大豆植物提取物的抗炎和镇痛作用研究

目的:研究大豆植物提取物的抗炎、镇痛作用。方法:采用小鼠耳廓肿胀法、大鼠卵白蛋白致足肿胀法、大鼠棉球肉芽肿法、小鼠热板法和小鼠扭体法。结果:大豆植物提取物能抑制二甲苯引起的小鼠耳廓炎性肿胀和大鼠卵白蛋白性足肿胀,并能减轻大鼠棉球肉芽肿重量,说明大豆植物提取物有明显的抗炎作用。镇痛试验表明,大豆植物提取物能显著提高热板试验小鼠的痛阈,有效抑制冰醋酸引起的小鼠扭体反应次数。结论:大豆植物提取物具有抗炎和镇痛作用。     

灰毡毛忍冬芽提取物的抑菌活性及其镇痛抗炎解热作用的研究

目的：观察灰毡毛忍冬芽提取物的抑菌活性和镇痛抗炎解热作用。方法：采用平板纸片法和微孔稀释法观察其抑菌活性并考察其抑菌稳定性;以小鼠福尔马林致痛及醋酸扭体实验观察其镇痛作用;以小鼠耳廓肿胀模型和角叉菜胶致大鼠足肿胀模型观察其抗炎作用;用酵母致动物发热法观察其解热作用。结果：灰毡毛忍冬芽提取物对金黄色葡萄球菌、大肠杆菌、八叠微球菌、绿脓杆菌、枯草芽孢杆菌和伤寒杆菌均有抑菌效果,其MIC分别为375、187.5、93.75、187.5、187.5、187.5mg·mL-1,MBC分别为1500、750、375、1500、750、1500mg·mL-1。提取物在pH1～3的酸性条件下抑菌效果最好,但高温长时间处理和紫外光长时间照射均可降低其抑菌活性;与纯水组相比,生药含量为15g·kg-1的灰毡毛忍冬芽提取物组能显著提高小鼠福尔马林实验中的痛域,减少醋酸所致小鼠的扭体次数,对二甲苯所致小鼠耳廓的肿胀度抑制率达36.62%,可以抑制角叉菜胶所致的大鼠足肿胀,并能有效对抗酵母所致大鼠的体温升高。结论：灰毡毛忍冬芽提取物在体外对金黄色葡萄球菌、大肠杆菌、八叠微球菌、绿脓杆菌、枯草芽孢杆菌和伤寒杆菌均有良好的抑菌效果,并具有一定的镇痛、抗炎、解热作用。     

七叶莲果实的抗炎镇痛作用研究

目的:研究七叶莲果实水提物的抗炎镇痛作用。方法:采用热板法疼痛模型、醋酸诱发的小鼠扭体疼痛模型评价水提物的镇痛作用和二甲苯致小鼠耳廓肿胀模型评价水提物的抗炎作用。结果:七叶莲果实水提物对热板、醋酸导致的疼痛,二甲苯所致的耳廓肿胀均有不同程度的抑制作用。结论:七叶莲果实水提物有较强的抗炎镇痛作用。     

苦荞籽提取物的抗炎镇痛作用和急性毒性试验研究

目的：研究苦荞籽乙醇提取物的抗炎镇痛作用和急性毒性。方法：采用二甲苯致小鼠耳肿胀法和大鼠蛋清性足肿胀法观察抗炎作用;采用小鼠热板法和醋酸扭体法观察镇痛作用;用最大浓度,最大给药体积的药液灌胃给药。结果：苦荞籽提取物可明显抑制二甲苯所致小鼠耳廓的肿胀度,抑制蛋清所致大鼠足肿胀;可提高热板所致小鼠痛阈值,减少醋酸所致小鼠的扭体次数;最大给药量为374.5g/kg bw,相当于成人日用量的1498 倍。结论：苦荞籽提取物具有明显抗炎镇痛作用,无明显毒性。     

陈皮中柠檬苦素的响应面提取及其抗炎作用研究

以陈皮为原料,研究陈皮柠檬苦素超声辅助提取工艺及其抗炎作用。采用超声提取陈皮柠檬苦素,利用响应面分析法优化其提取工艺,并对陈皮柠檬苦素对小鼠植入棉球致肉芽肿和小鼠扭体产生抑制作用进行分析。表明陈皮柠檬苦素萃取最佳工艺条件为:液料比32∶1(m L/g)。超声功率为265.1 W,超声提取时间为30 min,乙醇体积分数为85.3%。对小鼠植入棉球致肉芽肿研究表明陈皮柠檬苦素有较强的抗炎作用。     

妇炎清胶囊抗炎镇痛作用的实验研究

目的　观察妇炎清胶囊的抗炎、镇痛药理作用。方法　采用热板法和扭体法观察胶囊对小鼠的镇痛作用,采用小鼠耳肿胀法观察胶囊的抗炎作用。结果　妇炎清胶囊低、高剂量均可显著提高1h、1 .5h小鼠痛阈百分率,并呈剂量依赖关系;能显著减少醋酸所致小鼠扭体的次数;显著减轻二甲苯致炎小鼠的耳郭肿胀度,并呈剂量依赖关系。结论　动物实验表明妇炎清胶囊具有明显的抗炎镇痛作用,与临床疗效相符。     

氧化苦参碱体内抗炎作用的实验研究

目的:观察苦豆子提取物氧化苦参碱(Oxymatrine,OMT)的体内抗炎作用。方法:采用角叉菜胶(Carrageenin)、二甲苯(Xylene)和冰醋酸(Acetic acid)制作动物炎症模型,设置OMT高、中、低、剂量组、阳性药物对照组以及空白对照分组并灌胃给药,测量抗炎指标。结果:氧化苦参碱低、中、高剂量组可降低小鼠耳廓肿胀度(P<0.05);氧化苦参碱中、高剂量组均可减少实验小鼠扭体的次数及缓解大鼠足部的肿胀度(P<0.05);氧化苦参碱对小鼠体重和死亡率没有显著影响。结论:氧化苦参碱具有明显的体内抗炎作用。     

新疆哈萨克族传统发酵驼乳抗炎作用的初步研究

研究了新疆哈族传统发酵发酵驼乳的抗炎作用及抗炎机制。急性抗炎模型采用角叉菜胶致小鼠足肿胀模型，慢性抗炎模型采用棉球植入大鼠腋下致肉芽肿模型和角叉菜胶致大鼠背部气囊滑膜炎模型，测定渗出液液体量，渗出液中白细胞计数、C-反应蛋白（CRP）、丙二醛（MDA）含量及血清中CRP和MDA，以布洛芬作为阳性对照，观察发酵驼乳的抗炎作用。结果表明，新疆哈族传统发酵发酵驼乳对角叉菜胶致小鼠足肿胀和棉球致大鼠肉芽肿形成均有显著的抑制作用，传统发酵发酵驼乳能明显减少角叉菜胶致大鼠背部气囊滑膜炎模型渗出液体量，降低灌洗液中WBC数量和血清中CRP和MDA含量。结论是发酵驼乳具有显著的抗炎作用，其抗炎机制与抑制炎性因子的渗出、降低CRP含量及消除自由基、抑制脂质过氧化有关。     

菊葛天麻颗粒镇痛作用及对血瘀动物模型的影响

目的探讨菊葛天麻颗粒(JGTM)的镇痛作用及对血瘀动物模型的影响。方法采用扭体法、热板法观察JGTM对小鼠的镇痛作用;采用大鼠体内血栓形成试验,肾上腺素致小鼠耳廓微循环障碍试验,观察JGTM的活血化瘀作用。结果JGTM可明显延长小鼠疼痛潜伏期,减轻H+所致小鼠疼痛扭体反应,明显提高热板法所致小鼠的痛阈值;具有延长大鼠体内血栓形成时间,拮抗肾上腺素所致血瘀小鼠耳廓微循环障碍的作用。结论 JGTM具有镇痛作用及活血化瘀的作用。     

椪柑中类柠檬苦素提取及产业化研究

柠檬苦素类似物是一类具有广泛生物活性的三萜化合物,富含于柑桔属的橘、橙、柚中.本文重点概述了椪柑中柠檬苦素的含量分布和提取纯化的方法,并探讨椪柑中柠檬苦素所具有的抗肿瘤、抗病毒、镇痛、抗炎、抗氧化等功能的产业化应用开发.     

Biochemistry and biological functions of citrus limonoids

Abstract

Limonoids are one of bitter principles in citrus juices. Excessive bitterness lowers the quality and value of citrus juices. Nomilin is considered to be the precursor of all other limonoids accumulated in Citrus and related species. It is biosynthesized from acetate via the terpenoid biosynthetic pathway in the phloem region of stems and then translocated to the leaves, fruit tissues, peels, and seeds where it is further metabolized to other limonoids. The citrus limonoid aglycones are then glucosidated by limonoid UDP‐D‐glucose transferase in maturing fruit tissues and seeds. These limonoid glucosides are accumulated in such high concentrations that they are one of major secondary metabolites in citrus fruit tissues, and they play an important role in fruit quality and possibly in human health. Research on creation of transgenic citrus trees that produce fruits free of the limonoid bitterness problem is in progress. Limonoids have been shown to induce glutathione S‐transferase activity and inhibit the formation of certain chemically induced carcinogenesis in laboratory animals. Some of the limonoids possess antifeedant activity against insects, suggesting that one of the biological functions of limonoids in plants is pest control. The citrus limonoids are unique for many species and varieties, and make excellent taxonomic markers. Thus, limonoids are important citrus constituents to citrus growers, processors, breeders, and the consumer.     

Limonoids as cancer chemopreventive agents

Nutritional research on the health benefits of substances in plant foods has recently advanced to a new stage. The research frontier has moved from study of classical vitamin deficiency diseases to study of the thousands of phytochemicals that may have important physiological effects. Recent research suggests that citrus fruit consumers may be getting another health benefit from orange juice and other citrus products called limonoids, which appear to possess substantial anticancer activity. Limonoids are highly oxidized triterpenes present in Rutaceae and Maliaceae families. Several citrus limonoids have recently been subjected to anticancer screening utilizing laboratory animals and human breast cancer cells. The experimental results described that citrus limonoids may provide substantial anticancer actions. The compounds have been shown to be free of toxic effects in animal models, so potential exists for the use of limonoids against human cancer in either natural fruits, in citrus fortified with limonoids, or in purified forms of specific limonoids. Although the initial studies are very promising they have been conducted primarily with in vitro cell culture and animal models. Thus, research is needed to determine whether the limonoids may be useful in preventing or treating cancer in humans. Copyright © 2005 Society of Chemical Industry     

柑橘果汁中的类柠檬苦素及其脱苦方法

介绍了柑橘果汁中的类柠檬苦素苦味，类柠檬苦素苦味物质的结构，由类柠檬苦素引起的后苦味的形成机理．以及目前研究的类柠檬苦素苦味物质的脱除方法。     

茵陈黄酮的抗氧化及镇痛作用研究

对茵陈黄酮体外抗氧化活性及对小鼠致痛作用的抑制研究表明,与Vc相比,在体外实验中,茵陈黄酮粗提物和茵陈黄酮纯化物对.OH基和DPPH自由基具有良好的清除能力,对花生油氧化有明显的抑制效果,在小鼠体内实验中,茵陈黄酮黄酮粗提物和纯化物可显著降低由腹腔注射醋酸引起的小鼠扭体次数,茵陈黄酮纯化物对小鼠小鼠扭体反应的抑制力达到60.67%,同时也可减少热刺激和甲醛诱导的小鼠舔足次数,说明茵陈黄酮对化学物质和炎症引起的疼痛均具有一定的缓解作用。茵陈黄酮抗氧化及镇痛活性显著。     

柠檬皮中柠檬苦素对根霉的抑菌活性和机理

通过测定柠檬皮中柠檬苦素对根霉的最小抑菌浓度(MIC)、最小杀菌浓度(MBC)、孢子萌发抑制率、菌丝萌发抑制率确定其抑菌活性,根据测定各因素对抑菌活性的影响确定抑菌活性的稳定性;并通过扫描电镜观察和测定根霉细胞外碱性磷酸酶(AKP)含量和蛋白质含量,菌丝体的总糖含量,分析柠檬皮中柠檬苦素对根霉的抑菌机理。结果表明:柠檬皮中柠檬苦素对根霉的最低抑菌浓度(MIC)和最小杀菌浓度(MBC)分别为1250、5000 μg/mL;对根霉孢子萌发的抑制效果更强,对孢子萌发和菌丝生长抑制的EC₅₀值分别为918.34和1707.31 μg/mL。柠檬苦素对根霉的抑菌活性不受温度和明胶的影响;pH为4时,抑菌活性最强;Fe3+、Fe2+均能显著(p<0.05)提高柠檬苦素的抑菌活性。柠檬苦素能使根霉的糖、蛋白质、AKP等胞内物质渗出;扫描电镜观察也发现经柠檬苦素处理的根霉孢子凹陷和皱缩严重,且溶出物明显;菌丝出现断裂扭曲、变形、变细。因此,柠檬苦素能破坏根霉的细胞壁和细胞膜的完整性,使胞内物质渗出,菌丝体和孢子变形,从而使根霉生长代谢受到影响。     

Purification of citrus limonoids and their differential inhibitory effects on human cytochrome P450 enzymes

Recent studies demonstrated that citrus limonoids and flavonoids possess numerous health promoting properties. In the present study, glucosides of limonoids and flavonoids were purified from citrus molasses and limonoid aglycones from citrus seeds. Glucosides were separated on styrene (divinylbenzene), Q‐sepharose resins with increasing concentration of sodium chloride. A pH‐dependent cold precipitation was carried out for the isolation of naringin in large quantity. Major aglycones such as limonin and nomilin were isolated from seeds by direct crystallization and minor limonoids were purified by vacuum liquid chromatography. The structures of the isolated compounds were confirmed by NMR spectra. Individual limonoids were tested for O‐dealkylase and hydroxylase activities of human cytochrome P450 (CYP) isoenzymes such as CYP1A2, CYP1B1, CYP3A4 and CYP19, using ethoxyresorufin, methoxyresorufin and dibenzylfluorescein as substrates. Partial to high inhibition of CYPs was observed in dose‐dependent assays. Significant (P < 0.001) reductions in enzyme activities were observed with purified compounds above 2 µmol. Kinetic analyses indicated that limonin glucoside inhibited CYP19 competitively (IC₅₀, 7.1 µ mol L^?1), whereas Nomilinic acid glucoside inhibited it noncompetitively (IC₅₀, 9.4 µ mol^?1). Nomilinic acid glucoside was the most potent limonoid, with an overall IC₅₀ of < 10 µ mol, for all the enzymes tested. The differential inhibition of CYPs can be ascribed to structural variations of the limonoid nucleus. Limonoid inhibition of key CYPs involved in carcinogenesis supports growing evidence that citrus limonoids act as anticancer agents. Copyright © 2007 Society of Chemical Industry     

柑橘加工副产物中有效成分开发利用的研究进展

本文综述了柑橘类果实加工副产物中有效成分，包括香精油、柑橘果胶、桔皮色素、膳食纤维、黄酮类化合物和类柠檬苦素的功能特性，详细介绍了国内外对这些副产物的开发利用进展概况，并对我国柑橘副产物的加工利用提出建议。     

An Overview on Chemical Aspects and Potential Health Benefits of Limonoids and Their Derivatives

Limonoids are heavily oxygenated, modified triterpenes dominant in Meliaceae and Rutaceae plant families. The term ‘limonoid’ is derived from limonin, which was first identified as the bitter constituent of Citrus seeds in 1841. This group of secondary metabolites exhibits a wide range of biological properties, including anticancer, antibacterial, antifungal, antimalarial, and antiviral activities. Significant progress on the role of limonoids as promising candidates for cancer chemoprevention and/or therapy has been achieved in particular in recent years. The aim of this review article is to discuss the recent developments on limonoids chemical aspects and biological activities with the relationship between structure and activity, supporting the new possibilities for the medicinal and/or nutraceutical use of these compounds.