A. Ashour, S. El-Sharkawy, M. Amer, F. A. Bar, A. Mera, Toshiro Nagata, R. Kondo, Kuniyoshi Shimizu
{"title":"Biotransformation of Khellin to Khellol by Aspergillus Niger and the Evaluation of their Biological Activities","authors":"A. Ashour, S. El-Sharkawy, M. Amer, F. A. Bar, A. Mera, Toshiro Nagata, R. Kondo, Kuniyoshi Shimizu","doi":"10.2174/1874847320130628001","DOIUrl":"https://doi.org/10.2174/1874847320130628001","url":null,"abstract":"Biotransformation of khellin using Aspergillus niger ATCC 10549 resulted in the production of khellol. The biological activities of the transformed product and khellin were established by antioxidant and acetylcholine esterase in- hibitory assays. Khellol exhibited a higher degree of antioxidant and acetylcholine esterase inhibitory activities compared to khellin. This is the first report on the biotransformation of khellin by microorganisms and the first evaluation of the neuroprotective activity of either khellin or khellol.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115848526","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}
H. Piotrowska, M. Kucińska, M. Wierzchowski, Urszula Kazmierczak-Majchrzak, M. Murias
{"title":"Effect of resveratrol and its hydroxylated analogues on proliferation and apoptosis oftwo cervix cancer derived cancer cell lines. The role of mitochondrial superoxidedismutase","authors":"H. Piotrowska, M. Kucińska, M. Wierzchowski, Urszula Kazmierczak-Majchrzak, M. Murias","doi":"10.2174/1874847320130701002","DOIUrl":"https://doi.org/10.2174/1874847320130701002","url":null,"abstract":"The naturally occurring polyphenol resveratrol (3,4',5-trihydroxy-stilbene, 3,4',5-THS, RES) has been shown as a chemopreventive and proapototic agent. Resveratrol is extensively metabolized by CYP450 enzymes. The monohy- droxylation of resveratrol is catalyzed by CYP1B1 to form 3,3',4',5-THS (piceatannol), a metabolite with higher antican- cer activity and stronger antioxidant properties. It was hypothesized that RES analogues (HHRAs) possessing more than 3 hydroxyl groups may act stronger against cancer cells than RES due to reactive oxygen species formed in redox-cycling reactions. In order to investigate a structure-activity relationship between pro/antioxidant properties and cytotoxicity, the HHRAs with at least 2 phenolic groups in neighborhood- 3,4,4',5-HS and 3,3',4,4',5,5'-HS were synthesized. In the present study we tested this hypothesis in a cell culture model using HeLa and C33A cancer cell lines. The results of our experi- ments support a hypothesis that MnSOD overexpressing HeLa cells are much more resistant to superoxide generating HHRAs than C33A cells.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"69 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123004992","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}
P. Carillo, C. Cozzolino, B. D’Abrosca, F. Nacca, M. DellaGreca, A. Fiorentino, A. Fuggi
{"title":"Effects of the Allelochemicals Dihydrodiconiferyl Alcohol and Lariciresinol on Metabolism of Lactuca sativa","authors":"P. Carillo, C. Cozzolino, B. D’Abrosca, F. Nacca, M. DellaGreca, A. Fiorentino, A. Fuggi","doi":"10.2174/1874847301003010018","DOIUrl":"https://doi.org/10.2174/1874847301003010018","url":null,"abstract":"Dihydridiconiferyl alcohol and lariciresinol, known as phytotoxic lignans, acting on the germination of Lactuca sativa have been tested for lettuce seedling development. It has been evidenced that sucrose grown plants respond to such lignans differently from those grown without sucrose. Dihydridiconiferyl alcohol, which is more active than lariciresinol, reduced chlorophyll and carotenoid synthesis in sucrose grown plants. It also caused a greater decrease of photosystem efficiency, lowering of Yield and non-photochemical quenching in treated plants in respect to those in controls. Both lignans affected carbon and nitrogen metabolism, reducing, in particular, glucose-6-phosphate dehydrogenase (G6PDH) and glutamate synthase (GOGAT) activities in sucrose grown plants. The decrease of G6PDH (-80%) and GOGAT (-65%) activities was correlated to an increase of soluble sugars (up to + 100%) and glutamine (+70%), respectively. This is the first time an allelochemical affecting GOGAT activity has been reported.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"90 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2010-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115846203","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}
{"title":"Cytokine-Modulatory Activity and Therapeutic Efficacy of 7-Amino-4-Methylcoumarin in Murine Collagen-Induced Arthritis","authors":"M. Kurokawa, M. Imakita, K. Shiraki","doi":"10.2174/1874847301003010012","DOIUrl":"https://doi.org/10.2174/1874847301003010012","url":null,"abstract":"Amino-4-methylcoumarin (AMC) was previously shown to suppress pro-inflammatory cytokine production and prevent death in an endotoxic shock model in mice. In the present study, we investigated the effectiveness of AMC as a potential cytokine modulator in alleviating autoimmune diseases. We examined the efficacy and cytokine-modulatory activity of AMC in collagen-induced arthritis (CIA) in mice. Mice were immunized with type II collagen. AMC at 0, 3, or 30 mg/kg was administered orally to the immunized mice once daily for three weeks before and/or three times daily for two weeks after the onset of CIA. The development of arthritis of the paws and cytokine levels in serum were examined. AMC significantly reduced the incidence and severity of CIA prophylactically and therapeutically, and suppressed the rise of systemic interleukin-6 and interferon-� �to the basal levels in the early phase of CIA. AMC also significantly suppressed the level of tumor necrosis factor-� in the severe phase of CIA. However, the levels of interleukin-10 and anti-collagen antibody were not affected by AMC. In the early phase of CIA, the suppression of interleukin-6 and interferon-� � by AMC correlated with the amelioration of symptoms of CIA in a dose-dependent manner. AMC may inhibit the onset of cytokine-mediated disease rather than suppressing disease progression without toxicity or affecting anti-collagen antibody production. AMC was significantly effective against CIA in mice and confirmed to possess cytokine-modulatory activity in vivo. The results suggest that AMC is a potential therapeutic agent for autoim- mune diseases.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"94 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2010-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"132562534","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}
I. Kubo, N. Masuoka, T. Ha, Kuniyoshi Shimizu, K. Nihei
{"title":"Multifunctional Antioxidant Activities of Alkyl Gallates","authors":"I. Kubo, N. Masuoka, T. Ha, Kuniyoshi Shimizu, K. Nihei","doi":"10.2174/1874847301003010001","DOIUrl":"https://doi.org/10.2174/1874847301003010001","url":null,"abstract":"A series (C 1 to C 16 ) of alkyl gallates was tested for their antioxidant activity for food protection and human health. One molecule of alkyl gallate, regardless of alkyl chain length, scavenges six molecules of 1,1-diphenyl-2- picrylhydrazyl (DPPH). Alkyl gallates inhibited the linoleic acid peroxidation catalyzed by soybean lipoxygenase-1 (EC 1.13.11.12, Type 1) without being oxidized. The progress curves for enzyme reactions were recorded by both spectropho- tometric and polarographic methods and the inhibitory activity was a parabolic function of their lipophilicity (log P) and maximized with alkyl chain length between C 12 and C 16 . Tetradecanyl (C 14 ) gallate exhibited the most potent inhibition with an IC 50 of 0.06 µM. The inhibition kinetics of dodecyl gallate (C 12 ) revealed competitive and slow-binding inhibi- tion. Alkyl gallates chelate transition metal ions and this chelation ability should be of considerable advantage as antioxi- dants. Additionally, gallic acid was found to inhibit superoxide anion generated by xanthine oxidase (EC 1.1.3.22) but did not inhibit enzymatically catalyzed uric acid formation.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2010-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130941525","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}
{"title":"Inhibitory Effects of Two Ferulates from Angelica Sinensis on Platelet Aggregation and Oxytocin-induced Uterine Contraction","authors":"Y. Yu, B. Lin, L. Yu, Y. Hua, J. Duan, S. P. Li","doi":"10.2174/1874847300902010043","DOIUrl":"https://doi.org/10.2174/1874847300902010043","url":null,"abstract":"Ferulic acid (FA) is widely considered as a biologically active component in Angelica sinensis, and used as one of the marker compounds for the quality control of Angelica sinensis. However, in A. sinensis, FA mainly exists as its es- ter, coniferyl ferulate (CF). CF is unstable and readily hydrolyzed into FA during conventional extraction. Herein, their antiplatelet aggregation activities and relaxant effects on oxytocin-induced mouse uterine muscle contraction were inves- tigated and compared. The results showed that FA inhibited arachidonic acid (AA), adenosine diphosphate (ADP) and thrombin (THR)-induced platelet aggregation with IC 50 values of 974.8 ± 97.5, 737.9 ± 40.2 and 244.6 ± 25.6 µg/ml, re- spectively. The potency of CF is much higher than that of FA, and the IC 50 values for AA, ADP and THR were 7.1 ± 0.3, 276.4 ± 53.4 and 77.5 ± 23.1 µg/ml, respectively. IC 50 of FA was 23.8 ± 6.2 ∝g/ml for oxytocin-induced uterine contrac- tion in vitro. CF could only be tested at low concentration and its IC 50 could not be calculated thereafter because of its strong hydrophobic property. So CF has more potent antiplatelet aggregation activity, while FA has stronger inhibitory ef- fect on oxytocin-induced uterine contraction in vitro.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130859968","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}
Jie Liu, Jun Shiono, Y. Tsuji, Kuniyoshi Shimizu, R. Kondo
{"title":"Methyl Ganoderic Acid DM: A Selective Potent Osteoclastogenesis Inhibitor","authors":"Jie Liu, Jun Shiono, Y. Tsuji, Kuniyoshi Shimizu, R. Kondo","doi":"10.2174/1874847300902010037","DOIUrl":"https://doi.org/10.2174/1874847300902010037","url":null,"abstract":"Increased osteoclastic bone resorption plays a central role in the pathogenesis of many bone diseases, and osteoclast inhibitors are the most widely used treatments for these diseases. Ganoderic acid DM, the main component of Ganoderma lucidum, has been known for its medicinal effects such as anti-androgen and anti-proliferative activities. In this study, we investigated the inhibitory effects of ganoderic acid DM and its analog (methyl ganoderic acid DM and 7- oxo-methyl ganoderic acid Z) on osteoclastogenesis using RAW264 cell in vitro. Methyl ganoderic acid DM blocked osteoclastogenesis completely at 12.5 μM with low cytotoxicity less than 30%. On the other hands, ganoderic acid DM blocked osteoclastogenesis completely at the higher concentration of 50 μM, but 7-oxo-methyl ganoderic acid Z did not up to 100 μM. These results implicated the carbonyl group at C-3 is essentially for selective osteoclastogenesis inhibitory activity, and methyl esters at C-26 should play an important role in enhancing its osteoclastogenesis inhibitory activity. Keyword: Ganoderma lucidum, methyl ganoderic acid DM, osteoporosis, rheumatoid arthritis.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"17 5","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-11-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131957118","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}
{"title":"Bioactive Alkaloids from South American Psychotria and Related Species","authors":"D. D. Porto, A. Henriques, A. Fett-Neto","doi":"10.2174/1874847300902010029","DOIUrl":"https://doi.org/10.2174/1874847300902010029","url":null,"abstract":"Many important molecules have been discovered from tropical and sub-tropical plant biodiversity. However, the largest part of the chemical profile of such biodiversity remains unknown. Combining ethnopharmacological and chemotaxonomical investigation can be a good strategy in bioactive compound discovery. South American Psychotria species studied by this approach proved to be a rich source of new bioactive alkaloids, some of which bear unique chemi- cal skeletons.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"25 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-09-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134594467","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}
{"title":"Development of Drug Resistance in Trichomonas vaginalis and its Overcoming with Natural Products","authors":"Stefanie M. Gehrig, T. Efferth","doi":"10.2174/1874847300902010021","DOIUrl":"https://doi.org/10.2174/1874847300902010021","url":null,"abstract":"Trichomoniasis is an infectious disease afflicting women worldwide. The protozoan parasite Trichomonas vaginalis is the causative agent of this sexually-transmitted disease, including also men in its infection cycle. The disease is usually not life-threatening, but has been associated with the development of cervical cancer and increased susceptibil- ity to HIV. Approved drugs are 5-nitroimidazoles, with metronidazole being the drug of first choice. These drugs act via induction of oxidative stress and DNA-damage, leading to cell death in the parasite. Nevertheless, with the development of resistant T. vaginalis strains the treatment of the disease becomes exceedingly difficult. Mechanisms of drug resistance are characterized by reduced expression or even loss of proteins necessary for drug activation and a decreased reductive nature in the parasite. A promising strategy for research into new drugs and moreover, to overcome drug resistance, are compounds derived from natural sources. The present study provides a summary of all so far investigated small molecules with antitrichomonal activity; promisingly, some also show efficacy against resistant strains. Whereas the list of chemically characterized compounds derived from plants is rather short, literature provides immense applications of crude plant extracts tested against T. vaginalis. This demonstrates the absence of studies in this field aimed to identify and isolate single natural products exhibiting antitrichomonal features. Likewise, elucidating their mode of action on a molecular basis is of paramount importance.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130282631","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}
{"title":"Colon and Breast Anti-cancer Effects of Peptide Hydrolysates Derived from Rice Bran","authors":"A. Kannan, N. Hettiarachchy, S. Narayan","doi":"10.2174/1874847300902010017","DOIUrl":"https://doi.org/10.2174/1874847300902010017","url":null,"abstract":"Rice bran is an economical, under-utilized co-product of rough rice milling. The objective of this study was to produce rice-bran peptides and investigate for anti-cancer activity. Protein hydrolysates were prepared by treating heat stabilized defatted rice-bran with food grade Alcalase enzyme, followed by treatment with simulated gastric and intestinal juices to obtain resistant peptides. Resistant peptides were fractionated into >50, 10-50, 5-10, and <5 kDa sizes, freeze dried, and evaluated for inhibitory and cytotoxicity activities on human colon (HCT-116) and breast (HTB-26) cancer cell lines. The results showed that <5 kDa fraction of rice-bran is a potent anti-cancer agent. The cytotoxicity of the fraction to both cancer cell types was more pronounced after the treatment with 500 � g/mL. The IC50 of the peptide fraction was ap- proximately 750 � g/mL. These results indicate that the <5 kDa peptide fraction separated from rice bran protein hydro- lysate has a potent anti-tumor activity for colon cancer cells. The peptide fractions that demonstrate anti-cancer activities have the potential for use as functional food ingredients for health benefits.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"23 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"125294276","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}