Acetylcholinesterase Inhibition,Antioxidant, Antiinflammatory,Antimicrobial and Phytochemical Properties of Huernia hystrix

Huernia species are typical famine‐food plants consumed in southern Ethiopia. H. hystrix is a heavily exploited ethnomedicinal succulent plant traded in traditional medicine systems especially on South Africa's eastern seaboard. This study investigated the acetylcholinesterase (AChE) inhibition, antioxidant, antiinflammatory and antimicrobial properties of extracts obtained from the stems and roots of this plant. At the same concentration level (625.0, 312.5 or 156.3 µg/mL), the whole plant extract showed higher AChE inhibitory activity when compared with the stem and root extracts; a finding suggesting the presence of AChE inhibitors acting additively or synergistically in the whole plant extract. The roots showed strong antioxidant activity (in DPPH and β‐carotene assays) comparable to that of butylated hydroxytoluene (BHT), indicating the presence of potent antioxidant compound(s) that can be exploited as alternatives for use in the food and cosmetic industries and/or as nutraceuticals. All the petroleum ether (PE) (except root PE) and dichloromethane (DCM) extracts demonstrated good inhibitory activity (> 70%) in cyclooxygenase (COX‐1 and COX‐2) assays at a 0.25 µg/μL concentration. Most of the extracts showed broad‐spectrum inhibitory and lethal activities against the microorganisms used in this study. The observed biological activities might be due to the iridoid, phenolic and flavonoid contents of the plants. Copyright © 2011 John Wiley & Sons, Ltd.     

Antibacterial constituents of Alchornea cordifolia leaves

Alchornea cordifolia (Euphorbiaceae), a traditional African medicinal plant, is widely distributed in West Africa. A number of phenolic acids, notably gallic acid, protocatechuic acid, quercetin, quercetin arabinose and galactose glycosides, together with triisopentenyl guanidine were isolated from a methanolic extract of the leaves. The first two, and last one of these compounds showed considerable antibacterial activity.     

小檗碱类成分对乙酰胆碱酯酶的抑制作用及血脑屏障透过性分析

目的 从药靶结合亲和力和动力学角度研究非洲防己碱等小檗碱类成分对乙酰胆碱酯酶的抑制作用;并在不同多成分背景下研究这类成分的血脑屏障透过性。方法 采用Ellman改良的光度检测法测量非洲防己碱等小檗碱类成分对乙酰胆碱酯酶的半数抑制浓度（IC₅₀）;采用酶活恢复方法测定这类成分与乙酰胆碱酯酶结合的动力学参数（K_off）;采用超高效液相色谱-高分辨率质谱法（UPLC-HRMS）对各成分在不同背景下（药材与复方）透过血脑屏障到达脑组织的定性分析。结果 非洲防己碱等小檗碱类成分对乙酰胆碱酯酶有较强的抑制活性,其IC₅₀可达到纳摩尔级,并且多个生物碱成分具有优于阳性药盐酸多奈哌齐的药靶结合动力学特征（更小的K_off,P<0.01）,表明该类成分可在乙酰胆碱酯酶上持续更长时间的抑制;非洲防己碱等小檗碱类成分以单体形式、以及在黄连和黄柏药材提取物和复方黄连解毒汤的多成分背景下都可以透过血脑屏障到达脑组织。结论 非洲防己碱等小檗碱类成分对乙酰胆碱酯酶具有较强的抑制作用且在多种成分背景下均可入脑。这在药效物质基础层面上可以佐证临床上复方黄连解毒汤改善阿尔茨海默病的效果,为阐明复方黄连解毒汤的药效物质基础提供了数据支持。     

Antioxidant/Antibacterial Activities of a Topical Phytopharmaceutical Formulation Containing a Standardized Extract of Baccharis incarum,an Extremophile Plant Species from Argentine Puna

The antimicrobial and antioxidant activities of standardized extracts of Baccharis incarum in 60° and 80° ethanol and of a phytopharmaceutical formulation obtained from them were measured. Baccharis tinctures showed antimicrobial activity against clinically isolated antibiotic resistant Staphylococcus aureus and Enterococcus faecalis, with MIC values of 40–80 µg GAE/mL. Both tinctures exhibited ABTS^●+ scavenging activity with SC₅₀ values between 1.6 and 4.0 µg GAE/mL. The tinctures were not genotoxic in the Salmonella assay. For this reason, the tincture in 60° ethanol was incorporated into a topical pharmaceutical formulation (Hydrogel/ Carbopol® 934). The phytopharmaceutical formulation also showed antibacterial and antioxidant activities in the in vitro assays. The hydrogel showed microbiological, chemical, physical and functional stability during storage at room temperature. Studies that measure drug release as a determination of bioavailability were also carried out using the Franz diffusion cell (FC). The results demonstrated the release of two bioactive compounds (chlorogenic acid and 4′,5‐dihydroxy‐3′,3,6,7,8‐pentamethoxyflavone) from the phytotherapic preparation in HPLC studies of FC receptor solution. In consequence, the phytopreparation applied topically could be used to treat skin and soft tissue infection produced by methicillin‐resistant Staphylococcus aureus (MRSA) or Enterococcus faecalis and opens new opportunities for the use of active natural ingredients in the cosmeceutical field as antiacne and antioxidant. Copyright © 2012 John Wiley & Sons, Ltd.     

姜黄素衍生物的合成、表征及其体外抗菌活性

目的:研究姜黄素衍生物的合成,表征以及体外抗菌活性。方法:基于姜黄素分子结构含有两个羰基的特点,采用苯胺,4-甲基苯胺,苯肼,2,4-二硝基苯肼以及姜黄素为原料,合成4种稳定的姜黄素Schiff碱衍生物;并对其进行体外抗菌活性测定。结果:合成了4种姜黄素Schiff碱,其中3个未见文献报道,并采用元素分析、紫外、红外以及核磁氢谱对其结构进行表征。4种化合物体外均有抗菌活性。结论:4种姜黄素衍生物都有一定的抗菌活性,其中Schiff碱(4)的抗菌活性较好。     

痰热清注射液化学成分、药理作用及临床应用研究进展

痰热清注射液具有清热、化痰、解毒的功效,主要含有氨基酸类、环烯醚萜类、黄酮类、苯乙醇苷类、甾体类等化学成分,具有抗炎、抗菌、抗病毒、抑制肝损伤等药理活性。近年来,国内外学者对痰热清注射液做了大量的研究工作。对其化学成分、药理活性及临床应用进行综述,以期为痰热清注射液的进一步研究提供参考。     

双黄连制剂中酚酸与黄酮类成分的含量测定及药代动力学分析

目的:建立同时测定大鼠灌服双黄连制剂后血浆中酚酸类(新绿原酸、绿原酸及隐绿原酸)与黄酮类(黄芩苷、千层纸素A-7-O-β-D-葡萄糖苷、汉黄芩苷、黄芩素、汉黄芩素及千层纸素A)成分的超高效液相色谱-串联质谱法(UPLC-MS/MS),并研究其药代动力学。方法:血浆样品采用乙酸乙酯-正丁醇(1∶1)萃取,流动相0.4%甲酸水溶液-[乙腈-甲醇(4∶1)混合液]梯度洗脱,流速0.4 m L·min-1,采用电喷雾离子化,多反应监测离子扫描模式,选用响应较高的正离子模式。结果:建立的同时测定血浆中9种成分的UPLC-MS/MS线性良好(R20.992),精密度RSD均14.2%,准确度85.49%~114.76%,复方中新绿原酸、绿原酸、隐绿原酸、黄芩苷、千层纸素A-7-O-β-D-葡萄糖苷、汉黄芩苷、黄芩素的药时曲线下面积AUC0-t与AUC0-∞与单味药提取物相比显著增加,而酚酸和黄酮类成分的消除速率较单味药提取液缓慢。结论:建立的UPLC-MS/MS特异、快速、准确及灵敏,可用于双黄连制剂中9种主要活性成分在大鼠体内的药代动力学研究。     

雄黄超高压射流粉表征及抑菌效果

目的:研究经超高压射流粉碎后雄黄表征差异,探讨粉体粒径对抑菌效果的影响。方法:利用超高压射流技术对雄黄进行粉碎,比较雄黄普通粉、水飞粉和射流粉的粉体表征、体外抑菌效果。结果:雄黄粉体平均粒径由23.756μm降到1.427μm,比表面积由1.251 m2.cm-3增至11.653 m2.cm-3,休止角增大,松密度降低,主要成分无明显变化;对大肠杆菌最低抑菌浓度(MIC)由8%降到2%,对金黄色葡萄球菌MIC由1%降到0.5%。结论:雄黄经超高压射流技术粉碎后,粒径明显减小,比表面积显著增大,孔隙率大大增大,流动性变差,主要成分符合《中国药典》规定,体外抑菌效果与粉体粒径大小呈负相关。超高压射流技术用于雄黄粉碎是可行的。     

Cranberry Juice Extract,A Mild Prooxidant with Cytotoxic Properties Independent of Reactive Oxygen Species

A cranberry juice extract (CJE), rich in proanthocyanidins, had weak prooxidant properties, generating low levels of hydrogen peroxide (H₂O₂) and superoxide. Generation of H₂O₂ was pH dependent, increasing at alkaline pH, and was lowered in the presence of catalase and, to a lesser extent, of superoxide dismutase (SOD). Growth inhibition and cytotoxicity were noted towards human oral carcinoma HSC‐2 cells, with midpoint cytotoxicity at 200 µg/mL CJE, but not towards human gingival HF‐1 fibroblasts. Being a mild prooxidant, CJE toxicity was unaffected by exogenous catalase and pyruvate, scavengers of H₂O₂, but triggered intracellular synthesis of reduced glutathione, as confirmed by cell staining with Cell Tracker? Green. The presence of exogenous SOD potentiated the toxicity of CJE, possibly by stabilizing the CJE phenols and hindering their degradative autooxidation. Conversely, ‘spent’ CJE, i.e. CJE added to cell culture medium and incubated for 24 h at 37 °C prior to use, was much less toxic to HSC‐2 cells than was freshly prepared CJE. These differences in toxicity between SOD‐stabilized CJE, freshly prepared CJE, and ‘spent’ CJE were confirmed in HSC‐2 cells stained with aceto‐orcein, which also indicated that the mode of cell death was by the induction of apoptosis. Copyright © 2012 John Wiley & Sons, Ltd.     

Assessment of Cytotoxic Properties of Safranal and Nanoliposomal Safranal in Various Cancer Cell Lines

Saffron (Crocus sativus) is a widely used food additive used for its color and taste. It has been reported that saffron possesses significant in vivo and in vitro anti‐tumor activity. In the present study, anti‐tumor effects of safranal, the major aromatic compound in saffron, and its liposomal form were investigated. The role of apoptosis has also been explored in this toxicity. HeLa, MCF7 and L929 cell lines were cultured and exposed to safranal (0.01–3 mM) or liposomal safranal (0.04–0.32 mM). 3‐(4,5‐Dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium (MTT) assay was performed to assess cytotoxicity. Apoptosis was evaluated by staining cells with propidium iodide and quantifying sub‐Gl peak by flow cytometry. MTT assay revealed a significant and concentration‐dependent cytotoxic effect of safranal on HeLa and MCF7 cell lines. Liposomal safranal showed enhanced effect compared to the safranal solution, as compared by their IC₅₀ concentrations. Flow cytometry results revealed induction of apoptosis by safranal. It might be concluded that safranal could be involved in saffron‐induced cell death in HeLa and MCF7 cells. Liposome encapsulation improved anti‐tumor effect of safranal. Safranal and particularly its liposomal form could be investigated as promising chemotherapeutic agents in cancer treatment. Copyright © 2013 John Wiley & Sons, Ltd.     

Antibacterial activity of flavonoids and their structure–activity relationship: An update review

Based on World Health Organization reports, resistance of bacteria to well‐known antibiotics is a major global health challenge now and in the future. Different strategies have been proposed to tackle this problem including inhibition of multidrug resistance pumps and biofilm formation in bacteria and development of new antibiotics with novel mechanism of action. Flavonoids are a large class of natural compounds, have been extensively studied for their antibacterial activity, and more than 150 articles have been published on this topic since 2005. Over the past decade, some promising results were obtained with the antibacterial activity of flavonoids. In some cases, flavonoids (especially chalcones) showed up to sixfold stronger antibacterial activities than standard drugs in the market. Some synthetic derivatives of flavonoids also exhibited remarkable antibacterial activities with 20‐ to 80‐fold more potent activity than the standard drug against multidrug‐resistant Gram‐negative and Gram‐positive bacteria (including Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus). This review summarizes the ever changing information on antibacterial activity of flavonoids since 2005, with a special focus on the structure–activity relationship and mechanisms of actions of this broad class of natural compounds.     

余甘子总酚酸和总黄酮配伍抑制肝癌细胞增殖及 对免疫功能的调节作用

目的: 观察余甘子总酚酸和总黄酮不同配伍比例对癌细胞的抑制作用及观察对免疫系统的影响。方法: 在96孔培养板中,每孔加入100 μL (含有5 000个／mL肿瘤细胞) RPMI 1640培养液,采用MTT法观察不同配伍比例的余甘子总黄酮和总酚酸对人肝癌细胞株HepG2的体外抑制作用; 将64只小鼠随机分成8组,分别为正常对照组和余甘子总酚酸总黄酮配伍后的给药组,每天ig给药1次,连续9 d,采用MTT法测定小鼠脾淋巴细胞的转化增殖,测定小鼠血清白介素-2(IL-2)和干扰素-γ(IFN-γ)含量,测定不同配伍比例的余甘子总酚酸和总黄酮的免疫调节作用。结果: MTT法测定的结果均显示,不同比例余甘子总酚酸+总黄酮的配伍,对肝肿瘤细胞的抑制作用明显,其中以总黄酮比总酚酸10∶1(110 mg · L^-1∶11 mg · L^-1)时抑制率最高,抑制率为60.35%。余甘子总黄酮与总酚酸配伍能促进小鼠脾淋巴细胞增殖,其中每天以总酚酸329.5 mg ·kg^-1总黄酮228 mg ·kg^-1对小鼠ig给药组脾淋巴细胞增殖率最高,刺激指数比空白组高了0.786。并且促进小鼠淋巴细胞分泌因子的生成。结论: 余甘子总酚酸和总黄酮对肝脏肿瘤细胞增殖有明显的抑制作用,并且能增强机体特异性免疫功能和非特异性免疫功能的作用。     

Angiotensin‐Converting Enzyme Inhibitory Activity and Antioxidant Properties of Nepeta crassifolia Boiss & Buhse and Nepeta binaludensis Jamzad

This article reports phytochemical and biological studies on Nepeta binaludensis and Nepeta crassifolia. Both species were investigated for their angiotensin‐converting enzyme (ACE) inhibitory activity and antioxidant properties through three in vitro models [2,2‐diphenyl‐1‐picrylhydrazyl (DPPH), 2,2'‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulphonic acid) (ABTS) and ferric reducing antioxidant power (FRAP) assay]. Aerial parts were extracted with methanol and partitioned between water and subsequently n‐hexane, ethyl acetate and n‐butanol. N. binaludensis methanol extract exerted significantly higher reducing power (1.9 μM Fe(II)/g) than did the positive control butylhydroxytoluene (63.2 μM Fe(II)/g) in FRAP assay. The highest DPPH radical scavenging activity was found for N. crassifolia, with IC₅₀ values of 9.6 and 12.1 µg/mL for ethyl acetate and n‐butanol fractions, respectively. n‐Butanol fraction of both species showed the highest ACE inhibitory activity, with IC₅₀ values of 59.3 and 81.7 µg/mL for N. binaludensis and N. crassifolia, respectively. Phytochemical investigations resulted in the isolation of ursolic acid, oleanolic acid, apigenin, luteolin and ixoroside. Apigenin‐7‐O‐glucoside, 8‐hydroxycirsimaritin and cirsimaritin were furthermore identified in N. crassifolia ethyl acetate‐soluble fraction. Nepetanudoside B was isolated from the n‐butanol fraction of N. binaludensis. Copyright © 2012 John Wiley & Sons, Ltd.     

The Genus Trollius—Review of Pharmacological and Chemical Research

Three species of the genus Trollius (Ranunculaceae) are traditionally used to treat upper respiratory tract infections, pharyngitis, tonsillitis, bronchitis, cold with fever, acute tympanitis, aphthae, mouth sore, hemorrhage and pain of gums, acute lymphangitis and acute periostitis. However, only a few studies support its traditional use. These are studies of the biological activity of extracts and/or compounds of selected species of Trollius, but there are no clinical studies proving the effectiveness or possible toxic effects. Until now, the following activity of extracts and/or compounds from certain species of Trollius used in traditional medicine has been proven: antiviral, antibacterial, antiinflammatory and antioxidant. The review showed that flavonoids, mainly C‐glycosides, were characteristic of the species Trollius. Furthermore, other main groups of compounds are carotenoids, organic acids, terpenes, alkaloids, sterols, lactones and carbohydrates. The essential oil mainly contains compounds from the group of benzenoids, nitrogen‐containing compounds, monoterpenoids and sesquiterpenoids, irregular terpenes and macrocyclic epoxide. Copyright © 2015 John Wiley & Sons, Ltd.     

含量测定结合指纹图谱筛选泽兰总黄酮(酚酸)精制的树脂类型

目的:研究泽兰总黄酮(酚酸)精制的树脂类型。方法:以总黄酮(酚酸)、咖啡酸含量结合指纹图谱主要特征峰面积转移率为考察指标;采用紫外分光光度法测定总黄酮(酚酸)含量,HPLC法测定咖啡酸含量,HPLC法分析主要特征指纹峰。结果:通过对S-8,D-101,NKA,AB-8,X-5,D-4020,D-301等不同树脂的静态吸附与动态吸附研究表明,S-8型大孔树脂对泽兰的总黄酮(酚酸)类成分有较好的吸附与解吸特性。结论:S-8型大孔树脂适合应用于泽兰总黄酮(酚酸)的分离与纯化。     

药用菊非药用部位的资源化利用现状与展望

菊花Chrysanthemum morifolium是我国传统中药材,其非药用部位的产量远远高于花序,仅菊茎叶产量就为药用部位的3.5倍;长期以来,菊非药用部位未得到充分利用,造成了极大的资源浪费和环境污染,因此,药用菊非药用部位的深入研究与开发值得关注。研究表明,菊非药用部位富含挥发油类、黄酮类、酚酸类以及多糖类等成分,具有抗菌、抗炎、抗氧化、抗惊厥和改善肠道失调等功效。通过对药用菊在栽培和生产过程中所产生的茎、叶、根等非药用部位的化学成分、药理作用及其资源利用现状进行归纳分析,以期为药用菊非药用部位的资源价值发现与产业化提供科学依据和参考。     

Antibacterial Properties of Helianthemum glomeratum,a Plant Used in Maya Traditional Medicine to Treat Diarrhoea

Ethnobotanical studies indicate that Helianthemum glomeratum is a plant widely used in Maya communities to treat diarrhoeas. A possible mechanism to counteract infectious diarrhoea would be by inhibiting the growth of the enteropathogen causing the disease. The aim of this work was to study the antimicrobial activity of H. glomeratum against bacterial enteropathogens isolated from faeces of children with acute diarrhoea or dysentery. A methanol extract obtained from the leaves and stems was highly active against Shigella spp and Vibrio cholerae ; activity against Salmonella spp and Escherichia coli isolates was also present. Acetone/water extract from the roots was also highly active against Shigella and Vibrio isolates. Further chemical fractionation indicated that antibacterial activity was associated with the polyphenolic fraction. Shigella spp causes severe dysentery in children and Vibrio cholerae causes severe watery diarrhoea. Antidiarrhoeal activity of H. glomeratum may be due, at least in part, to the antimicrobial activity of polyphenolics against bacterial enteropathogens commonly associated with the disease. © 1997 by John Wiley & Sons, Ltd.     

夏枯草化学成分及药理作用研究进展

夏枯草Prunella vulgaris为临床常用中药,具有清火明目、软坚散结的功效。夏枯草中主要含有萜类、酚酸类、黄酮类、甾醇类、香豆素类、有机酸类、挥发油类及糖类等成分,具有降压、降糖、抗菌消炎、免疫抑制、清除自由基及抗氧化、抗肿瘤、抑制病毒生长等多种药理作用。查阅近年来国内外文献,对夏枯草的化学成分、药理作用等方面进行综述,为夏枯草的研究和临床应用及进一步开发提供参考。     

Medicinal and edible lignicolous fungi as natural sources of antioxidative and antibacterial agents

The antioxidant activity of organic extracts of eight fungal species, Ganoderma lucidum, Ganoderma applanatum, Meripilus giganteus, Laetiporus sulphureus, Flammulina velutipes, Coriolus versicolor, Pleurotus ostreatus and Panus tigrinus, was evaluated for free radical (DPPH^· and OH^·) scavenging capacity and an effect on lipid peroxidation, and the antibacterial activity was tested by the agar well diffusion method. The highest DPPH^· scavenging activity was found in the methanol extract of G. applanatum (12.5 μg/mL, 82.80%) and the chloroform extract of G. lucidum (510.2 μg/mL, 69.12%). The same extracts also showed the highest LP inhibition (91.83%, 85.09%) at 500 μg/mL, while the methanol extracts of G. applanatum and L. sulphureus showed the highest scavenging effect on OH^· radicals (68.47%, 57.06%, respectively) at 400 μg/mL. A strong antibacterial activity against Gram‐positive bacteria was also manifested. The antioxidative potencies correlated generally with the total phenol content (0.19–9.98 mg/g). The HPLC determination showed that the majority of analysed species contained gallic and protocatechic acids. Consequently, these fungi are shown to be potential sources of antioxidative and antibacterial agents. Copyright © 2010 John Wiley & Sons, Ltd.