马桑根的化学成分研究

从马桑(Coria rianepalensis Wal,i.e._{Coriaria sinica} Maxim)的根茎中分得9个化合物。根据理化性质及IR,UV,MS,¹HNMR,¹³HNMR数据鉴定它们的结构分别为布拉易林(I),去甲布拉易林(I),双氢马桑毒素(II),马桑毒素(IV),羟基马桑毒素(V),马桑亭(VI),阿朴羟基马桑毒素(VII),羟基马桑亭(VII)和没食子酸(IX)。其中,I,II为首次从该植物分离得到,II为首次从植物中发现,VII,VII为新化合物。     

中药秦皮的化学成分

目的：对中药秦皮的化学成分进行研究。方法：采用硅胶柱层析、Sephadex LH-20凝胶柱层析对秦皮的化学成分进行分离，通过理化性质和波谱方法鉴定其结构。结果和结论：从秦皮中分离得到13个化学物，其中首次分得的化合物有咖啡酸(caffic acid，1)，芥子醛葡萄糖苷(sinapaldehyde glucoside，2)，对羟基苯乙醇三十烷酸酯(triacontanoic acid，2-(4-hydroxyphenyl)ethyl triacontanate，3)，丁香醛(syringaldehyde，5)，芥子醛(sinaoaldehyde，6)，Osmanthuside H(8)，三十烷酸(triacontanoic acid，13)，其余为对羟基苯乙醇(4)，丁香苷(7)，( )松脂素-4’-O—β-D-葡萄糖苷(9)，β-谷甾醇(10)，胡萝卜苷(11)，熊果酸(12)，三十三烷酸(13)。     

Inhibition of carbonic anhydrase IX as a novel anticancer mechanism

Carbonic anhydrases (CA, EC 4.2.1.1) catalyze the interconversion bewteen carbon dioxide and bicarbonate with generation of protons. The carbonic anhydrase isozyme IX (CA IX) is highly overexpresed in hypoxic tumors and shows very restricted expression in normal tissues. CA IX is a dimeric protein possessing very high catalytic activity for the hydration of carbon dioxide to protons and bicarbonate. Its quaternary structure is unique among members of this family of enzymes, allowing for structure-based drug design campaigns of selective inhibitors. Inhibition of CA IX with sulfonamide and/or coumarin inhibitors was recently shown to lead to a potent retardation for the growth of both primary tumors and metastases. Some fluorescent sulfonamides were shown to accumulate only in hypoxic tumor cells overexpressing CA IX, and might be used as diagnostic tools for imaging of hypoxic cancers. Sulfonamide inhibitors were also more effective in inhibiting the growth of the primary tumors when associated with irrdiation. CA IX is thus both a diagnostic and therapeutic validated target for the management of hypoxic tumors normally non-responsive to classical chemio- and radiotherapy.     

Chemical constituents of Selinum cryptotaenium

A new pyranocoumarin, named secryptotaenin A, determined as 3'(S)-angeloyloxy-3',4'-dihydroseselin, was isolated from the roots of Selinum cryptotaenium, along with thirteen known compounds, umbelliferone, osthol, coumurrayin, (+)-heraclenol, longshengensin A, anomalin, ferulic acid, galactitol, stearic acid, melissic acid, lignoceric acid, β-sitosterol and daucosterol. Their structures were determined on the basis of spectroscopic methods.     

Synthesis and relative binding affinity to human steroid receptors of substituted 3-aryloxycoumarins

The synthesis of a set of substituted 3-aryloxycoumarins was performed. The study of the relations between their structure and their relative binding affinity to human androgen, progesterone, alpha and beta estrogen receptors was achieved.     

蛇床子素对去卵巢大鼠近侧胫骨代谢影响的定量研究

切除3月龄SD大鼠双侧卵巢12周后,其骨形成的参数值明显增加(%L.Pm+58%,BFR/BV+105%,BFR/BS+74%,%O.Pm+188%),同时骨吸收的参数值增加(%Er.Pm+155%),荧光标记周长与吸收周长的比率-41%,由于骨吸收大于骨形成,骨质丢失(%Tb.Ar-59%,Tb.Th-14%),出现高转换型骨质疏松。分别用蛇床子素(osthole)6.7mg·kg^-1ig,每周6次,尼尔雌醇(nilestri-ol) 1 mg·kg^-1ig,每周1次,持续12周,均能明显抑制去卵巢诱导的骨高转换,防止骨质丢失。但蛇床子素抑制骨高转换的效应比尼尔雌醇低(蛇床子素治疗组比尼尔雌醇治疗组%Tb.Ar-55%)。     

Quantity and quality of potential drug interactions with coumarin anticoagulants in the Netherlands

Objective Coumarin anticoagulants are prone to potentially life-threatening drug-drug interactions due to a combination of unfavorable properties. However, real life data on the actual occurrence are scarce. The aim of this study was to quantify and qualify potential drug interactions with coumarin anticoagulants in daily practice. Methods A cohort study including all users of phenprocoumon or acenocoumarol during the period 1991–2003 in the PHARMO Record Linkage System. All 24 individual drugs and 11 drug groups interacting with coumarins according to central database used in the Dutch pharmacies were considered. Main outcome measure Frequency and type of potential drug interactions during anticoagulant therapy with coumarins. Results 48,627 out of 76,455 mainly acenocoumarol-users (64%) were dispensed at least one potentially interacting drug (PID) during anticoagulant therapy. About 35% of these cases were dispensed a (very) strongly interacting drug, whereas 3% were dispensed a contraindicated drug. Antibacterial drugs and NSAIDs (39% and 37% of all users, respectively) were the most frequently dispensed PIDs. Conclusion Potential drug interactions with coumarins frequently occur in daily practice, confronting two-thirds of patients with an increased risk of bleeding. To a large part, this is attributable to commonly prescribed medication like antibacterial drugs and NSAIDs. This situation substantiates the need for proper monitoring or new anticoagulants with less drug–drug interactions.     

Constituents of the fruits and leaves of Euodia daniellii

Four flavonoid glycosides, flavaprin (7), evodioside B (8), vitexin (11), and hesperidin (12), as well as the coumarins bergapten (1), xanthotoxin (2), and isopimpinellin (3), the lignan simplexoside (10), the steroids beta-sitosterol (4) and daucosterol (5), the limonoids isolimonexic acid (6) and limonin (9), and uracil (13) and myo-inositol (14) have been isolated from Euodia daniellii. The structures of these compounds were established from spectral data. Among the isolates, bergapten showed cyclooxygenase-2 inhibitory activity with an IC50 value of 6.2 microg/ml. Flavonoids isolated from this plant exhibited no cytotoxic activity against the human tumor cell lines, A549, SKOV-3, SKMEL-2, XF498, and HCT15.     

水曲柳HPLC指纹图谱研究

目的:建立水曲柳药材的高效液相(HPLC)指纹图谱,为水曲柳的鉴别及质量控制提供依据。方法:对不同产地、不同采集时间的水曲柳药材皮中的香豆素成分进行指纹图谱研究。结果:HPLC指纹图谱中峰的分离度均好,共得到10个共有峰;10批样品的相似度较好。结论:所建立的指纹图谱可用于水曲柳药材的鉴定及质量评价。     

秦皮总香豆素超声辅助提取工艺优化

目的:优化秦皮总香豆素的超声醇提工艺。方法:采用单因素试验方法研究超声辅助提取过程中乙醇体积分数、料液比、提取温度、提取时间和超声频率对秦皮总香豆素提取率的影响,并采用正交试验确定最佳提取工艺条件。结果:秦皮总香豆素超声辅助提取的最佳提取工艺为:按1∶10(质量-体积比)的料液比加入60%乙醇,于50℃条件下用175 W超声辅助提取50 min,秦皮总香豆素提取率可达到6.283%。结论:与传统索氏提取相比,该工艺具有耗时少、耗能少和提取率高等优点。