• Title/Summary/Keyword: Cytotoxic and antifungal activities

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C-Flavonoidal Glycosides from Erythrina caffra Flowers

  • El-Masry, Sawsan;Hammoda, Hala M.;Radwan, Mohamed M.;Ross, Samir A.;Zaatout, Hala H.
    • Natural Product Sciences
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    • v.16 no.4
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    • pp.217-222
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    • 2010
  • A phytochemical investigation of the ethanolic extract of Erythrina caffra flowers from an Egyptian origin yielded three C-flavonoidal glycosides; 5,7,4'-trihydroxyflavone-8-C-$\beta$-D-glucopyranoside (vitexin) (1), 5,7,4'-trihydroxyflavone-6-C-$\beta$-D-glucopyranosyl-(1 $\rightarrow$ 2)-$\beta$-D-glucopyranoside (isovitexin-2"-$\beta$-D-glucopyranoside) (2), 5, 7, 4'-trihydroxyflavone-6, 8-di-C-$\beta$-D-glucopyranoside (vicenin-2) (3) and one O-flavonoidal glycoside; kaempferol-3-O-$\beta$-D.glucopyranosyl) (1 $\rightarrow$ 2)-$\beta$-D-glucopyranoside (4). The structures of the isolated compounds (1 - 4) were elucidated using different spectral techniques (UV, 1D and 2D NMR and HRESIMS). This is the first report for the isolation of flavonoidal glycosides from Erythrina caffra. The antibacterial, antifungal, antimalarial, and antileishmanial activities of the isolates were evaluated. In addition, the cytotoxic activity of the ethanolic extract and the main fractions were tested using brine shrimp bioassay.

Influences of Hinge Region of a Systhetic Antimicrobial Peptide, Cecropin A(1-13)-Melittin(1-13) Hybrid on Antibiotic Activity

  • 신송엽;강주현;이동건;장소윤;서무열;김길룡;함경수
    • Bulletin of the Korean Chemical Society
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    • v.20 no.9
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    • pp.1078-1084
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    • 1999
  • A synthetic cecropin A(1-13)-melittin(1-13) [CA-ME] hybrid peptide was known to be an antimicrobial peptide having strong antibacterial, antifungal and antitumor activity with minimal cytotoxic effect against human erythrocyte. Analogues were synthesized to investigate the influences of the flexible hinge region of CA-ME on the antibiotic activity. Antibiotic activity of the peptides was measured by the growth inhibition against bac-terial, fungal and tumor cells and vesicle-aggregating or disrupting activity. The deletion of Gln-Gly-Ile (P1) or Gly-Gln-Gly-Ile-Gly (P3) from CA-ME brought about a significant decrease on the antibiotic activities. In contrast, Gly-Ile-Gly deletion (P2) from CA-ME or Pro insertion (P5) instead of Gly-Gln-Gly-Ile-Gly of CA-ME retained antibiotic activity. This result indicated that the flexible hinge or β-bend structure provided by Gly-Gln-Gly-Ile-Gly, Gln-Gly, or Pro in the central region of the peptides is requisite for its effective antibiotic activity and may facilitate easily the hydrophobic C-terminal region of the peptide to penetrate the lipid bilayers of the target cell membrane. In contrast, P4 and P6 with Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central region of the peptide caused a drastic reduction on the antibiotic activities. This result suggested that the con-secutive β-bend structure provided by Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central hinge region of the peptide seems to interrupt the ion channel/pore formation on the target cell membranes.

Crotamine stimulates phagocytic activity by inducing nitric oxide and TNF-α via p38 and NFκ-B signaling in RAW 264.7 macrophages

  • Lee, Kyung Jin;Kim, Yun Kyu;Krupa, Martin;Nguyen, Anh Ngoc;Do, Bich Hang;Chung, Boram;Vu, Thi Thu Trang;Kim, Song Cheol;Choe, Han
    • BMB Reports
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    • v.49 no.3
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    • pp.185-190
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    • 2016
  • Crotamine is a peptide toxin found in the venom of the rattlesnake Crotalus durissus terrificus and has antiproliferative, antimicrobial, and antifungal activities. Herein, we show that crotamine dose-dependently induced macrophage phagocytic and cytostatic activity by the induction of nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α). Moreover, the crotamineinduced expression of iNOS and TNF-α is mediated through the phosphorylation of p38 and the NF-κB signaling cascade in macrophages. Notably, pretreatment with SB203580 (a p38-specific inhibitor) or BAY 11-7082 (an NF-κB inhibitor) inhibited crotamine-induced NO production and macrophage phagocytic and cytotoxic activity. Our results show for the first time that crotamine stimulates macrophage phagocytic and cytostatic activity by induction of NO and TNF-α via the p38 and NF-κB signaling pathways and suggest that crotamine may be a useful therapeutic agent for the treatment of inflammatory disease.

Antishigellosis and Cytotoxic Potency of Crude Extracts and Isolated Constituents from Duranta repens

  • Nikkon, Farjana;Habib, M. Rowshanul;Karim, M. Rezaul;Hossain, M. Shamim;Mosaddik, M. Ashik;Haque, M. Ekramul
    • Mycobiology
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    • v.36 no.3
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    • pp.173-177
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    • 2008
  • The crude ethanol extracts (stem and fruits), their fractions and two triterpenes, $\beta$-Amyrin and 12-Oleanene 3$\beta$, 21$\beta$-diol, isolated as a mixture from the chloroform soluble fraction of an ethanolic extract of Duranta repens stem, were evaluated for antibacterial, antifungal activities by the disc diffusion method and cytotoxicity by brine shrimp lethality bioassay. The structures of the two compounds were confirmed by IR, $^1H$-NMR, $^{13}C$-NMR and LC-MS spectral data. The chloroform soluble fraction of stem and ethanol extract of fruits possess potent antishigellosis activity and also exhibited moderate activity against some pathogenic bacteria and fungi but the isolated compound 1 (mixture of $\beta$-Amyrin and 12-Oleanene 3$\beta$, 21$\beta$-diol) showed mild to moderate inhibitory activity to microbial growth. The minimum inhibitory concentrations (MICs) of the extracts (stem and fruits), their fractions and compound 1 were found to be in the range of 32$\sim$128 ${\mu}g/ml$. The chloroform soluble fractions of stem and ethanol extract of fruit showed significant cytotoxicity with $LC_{50}$ value of 0.94 ${\mu}g/ml$ and 0.49 ${\mu}g/ml$, respectively against brine shrimp larvae.

Antimicrobial, Antioxidant and Cytotoxic Activities of Dendropanax morbifera Léveille extract for mouthwash and denture cleaning solution

  • Kim, Ryeo-Woon;Lee, Sook-Young;Kim, Su-Gwan;Heo, Yu-Ri;Son, Mee-Kyoung
    • The Journal of Advanced Prosthodontics
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    • v.8 no.3
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    • pp.172-180
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    • 2016
  • PURPOSE. The purpose of this study was to analyze the antimicrobial, antioxidant activity and cytotoxicity of Dendropanax morbifera $L{\acute{e}}veille$ extract for assessing whether Dendropanax morbifera $L{\acute{e}}veille$ can be used for the development of natural mouthwash and denture cleaning solution. MATERIALS AND METHODS. The extract was obtained from branches of Dendropanax morbifera $L{\acute{e}}veille$. The solvent fractions were acquired by fractionating Dendropanax morbifera $L{\acute{e}}veille$ extract using n-hexane, ethyl acetate, chloroform and butanol solvent. Paper disc test was used to evaluate the antimicrobial and antifungal activity of Dendropanax morbifera $L{\acute{e}}veille$ extract and solvent fractions against Streptococcus mutans and Candida albicans. The analysis of antioxidant activity was carried out through DPPH radical scavenging assay. The cytotoxicity of Dendropanax morbifera $L{\acute{e}}veille$ extract was analyzed through MTT assay using normal human oral keratinocytes. RESULTS. Dendropanax morbifera $L{\acute{e}}veille$ extract showed antimicrobial activity against Streptococcus mutans and especially Candida albicans. The solvent fractions of Dendropanax morbifera $L{\acute{e}}veille$ showed strong antimicrobial activity against Streptococcus mutans and Candida albicans in n-hexane and butanol solvent fraction, respectively. Dendropanax morbifera $L{\acute{e}}veille$ extract also showed outstanding antioxidant activity. Butanol, ethyl acetate, and chloroform solvent fraction of Dendropanax morbifera $L{\acute{e}}veille$ tended to have increased antioxidant activity as the concentration increased. Dendropanax morbifera $L{\acute{e}}veille$ extract showed high cell survival rate in cytotoxicity test. CONCLUSION. Dendropanax morbifera $L{\acute{e}}veille$ extract turned out to have antimicrobial, antioxidant activity and cytophilicity. Based on these results, it is expected that Dendropanax morbifera $L{\acute{e}}veille$ is applicable as an ingredient for natural mouthwash and denture cleanser.

Extraction and Application of Bulk Enzymes and Antimicrobial Substance from Spent Mushroom Substrates

  • Lim, Seon-Hwa;Kwak, A Min;Min, Kyong-Jin;Kim, Sang Su;Kang, Hee Wan
    • 한국균학회소식:학술대회논문집
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    • 2014.10a
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    • pp.19-19
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    • 2014
  • Pleurotus ostreatus, P. eryngii, and Flammulina velutipes are major edible mushrooms that account for over 89% of total mushroom production in Korea. Recently, Agrocybe cylindracea, Hypsizygus marmoreus, and Hericium erinaceu are increasingly being cultivated in mushroom farms. In Korea, the production of edible mushrooms was estimated to be 614,224 ton in 2013. Generally, about 5 kg of mushroom substrate is needed to produce 1 kg of mushroom, and consequently about 25 million tons of spent mushroom substrate (SMS) is produced each year in Korea. Because this massive amount of SMC is unsuitable for reuse in mushroom production, it is either used as garden fertilizer or deposited in landfills, which pollutes the environment. It is reasonably assumed that SMS includes different secondary metabolites and extracellular enzymes produced from mycelia on substrate. Three major groups of enzymes such as cellulases, xylanases, and lignin degrading enzymes are involved in breaking down mushroom substrates. Cellulase and xylanase have been used as the industrial enzymes involving the saccharification of biomass to produce biofuel. In addition, lignin degrading enzymes such as laccases have been used to decolorize the industrial synthetic dyes and remove environmental pollutions such as phenolic compounds. Basidiomycetes produce a large number of biologically active compounds that show antibacterial, antifungal, antiviral, cytotoxic or hallucinogenic activities. However, most previous researches have focused on therapeutics and less on the control of plant diseases. SMS can be considered as an easily available source of active compounds to protect plants from fungal and bacterial infections, helping alleviate the waste disposal problem in the mushroom industry and creating an environmentally friendly method to reduce plant pathogens. We describe extraction of lignocellulytic enzymes and antimicrobial substance from SMSs of different edible mushrooms and their potential applications.

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Physiological and Pharmacological Activites of Nutraceutical Tea by Leaves and Flowers of Domestic Camellia(Camellia japonica)

  • Lee, Sook-Young;Cha, Young-Ju;Lee, Jang-Won;Hwang, Eun-Ju;Kwon, Su-Jung;Cho, Su-In
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2003.10b
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    • pp.48-49
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    • 2003
  • This project was conducted to development several camellia tea mixed herb teas having any physiological effects. Leaves of tea tree contain many compounds, such as polysaccharides, volatile oils, vitamins, minerals, purines, alkaloids(eg. caffeine) and polyphenols(catechins and flavonoids). Although all three tea types(green, oolonr and black) have antibacterial and free radical capturing(antioxidizing) activities, the efficacy decreases substantially the darker the variety of tea is. This is due to lower contents of anti-oxidizing polyphenols remaining in the leaves. Unlike tea tree(Camellia sinensis), the biochemical features and effects of camellia(Camellia japonica) are not well known. Fresh mature leaf of sasanqua camellia(C. sasanqua), roasted young leaf tea(C. japonica) and fresh mature leaf and bark of camellia had high antibacterial activity against P. vulgaris and B. subtilis. In antifungal activity bioassay, young leaf roasted teas of camellia and sasanqua camellia had high activity against C. albicans and T. beigelil. Plant extracts from Camelia japonica had higher inhibitory activity against fungi than against bacteria. In cytotoxic effect against human acute myelogenous leukaemia cell extracts including fresh leaf(200$\mu\textrm{g}$/m1), bark(230$\mu\textrm{g}$/ml) and flower tea (320$\mu\textrm{g}$/m1)inhibited growth of AML cells.(중략)

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The Beneficial Effects of Extract of Pinus densiflora Needles on Skin Health (솔잎추출물의 피부건강 개선효과)

  • Choi, Jieun;Kim, Woong;Park, Jaeyoung;Cheong, Hyeonsook
    • Microbiology and Biotechnology Letters
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    • v.44 no.2
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    • pp.208-217
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    • 2016
  • Pinus densiflora Sieb. et Zucc. (P. densiflora) contains several phenolic compounds that exhibit biological activities, such as antimicrobial, antioxidant, and antihypertensive effects. However, the anti-inflammatory effect of P. densiflora on skin has rarely been reported. Malassezia furfur (M. furfur) is a commensal microbe that induces skin inflammation and is associated with several chronic disorders, such as dandruff, seborrheic dermatitis, papillomatosis, and sepsis. The aim of our study was to identify the anti-inflammatory effects of P. densiflora needle extracts on skin health subjected to M. furfur-induced inflammation. The methanolic extract of the pine needles was partitioned into n-hexane, EtOAc, n-BuOH, and water layers. We measured the anti-inflammatory effects (in macrophages) as well as the antioxidant, antifungal, and tyrosinase inhibitory activity of each of these layers. The antioxidant activity of the individual layers was in the order EtOAc layer > n-BuOH layer > water layer. Only the n-BuOH, EtOAc, and n-hexane layers showed antifungal activity. Additionally, all the layers possessed tyrosinase inhibition activity similar to that of ascorbic acid, which is used as a commercial control. The EtOAc layer was not cytotoxic toward the RAW 264.7 cell line. Interleukin 1 beta and tumor necrosis factor (TNF)-α expression levels in M. furfur-stimulated RAW 264.7 cells treated with the EtOAc layer were decreased markedly compared to those in cells treated with the other layers. Taken together, we believe that the needle extracts of P. densiflora have potential application as alternative anti-inflammatory agents or cosmetic material for skin health improvement.

Induction of Apoptosis and Antitumor Activity by Stichoposide D through the Generation of Ceramide in Human Leukemia Cells (Stichoposide D의 백혈병 세포주에서 세라마이드 생성을 통한 세포 사멸 유도 및 항암 작용)

  • Park, Eun-Seon;Yun, Seung-Hoon;Shin, Sung-Won;Kwak, Jong-Young;Park, Joo-In
    • Journal of Life Science
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    • v.22 no.6
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    • pp.760-771
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    • 2012
  • Marine triterpene glycosides are physiologically active natural compounds isolated from sea cucumbers(holothurians). It was demonstrated that they have a wide range of biological activities, including antifungal, cytotoxic, and antitumor effects. A previous study showed that stichoposide C (STC) isolated from Thelenota anax induces apoptosis through generation of ceramide by activation of acid sphingomyelinase (SMase) and neutral SMase in human leukemia cells. In this study, we investigated whether STD, a structural analog of STC, can induce apoptosis and examined the molecular mechanisms for its activity. It was found that STC and STD induce apoptosis in a dose- and time-dependent manner and lead to the activation of caspase-8, mitochondrial damage, activation of caspase-9, and activation of caspase-3 in K562 and HL-60 cells. STC activates acid SMase and neutral SMase, which results in the generation of ceramide. Specific inhibition of acid SMase or neutral SMase partially blocked STC-induced apoptosis, but not STD-induced apoptosis. In contrast, STD generates ceramide through the activation of ceramide synthase. Specific inhibition of ceramide synthase partially blocked STD-induced apoptosis, but not STC-induced apoptosis. Moreover, STC and STD markedly reduced tumor growth of HL-60 xenograft tumors and increased ceramide generation in vivo. These results indicate that STC and STD can induce apoptosis and have antitumor activity through the different molecular mechanisms, because they have a different sugar residue attached to aglycones. Thus, these results suggest that their actions are affected by a sugar residue attached to aglycones and they can be used as anticancer agents in the treatment of leukemia.