• Title/Summary/Keyword: Bioactive agent

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Pancreatic Lipase Inhibitory and Antioxidant Activities of Polygonum aviculare Extract (마디풀 추출물의 Pancreatic Lipase 저해 및 항산화 활성 평가)

  • Kim, Tae-Hoon
    • Food Science and Preservation
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    • v.18 no.2
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    • pp.250-255
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    • 2011
  • As part of our continuing search for novel bioactive natural products, antioxidant and pancreatic lipase inhibitory activities of the aqueous ethanolic extract of Polygonum aviculare were investigated. In addition, the total phenolic content was quantified by a spectrophotometric method. The antioxidant properties of the extract were evaluated by radical scavenging assays such as DPPH and $ABTS^+$ radicals. The anti-obesity efficacy of P. aviculare extract was tested by porcine pancreatic lipase assay. All tested samples showed a dose-dependent pancreatic lipase inhibitory and radical scavenging activities. In terms of the $IC_{50}$ value, the ethyl acetate (EtOAc) soluble portion was most potent than other solvent soluble portions. The results suggested that P. aviculare could be considered as a new potential source of natural antioxidant and anti-obesity agent for food, nutraceutical, cosmetics industries.

Synthesis and Reaction of 1,5,3,7-Diazadiphosphocine-1,5-Dicarboxylic Acids (1,5,3,7-Diazadiphosphocine-1,5-Dicarboxylic Acids의 합성과 반응)

  • Cho, Seung-Hwan;Song, Ju-Hyun;Lee, Do-Hun;Lee, Yong-Gyun;Park, Yu-Mi;Choi, Soon-Kyu;Hahn, Jung-Tai;Jung, Dai-Il
    • Journal of Life Science
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    • v.17 no.7 s.87
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    • pp.910-914
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    • 2007
  • In order to synthesize new bioactive compounds and contrasting agents, reactions of glycine and glutamic acid as an animo acid with paraformaldehyde and hypophosphorous acid were executed. Products are 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid 1 and 3,7-dihydroxy-3,7- dioxoperhydre-1,5,3,7-diazadiphosphocine-1,5-di-(2-glu taric acid) 3. 2-[5-(1,2-Dicarboxyethyl)-3,7-dihydroxy-3,7-dioxo-315.715-[1,5,3,7] diazadiphosphocan-1-yl]-succinic acid 2 by using aspartic acid was not obtained. Esterification of 3,7- dihydroxy-3,7-dioxoperkydro-1,5,3,7-diaza-diphosphocine-1,5-diacetic acid 1 by treatment of methanol, ethanol, and propanol were executed. 3,7-Dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid methyl ester 4, 3.7-dihydroxy-3,7-dioxoperhydro-1,5,3,f-diazadiphosphocine-1.5-diacetic acid ethyl ester 5, and 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid propyl ester 6 were respectively synthesized in good yields. Continuously, we will try synthesis of novel compounds and evaluation of biological activity.

Resveratrol Induces Glioma Cell Apoptosis through Activation of Tristetraprolin

  • Ryu, Jinhyun;Yoon, Nal Ae;Seong, Hyemin;Jeong, Joo Yeon;Kang, Seokmin;Park, Nammi;Choi, Jungil;Lee, Dong Hoon;Roh, Gu Seob;Kim, Hyun Joon;Cho, Gyeong Jae;Choi, Wan Sung;Park, Jae-Yong;Park, Jeong Woo;Kang, Sang Soo
    • Molecules and Cells
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    • v.38 no.11
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    • pp.991-997
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    • 2015
  • Tristetraprolin (TTP) is an AU-rich elements (AREs)-binding protein, which regulates the decay of ARE-scontaining mRNAs such as proto-oncogenes, anti-apoptotic genes and immune regulatory genes. Despite the low expression of TTP in various human cancers, the mechanism involving suppressed expression of TTP is not fully understood. Here, we demonstrate that Resveratrol (3,5,4'-trihydroxystilbene, Res), a naturally occurring compound, induces glioma cell apoptosis through activation of tristetraprolin (TTP). Res increased TTP expression in U87MG human glioma cells. Res-induced TTP destabilized the urokinase plasminogen activator and urokinase plasminogen activator receptor mRNAs by binding to the ARE regions containing the 3' untranslated regions of their mRNAs. Furthermore, TTP induced by Res suppressed cell growth and induced apoptosis in the human glioma cells. Because of its regulation of TTP expression, these findings suggest that the bioactive dietary compound Res can be used as a novel anti-cancer agent for the treatment of human malignant gliomas.

Preparation of Chitosan/Poly-${\gamma}$-glutamic Acid Nanoparticles and Their Application to Removal of Heavy Metals (키토산/폴리감마글루탐산 나노입자의 제조 및 중금속 제거에의 응용)

  • Sung, Ik-Kyoung;Song, Jae Yong;Kim, Beom Soo
    • Korean Chemical Engineering Research
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    • v.49 no.4
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    • pp.475-479
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    • 2011
  • Chitosan is a natural polymer that has many physicochemical(polycationic, reactive OH and $NH_2$ groups) and biological(bioactive, biocompatible, and biodegradable) properties. In this study, chitosan nanoparticles were prepared using poly-${\gamma}$-glutamic acid(${\gamma}$-PGA) as gelling agent. Nanoparticles were formed by ionic interaction between carboxylic groups in ${\gamma}$-PGA and amino groups in chitosan. Chitosan(0.1~1 g) was dissolved in 100 ml of acetic acid (1% v/v) at room temperature and stirred overnight to ensure a complete solubility. An amount of 0.1 g of ${\gamma}$-PGA was dissolved in 90 ml of distilled water at room temperature. Chitosan solution was dropped through needle into beaker containing ${\gamma}$-PGA solution under gentle stirring at room temperature. The average particle sizes were in the range of 80~300 nm. The prepared chitosan/${\gamma}$-PGA nanoparticles were used to examine their removal of several heavy metal ions($Cd^{2+}$, $Pb^{2+}$, $Zn^{2+}$, $Cu^{2+}$, and $Ni^{2+}$) as adsorbents in aqueous solution. The heavy metal removal capacity of the nanoparticles was in the order of $Cu^{2+}$ > $Pb^{2+}$ > $Cd^{2+}$ > $Ni^{2+}$ > $Zn^{2+}$.

Antifungal and Insecticidal Activity of Essential Oil from Asarum sieboldii against Wood Contaminant Fungi and Lasioderma serricorne L. (세신 정유추출물의 목재부후균과 궐련벌레에 대한 항진균 및 살충활성)

  • Kang, Soyeong;Chung, Yong Jae;Lim, Jin A
    • Journal of Conservation Science
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    • v.28 no.4
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    • pp.395-401
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    • 2012
  • To investigate bioactive materials for development of natural conservative agent on organic cultural heritage, essential oil from Asarum sieboldii was screened for antifungal and insecticidal activity against 4 wood rotting fungi and adult of Lasioderma serricorne. Antifungal activity of essential oil was tested by using paper disc soaking method. Antifungal activity expressed as $IC_{50}$ value showed $1.50{\sim}2.84{\mu}l/disc$ range and the most significant antifungal activity was observed in Lentinus lepideus. The insecticidal activity of essential oil was examined by topical application method against L. serricorne adults. 50% and 100% of essential oil gave 98.3% and 100% mortality for 24 hours, respectively. The major components of the essential oil were methyl eugenol (56.32%), eucarvone (11.53%), safrole (5.79%), ${\delta}$-3-carene (2.09%), which were identified by gas chromatography-mass spectrometry. From these results, essential oil from A. sieboldii could be useful for conservation of organic cultural heritage against biological deterioration by insect and wood rotting fungi.

Pancreatic Lipase Inhibitory and Antioxidant Activities of Zingiber officinale Extracts (생강 추출물의 pancreatic lipase 저해 및 항산화 활성)

  • Bae, Jong-Sup;Kim, Tae-Hoon
    • Food Science and Preservation
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    • v.18 no.3
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    • pp.390-396
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    • 2011
  • Ginger (Zingiber officinale) is a well-known herb that is widely consumed as spice for the flavoring of foods. As part of our continuing search for bioactive materials, the in vitro pancreatic lipase inhibition and antioxidant properties of an aqueous ethanolic extract of Z. officinale were investigated. The total phenolic content was determined using a spectrophotometric method. The antioxidant efficacies of the extract was studied with radical scavenging assays using DPPH and $ABTS^+$ radicals. Further more, the antiobesity effect of the extract was evaluated by porcine pancreatic lipase assay. In particularly, the pancreatic lipase inhibitory activity of the ethyl acetate (EtOAc)-soluble portion from Z. officinale was significantly higher than that of the other solvent-soluble portions. The results suggest that Z. officinale may have therapeutic potential that may be useful in development of an anti-obesity agent or its precursors.

Non-Polar Myxococcus fulvus KYC4048 Metabolites Exert Anti-Proliferative Effects via Inhibition of Wnt/β-Catenin Signaling in MCF-7 Breast Cancer Cells

  • Park, Juha;Yoo, Hee-Jin;Yu, Ah-Ran;Kim, Hye Ok;Park, Sang Cheol;Jang, Young Pyo;Lee, Chayul;Choe, Wonchae;Kim, Sung Soo;Kang, Insug;Yoon, Kyung-Sik
    • Journal of Microbiology and Biotechnology
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    • v.31 no.4
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    • pp.540-549
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    • 2021
  • The Wnt/β-catenin signaling pathway is involved in breast cancer and Myxococcus fulvus KYC4048 is a myxobacterial strain that can produce a variety of bioactive secondary metabolites. Although a previous study revealed that KYC4048 metabolites exhibit anti-proliferative effects on breast cancer, the biochemical mechanism involved in their effects remains unclear. In the present study, KYC4048 metabolites were separated into polar and non-polar (ethyl acetate and n-hexane) fractions via liquid-liquid extraction. The effects of these polar and non-polar KYC4048 metabolites on the viability of breast cancer cells were then determined by MTT assay. Expression levels of Wnt/β-catenin pathway proteins were determined by Western blot analysis. Cell cycle and apoptosis were measured via fluorescence-activated cell sorting (FACS). The results revealed that non-polar KYC4048 metabolites induced cell death of breast cancer cells and decreased expression levels of WNT2B, β-catenin, and Wnt target genes (c-Myc and cyclin D1). Moreover, the n-hexane fraction of non-polar KYC4048 metabolites was found most effective in inducing apoptosis, necrosis, and cell cycle arrest, leading us to conclude that it can induce apoptosis of breast cancer cells through the Wnt/β-catenin pathway. These findings provide evidence that the n-hexane fraction of non-polar KYC4048 metabolites can be developed as a potential therapeutic agent for breast cancer via inhibition of the Wnt/β-catenin pathway.

Can Hinokitiol Kill Cancer Cells? Alternative Therapeutic Anticancer Agent via Autophagy and Apoptosis (Hinokitiol에 의해 유도된 Autophagy 및 Apoptosis에 의한 대체 항암요법 연구)

  • Lee, Tae Bok;Jun, Jin Hyun
    • Korean Journal of Clinical Laboratory Science
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    • v.51 no.2
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    • pp.221-234
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    • 2019
  • Cancer is genetically, metabolically and infectiously induced life threatening disorder showing aggressive growing pattern with invasive tendency. In order to prevent this global menace from jeopardizing human life, enormous studies on carcinogenesis and treatment for chemotherapy resistance have been intensively researched. Hinokitiol (${\beta}$-thujaplicin) extracted from heart wood of cupressaceous is a well-known bioactive compound demonstrating anti-inflammation, anti-bacteria and anti-cancer effects on several cancer types via apoptosis and autophagy. This study proposed that hinokitiol activates transcription factor EB (TFEB) nuclear translocation for autophagy and lysosomal biogenesis regardless of nutrient condition in cancer cells. Mitophagy and ${\beta}$-catenin translocation into the nucleus under treatment of hinokitiol on non-small cell lung cancer (NSCLC) cells and HeLa cells were investigated. Hinokitiol exerted cytotoxicity on HeLa and HCC827 cells; moreover, artificially induced autophagy by overexpression of TFEB granted imperfect sustainability onto HeLa cells. Taken together, hinokitiol is the prominent autophagy inducer and activator of TFEB nuclear translocation. Alternative cancer therapy via autophagy is pros and cons since the autophagy in cancer cells is related to prevention and survival mechanism depending on nutrition. To avoid paradox of autophagy in cancer therapy, fine-tuned regulation and application of hinokitiol in due course for successful suppressing cancer cells are recommended.

UPLC Analysis of Pinocembrin and Antimicrobial Activity of Propolis Collected from Different Regions in Korea (지역별 국산 프로폴리스의 항균활성 및 Pinocembrin의 UPLC 분석)

  • Kim, Se Gun;Hong, In Pyo;Woo, Soon Ok;Jang, Hye Ri;Han, Sang Mi
    • Journal of Apiculture
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    • v.32 no.3
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    • pp.253-259
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    • 2017
  • Propolis, natural antibacterial agent, which has been used traditional medicine across the globe, is resinous mixture to include abundant bioactive substances. In present study, we investigated antimicrobial activity according to quality characteristics of propolis collected from 9 different regions in Korea. Antimicrobial activity was evaluated by measuring growth inhibition zone using agar well diffusion method against Streptococcus mutans. Constituents analysis of propolis samples were measured through total phenolic contents, total flavonoid contents and quantitative analysis of major compound (pinocembrin) by ultra performance liquid chromatography. As a result, 9 different propolis (10mg/mL) and pinocembrin (1mg/mL) showed antimicrobial activity that has growth inhibition zone more than 11.9mm on S. mutans. The total flavonoid contents of 8 different propolis excluding Jeju island were in compliance with standard of health functional food in Korea and were found to affect antimicrobial activity on S. mutans when contained over 10mg/g. In addition, when content of pinocembrin in propolis was ranged from 12mg/g to 32mg/g, each propolis excluding Jeju island exhibited antimicrobial activity alike. These results indicate that pinocembrin plays a important role for antimicrobial activity of propolis collected from 8 different regions in Korea, and that it can be used as basic data for standardization of Korean propolis.

Anti-melanogenic Effects of Cnidium japonicum in B16F10 Murine Melanoma Cells (B16F10 피부 흑색종세포에서 갯사상자 추출물의 멜라닌 합성 저해 효과)

  • Jo, Hyun Jin;Karadeniz, Fatih;Oh, Jung Hwan;Seo, Youngwan;Kong, Chang-Suk
    • Journal of Life Science
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    • v.32 no.5
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    • pp.331-339
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    • 2022
  • Melanin is a pigment produced by melanocytes to protect the skin from external stimuli, mainly ultraviolet (UV) rays. However, abnormal and excessive production of melanin causes hyperpigmentation disorders, such as freckles, age spots, and discoloration. Natural cosmeceuticals are a new trend for treating or preventing hyperpigmentation due to fewer side effects and biocompatibility. In this context, the current study focused on Cnidium japonicum, a halophyte with several uses in folk medicine, to evaluate its potential as a skin-whitening agent. The effect of C. japonicum extract (CJE) on melanin production was analyzed in melanogenesis-stimulated B16F10 melanoma cells. The results showed that CJE successfully inhibited the oxidation of tyrosine and L-DOPA by tyrosinase and subsequently decreased the production of the key enzymes responsible for melanin production: tyrosinase, tyrosinase-related protein-1, and protein-2. This effect was confirmed by decreased intracellular and extracellular melanin levels in B16F10 melanoma cells after CJE treatment. Further experiments to elucidate the action mechanism revealed that CJE treatment suppressed melanin production by inhibiting the activation of glycogen synthase kinase 3 β (GSKβ)/β-catenin and protein kinase A (PKA)/cAMP-response element binding protein (CREB) pathways, which are the upstream activators of melanogenesis. In conclusion, the present study suggests that C. japonicum is a potential natural source of bioactive substances for the development of novel cosmeceuticals that can act against hyperpigmentation.