• Title/Summary/Keyword: Bioactive

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Kanakugiol, a Compound Isolated from Lindera erythrocarpa, Promotes Cell Death by Inducing Mitotic Catastrophe after Cell Cycle Arrest

  • Lee, Jintak;Chun, Hyun-Woo;Pham, Thu-Huyen;Yoon, Jae-Hwan;Lee, Jiyon;Choi, Myoung-Kwon;Ryu, Hyung-Won;Oh, Sei-Ryang;Oh, Jaewook;Yoon, Do-Young
    • Journal of Microbiology and Biotechnology
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    • v.30 no.2
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    • pp.279-286
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    • 2020
  • A novel compound named 'kanakugiol' was recently isolated from Lindera erythrocarpa and showed free radical-scavenging and antifungal activities. However, the details of the anti-cancer effect of kanakugiol on breast cancer cells remain unclear. We investigated the effect of kanakugiol on the growth of MCF-7 human breast cancer cells. Kanakugiol affected cell cycle progression, and decreased cell viability in MCF-7 cells in a dose-dependent manner. It also enhanced PARP cleavage (50 kDa), whereas DNA laddering was not induced. FACS analysis with annexin V-FITC/PI staining showed necrosis induction in kanakugiol-treated cells. Caspase-9 cleavage was also induced. Expression of death receptors was not altered. However, Bcl-2 expression was suppressed, and mitochondrial membrane potential collapsed, indicating limited apoptosis induction by kanakugiol. Immunofluorescence analysis using α-tubulin staining revealed mitotic exit without cytokinesis (4N cells with two nuclei) due to kanakugiol treatment, suggesting that mitotic catastrophe may have been induced via microtubule destabilization. Furthermore, cell cycle analysis results also indicated mitotic catastrophe after cell cycle arrest in MCF-7 cells due to kanakugiol treatment. These findings suggest that kanakugiol inhibits cell proliferation and promotes cell death by inducing mitotic catastrophe after cell cycle arrest. Thus, kanakugiol shows potential for use as a drug in the treatment of human breast cancer.

Effects of Quercetin on $TNF-{\alpha}-Induced$ Cytokine Secretion and Nitric Oxide Production in MC3T3-E1 Osteoblastic Cells

  • Jeon, Young-Mi;Kim, Beom-Tae;Son, Young-Ok;Kook, Sung-Ho;Lee, Keun-Soo;Kim, So-Soon;Lim, Ji-Young;Kim, Jong-Ghee;Lee, Jeong-Chae
    • Natural Product Sciences
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    • v.11 no.2
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    • pp.103-108
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    • 2005
  • Bioflavone quercetin is thought to have an important role to inhibit bone loss by affecting osteoclastogenesis and regulating a number of systemic and local factors such as hormones and cytokines. In this study, we examined how quercetin acts on cytokine production and mineralization of osteoblast in the presence of tumor necrosis factor-alpha $(TNF-{\alpha})$ which has been known to play a pivotal role in bone metabolic diseases. Quercetin inhibited $TNF-{\alpha}-induced$ secretion of $IFN-{\gamma}$ and IL-6 in differentiated MC3T3-E1 cells. As indicated by the markers that are characteristics of the osteoblast phenotype, such as alkaline phosphatase (ALP) activity and calcium deposition, quercetin treatment slightly prevented the $TNF-{\alpha}-induced$ dramatic inhibition of differentiation and mineralization of MC3T3-E1 cells. Further, quercetin inhibited the production of nitric oxide induced by $TNF-{\alpha}$ in the cells. Collectively, our findings indicate that quercetin inhibites $TNF-{\alpha}-induced$ secretion of inflammatory cytokines in differentiated MC3T3-E1 cells without any cytotoxic effects.

Thermal Stability of Representative Bioactive Compounds in Biopesticide Derived from Castor Oil or Wormseed Extract under Controlled Temperature (피마자유와 양명아주 추출물을 원료로 하는 유기농업자재 유효성분의 열 안정성 평가)

  • Choi, Geun-Hyoung;Jeong, Dong-Kyu;Jin, Cho-Long;Rho, Jin-Ho;Park, Byung-Jun;Moon, Byung-Cheol;Kim, Jin-Hyo
    • Korean Journal of Environmental Agriculture
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    • v.36 no.1
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    • pp.17-21
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    • 2017
  • BACKGROUND: Castor oil and wormseed extract are important active ingredients for biopesticide, and ricinoleic acid in castor oil and three monoterpenes (ascaridole, carvacrol and p-cymene) in wormseed extract are known bioactive substances. However, their stabilities had not been studied, even though the stability was the core property for estimation of shelf-life of biopesticide. Aimed to investigate the thermal stabilities of the bioactive substances in castor oil and wormseed extracts. METHODS AND RESULTS: The contents of ricinoleic acid and three monoterpenes (ascaridole, carvacrol and p-cymene) were analyzed by gas chromatography (GC). The thermal stabilities of the bioactive substance were measured at $0^{\circ}C$, $23^{\circ}C$, $30^{\circ}C$, $40^{\circ}C$, $45^{\circ}C$ and $54^{\circ}C$ for 84 d. The half-lives of ricinoleic acid in biopesticides was ranged from 28.9 d to 57.8 d at $30^{\circ}C$, and the stability of pure castor oil were located in the range ($t_{1/2}$=46.2d for Indian product and 27.7 d for Korean product) at the same temperature. The half-lives of the total monoterpenes in biopesticides were ranged from 3.9 d to 27.7 d at $30^{\circ}C$. Among the monoterpenes, the stability ascaridole and p-cymene were decreased in acidic condition. All the bioactive substances showed similar stability on the different thermal conditions. CONCLUSION:The half-lives of most bioactive substance from castor oil and wormseed extracts were less than 100 d. To increase the stability of bioactive substance in biopesticide, stabilizing additives like antioxidant and oxygen remover should be considered to extend of the shelf-life.

Screening of Bioactive Materials from Freshwater Microalgae (담수산 미세조류로부터 생리활성물질의 탐색)

  • Lee, Wan-Seok;Choi, Ae-Ran;Ahn, Chi-Yong;Oh, Hyun-Cheol;Ahn, Jong-Seog;Oh, Hee-Mock
    • ALGAE
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    • v.19 no.3
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    • pp.271-276
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    • 2004
  • One hundred and fifty four micro algal strains, newly isolated from nationwide freshwaters in Korea, were screened for their anticancer, ant diabetic, and antibiotic activities. The micro algal strains were cultured with different nutritional conditions that were divided into 4 groups as follows; a normal Allen medium, nitrogen (N)-limited medium, phosphorus (P)-limited medium, and N and P-limited medium. Algal biomass was extracted with a mixture of acetone:H₂O (1:1, v:v) and the extracts were used for the screening of bioactive materials. Anticancer, ant diabetic, and antibiotic materials were screened by the methods of vaccinia Hl-related protein tyrosine phosphates (VHR DS-PTPase) inhibition, protein tyrosine phosphates 1B (PTP1B) inhibition, and paper disk. The inhibition activity of VHR DS-PTPase was observed in 18 strains, having a maximum 79% inhibition from Anabaena affinis and the inhibition activity of PTP1B was observed in 9 strains, having a maximum 97% from Sphaerocystis schroeteri. Microcystis aeruginosa incubated in an N and P-limited medium showed antibiotic activity in 8 species out of 13 pathogenic bacteria. As a whole, it seemed that the stressed condition such as N and/or P limitation increased the production of bioactive materials in micro algae.

Synthesis of Heterocyclic Chalcone Derivatives and Their Radical Scavenging Ability Toward 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) Free Radicals

  • Hwang, Ki-Jun;Kim, Ho-Seok;Han, In-Cheol;Kim, Beom-Tae
    • Bulletin of the Korean Chemical Society
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    • v.33 no.8
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    • pp.2585-2591
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    • 2012
  • A series of heterocyclic chalcone derivatives bearing heterocycles such as thiophene or furan ring as an isostere of benzene ring were carefully prepared, and the influence of heterocycles on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities was systematically investigated. Structure-activity relationships (SAR) analysis showed that the activities of thiophene ring-containing chalcones were higher than those of furan ring-containing chalcones, and the presence of methyl substituent of heterocyclic ring distinctly affected the activities compared with non-substituted heterocycles in an opposite manner, with the 4'-methyl group of thiophene ring increasing activity and the 3'-methyl group of the furan ring decreasing activity. The distinct isosteric effect of heterocycles (i.e., thiophene or furan ring) on radical scavenging activities of heterocyclic chalones was distinctly demonstrated in our work.

Determination of Bioactive Compounds and Antioxidant Activity of Yam (Dioscorea batatas DECNE.) on Thermal Treatment

  • Duan, Yishan;Kim, Gyeong-Hwuii;Kim, Han-Soo
    • Journal of the Korean Applied Science and Technology
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    • v.32 no.2
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    • pp.302-311
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    • 2015
  • To better investigate the antioxidative property of thermal treatment yam (Dioscorea batatas DECNE.) in Korea, some established methods were used. 70% Methanol, 70% ethanol and chloroform-methanol (CM, 2:1, v/v) extracts were collected. 70% Methanol extract exhibited stronger antioxidative activity evaluated by ferrous ion chelating activity, NO radical scavenging activity and ${\beta}$-carotene bleaching assays. On the contrary, CM extract was the most effective in inhibiting linoleic acid peroxidation. Yam available in Korea was also analyzed for its bioactive compounds such as lycopene, chlorophyll a, b, tannin, phytic acid and total saponin contents. Total saponin was abundant in thermal treatment, which determined to be $42.52{\pm}1.88mg/g$. Based on the results obtained from this study, thermal treatment yam could be used as natural antioxidant source due to its high antioxidant activity and bioactive compound contents.

Characteristic Effects of Dangnyo-hwan for Diabetes Control Studied Using LC-MS/MS and ICP (LC-MS/MS 및 ICP를 이용한 당뇨환의 화학적 특성 분석)

  • In, Jeong-do;Im, Dai-sig;Moon, Seung-ho;Ki, Won-ill
    • The Journal of Internal Korean Medicine
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    • v.36 no.3
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    • pp.217-227
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    • 2015
  • Objectives: The primary aim of this study was to identify bioactive compounds in Dangnyo-hwan, a Korean herbal medicine, through instrumental analysis using LC-MS/MS and ICP, and investigate its potential use in diabetes treatment. Methods: The extract of Dangnyo-hwan has 12 medicinal herbs; these were compared with 18 marker substances selected from literature survey. Results: LC-MS/MS analysis could detect 9 of the 18 bioactive compounds: citruline, catalpol, berberine, ginsenoside Rb1, ginsenoside Rg1, oleanolic acid, β-sitosterol, mangiferin, and schizandrin. While harmful heavy metals such as As, Pb, Cd, Hg, Ni, and Cu were not present in high concentrations, Zn concentration was 4.2 mg in 100 g Dangnyo-hwan. Conclusions: Instrumental analysis such as LC-MS/MS and ICP was successfully used to identify bioactive compounds in Dangnyo-hwan. Detection of 9 bioactive substances and Zn from the herb medicine is a valuable finding, and suggests that Dangnyo-hwan is a candidate medicine for diabetes. Further investigations like in vitro assay, percent GPR 119 activity, and percent human DGAT-1 inhibition are underway.