• Title/Summary/Keyword: tumor inhibition ratio

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상황버섯으로부터 분리한 고분자 다당류의 약리활성 (Pharmacological Activities of the Polysaccharide extracted from Phellinus linteus)

  • 이은숙;서부일
    • 대한한의학방제학회지
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    • 제8권1호
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    • pp.281-289
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    • 2000
  • 상황버섯 자실체의 열수 및 알칼리 추출다당류에 대한 약리 효과는 다음과 같다. 1. 분자량은 10kD 부근에서 주를 이루고 있었으며, IR은 다당류의 전형적인 peak 흡수대를 나타냈다. 2. 항암 활성과 보체 활성에 있어서는 열수추출 다당류에서 높게 나타났으며, 지질 과산화 저해능은 알칼리 추출 및 열수 추출 분획에서 각각 71.3%와 55.8%의 저해율을 나타내었다. 상기와 같은 결과를 종합하여 볼 때 상황버섯 자실체의 열수 및 알칼리 추출물은 당과 단백질로 구성된 단백 다당류였으며, 열수 추출과 알칼리 추출에 의한 약리활성 정도는 유사한 것으로 조사되었다.

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목향에탄올추출물의 ROS-MAPKs 경로를 통한 세포사멸 유도 (Ethanol Extract of Saussurea lappa Root Induces Apoptosis through an ROS-MAPKs-Linked Cascade)

  • 김대성;이성진;이장천;우원홍;임규상;문연자
    • 약학회지
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    • 제56권3호
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    • pp.173-179
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    • 2012
  • Saussurea lappa (SL) and major compounds, sesquiterpene lactones, have been suggested to possess various biological effects, including anti-tumor, anti-ulcer, anti-inflammatory, anti-viral and cardiotonic activities. Therefore, the ethanol extract of Saussurea lappa root (ESL) is studied for the mechanism of its action in apoptotic pathway. ESL-treated cells manifested nuclear condensation, and fragmentation. ESL also triggered the mitochondrial apoptotic pathway, as indicated by a change in Bax/Bcl2 ratio and caspase-9/-3 activation. ESL induced p38 MAPK/JNK, p53, and ASK1 phosphorylation. ROS scavenger reversed ESL-induced apoptotic cell death via inhibition of caspase-3 and p38 MAPK/JNK phosphorylation. These results suggest that ESL induced apoptosis in HepG2 cells through the ROS-p38/JNK pathway.

Effects of the Antitumor Component, F-D-P, Isolated from Elfvingia applanata on the Immune Response

  • Kim, Young-So;Ryu, Ku-Hyun;Mo, Young-Keun;Lee, Chong-Kil;Han, Seong-Sun
    • 생약학회지
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    • 제25권4호통권99호
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    • pp.348-355
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    • 1994
  • An antitumor component, F-D-P, was purified from the hot water extract of the carpophores of Elfvingia applanata by precipitation with ethanol, dialysis, and passage through a column of DEAE-cellulose ion exchange. F-D-P inhibited the growth of Sarcoma 180 in mice showing the tumor inhibition ratio of 88.3% in doses of 20 mg/kg for ten days. Chemical analysis of F-D-P showed that it was composed of polysaccharide(65.3%) and protein(6.5%0, and that the monosaccharides consisting of the polysaccharide was glucose(89.1%) and mannose(10.9%). The immunomodulatory activities of F-D-P were explored by determining its effect on the proliferation of the whole and subpopulations of lymphocytes, and on the generation of natural killer(NK) cell activity in vitro. F-D-P was mitogenic to total lymphocytes and B cells, but not to purified T cells, even in the presence of accessory cells. F-D-P did not increase NK cell activity when added to cultures of resting lymphocytes. From these results, it is clear that F-D-P modulates primarily the humoral immune responeses.

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Antitumor and Immunopotentiating Effects of Manda Enzyme

  • Hwang, Woo-Ik;Hwang, Yoon-Kyung;Lee, Ji-Young;Lee, Jae-Yeon;Okuda, Hiromichi
    • Natural Product Sciences
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    • 제2권1호
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    • pp.29-36
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    • 1996
  • This study was to evaluate the antitumor and immunopotentiation effects of Manda Enzyme (ME). Oral administration of ME (0.2ml/mouse) to tumor bearing mice significantly prolonged survival rate compared to the control group with the prolongation ratio of 40%. The inhibition ratios for the first and the second experiments were 51.8% and 26.4%, respectively. Only the spleen index was significantly increased in the MEF-treated group, but not in the control group. Gamma globulin level of the MEF-treated group was elevated when mice were injected with sarcoma-180 cells on the left groin. Activities of natural killer (NK) and lymphokineactivated killer (LAK) cells were observed by $^{51}Cr-release$ method. Activities of NK cell against YAC-1 cells were significantly increased in the MEF treated group. And LAK cell activities against P815 cells were also significantly increased in the experimental group. These observations, therefore, suggest that ME may have an anticancer effect and immunopotentiating effect in vivo.

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눈꽃동충하초(Paecilomyces japonica DGUM 32001) 균사배양물의 항암 효과에 관한 유세포분석학적 연구 (Flow Cytometrical Investigation on Antitumor Activity of Mycelial Culture of Insect-born Fungus Paecilomyces japonica DGUM 32001)

  • 이지선;이임선;정경수;김용해;한영환;이만형
    • 약학회지
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    • 제45권1호
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    • pp.64-70
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    • 2001
  • Protein-polysaccharide fractions, PJ-3 and PJ-4, were prepared from mycelial culture filtrate of an insect-born fungus, Paecilomyces japonica DGUM 32001, and subjected to a flow cytometrical analysis for their vivo antitumor and immunomodulating activity in ICR mice. When i.p. injected once daily for semen days at 100 mg/kg, PJ-4 exerted a strong antitumor activity showing the growth inhibition ratio of 85.1% against i.p. implanted sarcoma 180 cells, while PJ-3 showed only a weak activity. Moreover, PJ-4 signiscantly increased the expression level of CD25 (IL-2R $\alpha$-chain) as well as forward scatter (FSC) values of splenic CD8$^{8}$ T cells. It is also noteworthy that PJ-4 strongly induced the peritoneal exudate cells in the same experiment. In an in vitro study, PJ-4 slightly inhibited the growth of sarcoma 180 cells at the concentration of 50$\mu$g/ml or higher. These results strongly suggest that PJ-4 might exert its antitumor activity through immunostimulation as well as direct inhibitory activity on the tumor cells.

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Synthesis and Evaluation of 2-[123I]iodoemodin for a Potential Breast Cancer Imaging Agent

  • Park, Jeong-Hoon;Kim, Sang-Wook;Yang, Seung-Dae;Hur, Min-Goo;Chun, Kwon-Soo;Yu, Kook-Hyun
    • Bulletin of the Korean Chemical Society
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    • 제29권3호
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    • pp.595-598
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    • 2008
  • Emodin (3-methyl-1,6,8-trihydroxyanthraquinone) is a natural chemotherapeutic compound with diverse biological properties including an antitumor activity. Emodin, a specific inhibitor of the protein tyrosine kinase, has a number of cellular targets in related to it. Its inhibition activity affects the mammalian cell cycle regulation in specific oncogene. Practically, it has been proven to inhibit HER-2/neu tyrosine kinase expressing breast cancer cells as an anticancer agent. 2-[123I]iodoemodin has been synthesized and evaluated human breast cancer cells (MDA-MB-231, MCF-7, fibroblast as a control) which express basal levels of HER-2/neu tyrosine kinase to investigate its suitability as a breast cancer imaging agent and 2-iodoemodin has been synthesized as a standard compound. The radiochemical yield of the 2-[123I]iodoemodin was about 72% and its radiochemical purity was over 97% after purification. The radioactivity of the 2-[123I]iodoemodin was increased in a time dependent manner in both cell lines and the ratio of MDA-MB-231 and MCF7 to fibroblast was 2.9 and 1.7, respectively.

Antitcoagulant and antiplatelet activities of scolymoside

  • Yoon, Eun-Kyung;Ku, Sae-Kwang;Lee, Wonhwa;Kwak, Soyoung;Kang, Hyejin;Jung, Byeongjin;Bae, Jong-Sup
    • BMB Reports
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    • 제48권10호
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    • pp.577-582
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    • 2015
  • Cyclopia subternata is a medicinal plant commonly used in traditional medicine to relieve pain. Here, the anticoagulant effects of scolymoside, an active compound in C. subternata, were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of thrombin and activated factor X (FXa). The effects of scolymoside on plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) expression were evaluated in tumor necrosis factor (TNF)-α-activated human endothelial cells. Treatment with scolymoside resulted in prolonged aPTT and PT and the inhibition of thrombin and FXa activities and production. In addition, scolymoside inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. Scolymoside also elicited anticoagulant effects in mice, including a significant reduction in the PAI-1 to t-PA ratio. Collectively, these findings indicate that scolymoside possesses anticoagulant activities and could be developed as a novel anticoagulant.

Expression of the Proto-oncogene Pokemon in Colorectal Cancer - Inhibitory Effects of an siRNA

  • Zhao, Gan-Ting;Yang, Li-Juan;Li, Xi-Xia;Cui, Hui-Lin;Guo, Rui
    • Asian Pacific Journal of Cancer Prevention
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    • 제14권9호
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    • pp.4999-5005
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    • 2013
  • Objective: This study aimed to investigate expression of the proto-oncogene POK erythroid myeloid ontogenic factor (Pokemon) in colorectal cancer (CRC), and assess inhibitory effects of a small interference RNA (siRNA) expression vector in SW480 and SW620 cells. Methods: Semi-quantitative reverse transcription-polymerase chain reaction (PCR) and immunohistochemistry were performed to determine mRNA and protein expression levels of Pokemon in CRC tissues. Indirect immunofluorescence staining was applied to investigate the location of Pokemon in SW480 and SW620 cells. The siRNA expression vectors that were constructed to express a short hairpin RNA against Pokemon were transfected to the SW480 and SW620 cells with a liposome. Expression levels of Pokemon mRNA and protein were examined by real-time quantitative-fluorescent PCR and western blot analysis. The effects of Pokemon silencing on proliferation of SW480 and SW620 cells were evaluated with reference to growth curves with MTT assays. Results: The mRNA expression level of Pokemon in tumor tissues ($0.845{\pm}0.344$) was significantly higher than that in adjacent tumor specimens ($0.321{\pm}0.197$). The positive expression ratio of Pokemon protein in CRC (87.0%) was significantly higher than that in the adjacent tissues (19.6%). Strong fluorescence staining of Pokemon protein was observed in the cytoplasm of the SW480 and SW620 cells. The inhibition ratios of Pokemon mRNA and protein in the SW480 cells were 83.1% and 73.5% at 48 and 72 h, respectively, compared with those of the negative control cells with the siRNA. In the SW620 cells, the inhibition ratios of Pokemon mRNA and protein were 76.3% and 68.7% at 48 and 72 h, respectively. MTT showed that Pokemon gene silencing inhibited the proliferation of SW480 and SW620 cells. Conclusion: Overexpression of Pokemon in CRC may have a function in carcinogenesis and progression. siRNA expression vectors could effectively inhibit mRNA and protein expression of Pokemon in SW480 and SW620 cells, thereby reducing malignant cell proliferation.

Cisplatin과 보정방암탕에 의한 백서 사구체 혈관사이세포의 세포사멸 기전 연구 (Machanism of Cisplatin-induced Apoptosis and Bojungbangam-tang-mediated Anti-apoptotic Effect on Cell Proliferation in Rat Mesangial Cells)

  • 주성민;김성훈;김영목;전병훈;김원신
    • 동의생리병리학회지
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    • 제27권1호
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    • pp.43-48
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    • 2013
  • Cisplatin is a anti-neoplastic agent which is commonly used for the treatment of solid tumor. Cisplatin activates multiple signal transduction pathways involved in the stress-induced apoptosis in a variety of cell types. Previous study reported that cisplatin induces apoptosis through activation of ERK, p38 and JNK in rat mesangial cells, but apoptotic pathway remain known. The present study investigated the apoptotic pathway for cisplatin-indcued apoptosis in rat mesangial cells. cisplatin-induced apoptosis was associated with activation of caspase-3, caspase-8, caspase-9. Caspase-8 inhibition prevented the activation of both caspase-3 and caspase-9. In addition, cisplatin-induced apoptosis increased the expression of Bax, but not the level of Bcl-2. These change of Bax/bcl-2 ratio caused the release of cytochrome c from mitochondria into cytosol. In previous study, the ethanol extract of Bojungbangam-tang (EBJT) inhibited cisplatin-induced apoptosis in rat mesangial cells through inhibition of ERK and JNK activation. However, EBJT did not increase cell proliferation, because it did not prevent cisplatin-induced G2/M phase arrest. These effect of EBJT may be related to p38 activation. Cisplatin-induced G2/M phase arrest are inhibited by treatment with p38 inhibitor and EBJT in rat mesangial cells. Also, p38 inhibition and EBJT treatment on cisplatin-induced G2/M phase arrest are markedly increased the G0/G1 phase and reduced the sub-G1. In conclusion, anti-apoptotic effet of EBJT did not increases cell proliferation, because EBJT did not reduce p38 activation related to cisplatin-induced G2/M phase arrest.

Inhibition of Wntless/GPR177 suppresses gastric tumorigenesis

  • Seo, Jaesung;Kee, Hyun Jung;Choi, Hye Ji;Lee, Jae Eun;Park, Soo-Yeon;Lee, Seung-Hyun;Jeong, Mi-Hyeon;Guk, Garam;Lee, SooYeon;Choi, Kyung-Chul;Choi, Yoon Young;Kim, Hyunki;Noh, Sung Hoon;Yoon, Ho-Geun;Cheong, Jae-Ho
    • BMB Reports
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    • 제51권5호
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    • pp.255-260
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    • 2018
  • Wntless/GPR177 functions as WNT ligand carrier protein and activator of $WNT/{\beta}$-catenin signaling, however, its molecular role in gastric cancer (GC) has remained elusive. We investigated the role of GPR177 in gastric tumorigenesis and provided the therapeutic potential of a clinical development of anti-GPR177 monoclonal antibodies. GPR177 mRNA expression was assessed in GC transcriptome data sets (GSE15459, n = 184; GSE66229, n = 300); protein expression was assessed in independent patient tumor tissues (Yonsei TMA, n = 909). GPR177 expression were associated with unfavorable prognosis [log-rank test, GSE15459 (P = 0.00736), GSE66229 (P = 0.0142), and Yonsei TMA (P = 0.0334)] and identified as an independent risk predictor of clinical outcomes: GSE15459 [hazard ratio (HR) 1.731 (95% confidence interval; CI; 1.103-2.715), P = 0.017], GSE66229 [HR 1.54 (95% CI, 1.10-2.151), P = 0.011], and Yonsei TMA [HR 1.254 (95% CI, 1.049-1.500), P = 0.013]. Either antibody treatment or GPR177 knockdown suppressed proliferation of GC cells and sensitized cells to apoptosis. And also inhibition of GPR177 suppresses in vitro and in vivo tumorogenesis in GC cells and inhibits $WNT/{\beta}$-catenin signaling. Finally, targeting and inhibition of GPR177 with antibody suppressed tumorigenesis in PDX model. Together, these results suggest GPR177 as a novel candidate for prognostic marker as well as a promising target for treatment of GC patients.