空心莲子草中三萜皂苷类化学成分的研究

为了研究苋科植物空心莲子草[Alternanthera philoxeroides(Mart.)Griseb]抗病毒活性的物质基础,对其化学成分进行了研究。本文主要报道从空心莲子草正丁醇部位分离得到的5个三萜皂苷类化合物,经图谱分析,结构分别鉴定为:3-O-β-D-吡喃葡萄糖(1→3)-O-[β-D-吡喃葡萄糖]-齐墩果酸-28-O-β-D-葡萄糖醛酸苷(1)、齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸苷(2)、齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸-28-O-β-D-吡喃葡萄糖苷(竹节参苷Ⅳa,3)、3-O-β-D-吡喃葡萄糖醛酸丁酯-齐墩果酸-28-O-β-D-吡喃葡萄糖苷(4)和3-O-β-D-吡喃葡萄糖醛酸-常春藤皂苷K(尼泊尔常春藤皂苷K,5),其中化合物1为新化合物,化合物4和5为首次从该植物中分离得到。     

高效液相色谱法测定陕西境内不同产地、不同生长期女贞子中2组分的含量

目的:建立用高效液相色谱法测定陕西境内不同产地、不同生长期女贞子中齐墩果酸与熊果酸含量的方法。方法:采收陕西境内关中3市(渭南、西安、宝鸡)与陕南2市(安康、汉中)10月产女贞子;并采收西安8、9、10、11和12月产女贞子,去杂质阴干,室温密闭贮藏。色谱柱为LichrospherC18(250mm×4.6mm,5μm),流动相为乙腈-甲醇-水-磷酸-三乙胺(50∶30∶20∶0.02∶0.04),流速为1mL.min-1。结果:安康产女贞子中齐墩果酸与熊果酸含量均达到同期最高。不同生长期女贞子在10月份出现齐墩果酸含量最高值;而熊果酸在幼果中(8月)含量最高并随生长期延长逐渐下降。到12月时二者含量均降至最低。结论:女贞子在不同产地、不同生长期齐墩果酸和熊果酸的含量是不同的,故在实际应用时应根据不同需要适时采收。     

女贞子化学成分研究

目的:研究女贞子的化学成分。方法:采用硅胶、反相ODS、Sephadex LH-20、反相HPLC等色谱分离手段对女贞子乙酸乙酯萃取部位进行分离纯化,通过ESI-MS、NMR等波谱技术和化学方法鉴别所分离得到化合物的结构。结果:从中分离得到8个化合物,分别鉴定为:齐墩果酸(oleanolic acid,1)、2α-羟基齐墩果酸(2α-hydroxy oleanolic acid,2)、19α-羟基-乌苏酸(19α-hydroxy ursolic acid,3)、委陵菜酸(tormentic acid,4)、3β-O-顺式-香豆酰-2α-羟基-齐墩果酸[3β-O-(cis-p-Coumaroyl)-2α-hydroxy oleanolic acid,5]、3β-O-反式-香豆酰-2α-羟基-齐墩果酸[3β-O(-trans-p-Coumaroyl)-2α-hydroxy oleanolic acid,6]、3-O-顺式-香豆酰-委陵菜酸(3-O-cis-p-Coumaroyl tormentic acid,7)、3-O-反式-香豆酰-委陵菜酸(3-O-trans-p-Coumaroyl tormentic acid,8)。结论:化合物3、5、7、8为首次从该属植物中分离得到。     

高效液相色谱法测定不同炮制法的女贞子中齐墩果酸的含量

目的:探讨不同炮制法对女贞子中齐墩果酸含量的影响.方法:采用高效液相色谱法,以shim-pack-ods(150mm×4.6 mm,5μm)为分析柱.甲醇-水(95:5)为流动相,流速为1.0mL·min,柱温为室温,检测波长为210 nm.结果:在浓度0.05～1.6 g·L-1范围内,齐墩果酸的浓度与峰面积线性关系良好(r=0.999 7),平均回收率为98.54%(n=6).结论:炮制方法不同对女贞子中齐墩果酸的溶出有影响,对女贞子的炮制及从女贞子中提取齐墩果酸具有参考意义.     

正交试验法优选女贞子中齐墩果酸的提取工艺

目的优选女贞子中提取齐墩果酸的最佳提取工艺条件。方法采用正交试验法,以高效液相色谱法(HPLC)测定齐墩果酸的含量,对提取工艺进行考察。结果影响提取的主要因素是浸泡时间,其次是加水量,再次是提取次数。从女贞子中提取齐墩果酸的最佳工艺为药材加水量为10倍,浸泡时间为8h,提取次数(2h/次)为3次。结论该工艺可提高女贞子中齐墩果酸的提取率和纯度。     

女贞子及其有效成分的保肝作用研究进展

女贞子具有保肝的药理作用,已经证实齐墩果酸、红景天苷、女贞子多糖等化合物是其保肝的有效成分。女贞子提取物及其有效成分能对抗多种化学性肝损伤、对抗免疫性或缺血再灌注性肝损伤以及抗肝纤维化,其中齐墩果酸的保肝作用被研究得最为广泛而深入;抗氧化应激、抗炎、抑制肝星状细胞增殖和活化、促进其凋亡以及肝细胞再生可能是它们共同的保肝机制。综述了女贞子粗提物、女贞子多糖和红景天苷保肝作用的研究进展。     

珠子参的化学成分

目的对珠子参[PanaxjaponicusC.A.Mey.var.major(Buck.)C.Y.Wu et K.M.Feng]根茎的化学成分进行研究。方法采用硅胶柱色谱进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果分离得到8个化合物,分别鉴定为苯甲酸(benzoin acid,1)、豆甾醇(stigmasterol,2)、齐墩果酸(oleanolic acid,3)、胡萝卜苷(daucosterol,4)、齐墩果酸-28-O-β-D-吡喃葡萄糖苷(oleanolicacid-28-O-β-D-glucopyranoside,5)、齐墩果酸-3-O-β-D-吡喃葡萄糖基(1→2)-β-D-(6′-丁酯)吡喃葡萄糖醛酸苷(oleanolic acid-3-O-β-D-glucopyranoside(1→2)-β-D-glucorunopyranosy-6′-O-butylester,6)、竹节参皂苷IVa(chikusetsusaponinⅣa,7)、人参皂苷Ro(ginsenoside,8)。结论化合物6为新化合物,化合物1、2为首次从该种植物中分离得到。     

一测多评法同时测定二至丸中8个成分

目的:建立一测多评(QAMS)法同时测定二至丸(女贞子、墨旱莲)中红景天苷、女贞苷、特女贞苷、橄榄苦苷、木犀草素、蟛蜞菊内酯、芹菜素和齐墩果酸的含有量.方法:采用高效液相色谱法,使用Agilent ZOBAX C18(250 mm × 4.6 mm,5 μm)色谱柱,以乙腈-0.2％磷酸水溶液为流动相,梯度洗脱,流速1...     

栀子根化学成分的分离与鉴定

目的对栀子(Gardenia jasminoides Ellis)的根进行化学成分研究。方法应用硅胶柱色谱、ODS柱色谱和Sephadex LH-20柱色谱等分离手段进行分离纯化,根据理化性质及波谱数据鉴定化合物的结构。结果从栀子根体积分数为70%的乙醇提取物中分离得到10个化合物,分别鉴定为桦木酸(betulinic acid,1)、齐墩果酸(oleanolic acid2,)、齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸苷-6'-O-甲酯(oleanolic acid 3-O-β-D-glucuronopyranoside-6'-O-methyl ester,3)、常春藤皂苷元-3-O-β-D-吡喃葡萄糖醛酸苷-6'-O-甲酯(hederagenin 3-O-β-D-glucuronopyranoside-6'-O-methyl ester,4)、竹节参苷(chikusetsusaponinⅣa,5)、豆甾醇(stigmasterol,6)、β-谷甾醇(β-sitosterol,7)、胡萝卜苷(dau-costerol,8)、香草酸(vanillic acid,9)、丁香酸(syringic acid,10)。结论化合物3～5、8～10为首次从栀子属植物中分离得到,化合物12、7、为首次从栀子根中分离得到。     

大孔吸附树脂纯化女贞子中齐墩果酸的研究

目的建立应用大孔吸附树脂纯化齐墩果酸的方法。方法以齐墩果酸的吸附量,齐墩果酸的含量和齐墩果酸的提取率为考察指标,确定大孔吸附树脂提取齐墩果酸的工艺条件。结果AB-8型树脂对女贞子中齐墩果酸有良好的吸附分离性能,可用于提取女贞子中齐墩果酸的工业化生产,其工艺条件为:齐墩果酸最大吸附量为108mg·g^-1,吸附流速为2BV·h^-1,洗脱剂为95%乙醇,解吸流速为2BV·h^-1。洗脱液经浓缩,乙醇溶解,活性炭脱色,重结晶得到结晶性粉末齐墩果酸,熔点为306～308℃,产品纯度大于98%,提取率平均达89.58%。用IR表征了产物结构。结论该工艺简单易行,提取率高,可用于女贞子中齐墩果酸的提取。     

CATECHOLAMINE INACTIVATION IN UTERINE TISSUES: CHANGES IN PREGNANCY IN THE RAT

1. In vitro metabolism of [3H]-(-)-noradrenaline (3H-NA), 0.2 mumol/l, was measured in rat endometrial and myometrial slices at different stages of gestation and compared with that in dioestrous rats. Metabolism of 3H-NA, 0.2 mumol/l, was measured in rat placental slices from day 14 of gestation onwards. 2. 3H-NA was metabolized mainly by deamination in rat myometrium, with [3H]-3,4-dihydroxyphenylethylene glycol, (3H-DOPEG) being the major metabolite. Cocaine, 30 mumol/l, inhibited 3H-DOPEG formation and the amount of 3H-NA remaining in the tissue. O-methylated metabolite formation was unaffected by cocaine. 3. O-methylation and deamination were equally active pathways for metabolizing 3H-NA in rat endometrium. O-methylation to [3H]-normetanephrine (3H-NMN) predominated in the placenta. In both tissues O-methylated metabolite formation was inhibited by 30 mumol/l cocaine. 4. In myometrium, metabolite formation per gram was constant in the first half of pregnancy and was similar to that in dioestrous animals. By day 17 of gestation, however, [3H]-O-methylated deaminated metabolites (3H-OMDA), comprising 3-methoxy, 4-hydroxy-phenylethylene glycol and vanillylmandelic acid, and 3H-NMN formation were less than in dioestrous animals. 5. Endometrial 3H-NMN and 3H-DOPEG formation per gram were higher in rats at day 5 of gestation than in dioestrous rats but metabolite formation per gram declined thereafter to reach values equal to (3H-DOPEG) or less than (3H-OMDA and 3H-NMN) those in dioestrous rats. 6. 3H-NMN and 3H-OMDA formation per gram decreased from day 14 to day 20 of gestation in rat placentae.(ABSTRACT TRUNCATED AT 250 WORDS)     

2005年北京地区海洛因毒品中稀释剂的分析

目的:对2005年收缴的"零包"海洛因毒品中的稀释剂进行分析。方法:准确称取可疑毒品适量,用SKF525做内标,用乙醇配制成1.0mg.kg-1的样品溶液,取1μl进行GC/MS分析。结果:在408份"零包"海洛因毒品中,检测出含有机稀释剂的323份,占79.2%。检测出的有机稀释剂是烟酰胺(231份,占总份数的56.6%)、咖啡因(135份,占总份数的33.1%)、扑热息痛(51份,占总份数的12.5%)、氨基比林(39份,占总份数的9.6%)、茶碱(37份,占总份数的9.1%)、非那西丁(29份,占总份数的7.1%)、脑复康(28份,占总份数的6.9%)、镇静催眠药(10份,占总份数的2.4%)、曲马朵及其它(10份,占总份数的2.4%)。结论:北京地区"零包"海洛因毒品中多数有有机稀释剂,且种类繁多。脑复康是一个新发现的稀释剂。     

PRESENCE OF CHOLINOCEPTORS IN MESENCEPHALIC RAPHE NUCLEI CONCERNED IN THERMOREGULATION IN RABBITS

1. The thermal effects of cholinomimetics and cholinoceptor blocking agents microinjected into mesencephalic nucleus raphe medianus (NRM) were investigated in rabbits to determine the nature and role of these cholinoceptors in thermoregulation. 2. Microinjection of cholinoceptor agonists, carbachol and pilocarpine, into NRM resulted in significant hyperthermia which could be blocked by local pretreatment with chlorisondamine (a nicotinic receptor blocker) as well as by ethybenztropine (a muscarinic receptor blocker). 3. Intracerebroventricular pretreatment with LM 5008 (serotonin reuptake blocker) significantly inhibited the carbachol-induced hyperthermia. 4. Both nicotinic and muscarinic cholinoceptors are present in mesencephalic NRM which may be involved in thermoregulation in rabbits. Activation of these cholinoceptors in NRM results in hyperthermia which seems to be due to an inhibition of a serotonin sensitive hypothalamic heat loss mechanism.     

反式曲马朵在大鼠肝微粒体O-去甲基代谢中的立体选择性

目的研究反式曲马朵O-去甲基代谢的立体选择性.方法高效毛细管电泳法测定大鼠肝微粒体孵育液中反式曲马朵和O-去甲基曲马朵对映体的浓度,酶促动力学方法研究O-去甲基曲马朵对映体的生成.结果 (-)-O-去甲基曲马朵生成有较大的Vmax;反式曲马朵两对映体间存在相互作用,使(+)-O-去甲基曲马朵生成的Vmax明显减慢;奎宁及奎尼丁对(+)-O-去甲基曲马朵生成的抑制作用较强.结论反式曲马朵O-去甲基代谢有立体选择性,对映体间的相互作用及酶抑制剂使其立体选择性程度加强.     

国产阿克拉霉素A的体内外抗肿瘤作用

国产阿克拉霉素A(aclacinomycin;ACM-A)能明显抑制体外培养小鼠白血病P₃₈₈和人体胃癌SGC-7901细胞的生长。在0.01 μg/ml浓度时能抑制65.4%的克隆形成,ED₅₀为0.0085μg/ml。ACM-A对白血病小鼠有显著治疗作用,延长小鼠生命时间143%,并有半数小鼠获得治疗。对Ehrlich腹水癌和肉瘤-180也有较强的抑制作用,对肉瘤-180的作用与adriamycin相似。ACM-A主要抑制³H-TDR和。H-UR分别参人人体胃癌细胞的DNA和RNA;大剂量时对蛋白质合成也有影响。P₃₈₈细胞实验中证明ACM-A对DNA合成的抑制程度与adriamycin相似,低于daunomycin。     

INCREASE IN HAEMATOCRIT IN BORDERLINE HYPERTENSIVE MEN

1. Haematologic parameters were measured in untreated borderline hypertensive (BHT) men, and weight and age matched with normotensive men to determine whether previously described increased haematocrit (Hct) in established hypertension is evident in borderline hypertension. 2. Haematocrit was significantly increased in BHT men (mean 0.46, s.d. 0.032) compared with normotensive men (mean 0.43, s.d. 0.014) and correlated significantly with mean arterial pressure in this group (r = 0.67, P= 0.036) independent of weight. 3. The correlation of blood pressure with Hct in BHT men supports the concept that increased Hct may contribute to increased blood viscosity and thus to raised arterial pressure.     

HAEMODYNAMIC CHANGES IN ACTH-INDUCED HYPERTENSION IN SHEEP

1. ACTH (20 μg/kg per day) produced an elevation in blood pressure associated with an increase in cardiac output in conscious sheep, due in the first 72 h to a rise in heart rate. Stroke volume did not rise until the fourth day of ACTH treatment. 2. Calculated total peripheral resistance did not change. 3. Intravenous administration of acebutolol prior to and during ACTH administration did not modify the rise in blood pressure, but this was associated with a rise in total peripheral resistance. 4. These studies show that while ACTH-induced hypertension is usually associated with increased cardiac output, rather than total peripheral resistance it still occurs, but is associated with a rise in total peripheral resistance if the rise in cardiac output is prevented by /J-adrenoreceptor blockade.     

PLASMA LEVELS OF ATRIAL NATRIURETIC PEPTIDE IN MAN IN PRIMARY ALDOSTERONISM, IN GORDON''S SYNDROME AND IN BARTTER''S SYNDROME

Plasma levels of ANP were measured in normal subjects and in three conditions associated with disturbed volume homeostasis. Levels of ANP were appropriately raised in seven patients with primary aldosteronism, and fell to normal following removal of an aldosterone-producing adenoma in six and dexamethasone treatment in one patient with glucocorticoid-suppressible hyperaldosteronism. The level of ANP in one patient with Gordon's syndrome (a condition associated with plasma volume expansion) was lower than in the patients with primary aldosteronism, both before and after saline infusion. This is consistent with reduced ANP responsiveness in this condition. responsiveness in this condition. Levels of ANP were inappropriately elevated in three patients with Bartter's syndrome (a condition with plasma volume contraction) and rose further during saline infusion. This is consistent with primary hypersecretion of ANP.     

藿胆丸薄层色谱鉴别方法的改进

本文对《中国药典》收载的藿胆丸的薄层鉴别（2）进行了改进，使操作过程简便、快速，同时减少了溶剂的用量，避免了高浓度碱液对玻璃器皿的损伤。