赤芝子实体中三萜化学成分的研究

自赤芝[Ganoderma lucidum (Fr.)Karst]的二氯甲烷溶解部分分离得到一个新的三萜内酯化合物,命名为灵芝内酯(ganolactone)。根据光谱(UV,IR,¹HNMR,¹³CNMR,MS和2DNMR)解析,确定其结构为I式。同时还从赤芝子实体中分到三个已知化合物,即灵芝醇A(ganoderiolA,II),灵芝醇B(ganoderiolB,II)和灵芝三醇(ganodermatriolIV)。     

Triterpenoids from the Fruiting Body of Ganoderma lucidum

自赤芝［Ｇａｎｏｄｅｒｍａｌｕｃｉｄｕｍ（Ｆｒ．）Ｋａｒｓｔ］的二氯甲烷溶解部分分离得到一个新的三萜内酯化合物，命名为灵芝内酯（ｇａｎｏｌａｃｔｏｎｅ）。根据光谱（ＵＶ，ＩＲ，１ＨＮＭＲ，１３ＣＮＭＲ，ＭＳ和２ＤＮＭＲ）解析，确定其结构为１式。同时还从赤芝子实体中分到三个已知化合物，即灵芝醇Ａ（ｇａｎｏｄｅｒｉｏｌＡ，２），灵芝醇Ｂ（ｇａｎｏｄｅｒｉｏｌＢ，３）和灵芝三醇（ｇａｎｏｄｅｒｍａｔｒｉｏｌ４）。     

灵芝的化学成分

目的研究灵芝[Ganoderma lucidum(Leys.ex Fr.)Karst]的化学成分。方法采用硅胶柱色谱、反相ODS柱色谱、反相HPLC等手段从体积分数为90%的灵芝醇提物中分离得到14个化合物,并利用波谱学方法鉴定它们的化学结构。结果分离得到14个化合物,分别鉴定为灵芝酸A(1)、灵芝烯酸A(2)、灵芝酸H(3)、灵芝酸C2(4)、灵芝酸A甲酯(5)、灵芝酸B(6)、20-羟基灵芝酸G(7)、灵芝烯酸D甲酯(8)、灵芝烯酸D(9)、赤芝酸D2甲酯(10)、灵芝烯酸G(11)、灵芝酸D(12)、山奈酚(13)、金雀异黄素(14)。结论化合物13、14为本属首次分离得到的化合物,化合物11为本植物首次分离得到的化合物。     

赤芝子实体中一个新的三萜化合物(英文)

赤芝 (Ganoderma lucidum) 是我国及东亚地区常用的民间草药, 具有良好的治疗及保健作用。本文对赤芝子实体的化学成分进行了研究, 从中分离并鉴定了两个羊毛甾烷型三萜类化合物, 其中化合物1为新化合物, 鉴定为 (24S)-羊毛甾-7-氧-8-烯-3β, 24, 25-三醇, 并命名为灵芝三醇 M (1); 化合物2为灵芝酸ε 。     

赤芝子实体的化学成分及其抗肿瘤活性

目的:研究赤芝子实体的化学成分及其体外抗肿瘤活性。方法:用硅胶柱色谱法,Sephadex LH-20柱色谱法及制备型高效液相色谱法进行分离纯化,依据理化性质和光谱数据鉴定化合物结构;用MTT法测试化合物体外抗肿瘤活性。结果:分离得到6个化合物,其结构鉴定为ganoderone A(1)、麦角甾醇(2)、麦角甾醇过氧化物(3)、麦角甾-7、22-二烯-3β,5α,6β-三醇(4)、灵芝酸DM (5)和7-oxo-灵芝酸Z(6);化合物1,3对人慢性粒细胞白血病细胞K562和人结肠癌细胞SW620的IC₅₀分别为9.61,10.70 mg·L^-1和22.38,32.48 mg·L^-1,化合物1~6对人急性髓系白血病细胞HL60的IC₅₀分别为7.14,11.07,2.80,7.54,51.82和7.39 mg·L^-1。结论:ganoderone A为首次从赤芝中分离得到;灵芝中的甾醇及三萜类化合物均有一定抗肿瘤活性。     

赤芝子实体中三萜酸类成分及其抗人乳腺癌SKBR3细胞增殖活性

目的 研究赤芝Ganoderma lucidum子实体中三萜酸类成分及其抗肿瘤活性.方法 用硅胶柱色谱、反相ODS柱色谱、反相HPLC等方法分离得到13个化合物,利用波谱学方法鉴定它们的化学结构,并进一步确定各化合物对乳腺癌SKBR3细胞的生物活性.结果 分离得到13个三萜酸类的化合物,分别鉴定为灵芝烯酸C(1)、灵芝酸C2 (2)、灵赤酸A(3)、灵芝酸G(4)、灵芝烯酸B(5)、灵芝酸B(6)、灵芝酸H(7)、灵芝烯酸A(8)、灵芝酸Ⅰ(9)、灵芝酸A (10)、灵芝烯酸K (11)、灵芝烯酸D(12)、灵芝酸D(13).化合物6在20 μmol/L浓度下对人乳腺癌细胞SK-BR-3的抑制率为40.3％.结论 化合物11是首次从该植物中分离得到的,化合物6对人乳腺癌细胞SK-BR-3显示了一定的抑制活性,其他化合物在该浓度下未显示活性.     

灵芝一测多评质量控制方法的研究

摘 要 目的：采用一测多评法对灵芝子实体中灵芝酸C2、灵芝酸B、灵芝酸G、灵芝酸A、赤芝酸A、灵芝烯酸D、灵芝酸F7种成分进行测定。方法: 采用HPLC色谱法测定,色谱柱为WatersX bridge C18（250 mm×4.6 mm,5 μm）,流动相为乙腈（A） 1%冰乙酸（B）（28∶〖KG-*2〗72）,梯度洗脱0~30 min A的体积分数28%→38%;30~45 min A的体积分数38%→55%;体积流量为1.0 ml·min-1,柱温为30 ℃,检测波长为254 nm。以灵芝酸A为内参物,计算灵芝酸C2、灵芝酸B、灵芝酸G、赤芝酸A、灵芝烯酸D、灵芝酸F的校正因子,同时用外标法计算7种成分的含量,验证一测多评法的可行性和适用性。结果:一测多评法的相对校正因子重现性良好,采用相对校正因子计算所得16批赤芝样品中6种成分的含量与外标法实测值相对偏差均在2%以内。结论:建立的一测多评法测定7种灵芝三萜成分方法准确可靠。     

灵芝子实体的化学成分研究

目的 研究灵芝（Ganoderma lucidum）子实体中的化学成分。方法 用硅胶柱色谱法及Sephadex LH-20柱色谱法进行分离纯化，依据理化性质和光谱数据鉴定化合物结构。结果 从灵芝的乙酸乙酯提取物中分离得到10个化合物，分别被鉴定为：灵芝烯酸B（ganoderenic acid B，1）、灵芝酸A（ganoderic acid A，2）、甲基灵芝酸A（methyl ganoderate A，3）、甲基灵芝酸B（methyl ganoderate B，4）、灵芝酸E（ganoderic acid E，5）、甲基灵芝酸E（methyl ganoderate E，6）、灵芝酸Q（ganoderic acid C3，7）、灵芝酸DM（ganoderic acid DM，8）和灵芝酸G（ganoderic acid G，9），2．（2’-hydroxydocosanoylamino）octadocane-1，3，4-triol（10）。结论 化合物10为新化合物。     

灵芝三萜成分分析

目的建立灵芝子实体、孢子粉、发酵菌丝体三萜成分的HPLC含量测定方法.方法以赤芝孢子酸A(ganosporeric acid A,1),赤芝酸A(lucidenic acid A,2),灵芝酸B(ganoderic acid B,3)和灵芝酸C(ganoderic acid C,4)为对照品;色谱柱:反相C18;流动相:乙腈-水(37∶63);流速:1.0 mL*min-1;检测波长:UV 254 nm.结果进样量在0.2～1 μg有良好的线性关系,(1),(2),(3)和(4)的加样回收率分别为100.9%,101.2%,101.3%和101.7%.结论本法快速、简便、灵敏和分离度好,适用于灵芝子实体、孢子粉、发酵菌丝体及相关制剂的三萜类物质检查和含量测定.     

鹰爪种子的木脂素和半萜化学成分

从药用植物鹰爪种子分得4个木脂素：异洋商陆素A（soamericanin A,1)，异洋商陆醇A（isoamericanol A,2)，洋商陆素B（americainin,B,3),鹰爪木脂醇（atabotrycinol,4)和一个半萜 ：（R）－鹰爪三醇[(R)-arttaboriol,5],以及棕榈酸（6），β谷甾醇（7）和胡萝卜苷（8），根据光谱数据（IR，UV，MS，1D，2D－NMR）分析，确定它们的化学结构，其中，鹰爪木脂醇（4）是一个新木脂素，（R）－鹰爪三醇（5）是一个新半萜醇，木脂素化合物1，2和3是首次从该植物分得。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.