川乌的纤维素酶酶解提取工艺研究

目的 比较纤维素酶、半仿生、乙醇回流提取方法对川乌中乌头碱、乌头总碱的影响,筛选最佳方法。 方法 利用纤维素酶辅助提取川乌生物碱,以乌头碱、乌头总碱提取率为指标,正交试验优化纤维素酶的最佳提取条件,再与半仿生、乙醇提取方法进行比较。 结果 提取乌头碱、乌头总碱的最佳酶解条件为：温度45 ℃,pH值4.5,酶用量8 mg/g,酶解时间5 h,乌头碱提取率为0.002 447%,乌头总碱提取率为0.244 410%,半仿生提取乌头碱、乌头总碱的提取率分别为0.001 735%、0.189 340%,乙醇回流提取乌头碱、乌头总碱提取率分别为0.001 869%、0.200 720%,纤维素酶提取法具有明显的优势。 结论 酶解提取法可显著提高乌头碱、乌头总碱的提取率,可在实际生产中推广应用。     

An autopsy case of postpartum acute myocardial infarction associated with postpartum ergot alkaloids administration in old-aged pregnant women

Cases of acute myocardial infarction (AMI) that occur during pregnancy or postpartum are rarely reported. Ergot derivatives are known to induce the spasmodic contraction of coronary arteries. Administration of ergot derivatives can cause AMI, even in normal healthy people. In several reported cases, ergot derivatives triggered severe AMI during the postpartum period. Here, we report the case of a forty-year-old woman who was successfully impregnated by artificial fertilization and died after treatment with ergot derivatives. The autopsy revealed AMI with severe coronary atherosclerosis. This is the first case that reports aggravation of pre-existent severe coronary atherosclerosis after postpartum infusion of ergot derivatives.     

Peptide alkaloids from Zizyphus sativa bark

Two new cyclopeptide alkaloids, sativanine-N and sativanine-O were isolated from the stem bark of Zizyphus sativa and their structures were established by spectral analysis.     

Generalized dermatitis due to codeine. Cross-sensitization among opium alkaloids

Opium alkaloids can cause immunological reactions. Cross-sensitization among them must be considered in these situations.     

A general procedure for the enantioselective synthesis of the minor tobacco alkaloids nornicotine, anabasine, and anatabine

The minor tobacco alkaloids nornicotine, anabasine, and anatabine from Nicotiana tobacum are known to possess nicotinic receptor agonist activity, although they are relatively less potent than S-(-)-nicotine, the principal tobacco alkaloid. Previous pharmacological investigations and structure-activity studies have been limited owing to the lack of availability of the optically pure forms of these minor alkaloids. We now report a 2-step synthetic procedure for the enantioselective synthesis of the optical isomers of nornicotine and anabasine, and a modified procedure for the synthesis of anatabine enantiomers. These procedures involve initial formation of the chiral ketimine resulting from the condensation of either 1R, 2R, 5R-(+)- or 1S, 2S, 5S-(-)-2-hydroxy-3-pinanone with 3-(aminomethyl)pyridine followed by enantioselective C-alkylation with an appropriate halogenoalkane or halogenoalkene species, N-deprotection, and base-catalyzed intramolecular ring closure, to form the appropriate, chirally pure minor tobacco alkaloid. Using this approach, the R-(+)- and S-(-)-enantiomers of the above minor tobacco alkaloids were obtained in good overall chemical yield and excellent enantomeric excess.     

Selective Inhibition of Bitter Taste of Various Drugs by Lipoprotein

Previously, we demonstrated that lipoprotein composed of phosphatidic acid (PA) and -lactoglobulin (LG) selectively and reversibly suppress the frog taste nerve response to bitter substances. In the present study, we examined the effects of various lipoproteins on the taste sensation to various stimuli in humans by a psychophysical method. Among various lipoproteins composed of different of lipids and proteins, the lipoproteins composed of PA and proteins were most effective in suppressing bitter taste. The lipoproteins composed of PA and LG, bovine serum albumin, ovalbumin, -lactoalbumin or casein similarly suppressed effects on sensation of bitter taste. Using PA-LG, the effects on taste sensation to various stimuli were examined. The bitter taste of all twelve substances examined was inhibited, while saltiness of NaCl and sweetness of sucrose were not inhibited. The inhibition of bitter taste was completely reversible. Masking of the target sites for bitter substances on the taste receptor membranes with PA-LG seems to contribute to the inhibition of bitter taste. Direct binding of the bitter substances to PA-LG in the medium also contributes to the inhibition of bitter taste of certain substances. Among various drugs, basic and hydrophobic substances such as quinine, denatortium and propranolol have low taste thresholds and are said to be the most bitter. PA-LG most effectively suppressed the bitter taste of such substances. PA originates from soybeans and the proteins used except for bovine serum albumin originate from milk or eggs, and hence the lipoproteins can be safely used to mask the bitter taste of drugs.     

Monoterpenoid indole alkaloids from Alstonia mairei and their cytotoxicity

Phytochemical investigation on the 70% ethanol extract of the leaves of Alstonia mairei resulted in the isolation of three new monoterpenoid indole alkaloids, alstomairines A–C (1–3), along with one known compound, alpneumine A (4). Structural elucidation of all the compounds was accomplished by spectral methods such as 1D and 2D NMR, IR, UV, and HRESIMS. The isolated compounds were tested in vitro for cytotoxic activities against four osteosarcoma cell lines. Consequently, alkaloids 2 and 3 exhibited cytotoxic activities for all tested tumor cell lines with IC₅₀ values from 9.2 to 13.0 μM.     

两面针果壳的化学成分分析及活性

目的:利用高效液相色谱-线性离子阱/静电场轨道阱高分辨质谱(HPLC-LTQ/Orbitrap-MS)技术对两面针非药用部位果壳中的生物碱类成分进行分析和鉴定,并对其抗氧化活性进行研究,为两面针植物更深入地研究开发提供科学依据。方法:采用HPLC-LTQ/Orbitrap-MS采集数据后,对各色谱峰的质谱图高分辨一级和二级质谱数据进行解析,与文献数据库进行对比,对各色谱峰进行结构推测和确认。采用1,1-二苯基-2-三硝基苯肼(DPPH)清除自由基能力法及2,2'-联氮-双-3-乙基苯并噻唑啉-6-磺酸(ABTS)自由基清除能力对两面针果壳样品抗氧化活性进行研究。结果:从两面针果壳中共鉴定了25个生物碱类化合物,主要化学成分为异喹啉类生物碱(两面针碱、鹅楸掌碱、木兰箭毒碱),吡咯类生物碱(别隐品碱、氧化苦参碱、氧化槐果碱),喹啉类生物碱(木兰花碱、氯化两面针碱),有机胺类生物碱(γ-山椒素)。DPPH清除自由基能力法及ABTS自由基清除能力对其抗氧化活性进行了研究,结果显示在测定的浓度范围内,抗氧化活性均随着试样浓度的增加而逐渐增强,呈现良好的剂量依赖性。结论:该文对两面针果壳进行了化学成分及活性的研究,研究证明其具有多种生物碱类成分,并具有较好的抗氧化活性,为两面针植物更深入地研究开发提供了参考。     

香港鹰爪花枝叶中的化学成分研究

目的研究番荔枝科鹰爪花属植物香港鹰爪花Artabotrys hongkongensis枝叶中的化学成分。方法综合运用硅胶柱色谱、ODS柱色谱、SephadexLH-20凝胶柱色谱以及制备型高效液相色谱等现代色谱分离方法进行系统分离,根据化合物的理化性质及其波谱学数据鉴定化合物的结构。结果从香港鹰爪花枝叶的90%乙醇提取物中分离得到了16个化合物,分别鉴定为melilotocarpanA(1)、medicarpin(2)、5,7,8-trimethoxyflarone(3)、2′-hydroxy-3′,4′,6′-trimethoxychalcone(4)、piperolactam C(5)、uvarilactam(6)、artacinatine(7)、p-coumaroyl-β-phenethylamine(8)、artapilosol A(9)、大花紫玉盘醇B(10)、1,6-desoxypipoxide(11)、1β,11-dihydroxy-5-eudesmen(12)、黑麦草内酯(13)、4-hydroxy-3-methoxybenzaldehy(14)、syringlaldehyde(15)和rabdosia acid A(16)。结论所有化合物均为首次从香港鹰爪花中分离得到,除化合物2、7和9以外,其他化合物均为首次从鹰爪花属植物中分离得到。