雪松松针提取物抑菌活性及抑菌稳定性研究

目的研究雪松松针不同溶剂提取物的抑菌效果和抑菌稳定性。方法分别用水、95%乙醇、乙酸乙酯、石油醚对雪松松针进行提取,采用滤纸片法比较不同溶剂提取物的抑菌活性。采用不同体积分数的乙醇提取,确定提取雪松松针抑菌成分的最适溶剂。探讨热处理、介质pH和糖含量对松针提取物抑菌稳定性的影响。结果松针50%乙醇的提取物抑菌活性最佳,热处理对抑菌活性无明显影响,介质pH和糖含量可在一定程度上影响抑菌活性。结论雪松松针提取物具有较好的抑菌作用,可作为一种天然防腐剂加以开发利用。     

鸡眼草3种不同溶剂提取物对ABTS自由基和羟自由基清除活性的研究

目的:研究鸡眼草3种不同溶剂提取物对ABTS自由基(ABTS·+)和羟自由基(·OH)的清除活性。方法:用冷浸法得到鸡眼草乙醇、丙酮和乙酸乙酯提取物,以UV法测定3种提取物的总黄酮含量,并测定3种提取物对ABTS·+和·OH的清除活性。结果:鸡眼草丙酮提取物的总黄酮含量最高(131.41mg·g-1),对自由基的清除效果也最好,其对ABTS·+和·OH的清除率最高可达到88.79%和95.81%。结论:鸡眼草乙醇、丙酮和乙酸乙酯提取物都具有较强的自由基清除能力,有作为天然抗氧化剂开发利用的潜力。     

不同来源白英乙醇提取物抗肿瘤活性比较

目的考察不同来源白英乙醇提取物抗肿瘤活性。方法采用MTT法对不同来源白英乙醇提取物进行抗肿瘤活性测定,通过比较IC50值来评价其抗肿瘤活性。结果不同来源白英乙醇提取物对体外培养的Hela细胞增殖抑制作用存在差异,IC50值在1.91～24.26 mg/mL范围内。结论广西柳州产地白英乙醇提取物抗肿瘤活性最高,浙江宁波产地次之,广东佛山产地活性最低。     

海南16种红树植物的肿瘤细胞毒活性筛选

目的研究海南红树植物提取物对HeLa细胞的生长抑制作用。方法用乙醇对采自海南文昌县的16种红树植物进行提取,所得提取物分散于水中,用醋酸乙酯萃取后得到醋酸乙酯提取物和水提取物;利用MTT法测定各红树植物的提取物对HeLa细胞的生长抑制率。结果共有6种红树植物的醋酸乙酯提取物显示了对HeLa细胞的生长抑制活性,其中卤蕨和银叶树的醋酸乙酯提取物活性较强,IC50分别为6.3μg.mL-1和9.5μg.mL-1。结论16种红树植物中有6种植物的醋酸乙酯提取物对HeLa细胞显示了生长抑制活性,红树植物的水提物均未显示出活性。     

瓦松提取物对实验性胃溃疡的治疗作用

目的：观察瓦松提取物对实验性胃溃疡的治疗作用。方法：以Wistar大鼠和昆明种小鼠为研究对象,复制5种实验性胃溃疡动物模型（小鼠束缚水浸应激致胃溃疡模型、吲哚美辛致小鼠胃溃疡模型、乙醇致大鼠胃溃疡模型、乙酸致大鼠胃溃疡模型和大鼠幽门结扎致胃溃疡模型）。将大鼠随机分为瓦松提取物400、200、100mg/kg剂量组、阳性对照组和模型对照组;小鼠随机分成瓦松提取物800、400、200mg/kg剂量组、阳性对照组和模型对照组。测定胃溃疡指数、胃液游离酸排出量及总酸排出量。结果：瓦松提取物400、800mg/kg剂量组能降低小鼠应激性溃疡溃疡指数（P〈0.05）;200～800mg/kg瓦松提取物对吲哚美辛致小鼠胃溃疡溃疡指数有明显的降低作用（P〈0.05或P〈0.01）;同时对乙醇引起的大鼠胃溃疡也具有明显的抑制作用（P〈0.05）,并可明显促进乙酸致大鼠胃溃疡溃疡的愈合,但对动物胃液分泌及胃蛋白酶活性无明显影响。结论：瓦松提取物对实验性胃溃疡有明显的预防和治疗作用。     

鸢尾乙醇提取物的抗炎作用研究

研究鸢尾乙醇提取物对组胺所致的小鼠皮肤毛细管通透性的影响，为鸢尾药理活性进一步的研究提供义献依据：试验结果认为其乙醇提取物对组胺所致的小鼠皮肤毛细管通透性有明显的抑制作用。     

48种中药材的乙酰胆碱酯酶抑制活性研究(英文)

乙酰胆碱酯酶(AChE)抑制剂是治疗阿尔茨海默病的一个重要策略。本研究对48种中药材的乙醇提取物和水提取物进行了体外AChE抑制活性的筛选,微板测试法结果表明28种中药材的乙醇提取物和11种中药材的水提取物具有AChE抑制活性。其中,香薷、益智仁、生地黄和荷叶乙醇提取物的AChE抑制活性最强,它们在终浓度为0.1mg/mL时的抑制活性分别为(68.63±1.12)%,(44.49±3.66)%,(43.78±4.76)%和(42.63±8.31)%。薄层色谱–生物自显影的方法亦证明了这四种中药材具有抑制AChE的活性成分。本实验结果为治疗阿尔茨海默病中药的传统应用提供了部分支持。     

倒卵叶五加大孔树脂不同体积分数乙醇洗脱组分对血小板聚集率及纤溶活性的影响

目的研究倒卵叶五加提取物D101大孔树脂不同体积分数乙醇洗脱组分对血小板聚集率及纤溶活性的影响。方法采用体外实验,比浊法测定倒卵叶五加提取物0%~80%不同体积分数乙醇洗脱组分在ADP聚集诱导剂作用下的血小板聚集率;采用纤维蛋白平板法测定倒卵叶五加提取物0%~80%不同体积分数乙醇洗脱组分纤溶活性。结果倒卵叶五加提取物体积分数10%~70%乙醇洗脱组分可明显抑制血小板聚集(P<0.05或P<0.01);体积分数20%~40%乙醇洗脱组分抗血小板聚集作用最强(P<0.01);体积分数20%~60%乙醇洗脱组分可明显提高纤溶活性(P<0.05或P<0.01);体积分数20%~50%乙醇洗脱组分纤溶活性最强(P<0.01)。结论倒卵叶五加具有明显的抗血小板聚集以及提高纤溶活性的作用,其作用与洗脱剂不同体积分数乙醇中的组分不同有关。     

野生和栽培金铁锁抗氧化活性比较

目的野生和栽培金铁锁抗氧化活性比较。方法以Vc和BHA为参照,采用DPPH方法对野生和栽培金铁锁根乙醇、石油醚、乙酸乙酯、正丁醇和水提取物抗氧化活性进行测试。结果野生和栽培金铁锁根乙酸乙酯、正丁醇提取物抗氧化活性IC50值分别为443μg/mL、1265μg/mL和378μg/mL、1877μg/mL。结论①野生和栽培金铁锁各提取物抗氧化活性基本一致;②无论野生还是栽培金铁锁抗氧化作用都比较弱;③无论栽培还是野生金铁锁,抗氧化活性物质基本都集中在乙酸乙酯提取物和正丁醇提取物之中,均以乙酸乙酯提取物最强;④虽然栽培金铁锁乙酸乙酯提取物抗氧化活性要强于野生金铁锁、野生金铁锁正丁醇提取物抗氧化活性要强于栽培金铁锁,但相对于阳性对照Vc和BHA来说均很小,差异并不是很明显。     

2种藏紫草体外抗氧化及抗菌活性比较

目的 比较长花滇紫草和团花滇紫草75％乙醇提取物的体外抗氧化及抗菌活性.方法 采用ABTS法、FRAP法、邻苯三酚自氧化法测定体外抗氧化能力,并采用肉汤连续稀释法初步考察了 2种藏紫草体提取物体外对15种不同菌株的抗菌作用.结果 不同浓度藏紫草的75％乙醇提取物对ABTS自由基和超氧阴离子都有较强的清除能力,与BHT阳...     

SV预防血栓药理学作用及其机制研究探讨

血栓栓塞性疾病是人类首要致死病因,临床预防血栓药物均存在出血危险。选择性的内源性凝血途径抑制剂已成为低出血倾向预防血栓药物研发的重点方向。SV是以天然岩藻糖化糖胺聚糖(FG)为先导化合物经结构优化获得的选择性内源性凝血因子Xase抑制剂(IC50=30 nm),其抑制内源性凝血活性与依诺肝素相当,在等效抗凝血剂量的倍数剂量下出血倾向显著降低。本文探讨低出血倾向的SV预防血栓药理学作用及其机制,为选择性Xase抑制剂及其新药发现研究提供参考依据。     

Antifertility Activity of Stems of Plumbago rosea in Female Albino Rats

In the present study, Plumbago rosea Linn. (Plumbaginaceae), one of the folk medicinal plants commonly used as an antifertility agent, was evaluated for its antifertility effect. Five successive solvent extracts, petroleum ether, chloroform, acetone, ethanol, and water extracts, of the stems of P. rosea were studied on estrous cycle at two dose levels, 200 and 400 mg/kg respectively. Of these, the acetone extract was found to be most effective in interrupting the normal estrous cycle of rats (p < 0.05) (p < 0.01). The rats exhibited prolonged diestrous stage of the estrous cycle with consequent temporary inhibition of ovulation. The antiovulatory activity was reversible on withdrawal of the extract. The effective acetone extract was further studied on estrogenic functionality in rats. The acetone extract showed significant estrogenic and antiestrogenic activity (p < 0.05) (p < 0.001). Histological studies of the uteri further confirmed the estrogenic activity of acetone extract. The results indicated the antifertility activity of stems of Plumbago rosea in female Wistar rats.     

Antipyretic, analgesic and anti-inflammatory effects of delta 9-tetrahydrocannabinol in the rat

The effects on body temperature produced by graded doses of Δ⁹-tetrahydrocannabinol (Δ⁹-THC) and phenylbutazone were compared in both normal and pyretic rats. Dose related hypothermic responses were produced by the oral administration of Δ⁹-THC in normal animals. Moreover, Δ⁹-THC significantly reduced elevated temperatures in yeast-induced pyretic rats to near normal levels at doses which exhibited little hypothermic activity in normal rats. The oral antipyretic potency of Δ⁹-THC was approximately 2 times that of phenylbutazone. The comparative oral antinociceptive activity of Δ⁹-THC and selected narcotic and non-narcotic analgesics was determined by the increase in response latency to pressure applied to normal and yeast-inflamed paws. Δ⁹-THC administered orally was essentially inactive at dose levels below those producing pronounced central nervous system depression. The oral anti-inflammatory efficacy of Δ⁹-THC was compared to phenylbutazone and acetylsalicylic acid. Δ⁹-THC was ineffective in inhibiting carrageenin-induced edema of the rat paw following acute or chronic administration.     

Psychopharmacological effects of Artemisia copa aqueous extract in mice

Objective: To evaluate the aqueous extract from aerial parts of Artemisia copa Phil. (Asteraceae) administered orallyfor its psychopharmacological activities in several experimental models

Methods: The extract was administered p.o. in Swiss albino mice and tested on pentobarbital-induced hypnosis, locomotor activity, exploration in the hole-board, anxiolytic like profile evaluated in the marble-burying test and anticonvulsant activity on convulsions induced by pentylenetetrazol.

Results: Artemisia copa at doses up to 1.5?g/kg produced a dose-dependent sleep induction and potentiation of sub-hypnotic and hypnotic doses of pentobarbital. The extract also produced a dose-dependent increase and decrease in the spontaneous motor activity (0.5–1.5?g/kg, respectively), no disruption or a decrease on exploratory (hole-board) behavioral profiles (0.5–1.5?g/kg respectively) and a dose-related anxiolytic-like activity as indicated by increases in the percentage of marbles they left uncovered in the marble-burying test at doses (0.5?g/kg) that do not disrupt the motor activity. In addition, the extract (1.5?g/kg) produced a significant increase in the latency time and a decrease in the duration of seizures and mortality induced by PTZ 75?mg/kg in mice.

Conclusion: These results suggest that the aqueous extract of Artemisia copa may contain sedative principles with potential anxiolytic and anticonvulsant activities.     

Antimicrobial and antineoplastic activities of agelasine analogs modified in the purine 2-position

Agelasines are 7,9-dialkylpurinium salts found in marine sponges (Agelas sp.), which display a variety of antimicrobial and cytotoxic effects. We have synthesized simplified agelasine analogs modified in the purine 2-position and examined their antimicrobial and anticancer activities. The compounds were screened against Staphylococcus aureus, Escherichia coli, Mycobacterium tuberculosis, Candida krusei, and Candida albicans, protozoa causing tropical diseases (Plasmodium falciparum, Leishmania infantum, Trypanosoma cruzi, and Trypanosoma brucei), a panel of human cancer cell lines (U-937 GTB, RPMI 8226/s, CEM/s, and ACHN) as well as VERO and/or MRC-5 cells. The results indicate that the introduction of a methyl group in the purine 2-position is beneficial for antimycobacterial and antiprotozoal activity, and that amino groups may enhance activity against several cancer cell lines.     

Antidepressant and antinociceptive activities in animal models and in vitro assessment of the anti-thyroid activity of bis(DL-pyroglutamate)magnesium complex

BackgroundMagnesium is an essential element related with biochemistry of the brain and different types of depression have been associated with its deficiency.MethodsThe structure of a novel magnesium bis(DL-pyroglutamate) (Mg(DL-pGlu)₂) was elucidated by X-ray crystallography. Wistar rats were used in the in vivo experiments. The antidepressant-like effect was assessed by the forced swim test (FST) and the antinociceptive activity was evaluated using hot plate test. In both, non-specific effects were evaluated by the open field test. Anti-thyroid activity was examined using Lang’s method. Albumin binding behavior was evaluated by 3D fluorescence spectroscopy.ResultsFor the Mg(DL-pGlu)₂ complex (30 mg/kg), the FST test on Wistar rats revealed a decrease of 22% in the immobility time and an increment of 106% in the swimming time. The compound alters neither the locomotor activity nor the body weight after chronic administration. At the same dose, it showed antinociceptive activity, increasing the response latency. It blocks iodination reactions generating a charge transfer complex with iodine hence indicating anti-thyroid activity (K_c = 45366.5 ± 29 M^?1). Albumin 3D fluorescence spectroscopy experiments showed intensity increase of peak A and decrease of peak B.ConclusionsThe results showed that the new compound produced a lowering of the immobility time and an increment of the swimming ability of the rats. The compound is able to increase the response latency in 70.0%, to capture iodine (anti-thyroid activity) and to interact with albumin through covalent type of interaction of the free NH groups.     

头孢硫咪体外抗菌活性测定

目的：评价第一代头孢菌素头孢硫脒对近期从临床分离的致病菌的体外抗菌活性。方法：用对倍稀释法测定头孢硫咪的最小抑菌浓度（ＭＩＣ）并与头孢唑啉、头孢呋辛、头孢他啶体外抗菌活性进行了对比。结果：头孢硫脒对肺炎球菌、化脓性链球菌、ＭＳＳＡ、ＭＳＳＥ和卡他布汉氏菌有较强的抗菌活性。结论：头孢硫脒对Ｇ^＋球菌有较强的抑菌活性和杀菌活性,对肠球菌亦显示有很强的体外抗菌活性。     

Synergistic activity of baicalein with ribavirin against influenza A (H1N1) virus infections in cell culture and in mice

Baicalein is a flavonoid derived from the root of Scutellaria baicalensis, a traditional Chinese medicine that has been used for hundreds of years; baicalein has also been demonstrated to have antiviral activity with low toxicity. The synergistic activity of baicalein with ribavirin against influenza virus infections in cell culture and in mice was investigated for the first time in our research. In vitro, maximal synergy at lower concentrations of baicalein (0.125 μg/ml) and ribavirin (12.5 μg/ml) was observed, and the reduced expression of the viral matrix protein (M) gene suggested that drug combinations caused greater inhibition than ribavirin alone, especially the combination of 0.5 μg/ml baicalein and 5 μg/ml ribavirin. In vivo, combinations of baicalein and ribavirin provided a higher survival rate and lower body weight loss. Moreover, fewer inflammatory responses in the lungs of mice infected with virus and treated with baicalein and ribavirin were observed; the mean scores were 1.0, 0.8, and 1.2 with the doses of ribavirin at 50 mg/kg/d combined with baicalein at 100 mg/kg/d, 200 mg/kg/d, and 400 mg/kg/d respectively, while the placebo group had a mean pathology score of 3.2. Thus, the data demonstrates that combinations of baicalein and ribavirin provide better protection against influenza infection than each compound used alone and could potentially be clinically useful.     

低分子肝素在麻醉大鼠胃肠道的吸收

以血浆抗Ｘａ活性及体内抗静脉血栓形成为指标，考察了低分子肝素溶液及乳剂在麻醉大鼠胃肠道的吸收情况。     

大规模提取罗汉果叶和藤及其多种生物活性的研究

目的大规模制备罗汉果叶和藤提取物并研究其抗菌、抗氧化和促进胰岛素分泌的多种活性。方法制备罗汉果叶和藤提取物,并通过离子交换树脂进一步分离。通过活性测试对提取物和各馏分进行抗菌、抗氧化和促进胰岛素分泌的试验。结果罗汉果叶和藤提取物以及分离得到的馏分表现出抗菌、抗氧化和促进胰岛素分泌的活性。结论罗汉果叶和藤提取物具有抗菌、抗氧化和促进胰岛素分泌的活性。罗汉果叶和藤具有开发为药物和功能性食品的潜力。