黄荆叶不同溶剂提取物的抗炎镇痛作用研究

目的:观察黄荆叶不同溶剂(氯仿、乙酸乙酯、水)提取部分的抗炎、镇痛作用.方法:采用二甲苯诱导小鼠耳廓肿胀和角叉菜胶诱导大鼠足肿胀建立炎症模型观察黄荆叶不同溶剂提取物的抗炎作用;采用扭体法和热板法观察黄荆叶不同溶剂提取物的镇痛作用.结果:乙酸乙酯提取部分(16g·kg<'-1>、8g·kg<'-1>)对二甲苯诱导的小鼠耳肿胀抑制作用最为显著(P<0.01);氯仿提取部分(16g·kg<'-1>)能明显抑制角义菜胶诱导的大鼠足肿胀(P<0.01).对热刺激和醋酸刺激引起的小鼠疼痛,乙酸乙酯提取部分(16g.k<'-1>、8g.<'-1>)和水提物各剂量组具有显著的镇痛作用(P<0.01),氯仿提取部分各剂量组镇痛作用不明显(P>0.05).结论:黄荆叶不同溶剂提取部位的抗炎镇痛作用有差异,乙酸乙酯提取物具有明显的抗炎和镇痛作用.而氯仿提取物抗炎作用较强,水提取物的镇痛作用较强.     

猕猴桃根抗肿瘤作用研究

目的评价猕猴桃根提取物的体外、内抗肿瘤活性。方法猕猴桃根活性成分的分离、纯化采用传统的天然产物化学方法,猕猴桃根先用甲醇回流提取,然后用乙酸乙酯、氯仿、正丁醇萃取。不同组分对体外培养的肿瘤细胞增殖的作用采用磺酰罗丹明B方法;猕猴桃根的体内抗肿瘤作用采用小鼠肿瘤和人肿瘤裸小鼠移植瘤模型评价。结果氯仿提取物对肿瘤细胞增殖抑制作用最强,甲醇提取物次之。体内实验证实氯仿提取物有效地抑制小鼠肝癌模型和人肝癌裸小鼠移植瘤模型的生长,抑制率大概在38.0%。结论猕猴桃根提取物有一定的抗肿瘤作用;其活性成分主要存在于极性较小的组分。     

黄荆子不同溶剂提取物的抗炎镇痛作用

目的:观察黄荆子不同溶剂(氯仿、醋酸乙酯、水)提取部分的抗炎、镇痛作用。方法:采用二甲苯诱导小鼠耳郭肿胀和角叉菜胶诱导大鼠足肿胀建立炎症模型观察黄荆子不同溶剂提取物的抗炎作用;采用扭体法和热板法观察黄荆子不同溶剂提取物的镇痛作用。结果:氯仿提取部分(16,8 g.kg-1)对二甲苯诱导的小鼠耳肿胀抑制作用最为显著(P<0.01);氯仿提取部分(16 g.kg-1)能明显抑制角叉菜胶诱导的大鼠足肿胀(P<0.01)。对热和醋酸刺激引起的小鼠疼痛,水提物具有显著的镇痛作用(P<0.01),氯仿提取部分各剂量组镇痛作用不明显(P>0.05)。结论:黄荆子不同溶剂提取部位的抗炎镇痛作用有差异,氯仿提取物抗炎作用较强,水提取物的镇痛作用较强。     

天麻对小鼠脑内单胺氧化酶活性的影响

目的：考察天麻提取物对D－半乳糖所致亚急性损伤小鼠脑内单胺氧化酶B（MAO－B）活性的影响。方法：采用D－半乳糖诱导小鼠脑内MAO－B活性升高，小鼠腹腔注射（ip)天麻提取物30d后，测定其脑内MAO－B的活性。结果：小鼠ip天麻提取物0．25，0．5，1．0g.kg^-1 30d后，均能显著降低MAO－B活性，与D－半乳糖模型组比较，差异有极显著性（P＜0．01），结论：说明天麻提取物能抑制D－半乳糖所致亚急性损伤小鼠脑内MAO－B的活性，减缓生化损害。     

黄芩抗乙酰胆碱酯酶活性部位的RRLC-DAD-ESI-MS/MS分析

目的：筛选黄芩体外抑制乙酰胆碱酯酶（AChE）的活性部位，并对其化学成分进行分析。方法：黄芩提取物经反相C₁₈填料进行固相萃取（SPE）制备不同浓度甲醇醇梯度洗脱部位，以体外抑制AChE能力评价其抗阿尔茨海默症（AD）作用，采用高分离快速液相色谱-质谱联用技术（RRLC-MS/MS）对黄芩抑制AChE活性部位化学成分进行分析。结果：黄芩提取物的50%甲醇洗脱部位的AChE抑制活性明显强于其他洗脱部位并存在明显的量效关系，为其体外抑制的活性部位，经液质联用分析共鉴定出15种化合物。结论：黄芩具有体外抑制AChE活性，其主要有效部位为50%甲醇洗脱部位，其主要有效成分为黄芩苷为代表的黄酮类成分。     

莲雄蕊提取物和黄酮类化合物具抗氧化活性

从莲Nelumbo nucifera Gaertn.的雄蕊中分离的提取物和黄酮类化合物可抑制活性氧(ROS)的形成,抑制DPPH和脂质过氧化离子的活性,防治氧化应激引起的疾病。莲的雄蕊用水、甲醇、丁醇等极性溶剂或醋酸乙酯、正己烷、二氯甲烷或氯仿等非极性溶剂提取得到具抗氧化作用的粗提物。莲雄蕊提取物和黄酮类化合物具抗氧化活性     

青果抗人免疫缺陷病毒活性部位的筛选研究

目的:筛选青果中作用于人免疫缺陷病毒(HIV)gp41抑制HIV-1与靶细胞融合的活性部位。方法:分别用水蒸气蒸馏法、溶剂梯度萃取法获得青果挥发油、青果10%水提液的石油醚、氯仿、乙酸乙酯、正丁醇萃取部位,用酶联免疫吸附(ELISA)法检测以上各部位抑制HIV-1与靶细胞融合的活性;测定活性部位中鞣质的含量,以确定青果中非鞣质成分与活性的关系。结果:青果10%水提液的石油醚、氯仿、乙酸乙酯萃取部位均有较强的抑制HIV-1与靶细胞融合的活性,其半数抑制浓度分别为(3.97±0.38)、(26.78±0.47)、(6.80±0.10)μg.mL-1;各部位中鞣质的含量分别为8.0%、9.6%、32%。结论:青果抑制HIV与靶细胞融合的活性部位为水提液的石油醚、氯仿和乙酸乙酯萃取部位,其中石油醚萃取部位活性最强,且很可能含有非鞣质类的活性物质。     

10株东海海水来源真菌的抗肿瘤活性筛选研究

目的运用MTT法抗肿瘤生物活性模型对来源于东海海水的10株真菌提取物进行生物活性筛选。方法对10株海水来源真菌的发酵液乙酸乙酯提取物进行体外抗肿瘤活性(MTT法)筛选研究评估。结果菌株12010104、12010103、12010101和08010101的发酵液提取物对PC12肿瘤细胞的细胞毒性较强,当浓度为200μg·mL-1时抑制率可达70%以上。菌株12010104、12010109、及08010101的发酵液提取对HepG2肿瘤细胞物表现出较强的抑制活性,抑制率在浓度为200μg·mL-1时可达85%以上,真菌12010101的抑制活性次之,在同浓度为77%。而菌株12010104、12010101及08010101在浓度为100μg·mL-1时对U937肿瘤细胞具有较强的细胞毒性,抑制率可达90%以上。结论菌株12010104、12010101和08010101的发酵液提取物在体外具有较好的PC12、HepG2、U937细胞毒活性,具有潜在的海洋药物研究价值。     

针毛蕨治疗慢性非细菌性前列腺炎的活性部位研究

摘 要 目的： 探讨针毛蕨甲醇提取物对慢性非细菌性前列腺炎（CNP）模型大鼠的治疗效果,初步确定其活性部位。方法: 粉碎的针毛蕨根茎用甲醇提取,所得浸膏依次用氯仿和乙酸乙酯萃取后得到氯仿部位、乙酸乙酯部位和水部位;建立角叉菜胶诱导的CNP模型,将实验大鼠随机分成正常对照组、模型组、阳性对照组、甲醇提取物组、乙酸乙酯组、氯仿组和水部位组,测定各组的前列腺指数,利用ELISA试剂盒测定各组大鼠血清中白细胞介素-10（IL-10）、肿瘤坏死因子-α（TNF-α）、环氧合酶-2（COX-2）和前列腺素E₂（PGE₂）的含量,前列腺组织HE染色后进行病理学观察。结果: 与模型组相比较,黄酮含量较高的乙酸乙酯组和甲醇提取物组大鼠的前列腺指数明显减小（P<0.01）,前列腺组织病理学改善显著,细胞因子IL-10、TNF-α、COX-2和PGE₂的含量显著降低（P<0.05或P<0.01）,尤其是乙酸乙酯组。结论:针毛蕨对CNP具有较好的治疗效果,初步确定乙酸乙酯部位为其活性部位。     

桂枝汤方剂不同提取部位免疫抑制活性的考察

目的 筛选桂枝汤方剂免疫抑制活性部位。方法 处方药材分别水煎浓缩为水提部位,乙醇提取为乙醇提取部位。同时将乙醇部位分别用石油醚、氯仿、乙酸乙酯、正丁醇萃取得石油醚部位、氯仿部位、乙酸乙酯部和正丁醇部位。CCK-8法考察桂枝汤不同提取物对ConA激活T细胞和LPS激活B细胞增殖的抑制作用。同时用二硝基氯苯对昆明种小鼠皮肤致敏和诱发,制成迟发型超敏反应模型,观察桂枝汤方剂不同部位对迟发型超敏反应的干预作用。结果 桂枝汤方剂水提物、乙醇提取物、石油醚萃取部位有显著免疫抑制功效,乙醇和石油醚提取物效果最佳。浓度200 mg·L-1时T细胞增殖抑制率分别为48.3%、45.9%,B细胞抑制率大于30%。乙醇提取物、石油醚萃取部位对迟发型超敏反应小鼠耳廓肿胀有显著抑制作用,对胸腺和脾脏无明显影响。结论 桂枝汤方剂乙醇提取物和石油醚萃取物为免疫抑制活性部位,能显著抑制T细胞和B细胞的增殖,抑制小鼠耳廓肿胀,对正常细胞、胸腺、脾脏无毒性。     

对—羟基苯甲醛和对—羟基苯甲酸对单胺氧化酶活性的影响

小鼠灌服对一羟基苯甲醛(PHBAD)和对一羟基苯甲酸(PHBZA)能明显抑制脑和肝组织的单胺氧化酶(MAO)活性,且对MAO—B的抑制作用强于MAO—A。PHBAD(200～400mg·kg~(-1)对小鼠脑MAO—B抑制作用强于PHBZA。体外实验证明,二者对MAO—B的抑制作用随浓度增加而明显增强。另外,PHBAD对MAO—B呈竞争型抑制;对MAO—A呈混合型抑制;而PHBZA对MAO-B、MAO—A均呈混合型抑制。     

Effect of cinnamon, clove and some of their constituents on the Na(+)-K(+)-ATPase activity and alanine absorption in the rat jejunum.

The effect of a water extract of some spices on the in vitro activity of the rat jejunal Na(+)-K(+)-ATPase was investigated. Extracts of nutmeg, cinnamon, clove, cumin, coriander, turmeric and caraway all inhibited the ATPase, while anise seed and white pepper exerted no significant effects. The extracts of clove and cinnamon had the most potent inhibitory effect on the intestinal ATPase as compared to extracts of other spices. They also inhibited the in vitro Na(+)-K(+)-ATPase activity in a crude kidney homogenate and the activity of an isolated dog kidney Na(+)-K(+)-ATPase. The alcoholic extract of cinnamon, compared to the aqueous extract, had a stronger inhibitory action on the jejunal enzyme and a lower IC(50) value, which was not significantly different from the one observed with cinnamaldehyde, the major volatile oil present cinnamon, suggesting that in alcoholic extracts cinnamaldehyde is the major inhibitory component. The IC(50) values of eugenol, aqueous clove extract and ethanolic clove extract all fell within the same range and were not significantly different from each other, suggesting that eugenol is the major inhibitory component in both alcoholic and aqueous extracts. Based on the IC(50) values, the order of sensitivity of the enzyme to the spices extracts is as follows: isolated dog kidney ATPase>rat kidney ATPase>rat intestine ATPase. The aqueous extracts of clove and cinnamon also significantly lowered the absorption of alanine from the rat intestine. It was concluded that the active principle(s) in clove and cinnamon can permeate the membrane of the enterocytes and inhibit the Na(+)-K(+)-ATPase that provides the driving force for many transport processes.     

Antibacterial Activity of Jordanian Medicinal Plants

The antibacterial activity of ethanol extracts of 15 plant species used in the traditional medicine in Jordan and other Middle East countries were tested. Extracts of certain parts of these plants were tested in vitro against 14 pathogenic bacterial species and strains using the agar diffusion method. Results evaluated as the diameter of inhibition zone of bacterial growth showed that 25 mg/well of 12 plant extracts have antibacterial activity on one or more of the tested bacteria. Three plants exhibited broad spectrum antibacterial activity: Punica granatum L., Quercus infectoria Olive., and Rhus coriaria L. The most susceptible bacteria were Pseudomonas aeruginosa, Bacillus cereus and Streptococcus pyogenes (ATCC 12351), and the most resistant species were Escherichia coli (ATCC 25922 and clinical isolates), Klebsiella pneumoniae, Shigella dysentriae (ATCC 49345), and Yersinia enterocolitica (ATCC 9610). The minimum inhibitory concentrations (MIC) of active extracts ranged from 4-32 mg/ml while the minimum bactericidal concentrations (MBC) were exerted at higher doses 8-62 mg/ml.     

Monoamine oxidase inhibitory activity of some Hypericum species native to South Brazil

The total methanol crude extracts and petroleum ether, chloroform, and methanol fractions obtained from Hypericum species, H. caprifoliatum, H. carinatum, H. connatum, H. cordatum, H. myrianthum, H. piriai, H. polyanthemum and H. brasiliense, all native to South Brazil, were assayed for monoamine oxidase A (MAO A) and MAO B inhibitory activity in rat brain mitochondrial preparations at concentrations ranging from 1 to 20microg mL(-1). Three benzopyrans, HP1 (6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran), HP2 (7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethylbenzopyran) and HP3 (5-hydroxy-6-isobutyryl-7-methoxy-2,2dimethylbenzopyran) isolated from H. polyanthemum were also tested at maximal concentrations of 150, 150 and 75/microM, respectively. The lipophilic extracts of H. polyanthemum, H. caprifoliatum and H. piriai displayed MAO A inhibitory activity greater than 50%. Among the benzopyrans, only HP3 showed significant activity, with an IC50 value of 22 microM. The total methanol crude extracts of aerial parts from H. carinatum, H. connatum, H. cordatum, H. polyanthemum and H. piriai were evaluated for antidepressant activity in the Porsolt's forced swimming test in Wistar rats (270 mg kg(-1) day(-1); i.p); however, none of them showed activity.     

Comparative evaluation of 12 immature citrus fruit extracts for the inhibition of cytochrome P450 isoform activities

In a previous study we found that 50% ethanol extracts of immature fruits of Citrus unshiu (satsuma mandarin) have anti-allergic effects against the Type I, II and IV allergic reactions. However, many adverse interactions between citrus fruit, especially grapefruit juice, and drugs have been reported due to the inhibition of cytochrome P450 (CYP) activities. The purpose of this study was to examine the competitive inhibitory effects of extracts from immature citrus fruit on CYP activity. Extracts were prepared from 12 citrus species or cultivars, and were tested against three kinds of major CYPs, CYP2C9, CYP2D6 and CYP3A4, in human liver microsomes. We also estimated the amounts of flavonoids (narirutin, hesperidin, naringin and neohesperidin) and furanocoumarins (bergapten, 6',7'-dihydroxybergamottin and bergamottin) in each extract using HPLC. Citrus paradisi (grapefruit) showed the greatest inhibition of CYP activities, while Citrus unshiu which has an antiallergic effect, showed relatively weak inhibitory effects. Extracts having relatively strong inhibitory effects for CYP3A4 tended to contain higher amounts of naringin, bergamottin and 6',7'-dihydroxybergamottin. These results, providing comparative information on the inhibitory effects of citrus extracts on CYP isoforms, suggest that citrus extracts containing high levels of narirutin and hesperidin and lower levels of furanocoumarins such as C. unshiu are favorable as antiallergic functional ingredients.     

Inhibition of malonaldehyde formation from blood plasma oxidation by aroma extracts and aroma components isolated from clove and eucalyptus

The inhibitory effect of aroma extracts isolated from clove buds [Syzygium aromaticum (L.) Merr. et Perry] and eucalyptus leaves (Eucalyptus polyanthemos Schauer) on malonaldehyde (MA) formation from horse blood plasma oxidized with Fenton's reagent was determined by gas chromatography. Aroma chemicals such as eugenol, thymol and benzyl alcohol, identified in the aroma extracts, were examined for their inhibitory effect on the same system. Between the two aroma extracts tested, clove exhibited the most potent antioxidant activities. Extracts of eucalyptus and clove inhibited MA formation by 23 and 48%, respectively, at the level of 400 μg/ml, whereas, -tocopherol and BHT inhibited MA formation by 52 and 70%, respectively, at the same level. Eugenol, thymol and benzyl alcohol inhibited MA formation by 57, 43 and 32%, respectively, at the level of 400 μg/ml.     

Antioxidant and cytotoxic activities of ethanolic extracts and isolated fractions of species of the genus Phellinus Quél. (Aphyllophoromycetideae)

Ethanolic extracts of fruit bodies of 5 species (8 strains) of the genus Phellinus, and isolated fractions derived from 1 of these extracts (Ph. baumii PB-10), were evaluated for antioxidant activity, inhibitory effects on the growth of human tumor cells, and the capacity to protect PC12 cells against H2O2-induced oxidative damage. Extracts of all 8 strains of Phellinus spp. exhibited antioxidant activity and protected PC12 cells against oxidative damage at different magnitudes of potency. The strongest antioxidant activity was exhibited by extracts of Ph. baumii PB-10, with recorded IC50 values for superoxide radical and hydrogen peroxide scavenging activity of 3.76 microg/mL and 4.24 microg/mL, respectively. Radical-scavenging activity and protection levels against H2O2-induced damage to PC12 cells were highly correlated with the flavonoid content of the extracts and isolated fractions. All the extracts inhibited L1210, SW620, and MCF-7 tumor cell proliferation at 200 microg/mL concentrations, but inhibition was not correlated with the flavone content of the test samples and was clearly dependent upon the presence of other, as yet, unidentified components. Our data indicate that fruit bodies of species of the genus Phellinus represent a potentially valuable source of natural antioxidants of relevance to both the health and food industries.     

Increase of brain endogenous monoamine oxidase inhibitory activity (tribulin) in experimental audiogenic seizures in rats: evidence for a monoamine oxidase A inhibiting component of tribulin.

Brain tribulin activity in rats with an inherited predisposition to audiogenic epilepsy was studied after seizures of different intensity were induced by an electric bell. Weak seizures (from 0 to 2 arbitrary units) did not produce any changes in endogenous inhibitory activity towards either monoamine oxidase (MAO) A or B. Moderate seizures were characterized by increases in both MAO A and MAO B inhibitory activity (up to 1.9-fold). Complete tonic epileptiform seizures with total areflexia (4 arbitrary units) induced further augmentation (up to 2.5-fold) of MAO A but not of MAO B inhibitory activity. This dissociation between the two inhibitory activities points to the existence of a separate MAO A-inhibiting component of brain tribulin which is different from isatin.     

Goldenseal (Hydrastis canadensis L.) extracts synergistically enhance the antibacterial activity of berberine via efflux pump inhibition

Goldenseal (Hydrastis canadensis L.) is used to combat inflammation and infection. Its antibacterial activity in vitRO has been attributed to its alkaloids, the most abundant of which is berberine. The goal of these studies was to compare the composition, antibacterial activity, and efflux pump inhibitory activity of ethanolic extracts prepared from roots and aerial portions of H. canadensis. Ethanolic extracts were prepared separately from roots and aerial portions of six H. canadensis plants. Extracts were analyzed for alkaloid concentration using LC-MS and tested for antimicrobial activity against Staphylococcus aureus (NCTC 8325-4) and for inhibition of ethidium bromide efflux. Synergistic antibacterial activity was observed between the aerial extract (FIC 0.375) and to a lesser extent the root extract (FIC 0.750) and berberine. The aerial extract inhibited ethidium bromide efflux from wild-type S. aureus but had no effect on the expulsion of this compound from an isogenic derivative deleted for norA. Our studies indicate that the roots of H. canadensis contain higher levels of alkaloids than the aerial portions, but the aerial portions synergize with berberine more significantly than the roots. Furthermore, extracts from the aerial portions of H. canadensis contain efflux pump inhibitors, while efflux pump inhibitory activity was not observed for the root extract. The three most abundant H. canadensis alkaloids, berberine, hydrastine, and canadine, are not responsible for the efflux pump inhibitory activity of the extracts from H. canadensis aerial portions.