trans,trans-6,12-diene-8,10-diyne-1,5,14-triol(4)、1-(4′-hydroxy-3′-methoxyphenyl)-2-[4″-(3-hydroxypropyl)-2″,6″-dimethoxyphenoxy]propane-1,3-diol(5)、1-(4-hydroxy-3-methoxyphenyl)-2-O-(6-hydroxy-2-methoxy-4-omegahydroxypropylphenyl)propane-1,3-diol-4-O-demethylforsythenin(6)、siringaresinol(7)、5-甲氧基-(+)-异落叶松脂素(8)、salicifoliol(9)、caruilignan D(10)和7R,8S-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-5-(3-methoxyallyl)-7-methoxycoumaran(11)。结论:其中,化合物4～11为首次从该属植物中分离得到。     

瓦山安息香树皮中木脂素类成分研究

目的:研究瓦山安息香树皮的化学成分。方法:采用柱色谱手段,结合波谱方法分离鉴定瓦山安息香树皮的化学成分。结果:从瓦山安息香树皮的95%乙醇提取物中分离得到10个木脂素类化合物,分别鉴定为:pinoresinol 4-O-β-D-glucopyranoside(1)、穗罗汉松树脂酚苷(2)、styraxlignolide B(3)、3-(β-D-glucopyranosyloxymethyl)-2-(4-hydroxy-3-methoxyphenyl)-5-(3-hydroxypropyl)-7-methoxy-(2R,3S)-dihydrobenzofuran(4)、burselignan(5)、(+)-neo-olivil(6)、threo-1-(4-hydroxy-3-methoxyphenyl)-2-[4-(3-hydroxypropyl)-2-methoxyphenoxy]-1,3-propanediol(7)、erythro-1-(4-hydroxy-3-methoxyphenyl)-2-[4-(3-hydroxypropyl)-2-methoxyphenoxy]-1,3-propanediol(8)、isolariciresinol(9)、(+)-lariciresinol(10)。结论:其中,化合物5~10为首次从安息香属植物中分离得到。     

乌桕叶化学成分研究

通过利用正相硅胶色谱、大孔吸附树脂柱色谱、葡聚糖凝胶LH-20色谱、制备薄层色谱和半制备HPLC等多种分离方法,运用现代波谱技术对所分离的化合物进行结构鉴定,从乌桕Sapium sebiferum叶中分离得到15个化合物,分别鉴定为(+)-(7R,7′R,7"S,7(')S,8S,8′S,8"S,8(')S)-4",4(')-dihydroxy-3,3′,3",3('),5,5′-hexamethoxy-7,9';7',9-diepoxy-4,8";4′,8(')-bisoxy-8,8′-dineo-lignan-7",7('),9",9(')-tetraol(1),1-(4′-hydroxy-3'-methoxyphenyl)-2-[4"-(3-hydroxy propyl)-2",6"-dimethoxyphenoxy]propane-1,3-dio1(2),苏式-2,3-二-(4-羟基-3-甲氧基苯)-3-甲氧基丙醇(3),threo-5-hydroxy-3,7-dimethoxyphenylpropane-8,9-diol(4),boropinol B(5),threo-8S-7-methoxysyringylglycerol(6),5-羟甲基糠醛(7),5-甲氧甲基-1H-吡咯-2-甲醛(8),槲皮素(9),山柰酚(10),没食子酸乙酯(11),松柏醛(12),香草醛(13),7-羟基-6-甲氧基香豆素(14),正二十七烷醇(15),除化合物9～ 11,14外,以上化合物均为首次从乌桕中分离得到.     

Discovery of natural products from Curcuma longa that protect cells from beta-amyloid insult: a drug discovery effort against Alzheimer's disease

From Curcuma longa, two novel compounds, 4' '-(3' "-methoxy-4' "-hydroxyphenyl)-2' '-oxo-3' '-enebutanyl 3-(3'-methoxy-4'hydroxyphenyl)propenoate (calebin-A, 1) and 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,4,6-heptatrien-3-one (2), and seven known compounds, 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (curcumin, 3), 1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione (demethoxycurcumin, 4), 1,7-bis(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione (bisdemethoxycurcumin, 5), 1-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)-6-heptene-3,5-dione (6), 1,7-bis(4-hydroxyphenyl)-1-heptene-3,5-dione (7), 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (8), and 1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadien-3-one (9), were isolated following a bioassay-guided fractionation scheme utilizing an assay to detect protection of PC12 cells from beta-amyloid insult. Compounds 1, 3-5, and 7 were found to more effectively protect PC12 cells from betaA insult (ED(50) = 0.5-10 microg/mL) than Congo red (10) (ED(50) = 37-39 microg/mL).     

分心木中的木脂素类化学成分及其抗HIV活性研究

目的研究分心木Diaphragma Juglandis Fructus中的木脂素类化学成分及其抗人免疫缺陷病毒(HIV)活性。方法运用柱色谱方法对分心木的95%甲醇提取物进行分离纯化,结合波谱技术与理化常数鉴定结构,通过LEDGF/p75-IN蛋白复合体ELISA筛选模型对化合物进行抗HIV活性筛选。结果从分心木95%甲醇提取物中分离得到16个木脂素类化合物,分别鉴定为(-)-丁香脂素(1)、(+)-松脂素(2)、(+)-(7R,7′R,7″S,7′′′S,8S,8′S,8″S,8′′′S)-4″,4′′′-dihydroxy-3,3′,3″,3′′′,5,5′-hexamethoxy-7,9′;7′,9-diepoxy-4,8″;4′,8′′′-bisoxy-8,′-dineolignan-7″,7′′′,9″,9′′′-tetraol(3)、2,3-二羟基-1-(4′-羟基-3′-甲氧基苯基)-丙-1-酮(4)、3-羟基-1-(4′-羟基-3′-甲氧基苯基)-丙-1-酮(5)、3′,4′-二甲氧基苯丙二醇(6)、(2S)-3,3-二-(4-羟基-3-甲氧基苯基)-丙-1,2-二醇(7)、3-羟基-1-(4′-羟基-3′,5′-二甲氧基苯基)-丙-1-酮(8)、(1R,5R,6R)-6-{4′-O-[8″-(7″-(4″-hydroxy-3″-methoxyphenyl))glyceol]-3′,5′-dimethoxyphenyl}-3,7-dioxabicyclo[3.3.0]octan-2-one(9)、curcasinlignan B(10)、evofolin-B(11)、(7S,8R)-dihydrodehydrodiconiferyl alcohol(12)、pinnatifdanin C I(13)、(+)-(7S,8S)-4,1′-dihydroxy-3,3′,5′-trimethoxy-7,8,9-trinor-8,4′-oxyneolignan-7,9-diol(14)、八角莲醇(15)、1-(4′-羟基-3′-甲氧基苯基)-2-[4″-(3-羟丙基)-2″,6″-二甲氧基苯基]-丙-1,3-二醇(16)。结论所有化合物均为首次从分心木中分离得到,其中化合物13具有潜在的抑制HIV-1的活性。     

瑶山润楠根的化学成分研究

对樟科润楠属植物瑶山润楠Machilus yaoshansis根乙醇提取物的化学成分进行研究。利用多种色谱技术从瑶山润楠的醋酸乙酯萃取物中分离得到15个化合物;通过理化性质和波谱数据鉴定其结构为12个木脂素类(+)-愈创木素(1),kadsuralignan C(2),(+)-异落叶松脂素(3),(+)-5’-甲氧基异落叶松脂素(4),南烛木树脂酚(5),内消旋-裂环异落叶松树脂酚(6),异落叶松脂素-9’-O-β-D-吡喃木糖苷(7),5’-甲氧基-异落叶松脂素-9’-O-β-D-吡喃木糖苷(8),南烛木树脂酚9’-O-β-D-吡喃木糖苷(9),(2R,3R)-2,3-二氢-2-(4-羟基-3-甲氧基苯基)-7-甲氧基-3-甲基-5-(E)-丙烯基苯并呋喃(10),3,5’-二甲氧基-4’,7-环氧-8,3’-新木脂素-4,9,9’-三醇(11),甘密树皮素B(12),和3个黄烷类(+)-儿茶素(13),(-)-表儿茶素(14),bis-8,8’-catechinylmethane(15)。化合物1～15均为首次从该植物中分离得到。     

Bromophenol derivatives from the red alga Rhodomela confervoides

Eight new bromophenol derivatives, 2,3-dibromo-4,5-dihydroxybenzyl methyl sulfoxide (1), 4-(2,3-dibromo-4,5-dihydroxyphenyl)-3-butene-2-one (2), 2-(3-bromo-5-hydroxy-4-methoxyphenyl)-3-(2,3-dibromo-4,5-dihydroxyphenyl)propionic acid (3), 2-(3-bromo-5-hydroxy-4-methoxyphenyl)-3-(2,3-dibromo-4,5-dihydroxyphenyl)propionic acid methyl ester (4), 2-phenyl-3-(2,3-dibromo-4,5-dihydroxyphenyl)propionic acid (5), 4'-methoxy-2',3',3'-tribromo-4',5',5'-trihydroxydiphenylacetic acid (6), and 3-bromo-5-hydroxy-4-methoxyphenylacetic acid (7) and its methyl ester (8), together with a known bromophenol, 3-bromo-5-hydroxy-4-methoxybenzoic acid (9), were isolated from the red alga Rhodomela confervoides. Their structures were elucidated by spectroscopic methods including IR, EIMS, FABMS, ESIMS, HRFABMS, HRESIMS, 1D and 2D NMR, and single-crystal X-ray structure analysis. Compounds 1-4, 8, and 9 were found inactive against several human cancer cell lines and microorganisms.     

��Ӣˮ��ȡ��Ļ�ѧ�ɷ��о�

??OBJECTIVE To study the chemical components of the aqueous extract of Solanum lyratum. METHODS The compounds were isolated and purified by column chromatography and their structures were elucidated by spectroscopic methods. RESULTS Nine phenylpropanoids were obtained from aqueous extracts of Solanum lyratum. The structures were determined as chlorogenic acid(1), crptochlorogenic acid(2), neochlorogenic acid(3), erythro-1,2-bis-(4-hydroxy-3- methoxyphenyl)-1,3-propanediol(4), threo-1,2-bis-(4-hydroxy-3-methoxyphenyl)-1,3-propanediol(5), erythro-2,3-bis-(4-hydroxy-3-methoxyphenyl)-3-methoxypropanol(6), threo-2,3-bis-(4-hydroxy-3- methoxyphenyl)-3-methoxypropanol(7), syringaresinol(8), and liriodendrin(9). CONCLUSION Compounds 2-9 are isolated from Solanum lyratum for the first time.     

�ɽ��н�����ɷֵķ������

??OBJECTIVE To study the chemical constituents of Zingiber officinale Rosc. METHODS Various column chromatographic techniques were used to isolate and purify the chemical constituents and their structure were elucidated by spectral analysis. RESULTS Ten compounds were isolated and identified as 6-shogoal (??), 9-shogoal (??), 10-shogoal (??), 12-paradol (??), 6-gingerol (??), 6-isodehydrogingerdione (??), 8-isodehydrogingerdione (??), 5-hydroxy-1-(4'-hydroxy-3'-methoxyphenyl)-4-hexa-decen-3-one (??), (E)-geranylferulic acid (??), and 5-ethoxy-1-(4-hydroxy-3-methoxyphenyl)tetradecan-3-one (??). CONCLUSION The compounds ??, ??, ??, ??, ?? and ?? are isolated from Zingiberis Rhizoma for the first time.     

Aromatase inhibitors from Broussonetia papyrifera.

Bioassay-guided fractionation of an ethyl acetate-soluble extract from the whole plants of Broussonetia papyrifera, using an in vitro aromatase inhibition assay, led to the isolation of five new active compounds, 5,7,2',4'-tetrahydroxy-3-geranylflavone (1), isogemichalcone C (8), 3'-[gamma-hydroxymethyl-(E)-gamma-methylallyl]-2,4,2',4'-tetrahydroxychalcone 11'-O-coumarate (9), demethylmoracin I (10), and (2S)-2',4'-dihydroxy-2' '-(1-hydroxy-1-methylethyl)dihydrofuro[2,3-h]flavanone (11), and 10 known (12-21) compounds which were also found to be active. Of these compounds, the most potent were 9 (IC(50) 0.5 microM), 11 (IC(50) 0.1 microM), isolicoflavonol (12, IC(50) 0.1 microM), and (2S)-abyssinone II (13, IC(50) 0.4 microM). Additionally, six new compounds, 5,7,3',4'-tetrahydroxy-6-geranylflavonol (2), 5,7,3',4'-tetrahydroxy-3-methoxy-6-geranylflavone (3), (2S)-7,4'-dihydroxy-3'-prenylflavan (4), 1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)propane (5), 1-(2,4-dihydroxy-3-prenylphenyl)-3-(4-hydroxyphenyl)propane (6), and 1-(4-hydroxy-2-methoxyphenyl)-3-(4-hydroxy-3-prenylphenyl)propane (7), were isolated and characterized, but proved to be inactive as aromatase inhibitors, as were an additional 21 known compounds. The structures of the new compounds (1-11) were elucidated by spectroscopic methods. Structure-activity relationships in the aromatase assay were determined for the benzofurans, biphenylpropanoids, coumarins, and various types of flavonoids (chalcones, flavans, flavanones, and flavones) obtained among a total of 42 constituents of B. papyrifera.     

Neoclerodane diterpenoids from Croton eluteria

Five new neoclerodane diterpenoids, rel-(3R,4S,5R,7R,8S,9R,10S,12R,20S)-7-acetoxy-15,16,12,20-diepoxy-3,4-dihydroxy-20-methoxyneocleroda-13(16),14-diene (1), rel-(3R,4S,5R,7R,8S,9R,10S,12R,20S)-7-acetoxy-15,16,12,20-diepoxy-3,4,20-trihydroxyneocleroda-13(16),14-diene (2), rel-(3R,4S,5S,6R,7S,8S, 9R,10S,12R,20S)-6,7-diacetoxy-3,4,15,16,12,20-triepoxy-20-hydroxyneocleroda-13(16),14-diene (3), rel-(3R,4S,5R,7R,8S,9R,10S,12R,20S)-7-acetoxy-3,4,15,16,12,20-triepoxy-20-hydroxyneocleroda-13(16),14-diene (4), and rel-(3R,4S,5R,7R,8S,9R,10S,12R,20R)-7,20-diacetoxy-3,4,15,16,12,20-triepoxyneocleroda-13(16),14-diene (5), have been isolated from the bark of Croton eluteria. The structures of the compounds 1-5 (cascarillins E-I) were determined by spectroscopic data interpretation.