Quercetin reduced the formation of N‐acetyl‐p‐benzoquinoneimine,a toxic metabolite of paracetamol in rats and isolated rat hepatocytes

N‐acetyl‐p‐benzoquinoneimine (NAPQI) is toxic metabolite of paracetamol formed primarily by cytochrome P4502E1 (CYP2E1) metabolic pathway when administered at therapeutic doses or overdose. The influence of quercetin (flavonoid) on the bioactivation of paracetamol to NAPQI was investigated using rat liver microsomes and rats in vivo. Paracetamol (80 mg/kg) was administered orally without or with silymarin (100 mg/kg), a known inhibitor of CYP2E1, CYP3A4 and quercetin (10 and 20 mg/kg) to rats for 15 consecutive days. Area under the plasma concentration–time curve (AUC_0‐∞) and the peakplasma concentration (C_max) of paracetamol were dose‐dependently increased with quercetin (10 and 20 mg/kg) compared to paracetamol control group (p < 0.001). On the other hand, the AUC_0‐∞ and C_max of NAPQI were decreased significantly with quercetin. The same results were observed with silymarin also. The elevated liver and kidney functional enzymes/compounds were significantly reduced by quercetin and silymarin compared to paracetamol control group. The formation of NAPQI was reduced in the incubation samples in presence of quercetin in experiment using isolated rat hepatocytes. The presentstudy results revealed that quercetin might be inhibited the CYP2E1‐mediated metabolism of paracetamol; thereby decreased the formation of NAPQI and protected the liver and kidney.     

Antiprotozoal activities of Centipeda minima

In vitro activity against Giardia intestinalis was used for bioassay-guided fractionation of crude extracts from C. minima. The sesquiterpene lactone, brevilin A was isolated and found to have antigiardial activity (IC₅₀ = 16.1 μM) and was similarly active in vitro against Entamoeba histolytica (IC₅₀ between 4.5 and 9 μM) and against Plasmodium falciparum (IC₅₀ = 9.42 μM). Three flavonoids, quercetin, quercetin 3-methyl ether and kaempferol 7-glucosylrhamnoside were also isolated.     

The Antiinflammatory Effect of an Extract of Tripterygium wilfordii Hook F on Adjuvant-induced Paw Oedema in Rats and Inflammatory Mediators Release

Tripterygium wilfordii Hook F (TWH), commonly known as the Thunder-God-Vine, is a popular remedy for rheumatism in southern China. In this study, we investigated the effect of T2 (an extract from TWH) on adjuvant-induced paw oedema in rats and inflammatory mediators. The results showed that an intraperitoneal injection of T2 could significantly decrease the adjuvant-induced paw oedema of rats. During in vitro study, lipopolysaccharide (LPS)-stimulated human mononuclear prostaglandin E₂ (PGE₂) in the culture supernatant was significantly inhibited by T2 at a concentration of 2 μg/mL compared with the control group without T2 treatment (22352±4725 vs 43433±9014 pg/mL, p <0.05). When rat neutrophils were treated with 3 μg/mL of T2, the superoxide production was significantly lower than that of the group without T2 treatment (0.72±0.07 vs 1.37±0.04 nmol, p <0.05). T2 failed to suppress the β-glucuronidase release from rat neutrophils but when the concentration was 30 μg/mL, it expressed a significant inhibition of lysozyme release (20.7±2.9 vs 38.2±4.0 in the control, p <0.05). The findings suggest this Chinese herb, like non-steroid antiinflammatory drugs, expresses a potential antiinflammatory effect through its inhibition of PGE₂ and superoxide function and lysozyme release. © 1997 by John Wiley & Sons, Ltd.     

Herbal formulation “turmeric extract,black pepper,and ginger” versus Naproxen for chronic knee osteoarthritis: A randomized,double‐blind,controlled clinical trial

Osteoarthritis is the most common articular disease that can lead to chronic pain and severe disability. Curcumin—an effective ingredient in turmeric with anti inflammatory property—plays an important role in protecting the joints against destructive factors. Gingerols and piperine, are the effective ingredients of ginger and black pepper, which may potentially enhance and sustain the effect of curcumin in this direction. To determine the effect of cosupplementation with turmeric extract, black pepper, and ginger on prostaglandin E₂ (PGE₂) in patients with chronic knee osteoarthritis, compared with Naproxen. Sixty patients with two different levels of knee osteoarthritis (Grade 2 and 3) were studied. Individuals were randomly assigned to receive daily turmeric extract, ginger, and black pepper together or Naproxen capsule for 4 weeks. PGE₂ was evaluated by ELISA method. 24‐hr recall was also assessed. All of participants completed the study. PGE₂ decreased significantly in both groups (p < .001), but there was no significant differences between groups. The results of this study indicated that intake of the selected herbs twice a day for 4 weeks may improve the PGE₂ levels in patients with chronic knee osteoarthritis similar to Naproxen drug.     

沙棘总黄酮的大鼠肠吸收特性考察

目的:考察沙棘总黄酮在大鼠小肠的吸收特性.方法:运用大鼠在体单向灌流和离体外翻肠囊模型,采用HPLC测定槲皮素、山奈酚、异鼠李素含量,计算沙棘总黄酮在大鼠小肠的吸收参数.结果:沙棘总黄酮中槲皮素、山奈酚、异鼠李素的最佳吸收部位分别为回肠、回肠、十二指肠,吸收速率常数(Ka)分别为3.405×10-2,3.649×10-2,5.671×10-2,沙棘总黄酮质量浓度在50 ～200 mg·L-1时,Ka和表观吸收系数无显著性差异.累积吸收量随药物质量浓度升高呈线性增加.结论:沙棘提取物中3种黄酮类成分均呈现一级动力学特征,吸收机制均为被动扩散,且在小肠有特定吸收部位.     

In vitro protective effects of an aqueous extract of Clitoria ternatea L. flower against hydrogen peroxide‐induced cytotoxicity and UV‐induced mtDNA damage in human keratinocytes

The traditional practice of eating the flowers of Clitoria ternatea L. or drinking their infusion as herbal tea in some of the Asian countries is believed to promote a younger skin complexion and defend against skin aging. This study was conducted to investigate the protective effect of C. ternatea flower water extract (CTW) against hydrogen peroxide‐induced cytotoxicity and ultraviolet (UV)‐induced mitochondrial DNA (mtDNA) damage in human keratinocytes. The protective effect against hydrogen peroxide‐induced cytotoxicity was determined by 3‐(4, 5‐dimethylthiazol‐2‐yl)‐5‐(3‐carboxymethoxyphenyl)‐2‐(4‐sulfophenyl)‐2H‐tetrazolium assay, and mtDNA damage induced by UV was determined by polymerase chain reaction. Preincubation of HaCaT with 100, 250, and 500 μg/ml CTW reduced cytotoxicity effects of H₂O₂ compared with control (H₂O₂ alone). CTW also significantly reduced mtDNA damage in UV‐exposed HaCaT (p < .05). CTW was chemically‐characterized using high resolution liquid chromatography–mass spectrometry. The main compounds detected were assigned as anthocyanins derived from delphinidin, including polyacylated ternatins, and flavonol glycosides derived from quercetin and kaempferol. These results demonstrated the protective effects of C. ternatea flower extracts that contain polyacylated anthocyanins and flavonol glycosides as major constituents, against H₂O₂ and UV‐induced oxidative stress on skin cells, and may provide some explanation for the putative traditional and cosmetic uses of C. ternatea flower against skin aging.     

蒙古黄芪中黄酮类成分抗超氧阴离子活性研究及构效关系分析

 目的研究蒙古黄芪[Astragalus membranaceus(Fish.)Bge.var.mongholicus(Bge.)Hsiao]中有效成分对超氧阴离子(O^2-)的清除能力,并探讨黄酮类物质抗氧化能力与结构之间的关系。方法对蒙古黄芪中的黄酮类成分进行分离,通过化学发光法测定这些成分对邻苯三酚-鲁米诺-碳酸缓冲液(pH10.2)体系产生的超氧阴离子的清除能力。结果从蒙古黄芪中分离出12个黄酮类单体,分别为:槲皮素(Ⅰ),异槲皮苷(Ⅱ),芦丁(Ⅲ),山柰酚(Ⅳ)和异鼠李素(Ⅴ),芒柄花素(Ⅵ),芒柄花苷(Ⅶ),毛蕊异黄酮(Ⅷ),(3R)-8,2′-二羟基-7,4′-二甲氧基异黄烷(Ⅸ),2′,4′-二甲氧基-3′-羟基异黄烷-6-O-β-葡萄糖苷(Ⅹ),(6aR,11aR)-10-羟基-3,9-二甲氧基紫檀烷(Ⅺ),(6aR,11aR)9,10-二甲氧基紫檀烷-3-O-β-D-葡萄糖苷(Ⅻ)。结果表明,所有成分在一定浓度范围内(此浓度范围所对应的清除率在10%～90%之间),量效呈对数关系(y=alogx+b)。构效关系结果显示,化合物的分子结构决定其抗氧化活性。结论黄芪中的黄酮类成分具有明显的清除超氧阴离子活性,是黄芪抗氧化作用的主要活性成分,且黄酮类成分的清除超氧阴离子活性与其结构有明显的相关性。     

腰痛宁胶囊活性部位组合对PGE2、IL-2、NO细胞因子的影响及其相互作用

目的 评价腰痛宁胶囊中不同活性部位组合的抗炎、免疫及活血活性,以及活性部位间的相互作用.方法 按照腰痛宁组方原则、组合化学思想及各活性部位在腰痛宁中的重要性,在马钱子与麻黄总生物碱基础上依次加入腰痛宁组方药材的总黄酮、总皂苷、挥发油和多糖等活性部位,得到由不同活性部位混合组成腰痛宁拆方、组方及全方共计6个样品.运用脂多糖(LPS)诱导Ana-1细胞释放前列腺素E₂(PGE₂)模型,有丝分裂原(ConA)诱导脾淋巴细胞产生白细胞介素-2(IL-2)模型及刺激人脐静脉内皮细胞释放NO模型,测定各样品抑制PGE₂产生的半数抑制浓度(IC₅₀),促进IL-2和NO分泌的半数有效浓度(EC₅₀);同时采用最小二乘优化方法,计算各样品的IC₅₀/EC₅₀叠加值,将其与IC₅₀/EC₅₀实验值进行比较,分析不同模型下各活性部位间的相互作用类型.结果 6个样品均有抑制PGE₂产生及促进IL-2分泌的活性,但只有由总生物碱、总黄酮和总皂苷组成的样品III有刺激人脐静脉内皮细胞释放NO的EC₅₀,且样品III在以PGE₂、IL-2及NO为指标的抗炎、免疫及活血模型中均表现出优于其他样品的活性,不同的活性部位组合在这3个模型下产生的相互作用类型不同.只有样品III中的总生物碱、总黄酮及总皂苷3个活性部位在3个模型下均存在协同增效作用.结论 腰痛宁拆方、组方及全方样品对Ana-1细胞中PGE₂的产生均表现出良好的抑制作用、对小鼠脾淋巴细胞分泌IL-2也表现出良好的促进作用,显示出腰痛宁处方的合理性、科学性及优良的抗炎和免疫活性.腰痛宁中总生物碱、总黄酮与总皂苷间的协同增效作用使腰痛宁拆方样品III在抗炎、免疫与活血方面的活性均优于其他样品,表明腰痛宁组方具有优化空间.可望以样品III为基础精简腰痛宁组方,开发高效、质量易控的治疗风湿痹病新药.     

Investigation of CYP3A4 and CYP2D6 Interactions of Withania somnifera and Centella asiatica in Human Liver Microsomes

Withania somnifera is commonly used as a rejuvenator, whereas Centella asiatica is well known for its anxiolytic and nootropic effects. The present study aims at investigating the effect of crude extracts and principal phytoconstituents of both the medicinal plants with CYP3A4 and CYP2D6 enzyme activity in human liver microsomes (HLM). Phytoconstituents were quantified in the crude extracts of both the medicinal plants using reverse phase HPLC. Crude extracts and phytoconstituents of W. somnifera showed no significant interaction with both CYP3A4 and CYP2D6 enzymes in HLM. Of the crude extracts of C. asiatica screened in vitro, methanolic extract showed potent noncompetitive inhibition of only CYP3A4 enzyme (Ki—64.36 ± 1.82 µg/mL), whereas ethanol solution extract showed potent noncompetitive inhibition of only CYP2D6 enzyme (Ki—36.3 ± 0.44 µg/mL). The flavonoids, quercetin, and kaempferol showed potent (IC₅₀ values less than 100 μM) inhibition of CYP3A4 activity, whereas quercetin alone showed potent inhibition of CYP2D6 activity in HLM. Because methanolic extract of C. asiatica showed a relatively high percentage content of quercetin and kaempferol than ethanol solution extract, the inhibitory effect of methanolic extract on CYP3A4 enzyme activity could be attributed to the flavonoids. Thus, co‐administration of the alcoholic extracts of C. asiatica with drugs that are substrates of CYP3A4 and CYP2D6 enzymes may lead to undesirable herb‐drug interactions in humans. Copyright © 2015 John Wiley & Sons, Ltd.     

兔儿伞总黄酮抗炎作用研究

目的:观察兔儿伞总黄酮的抗炎作用.方法:以二甲苯致小鼠耳肿胀模型、醋酸致小鼠腹腔毛细血管通透性增加模型,棉球诱发小鼠肉芽肿及小鼠气囊炎模型,观察兔儿伞总黄酮对不同炎症模型的抗炎作用.动物均分为模型(生理盐水)组、地塞米松(2.0 mg· kg-1)组、兔儿伞总黄酮高、中、低(400,200,100 mg·kg-1)组,1次/d,灌胃给药,连续7d.结果:兔儿伞总黄酮各剂量组能显著降低小鼠毛细血管通透性(P＜0.01);兔儿伞总黄酮高剂量组对二甲苯致小鼠耳肿胀有抑制作用,肿胀抑制率51.55％ (P ＜0.01);兔儿伞总黄酮能减轻小鼠肉芽肿,兔儿伞总黄酮各剂量组气囊渗出液中前列腺素E2(PGE2)和白细胞数含量低于对照组(P＜0.01).结论:兔儿伞总黄酮具有较强的抗炎作用,其抗炎作用可能与其降低血管通透性、抑制PGE2的生物合成或释放有关.     

Inhibition of Inducible Nitric Oxide Synthase and Cyclooxygenase‐2 Expression by Phenolic Compounds from Roots of Rhododendron mucronulatum

The roots of Rhododendron mucronulatum Turzaninov have been used in Oriental traditional medicine for the treatment of dysuria, fever, increase of digestive activity and tonics in China and Korea. Activity guided isolation of the roots of Rhododendron mucronulatum Turzaninov has led to the isolation of three flavonoids, one flavan 3‐ol and one proanthocyanidin. Chemical investigation of the 80% Me₂CO extract from the roots of Rhododendron mucronulatum led to the isolation and identification of five compounds: taxifolin (1), taxifolin 3‐O‐β‐d ‐glucopyranoside (2), quercetin 3‐O‐α‐l ‐arabinofuranoside (3), (‐)‐epicatechin (4), procyanidin B‐3 (5). To investigate the antioxidative and antiinflammatory effects of these compounds, their 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) radical scavenging activities and the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase‐2 (COX‐2) in LPS‐stimulated HaCaT cells were also quantified by western blotting and their end products, nitric oxide (NO) and prostaglandin E₂ (PGE₂), respectively. Compounds (1–5) showed potent DPPH radical scavenging compared with positive controls (l ‐ascorbic acid). Also, compounds 1 and 2 dose‐dependently inhibited the expressions of inflammatory mediators, NO and PGE₂, suggesting they are promising candidates as antiinflammatory agents. Copyright © 2011 John Wiley & Sons, Ltd.     

Blood Glucose‐lowering Effect of T. procumbens L.: A Pilot Clinical Study in Individuals with Type 2 Diabetes

Traditional knowledge, in vitro studies, and studies using animal models suggest that Tridax procumbens L. exhibits blood glucose‐lowering properties and antiinflammatory effects. In this study, we evaluated the blood glucose‐lowering effect of T. procumbens supplementation in individuals with type 2 diabetes. An extract (asava) of T. procumbens L. was prepared following Ayurveda guidelines. Chemical and microbial analyses indicated presence of phenolics, flavonoids, and carotenoids, and absence of microbial contamination, aflatoxins, heavy metals, and pesticide residues. A chemical fingerprint of T. procumbens L. asava, developed using Ultra high pressure liquid chromatography/electron spray ionization‐mass spectrometry (UPLC/ESI‐MS) in negative mode, suggest the presence of several compounds including polyphenols. T. procumbens asava demonstrated strong total antioxidant capacity, Fe³⁺ reducing potential, Fe²⁺ chelation, H₂O₂ scavenging activity, and inhibition of lipid peroxidation. We recruited 20 type 2 diabetic individuals from Kolhapur, India. Participants received 15 mL of T. procumbens asava, twice daily, for 4 weeks, while continuing their prescribed antidiabetic medications. Fasting blood glucose decreased by 11% in men (p < 0.01) and 20% in women (p < 0.05), and post‐prandial blood glucose concentrations were lowered by 26% in men (p < 0.001) and 29% in women (p < 0.001) following 4 weeks of asava supplementation. No adverse events or side effects were reported. This is the first clinical study demonstrating a significant blood glucose‐lowering effect of T. procumbens asava in type 2 diabetes. Copyright © 2015 John Wiley & Sons, Ltd.     

一测多评法测定昆仙胶囊中10种黄酮类成分

目的建立一测多评法同时测定昆仙胶囊中10种黄酮类成分的含量,并验证此方法在昆仙胶囊中应用的可行性和适用性。方法采用HPLC法,以金丝桃苷为内参物,建立朝藿苷A、朝藿苷C、朝藿苷B、淫羊藿苷、木犀草素、槲皮素、川陈皮素、山柰酚和宝藿苷I的相对校正因子(fs/i),并利用fs/i计算昆仙胶囊样品中成分的含量,同时用外标法计算各成分的含量,比较两种方法的差异,采用t检验法比较分析昆仙胶囊中10种黄酮类成分的含量。结果朝藿苷B、朝藿苷A、朝藿苷C、淫羊藿苷、木犀草素、槲皮素、川陈皮素、山柰酚和宝藿苷I的fs/i分别为0.756 5、2.199 4、1.232 7、1.008 5、0.635 7、0.576 0、0.487 5、0.545 6、0.675 8。采用一测多评法与外标法得到的10批昆仙胶囊样品含量测定结果 RSD2.0%,无显著差异。结论以金丝桃苷为内参物建立fs/i准确、可行,一测多评法可用于昆仙胶囊的质量评价。     

Chemical Composition and Biological Activities of Polar Extracts and Essential Oil of Rose‐scented Geranium,Pelargonium graveolens

Pelargonium graveolens (Geraniaceae) was characterized with respect to its chemical composition, antioxidant potential and antimicrobial activities. This is the first investigation focusing on the comparison of both essential oil and polar extracts from this species. The chemical composition of the essential oil of the aerial parts of P. graveolens was analyzed by gas chromatography/mass spectrometry. The main constituents of the oil were found to be β‐citronellol (21.9%), citronellyl formate (13.2%), geraniol (11.1%), 10‐epi‐γ‐eudesmol (7.9%), geranyl formate (6.2%) and (l)‐linalool (5.6%). Nine flavonoids were identified by high‐performance liquid chromatography–MS in leaf and flower extracts. Kaempferol 3‐O‐rhamnoside‐glucoside, isorhamnetin aglycone, quercetin 3‐O‐glucoside, kaempferol 3,7‐di‐O‐glucoside, quercetin 3‐O‐pentose and kaempferol 3‐O‐glucoside, quercetin 3‐O‐rhamnoside‐glucoside, quercetin 3‐O‐pentoside‐glucoside, myrisetin 3‐O‐glucoside‐rhamnoside flavonoids were detected in methanolic and aqueous extracts, respectively. The total flavonoids ranged between 29.9 and 78.2 mg QE/g in flower water and methanol extracts, respectively, and 22.5 and 71.2 mg QE/g dry weight in leaf water and methanol extracts, respectively. The highest antioxidant activities using two methods of free radical scavenging capacities were obtained with the essential oil (9.16 mM of Trolox and 2.68 µg/ml). All P. graveolens essential oil and polar extracts were active against at least one bacterium. Copyright © 2012 John Wiley & Sons, Ltd.     

Antihyperlipidemic Components of Cassia auriculata Aerial Parts: Identification Through In Vitro Studies

Cassia auriculata (Caesalpiniaceae) is a common Asian beverage and medicinal plant widely used in tradition medicine for diabetes, hyperlipidemia and various other disease conditions. Previous studies on crude extracts of C. auriculata have documented the scientific basis for some of its traditional medicinal uses. The present study investigates the antilipase activity of the ethanol extract of the aerial parts along with the previously isolated compounds (kaempferol‐3‐O‐rutinoside, rutin, kaempferol, quercetin and luteolin). The crude extract displayed inhibitory activity against pancreatic lipase with IC₅₀ of 6.0 ± 1.0 µg/mL. The most active antilipase compound was kaempferol‐3‐O‐rutinoside with IC₅₀ value (2.9 ± 0.50 μM) only about twice weaker than the standard antilipase drug, orlistat (IC₅₀ = 1.45 ± 0.26 μM). Luteolin, quercetin and rutin were found to be weak pancreatic lipase inhibitors (IC₅₀ over 100 μM), whereas kaempferol showed no activity up to 250 μM. The antihyperlipidemic effect of C. auriculata could be attributed to direct lipase inhibitory effect of the plant constituents. Copyright © 2012 John Wiley & Sons, Ltd.     

The effect of carvacrol on muscarinic receptors of guinea‐pig tracheal chains

The effects of three concentrations of carvacrol, the constituent of Zataria multiflora Boiss (a monoterpenoid phenol, C₁₀H₁₄O) and 10 nm atropine on muscarinic receptors were tested on: non‐incubated (n = 7), incubated tracheal chains with propranolol and chlorpheniramine (n = 6) and incubated with propranolol (n = 5). The EC₅₀ of all three concentrations of carvacrol in incubated tissues with propranolol and chlorpheniramine was significantly greater than those of incubated tissues with propranolol and non‐incubated trachea (p < 0.05 to p < 0.001). The EC₅₀ of two higher concentrations of carvacrol (0.2 and 0.4 µg/mL) in incubated tissues with propranolol was also significantly greater than those of non‐incubated trachea (p < 0.01 to p < 0.001). The maximum response in the presence of all concentrations of carvacrol in non‐incubated and incubated tissues with propranolol and chlorpheniramine and those of its two higher concentrations (0.2 and 0.4 µg/mL) in incubated tissues with propranolol were lower than saline (p < 0.05 to p < 0.001). There were parallel rightward shifts in the concentration–response curves in the presence of all concentrations of carvacrol in non‐incubated and incubated tissues with propranolol and its lower concentration in incubated tissues with propranolol and chlorpheniramine. These results indicated an inhibitory effect of carvacrol on muscarinic receptors. A β‐adrenoceptor stimulatory effect was also suggested for carvacrol. Copyright © 2010 John Wiley & Sons, Ltd.     

准噶尔大戟根中黄酮类成分的研究

 目的研究新疆产准噶尔大戟根的黄酮类化学成分,阐明其药理作用的物质基础。方法通过反复硅胶柱色谱,运用硅胶薄层制备以及凝胶柱色谱等方法分离纯化化合物,利用核磁共振等现代波谱技术解析化合物结构。结果从准噶尔大戟根的氯仿部分分离得到了4个黄酮类化合物:山柰酚(Ⅰ),槲皮素(Ⅱ),芹菜素(Ⅲ)和鼠李素(Ⅳ);从其正丁醇部分分离得到了3个黄酮苷类化合物:槲皮苷(Ⅴ),槲皮素-3-O-α-D-阿拉伯糖苷(Ⅵ),芹菜素-7-O-β-D-葡萄糖苷(Ⅶ)。结论上述化合物均首次从该植物中分离得到。     

三七茎叶黄酮类成分的研究

 目的对三七[Panax notoginseng(Burk.)F.H.Chen]茎叶的黄酮类成分进行分离鉴定。方法利用水煎煮提取、大孔吸附树脂吸附、硅胶柱色谱、ODS柱色谱等方法分离提纯,通过理化性质及IR,UV,MS,¹H-NMR,¹³C-NMR等光谱数据鉴定其结构。结果分离得到6个黄酮类单体化合物,分别鉴定为:山柰酚(kaempferol,Ⅰ)、槲皮素(quercetin,Ⅱ)、山柰酚-7-O-α-L-鼠李糖苷(kaempferol 7-O-α-L-rhamnoside,Ⅲ)、山柰酚-3-O-β-D-半乳糖苷(kaempferol 3-O-β-D-galactoside,Ⅳ)、山柰酚-3-O-β-D-半乳糖(2→1)葡萄糖苷[kaempferol 3-O-(2″-β-D-glucopyranosyl)-β-D-galactopyranoside,Ⅴ]、槲皮素-3-O-β-D-半乳糖(2→1)葡萄糖苷[quercetin3-O-(2″-β-D-glucopyranosyl)-β-D-galactopyranoside,Ⅵ]。结论除山柰酚(kaempferol,Ⅰ)、槲皮素(quercetin,Ⅱ)之外,其余4个化合物皆为首次从该植物中分离得到,Ⅲ与Ⅵ为首次从该属植物中分离得到。     

Modulatory Effect of an Urera Aurantiaca Extract on Immune and Tumoral Cells During Inflammation

There is a well known link between inflammation and cancer during initiation, propagation and metastasis. Urera aurantiaca (UA) Wedd. (Urticaceae) is a medicinal plant used in traditional medicine to treat inflammatory processes with proven in vivo antiinflammatory and antinociceptive effects. The effects of a methanolic extract (UA) and a purified fraction (PF) on the proliferation of normal and tumoral lymphocytes under the effect of prostaglandin E₂ (PGE₂) and on nitric oxide production by lipopolysaccharide‐stimulated macrophages was evaluated. Both UA and PF stimulated normal lymphocytes but, in presence of PGE_2, a modulatory effect was observed. The normal lymphocyte proliferation induced by PGE₂ was driven by pathways involving both PKC and H₂O₂. In macrophages, UA and PF did not modify cell viability and abrogated the synthesis of nitric oxide induced by lipopolysaccharide. In tumoral lymphocytes, the UA exerted a biphasic effect: at low concentrations it increased cell proliferation, while at high concentrations, it displayed an antiproliferative effect. UA and PF were capable of reverting the proliferative action of PGE₂. The tumoral cell proliferation induced by PGE₂ is related to PKC, ERK 1/2 and MAP Kinase P38 pathways. The observed effects could be attributed to polyphenols, flavonoids and tannins. This work demonstrates the modulatory effects of the UA on different cell types during inflammatory conditions, which reinforces its antiinflammatory action. Copyright © 2016 John Wiley & Sons, Ltd.     

Hepatoprotective activity of praecoxin A isolated from Melaleuca ericifolia against carbon tetrachloride‐induced hepatotoxicity in mice. Impact on oxidative stress,inflammation, and apoptosis

The hepatoprotective activity of praecoxin A, an ellagitannin from Melaleuca ericifolia, was determined against CCl₄‐induced toxicity in mice. Praecoxin A was administered (25, 50, and 100 mg/kg) for 5 days followed by CCl₄. Praecoxin A markedly ameliorated the CCl₄‐induced increase in AST (by 19, 52, and 56%), ALP (22, 45, and 48%), ALT (11, 47, and 54%), total bilirubin (14, 27, and 28%), and MDA (26, 44, and 51%) at the tested doses, respectively, as compared with CCl₄ group. It was evident that praecoxin A significantly (p < 0.001) increased the antioxidant parameters GSH (45, 99, and 137%) and SOD (61, 129, and 159%). Histological findings revealed a marked amelioration of hepatocyte degeneration, necrosis, inflammatory cell infiltration, and hemorrhage in the groups treated with praecoxin A. COX‐2 and caspase‐3 hepatic expressions were significantly downregulated (p < 0.001) in praecoxin A‐treated groups (up to 57, 83, and 93% for COX‐2 and by 30, 82, and 99% for caspase‐3). These findings suggest that praecoxin A exerts a beneficial effect against oxidative stress by reducing lipid peroxidation, enhancing the antioxidant defense status, and protecting against the histopathological changes induced by CCl₄. This study highlights a promising natural hepatoprotective candidate derived from M. ericifolia that might be an alternative to silymarin.