矢镞叶蟹甲草中1个新的8-O-3'型新木脂素

目的研究矢镞叶蟹甲草Parasenecio rubescens全草的化学成分。方法采用硅胶柱色谱、MCI小孔树脂柱色谱、Sephadex LH-20凝胶柱色谱及半制备高效液相色谱法对矢镞叶蟹甲草全草化学成分进行分离纯化,并通过NMR等波谱学技术鉴定所分离得到的单体化合物的结构;运用MTT法测试细胞毒活性。结果从矢镞叶蟹甲草90%丙酮提取物中分离得到10个化合物,分别鉴定为7R,8S-3-(3,4-methylenedioxybenzyl)-7,9-diangeloyloxy-5’-methoxy-9’-hydroxy-8-O-3’-neolignan (1)、黄体酮(2)、孕甾-1,4-二烯-3,20-二酮(3)、β-谷甾醇(4)、胡萝卜苷(5)、珊瑚菜内酯(6)、异茴芹素(7)、咖啡酸乙酯(8)、(+)-annuionone D (9)、(-)-asperentin (10)。结论化合物1～10均为首次从该植物中分离得到。化合物1为1种新的8-O-3’型新木脂素,命名为矢镞叶蟹甲草素W。化合物2和3为植物来源的较少见的孕甾烷类成分。化合物1在给药浓度为100μmol/L时,对小鼠黑色...     

望春花中的木脂素类化学成分研究

目的 研究望春花Magnolia biondii花蕾的木脂素类化学成分，为制定辛夷的质量标准寻找标准物庾，也为了进一步了解其有效成分。方法 硅胶柱色谱分离，波谱分析(UV、IR、MS、3H-NMR、13C-NMR)鉴定结构。结果 分离并鉴定了4个木脂素(Ⅰ～Ⅳ)和1个新木脂素(Ⅴ)类化合物：veraguensin(Ⅰ)、松脂素二甲醚(pinoresinol dimethyl ether，Ⅰ)、木兰脂素(magnolin，in)、里立脂素B二甲醚(1irioresinol—B dimethyl ether，Ⅳ)和denudatone(Ⅴ)。结论 化合物Ⅰ和Ⅴ系首次从该植物中分离得到。     

石南藤中木脂素和新木脂素成分的研究

目的:对石南藤的化学成分进行研究.方法:采用各种色谱技术进行分离纯化,并利用理化常数和波谱数据鉴定化合物结构.结果:从石南藤50%乙醇提取物的二氯甲烷萃取部位分离并鉴定了9个化合物,其中包括1个木脂素(-)-gal-belgin(1)和8个新木脂素:玉兰脂B(2),山蒟素D(3),(+)-licarin A(4),海风藤酮(5),南藤素(6),山蒟素C(7),山蒟素B(8),(+)-burchellin(9).结论:化合物1,3,4,8,9为首次从该植物中分离得到.     

北沙参中的新8-O-4′型异木脂素

为了研究北沙参的化学成分，通过大孔树脂吸附柱色谱、 Sephadex LH-20及反相ODS柱色谱进行化合物的分离， 利用多种波谱技术鉴定化合物结构。从醇提物的乙酸乙酯溶部分， 分离得到1个新化合物， 命名为可来灵素D(glehlinoside D，1)， 以及5个已知化合物： 裂异落叶松脂醇(2)、 阿魏酸(3)、 咖啡酸(4)、 香草酸(5)和丁香苷(6)。化合物1为一新的8-O-4′型异木脂素类化合物。     

Pharmacokinetics and Metabolism of 4‐O‐Methylhonokiol in Rats

The purpose of this study was to characterize the pharmacokinetics and metabolism of 4‐O‐methylhonokiol in rats. The absorption and disposition of 4‐O‐methylhonokiol were investigated in male Sprague–Dawley rats following a single intravenous (2 mg/kg) or oral (10 mg/kg) dose. Its metabolism was studied in vitro using rat liver microsomes and cytosol. 4‐O‐Methylhonokiol exhibited a high systemic plasma clearance and a large volume of distribution. The oral dose gave a peak plasma concentration of 24.1±3.3 ng/mL at 2.9±1.9 h and a low estimated bioavailability. 4‐O‐Methylhonokiol was rapidly metabolized and converted at least in part to honokiol in a concentration‐dependent manner by cytochrome P450 in rat liver microsomes, predicting a high systemic clearance consistent with the pharmacokinetic results. It was also shown to be metabolized by glucuronidation and sulfation in rat liver microsomes and cytosol, respectively. 4‐O‐Methylhonokiol showed a moderate permeability with no apparent vectorial transport across Caco‐2 cells, suggesting that intestinal permeation process is not likely to limit its oral absorption. Taken together, these results suggest that the rapid hepatic metabolism of 4‐O‐methylhonokiol could be the major reason for its high systemic clearance and low oral bioavailability. Copyright © 2013 John Wiley & Sons, Ltd.     

Anti‐platelet Activity of Erythro‐(7S,8R)‐7‐acetoxy‐3,4,3′,5′‐tetramethoxy‐8‐O‐4′‐neolignan from Myristica fragrans

Platelets play a critical role in pathogenesis of cardiovascular disorders and strokes. The inhibition of platelet function is beneficial for the treatment and prevention of these diseases. In this study, we investigated the anti‐platelet activity of erythro‐(7S,8R)‐7‐acetoxy‐3,4,3′,5′‐tetramethoxy‐8‐O‐4′‐neolignan (EATN), a neolignan isolated from Myristica fragrans, using human platelets. EATN preferentially inhibited thrombin‐ and platelet‐activating factor (PAF)‐induced platelet aggregation without affecting platelet damage in a concentration‐dependent manner with IC₅₀ values of 3.2 ± 0.4 and 3.4 ± 0.3 μM, respectively. However, much higher concentrations of EATN were required to inhibit platelet aggregation induced by arachidonic acid. EATN also inhibited thrombin‐induced serotonin and ATP release, and thromboxane B₂ formation in human platelets. Moreover, EATN caused an increase in cyclic AMP (cAMP) levels and attenuated intracellular Ca²⁺ mobilization in thrombin‐activated human platelets. Therefore, we conclude that the inhibitory mechanism of EATN on platelet aggregation may increase cAMP levels and subsequently inhibit intracellular Ca²⁺ mobilization by interfering with a common signaling pathway rather than by directly inhibiting the binding of thrombin or PAF to their receptors. This is the first report of the anti‐platelet activity of EATN isolated from M. fragrans. Copyright © 2013 John Wiley & Sons, Ltd.     

油丹化学成分的研究

从油丹Ａｌｓｅｏｄａｐｈｎｅ ｈａｉｎａｎｅｎｓｉｓ Ｍｅｒｒ,树皮中分离得到４个化合物,根据ＨＲ－ＳＩＭＳ、＾１ＨＮＭＲ、＾１３ＣＮＭＲ及二维核磁共振技术鉴定其结构分别为：一个木脂素ｅｕｓｉｄｅｒｉｎ Ａ「７Ｒ,８Ｒ）－３,４,５,３’－四甲氧基－△＾８’,９’－８－Ｏ－４‘,７－Ｏ－５’木脂素」（Ⅰ）;两个苄基异喹啉类生物碱（６,７－二甲氧基异喹啉基）－（４’－甲氧基苯基）甲酮（Ⅱ）、（６,７     

Enzymatic synthesis of a dihydrobenzofuran neolignan by oxidative coupling

The oxidative dimerization of ferulic acid has been carried out using horse-radish peroxidase as catalyst to give a dihydrobenzofuran neolignan (1), the structure of which was elucidated as (2SR,3RS)-2,3-dihydro-2-(4-hydroxy-3-methoxyphenyl)-3-n-buto xycarbonyl-5-(2E-carboxyethenyl)-7-methoxybenzofuran by spectroscopic analyses. This compound showed more potent cytotoxicity against several tumor cell lines than the starting material.     

肉豆蔻的化学成分研究

目的 对生品肉豆蔻Myristicae Semen的化学成分进行研究.方法 采用硅胶柱色谱、Sephadex LH-20柱色谱和制备型HPLC等方法进行分离纯化,结合波谱数据分析鉴定化合物结构.结果 从肉豆蔻75%醇提物的醋酸乙酯萃取物中分离得到18个化合物,分别鉴定为香草酸(1)、紫铆因(2)、(2R)-3-(3', 4', 5'-三甲氧基苯基)-1, 2-丙二醇(3)、硫磺菊素(4)、3-甲氧基-4, 5-亚甲二氧基肉桂酸(5)、7, 3', 4'-三羟基黄酮(6)、7-羟基色原酮(7)、verrucosin(8)、(+)-赤-(7S, 8R)-Δ^8'-7-羟基-3, 4, 3', 5'-四甲氧基-8-氧代-4'-新木脂素(9)、(-)-赤-(7R, 8S)-Δ^8'-7-乙酰基-3, 4, 3', 5'-四甲氧基-8-氧代-4'-新木脂素(10)、nectandrin B(11)、(-)-(7S, 7'R, 8S, 8'R)-4, 4'-二羟基-3, 5, 3'-三甲氧基-7, 7'-环氧木脂素(12)、fragransin B₃(13)、fragransin B₁(14)、(-)-enantiomer(15)、(-)-赤-(7R, 8S)-Δ^8'-7-羟基-3, 4, 5, 3', 5'-五甲氧基-8-氧代-4'-新木脂素(16)、(+)-赤-(7S, 8R)-Δ^8'-7, 4-二羟基-3, 5, 3', 5'-四甲氧基-8-氧代-4'-新木脂素(17)、(+)-5-甲氧基脱氢二异丁香酚(18).结论 化合物2、4～7为从肉豆蔻属植物中首次分离得到,化合物1为从该植物中首次分离得到.