芫花炮制前后羟基芫花素、芫花素的含量测定

应用双波长薄层扫描法对芫花炮制前后羟基芫花素和芫花素的含量进行了测定对比,结果表明:醋炙芫花中羟基芫花素、芫花素的含量均高于生芫花,不同的醋制品种中其含量亦有差别。     

不同炮制方法对芫花中4种黄酮苷元含量的影响

目的:采用高效液相色谱法分析芫花不同炮制品中4种黄酮苷元成分的含量,研究不同炮制方法对4种成分的影响。方法:采用Hanbon Hedera C18柱(250mm×4.6mm,5μm),流动相甲醇-0.4%醋酸水溶液(70∶30),流速1.0mL.min-1,柱温30℃,检测波长338nm。结果:在线性范围内,木犀草素、芹菜素、3'-羟基芫花素、芫花素4种化合物分离度良好。在相应浓度范围内,4种化合物线性关系良好,r均在0.999 8以上;精密度RSD≤1.64%;平均加样回收率为99.69%～101.70%。结论:该方法快速、准确,适用于芫花不同炮制品中4种化学成分的定量分析。在7种炮制方法中,醋制法(药典)较其他6种方法能明显提高木犀草素、芹菜素、3'-羟基芫花素、芫花素的含量,同时能提高总黄酮苷元含量。     

白木香叶中黄酮类成分结构与抗氧化功能的相关性研究

目的：研究白木香叶中黄酮类成分清除O2^·-,H2O2,·OH的能力,探讨其抗氧化活性与结构的关系。方法：对白木香叶中黄酮类成分进行分离,采用化学发光法,测定所得成分对邻苯三酚-鲁米诺-碳酸缓冲液体系产生的超氧阴离子（O2^·-）,H2O2-鲁米诺-碳酸缓冲液体系产生的过氧化氢（H2O2）,以及邻菲罗啉-Cu2＋-抗坏血酸-H2O2体系产生的羟自由基（·OH）的清除能力。结果：分得6种黄酮类成分,经鉴定分别为：洋芹素-7,4′-二甲醚（Ⅰ）、5-羟基-7,3′,4′-三甲氧基黄酮（Ⅱ）、木犀草素-7,4′-二甲醚（Ⅲ）、芫花素（Ⅳ）、木犀草素（Ⅴ）、羟基芫花素（Ⅵ）。6种黄酮类化合物具有良好的清除自由基活性。构效关系分析显示,其清除超氧阴离子（O2^·-）、过氧化氢（H2O2）、羟自由基（·OH）的活性强弱与母核上连接的酚羟基数目和位置直接相关。结论：白木香叶中的黄酮类成分具有明显的清除自由基活性,可能为白木香叶的主要抗氧化活性成分。     

Antioxidant effects of Genkwa flos flavonoids on Freund׳s adjuvant-induced rheumatoid arthritis in rats

Ethnopharmacological relevance

Genkwa flos (Daphne genkwa Sieb. et Zucc.), a Chinese herbal medicine, has been traditionally used for over two thousand years in China for inflammation related symptoms, including joint pain. To evaluate the antioxidative effects of flavonoid aglycones (FA) isolated from Genkwa flos on adjuvant arthritis in rats and to identify the relationship between antioxidant potential and whole blood viscosity (WBV).

Materials and methods

FA compounds were identified using LC–MS and the content was assayed by HPLC. Arthritis was induced by an intradermal injection of Freund?s complete adjuvant in the footpad. The effects of FA on paw volumes, secondary arthritis scores, histopathology of joints, and body and organ weights were measured. The antioxidant effects of FA and WBV were determined.

Results

LC–MS analysis showed that the FA contained four major compounds: luteolin, apigenin, hydroxygenkwanin and genkwanin. FA significantly decreased paw edema, arthritis scores, and weight loss. These observations were consistent with the reduction of oxidative stress and the improvement of the WBV.

Conclusion

FA significantly decreased arthritis in a rat model through antioxidant and hemorheological modulatory mechanisms. The Genkwa flos flavonoids may have clinical potential for the treatment of rheumatoid arthritis.     

薄层扫描法测定芫花中芫花素含量

采用薄层扫描法对芫花不同工艺炮制品中的芫花素进行了含量测定,结果表明芫花不同工艺的炮制品中其含量为0.128%～0.389%,回收率为98.8%,为芫花的最佳炮制工艺筛选提供了部分参考依据。     

大孔吸附树脂分离纯化芫花黄酮苷元工艺研究

目的:研究考察大孔吸附树脂用于芫花中2种主要黄酮苷元-芹菜素和芫花素的分离纯化效果。方法:采用静态和动态吸附法,利用高效液相对芹菜素和芫花素进行定量分析,筛选最佳分离纯化工艺。结果:最佳工艺条件为AB-8树脂,上样液的质量浓度0.1 g.mL-1,吸附流速2 BV.h-1,上样体积5 BV。再以9 BV 95%乙醇洗脱,洗脱流速2 BV.h-1,体积9 BV。经树脂处理后2种黄酮苷元纯度均达到20%以上。结论:大孔树脂对芫花中芹菜素和芫花素具有较好分离纯化效果,优选工艺操作简单、稳定可行。`     

Isolation of flavonoids, a biscoumarin and an amide from the flower buds of Daphne genkwa and the evaluation of their anti-complement activity

As part of an ongoing study aimed at identifying the anti-complement active compound from the flower buds of Daphne genkwa, ten flavonoids, one biscoumarin and one amide were isolated. Their structures were identified from spectroscopic and physicochemical data as genkwanin 5-O-beta-d-primveroside (1), apigenin 7-O-beta-d-glucuronide (2), genkwanin 5-O-beta-d-glucopyranoside (3), apigenin 5-O-beta-d-glucopyranoside (4), genkwanin (5), apigenin (6), luteolin 7-methyl ether (7), luteolin (8), daphnoretin (9), velutin (10), 7-methoxyacacetin (11) and aurantiamide acetate (12). Among them, compounds 9, 10 and 12 were isolated from this plant for the first time. The anti-complement activity of these compounds was tested against the classical pathway of the complement system. Among the compounds, daphnoretin (9) exhibited significant anti-complement activity with an IC(50) value of 11.4 microm, whereas the other compounds were not active in the assay.     

炮制对芫花中芫花素含量的影响

采用薄层扫描法对芫花不同工艺炮制品和全国各大区芫花样品中的芫花素以及将芫花素单体经不同模拟炮制工艺处理的样品进行了含量测定。     

HPLC法分析芫花素模拟醋炙前后的变化

用ＨＰＬＣ法分析了芫花素模拟醋炙前后的变化。结果表明：模拟醋炙前后，芫花素质和量均无明显变化，说明醋酸并非醋炙引起芫花中芫花素含量下降的主要因素。     

HPLC法分析炮制对芫花中芫花素的影响

用HPLC法分析了芫花各种炮制品中芫花素的含量变化。结果表明:芫花经不同方法炮制后芫花素的含量均有所降低,以醋炙降低最少。并对各大区芫花饮片的芫花素含量进行了定量分析,为制订芫花饮片的质量标准提供了实验依据。     

HPLC法测定芫花中芫花素的含量

采用Lichrosorb5RP-18柱,甲醇-水-冰乙酸(65:35:5)为流动相,332nm检测,建立了HPLC测定芫花中芫花素含量的方法,加样回收率为95.46%,RSD为1.15%,测得芫花中芫花素的含量为0.1555%。     

UPLC-QTOF/MS分析芫花诱导人肝细胞L02损伤的毒性物质基础

目的: 研究芫花提取物诱导人肝细胞L02损伤的毒性物质基础。 方法: 选取人肝细胞L02作为体外实验模型,运用MTT法测定芫花提取物对细胞增殖的影响,并且采用超高效液相色谱串联四级杆飞行时间质谱(UPLC-QTOF/MS)对芫花提取物及与L02细胞亲和后胞内化学成分进行定性分析。 结果: 芫花提取物对L02细胞的生长抑制呈明显的剂量依赖关系,48 h的IC₅₀为(48.34±4.66)mg·L^-1。通过UPLC-QTOF/MS鉴定的黄酮类成分主要有:芹菜素、3'-羟基芫花素、芫花素、5,4'-二羟基-7,3'-二甲氧基黄酮;二萜原酸酯类成分主要有:芫花酯戊、genkwanine L、芫花酯丙、芫花烯、芫花酯丁、芫花酯庚、芫花酯乙、芫花酯己、芫花酯甲。在芫花提取物亲和的L02细胞中鉴定出3'-羟基芫花素、芫花素、5,4'-二羟基-7,3'-二甲氧基黄酮、芫花酯戊、芫花烯、芫花酯丁、芫花酯乙、芫花酯甲。其中二萜原酸酯类成分芫花酯甲作用L02细胞48 h的IC₅₀为(29.57±2.01) mg·L^-1,黄酮类成分芫花素(0.1～100 mg·L^-1)未发现对L02有显著的细胞毒作用。 结论: 芫花提取物对人肝细胞L02具有细胞毒作用,其中二萜原酸酯类成分与细胞有明显的亲和作用,并具显著的细胞毒作用,是芫花提取物中主要的活性物质。     

尖萼耧斗菜中黄酮类成分的研究

目的：对尖萼耧菜斗菜进行化学成分研究。方法：利用各种色谱技术进行分离纯化,根据理化性质和光谱分析进行结构鉴定。结果：从该植物中分离得到５个黄酮类化合物,分别鉴定为芫花素,芹菜素,木樨草素,当药甙,日本椴甙。结论：所有化合物均为首次从该植物中分离得到。     

了哥王中的1个新双香豆素

目的:研究了哥王茎皮的化学成分。方法:通过硅胶、ODS柱色谱分离化合物,利用质谱、核磁共振等现代波谱技术鉴定化合物结构。结果:分离鉴定了7个化合物,分别鉴定为西瑞香素(Ⅰ)、5,7,4′-三羟基-3′,5′-二甲氧基黄酮(Ⅱ)、胡萝卜苷(Ⅲ)、β-谷甾醇(Ⅳ)、伞形花内酯(Ⅴ)、芫花素(Ⅵ)、6-′OH,7-O-7′-双香豆素(Ⅶ)。结论:化合物Ⅶ为新化合物,化合物Ⅲ,Ⅴ为首次从该植物中分离得到。     

十枣汤理法应用

十枣汤主治太阳中风,有形之水客居胸胁之悬饮证。由甘遂、大戟、芫花、大枣四味组成,乃张仲景治水常用方剂,《伤寒论》、《金匮要略》均有论述。《外台秘要》引深之朱雀汤,即本方。现代药理作用已有报告。用药时间《伤寒论》指明在六经病"欲解时","平旦服";热则行、凉则滞,欲期冀其药扬辛开之性,又不失苦降之能故当温服。用法有枣汤送服、先服枣汤、枣肉为丸、体外贴敷、枣汤煎服、枣肉夹粉等。十枣汤实为峻下逐水之剂,具猛、毒之性,运用应遵循"衰其大半而止"原则。现代医家扩大治疗各种水饮停聚胸腹属邪实之证,以结核性渗出性胸膜炎、肝硬化腹水、肾性水肿等病应用最为广泛。在妇科、骨科创伤并发症、眼科、心包积液应用,也取得一定研究进展。     

Active components from Artemisia iwayomogi displaying ONOO(-) scavenging activity

Peroxynitrite (ONOO(-)) is one of cytotoxic species produced by the reaction between superoxide (*O(2) (-)) and nitric oxide (NO). The main aim of this study was to identify ONOO(-) scavenging constituents from herbs. Methanolic extracts derived from one hundred thirty eight herbs were screened out for their ONOO(-) scavenging activities. Twenty herbs showed excellent ONOO(-) scavenging activity in a dose dependent manner. Of them, Artemisia iwayomogi, which showed the highest activity, was fractioned with several solvents. The ONOO(-) scavenging activity of fractions was in order of ethyl acetate (EtOAc) > n-butanol (BuOH) > dichloromethane (CH(2)Cl(2)) > water (H(2)O) fraction. The EtOAc and the n-BuOH fractions were further purified to isolate active principles by column chromatography. Apigenin 7-methylether (genkwanin), apigenin 7,4'-di-O methylether, jaceosidin, and scopoletin from the EtOAc fraction and chlorogenic acid, 2,4-dihydroxy 6-methoxy acetophenone 4-O-beta-D-glucoside, quebrachitol, and scopolin from the n-BuOH fraction were identified. The scavenging activities of chlorogenic acid (IC(50) = 0.52 +/- 0.04 microM), genkwanin (IC(50) = 1.01 +/- 0.10 microM), and scopoletin (IC(50) = 1.03 +/- 0.15 micro M) were higher than or comparable to a well-known ONOO(-) scavenger, penicillamine (IC(50) = 1.76 +/- 0.18 microM), suggesting that those compounds might be developed as effective ONOO(-) scavengers for, prevention of the ONOO(-)-involved diseases.     

舒肺贴提取工艺优选研究

目的：优选复方制剂舒肺贴中芫花、延胡索等药物的提取工艺。方法：采用单因素考察、正交试验,以高效液相色谱法测定提取液中芫花素的含量,优选最佳提取工艺。结果：70%乙醇10倍量回流提取3次,每次1 h为最佳提取工艺。结论：优化后的工艺合理、稳定、可行,适于舒肺贴中芫花等药物的精制提取。     

芫花不同药用部位芫花素和芫花酯甲含量比较

目的比较芫花根、叶、花蕾中芜花素和芫花酯甲含量差异,为该植物资源的可持续发展提供试验数据。方法采用高效液相色谱法,色谱柱为Kromasil C18柱（4．6mm×250mm,5μm）,芫花素流动相为甲醇-水-冰醋酸（65：35：0．5）,流速0．8mL／min,柱温为40℃,检测波长338nm;芜花酯甲流动相为甲醇-水（82：18）,柱温为40℃,流速1．0mL／min,检测波长233nm。结果芫花素在3个部位中的含量从高到低依次为：花蕾（0．30％）、叶（0．038％）,根申未检测到该成分;芫花酯甲在3个部位中的含量从高到低依次为：叶（0．028％）、根（0．025％）、花蕾（0．0039％）。结论以叶代根、花蕾提取芫花酯甲,可以拓宽药源,实现植物资源的可持续发展。     

炮制对芫花毒性和药效的影响

芫花为毒性较强的中药，为保证临床用药安全有效，须炮制后供用。本文探讨炮制对芫花毒性和药效的影响。结果表明：醋炙品毒性较小，利尿作用较强。芫花素及其模拟醋炙品均有镇咳祛痰作用，作用强度二者无显著差异。芫花酯甲及其模拟醋炙品１∶１×１０^－５～１×１０^－６浓度均可引起离体子宫及肠管收缩，但二者作用强度未见明显差异。对未孕大鼠及妊娠子宫作用比较，妊娠大鼠子宫更敏感。     

Flavonoid glycosides from the stem bark of Margaritaria discoidea demonstrate antibacterial and free radical scavenging activities

One new flavonoid glycoside, along with three known flavonoid glycosides were isolated from the stem bark of Margaritaria discoidea, which is traditionally used in the management of wounds and skin infections in Ghana. The new flavonoid glycoside was elucidated as hydroxygenkwanin‐8‐C‐[α‐rhamnopyranosyl‐(1 → 6)]‐β‐glucopyranoside (1) on the basis of spectroscopic analysis. The isolated compounds demonstrated free‐radical scavenging as well as some level of antibacterial activities. Microorganisms including Staphylococcus aureus are implicated in inhibiting or delaying wound healing. Therefore, any agent capable of reducing or eliminating the microbial load present in a wound as well as decreasing the levels of reactive oxygen species may facilitate the healing process. These findings therefore provide some support to the ethnopharmacological usage of the plant in the management of wounds. Copyright © 2013 John Wiley & Sons, Ltd.