• Title/Summary/Keyword: cytotoxicities

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Screening of Natural Compounds for Cancer Prevention by Cytotoxicities and AP-1 Reporter Gene Activities (천연물 지표성분들의 세포독성 및 AP-1 활성 평가를 통한 암예방 기능성 탐색)

  • Choi, Bu-Young;Cho, Seok-Cheol
    • Journal of Convergence for Information Technology
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    • v.7 no.6
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    • pp.89-95
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    • 2017
  • Cancer-inducing PMA stimulates cells to increase the expression of transcription factor c-Jun/c-fos and then increase the activity of AP-1 in the nucleus. The activity of AP-1 has been reported to cause cancer. In this study, We conducted cytotoxicity experiments to assess the safety of natural marker compounds and also observed inhibition of activator protein(AP-1) activity to predict cancer-preventing effects. The results of this experiment indicated that arctigenin, manassantin A, and B can predict the development of cancer prevention agents.

Cytotoxic and ACAT-inhibitory Sesquiterpene Lactones from the Root of Ixeris dentata forma albiflora

  • Ahn, Eun-Mi;Bang, Myun-Ho;Song, Myoung-Chong;Park, Mi-Hyun;Kim, Hwa-Young;Kwon, Byoung-Mog;Baek, Nam-In
    • Archives of Pharmacal Research
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    • v.29 no.11
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    • pp.937-941
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    • 2006
  • Ixeris dentata forma albiflora was extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH and $H_{2}O$. Eight sesquiterpenes were isolated through repeated silica gel and octadecyl silica gel ($C_{18},\;ODS$) column chromatography of the EtOAc and n-BuOH fractions. Physicochemical analysis using NMR, MS and IR revealed the chemical structures of the sesquiterpenes, which were zaluzanin (1), 9a-hydroxyguaian-4(15), 10(14), 11 (13)-triene-6, 12-olide(2), $3{\beta}-O-{\beta}-D-glucopyranosyl-8{\beta}-hydroxyguaian$-4(15), 10(14)-diene-6, 12-olide (3), $3-O-{\beta}-D-glucopyranosyl-8{\beta}-hydroxyguauan$-10(14)-ene-6, 12-olide (4), ixerin M (5), glucozaluzanin C (6), crepiside I (7), and ixerin D (8). This is the first time that these sesquiterpene lactones have been isolated from this plant. Compounds 1, 2 and 7 revealed relatively high cytotoxicities on human colon carcinoma cell and lung adeno-carcinoma cell, while compounds 5 and 7 showed acyl-CoA: cholesterol acyltransferase (ACAT) inhibitory activity.

Recent Advances on the Study of Hsp90 Inhibitory Natural Products (Hsp90 저해기전을 가진 천연물들의 최근 연구동향)

  • Oh, Yeon Il;Kim, Nan A;Kim, Ye Hyun;Lee, Tae Hoon;Lee, Yong Sup
    • Korean Journal of Pharmacognosy
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    • v.44 no.3
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    • pp.209-219
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    • 2013
  • Heat shock protein 90 (Hsp90) is a molecular chaperone that assists protein folding and contributes to the stability of various proteins. It also stabilizes a number of proteins involved in tumor growth to consider it as a promising target for the treatment of cancer. Natural products have been a rich source of agents of value in medicine, therefore discovering lead compounds from them is one of important strategy in the drug development. In this regard, geldanamycin, radicicol, novobiocin and celastrol have been utilized as leads for the development of Hsp90 inhibitory anticancer agents. This review summerizes recent findings of natural products as Hsp90 inhibitiors. The Hsp90 inhibitory activities, mode of actions on Hsp90 and cytotoxicities on human cancer cell lines of natural products including bulgarialactone B, curcumin, (-)-gambogic acid, quercetin, sansalvamide A, silybin, and withaferin A were discussed.

Mechanical Properties and cytotoxicity of nitrided 630 Stainless by ion nitriding (플라즈마 이온질화에 따른 STS 630의 기계적 특성과 세포독성에 관한 융합적 연구)

  • Hwang, Gab-Woon
    • Journal of the Korea Convergence Society
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    • v.10 no.11
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    • pp.241-246
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    • 2019
  • In this study, we have examined the possibility to improve the material properties and biocompatibility of the 630 stainless steel for the application of medical instruments. The evaluation of mechanical properties and biocompatibility of the 630 stainless steel were studied by aging, nitriding, SEM measurement, Vicker's hardness, tensile strength and MTT cytotoxicity using IGF cells, respectively. The results showed that the tensile strength and Vicker's hardness of 630 stainless steel was increased with aging and ion nitriding time. The cytotoxicities of the 630 stainless decreased compared with the 420 stainless on MTT cytotoxicity using IGF cells. Ion nitriding of 630 stainless led to an enhanced application of medical instruments and biocompatibility performance.

Analysis of Nutritional Composition and Antioxidant Activity of Black Chestnut by Aging (숙성에 의한 흑밤의 영양성분 분석과 항산화 활성)

  • Moon Hee Lee;Ji Su Lee;Ji Won Yang;In Beom Kim;Youn-Je Park
    • The Korean Journal of Food And Nutrition
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    • v.37 no.1
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    • pp.30-39
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    • 2024
  • Black chestnut (BC) was obtained through aging of fresh chestnut (FC) at 80℃ for 15 days. Proximate and mineral compositions along with colors of FC and BC were evaluated. With aging, moisture contents decreased by 50%, whereas sugar contents, carbohydrate contents, and calories increased. Contents of minerals (Fe, P, Ca, Na, Mg, K) were significantly higher in FC than in BC, showing an order of Mg < Ca < P < K in both FC and BC. Using a Hunter color system, it was found that lightness (L), redness (a), and yellowness (b) values of FC were higher than those of BC. Antioxidant and cytotoxic activities of hot water and ethanol (50, 80, 100%) extracts prepared from FC and BC were evaluated. Extraction yields were lower with FC than with BC. Among water and ethanol extracts, water extract showed the highest DPPH radical scavenging activity for both FC and BC. IC50 values for ABTS+ radical scavenging activities increased after aging. Cytotoxicities of FC and BC extracts were similar to each other. They were different against various cell lines (3T3, HeLa, and Sarcoma-180). These results suggest that BC could be used as a new processed food using chestnut.

Effects of complex extracts having Drynariae Rhizoma on suppression of collagenolysis and bone resorption in mouse calvarial osteoblasts (골쇄보(骨碎補) 복합제제가 생쥐의 calvarial osteoblast에서 collagen 용해와 골재흡수에 미치는 영향)

  • Hong, Shi-Nae;Jeong, Ji-Cheon
    • The Journal of Dong Guk Oriental Medicine
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    • v.9
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    • pp.179-191
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    • 2000
  • Anti-bone resorption properties of the Korean herbal medicine, CEDR, which is comprised 5 herbs of [Drynariae Rhizoma, Loranthi Ramus, Cibotii Rhizoma, Amydae carapax, Psoraleae semen], were investigated. Mouse calvarial osteoblast cells were isolated and cultured. Mouse osteoblasts, which were stimulated by PTH, $1,25(OH)_2D_3$, $TNF-\alpha$ and IL-1 as bone resorption agents, showed increased collagenolysis by producing the active gelatinase. IL-1 in stimulating bone resorption was examined using fetal mouse long bone organ culture. IL-1 stimulated bone resorption and produced marked resorption when present simultaneously. The results of in vitro cytotoxicities showed that CEDR extracts have no any cytotoxicities in concentrations of $1-60{\mu}g/ml$ and furthermore there is no any cytotoxicity even in concentration of $120{\mu}g/ml$ on mouse calvarial bone cells. CEDR extracts had protective activity against PTH (5 units/ml, or $IL-1{\alpha}$ (1 ng/ml) or $TNF-\alpha$ or $1,25(OH)_2D_3$ (20 ng/ml), $IL-1{\alpha}$ and $IL-1{\beta}-induced$ collagenolysis in the mouse calvarial cells. Pretreatment of the CEDR extracts for 1 h, which by itself had little effect on cell survival, did not enhance the collagenolysis, nor significantly reduced the collagenolysis by pretreatment. Furthermore, the medicinal extracts were shown to have the protective effects against collagenolysis induced by $IL-1{\alpha}$ and $IL-1{\beta}$. Pretreatment of the extracts for 1 h significantly reduced the collagenolysis. Interestingly, the CEDR extracts were shown to have the inhibiting effects against gelatinase enzyme and processing activity induced by the bone resorption agents of PTH, $1,25(OH)_2D_3$, $TNF-\alpha$, $IL-1{\beta}$ and $IL-1{\alpha}$ with strong protective effect in pretreatment with the extracts. CEDR extracts were shown to have the inhibiting effects against $IL-1{\alpha}-$ and $IL-1{\beta}-stimulated$ bone resorption and the effect of the pretreatment with a various concentrations of the medicinal extracts were significant. These results indicated that the CEDR extracts are highly stable and applicable to clinical uses in osteoporosis.

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A Study on Bone Formation & Osteoporosis by Taeyoungion-Jahage Extracts

  • Kim, Yi-Geun;Seong, Jun-Ho;Kim, Dong-Il;Lee, Tae-Kyun;Kim, Jun-Ki;Park, Young-Duck
    • The Journal of Korean Obstetrics and Gynecology
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    • v.15 no.4
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    • pp.45-60
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    • 2002
  • Mouse calvarial osteoblast cells were isolated and cultured. To examine whether the cells produce active gelatinases in culture medium or not,the cells were analyzed using by zymograsphic analysis on sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). We show that mouse calvarial osteoblasts in culture constitutively synthesize progelatinase- A. Then, mouse osteoblasts, which were stimulated by PTH, $1,25(OH)_2D_3$, mononuclear cell conditioned medium (MCM) and IL-1 as bone resorption agent's, showed increased collagenolysis by producing the active gelatinase. However, treatment of indomethacin and dexamethasone significantly decreased those effects of collagenolysis in mouse osteoblastic cells. On the other hand, IL-1 in stimulating bone resorption was examined using fetal mouse long bone organ culture. IL-1 stimulated bone resorption and produced marked resorption when present simultaneously. Furthermore, when it was examined the effects of indomethacin and dexamethasone on the dose dependent responses of $IL-1{\alpha}$, indomethacin and dexametasone produced a rightward shift in the IL-1 dose response curve. The results of in vitro cytotoxicities showed that Taeyoungjon-Jahage water extracts(T.Y.J-J.H.G extracts) have no any cytotoxicities in concentrations of $1-200\;{\mu}g/ml$ and furthermore there is no any cytotoxicity even in concentration of $300\;{\mu}g/ml$ on mouse calvarial bone cells. T.Y.J.-J.H.G. extracts had protective activity against PTH (2 units/mI), or MCM (5%, v/v), or $rhIL-1{\alpha}$ (1 ng/mI) or $1,25(OH)_2D3$ (10 ng/ml) , $IL-1{\alpha}$ and $IL-1{\beta}-induced$ collagenolysis in the mouse calvarial cells. Pretreatment of the T.Y.J.-J.H.G.extracts for 1 h, which by itself had little effect on cell survival, did not enhance the collagenolysis, nor significantly reduced the collagenolysis by pretreatment. Furthermore. the medicinal extracts were shown to have the protective effects against collagenolysis induced by $IL-1{\alpha}$ and $IL-1{\beta}$. Pretreatment of the extracts for 1 h significantly reduced the collagenolysis. Interestingly, the T.Y.J.-J.H.G. extracts were shown to have the inhibiting effects against gelatinase enzyme and processing activity induced by the bone resortion agents of PTH, $1,25(OH)_2D_3$, $IL-1{\beta}$ and $IL-1{\alpha}$, with strong protective effect in pretreatment with the extracts. T.Y.J.-J.H.G. extracts were shown to have the inhibiting effects against $IL-1{\alpha}-$ and $IL-1{\beta}-stimulated$ bone resorption and the effect of the pretreatment with a various concentrations of the medicinal extracts were significant. The inhibition extent and phenomena of IL-1 stimulated bone resorption by nonsteroidal anti-inflammatory agents of indomethacin and dexamethasone were similar to those obtained by T.Y.J.-J.H.G. extracts treatment in the mouse calvarial tissue culture system. These results indicated that the T.Y.J.-J.H.G.-water extracts are highly stable and applicable to clinical uses in osteoporosis.

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Effects of Cheongjogupye-tang(淸燥救肺湯) and Yieum-jeon(理陰煎) on Secretion of Mucin from Respiratory Epithelial Cells (청조구폐탕(淸燥救肺湯)과 이음전(理陰煎)이 호흡기 접액분비에 미치는 영향)

  • Park, Wan-Yeol;Seo, Un-Kyo
    • The Journal of Internal Korean Medicine
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    • v.29 no.2
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    • pp.318-333
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    • 2008
  • Objectives : In this study, the author tried to examine whether Cheogjogupye-tang (淸燥救肺湯, CGPT) and Yieum-jeon (理陰煎, YEJ) significantly affect in vitro and in vivo mucin secretion, MUC5AC gene expression in airway epithelial cells and contractility of isolated tracheal smooth muscle of rabbit. Materials and Methods : For in vitro experiment, confluent hamster tracheal surface epithelial (HTSE) cells were chased for 30 minutes in the presence of CGPT and YEJ to assess the effects of the agents on mucin secretion by enzyme-linked immunosorbent assay (ELISA), with removal of oriental herbal medicine extract from each agent-treated sample by centrifuge microfilter. Also, the effects of the agents on TNF-alpha or EGF-induced MUC5AC gene expression in human airway epithelial cells (NCI-H292) were investigated. Possible cytotoxicities of the agent were assessed by examining both LDH release from HTSE cells and the rate of survival and proliferation of NCI-H292 cells. For in vivo experiment, hypersecretion of airway mucin and goblet cell hyperplasia was induced by exposure of rats to $SO_2$ over 3 weeks. Effects of CGPT and YEJ orally administered for 1 week on in vivo mucin secretion from tracheal goblet cells of rats and hyperplasia of goblet cells were assessed using ELISA and histological analysis after staining the epithelial tissue with alcian blue, respectively. Also, the effects of CGPT and YEJ on contractility of isolated tracheal smooth muscle were investigated. Results : (1) CGPT significantly inhibited in vitro mucin secretion from cultured HTSE cells. However, YEJ did not affect in vitro mucin secretion; (2) CGPT and YEJ did not affect hypersecretion of in vivo mucin and hyperplasia of tracheal goblet cells; (3) CGPT and YEJ slightly increased the expression levels of TNF-alpha or EGF-induced MUC5AC gene in NCI-H292 cells; (4) CGPT and YEJ inhibited acetylcholine-induced contraction of isolated tracheal smooth muscle of rabbit; (5) CGPT and YEJ did not affect LDH release from HTSE cells and the survival and proliferation of NCI-H292 cells. Conclusion : The results from the present study suggest that CGPT and YEJ mainly affect the expression of mucin gene rather than secretion of mucin and do not show remarkable cytotoxicity to respiratory epithelial cells.

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Antitumor Activity of Corni Fructus Ethanol Extract in Sarcoma-180 Cancer Cells (산수유 에탄올 추출물의 Sarcoma-180 세포에 대한 항암 효과)

  • Kwon, Seong-Hyuk;Kwon, Soon-Jae;Kim, Jae-Yong;Kang, Kap-Suk;Shim, Ki-Hwan;Lee, Mi-Kyung;Seo, Kwon-Il
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.7
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    • pp.960-965
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    • 2010
  • To develop Corni Fructus as a cancer preventive food material, the in vitro cytotoxicities and in vivo antitumor activities of various concentrations of 80% Corni Fructus ethanol extract (CFEE) were investigated using sarcoma-180 cancer cell. Viability was decreased and cell death rate was increased in both dose- and time-dependent manners in cells treated with CFEE at 10, 100, 300, and $500\;{\mu}g/mL$ concentrations for 24, 48, and 72 hr. Proliferation was also inhibited more than 60% in cells treated with CFEE at the $100\;{\mu}g/mL$ concentration for 48 hr. In addition, the morphology of cells treated with CFEE at the 100 and $500\;{\mu}g/mL$ concentrations was distorted with shrunken cell masses and lower cell numbers compared to the control cells. In the cells treated with CFEE, the formation of apoptotic bodies and nuclear condensation were observed in dose dependent manners. CFEE also increased DNA fragmentation values at the 100 and $500\;{\mu}g/mL$ concentrations. The apoptosis induced by CFEE was connected to the proteolytic activation of caspase-3. When CFEE was administered at 100 and 300 mg/kg, ip, for 7 consecutive days in mice inoculated with sarcoma-180 cancer cell, the life span of the mice was found to be longer than that of the control mice that did not receive the extract. These results suggest that Corni Fructus may be used as a potential cancer preventive food material.

Effect of polymer of lysine on the mucin release from primary cultured hamster tracheal surface epithelial cells (염기성 아미노산인 라이신 중합체가 일차 배양된 햄스터 기관표면 상피세포에서의 점액소 유리에 미치는 영향)

  • Lee, Choong-Jae;Kim, Seon;Hong, Kyung-Hee
    • Journal of dental hygiene science
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    • v.2 no.1
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    • pp.25-29
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    • 2002
  • In the present study, we tried to investigate whether poly-L-lysine(PLL)(MW 78,000 and 9,600) significantly affect mucin release from cultured hamster airway goblet cells. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3H$-glucosamine for 24 hr and chased for 30 min in the presence of varying concentrations of PLL to assess the effects on $^3H$-mucin release. Possible cytotoxicities of PLL were assessed by measuring Lactate Dehydrogenase(LDH) release during treatment. The results were as follows : (1) PLL significantly inhibited mucin release from cultured HTSE cells in a dose-dependent manner; (2) there was no significant release of LDH by treatment of PLL 9,600; (3) however, in the case of treatment of PLL 78,000, there was significant release of LDH during treatment. We conclude that PLL which has molecular weight under 10,000 might inhibit mucin release from airway goblet cells without significant cytotoxicity. This finding suggests that PLL might be used as a tool of research for the hypersecretion of airway mucus.

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