• 제목/요약/키워드: inhibitory mechanism

검색결과 1,033건 처리시간 0.025초

위경탕(葦莖湯).가미위경탕(加味葦莖湯)의 B16-Fo에 대(對)한 항종양(抗腫瘍) 효과(效果)와 조직(組織) 변화(變化) (Effects of Wekyungtang and Kami-Wekyungtang on Pulmonary Tumor Cells and the Changes of Tissues)

  • 김현수;김성훈
    • 대한한의학회지
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    • 제16권2호
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    • pp.365-385
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    • 1995
  • In order to prove the antitumor effect of Wekyungtang(WKT) that was originated in Bigeubchunkeumyobang(備急千金要方), Wekyungtang with Houttuyniae Herba(WKT-I) and Wekyungtang with Oldenlandiae diffusae Herba(WKT-II) experimentally, the studies were done, We evaluated the cytotoxic activity against B16- Fo as well as the synergistic effects with anticancer drugs such as cyclophophamide (CPM), cisplatin(CPT) and 5-fluorouracil (5-FU) in vitro and measured body weight, survival time, hematological changes, changes of tissues in G57BL/6 implanted with B16-Fo. The results were obtained as follows: 1. In vitro cytotoxic effect against B16-Fo was shown in all groups as compared with control group, but the concentrations showing inhibitory growth rate below 55% of control was recognized in all concentrations of Wekyungtang(WKT) against B16-Fo and also concentration of $10^4$g/ml above in all group with cyclophophamide (CPM), concentration of $10^3$g/ml in Wekyungtang(WKT-l) with cisplatin(CPT) in synergistic effect, 2. In vivo body and tumor weight were significantly suppressed in all groups as compared with control group 3. The number of platelet, WBC, RBC were significantly increased in all groups, platelet aggregation was significantly increased in WKT-I and WKT-II as compared with control group. 4. In changes of tissues heavy infiltration oh cancer was shown in portal vein, pulmonary tissue, vein, peribronchiole, aveoli, while WKT-I was effective in antihepatic metastasis and WKT-II in pulmonary matastasis. From above results it was concluded that wekyungtang(WKT), wekyungtang with Houttuyniae Herba(WKT-I) and wekyungtang with Oldenlandiae diffusae Herba(WKT -II) had antitumor effect, and also wekyungtang combined with Houttuyniae Herba or Oldenlandiae diffusae Herba were more effective than wekyungtang only and also cyclophophamide (CPM), cisplatin(CPT) showed the more synergistic effect which suggests the necessity of continuous study on the mechanism of antitumor action of Houttuyniae Herba or Oldenlandiae diffusae Herba.

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구강암세포주에서의 Tamoxifen의 항암효과 (ANTICANCER EFFECT OF TAMOXIFEN IN ORAL CANCER CELL)

  • 정재화;윤필영;명훈;신재일;이종호;김명진
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제29권6호
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    • pp.365-373
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    • 2003
  • Tamoxifen is an selective estrogen receptor antagonist widely used in the management of patients with breast cancer for more than 30 years. It was thought to act primarily through occupying the estrogen receptor sites in ER positive breast cancer cells and directly on cancer cell proper. These inhibitory effects, which have been shown to be independent of the ER, highlight new mechanism of therapeutic action of tamoxifen. The purposes of this study were to identify ER in oral carcinoma cell lines and to evaluate ER independent cytotoxic effect of tamoxifen. KB(SCC), HSC-3(SCC) and A253(ACC) cell line were used and capacity of cell proliferation, apoptosis, in vitro invasion and gelatin zymography were tested. ER expression of each cell line were detected by RT-PCR and immunocytochemistry. Dose dependent inhibition of cell proliferation and inhibition of gelatinolytic activity were observed in all oral carcinoma cell lines and significant difference of apoptotic index were observed in A253 and KB. Tamoxifen inhibited in vitro invasion in all experimental groups. ER expression was detected in KB and A253. These data suggest that tamoxifen may play a role in management of oral carcinoma by independent cytotoxic effect and more advanced research must processed confirming ER-dependent cytotoxicity.

가미대강활탕(加味大羌活湯)이 Collagen II로 유발된 관절염에 미치는 영향 (Inhibitory Effects of Gamidaeganghwal-tang(Jiaweidaqianghuo-tang) on Rheumatoid Arthritis Induced by Type II Collagen)

  • 김민기;오민석
    • 한방재활의학과학회지
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    • 제19권2호
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    • pp.89-102
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    • 2009
  • Objectives : This study was carried out to understand the immunity responses and anti-oxidation effect of the Gamidaeganghwal-tang(GDT) on rheumatoid arthritis by using the THP-1 cells and the serum of CIA mice. Methods : For this purpose, GDT was orally administerd to mice with rheumatoid arthritis induced by collagen II. To investigate the immunity responses, value of cytokine and gene expression in the THP-1 cell, levels of cytokines in the serum of CIA(collagen type II induced arthritis) mice, number of immunocyte in PBMC of CIA mice were measured. Then, anti-oxidant activity, scavenging activity on DHHP(2,2-diphenyl-1-picrylhydrazyl) free radical and SOD(Superoxide dismutae)-like activity of GDT was observed. Results : 1. The levels of IL-$1{\beta}$, IL-6, IL-8, MCP-1 at 100, $50{\mu}g/m{\ell}$ of GDT were significantly reduced in the THP-1 cell. 2. The levels of TNF-${\alpha}$, COX-2 mRNA expression at 100, $50{\mu}g/m{\ell}$ of GDT and IL-$1{\beta}$, IL-6 at $100{\mu}g/m{\ell}$ of GDT were significantly reduced in the THP-1 cell line. 3. The levels of IL-6, TNF-${\alpha}$ and IL-$1{\beta}$ were significantly reduced in the serum of CIA mice. 4. The absolute number of CD3+, CD4+ and CD8+ cells were significantly induced, CD3+/CD69+, CD3+/CD49+, CD19+, B220+/CD23+ cells were significantly reduced in PBMC. 5. Scavenging activity on DPPH free radical and SOD-like activity were significantly induced in a concentration dependent manner. Conclusions : Taking all these observations, GDT considered to be effective in treating rheumatoid arthritis. Therefore we have to survey continuously in looking for the effective substance and mechanism in the future.

아토피 동물모델에서 고삼백선피복합방(GBBB)의 아토피 억제효과 (Inhibitory Effects of Gosambaeksunpibokhap-bang(GBBB) Extract in an Atopic Dermatitis Animal Model)

  • 이다영;승윤철;정규진
    • 디지털융복합연구
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    • 제14권11호
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    • pp.607-618
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    • 2016
  • 아토피 피부염(AD)에 대한 고삼백선피복합방(GBBB)의 치료적 가능성을 증명하기 위해 동물모델에서 다양한 면역 관련 인자들과 조직학적 변화에 대한 GBBB의 영향을 평가하였다. 실험 결과는 다음과 같다. GBBB도포군은 관능평가 결과에서 AD의 개선징후를 나타냈다. GBBB 도포군은 대조군에 비해 혈액 내 백혈구, 호중구, 림프구, 단핵구 면역세포 비율이 54%, 63%, 57%, 86%로 감소되었다. 또한 GBBB도포군은 대조군에 비해 혈청 내 IL-4, IL-5, IL-13, Histamine 및 IgE 생성량이 각각 40%, 80%, 62%, 61%, 57%로 유의성 있게 감소되었다. H&E 염색에서 GBBB 도포군은 대조군에 비하여 비만세포가 피부로 침윤되는 것이 억제되었으며 피부두께 역시 상대적으로 감소되었다. 이 결과를 바탕으로 GBBB는 피부에 직접 도포하는 AD 치료제로서 가능성이 있음이 확인하였다. 후속연구에서는 분자생물학적 연구를 통해 GBBB의 면역조절 기전을 구체적으로 밝히고자 한다.

Improved antimicrobial effect of ginseng extract by heat transformation

  • Xue, Peng;Yao, Yang;Yang, Xiu-shi;Feng, Jia;Ren, Gui-xing
    • Journal of Ginseng Research
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    • 제41권2호
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    • pp.180-187
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    • 2017
  • Background: The incidence of halitosis has a prevalence of 22-50% throughout the world and is generally caused by anaerobic oral microorganisms, such as Fusobacterium nucleatum, Clostridium perfringens, and Porphyromonas gingivalis. Previous investigations on the structure-activity relationships of ginsenosides have led to contrasting results. Particularly, the antibacterial activity of less polar ginsenosides against halitosis-related bacteria has not been reported. Methods: Crude saponins extracted from the Panax quinquefolius leaf-stem (AGS) were treated at $130^{\circ}C$ for 3 h to obtain heat-transformed saponins (HTS). Five ginsenoside-enriched fractions (HTS-1, HTS-2, HTS-3, HTS-4, and HTS-5) and less polar ginsenosides were separated by HP-20 resin absorption and HPLC, and the antimicrobial activity and mechanism were investigated. Results: HPLC with diode-array detection analysis revealed that heat treatment induced an extensive conversion of polar ginsenosides (-Rg1/Re, -Rc, -Rb2, and -Rd) to less polar compounds (-Rg2, -Rg3, -Rg6, -F4, -Rg5, and -Rk1). The antimicrobial assays showed that HTS, HTS-3, and HTS-4 were effective at inhibiting the growth of F. nucleatum, C. perfringens, and P. gingivalis. Ginsenosides-Rg5 showed the best antimicrobial activity against the three bacteria, with the lowest values of minimum inhibitory concentration and minimum bactericidal concentration. One major reason for this result is that less polar ginsenosides can more easily damage membrane integrity. Conclusion: The results indicated that the less polar ginsenoside-enriched fraction from heat transformation can be used as an antibacterial agent to control halitosis.

흰쥐에서 Ketamine에 의한 혈압하강 (Ketamine-Induced Blood Pressure Lowering in the Rat)

  • 유선봉;김상진;이문영;강형섭;김진상
    • 한국임상수의학회지
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    • 제22권3호
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    • pp.220-227
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    • 2005
  • Although ketamine has been used in the field of anesthetic medicine for its safety and favourable respiratory effects, the cardiovascular effects of ketamine is still controversial. To clarify the action and mechanism of ketamine upon cardiovascular system, arterial blood pressure, tension of aortic ring, left ventricular developed pressure and heart rate were measured in rats, Ketamine produced two types of effects on arterial blood pressure in anesthetized rats; monophasic effect (blood pressure lowering) and biphasic effect (initial transient blood pressure increasing following sustained lowering), The ketamine-induced lowering of aterial blood pressure showed a concentration-dependent manner, inhibited by the pretreament of $MgCl_2$ and potentiated by the pretreatment of $CaCl_2$. The ketamine-induced lowering of aterial blood pressure was suppressed by the pretreatment of nifedipine, verapamil or lidocaine. In phenylephrine-precontracted endothelium intact (+E) aortic rings, ketamine sometimes caused a small enhancement of contraction ($112.5{\pm}3.6{\%}$). However, in many experiments, ketamine produced a concentration-dependent relaxation in +E aortic rings precontracted with either phenylephrine or KCl. Ketamine-induced relaxation was significantly greater in KCl-precontracted strips than phenylephrine-precontracted strips. In phenylephrine-precontracted +E aortic rings, the ketamine-induced vasorelaxation was not suppressed by endothelium removal or by the pretreatment of a nitric oxide synthase inhibitors, L-$N^G$-nitro-arginine and a guanylate cyclase inhibitors, methylene blue, suggesting that the ketamine-induced vasorelaxation is not dependent on the endothelial function. In addition, ketamine elicited an increase in left ventricular developed pressure in perfused hearts accompanied by decrease in heart rate. These results suggest that ketamine could evoke a hypotension due to vasorelaxation and decrease in heart rate in rats. The inhibitory effect of cardiovascular system might be associated with modulation of $Ca^{2+}$ homeostasis.

제초제(除草劑) Cyhalofop-butyl ester의 벼와 피간(間) 선택성기작(選擇性機作) - 2. 제초제(除草劑) cyhalofop-butyl ester의 벼와 피간(間)에 미친 해부학적(解剖學的) 영향(影響) (Selective Mechanism of Cyhalofop-butyl ester between Rice and Echinochloa crus-galli - 2. Anatomical influence of Cyhalofop-butyl ester on rice and Echinochla crus-galli)

  • 박재읍;류갑희;이인용;이한규;신현승;이정운;김길웅
    • 한국잡초학회지
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    • 제14권3호
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    • pp.223-227
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    • 1994
  • 벼와 피의 속간(屬間) 선택성(選擇性)을 구명(究明)하기 위하여 제초제(除草除) cyhalofop-BE에 대(對)한 해부학적(解剖學的) 검경(檢鏡)을 통해 생장점(生長點)에 미친 영향(影響)을 조사(調査)한 결과(結果)는 다음과 같다. Cyhalofop-butyl ester 180ppm을 벼와 피에 처리시(處理時) 생장점(生長點)의 분제조직(分製組織) 저해(沮害) 양상(樣相)은 매우 유사(類似)하나 벼는 아주 경미(輕微)한 저해(沮害)를 보인 반면 피는 세포(細胞)의 분제(分製)이 억제(柳制)되고 배열(配列)이 불규칙(不規則)해지며 크게 위축(萎縮)되는 현상(現狀)을 보였다.

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Molecular Cloning of the DNA Gyrase Genes from Methylovorus Sp. Strain SS1 and the Mechanism of Intrinsic Quinolone Resistance in Methylotrophic Bacteria

  • Kim, Kwang-Seo;Kim, Jeong Hoon;Kim, Do Yeob;Kim, Hyun Jong;Park, Sang Tae;Kim, Young Min
    • Molecules and Cells
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    • 제20권3호
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    • pp.392-400
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    • 2005
  • The genes encoding the DNA gyrase A (GyrA) and B subunits (GyrB) of Methylovorus sp. strain SS1 were cloned and sequenced. gyrA and gyrB coded for proteins of 846 and 799 amino acids with calculated molecular weights of 94,328 and 88,714, respectively, and complemented Escherichia coli gyrA and gyrB temperature sensitive (ts) mutants. To analyze the role of type II topoisomerases in the intrinsic quinolone resistance of methylotrophic bacteria, the sequences of the quinolone resistance-determining regions (QRDRs) in the A subunit of DNA gyrase and the C subunit (ParC) of topoisomerase IV (Topo IV) of Methylovorus sp. strain SS1, Methylobacterium extorquens AM1 NCIB 9133, Methylobacillus sp, strain SK1 DSM 8269, and Methylophilus methylotrophus NCIB 10515 were determined. The deduced amino acid sequences of the QRDRs of the ParCs in the four methylotrophic bacteria were identical to that of E. coli ParC. The sequences of the QRDR in GyrA were also identical to those in E. coli GyrA except for the amino acids at positions 83, 87, or 95. The $Ser^{83}$ to Thr substitution in Methylovorus sp. strain SS1, and the $Ser^{83}$ to Leu and $Asp^{87}$ to Asn substitutions in the three other methylotrophs, agreed well with the minimal inhibitory concentrations of quinolones in the four bacteria, suggesting that these residues play a role in the intrinsic susceptibility of methylotrophic bacteria to quinolones.

Anticancer Activity of the Safflower Seeds (Carthamus tinctorius L.) through Inducing Cyclin D1 Proteasomal Degradation in Human Colorectal Cancer Cells

  • Park, Gwang Hun;Hong, Se Chul;Jeong, Jin Boo
    • 한국자원식물학회지
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    • 제29권3호
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    • pp.297-304
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    • 2016
  • The seed of safflower (Carthamus tinctorius L) has been reported to suppress human cancer cell proliferation. However, the mechanisms by which safflower seed inhibits cancer cell proliferation have remained nuclear. In this study, the inhibitory effect of the safflower seed (SS) on the proliferation of human colorectal cancer cells and the potential mechanism of action were examined. SS inhibited markedly the proliferation of human colorectal cancer cells (HCT116, SW480, LoVo and HT-29). In addition, SS suppressed the proliferation of human breast cancer cells (MDA-MB-231 and MCF-7). SS treatment decreased cyclin D1 protein level in human colorectal cancer cells and breast cancer cells. But, SS-mediated downregulated mRNA level of cyclin D1 was not observed. Inhibition of proteasomal degradation by MG132 attenuated cyclin D1 downregulation by SS and the half-life of cyclin D1 was decreased in SS-treated cells. In addition, SS increased cyclin D1 phosphorylation at threonine-286 and a point mutation of threonine-286 to alanine attenuated SS-mediated cyclin D1 degradation. Inhibition of ERK1/2 by PD98059 suppressed cyclin D1 phosphorylation and downregulation of cyclin D1 by SS. In conclusion, SS has anti-proliferative activity by inducing cyclin D1 proteasomal degradation through ERK1/2-dependent threonine-286 phosphorylation of cyclin D1. These findings suggest that possibly its extract could be used for treating colorectal cancer.

Artemisia fukudo essential oil attenuates LPS-induced inflammation by suppressing NF-${\kappa}B$ and MAPK activation in RAW 264.7 cells

  • Yoon, Weon-Jong
    • 한국자원식물학회:학술대회논문집
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    • 한국자원식물학회 2010년도 정기총회 및 추계학술발표회
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    • pp.13-13
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    • 2010
  • In the present study, the chemical constituents of Artemisia fukudo essential oil (AFE) were investigated using GC-MS. The major constituents were ${\alpha}$-thujone (40.28%), ${\beta}$-thujone (12.69%), camphor (6.95%) and caryophyllene (6.01%). We also examined the effects of AFE on the production of nitric oxide (NO), prostaglandin $E_2$ ($PGE_2$), tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-IL-$1{\beta}$ (IL-$1{\beta}$), and IL-6 in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Western blotting and RT-PCR analyses indicated that AFE has potent dose-dependent inhibitory effects on pro-inflammatory cytokines and mediators. We investigated the mechanism by which AFE inhibits NO and $PGE_2$ by examining the level of nuclear factor-${\kappa}B$ (NF-${\kappa}B$: p50 and p65) activation within the mitogen-activated protein kinase (MAPK: ERK, JNK and p38) pathway, which is an inflammation induced signal pathway in RAW 264.7 cells. AFE inhibited LPS-induced ERK, JNK and p38 phosphorylation. Furthermore, AFE inhibited the LPS-induced phosphorylation and degradation of $I{\kappa}B-{\alpha}$, which is required for the nuclear translocations of the p50 and p65 NF-${\kappa}B$ subunits in RAW 264.7 cells. Our results suggest that AFE might exert an anti-inflammatory effect by inhibiting the expression of pro-inflammatory cytokines. Such an effect is mediated by a blocking of NF-${\kappa}B$ activation which consequently inhibits the generation of inflammatory mediators in RAW 264.7 cells. AFE may be useful for treating inflammatory diseases.

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