• Title/Summary/Keyword: Anticancer agent

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Effect of Pore Size of Mesoporous Spherical Silica for the Purification of Paclitaxel from Plant Cell Cultures (식물세포배양으로부터 Paclitaxel 정제를 위한 메조다공성 실리카의 기공크기 영향)

  • Oh, Hyeon-Jeong;Jung, Kyeong Youl;Kim, Jin-Hyun
    • KSBB Journal
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    • v.28 no.3
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    • pp.208-212
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    • 2013
  • Four types of mesoporous spherical silica adsorbents with different physical properties were prepared by spray pyrolysis and were used for the purification of the anticancer agent paclitaxel from plant cell cultures. Pore size had a greater effect on the removal of plant-derived impurities during the pre-purification of paclitaxel compared with surface area and pore volume. An appropriate pore diameter (~9.07 nm) was required to achieve the highest purity (~46.1%) and yield (~82.3%) of paclitaxel. These results were confirmed by HPLC analysis of the absorbent after treatment and Thermogravimetric analysis of the organic substances bonded to the adsorbent.

Effects of Dojeokseungki-tang on the apoptosis of Leukemia Cell (도적승기탕이 백혈병세포의 Apoptosis에 미치는 효과)

  • Park Min Chul;Kwon Jin;Jeong Han Sol;Lee Kwang Gyu
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.17 no.2
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    • pp.338-345
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    • 2003
  • The purpose of this research was to investigate the anticancer effects of Dojeokseungki-tang(DJSKT) on the various leukemia cell lines. DJSKT treatment suppressed proliferation of cultured-HL60, Jurkat, L1210 cells and increased apoptosis of cultured-L1210, HL60, Molt4, Jurkat cells. DJSKT treatment induced apoptosis of Jurkat cells including the morphologic changes such as the 'ladder pattern' revealed by agarose gel electrophoresis of DNA in a dose-dependent manner. Administration of DJSKT induced apoptosis of transplanted-L1210 cells in vivo, and decreased of mitochondrial transmembrane potential of L 1210 and Jurkat cells in vitro. DJSKT treatment reduced the expression of bcl-2 proteins in Jurkat cells and increased ICE, c-myc, p53 mRNA expression in Molt4 cells. In conclusion, these results suggest that DJSKT might be usefully applied for anti-carcinogenic agent of leukemia.

Tamoxifen Suppresses Clusterin Level through Akt Inactivation and Proteasome Degradation in Human Prostate Cancer Cells

  • Shim, Jae-Ho;Choi, Chang-Su;Lee, Eun-Chang;Kim, Mie-Young;Chun, Young-Jin
    • Biomolecules & Therapeutics
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    • v.17 no.1
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    • pp.25-31
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    • 2009
  • Clusterin is a heterodimeric sulfated glycoprotein and plays a role in many different types of cancer as a cell survival factor and helps cancerous cells to evade stress-induced apoptosis. To investigate whether the regulation of clusterin expression is involved in the mechanism of anticancer agent, we studied the effect of tamoxifen on clusterin expression in human prostate cancer PC-3 cells. Treatment of PC-3 cells with tamoxifen reduced cellular proliferation. Western blot analyses showed that treatment with tamoxifen suppressed clusterin expression in a concentration-dependent manner. Transfection with clusterin siRNA plasmid showed that clusterin is required for PC-3 cell survival. We found that tamoxifen resulted in a rapid decrease in the phosphorylation of Akt on Ser473 leading to prevent kinase activity. Expression of myristoylated Akt prevented tamoxifen-mediated clusterin downregulation. Interestingly, MG132, a wellknown proteasome inhibitor also recovered clusterin expression suppressed by tamoxifen. These data indicate that clusterin expression may be regulated by activation of Akt and ubiquitin-proteasome pathway plays an important role in tamoxifen-mediated clusterin suppression.

Diallyl Disulfide (DADS) Induces Upregulation of PTEN in Human Leukemia Cells

  • Chung, Weon-Kuu;Lee, Byoung-Kil;Lee, Young-Rae;Park, Jin-Ny;Kwon, Hyoung-Chul
    • Journal of Food Hygiene and Safety
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    • v.24 no.1
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    • pp.38-45
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    • 2009
  • The differentiation of leukemia cells into mature cells is a major target of the human leukemia therapy. As differentiated leukemia cells lose their proliferative and tumor-forming abilities, differentiation inducers may be useful for the treatment of leukemia. In this study, the experiments were designed to determine whether diallyl disulfide (DADS) regulates expressions of tumor suppressor protein PTEN (phosphatase and tension homologue) in HL60 cells. DADS causes upregulation of PTEN in a time- and dose-dependent manner, which was correlated with decrease of phospho-Akt level. These results suggest that DADS induces upregulation of PTEN in human leukemia cells. These results suggest that DADS may be a useful anticancer agent for management of human leukemia.

Hematopoietic Characteristics of the Ethylacetate Fraction of Panax ginseng and Identification of the Chemical Constituents (인삼의 에칠아세테이트 추출분획의 조혈활성 특성 및 구성 성분 동정)

  • Park, Jong-Dae;Wee, Jae-Joon;Kim, Man-Wook;Lee, Hyong-Joo
    • Applied Biological Chemistry
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    • v.32 no.2
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    • pp.137-142
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    • 1989
  • The ethylacetate soluble fraction of Panax ginseng extract, which has been reported to exhibit hematopoietic effect, was divided into three subfractions, i.e., Fr. I, Fr. II and Fr. III by silica gel column chromatography. The hematopoietic effect of each subfraction was examined in rats treated with anticancer agent, Ara-C($1-{\beta}-D-arabinofuranosylcytosine)$). Among them, Fr. III showed 90% recovery of leucocyte and erythrocyte counts in bonemarrow cell depleted rats, suggesting it to be hematopoietic fraction. From Fr. III, two major compounds were isolated and identified as ginsenoside $Rh_1$ and $Rg_2$ by $^{13}C-NMR$ and degradation method.

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Comparison of Single-Dose Toxicity by Intravenous Infusion or Bolus Injection with CKD-602, a Camptothecin Anticancer Agent in Rats (II): Hematological and Serum Biochemical, and Histopathological Changes

  • Kim, Choong-Yong;Yang, Byung-Chul;Kim, Joon-Kyum;Kim, Jong-Choon;Kim, Yong-Beom;Kang, Boo-Hyon;Han, Sang-Seop
    • Toxicological Research
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    • v.20 no.4
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    • pp.381-389
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    • 2004
  • The toxicity of CKD-602 was investigated at doses of 3, 9, and 27 mg/kg in rats, when the same total dose of CKD-602 was administered over 24 hr-continuous infusion or bolus injection. At 3 and 9 mg/kg, the 24-hr infusion group showed a more decreased WBC count on day 3, compared with the bolus group. Administration of CKD-602 caused more toxic effects such as the significant decreases of RBC counts, hematocrit, hemoglobin, and platelet count on day 7 post-administarion in the 24-hr infusion group than in the bolus group. Administration of CKD-602 also caused histopathological changes such as extramedullary hemopoiesis of liver and spleen, hyperplasia of femoral bone marrow, and caecal dilation. These toxic effects were more severe in the 24-hr infusion group than in the bolus injection group, indicating that the toxicity of CKD-602 may be dependant upon the duration of administration.

Intraarterial Scintigraphy in Recurrent Cervix Cancer - The Evaluation of Radionuclide Therapeutic Trials - (자궁경부재발암 환자의 국소동맥 주입식 동위원소 검사 -방사성 동위원소의 치료시도를 위한 평가-)

  • Kim, Eun-Young;Suh, Jin-Suck;Park, Chang-Yun;Lee, Jong-Tae;Yoo, Hyung-Sik
    • The Korean Journal of Nuclear Medicine
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    • v.24 no.2
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    • pp.293-298
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    • 1990
  • We performed 17 intraarterial scintigraphies in six patients with recurrent cervix cancer. With Seldinger method, the agent (four different radiopharmaceuticals) was perfused at the same speed of infusion of anticancer drugs (25 cc/hour) through internal iliac artery. There were four different radiopharmaceuticals; I-131-Lipiodol, Tc (Technetium)-99m-HSa (Human Serum Albumin), $^{99m}Tc-Sucralfate$ and $^{99m}Tc-MAA$ (Macroaggraegated Albumin). We evaluate the distribution pattern of radioactivity by the use of ratio of Tumor/Extratumor uptake (T/ET ratio). Our results reveals that $^{99m}Tc-MAA$ scan showed the highest T/ET ratio and the other were not ideal agents for intraarterial therapy of recurrent cervix cancer. In conclusion, an ideal radioisotope and tracer which can block capillary, for example MAA, should be re-evaluated or produced in order to treat the patient with recurrent cervix cancer.

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N-acetylcysteine modulates cyclophosphamide-induced immunosuppression, liver injury, and oxidative stress in miniature pigs

  • Kang, Kyung Soo;Shin, Sangsu;Lee, Sang In
    • Journal of Animal Science and Technology
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    • v.62 no.3
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    • pp.348-355
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    • 2020
  • Cyclophosphamide, a cytotoxic anticancer agent, induces immunosuppression and has several adverse effects. N-acetylcysteine alleviates oxidative stress, liver injury, and intestinal tissue damage. The present study examined whether N-acetylcysteine modulates the adverse effects of cyclophosphamide in pigs. Miniature pigs (n = 15) were used as an experimental model to evaluate the effects of N-acetylcysteine treatment on immune reactions, liver injury, and oxidative stress after cyclophosphamide challenge. Corn-soybean meal based dietary treatments were as follows: control diet with either saline injection, cyclophosphamide injection, or 0.5% N-acetylcysteine and cyclophosphamide injection. N-acetylcysteine increased the number of immune cells and decreased TNF-α production after cyclophosphamide injection and decreased TNF-α, IFN-γ, NF-κB, and IL-8 expression and increased IL-10 expression in peripheral blood mononuclear cells. Serum levels of alanine transaminase and aspartate aminotransferase decreased, superoxide dismutase activity increased, and malondialdehyde activity decreased following N-acetylcysteine treatment after cyclophosphamide injection. N-acetylcysteine decreases immunosuppression, liver injury, and oxidative stress in cyclophosphamide-challenged miniature pigs. The present study suggests that N-acetylcysteine has therapeutic application in livestock for modulating immune reactions, liver injury, and oxidative stress.

Buccal Transport of Paclitaxel using Ethanol and Glyceryl Monooleate

  • Lee, Yoon-Jin;Kang, Myung-Joo;Park, Young-Mi;Choi, Young-Wook;Lee, Jae-Hwi
    • Journal of Pharmaceutical Investigation
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    • v.37 no.5
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    • pp.311-314
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    • 2007
  • Paclitaxel (PTX) is an antineoplastic agent approved for the treatment of ovarian and breast carcinomas. However, the use of paclitaxel as an anticancer drug is limited by its extremely poor water solubility (below $0.3\;{\mu}g/mL$). Furthermore, it has very low bioavailability when administered orally because paclitaxel is a substrate of P-glycoprotein (P-gp) efflux pump. In this study, buccal delivery of PTX was investigated as one of the alternatives for PTX delivery. Ethanol and glyceryl monooleate (GMO) were selected as permeation enhancing agents to increase solubility and permeation across buccal mucosa of PTX. At the different concentrations of ethanol solution ($30{\sim}70\;w/w\;%$), PTX permeation was studied, followed effects of GMO in the concentration range of $2.5{\sim}25%$ with ethanol vesicle. The transbuccal ability of PTX was evaluated in vitro using Franz diffusion cells mounted with rabbit buccal mucosa. As a result, incorporation of PTX into ethanol vesicle with GMO significantly enhanced the PTX permeation in rabbit buccal mucosa. Particularly, the mixtures of ethanol:water:GMO at the ratio of 50:47.5:2.5 showed the most excellent enhancing ability. The results showed a promising possibility for buccal delivery of PTX.

Selective Cytotoxicity of New Platinum (II) Complex Containing 1,3-Bis-phenylthiopropane (1,3-비스페닐치오 프로판을 배위자로 한 백금 (II)착체의 선택적 세포독성)

  • 노영수;윤기주;이경태;장성구;정지창
    • YAKHAK HOEJI
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    • v.43 no.3
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    • pp.369-377
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    • 1999
  • A new series of highly water soluble platinum(II) complexes {Pt(II)[1,3-bis(phenylthio) propane](trans- -1,2-diaminocyclohexane) (PC-1) and Pt(II)[1,3-bis-(phenythio)propane] cis-1,2-diaminocyclohexane(PC-2)} were synthesized, and characterized by their elemental analysis and by various spectroscopic techniques[infrared(IR), 13C-nuclear magnetic resonance (NMR)]. In vitro antitumor activity of new Pt(II) complexes was tested against P-388 and L-1210 mouse lymphocytic leukemia cell lines, PC-14 / P, PC-14/ADM and PC-14 / CDDP human pulmonary adenocarcinima, DU-145 human prostate carcinoma, HT-1376 human bladder carcinoma, ZR-75-1 human breast carcinoma, MKN-45/P and MKN-45/CDDP human gastric adenocarcinoma cell lines using colorimetric MTT[3-(4,5-dimethyl thiazol-2-yl)-2.5-diphenyltetrazoliumbromide] assay for cell survival and proliferation. PC-1 showed active against L-1210, P-388 leukemia, human lung, stomach, prostate, bladder and breast cancer cell lines, and the antitumor activity of these compounds were comparable or superior to those of PC-2 and displatin. The nephrotoxicities of PC-1 and PC-2 were found quite less than that of cisplatin using MTT and [3H] thymidine uptake in rabbit proximal tubule cells and human kidney cortical cells. Based on these results, this novel platinum (II) complex compound (PC-1) represents a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.

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