东阳元胡块茎中的生物碱的化学研究

从浙江省东阳元胡(Corydalis turtschaninovii Bess.f.yanhusuo Y.H.Chou et C.C.Hsü)的块茎中分离了15个生物碱。通过理化常数测定,光谱分析及衍生物制备等方法鉴定了结构,其中9个生物碱文献已报道。(+)-紫堇碱(Ⅰ),(±)-四氢巴马亭(Ⅱ),(—)-四氢黄连碱(Ⅲ),(—)-四氢非洲防己胺(Ⅳ),(+)-紫堇球碱(Ⅴ),去氢紫茧碱(Ⅵ),(+)-海罂粟碱(Ⅶ)普鲁托品(Ⅷ),α-别隐品碱(Ⅸ),5个为首次从该植物中得到的已知化合物(—)-四氢小檗碱(Ⅹ)巴马亭(Ⅺ),非洲防己胺(Ⅻ),(+)-N-甲基樟苍碱(ⅩⅢ)去氢海罂粟碱(ⅩⅣ),1个为新生物碱,暂命名为元胡宁(XV yuanhunine).     

某些四氢异喹啉类生物碱对大鼠脑内多巴胺和5-羟色胺受体的作用

本文报道十二种四氢异喹啉类生物碱对大鼠脑内D-2,5-HT₁和5-HT₂受体的结合特性。其中l-千金藤碱(l-STP)对这三种受体均有较高的亲和力,其Ki值分别为1.7×10^-7,9.4×10^-8和1.8×10^-7mol。l-莲碱(l-REM)对5-HT₂受体的亲和力与Z-STP相似(Ki=1.7×10^-7mol)。THB,THC和THJ对D-2受体的亲和力介于l-SPD和l-THP之间。本文报道的多数生物碱能同时影响两种或两种以上受体部位的结合特性,提示它们对单胺神经系统可能有复杂的相互作用。     

C-7位氧化的阿朴啡(Aporphine)型生物碱

作者从防己科植物Stephania venosa Spreng.(S.rotunde L.)中分离得2种新的7位羟基化的阿朴啡型生物碱Ayuthianine(1)和sukhodianine(2),均属C-6aR构型。同时分离得少量已知生物碱含笑碱A[(-)-Ushinsunine]。据文献记载及本实验结果表明,C-7位氧化的阿朴     

海南青牛胆生物碱的研究

目的:研究海南青牛胆(Tinospora hainanensis H.S.Lo et Z.X.Li) 藤茎中的生物碱成分。方法:用溶剂提取及硅胶柱色谱分离纯化化学成分,通过 MS, NMR, HMQC, HMBC 及X-ray 测定结构。结果:3种季铵生物碱以碘化物形式被分离并鉴定为: 非洲防己碱(colu mba mine ,I)、S-反式-N-甲基四氢非洲防己碱(S-trans-N-m ethyltetrahydrocolu mbamine , II) 及 S-反式-轮环藤酚碱(S-trans-cyclanoline , III) 。结论: I I I是新生物碱。     

雷公藤倍半萜生物碱的分离与结构

从雷公藤(Tripterygiu mwilfordii Hook.f.)根皮中分离到二个倍半萜生物碱,即碱Ⅰ和碱Ⅱ,根据理化性质和光谱(UV,IR,MS,HRMS,^lHNMR,¹³CNMR(COM和OFR),¹H-¹HCOSY,¹H-¹³CCOSY,NOESY和COLOC]解析,鉴定生物碱Ⅰ为euonymine,生物碱Ⅱ为一种新的生物碱,命名为雷公藤明碱(wilfordsine)。初步药理实验证明雷公藤明碱有免疫抑制活性。     

延胡索中的新生物碱——Corydione

作者从保加利亚的罂粟科植物延胡索(Corydalisbulbosa(L.)DC]的全草中分离得一新生物碱Cory-dione(4,5-dioxoaporphine,Ⅰ),以及去氢南天竹啡碱dehydronantenine)。(-)-stylopine、毕扣扣林[(+)bicuculline]、(-)-adlumidine、(+)-南天竹啡碱[(+)-nantenine]、球堇碱[(+)-bulbocapnine]、普     

伊贝碱甙B的分离和结构测定

本文报道自吉林栽培的伊贝母(Fritillaria pallidiflora Schrenk)中分得一种新的C-去甲-D-异甾体生物碱甙,命名为伊贝碱甙B(yibeinoside B)。根据红外、质谱、氢谱和碳谱确定了结构。     

弯喙乌头的化学成分研究

从弯喙乌头(Aconitum campylorrhynchum)中分离出一个微量新生物碱,经光谱和化学方法证明为8-乙酰嘟啦碱-(8-acetytdolaconine,Ⅰ),同时分离得到2个已知生物碱;即嘟啦碱(Ⅱ)和aconosine,(Ⅲ),后者是该植物的主要生物碱成分,在非生物碱部分还分离得到β-谷甾醇,棕榈酸和香豆酸。     

狭叶山胡椒根中的生物碱成分

目的研究狭叶山胡椒根中的生物碱成分。方法采用硅胶、MCI-DHP-20P反相填料柱色谱进行分离，通过MS，¹H NMR，¹³C NMR，HMQC，HMBC等波谱方法进行结构鉴定，同时采用半合成方法确证结构。结果共分离得到7个生物碱类化合物，分别为樟苍碱(I)、N-甲基樟苍碱(II)、波尔定(III)、异波尔定(IV)、降波尔定(V)、magnocurarine (VI)、N-乙氧甲酰基樟苍碱(VII)，通过合成方法验证了N-乙氧甲酰基樟苍碱的化学结构。结论所有化合物皆首次从该植物中分得，其中N-乙氧甲酰基樟苍碱为首次从自然界分离得到。     

猪毛菜中一新生物碱

研究猪毛菜中的生物碱。采用各种色谱技术进行分离，通过理化性质及波谱分析进行结构鉴定。从猪毛菜地上部分的95%乙醇提取物中分离得到4个酰胺类生物碱，其化学结构分别确定为N-反式阿魏酰基-3-甲基多巴胺(1)、3-［4-(β-D-吡喃葡糖氧基)-3-甲氧基苯基］-N-［2-(4-羟基-3-甲氧基苯基)乙基］-2-丙胺(2)，猪毛菜碱A(3)，猪毛菜碱B(4)。化合物4为一新化合物，命名为猪毛菜碱B，化合物2为首次从该属植物中分离得到。     

Two new metabolites from the mangrove endophytic fungus No. 2524

Two new metabolites, the cyclo-(l-Phe-l-Leu¹-l-Leu²-l-Leu³-l-Ile) (1) and (3S,4R)-dihydroxy-(6S)-undecyl-α-pyranone (2) have been produced by the endophytic fungus no. 2524 isolated from a seed of mangrove Avicennia marina in Hong Kong. The structures have been elucidated by spectra including two-dimensional NMR, ESI tandem mass spectrometry and CD. These compounds show no activity toward human cancer cell lines Bel-7402, NCI-4460 and the normal human cell lines L-02.     

A new flavan-3-ol from Artocarpus nitidus subsp. lingnanensis

Further investigation on the stems of Artocarpus nitidus subsp. lingnanensis led to the isolation and characterization of a new flavan-3-ol, named artoflavanocoumarin (1), along with three known compounds (+)-catechin (2), (+)-afzelechin 3-O-α-l-rhamnoside (3), and (+)-catechin 3-O-α-l-rhamnoside (4). Their structures were elucidated on the basis of spectroscopic data.     

Alkaloids from Clematis manshurica Rupr.

Three new alkaloids together with two known compounds have been isolated from the roots of Clematis manshurica. On the basis of their spectroscopic and chemical evidence, the new compounds were elucidated as methyl 7-ethoxy-3-indolecarbonate (2), methyl 7-O-α-l-rhamnopyranosyl-(1 → 6)-β-d-glucopyranosyl 3-indolecarbonate (3) and α-l-rhamnopyranosyl-(1 → 6)-β-d-glucopyranosyl 3-indolecarbonate (4).     

l-硝基芘在离体灌流肺中的生物转化及消除：大鼠以苯巴比妥、β-萘黄酮苯并蒽或其混合物

将150μg l-硝基芘（l-NP）气管内或血管内给药后，对大鼠离体肺进行灌流，定时自灌流液中取样，以HPLC和GC-MS测定并鉴定灌流液中未变的l-NP及代谢物。经鉴定代谢物为单羟基硝基芘和二羟基硝基芘。两种途径给药后，l-NP在灌流液中的浓度—时间数据符合一室药代动力学模型。预先以β-萘黄酮，苯并蒽或苯巴比妥和β-萘黄酮的混合物处理后的大鼠，肺灌流结果表明，显著降低l-NP的平均保留时间（MRT），促进l-NP的生物转化和气管给药后的吸收。以苯巴比妥预处理后的大鼠肺则对l-NP的药代动力学参数无显著影响。     

毛叶轮环藤生物碱的肌松药理作用研究

本文研究了从毛叶轮环藤分离到的汉防己甲素,高阿洛莫林碱,左旋箭毒碱和异谷树碱的肌松作用。家免垂头试验表明,他们的碘甲烷盐均有肌松作用,但以左旋箭毒碱和高阿洛莫林碱的作用较强。将左旋箭毒碱制备成二甲基左旋箭毒碱氯甲烷盐衍生物后,肌松作用增强1.5～3倍。对小鼠,家免,猫和狗的肌松作用比右旋筒箭毒碱约强0.5～4倍,对大鼠的肌松作用强度与右旋筒箭毒碱相当。左旋箭毒碱,二甲基左旋箭毒碱及高阿洛莫林碱的作用均类似于右旋筒箭毒碱,属于非去极化型肌松剂。给麻醉猫、狗快速静注2～3倍肌松剂量的左旋箭毒碱或二甲基左旋箭毒碱,有降压和组胺释放作用。对猫颈交感神经节无抑制作用。对离体家兔及豚鼠廻肠的阿托品样作用很弱。家兔连续静注达40～50倍垂头剂量,对心电图无明显影响,静注5～10倍垂头剂量,48-72小时后剖杀检查,未见对内脏器官有明显病理损害。小鼠及大鼠试验结果表明二甲基左旋箭毒碱的治疗指数高于右旋筒箭毒碱。     

Generation of microbubbles for diagnostic and therapeutic applications using a novel device

Developments in both diagnostic and therapeutic applications of microbubbles have greatly increased the need for more advanced preparation technologies which provide a well-defined, narrow microbubble size-distribution. In this paper, we demonstrate the use of a new device, consisting of a T-junction whose outlet capillary is fitted with an electrohydrodynamic spraying arrangement, to prepare phospholipid-coated air microbubbles, making significant advances in controlling and decreasing the size and size-distribution, and increasing the stability/lifetime of the bubbles prepared. The microbubbles were characterised via optical microscopy to determine the relationship between the size-distribution obtained and the process variables, specifically the flow rates of the phospholipid suspension and air (Q_l and Q_g), and the applied voltage (V). The formation of microbubbles in the device was also studied using high-speed photography. For the range of parameters investigated, the bubble diameter was found to scale with the product of the flow rate ratio (Q_l/Q_g) and the applied voltage, with a consistent bubble diameter of 5.1 ± 2 μm being obtained at Q_l/Q_g = 1.7 and V = 18 kV. The bubbles prepared using this method were found to be stable for at least 2 h at ambient temperature and pressure.     

毛叶轮环藤肌松有效成分的研究

毛叶轮环藤[Cyclea barbata(Wall)Miers]为防己科轮环藤属植物,在海南岛有野生。其根俗称“银不换”。主治喉炎、腹痛及牙痛,并用于跌打损伤。中国人民解放军第一八七医院首先发现并经临床试验,证明其总生物碱的碘甲烷盐,具有明显的横纹肌松弛作用。 国外,从该植物中,已分得十二种生物碱。本文报道从“银不换”的总生物碱中,除分得     

Functional Importance of Nucleus Accumbens Noradrenaline in the Rat

Abstract: l-Noradrenaline·HCl (l-NA), d-noradrenaline·HCl (d-NA) and dopamine·HCL (DA) were locally applied in the nucleus accumbens of awake rats. When the animals were observed in a dark open field arena it was found that low doses of l-NA or DA produced suppression of ambulatory activity followed by an increase in the activity at higher doses. l-NA was more potent than DA in producing these effects and about 4 times higher doses of DA were required to produce the same effect. d-NA was not without effects but was less efficient than DA.     

Long-term treatment of l-3-n-butylphthalide attenuated neurodegenerative changes in aged rats

It is shown that l-3-n-butylphthalide (l-NBP), the isomer of dl-NBP (racemic 3-n-butylphthalide, a new anti-cerebral ischemic agent) significantly attenuated cerebral hypoperfusion-induced learning dysfunction and brain damage in rats. In the present study, l-NBP (10 and 30 mg/kg) long-term (3-month) treatment of aged rat (21-month-old) significantly improved the learning and memory capability measured by the Morris water maze test. Hematoxylin–eosin-stained slices showed that both l-NBP at 30 mg/kg, and memantine as control at 20 mg/kg, attenuated the neurodegenerative changes in aged rats. l-NBP treatment significantly increased the choline acetyltransferase activity and dose-dependently decreased the acetylcholinesterases activity in the hippocampus of aged rats. The immunohistological study demonstrated that expressions of β-secretase and hyperphosphorylated tau protein were significantly increased in the hippocampus CA1 subfield and parietal cortex in aged rats. However, they were decreased significantly by treatment of l-NBP and memantine for 3 months. Our results indicated that long-term treatment with l-NBP might prevent age-related neurodegenerative changes by modulation of cholinergic system, reduction of phosphorylated tau and maintain structure and morphology of neurons. Therefore, l-NBP might be a potential drug for treatment of senile dementia.     

Levo-tetrahydropalmatine attenuates cocaine self-administration and cocaine-induced reinstatement in rats

Rationale Levo-tetrahydropalmatine (l-THP) is an alkaloid constituent of plants from the botanical genera Corydalis and Stephania and is contained in many traditional Chinese herbal preparations. In addition to its low-affinity antagonism of D2 dopamine (DA) receptors, we report that l-THP functions as a higher-affinity antagonist at D1 DA receptors and interacts with D3 DA receptors, suggesting that it may be effective for the treatment of drug addiction. Accordingly, l-THP has been reported to reduce heroin craving and relapse in recovering addicts. Objective This study investigated the effects of l-THP (3.75, 7.5, and 15.0 mg/kg, i.p.) on cocaine self-administration (SA) and cocaine-induced reinstatement. Materials and methods Rats were trained to self-administer cocaine and food by pressing separate response levers during sessions consisting of a multiple schedule of alternating 30-min FR4 cocaine and 15-min FR4 food reinforcement. During the cocaine components of each session, the available cocaine dose varied such that rats had access to low and high dose ranges in varying sequence on alternating days. After SA, cocaine-reinforced responding was extinguished, and effects of l-THP on cocaine-induced reinstatement (10 mg/kg, i.p.) were examined. Results l-THP produced a rightward and downward shift in the dose–response curve for cocaine SA and attenuated cocaine-induced reinstatement. l-THP also reduced food-reinforced responding and locomotor activity. However, reductions in cocaine SA were found at doses that failed to alter food-reinforced responding, and significant effects were not observed on food responding during reinstatement. Conclusions These findings suggest that l-THP is potentially useful for treating cocaine addiction. Electronic supplementary material The online version of this article (doi:) contains supplementary material, which is available to authorized users.