Synthesis of [7‐14C]bergapten

Bergapten (1) is a furocoumarin natural product and currently employed to treat skin disorders. Since past attempts to radiolabel 1 with ¹⁴C were limited to only its 5‐methoxy group, a synthesis of the required ring [7‐¹⁴C]1 is now described. The literature reported precursor 4‐methoxy‐6‐hydroxybenzofuran‐5‐carboxaldehyde (3) was Wittig reacted with stabilized [carbonyl‐¹⁴C]methoxycarbonylmethylenetriphenylphosphorane (4) to obtain [7‐¹⁴C]1 in 47% radiochemical yield, with the desired product being characterized by thin‐layer chromatography, HPLC, m.p. and proton NMR.     

Design,synthesis, and evaluation of new series of Imperatorin analogs with potential vasodilatory activity

Two series of imperatorin analogs were synthesized based on our previous research and evaluated for their vasodilatation activities on in vitro rat mesenteric artery, basilar artery, and renal artery ring models. Target compounds were characterized by infrared, ¹H NMR, and mass spectra. Most derivatives possessed significant vasodilatory activity on the mesenteric artery, and compound 3a exhibited favorable and broad vasodilatation activities on three kinds of rat artery ring models. The pharmacological results indicated that introducing nitrogen-contained ring in side chain or large steric hindrance at the distal end could increase the vasodilatory activity. Further, replacement of oxygen atom (–O–) in the skeleton of furocoumarin derivatives with nitrogen (–NH–) could cause the decrease of vasodilatory activity. The molecular docking also indicated that compound 3a showed a best affinity with α-1C receptor (PDB ID: 3G43). All these results suggested compound 3a would be a potential vasodilatory agent for hypertension.     

藏波罗花的化学成分研究

目的:对藏药材藏波罗花Incarvillea younghusbandii的化学成分进行分离纯化和结构鉴定。方法:采用正反相硅胶柱色谱和Sephadex LH-20凝胶柱色谱方法进行分离纯化,NMR和MS等波谱方法进行结构鉴定。结果:从藏波罗花的地上部分甲醇提取物中共分离鉴定出15个化合物:异佛手柑内酯(1),6-甲氧基当归素(2),欧前胡素(3),花椒毒内酯(4),珊瑚菜内酯(5),heraclenol(6),rivulobirin A(7),齐墩果酸甲酯(8),咖啡酸甲酯(9),银桦酸(10),boschniakinic acid(11),tert-O-β-D-glucopyranosyl-(R)-heraclenol(12),5-methoxy-8-O-β-D-glucopyranosyloxypsoralen(13),1′-O-β-D-glucopyranosyl-3-hydroxynodakenetin(14)和苯乙醇-O-β-D-吡喃葡萄糖-(1→2)-β-D-吡喃葡萄糖苷(15)。结论:上述化合物均为首次从该植物中分离得到,主要成分为呋喃香豆素类化合物。     

河北道地药材北沙参HPLC-PDA指纹图谱研究

目的:建立河北道地药材北沙参HPLC-PDA指纹图谱分析方法,并与不同产地北沙参药材指纹图谱特征进行比较,为科学评价与有效控制北沙参药材质量提供新方法。方法:采用DiamonsilTM C18(250 mm×4.6 mm,5m)色谱柱,流动相为甲醇-乙腈-0.05%磷酸水溶液,梯度洗脱,流速1.0 mL.min-1,柱温30℃,检测波长295 nm。结果:13批道地药材的相似度在0.9以上,化学组成一致性较好;不同产地饮片相似度只在0.1～0.4之间。结论:本方法操作简便、快速、准确,为北沙参药材的鉴别和质量的全面控制提供了依据。     

Coumarins Isolated from the Roots of Seseli resinosum. in Turkey

Abstract

Seseli resinosum. Freyn et Sint. (Umbelliferae) is a perennial herb that grows in the northern region of Anatolia, Turkey. The n.-hexane extract obtained from the roots of S. resinosum. was investigated for the presence of coumarins. Three angular-type pyranocoumarins and two linear-type furocoumarins were isolated from the roots. The compounds were identified as (+)-samidin [(3′S., 4′S.)-3′-senecioyloxy-4′-acetoxy-3′, 4′-dihydroseselin] (1), (?)-anomalin [(3′R., 4′R.)-3′, 4′-diangeloyloxy-3′, 4′-dihydroseselin] (2), calipteryxin (3′R., 4′R.)-3′-angeloyloxy-4′-senecioyloxy-3′, 4′-dihydroseselin (3), isoimperatorin (4), and deltoin (5). The structures were determined using spectroscopic methods (¹H NMR, ¹³C NMR, ¹H-¹H COSY, ¹H-¹³C COSY, HMBC, MS), physical methods (melting point and optical rotation), and chemical correlations with known compounds that have been described in the literature. The chemotaxonomic significance of these isolated coumarins is discussed in the genus Seseli. L.     

Heracleum mantegazzianum growth phases and furocoumarin content

The observation of photocontact dermatitis from Heracleum mantegazzianum Sommier et Levier in 2 gardeners at work prompted the analysis of furocoumarin content of stem, leaves and fruits of the plant during a period of 1 year. Their concentration was found to be maximal in fruit, intermediate in leaf, and minimal in stem. Psoralen was the most prevalent substance in the leaf and bergapten in the fruit. In the stem, in contrast, individual furocoumarins were found in lower but variable concentrations. 3 furocoumarin seasonal peaks were observed in the leaf: the maximal peak occurred in June, the intermediate in August, the minimal in November. This trend corresponds to 3 biological phases of the weed.     

Treatment of a case of mycosis fungoides and one of parapsoriasis en plaque with topical PUVA using a monofunctional furocoumarin derivative, 4,6,4'-trimethylangelicin

A case of plaque stage mycosis fungoides and one of parapsoriasis en plaque were treated with topical PUVA therapy using a monofunctional furocoumarin derivative, 4,6,4'-trimethylangelicin (TMA). Both patients showed complete clearance of eruptions within 16 treatments. The therapeutic effectiveness of TMA was confirmed by the fact that those eruptions exposed to UVA alone, without TMA application, showed slower and less significant improvement. Histologically, dermal infiltrates of mycosis cells and associated epidermotrophism disappeared almost completely in response to TMA PUVA. No side effects or changes in values in laboratory examinations were observed during treatment.     

少腹逐瘀颗粒联合左氧氟沙星治疗慢性盆腔炎的临床研究

欧洲药品管理局（EMA）于2007年10月颁布了《欧白芷Angelica archangelic L.制剂中含有的呋喃香豆素相关的风险评估报告》,建议了关于草药中呋喃香豆素的风险管理策略。欧盟当局及其成员国往往要求申报者依据该评估报告对含当归的草药制剂进行安全性评估。介绍该评估报告的主要内容,并勘误了关于当归Angelica sinensis的2处错误,阐述了笔者的观点,期望对中国含当归的中成药进入欧洲市场有所启示。