齐墩果酸和熊果酸的神经精神药理作用研究进展

齐墩果酸和熊果酸同属五环三萜酸类化合物,它们又是同分异构体.药理作用几乎相同,都具有抗氧化、抗炎、免疫调节、抗肿瘤、抗微生物、保肝、抗糖尿病、调脂、减肥、抗动脉粥样硬化作用.综述齐墩果酸和熊果酸保护神经细胞、镇痛、抗焦虑、抗神经分裂症、抗抑郁、改善学习记忆等神经精神药理作用,为齐墩果酸和熊果酸防治老年痴呆、帕金森病和抑郁症的研发提供依据.     

熊果酸和齐墩果酸对肺功能保护和抗肺癌作用的研究进展

熊果酸和齐墩果酸是同属五环三萜酸类的同分异构体,广泛存在于各种植物之中。熊果酸和齐墩果酸的药理作用几乎相同,都具有抗氧化、抗炎、免疫调节、抗肿瘤、抗微生物和保护心、肝、肾的作用,以及抗糖尿病、调血脂、抗肥胖、抗动脉粥样硬化和镇痛、抗焦虑、抗抑郁、改善学习记忆等神经保护作用,促进骨、肌肉生长和抗骨质疏松等药理作用。综述和分析熊果酸和齐墩果酸对抗二氧化硅、百草枯、脂多糖、盲肠结扎和刺穿、外伤出血性休克引起的肺损伤,以及抗肺癌作用的文献资料,为全方位开发熊果酸和齐墩果酸在临床上的应用提供参考。     

熊果酸和齐墩果酸抗皮肤癌与白血病药理作用的研究进展

熊果酸和齐墩果酸是化学立体结构相同的同分异构体,广泛存在于各种植物之中,具有广泛的生物活性(如保肝、抗炎、抗微生物、抗糖尿病和抗肿瘤)等作用。综述熊果酸和齐墩果酸抑制皮肤乳头瘤的形成、抗黑色素瘤、淋巴系和髓系白血病等药理作用及其机制的研究进展。     

齐墩果酸和熊果酸的抗微生物和原虫药理研究进展

近年来,国内外对齐墩果酸和熊果酸在抗微生物和原虫方面的药理作用的广泛研究,证实在体外熊果酸及其衍生物对G+和G-菌及酵母菌均有抗菌活性以及对病毒具有抑制作用。该文对齐墩果酸和熊果酸在抗病毒、抗菌及抗原虫方面的研究进展作一综述。     

熊果酸和齐墩果酸抗脑瘤作用的研究进展

熊果酸和齐墩果酸广泛存在于蔬菜、水果和中草药里,并被广泛研究。二者不仅同属五环三萜酸类化合物,又是同分异构体,药理作用几乎相同,都具有抗炎、抗变态反应、抗微生物、降血糖、调血脂、减肥、抗动脉粥样硬化、抗骨质疏松、保肝和免疫调节以及抗焦虑、抗抑郁、改善学习记忆等作用。熊果酸和齐墩果酸还具有广谱抗肿瘤作用,包括呼吸系肿瘤、消化系肿瘤、性器官肿瘤、皮肤癌和白血病等。综述熊果酸和齐墩果酸抗脑瘤作用及其机制的研究进展,为新药研发提供依据。     

熊果酸的药动学研究进展

熊果酸具有广泛的药理作用,包括抗炎、抗变态反应,抗肿瘤,保护心、血管、肝、肾、肺,抗糖尿病、调血脂抗肥胖,抗动脉粥样硬化等。但是其口服的生物利用度低,通过被动扩散被肠道吸收;将熊果酸制成分散体制剂能提高溶出度和生物利用度,且能浓集于肝脏,有利于治疗肝部疾病。综述熊果酸的药动学参数、体内过程和熊果酸分散体的药动学特征,总结其药动学研究进展,为合理用药提供参考。     

女贞子及其有效成分药理作用与皮肤科临床应用的进展

女贞子是中医皮肤科常用的中药,其成分中齐墩果酸及其同分异构体熊果酸、红景天苷及其苷元酪醇是女贞子皮肤药理的有效成分,不仅具有保肝、抗糖尿病、抗动脉粥样硬化、心血管保护、神经保护及抗微生物等药理作用.综述女贞子及其有效成分的药理作用和皮肤科临床抗皮肤炎症、变态反应,以及抗皮肤肿瘤、促进毛发生长和黑色素合成的药理作用的文献,并对其研究进展作一分析.     

熊果酸抗肿瘤作用及其机制研究进展

通过有关试验研究及查阅国内外近期文献资料,概述分析熊果酸在医药领域的研究进展.熊果酸属五环三萜类化合物,具有广泛的生物活性,抗肿瘤活性是其最主要的药理作用,其抗肿瘤作用是多方面的,并且资源丰富,开发应用前景广阔,但是在动物体内熊果酸生物利用度较低,需通过化学修饰的方法,进一步提高熊果酸的抗癌活性和生物利用度,此方面的研究将是熊果酸系列抗癌药物研发的重要步骤及未来开发的一个方向和热点,熊果酸有望成为一种高效低毒的抗肿瘤新药.     

熊果酸抗糖尿病并发症药理作用的研究进展

动物实验表明熊果酸能对抗糖尿病引起的各种并发症,熊果酸通过它的降脂、降糖和抗氧化作用以及对抗高浓度葡萄糖的氧化应激反应和醛糖还原酶的表达和活性,产生防治糖尿病并发症的效应。综述熊果酸抗糖尿病并发症的药理作用及其机制的文献资料,并对其研究进展作了分析。     

岩青兰的化学成分及药理学研究综述

唇形科青兰属植物岩青兰具有较高的药用价值,研究表明岩青兰中含有北美圣草素,木犀草素,柚皮素-7-O-β-D-葡萄糖苷等黄酮类化合物,熊果酸,白桦脂酸,间羟基苯甲酸等有机酸类,β-谷甾醇,白桦脂醇,正十八醇十八酸酯等挥发性油以及Ca、Mg、Fe等微量元素,具有血小板活化因子(PAF)拮抗,保护心肌,抗炎,抗癌等药理作用,临床应用广泛。本文就岩青兰的化学成分及其药理作用方面作一综述。     

Free and chemically bonded phenolic acids in barks of Viburnum opulus L. and Sambucus nigra L

Liquid column chromatography, planar chromatography (TLC) on modified and unmodified silica layers, reversed-phase high-pressure liquid chromatography (HPLC), as well as ESI-TOF MS and 1H-NMR have been used for separation, purification and identification of phenolic acids in the barks of Sambucus nigra and Viburnum opulus (Caprifoliaceae). By the use of these procedures three cinnamic acid derivatives: caffeic acid, p-coumaric, and ferulic acid, four benzoic acid derivatives: gallic acid, protocatechuic acid, syringic acid, 3,4,5-trimethoxybenzoic acid, two phenylacetic acid derivatives: 3,4-dihydroxyphenylacetic acid, homogentisic acid, and two depsides: chlorogenic acid and ellagic acid were detected and identified in the bark of Viburnum opulus. Caffeic acid, p-coumaric acid, ferulic acid, gallic acid, syringic acid, 3,4,5-trimethoxybenzoic acid and chlorogenic acid were also detected and identified in the bark of Sambucus nigra. Except for chlorogenic acid, this is the first time these phenolic acids have been isolated, detected, and identified in the bark of V. opulus and S. nigra.     

甘草酸及其苷元甘草次酸的糖皮质激素样作用

甘草酸在体内水解成甘草次酸,因此甘草酸是甘草次酸的前体药物,而甘草次酸的药理作用强于甘草酸.甘草次酸的化学结构类似于甾体激素.甘草次酸和甘草酸是甾体激素代谢失活酶抑制剂,可提高内源性和外源性糖皮质激素的活性.甘草次酸和甘草酸义町作为配体,与糖皮质激素受体结合,由于甘草次酸和甘草酸的糖皮质激素受体激动活性远低于糖皮质激素...     

蒙药塔布森-2中9种苯丙素类成分在Caco-2细胞中的吸收特性研究

目的 研究蒙药塔布森-2(Tabson-2 decoction,TBD)中苯丙素类成分在Caco-2细胞中的吸收特性,初步阐明TBD的口服吸收机制。方法 采用Caco-2细胞单层细胞模型,通过UPLC-MS/MS分析TBD在Caco-2细胞中的摄取成分,并建立UPLC-MS/MS分析方法测定TBD中吸收最好的9种苯丙素类成分原儿茶酸、新绿原酸、绿原酸、隐绿原酸、1,5-二咖啡酰奎宁酸、异绿原酸C、咖啡酸、二氢咖啡酸、3-羟基肉桂酸在Caco-2细胞中的含量,分别考察时间、浓度和P糖蛋白抑制剂对各成分的吸收影响。结果 研究发现咖啡酸、二氢咖啡酸的总摄取量在0~180 min为上升趋势,未呈现饱和;3-羟基肉桂酸在90 min左右吸收恒定趋于饱和;隐绿原酸、1,5-二咖啡酰奎宁酸、异绿原酸C、新绿原酸、绿原酸、原儿茶酸的摄取量约从90 min开始,随时间的增加先下降后上升。与苯丙素类成分相比,加入P-糖蛋白抑制剂维拉帕米及环孢菌素A后对二氢咖啡酸的吸收产生了影响,说明二氢咖啡酸是P-糖蛋白底物。结论 TBD主要苯丙素类成分进入Caco-2细胞以被动扩散为主,主动转运为辅,且除二氢咖啡酸外其他8个成分的吸收过程不受P-糖蛋白的外排作用影响。     

UPLC测定余甘子产地、采收时间和炮制对其质量关系影响

目的比较不同产地、采收时间及不同炮制方法对余甘子中没食子酸和鞣花酸的含量影响。方法采用UPLC法建立测定余甘子中没食子酸和鞣花酸的方法,利用ACQUITY UPLC BEH C 18(100mm×2.1mm,1.7μm)色谱柱,柱温为30℃,流动相以甲醇-0.1%磷酸溶液测定没食子酸(检测波长273nm),以乙腈-0.2%磷酸溶液测定鞣花酸(检测波长254nm);体积流量为0.2mL·min^-1,进样量为10μL。测定余甘子不同产地、采收时间和不同炮制品种没食子酸和鞣花酸的含量影响。结果不同的产地中,广东潮汕(没食子酸25.20%、鞣花酸23.73%)、福建泉州(没食子酸26.28%、鞣花酸33.18%)、广西梧州(没食子酸26.59%、鞣花酸20.80%)、四川凉山(没食子酸27.59%、鞣花酸22.48%)、云南楚雄(没食子酸28.36%、鞣花酸25.59%),其中以云南楚雄的余甘子中没食子酸的含量为最高,其他四地产地含量略低;福建泉州的余甘子鞣花酸含量最高,其他四地含量偏低。不同采摘时间的数据均显示在每年的六月中旬季节采收所得的没食子酸和鞣花酸的含量是最高。经过不同炮制方法后,没食子酸的含量:生品>醋炙≈酒炙>盐炙>蜜炙,鞣花酸相比与生品,酒炙、盐炙和蜜炙含量有不同程度的上升,醋炙含量略微下降。结论不同产地、采收季节和炮制工艺对余甘子中的活性成分含量有影响。     

Montmorillonite adsorbs uric acid and increases the excretion of uric acid from the intestinal tract in mice

Objectives The aim was to evaluate the adsorbing effect of montmorillonite on uric acid, promoting diffusion of uric acid from blood to intestine, preventing absorption of uric acid in intestine and reducing uric acid level in serum. Methods The adsorbing effect of montmorillonite on uric acid was observed in vitro. The intestine and blood vessel of rats were circularly perfused with intestinal perfusate and vascular perfusate, respectively. A model of hyperuricaemia in mice was prepared by intraperitoneal injection of hypoxanthine and potassium oteracil. The concentration of uric acid was determined by the method of urate oxidase and peroxide enzyme. Key findings The results showed that different concentrations of montmorillonite could adsorb uric acid in a concentration‐dependent manner. The adsorbing effect was fast. The adsorptive rate was high in acid solution and was low in alkaline solution. When blood vessels were circularly perfused by vascular perfusate containing uric acid, the concentration of uric acid in vascular perfusate was decreased and the concentration of uric acid in intestinal perfusate was increased, suggesting that uric acid in blood vessels diffused into the intestine. When the intestine was perfused with intestinal perfusate containing uric acid, the uric acid concentration in vascular perfusate was increased, but the uric acid concentration of intestinal perfusate was decreased, suggesting that uric acid was absorbed in the intestine. The uric acid concentrations of intestinal perfusate and vascular perfusate in montmorillonite 0.5 and 1.0 g/kg groups were lower than the control group. Concentrations of uric acid in serum and urine in the montmorillonite 1 and 2 g/kg groups were lower compared with mice in the hyperuricaemic group. Conclusions The results suggested that montmorillonite adsorbed uric acid and promoted diffusion of uric acid from blood vessels to intestine, prevented absorption of uric acid in intestine and decreased uric acid level in serum.     

建立大鼠原位肠-肝灌流模型评价绿原酸的代谢

目的：建立大鼠原位肠-肝灌流模型，运用该模型研究绿原酸在大鼠肠、肝中的代谢转化。方法：采用液相色谱质谱联用（HPLC-MS）法测定大鼠原位肠-肝灌流模型灌流液中绿原酸及其代谢产物咖啡酸、阿魏酸和马尿酸。结果：绿原酸十二指肠给药后，灌流液中主要活性代谢产物为阿魏酸，同时在灌流液中也检测到少量活性代谢产物咖啡酸和大量代谢终产物马尿酸。结论：大鼠原位肠-肝灌流模型适用于绿原酸生物转化和代谢动力学的研究；绿原酸在肠中存在广泛的代谢。     

Oral antipyretic therapy: Evaluation of the N-aryl-anthranilic acid derivatives mefenamic acid,tolfenamic acid and flufenamic acid

Summary The antipyretic activity of three N-aryl-anthranilic acid derivatives, mefenamic acid, tolfenamic acid and flufenamic acid, was compared and their optimal antipyretic dose determined in a trial in 87 children (aged 5 months to 15 years), who suffered from infections and fever exceeding 38.5°C. Tolfenamic acid proved to be the most potent antipyretic agent of the three drugs; it was eight times more powerful than mefenamic acid and three times more powerful than flufenamic acid. The optimal antipyretic doses were: mefenamic acid 4 mg/kg, tolfenamic acid 0.5 mg/kg and flufenamic acid 1.5 mg/kg. It is evident that the antipyretic activity of these anthranilic acid derivatives is even greater than their antirheumatic effect, the difference being most noticeable in the case of tolfenamic acid.     

系列甘草次酸衍生物的合成与波谱测定

目的:合成一系列的甘草次酸衍生物,并对其进行波谱测定。方法:对甘草次酸30位羧基进行修饰,合成甘草次酸甲酯和甘草次酸乙酯;对甘草次酸3位羟基进行修饰,合成甘草次酸甲酯-3-O-乙酸酯和甘草次酸乙酯-3-O-乙酸酯;对甘草次酸11位羰基进行修饰,合成脱氧甘草次酸和脱氧甘草次酸甲酯;对合成物进行波谱测定。结果:合成的甘草次酸衍生物经紫外、红外、质谱、核磁共振氢谱与碳谱的鉴定,均为目标化合物。结论:合成的甘草次酸衍生物可为其后续抗炎活性及毒副作用的研究奠定基础。     

Two new triterpenoids from the resin of Boswellia carterii

Two new triterpenoids, 3-oxotirucalla-7,9(11),24-trien-21-oic acid (1) and 18Hα,3β,20β-ursanediol (2), along with 15 known triterpenes, α-amyrin, α-boswellic acid, β-boswellic acid, acetyl α-boswellic acid, acetyl β-boswellic acid, 9,11-dehydro-β-boswellic acid, 9,11-dehydro-α-boswellic acid, acetyl 11α-methoxy-β-boswellic acid, 11-keto-β-boswellic acid, acetyl 11-keto-β-boswellic acid, acetyl α-elemolic acid, 3β-hydroxytirucalla-8,24-dien-21-oic acid, elemonic acid, 3α-hydroxytirucalla-7,24-dien-21-oic acid, and 3α-hydroxytirucall-24-en-21-oic acid, were isolated from the resin of Boswellia carterii Birdw.     

海金沙提取物中香豆酸和咖啡酸的测定及稳定性研究

目的建立了海金沙提取物中香豆酸和咖啡酸的测定方法,并研究了二者在不同条件下的稳定性。方法选用E-clipse XDB-C18色谱柱,以甲醇-1%乙酸水溶液作为流动相进行梯度洗脱;考察了光照、放置时间等因素对咖啡酸和香豆酸稳定性的影响。结果香豆酸和咖啡酸得到很好的分离。以水为溶剂,咖啡酸和香豆酸在冷藏避光条件下储存比较稳定。结论为香豆酸和咖啡酸的提取、分析及其相关制剂的生产提供参考。