翁布中黄酮类化合物的体外抗氧化活性研究

目的 研究藏药翁布中11种黄酮类化合物的体外抗氧化作用.方法 采用DPPH自由基清除活性、FRAP总抗氧化能力、ABTS总抗氧化能力和酪氨酸酶活性抑制等4种实验方法对11种黄酮化合物的自由基清除能力及抗氧化活性进行体外评价.结果 3,5,4'-三羟基-7-甲氧基黄酮、3,5,7-三羟基-4'-甲氧基黄酮、柽柳素、山奈酚、槲皮苷对DPPH自由基的清除较强(半数抑制浓度IC50低于维生素C);3,5,4 '-三羟基-7,3'-二甲氧基黄酮、山奈酚、5,7,4'-三羟基-3-O-β-D-葡萄糖醛酸、5,7,3',4'-四羟基-3-O-β-D-葡萄糖醛酸的ABTS总抗氧化值相对于Trolox标准溶液＞0.01 mmol· L-1;FRAP法测得11种黄酮类化合物具有总抗氧化能力,但均低于阳性对照Trolox;11种黄酮类化合物对酪氨酸酶活性具有抑制活性,但IC50均高于阳性对照曲酸.结论 11种黄酮类化合物中,3,5,4'-三羟基-7-甲氧基黄酮、3,5,7-三羟基-4'-甲氧基黄酮、柽柳素、山奈酚、槲皮苷具有较强的抗氧化活性.     

何首乌及首乌藤抗氧化活性研究

目的评价何首乌和首乌藤体外总抗氧化活性。方法采用清除二苯代苦味酰基（DPPH）自由基、清除〔2,2′-连氨-（3-乙基苯并噻唑啉-6-磺酸）二氨盐〕（ABTS）自由基和铁离子还原/抗氧化能力（FRAP）测定法。结果将测定结果与水溶性维生素E（6-羟基-2,5,7,8-四甲基苯并二氢吡喃-2-羧酸,Trolox）及阳性对照二丁基羟基甲苯（BHT）进行比较,发现何首乌的乙酸乙酯和甲醇提取物具有较强的清除DPPH自由基、清除ABTS自由基及还原Fe3＋的能力。结论何首乌的总的抗氧化活性好于首乌藤。在6种提取物中,何首乌的乙酸乙酯提取物抗氧化能力最强。同一药用部位,甲醇和乙酸乙酯提取物的抗氧化活性好于石油醚提取物。3种方法之间有很好的相关性,以DPPH法与ABTS法相关性最好（R=0.996）。     

肿节风中抗氧化活性成分的研究

目的 研究中药肿节风[Sarcandra glabra (Thunb. ) Nakai.]中的抗氧化活性成分。方法 利用聚酰胺、Sephadex LH-20、Lipophilic Sephadex LH-20柱色谱以及制备型HPLC等手段进行分离,根据化合物的理化性质和波谱数据鉴定结构;采用比色法测定肿节风总多酚部位及各单体化合物对DPPH自由基的清除能力,进行抗氧化活性筛选。结果 从肿节风中分离得到2个黄酮苷类和4个有机酸类化合物,分别鉴定为朝藿定C (1)、槲皮素-3-O-鼠李糖苷 (2)、3-甲氧基-4-羟基苯甲酸 (3)、迷迭香酸-4-O-β-D-葡萄糖苷 (4)、丁香酸 (5)和对羟基苯甲酸 (6)。 结论 6个化合物均为首次从该属植物中分离得到,抗氧化活性筛选结果表明,多酚类部位为肿节风的抗氧化活性部位,化合物 2、4、5具有较强的抗氧化活性。     

金钗石斛中的菲类和木脂素类成分及其抗氧化作用

研究金钗石斛茎中的抗氧化活性成分，并探讨它们的构效关系。综合运用现代色谱学和光谱学方法对金钗石斛60％乙醇提取物中的化学成分进行分离鉴定，采用DPPH自由基清除法评价化合物的抗氧化活性。从金钗石斛的活性部位中分离得到5个菲类化合物和4个木脂素类化合物，它们的结构鉴定为流苏菲（1），毛兰菲（2），4-甲氧基菲-2，7-二醇（3），2,5-二羟基-4，9-二甲氧基菲（4），3，7-二羟基-2，4-二甲氧基菲（5），丁香脂素（6），松脂素（7），5′-甲氧基松脂素（8），鹅掌揪树脂醇-A（9）。化合物2和6对DPPH自由基清除活性强于Vc；化合物3，4，5，7，8和9的活性弱于Vc，但强于BHT。所有化合物均为首次报道从金钗石斛中分离得到，化合物3，4和9为首次报道从石斛属植物中分离得到。在DPPH自由基清除法中，酚羟基的邻位存在具有供电作用的甲氧基时对菲类和木脂素类化合物的抗氧化活性具有积极的作用。     

头状蓼提取物体外抗氧化活性研究

目的:研究头状蓼提取物的体外抗氧化活性。方法:以脂溶性维生素E及二丁基羟基甲苯(BHT)作对照,采用清除二苯代苦味酰基(DPPH)自由基、清除[2,2′-连氨-(3-乙基苯并噻唑啉-6-磺酸)二氨盐](ABTS)自由基和铁离子(Fe3+)还原/抗氧化能力(FRAP)测定法检测头状蓼石油醚、乙酸乙酯、甲醇提取物的体外抗氧化活性。结果:与头状蓼石油醚、乙酸乙酯提取物比较,头状蓼甲醇提取物清除DPPH自由基、清除ABTS自由基及还原Fe3+的能力较强。结论:头状蓼甲醇提取物具有较好的体外抗氧化活性。3种方法中,DPPH方法和ABTS方法相关性最高。     

肿节风中咖啡酸衍生物及抗氧化活性

目的对肿节风中抗氧化活性成份进行分离鉴定和抗氧化活性测定。方法利用各种色谱技术进行分离纯化,利用波谱数据鉴定结构,采用DPPH自由基清除率法测定抗氧化活性。结果从肿节风中进一步得到4个化合物,分别鉴定为:4-O-咖啡酰基-奎宁酸(4-O-caffeoylquinic acid,1),3-O-咖啡酰基-奎宁酸(3-O-caffeoylquinic acid,2),4-O-咖啡酰基-奎宁酸甲酯(4-O-caffeoylquinic acidmethyl ester,3),3-O-咖啡酰基-奎宁酸甲酯(3-O-caffeoylquinic acid methyl ester,4),各化合物显示了不同强度的抗氧化活性。结论这4个化合物均为首次从该属中分离得到,各咖啡酸衍生物、丹参素衍生物,具有邻二酚羟基的黄酮类化合物是肿节风抗氧化活性部位的物质基础。     

化合物3,4,5-三羟基-N-[2-(4-羟基苯基)乙基]苯甲酰胺的抗氧化活性

目的对化合物3,4,5-三羟基-N-[2-(4-羟基苯基)乙基]苯甲酰胺(3,4,5-trihydroxy-N-[2-(4-hydroxyphenyl)ethyl]-benzamide,THHEB)的抗氧化活性进行研究。方法通过测定对有机自由基1,1-二苯基苦基苯肼(1,1-diphenyl-2-picrylhydrazyl,DPPH)的清除能力、6-羟基-2,5,7,8-四甲基苯并二氢吡喃-2-羧酸(6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid,Trolox)当量抗氧化能力(trolox-equivalent antioxidant capacity assay,TEAC),测定超氧自由基的清除活性实验、脂质过氧化法以及羟基自由基诱导DNA损伤的方法评价THHEB的抗氧化活性。结果5种方法检测结果均显示,THHEB具有很强的清除自由基的活性。其中,THHEB对稳定自由基DPPH和超氧自由基的清除能力超过抗坏血酸的相应活性,其IC50值分别为22.8、2.5μmol.L-1。用TEAC方法测定THHEB总的抗氧化能力大约为0.6,也比L-抗坏血酸相应值高。脂质过氧化法测定的THHEB活性要弱于著名的抗氧化化合物2,6-二叔基对甲苯酚(butylated hydroxytoluene,BHT)。此外,非常小浓度比如4μmo.lL-1的THHEB对羟基自由基导致的pBR322 DNA链断裂具有显著的保护作用。结论THHEB具有很强的清除自由基的活性。     

黔产苎麻根中有机酸类化学成分及抗氧化活性研究

目的研究黔产苎麻根中有机酸类的化学成分,并对各化学成分进行活性评估。方法苎麻根用95%乙醇提取后,提取物分别用石油醚、乙酸乙酯、正丁醇萃取,对乙酸乙酯萃取物采用各种色谱分离技术进行分离,并对所得各化学成分进行纯化,通过各化学成分理化性质和波谱分析鉴定单体化学结构,对各成分通过清除2,2-二苯代苦味肼基自由基(DPPH)作用实验,确定各成分的抗氧化活性。结果分离和鉴定得到7个化合物:对羟基苯甲酸、阿魏酸、原儿茶酸、焦性没食子酸、5-咖啡酰奎宁酸、绿原酸及咖啡酸。各成分通过抗氧化活性部位筛选,IC50值分别为32,57,38,54,39,76,58μg·m L^-1。结论化合物1-5为首次从该植物中分离得到,这7个化合物均具有一定的抗氧化活性。     

头花蓼抗氧化活性研究

目的:研究头花蓼抗氧化活性。方法:分别用石油醚、乙酸乙酯、甲醇提取头花蓼,用清除DPPH自由基、清除ABTS自由基和铁离子还原/抗氧化能力测定法,对头花蓼体外总抗氧化活性进行评价,并与6-羟基-2,5,7,8-四甲基苯并二氢吡喃-2-羧酸及阳性对照丁基羟基茴香醚(BHA)、二丁基羟基甲苯(BHT)比较。结果:头花蓼有较好的体外抗氧化活性。其甲醇提取物具有很强的清除DPPH自由基、ABTS自由基及还原Fe3+的能力,总抗氧化能力远远超过BHT的作用。结论:在3种提取物中,头花蓼甲醇提取物具有最高的抗氧化能力,乙酸乙酯提取物次之。3种方法中,DPPH方法和ABTS方法相关性(r=0.9917)最高。     

肉桂酸衍生物清除羟基自由基活性研究

目的:比较研究咖啡酸、氯原酸、连翘酯苷、阿魏酸、对-羟基香豆酸、邻-羟基香豆酸、间-羟基香豆酸、肉桂酸等中草药有效成分对HO·的清除能力.方法:利用邻菲罗啉化学发光体系.结果:咖啡酸、氯原酸、连翘酯苷、阿魏酸对HO·具有较强的清除能力,对-羟基香豆酸、邻-羟基香豆酸、间-羟基香豆酸对HO·的清除能力较弱,而肉桂酸对HO·的清除作用很小.结论:肉桂酸衍生物的酚羟基邻位有含孤对电子的杂原子取代基(-OH,-OCH3)时,清除HO·的能力可被提高;在-CHCHCOOH的对位含有酚羟基的化合物比在邻位或间位含有酚羟基化合物的活性强.     

全反式维甲酸对小鼠神经系统作用的一般药理试验研究

目的 通过小鼠自主活动实验、小鼠协调运动实验、与阈下剂量戊巴比妥钠协同作用实验考察全反式维甲酸（all-trans-retinoic acid,ATRA）对小鼠神经系统的影响。方法 ICR小鼠,♀♂各半,按体质量随机分为溶剂对照组、250.0,50.0,10.0 mg·kg^-1 ATRA组,各组小鼠禁食（不禁水）12 h后分别灌胃给予相应剂量ATRA,给药体积为0.02 mL·g^-1。小鼠自主活动实验,测定给药前及给药后6,120,180 min小鼠在5 min内的活动次数。小鼠协调运动试验,测定给药后120 min小鼠在转棒上的停留时间。与阈下剂量戊巴比妥钠协同作用试验,给药后120 min腹腔注射戊巴比妥钠阈下剂量,观察睡眠小鼠的例数。结果 ATRA 250.0 mg·kg^-1作用120 min后,小鼠自主活动次数显著减少,给予50.0,10.0 mg·kg^-1 ATRA 120,180 min后均可见小鼠自主活动减少的趋势;而250.0,50.0及10.0 mg·kg^-1 ATRA对小鼠的协调运动均无明显影响,与阈下剂量的戊巴比妥钠无协同作用。结论 ATRA能减少小鼠自主活动次数,对协调运动无明显影响,与阈下剂量戊巴比妥钠无协同作用。     

Landolphia owariensis leaf extracts reduce parasitemia in Plasmodium berghei-infected mice

Context Landolphia owariensis P. Beauv. (Apocyanaceae) leaf is used in southeast Nigeria to treat malaria.

Objective This study evaluated the antiplasmodial activity of L. owariensis leaf extract and fractions, also the phytoconstituents were standardized and analyzed.

Methods The effects of daily, oral administrations of 200, 400 and 800?mg/kg of L. owariensis leaf extract (LOE), its hexane (LOHF), ethyl acetate (LOEF) and methanol (LOMF) fractions on early, established and residual infections in Plasmodium berghei-infected albino mice were evaluated in vivo. The extract and fractions were subjected to phytochemical analysis and HPLC fingerprinting, and the acute toxicity of LOE was evaluated.

Results The extract and fractions elicited 29–86, 18–95 and 75–96% significant (p?<?0.001) suppression of parasitemia in early, established and residual infections, respectively. The ED₅₀ values for suppressive activity of LOE, LOHF, LOEF and LOMF were 266.56, 514.93, 392.95 and 165.70?mg/kg, respectively. The post-day 30-survival index was 16.7–50, 16.7, 16.7–66.7 and 50–83.3% for LOE, LOHF, LOEF, and LOMF, respectively. Extract-treated mice significantly (p?<?0.001) gained weight and had reduced mortality compared with negative control (untreated) mice. An oral LD₅₀ value >5000?mg/kg in mice was established for LOE. The LOMF showed the greatest antiplasmodial activity in all the models, suggesting that the antimalarial activity of the plant may be attributed to alkaloids, flavonoids, saponins and tannins present in the fraction.

Conclusion Results demonstrate the antiplasmodial activity of L. owariensis leaf, and provide a pharmacological rationale for its ethnomedicinal use as an antimalarial agent.     

国产替考拉宁体内外抗菌作用研究

目的：为了评价国产替考拉宁对510株临分离菌的体外抗菌活性，并与进口产品替考拉宁及万古霉素进行比较，方法：采用琼脂二倍稀释法和试管二倍稀释法测定药物的最低抑菌浓度（MIC）及最低杀菌浓度（MBC）。结果：国产替考拉宁的抗菌活性与万古霉素相似或略强，其对MRSDA和MSSA的MIC50分别为4、1mg/L，对MRSE和MSSE的MIC50分别为1、0.5mg/L。对所试大多数菌株MIC50为0．06－4mg/L，与进口的替考拉宁的抗菌活性无显著差异，替考拉宁在2－4MIC浓度时呈杀菌作用，替考拉宁的MIC值随接种菌量增加升高2－8倍，受PH和血清浓度影响不大，体内保护试验表明，替考拉宁静脉和皮下给药对金葡球菌981925、肺炎链球菌98135和肠球菌9804所致小鼠全身感染的ED50分别为0．59、0．38、0．17mg/kg（静脉注射）和1．08、0．87、0．36mg/kg（皮下注射）。其体内抗菌作用比万古霉素中6－12倍以上。     

初探胸腺肽的活性与其含量的相关性

目的　探索胸腺肽的活性与其含量是否存在完全正相关性。方法　将不同含量的胸腺肽,用脱E受体法测定其活性。结果　胸腺肽的活性与其含量有一定的相关性,其含量愈高,活性愈高,但没有正比关系。结论　胸腺肽的活性与其肽的含量不完全正相关(r =0 5 9)。     

Antinociceptive activity of steroid alkaloids isolated from Solanum trilobatum Linn.

Solasodine (1) was isolated for the first time from the roots of Solanum trilobatum Linn., a member of the Solanaceae, and assessed for its presumed antinociceptive activity using several experimental murine models, viz. the writhing, formalin, and hot plate tests. When used at doses of 2, 4, and 8 mg/kg, this steroidal alkaloid caused a significant and dose-dependent decrease in the nociception induced by an intraperitoneal injection of acetic acid (p < 0.001). It also led to a significant reduction of the painful sensation caused by formalin in both phases of the formalin test (p < 0.001). Furthermore, the alkaloid produced a significant increase in the reaction time in the hot plate test (p < 0.001). These results suggest that solasodine elicited antinociceptive activity through both central and peripheral mechanisms.     

Comparison of the effects of anticonvulsant drugs with diverse mechanisms of action in the formalin test in rats

The purpose of the present studies was to compare anticonvulsant drugs with diverse mechanisms of action in a persistent pain model, the formalin test. In addition, the anticonvulsant effects of the compounds were determined in the threshold electroshock tonic seizure test and the 6-Hz limbic seizure test. The effects of the compounds were also determined on locomotor activity. Carbamazepine, oxcarbazepine, lamotrigine, gabapentin and ethosuximide all produced statistically significant analgesic effects in the formalin test whereas phenytoin, topiramate, zonisamide, phenobarbital, tiagabine, valproate and levetiracetam did not. All compounds were anticonvulsant. In addition, morphine and phenobarbital increased locomotor activity while ethosuximide had no effect and all other compounds decreased locomotor activity. For those compounds that were analgesic, the doses required to produce analgesia were larger in magnitude than the anticonvulsant ED50 values in the threshold electroshock and 6-Hz tests, as well as larger than doses that altered locomotor activity. The present results demonstrate that the anticonvulsant and analgesic effects of clinically used antiepileptic drugs do not necessarily correlate and therefore suggest that the anticonvulsant and analgesic efficacy of these drugs may be due to different pharmacologic mechanisms.     

In vivo antiplasmodial activities of aqueous extract of Bridelia ferruginea stem bark against Plasmodium berghei berghei in mice

Context: Bridelia ferruginea Benth (Euphorbiaceae) is an indigenous medicinal plant in Nigeria. It is usually a gnarled shrub which sometimes reaches the size of a tree in suitable condition. Decoctions of parts of this plant have been employed in ethno medicine in many parts of Africa for treatment of many ailments including malaria fever.

Objective: In vivo antiplasmodial activity of aqueous stem bark extract of BF was investigated against Plasmodium berghei-infected mice.

Materials and methods: The aqueous stem bark extract of BF (100–400?mg/kg) was administered orally to P. berghei-infected mice in both early and established models of antiplasmodial studies.

Results: The extract exhibited significant (p?<?0.05) antiplasmodial activity in early and established infection tests with a considerable mean survival time comparable to that of chloroquine, 10?mg/kg. The oral LD₅₀ obtained was greater than 5000?mg/kg in mice.

Discussion and conclusions: The findings show that aqueous stem bark extract of Bridelia ferruginea possesses considerable antiplasmodial activity which can be developed in malaria therapy.     

The effects of ifenprodil on the activity of antidepressant drugs in the forced swim test in mice

BackgroundAccording to reports in the literature, more than 30% of depressive patients fail to achieve remission. Therapy with the conventional antidepressant drugs may induce the serious adverse reactions. Moreover, its benefits may be seen at least 2–4 weeks after the first dose. Therefore, the alternative strategies for prevention and treatment of depression are sought. The main aim of our study was to assess the effects of ifenprodil given at a non-active dose (10 mg/kg) on the activity of antidepressant agents from diverse pharmacological groups.MethodsThe antidepressant-like effect was assessed by the forced swim test in mice.ResultsIfenprodil potentiated the antidepressant-like effect of imipramine (15 mg/kg) and fluoxetine (5 mg/kg) while did not reduce the immobility time of animals which simultaneously received reboxetine (2.5 mg/kg) or tianeptine (15 mg/kg).ConclusionThe concomitant administration of certain commonly prescribed antidepressant drugs that affect the serotonergic neurotransmission (i.e., typical tricyclic antidepressants and selective serotonin reuptake inhibitors) with a negative modulator selectively binding to the GluN1/N2B subunits of the NMDA receptor complex (i.e., ifenprodil) may induce a more pronounced antidepressant-like effect than monotherapy. However, these findings still need to be confirmed in further experiments.     

地红霉素的AMES试验

目的:检测地红霉素的致突变活性.方法:采用组氨酸营养缺陷型鼠伤寒沙门杆菌TA系列4个菌株.试验在有和无代谢活化剂下对受试药品0.08～50μg·皿-1共5个浓度组进行测试.结果:各菌株回复突变菌落数未见明显增多.结论:地红霉素无致突变活性.     

Monitoring the rivers Rhine and Meuse in the Netherlands for mutagenic activity using the Ames test in combination with rat or fish liver homogenates

Organic concentrates of water of the rivers Rhine and Meuse and a control lake were tested for mulagenic activity with the Ames Salmonella/microsome assay at 3-mth intervals for more than 1 yr. The river samples were concentrated by adsorption on XAD (10³-fold) followed by elution with DMSO.Using strain TA 98, all Rhine water samples except one were found to contain both direct and indirect mutagens. No significant mutagenic activity was detected in the lake samples and most of the river Meuse samples. None of the samples were shown to be mutagenic when tested with strains TA 100 or TA 1535.On examining one Rhine location more frequently, the mutagenic activity was found to be persistent and to vary about 5- to 6-fold during one year.Finally, liver homogenates of bream (Abramis brama) from these waters were compared with the standard rat liver S-9 with regard to their ability to activate the indirect mutagens present in the water concentrates. Compared with the rat liver homogenates, the liver homogenates of Rhine fish were found to be equally active and those of Meuse fish somewhat less. No metabolic activation was observed with liver homogenates of the lake fish.