• Title/Summary/Keyword: bioactive metabolites

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Inhibitory Effects of 12 Ginsenosides on the Activities of Seven Cytochromes P450 in Human Liver Microsomes

  • Jo, Jung Jae;Shrestha, Riya;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • v.7 no.4
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    • pp.106-110
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    • 2016
  • Ginseng, a traditional herbal drug, has been used in Eastern Asia for more than 2000 years. Various ginsenosides, which are the major bioactive components of ginseng products, have been shown to exert numerous beneficial effects on the human body when co-administered with drugs. However, this may give rise to ginsenoside-drug interactions, which is an important research consideration. In this study, acassette assay was performed the inhibitory effects of 12 ginsenosides on seven cytochrome P450 (CYP) isoforms in human liver microsomes (HLMs) using LC-MS/MS to predict the herb-drug interaction. After incubation of the 12 ginsenosides with seven cocktail CYP probes, the generated specific metabolites were quantified by LC-MS/MS to determine their activities. Ginsenoside Rb1 and F2 showed strong selective inhibitory effect on CYP2C9-catalyzed diclofenac 4'-hydroxylation and CYP2B6-catalyzed bupropion hydroxylation, respectively. Ginsenosides Rd showed weak inhibitory effect on the activities of CYP2B6, 2C9, 2C19, 2D6, 3A4, and compound K, while ginsenoside Rg3 showed weak inhibitory effects on CYP2B6. Other ginsenosides, Rc, Rf, Rg1, Rh1, Rf, and Re did not show significant inhibitory effects on the activities of the seven CYPs in HLM. Owing to the poor absorption of ginsenosides after oral administration in vivo, ginsenosides may not have significant side effects caused by interaction with other drugs.

Sulfoquinovosylmonoacylglycerols regulating intestinal inflammation in co-culture system from the brown alga Turbinaria ornata

  • Lee, Seon Min;Kim, Na-Hyun;Ji, Yeong Kwang;Kim, Yun Na;Jeon, You-Jin;Heo, Jeong Doo;Jeong, Eun Ju;Rho, Jung-Rae
    • ALGAE
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    • v.35 no.2
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    • pp.201-212
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    • 2020
  • The inflammatory bowel diseases (IBD) including ulcerative colitis and Crohn disease are characterized by chronic inflammation throughout the gastrointestinal tract. The prevalence of IBD has been increasing worldwide, and has sometimes led to irreversible impairment of gastrointestinal structure and functions. In the present study, we identified a new sulfoquinovosylmonoacylglycerols (SQMG) (1) together with two known SQMGs (2 and 3) regulating intestinal inflammation from the brown alga Turbinaria ornata. The anti-inflammatory properties of two bioactive SQMGs, 1 and 2 were evaluated using an in vitro co-culture system consisting of human epithelial Caco-2 cells and PMA (phorbol 12-myristate 12-acetate)-differentiated THP-1 macrophages. Treatment with 1 or 2 inhibited the production nitric oxide and prostaglandin E2 induced by lipopolysaccharide and interferon γ challenge. The expressions of inducible nitric oxide synthase and cyclooxygenase 2 were markedly down-regulated in response to inhibition of nuclear factor κB translocation to nucleus. These findings suggest the potential use of the brown alga T. ornata and its biologically active metabolites SQMGs as pharmaceutical adjuvants in the treatment of inflammation-related diseases, including IBD.

Proteolytic System of Streptococcus thermophilus

  • Rodriguez-Serrano, G.M.;Garcia-Garibay, M.;Cruz-Guerrero, A.E.;Gomez-Ruiz, L.;Ayala-Nino, A.;Castaneda-Ovando, A.;Gonzalez-Olivares, L.G.
    • Journal of Microbiology and Biotechnology
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    • v.28 no.10
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    • pp.1581-1588
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    • 2018
  • The growth of lactic acid bacteria (LAB) generates a high number of metabolites related to aromas and flavors in fermented dairy foods. These microbial proteases are involved in protein hydrolysis that produces necessary peptides for their growth and releases different molecules of interest, like bioactive peptides, during their activity. Each genus in particular has its own proteolytic system to hydrolyze the necessary proteins to meet its requirements. This review aims to highlight the differences between the proteolytic systems of Streptococcus thermophilus and other lactic acid bacteria (Lactococcus and Lactobacillus) since they are microorganisms that are frequently used in combination with other LAB in the elaboration of fermented dairy products. Based on genetic studies and in vitro and in vivo tests, the proteolytic system of Streptococcus thermophilus has been divided into three parts: 1) a serine proteinase linked to the cellular wall that is activated in the absence of glutamine and methionine; 2) the transport of peptides and oligopeptides, which are integrated in both the Dpp system and the Ami system, respectively; according to this, it is worth mentioning that the Ami system is able to transport peptides with up to 23 amino acids while the Opp system of Lactococcus or Lactobacillus transports chains with less than 13 amino acids; and finally, 3) peptide hydrolysis by intracellular peptidases, including a group of three exclusive of S. thermophilus capable of releasing either aromatic amino acids or peptides with aromatic amino acids.

Anti-Inflammatory Effect of Violapyrones B and C from a Marine-derived Streptomyces sp.

  • Lee, Hwa-Sun;An, Bong-Jeun;Kim, Hyeon Jeong;Cho, Yong Hun;Kim, Dong In;Jang, Jae Yoon;Kwak, Jae Hoon;Lee, Hyi-Seung;Lee, Yeon-Ju;Lee, Jong Seok;Shin, Hee Jae
    • Natural Product Sciences
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    • v.21 no.4
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    • pp.251-254
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    • 2015
  • Recently, we reported violapyrones B, C, H and I, unusual 3, 4, 6-trisubstituted ${\alpha}-pyrones$ derivatives, from the culture broth of the marine Streptomyces sp. 112CH148. In previous studies, violapyrones have been shown to have antibacterial and antitumor activities. However, the anti-inflammatory effect of violapyrones has not been reported yet. As part of our ongoing study for the discovery of bioactive metabolites from marine microorganisms, we found that violapyrones also have anti-inflammatory activity. In this study, we investigated the effect of violapyrones on LPS-induced inflammatory responses in vitro. Violapyrones B and C did not affect the viability of RAW 264.7 cells at concentrations up to $25{\mu}M$. However, violapyrones B and C inhibited the production of NO compared to the LPS-induced control. In addition, violapyrones B and C down-regulated the expression of iNOS protein in LPS-stimulated RAW 264.7 cells. To the best of our knowledge, this is the first report on the anti-inflammatory activity of violapyrones B and C.

Screening for Antifungal Endophytic Fungi Against Six Plant Pathogenic Fungi

  • Park, Joong-Hyeop;Park, Ji-Hyun;Choi, Gyung-Ja;Lee, Seon-Woo;Jang, Kyoung-Soo;Choi, Yong-Ho;Cho, Kwang-Yun;Kim, Jin-Cheol
    • Mycobiology
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    • v.31 no.3
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    • pp.179-182
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    • 2003
  • A total of 187 endophytic fungi were isolated from 11 plant species, which were collected from 11 locations in Korea. Their antifungal activities were screened in vivo by antifungal bioassays after they were cultured in potato dextrose broth and rice solid media. Antifungal activity against plant pathogenic fungi such as Magnaporthe grisea(rice blast), Corticium sasaki(rice sheath blight), Botrytis cinerea(tomato gray mold), Phytophthora infestans(tomato late blight), Puccinia recondita(wheat leaf rust), and Blumeria graminis f. sp. hordei(barley powdery mildew) was determined in vivo by observing the inhibition of plant disease development. Twenty(11.7%) endophytic fungi fermentation broths were able to control, by more than 90%, at least one of the six plant diseases tested. Among 187 liquid broths, the F0010 strain isolated from Abies holophylla had the most potent disease control activity; it showed control values of more than 90% against five plant diseases, except for tomato late blight. On the other hand, fourteen(7.5%) solid culture extracts exhibited potent disease control values of more than 90% against one of six plant diseases. The screening results of this study strongly suggested that metabolites of plant endophytic fungi could be good potential sources for screening programs of bioactive natural products.

Chemical Constituents from the Aerial Parts of Vernonia cinerea L. and Their Anti-Inflammatory Activity (베르노니아 시네레아 지상부의 화학 성분 및 항염증 활성)

  • Youn, Ui Joung;Chang, Leng Chee
    • Korean Journal of Medicinal Crop Science
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    • v.24 no.6
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    • pp.437-443
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    • 2016
  • Background: Previous phytochemical studies of whole Vernonia cinerea L. plants have identified sesquiterpene lactones, sterols, and triterpenes, which possess anticancer, antifeedant, and antimalarial activities. However, there are no reports of other types of bioactive metabolites. Therefore, the present study aimed to identify phenolic compounds with anti-inflammatory activity in the aerial parts of the plant. Methods and Results: Compounds were isolated from the aerial parts of V. cinerea using a silica and C-18 gel columns and semi-preparative HPLC instrument, and the structures of the compounds were determined using one- and two- dimension nuclear magnetic resonance spectroscopy and mass spectroscopy. The chloroform soluble extracts and isolated compounds were evaluated for their anti-inflammatory potential based on their ability to inhibit nitric oxide production and $TNF-{\alpha}$ induced $NF-{\kappa}B$ activity. Conclusions: Phytochemical study of the aerial parts of V. cinerea led to the isolation of six phenolic compounds. Compound 1 was a major metabolite, and to the best of our knowledge, compounds 2 - 6 were isolated from V.cinerea for the first time. Among the isolates, compounds 1 and 3 exhibited $TNF-{\alpha}$-induced $NF-{\kappa}B$ activity with $IC_{50}$ values of 7.5 and 11.5 M, respectively, and the inhibitory activity of phenyl propanoid compound 3 on $TNF-{\alpha}$-induced $NF-{\kappa}B$ was evaluated for the first time.

Gibberellin-Producing Endophytic Fungi Isolated from Monochoria vaginalis

  • Ahmad, Nadeem;Hamayun, Muhammad;Khan, Sumera Afzal;Khan, Abdul Latif;Lee, In-Jung;Shin, Dong-Hyun
    • Journal of Microbiology and Biotechnology
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    • v.20 no.12
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    • pp.1744-1749
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    • 2010
  • The role of endophytic fungi in plant growth and development is well documented. However, endophytic fungi with growth promotion capacity have never been isolated from weeds previously. In the current study, we isolated 8 fungal endophytes from the roots of Monochoria vaginalis, a serious weed of rice paddy in Korea. These isolates were screened on Waito-C, in order to identify plant growth promoting metabolites. Two fungal isolates (M5.A & M1.5) significantly promoted the plant height and shoot length of Waito-C during preliminary screening experiments. The culture filtrates (CFs) of M5.A and M1.5 also promoted the shoot length of Echinocloa crusgalli. Gibberellins (GAs) analysis of the CFs of M5.A and M1.5 showed that these endophytic fungi secrete higher quantities of GAs as compared with wild-type G. fujikuroi KCCM12329. The CF of M5.A contained bioactive GAs ($GA_3$, 2.8 ng/ml; $GA_4$, 2.6 ng/ml, and $GA_7$, 6.68 ng/ml) in conjunction with physiologically inactive $GA_9$ (1.61 ng/ml) and $GA_{24}$ (0.18 ng/ml). The CF of M1.5 contained physiologically active GAs ($GA_3$, 1.64 ng/ml; $GA_4$, 1.37 ng/ml and $GA_7$, 6.29 ng/ml) in conjunction with physiologically inactive $GA_9$ (3.44 ng/ml), $GA_{12}$ (0.3 ng/ml), and $GA_{24}$ (0.59 ng/ml). M5.A and M1.5 were identified as new strains of Penicillium sp. and Aspergillus sp., respectively, based on their 18S rDNA sequence homology and phylogenetic analysis.

Potential Evaluation and Health Fostering Intrinsic Traits of Novel Probiotic Strain Enterococcus durans F3 Isolated from the Gut of Fresh Water Fish Catla catla

  • Alshammari, Eyad;Patel, Mitesh;Sachidanandan, Manojkumar;Kumar, Prashant;Adnan, Mohd
    • Food Science of Animal Resources
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    • v.39 no.5
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    • pp.844-861
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    • 2019
  • Over the last few years, marine environment was found to be a source of surplus natural products and microorganisms with new bioactive secondary metabolites of interest which can divulge nutritional and biological impact on the host. This study aims to assess the possible, inherent and functional probiotic properties of a novel probiotic strain Enterococcus durans F3 (E. durans F3) isolated from the gut of fresh water fish Catla catla. Parameters for evaluating and describing the probiotics described in FAD/WHO guidelines were followed. E. durans F3 demonstrated affirmative results including simulated bile, acid and gastric juice tolerance with exhibited significant bactericidal effect against pathogens Staphylococcus aureus, Salmonella Typhi, Escherichia coli and Pseudomonas aeruginosa. This can be due to the enterocin produced by E. durans F3 strain, which was resolute by sodium dodecyl sulphate polyacrylamide gel electrophoresis (SDS-PAGE) gel with amplification of the anticipated fragment of a structural gene; enterocin A, followed by antibiotic susceptibility assessment. Effective antioxidant potentiality against ${\alpha}$-diphenyl-${\alpha}$-picrylhydrazyl free radicals including lipase, bile salt hydrolase activity with auto-aggregation and cell surface hydrophobicity was similarly observed. Results are proving the potentiality of E. durans F3, which can also be used as probiotic starter culture in dairy industries for manufacturing new products that imparts health benefits to the host. Finding the potent and novel probiotic strains will also satisfy the current developing market demand for probiotics.

LAB Fermentation Improves Production of Bioactive Compounds and Antioxidant Activity of Withania somnifera Extract and Its Metabolic Signatures as Revealed by LC-MS/MS

  • Yu, Jinhui;Geng, Yun;Xia, Han;Ma, Deyuan;Liu, Chao;Wu, Rina;Wu, Junrui;You, Shengbo;Bi, Yuping
    • Journal of Microbiology and Biotechnology
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    • v.32 no.4
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    • pp.473-483
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    • 2022
  • In this study we investigated the effect of lactic acid bacteria (LAB) fermentation on the ingredients and anti-oxidant activity of Withania somnifera extract. Four strains of LAB could proliferate normally in medium containing W. somnifera extract after the pH reached 3.1~3.5. LAB fermentation increased the content of alcohols and ketones, endowing the extract with the characteristic aroma of fermentation. Compared to the control, the DPPH and ABTS free radical scavenging rates in the fermented samples were significantly improved, ranging from 48.5% to 59.6% and 1.2% to 6.4%. The content of total phenols was significantly increased by 36.1% during the fermentation of mixed bacteria. Moreover, the original composition spectrum of the extract was significantly changed while the differentially accumulated metabolites (DAMs) were closely related to bile secretion, tryptophan metabolism and purine metabolism. Therefore, LAB fermentation can be used as a promising way to improve the flavor and bioactivity of the extracts of W. somnifera, making the ferments more attractive for use as functional food.

Quality and composition of eggs laid by hens fed with Cordyceps militaris-supplemented feed (동충하초 첨가 사료가 달걀의 품질 및 조성에 미치는 영향)

  • Ayman, Turk;Min Hee, Kim;So Yeong, Jeong;Beom Seok, Kim;Sung-I, Woo;Won Ho, Lee;Mi Kyeong, Lee
    • Journal of Mushroom
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    • v.20 no.4
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    • pp.254-257
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    • 2022
  • Owing to its excellent nutritional value, eggs are among the most important components of the human diet. Gender and environmental factors, such as feed composition, may alter the nutritional profile and quality of eggs. Feed additives have recently been used to enhance the health and productivity of hens, which has resulted in the production of higher-quality eggs. The fungus Cordyceps militaris, a well-established source of traditional medicines, contains potential bioactive metabolites, which prompted us to examine the effects of C. militaris-supplemented diets on the quality of hens' eggs. The hens of two species (Gallus gallus domesticus and Araucana) were fed with one of three different diets: a control diet and diets supplemented with 2% or 5% of C. militaris. Egg quality was determined by measuring the Haugh Unit, yolk color, and shell thickness. In addition, egg and shell densities together with the ratio of yolk to albumen were calculated. Eggshell thickness and yolk color were both enhanced by the addition of C. militaris, whereas Haugh Unit values were somewhat reduced. Egg size, eggshell weight, and yolk and albumen production were all enhanced by C. militaris supplementation. Notably, in hens fed the 2% C. militaris-supplemented diet, enhancement was more evident in the yolk than in the albumen. The overall quality of the egg yolk was enhanced when 2% C. militaris was added to the hens' diet, which led to increases in both yolk color and quantity. Eggshell thickness and weight were also higher among eggs laid by hens fed the supplemented diets. Although these effects differed depending on the chicken species, we established that, in general, C. militaris contributes to improving egg quality.