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Anti-HSV-1 and antioxidant activities of dicaffeoyl and digalloyl esters of quinic acid 奎宁酸二咖啡酯和二烯丙酯抗hsv -1及抗氧化活性
Pub Date : 2014-01-01 DOI: 10.1016/j.bionut.2013.09.007
Celso O. Rezende Jr. , Caroline Rigotto , Wiliam Caneschi , Carlos A.M. Rezende , Mireille Le Hyaric , Mara R.C. Couri , Cláudia M.O. Simões , Mauro V. de Almeida

Nine caffeic and gallic acids derivatives were synthesized and evaluated for their antioxidant activity using the DPPH radical scavenging activity assay and for their antiherpes activity against HSV-1. All compounds displayed higher antioxidant activities than α-tocopherol. The most active antioxidant was compound 8 (IC50 = 177 μM). Five compounds (7, 10, 11, 12 and 14) were found to possess anti-HSV-1 activity with selectivity indices values ranging from 7.0 to 27.1. The most active was compound 10 (IC50 = 15.2 μM; SI = 27.1).

合成了9种咖啡酸和没食子酸衍生物,并利用DPPH自由基清除活性测定法评估了它们的抗氧化活性和对HSV-1的抗疱疹活性。所有化合物的抗氧化活性均高于α-生育酚。化合物8的抗氧化活性最高(IC50 = 177 μM)。5个化合物(7、10、11、12和14)具有抗hsv -1活性,选择性指数在7.0 ~ 27.1之间。活性最高的是化合物10 (IC50 = 15.2 μM;si = 27.1)。
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引用次数: 9
Marine derived natural products for osteoporosis 海洋衍生的骨质疏松症天然产品
Pub Date : 2014-01-01 DOI: 10.1016/j.bionut.2013.12.005
Kalimuthu Senthilkumar , Jayachandran Venkatesan , Se-Kwon Kim

Bone homeostasis is maintained through a balance between osteoblastic bone formation and osteoclastic bone resorption. Aging induces bone loss due to decreased osteoblastic bone formation and increased osteoclastic bone resorption. Osteoporosis with its accompanying decrease in bone mass is widely recognized as a major public health problem. It is undoubted that pharmacological and nutritional factors are involved in the prevention of age-related bone loss. In the search for the appropriate treatment of osteoporosis, there is an interesting area of marine organisms and phytopharmacology. Extracts of marine algae and other marine derived compounds have a favorable effect on bone metabolism. This review discusses the current pharmacological therapies for osteoporosis and bioactive natural products from marine for the anti-osteoporotic research.

骨稳态是通过成骨细胞骨形成和破骨细胞骨吸收之间的平衡来维持的。由于成骨细胞骨形成减少和破骨细胞骨吸收增加,衰老导致骨质流失。骨质疏松症及其伴随的骨量减少被广泛认为是一个重大的公共卫生问题。毫无疑问,药物和营养因素在预防老年性骨质流失中起着重要作用。在寻找骨质疏松症的适当治疗中,海洋生物和植物药理学是一个有趣的领域。海藻提取物和其他海洋衍生化合物对骨代谢有良好的作用。本文综述了目前骨质疏松症的药物治疗方法以及海洋生物活性天然产物在抗骨质疏松研究中的应用。
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引用次数: 15
Nutraceutical applications of gourd family vegetables: Benincasa hispida, Lagenaria siceraria and Momordica charantia 葫芦科蔬菜的营养保健应用:贝南卡菜、丝瓜Lagenaria siceraria和苦瓜
Pub Date : 2014-01-01 DOI: 10.1016/j.bionut.2013.03.004
S. Palamthodi, S.S. Lele

The use of food and food products as medicine has been in practice over centuries in many civilizations. The extracts from the family Cucurbitaceae have been used in the preparation of medicines for a variety of diseases in Ayurveda and ancient Chinese medicine. The article focuses on medicinal properties of extracts derived from different vegetative parts of three Cucurbitaceae species viz. ash gourd (Benincasa hispida), bottle gourd (Lagenaria siceraria) and bitter gourd (Momordica charantia). The competency of extracts derived from these plants using different extraction solutions and techniques were tested against various diseases. These plants were found to possess antioxidant activity, analgesic and anti-inflammatory activity, central nervous system activity, antihyperglycemic and antidiabetics, anti-hyperlipidemic activity, antimicrobial activity and anthelmintic activity, cytotoxic and anticancer activity, immunomodulatory effect, cardioprotective effects, hepatoprotective activity, bronchospasm protective activity, antidiarrheal activity, and diuretic activity.

在许多文明中,食品和食品制品作为药物的使用已经实践了几个世纪。在阿育吠陀和古代中医中,葫芦科植物的提取物已被用于制备治疗多种疾病的药物。本文主要研究了葫芦科三种植物——葫芦(Benincasa hispida)、葫芦(Lagenaria siceraria)和苦瓜(Momordica charantia)不同营养部位提取物的药用特性。采用不同的提取溶液和提取技术对这些植物的提取物进行了抗各种疾病的能力测试。这些植物被发现具有抗氧化活性、镇痛和抗炎活性、中枢神经系统活性、降糖和降糖活性、抗高血脂活性、抗菌活性和驱虫药活性、细胞毒性和抗癌活性、免疫调节作用、心脏保护作用、肝脏保护作用、支气管痉挛保护活性、止泻活性和利尿活性。
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引用次数: 41
Hibiscus sabdariffa: An ideal yet under-exploited candidate for nutraceutical applications 芙蓉:一个理想的但尚未开发的候选营养保健应用
Pub Date : 2014-01-01 DOI: 10.1016/j.bionut.2013.10.004
Seema Patel

The quest for wholesome nutraceutical sources is all-time high as acute and chronic ailments threaten human health. In this regard, a Malvaceae family member Hibiscus sabdariffa (roselle) holds plentiful potential. This plant with worldwide distribution is a powerhouse of phytochemicals viz. polyphenolics, especially anthocyanins. The nutritional abundance imparts it antioxidant, hypocholesterolaemic, antiobesity, hypotensive, antidiabetic, immunomodulatory, anticancer, hepatoprotective, antimicrobial, renoprotective, diuretic and anti-urolithiatic properties. Though this plant has a long history of use across cultures, the recent scientific validations have augmented its status as a nutrition resource. Food industries have started incorporating their calyces into various products. In the near future, the elaboration of more fortified foods is expected. This review is expected to be contributory in its popularization by kindling consumer as well as research interest.

由于急性和慢性疾病威胁着人类健康,对健康营养来源的追求空前高涨。在这方面,锦葵科的一名成员芙蓉(roselle)具有丰富的潜力。这种植物分布在世界各地,富含植物化学物质,如多酚类物质,特别是花青素。丰富的营养使其具有抗氧化、降胆固醇、抗肥胖、降血压、降糖尿病、免疫调节、抗癌、保肝、抗菌、保肾、利尿和抗尿石等特性。虽然这种植物在各种文化中都有悠久的使用历史,但最近的科学验证已经增强了它作为营养资源的地位。食品工业已经开始将它们的花萼整合到各种产品中。在不久的将来,预计会有更多的强化食品。本文对其进行了综述,希望对其在消费者中的推广和研究兴趣有所帮助。
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引用次数: 88
Wortmannin and its effects on tumor progression and proliferation Wortmannin及其对肿瘤进展和增殖的影响
Pub Date : 2014-01-01 DOI: 10.1016/j.bionut.2013.06.004
Shailendra Kapoor
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引用次数: 0
WITHDRAWN: Immunomodulatory effect of water-soluble polysaccharides isolated from Metroxylon sagu in rats 撤下:木杉水溶性多糖对大鼠的免疫调节作用
Pub Date : 2013-10-31 DOI: 10.1016/J.BIONUT.2013.06.008
P. Sireesha, S. Nagarjuna, S. Challa
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引用次数: 0
Formulation and characterisation of self-microemulsifying drug delivery system of pioglitazone 吡格列酮自微乳化给药体系的研制与表征
Pub Date : 2013-10-01 DOI: 10.1016/j.bionut.2013.09.005
P. Hyma , K. Abbulu

The aim of the study was to develop self-microemulsifying drug delivery system (SMEDDS) of a poorly water soluble drug, pioglitazone. Approximately 40% of new drug candidates have poor water solubility and the oral delivery of such drugs is frequently associated with implications of low bioavailability, high intra- and intersubject variability and lack of dose proportionality. Hydrophobic drugs can often be dissolved in microemulsion allowing them to be encapsulated in the form of fine globules, so that drug remains undissolved in the gut avoiding the dissolution step, which frequently limit the rate of absorption of hydrophobic drugs. Phase solubility studies were conducted for the maximum solubility of pioglitazone. Highest was found in Tween 80 (surfactant) polyethylene glycol 400 (cosurfactant) and cottonseed oil. Ternary phase diagrams were constructed to evaluate microemulsion regions. FTIR analysis was done for investigating the drug–excipient interactions. The mean globule size of SMEDDS was observed to be below 200 nm for the optimized formulations and the zeta potential was negative. The dissolution of emulsion formulations was compared with commercial tablets; the results indicated that the rate of dissolution of developed formulations containing pioglitazone was 2 to 3 folds increased compared with that of commercial tablets. SEM studies were done for the shape and morphology of the globules. Thus, SMEDDS can be regarded as novel and commercially feasible alternative to the current pioglitazone formulations.

本研究的目的是研制吡格列酮水溶性较差药物的自微乳化给药系统。大约40%的新候选药物水溶性较差,口服给药往往伴随着低生物利用度、高体内和体内变异性以及缺乏剂量比例的影响。疏水药物通常可以溶解在微乳液中,使其被包裹成细小的小球,使药物在肠道中保持不溶解,避免了溶解步骤,这往往限制了疏水药物的吸收速度。对吡格列酮的最大溶解度进行了相溶解度研究。以Tween 80(表面活性剂)、聚乙二醇400(共表面活性剂)和棉籽油含量最高。构建三元相图评价微乳区域。FTIR分析了药物与辅料的相互作用。优化后的SMEDDS平均粒径小于200 nm, zeta电位为负。并与市售片剂进行了溶出度比较;结果表明,所研制的吡格列酮溶出度比市售片提高了2 ~ 3倍。对球的形状和形态进行了扫描电镜研究。因此,SMEDDS可被视为目前吡格列酮制剂的新颖和商业上可行的替代品。
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引用次数: 17
Antioxidant properties of Lactuca sativa leaf extract involved in the protection of biomolecules 芥蓝叶提取物抗氧化性能涉及的生物分子保护
Pub Date : 2013-10-01 DOI: 10.1016/j.bionut.2013.06.003
S.N. Harsha , K.R. Anilakumar , M.V. Mithila

The aim of the present study was to evaluate the radical scavenging, and biomolecule protective property of Lactuca sativa, an important and commonly used leafy vegetable known for its medicinal properties. The hydro-alcohol extract of Lactuca sativa exhibited strong scavenging effect on 2,2-diphenyl-2-picryl hydrazyl (DPPH), superoxide and nitric oxide, protection against DNA and protein damage. IC 50 values of radical scavenging activity were found to be 162.8 μg/mL for super oxide, 492 μg/mL for nitric oxide radical, 558 μg/mL for metal chelating, and 1236.7 μg/mL for hydroxyl radical. DNA and protein oxidation was prevented dose-dependently and the tail length of DNA as observed in COMET assay was decreased by Lactuca sativa treatment. These results suggest that the extract of Lactuca sativa has potent activity against free radicals and oxidative damage to major biomolecules.

摘要本研究的目的是评价莴苣(lacuca sativa)的自由基清除和生物分子保护作用。莴苣是一种重要的、常用的叶菜,因其药用价值而闻名。摘要芥花水醇提取物对2,2-二苯基-2-苦酰肼(DPPH)、超氧化物和一氧化氮具有较强的清除作用,对DNA和蛋白质损伤具有保护作用。清除超氧化物的ic50值为162.8 μg/mL,清除一氧化氮自由基的ic50值为492 μg/mL,清除金属螯合自由基的ic50值为558 μg/mL,清除羟基自由基的ic50值为1236.7 μg/mL。通过剂量依赖性地抑制了DNA和蛋白质的氧化,并减少了DNA的尾长。上述结果表明,芥蓝提取物具有较强的抗自由基活性和抗主要生物分子氧化损伤活性。
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引用次数: 23
Diosgenin exhibits beneficial efficiency on human mammary carcinoma cell line MCF-7 and against N-nitroso-N-methylurea (NMU) induced experimental mammary carcinoma 薯蓣皂苷元对人乳腺癌细胞株MCF-7和n -亚硝基-n -甲基脲(NMU)诱导的实验性乳腺癌具有良好的抑制作用
Pub Date : 2013-10-01 DOI: 10.1016/j.bionut.2013.06.009
Jayaraman Jagadeesan , Kulanthaivel Langeswaran , Subbaraj Gowthamkumar , Maruthaiveeran Periyaswamy Balasubramanian

The purpose of the present study was to investigate the impact of diosgenin on the human mammary carcinoma cell line (MCF-7) and to investigate its therapeutic potential against NMU-induced experimental breast cancer. Mammary carcinoma cells were treated with different concentrations of diosgenin and its cytotoxicity effect was measured by MTT method, lactate dehydrogenase leakage and by estimating GSH assays. N-nitroso-N-methylurea (NMU) is a highly reliable carcinogen, mutagen and teratogen used in the present study to promote breast carcinogenesis in experimental rats. In in vitro studies, diosgenin significantly inhibited the proliferation of MCF-7 cells in a dose-dependent manner and the depletion of GSH and an increase of LDH activity were observed in MCF-7 cells due to cytotoxic nature of the drug. Elevated lipid peroxidation in NMU-induced breast cancer-bearing animals were drim down (P < 0.05) due to management with steroidal diosgenin. The altered lysosomal enzymes were neutralised by diosgenin and also, it protects macromolecular damage from oxidative stress and free fadicals production due to its antioxidant activity. From the results of our present analysis, it gives an idea about that diosgenin may be used as a chemoprotective agent against human mammary carcinoma.

本研究旨在探讨薯蓣皂苷元对人乳腺癌细胞系MCF-7的影响,并探讨其对nmu诱导的实验性乳腺癌的治疗潜力。用不同浓度的薯蓣皂苷元处理乳腺癌细胞,采用MTT法、乳酸脱氢酶渗漏法和谷胱甘肽测定法测定其细胞毒性。n -亚硝基-n -甲基脲(n -nitroso- n - methyllurea, NMU)是一种高度可靠的致癌物质、诱变剂和致畸剂,在本研究中用于促进实验大鼠乳腺癌的发生。在体外研究中,薯蓣皂苷元以剂量依赖的方式显著抑制MCF-7细胞的增殖,并且由于药物的细胞毒性,在MCF-7细胞中观察到GSH的消耗和LDH活性的增加。nmu诱导的乳腺癌动物脂质过氧化水平升高被降低(P <0.05),这是由于甾体薯蓣皂苷元的管理。改变的溶酶体酶被薯蓣皂苷元中和,并且由于其抗氧化活性,它可以保护大分子损伤免受氧化应激和游离自由基的产生。本研究结果提示薯蓣皂苷元可能作为一种化学保护剂用于人乳腺癌的治疗。
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引用次数: 11
Design, synthesis and biological evaluation of some isatin-linked chalcones as novel anti-breast cancer agents: A molecular hybridization approach 一些isatin-linked chalcones作为新型抗乳腺癌药物的设计、合成和生物学评价:分子杂交方法
Pub Date : 2013-10-01 DOI: 10.1016/j.bionut.2013.04.001
Chandrabose Karthikeyan , Viswas Raja Solomon , Hoyun Lee , Piyush Trivedi

Isatins are endogenous molecules present in human and mammals which exhibits diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures in numerous natural products belonging to the flavonoid family, show potent anticancer properties. A novel series of 3-(2-oxo-2-phenylethylidene)indolin-2-ones incorporating pharmacophoric elements of isatins and chalcones were designed and synthesized. The compounds were evaluated for anticancer activity against three breast cancer cell lines. Most of the compounds showed promising anticancer activity (< 20 μM) against the studied cell lines. Compound 2c, bearing a 5-chloro substituent in the benzo ring of the isatin moiety and 3,4-dimethoxy substitutions in the phenyl ring, was found to be the most active in the series with GI50 values of 8.54, 4.76 and 3.59 against MDA-MB231, MDA-MB468 and MCF7 cells, respectively. Overall, the findings of the study highlight 3-(2-oxo-2-phenylethylidene)indolin-2-one as a potential new lead in the search of drugs for the treatment of breast cancer.

Isatins是存在于人类和哺乳动物体内的内源性分子,具有多种药理特征,包括抗癌活性。类似地,查尔酮是许多天然产物中常见的亚结构,属于类黄酮家族,显示出有效的抗癌特性。设计并合成了一种新的3-(2-氧-2-苯基乙基)吲哚-2-酮类化合物,该化合物含有鸢尾素和查尔酮的药效成分。这些化合物对三种乳腺癌细胞系的抗癌活性进行了评估。大多数化合物显示出良好的抗癌活性(<20 μM)。化合物2c对MDA-MB231、MDA-MB468和MCF7细胞的GI50值分别为8.54、4.76和3.59,是该系列中活性最高的化合物,其isatin部分的苯环上有一个5-氯取代,苯基环上有3,4-二甲氧基取代。总的来说,这项研究的发现突出了3-(2-氧-2-苯基乙基)吲哚-2- 1作为寻找治疗乳腺癌药物的潜在新先导。
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引用次数: 47
期刊
Biomedicine & Preventive Nutrition
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