• Title/Summary/Keyword: Bioactive agents

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Synthesis and in Vitro Antimicrobial Evaluation of Benzothiazole Incorporated Thiazolidin-4-ones Derivatives

  • Agarwal, Shikha;Agarwal, Dinesh Kumar;Gautam, Naveen;Agarwal, Kshamta;Gautam, Dinesh Chandra
    • Journal of the Korean Chemical Society
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    • v.58 no.1
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    • pp.33-38
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    • 2014
  • In the course of work on new pharmacologically active antimicrobial agents, we have reported the synthesis of a new class of structurally novel derivatives, incorporating two bioactive structures, a benzothiazole and thiazolidin-4-one, to yield a class of compounds having interesting antimicrobial properties. The antimicrobial properties of the synthesized compounds were investigated against bacteria (Staphylococcus aureus and Escherchia coli) and fungi (Candida albicans and Aspergillus niger) using serial plate dilution method. The structure of the synthesized compounds have been established by elemental analysis and spectroscopic data.

Anti-inflammatory Effect of an Ethanolic Extract of Myagropsis yendoi in Lipopolysaccharide-Stimulated BV-2 Microglia Cells

  • Salih, Sarmad Ali;Kim, Hyeung-Rak
    • Fisheries and Aquatic Sciences
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    • v.17 no.1
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    • pp.27-35
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    • 2014
  • Marine brown algae have been identified as a rich source of structurally diverse bioactive compounds. Whether Myagropsis yendoi ethanolic extracts (MYE) inhibit inflammatory responses was investigated using lipopolysaccharide (LPS)-stimulated microglia BV-2 cells. MYE inhibited LPS-induced nitric oxide (NO) production in a dose-dependent manner and suppressed the expression of inducible nitric oxide synthase in BV-2 cells. MYE also reduced the production of pro-inflammatory cytokines in LPS-stimulated BV-2 cells. LPS-induced nuclear factor-${\kappa}B$ (NF-${\kappa}B$) transcriptional activity and NF-${\kappa}B$ translocation into the nucleus were significantly inhibited by MYE treatment through preventing degradation of the inhibitor ${\kappa}B-{\alpha}$. Moreover, MYE inhibited the phosphorylation of AKT, ERK, JNK, and p38 mitogen-activated protein kinase in LPS-stimulated BV-2 cells. These results indicate that MYE is a potential source of therapeutic or functional agents for neuroinflammatory diseases.

Screening of Arachidonic Acid Cascade Related Enzymes Inhibitors from Korean Indigenous Plants (2) (한국 자생식물로부터 아라키돈산 대사계 효소 저해제 검색 (2))

  • 정혜진;문태철;이은경;손건호;김현표;강삼식;배기환;안인파;권동렬
    • YAKHAK HOEJI
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    • v.47 no.2
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    • pp.69-77
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    • 2003
  • Arachidonic acid (AA), which is stored in membrane glycerophospholipids, is liberated by phospholipase $A_2$ (PLA$_2$) enzymes and is sequentially converted to cyclooxygenases (COXs) and lipoxygenases (LOXs) then to various bioactive PGs, and LTs. In order to find the specific inhibitors of AA metabolism especially PLA$_2$, COX-2, 5-LO and lyso PAF acetyltransferase, 120 Korean residential plants extracts were evaluated for their inhibitory activity on PGD$_2$, LTC$_4$ production from cytokine-induced mouse bone marrow-derived mast cells (BMMC) and arachidonic acid released from phospholipid and PAF production from lyso PAF. From this screening procedure, methanol extract of ten indigenous plant such as Salix gracilistyla, Sedum kamtschaticum, Cirsium chanroenicum, Hypericum ascyron, Astilbe chinensis, Agrimonia pilosa, Aristolochia manshuriensis, Vodia daniellii, Pyrola japonica, Styrax obassia were found to inhibit production of inflammatory mediators in vitro assay system.

Bacterial endophytes from ginseng and their biotechnological application

  • Chu, Luan Luong;Bae, Hanhong
    • Journal of Ginseng Research
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    • v.46 no.1
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    • pp.1-10
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    • 2022
  • Ginseng has been well-known as a medicinal plant for thousands of years. Bacterial endophytes ubiquitously colonize the inside tissues of ginseng without any disease symptoms. The identification of bacterial endophytes is conducted through either the internal transcribed spacer region combined with ribosomal sequences or metagenomics. Bacterial endophyte communities differ in their diversity and composition profile, depending on the geographical location, cultivation condition, and tissue, age, and species of ginseng. Bacterial endophytes have a significant effect on the growth of ginseng through indole-3-acetic acid (IAA) and siderophore production, phosphate solubilization, and nitrogen fixation. Moreover, bacterial endophytes can protect ginseng by acting as biocontrol agents. Interestingly, bacterial endophytes isolated from Panax species have the potential to produce ginsenosides and bioactive metabolites, which can be used in the production of food and medicine. The ability of bacterial endophytes to transform major ginsenosides into minor ginsenosides using β-glucosidase is gaining increasing attention as a promising biotechnology. Recently, metabolic engineering has accelerated the possibilities for potential applications of bacterial endophytes in producing beneficial secondary metabolites.

Effect of Puffing in the Extraction of Active Ingredients from the Roots of Paeonia lactiflora and Astragalus membranaceus

  • Lee, Hyojin;Jang, Kyoung Won
    • Natural Product Sciences
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    • v.28 no.2
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    • pp.89-92
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    • 2022
  • In Asia, the roots of Paeonia lactiflora and Astragalus membranaceus have been used as therapeutic agents for thousands of years. Once the medicinal plants are harvested, they are dried and their ingredients are extracted by heat-mediated reflux extraction. However, the condensed structure of organic products (especially roots) limits the extraction of bioactive components. In this study, we assessed the effect of the puffing method (using high temperature and pressure) before the extraction process in relation to the profile and antioxidant capacity of active ingredients. We demonstrated that the additional puffing process before extraction methods improves the yield of polyphenol concentrations and antioxidant activities from the roots of P. lactiflora and A. membranaceus.

Pharmacological potential of ginseng and ginsenosides in nonalcoholic fatty liver disease and nonalcoholic steatohepatitis

  • Young-Su Yi
    • Journal of Ginseng Research
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    • v.48 no.2
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    • pp.122-128
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    • 2024
  • Nonalcoholic fatty liver disease (NAFLD) is a chronic liver disease characterized by hepatic fat accumulation, while nonalcoholic steatohepatitis (NASH) is an advanced form of NAFLD characterized by hepatic inflammation, fibrosis, and liver injury, resulting in liver cirrhosis and hepatocellular carcinoma (HCC). Given the evidence that ginseng and its major bioactive components, ginsenosides, have potent anti-adipogenic, anti-inflammatory, anti-oxidative, and anti-fibrogenic effects, the pharmacological effect of ginseng and ginsenosides on NAFLD and NASH is noteworthy. Furthermore, numerous studies have successfully demonstrated the protective effect of ginseng on these diseases, as well as the underlying mechanisms in animal disease models and cells, such as hepatocytes and macrophages. This review discusses recent studies that explore the pharmacological roles of ginseng and ginsenosides in NAFLD and NASH and highlights their potential as agents to prevent and treat NAFLD, NASH, and liver diseases caused by hepatic steatosis and inflammation.

Comparative Reverse Screening Approach to Identify Potential Anti-neoplastic Targets of Saffron Functional Components and Binding Mode

  • Bhattacharjee, Biplab;Vijayasarathy, Sandhya;Karunakar, Prashantha;Chatterjee, Jhinuk
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.11
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    • pp.5605-5611
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    • 2012
  • Background: In the last two decades, pioneering research on anti-tumour activity of saffron has shed light on the role of crocetin, picrocrocin and safranal, as broad spectrum anti-neoplastic agents. However, the exact mechanisms have yet to be elucidated. Identification and characterization of the targets of bioactive constituents will play an imperative role in demystifying the complex anti-neoplastic machinery. Methods: In the quest of potential target identification, a dual virtual screening approach utilizing two inverse screening systems, one predicated on idTarget and the other on PharmMapper was here employed. A set of target proteins associated with multiple forms of cancer and ranked by Fit Score and Binding energy were obtained from the two independent inverse screening platforms. The validity of the results was checked by meticulously analyzing the post-docking binding pose of the picrocrocin with Hsp90 alpha in AutoDock. Results: The docking pose reveals that electrostatic and hydrogen bonds play the key role in inter-molecular interactions in ligand binding. Picrocrocin binds to the Hsp90 alpha with a definite orientation appropriate for nucleophilic attacks by several electrical residues inside the Hsp90-alpha ATPase catalytic site. Conclusion: This study reveals functional information about the anti-tumor mechanism of saffron bioactive constituents. Also, a tractable set of anti-neoplastic targets for saffron has been generated in this study which can be further authenticated by in vivo and in vitro experiments.

Ingestion of Gouda Cheese Ameliorates the Chronic Unpredictable Mild Stress in Mice

  • Yun, Bohyun;Yoo, Ja Yeon;Park, Mi Ri;Ryu, Sangdon;Lee, Woong Ji;Choi, Hye Jin;Kang, Min Kyoung;Kim, Younghoon;Oh, Sangnam
    • Food Science of Animal Resources
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    • v.40 no.1
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    • pp.145-153
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    • 2020
  • Depression is a kind of mood disorder characterized by decline in motivation, interest, attention, mental activity, and appetite. Although depression is caused by a variety of causes, including genetic, endocrine and environmental stress, mild depression has been reported to improve with diet. Therefore, various type of food sources including functional and nutritional supplement are required to treat the depressive patients. Cheese contains bioactive peptides that have beneficial effects on host health. In particular, Jersey milk has been reported to contain higher solids than does Holstein milk. This study investigated the effects of Gouda cheese from Jersey and Holstein milk on chronic, unpredictable, mildly stressed (CUMS) mice. Here, spontaneous alterations in cheese-fed stressed mice were noted to be effectively recovered with statistical significance regardless cow species. Interestingly, for the analysis of fecal microbiota, Bacteroidetes were noted to increase with a reduction in Firmicutes at the phylum level with Jersey cheese. Taken together, we suggest that cheese intake provided a beneficial effect on stressed mice in recovering recognition ability. In particular, changes in internal microbiota were observed, suggesting that the bioactive ingredients in cheese act as improvement agents with respect to mood and brain function.

Inhibition of MMP-2 and MMP-9 activities by solvent-partitioned Sargassum horneri extracts

  • Karadeniz, Fatih;Lee, Seul-Gi;Oh, Jung Hwan;Kim, Jung-Ae;Kong, Chang-Suk
    • Fisheries and Aquatic Sciences
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    • v.21 no.6
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    • pp.16.1-16.7
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    • 2018
  • Background: Matrix metalloproteinases (MMPs) are linked with several complications such as metastasis of cancer progression, oxidative stress, and hepatic fibrosis. Brown seaweeds are being extensively studied for their bioactive molecule content against cancer progression. In this context, Sargassum horneri was reported to possess various bioactivities including antiviral, antimicrobial, and anti-inflammatory partly due to its phenolic compound content. Methods: In this study, potential of S. horneri was evaluated through anti-MMP effect in HT1080 fibrosarcoma cells. S. horneri crude extract was fractionated with organic solvents, namely, water ($H_2O$), n-buthanol (n-BuOH), 85% aqueous methanol (85% aq. MeOH), and n-hexane. The non-toxicity of fraction samples (Sargassum horneri solvent-partitioned extracts (SHEs)) was confirmed by cell-viability assay. SHEs were tested for their ability to inhibit MMP enzymatic activity through gelatin digestion evaluation and cell migration assay. Expressions of MMP-2 and MMP-9 and tissue inhibitors of MMP (TIMPs) were evaluated by reverse transcription and Western blotting. Results: All fractions inhibited the enzymatic activities of MMP-2 and MMP-9 according to gelatin zymography. Except $H_2O$ fraction, fractions hindered the cell migration significantly. All tested fractions suppressed both mRNA and protein levels of MMP-2, MMP-9, TIMP-1, and TIMP-2. Conclusion: Overall, current results suggested that S. horneri has potential to be a good source for anti-MMP agents, and further investigations are underway for better understanding of the action mechanism and isolation and elucidation of the bioactive molecules.

Marine Algae and Their Potential Application as Antimicrobial Agents

  • Charway, Grace N.A.;Yenumula, Padmini;Kim, Young-Mog
    • Journal of Food Hygiene and Safety
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    • v.33 no.3
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    • pp.151-156
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    • 2018
  • The world is becoming overwhelmed with widespread diseases as antibiotic resistance increases at an alarming rate. Hence, there is a demanding need for the discovery and development of new antimicrobial drugs. The ocean is gifted with many organisms like phytoplankton, algae, sponges, cnidarians, bryozoans, mollusk, tunicates and echinoderms, which are known to produce a wide variety of bioactive secondary metabolites with pharmacological properties. Many new therapeutic drugs have emerged from marine invertebrates, although the large algal community is yet to be explored. The bioactivity possessing secondary metabolites of marine algae include polyphenols, phlorotannins, alkaloids, halogenated compounds, sulfated polysaccharides, agar, carrageenan, proteoglycans, alginate, laminaran, rhamnan sulfate, galactosylglycerol, and fucoidan. These metabolites have been found to have great antimicrobial activities against many human aliments. Studies show that the algal community represents about 9% of biomedical compounds obtained from the sea. This review looks at the evolution of drugs from the ocean, with a special emphasis on the antimicrobial activities of marine algae.