Pub Date : 2014-01-01DOI: 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).
{"title":"Anti-HSV-1 and antioxidant activities of dicaffeoyl and digalloyl esters of quinic acid","authors":"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","doi":"10.1016/j.bionut.2013.09.007","DOIUrl":"10.1016/j.bionut.2013.09.007","url":null,"abstract":"<div><p><span><span>Nine caffeic and gallic acids derivatives were synthesized and evaluated for their antioxidant activity using the </span>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 </span><strong>8</strong> (IC<sub>50</sub> <!-->=<!--> <!-->177<!--> <!-->μM). Five compounds (<strong>7, 10, 11, 12</strong> and <strong>14</strong><span>) were found to possess anti-HSV-1 activity with selectivity indices values ranging from 7.0 to 27.1. The most active was compound </span><strong>10</strong> (IC<sub>50</sub> <!-->=<!--> <!-->15.2<!--> <!-->μM; SI<!--> <!-->=<!--> <!-->27.1).</p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"4 1","pages":"Pages 35-38"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.09.007","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89806018","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2014-01-01DOI: 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.
{"title":"Marine derived natural products for osteoporosis","authors":"Kalimuthu Senthilkumar , Jayachandran Venkatesan , Se-Kwon Kim","doi":"10.1016/j.bionut.2013.12.005","DOIUrl":"10.1016/j.bionut.2013.12.005","url":null,"abstract":"<div><p><span><span>Bone homeostasis is maintained through a balance between osteoblastic bone formation and osteoclastic </span>bone resorption<span>. 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 </span></span>public health<span><span> 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 </span>bone metabolism. This review discusses the current pharmacological therapies for osteoporosis and bioactive natural products from marine for the anti-osteoporotic research.</span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"4 1","pages":"Pages 1-7"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.12.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80992178","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2014-01-01DOI: 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.
{"title":"Nutraceutical applications of gourd family vegetables: Benincasa hispida, Lagenaria siceraria and Momordica charantia","authors":"S. Palamthodi, S.S. Lele","doi":"10.1016/j.bionut.2013.03.004","DOIUrl":"10.1016/j.bionut.2013.03.004","url":null,"abstract":"<div><p><span><span>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 </span>Chinese medicine. The article focuses on medicinal properties of extracts derived from different vegetative parts of three Cucurbitaceae species viz. ash gourd (</span><em>Benincasa hispida</em>), bottle gourd (<em>Lagenaria siceraria</em>) and bitter gourd (<span><em>Momordica</em><em> charantia</em></span><span><span><span>). 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<span>, analgesic and anti-inflammatory activity, </span></span>central nervous system activity, antihyperglycemic and antidiabetics, anti-hyperlipidemic activity, </span>antimicrobial activity<span> and anthelmintic<span><span> activity, cytotoxic and anticancer activity<span>, immunomodulatory effect, cardioprotective effects, hepatoprotective activity, bronchospasm protective activity, </span></span>antidiarrheal<span> activity, and diuretic activity.</span></span></span></span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"4 1","pages":"Pages 15-21"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.03.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83654750","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2014-01-01DOI: 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.
{"title":"Hibiscus sabdariffa: An ideal yet under-exploited candidate for nutraceutical applications","authors":"Seema Patel","doi":"10.1016/j.bionut.2013.10.004","DOIUrl":"10.1016/j.bionut.2013.10.004","url":null,"abstract":"<div><p><span><span>The quest for wholesome nutraceutical<span> sources is all-time high as acute and chronic ailments threaten </span></span>human health. In this regard, a Malvaceae family member </span><span><em>Hibiscus</em><em> sabdariffa</em></span><span> (roselle) holds plentiful potential. This plant with worldwide distribution is a powerhouse of phytochemicals </span><em>viz</em><span><span>. polyphenolics, especially anthocyanins. The nutritional abundance imparts it antioxidant, hypocholesterolaemic, antiobesity, hypotensive, </span>antidiabetic<span>, 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.</span></span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"4 1","pages":"Pages 23-27"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.10.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75709220","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2014-01-01DOI: 10.1016/j.bionut.2013.06.004
Shailendra Kapoor
{"title":"Wortmannin and its effects on tumor progression and proliferation","authors":"Shailendra Kapoor","doi":"10.1016/j.bionut.2013.06.004","DOIUrl":"10.1016/j.bionut.2013.06.004","url":null,"abstract":"","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"4 1","pages":"Page 85"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.06.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82565697","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-10-31DOI: 10.1016/J.BIONUT.2013.06.008
P. Sireesha, S. Nagarjuna, S. Challa
{"title":"WITHDRAWN: Immunomodulatory effect of water-soluble polysaccharides isolated from Metroxylon sagu in rats","authors":"P. Sireesha, S. Nagarjuna, S. Challa","doi":"10.1016/J.BIONUT.2013.06.008","DOIUrl":"https://doi.org/10.1016/J.BIONUT.2013.06.008","url":null,"abstract":"","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2013-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91096936","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-10-01DOI: 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 200nm 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.
{"title":"Formulation and characterisation of self-microemulsifying drug delivery system of pioglitazone","authors":"P. Hyma , K. Abbulu","doi":"10.1016/j.bionut.2013.09.005","DOIUrl":"10.1016/j.bionut.2013.09.005","url":null,"abstract":"<div><p><span><span>The aim of the study was to develop self-microemulsifying drug<span> delivery system (SMEDDS) of a poorly water soluble drug, pioglitazone<span>. 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 </span></span></span>Tween 80<span><span> (surfactant) polyethylene glycol 400 (cosurfactant) and </span>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</span></span> <span><span>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. </span>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.</span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"3 4","pages":"Pages 345-350"},"PeriodicalIF":0.0,"publicationDate":"2013-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.09.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83252039","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-10-01DOI: 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.
{"title":"Antioxidant properties of Lactuca sativa leaf extract involved in the protection of biomolecules","authors":"S.N. Harsha , K.R. Anilakumar , M.V. Mithila","doi":"10.1016/j.bionut.2013.06.003","DOIUrl":"10.1016/j.bionut.2013.06.003","url":null,"abstract":"<div><p>The aim of the present study was to evaluate the radical scavenging, and biomolecule protective property of <em>Lactuca sativa</em>, an important and commonly used leafy vegetable known for its medicinal properties. The hydro-alcohol extract of <em>Lactuca sativa</em><span> exhibited strong scavenging effect on 2,2-diphenyl-2-picryl hydrazyl (DPPH), superoxide and nitric oxide, protection against DNA and protein damage. IC </span><sub>50</sub> 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<!--> <span>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 </span><em>Lactuca sativa</em><span> treatment. These results suggest that the extract of </span><em>Lactuca sativa</em><span> has potent activity against free radicals and oxidative damage to major biomolecules.</span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"3 4","pages":"Pages 367-373"},"PeriodicalIF":0.0,"publicationDate":"2013-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.06.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85614066","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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。
{"title":"Diosgenin exhibits beneficial efficiency on human mammary carcinoma cell line MCF-7 and against N-nitroso-N-methylurea (NMU) induced experimental mammary carcinoma","authors":"Jayaraman Jagadeesan , Kulanthaivel Langeswaran , Subbaraj Gowthamkumar , Maruthaiveeran Periyaswamy Balasubramanian","doi":"10.1016/j.bionut.2013.06.009","DOIUrl":"10.1016/j.bionut.2013.06.009","url":null,"abstract":"<div><p><span><span>The purpose of the present study was to investigate the impact of diosgenin<span> on the human mammary carcinoma cell line (MCF-7) and to investigate its therapeutic potential against NMU-induced </span></span>experimental breast cancer<span>. 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. </span></span><em>N</em>-nitroso-<em>N</em><span><span>-methylurea (NMU) is a highly reliable carcinogen, mutagen and </span>teratogen<span> used in the present study to promote breast carcinogenesis in experimental rats. In </span></span><em>in vitro</em><span> 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<span>. Elevated lipid peroxidation in NMU-induced breast cancer-bearing animals were drim down (</span></span><em>P</em> <!--><<!--> <span><span>0.05) due to management with steroidal diosgenin. The altered lysosomal enzymes were neutralised by diosgenin and also, it protects macromolecular damage from </span>oxidative stress<span> and free fadicals production due to its antioxidant activity<span>. 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.</span></span></span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"3 4","pages":"Pages 381-388"},"PeriodicalIF":0.0,"publicationDate":"2013-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.06.009","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90690917","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-10-01DOI: 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.
{"title":"Design, synthesis and biological evaluation of some isatin-linked chalcones as novel anti-breast cancer agents: A molecular hybridization approach","authors":"Chandrabose Karthikeyan , Viswas Raja Solomon , Hoyun Lee , Piyush Trivedi","doi":"10.1016/j.bionut.2013.04.001","DOIUrl":"10.1016/j.bionut.2013.04.001","url":null,"abstract":"<div><p><span><span><span>Isatins are endogenous molecules present in human and mammals which exhibits diverse pharmacological profiles including </span>anticancer activity. Similarly, </span>chalcones<span>, which are common substructures in numerous natural products belonging to the flavonoid<span> 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 (<</span></span></span> <!-->20<!--> <!-->μM) against the studied cell lines. Compound <strong>2c</strong>, 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 GI<sub>50</sub><span> 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<span> for the treatment of breast cancer.</span></span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"3 4","pages":"Pages 325-330"},"PeriodicalIF":0.0,"publicationDate":"2013-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.04.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91549606","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}