• Title/Summary/Keyword: antitumor cytotoxicity

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In Vitro and in Vivo Antitumor Evaluation of Berbamine for Lung Cancer Treatment

  • Hou, Zhi-Bo;Lu, Kai-Jin;Wu, Xiao-Li;Chen, Cong;Huang, Xin-En;Yin, Hai-Tao
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.4
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    • pp.1767-1769
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    • 2014
  • Purpose: Lung cancer, one of the most frequently diagnosed cancers in the world, is characterized by relatively high morbidity and mortality. Berbamine (BER) has been initially reported to exert anti-proliferative effects against a series of cancers. Methods: In this study the in vitro cytotoxicity of BER was measured by MTT assay. In vivo anti-cancer efficacy of BER was assessed in A549 xenografts. Results: Cytotoxicity tests showed dose-dependent cell growth inhibition effects of BER against A549 cells. Moreover, BER significantly reduced the growth of lung cancer in a dose-dependent manner in nude mice with prolonged survival time. Conclusion: Therefore, BER might be in herbal medicine for cancer therapy and further efforts are needed to explore therapeutic strategies.

Study on Antitumor and Antimetastatic Effect of Kamigedang-tang (가미저당탕의 항암 및 항전이 효과에 관한 연구)

  • Lee Dong Hoon;Kim Dong Hee;Kang In Cheol;Park Young Mi;Song Gyu Yong;Kim Sung Hoon
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.3
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    • pp.472-478
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    • 2002
  • The purpose of this study was to investigate the effect of Kamigedang-tang(KGDT) water extract on the antitumor and anti metastatic activity. The results were summarized as follows: KGDT extracts exhibited a significant cytotoxicity against P388, SK-MEL-2, SK-OV-3, and B16-F10 cell lines and showed significant inhibitoty effect on DNA topoisomerase I from calf thymus. The T/C% was 122.9% in KGDT treated group in S-180 bearing ICR mice. Also, KGDT extracts exhibited efficient affect adhesive effect of A549 cell to complex extracellular matrix. In CAM assay, KGDT extracts inhibited angiogenesis at 15㎍/egg concentration insignificantly as compared with control. These results suggested that KGDT extracts might be usefully applied for prevention and treatement of cancer.

Study on 2-thioDMNQ-S160, A Derivative of Shikonin, Antitumor Constituent of Lithospermum Erythrorhizon (자초의 항암성분 수도체 2-thioDMNQ-S160에 관한 연구)

  • Song Gyu Yong;Lee Hyo Jung;Khil Jae-Ho;Kim Sung Hoon
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.3
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    • pp.542-546
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    • 2002
  • The purpose of this study was to investigate the effect of 2-thioDMNQ-S160, shikonin analogue isolated from Uthospermum Erythrorhizon, on the antitumor activity. In the present study, 2-thioDMNQ-S160 exhibited a significant cytotoxicity against L1210, A549, U937, and 816-BL6 cell lines with IC/sub 50/s of 2.4ug/ml, 2,0ugjml. 4ug/ml and 20 ug/ml, respectively. 2-ThioDMNQ-S160 strongly inhibited adhesion of B16-BL6 cells to gelatin and matrigel coated matrices. Also, 2-ThioDMNQ-S160 exhibited anti-invasive effect of B16-BL6 cells. The T/C% was 123 % in 2-ThioDMNQ-S160 treated group in S-180 bearing ICA mice. These results suggested that 2-thioDMNQ-S160 might be a potent candidate of cancer drug.

Study on the Antitumor Substance Isolated from Oldenlandiae diffusae Herba (백화사활초(白花蛇活草)로부터 분리(分離)된 항암성물질(抗癌性物質)에 관(關)한 연구(硏究))

  • kim, Sung-Hoon
    • Journal of Haehwa Medicine
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    • v.4 no.2
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    • pp.273-297
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    • 1996
  • Hexane fraction of Oldenlandiae diffusae Herba(ODH) which was being used for the treatment of caner in oriental medicine showed the best cytotoxicity against L1210 and A549 in the solvent fractions. Antitumor substance isolated from hexane fraction of ODH was identified as ursolic acid(UA) by photometric analysis. IC50 of UA against cancer cells as SNU-1, HCT15, XF498, SK-MEL2 and A549 was $13{\mu}g/m{\ell}$, $15{\mu}g/m{\ell}$, $12{\mu}g/m{\ell}$, $9{\mu}g/m{\ell}$ and $11{\mu}g/m{\ell}$ respectively. It significantly inhibited the metastasis to lungs and kidneys from pulmonary colonization assay and study on histological changes of organs and showed the enhancing effect on B cell dosage-dependently by FACS analysis. T/C % of UA against S-180 cells was 171 % and its cytotoxicity against SNU-1 iant was confirmed from the morphological changes by elctronic microscopes such as SEM and TEM that it induced undulated membrane 4 hr after UA treatment, and the breakdown of cell membrane and nucleus 24 hr after UA treatment.

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Study on Antitumor Activity of Kamisagoonjatang, Kamijihwangtang and Kamigoonjajihwangtang (가미지황탕(加味地黃湯), 가미사군자탕(加味四君子湯) 및 가미군자지황탕(加味君子地黃湯)의 항종양활성(抗腫瘍活性))

  • Kim, Dong-hee;Kim, Sung-hoon
    • Journal of Haehwa Medicine
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    • v.8 no.1
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    • pp.131-146
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    • 1999
  • To evaluate the antitumor activity of Kamisagoonjatang(KST), Kami-jihwangtang (KJT) and Kamigoonjajihwangtang(KKJT), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against B16-F10, HT1080, SNU, and L1210, con-centration inhibiting cell growth up to below 50% of control was recognized at $10^{-3}g/ml$ of KKJT. 2. In cytotoxicity against A549, SK-OV-3, XF498 and HCT15, concentration inhibiting cell growth up to below 30% of control was over $400{\mu}g/ml$ of KKJT only and also over $200{\mu}g/ml$ against SK-MEL-2. 3. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $200-400{\mu}g/m{\ell}$, of KST, over $400{\mu}g/m{\ell}$ of KJT and $100-200{\mu}g/m{\ell}$ of KKJT. 4. The T/C% was 122.8 in KJT, 127.4 in KST and 158.4 in KKJ-Ttreated group in S-180 bearing ICR mice. 5. In hematological changes in S-180 bearing ICR mice, numbers of WBC were decreased significantly in KJT and KKJT treated groups as compared with control, whereas those of platelet were increased with no significance in all groups as compared with control. From above results it was concluded that KKJT could be usefully applied for the prevention and treatment of cancer.

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Synthesis of 6-Aziridinylbenzimidazole Derivatives and Their In Vitro Antitumor Activities

  • Ahn, Chan-Mug;Kim, Soo-Kie;Han, Jeong-Lim
    • Archives of Pharmacal Research
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    • v.21 no.5
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    • pp.599-609
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    • 1998
  • In search for new antitumor agents, twelve 6-aziridinylbenzimidazole derivatives were synthesized and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia P388 and B16, and human gastric carcinoma SNU-16). From 4-amino-3-nitrotoluene as the starting material, 2-(acetoxymethyl)benzimidazoles (5a-d) were obtained by Phillips reaction. These benzimidazoles were then reacted with Fremy's salt to give a mixture of three 2-(acetoxymethyl) (8a-c) and four 2-(hydroxymethyl)benzimidazole-4,7-diones (9a-d). Addition of these quinones with aziridine afforded 6-aziridinyl-2-(acetoxymethyl) (10a-c) and 6-aziridinyl-2-(hydroxymethyl)benzimidazole-4,7-diones (11a-d). Utilizing 2-(hydroxymethyl)benzimidazole-4,7-diones (9b,d), esters 10d and 13e-h were prepared by the sequential reactions of esterification and addition. The synthesized compounds show potent cytotoxicity against all of three cell lines tested. The cytotoxicities of 10a-d or 11a-d against SNU-16 were wuperior to those of 13e-h, and were equal to or slightly higher than that of mitomycin C. compounds 11a-d were slightly more cytotoxic than 10a-d in all cell lines tested.

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Antitumor activities of hypericin as a protein tyrosine kinase blocker

  • Kil, Kwang-Sup;Yum, Young-Na;Seo, Seung-Hoon;Lee, Kyung-Tae
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.490-496
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    • 1996
  • Naphtodianthrone hypericin produced a potent antitumor activity in vitro against several tumor cells. However, it did not show any cytotoxicity on normal cells such as Macaccus rheus monkey kidney cells (MA-104) and primary cultured rat hepatocytes up to $500{\mu}M$ concentration. Hypericin added to A431 human epidermoid carcinoma cell membrane inhibited the autophosphorylation of the epidermal growth factor (EGF) receptor and the tyrosine phosphorylation of RR-SRC peptide catalyzed by an EGF-receptor. Similarly, treatment of the A431 cells with hypericin inhibited the tyrosine phosphorylation of EGF-dependent endogenous EGF-receptor by western blotting analysis. Hypericin also inhibited the T cell PTK, $P56^{lck}$, in a dose-dependent fashion with an $IC_{50}=5{\mu}M$. The tyrosine phosphorylation, on RR-SRC peptide and EGF-induced receptor autophosphorylation, either in vitro or in intact cells was inhibited by hypericin at the same concentration as that in A431 cell proliferation. These data suggest that hypericin directly inhibits EGF-receptor and $P56^{lck}$ PTK activity in vitro and can mediate such action in vivo.

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Synthesis and in vitro Antitumor Activity of 2-Alkyl, 2-Aryl, and 2-Piperazinyl Benzimidazole-4, 7-dione Derivatives

  • Ahn, Chan-Mug;Tak, Jung-Ae;Choi, Sun-Ju
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.288-301
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    • 2000
  • A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (I6 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

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Influence for Carcinoma Cell and Lymphatic Cell of Acetyl Arsonate (아세틸 아르소네이트의 면역세포와 암세포에 미치는 영향: L1210, Sarcoma 180, MOLT-4 등 사람과 생쥐에 대한 작용비교)

  • Jeong, Yong-Ja;Seong, Yeong-Gi
    • YAKHAK HOEJI
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    • v.40 no.5
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    • pp.599-607
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    • 1996
  • Acetylarsonate was prepared for testing antitumor and immunological effects. It showed cytotoxicity directly on Sarcoma 180. L1210 and MOLT-4 by MTT assay. It did not seemed to trigger the mitosis of human lymphocytes in culture, but that showed the cytotoxicity with higher dose. The rosette formation and spleen weight of mouse which acetylarsonate was administered to for 2 weeks were increased. Furthermore, peripheral helper T- and cytotoxic/suppressor T-lymphocytes were increased in acetylarsonate-injected-mice significantly when it was estimated with simultaneous 2 color analysis using anti Lyt2-FITC and L3T4-PE monoclonal antibody by Flow cytometer.

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Hydrolysable Tannins and Related Compound having Cytotoxic Activity from the Fruits of Terminalia chebula

  • Lee, Seung-Ho;Ryu, Shi-Yong;Choi, Sang-Un;Lee, Chong-Ock;No, Zaesung;Kim, Seong-Kie;Ahn, Jong-Woong
    • Archives of Pharmacal Research
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    • v.18 no.2
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    • pp.118-120
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    • 1995
  • The cytotoxicity-directed fractionation of MeOH extract of Terminalia chebula fruits led to the isolation of three hydrolyzed tannins and a related compound, gallic acid(1), $1,2,3,4,6-penta-O-galloy-{\beta}-_D/-glucopyranose(II)$,. chebulagic acid (III) and chebulinic acid(IV), as active principles. They were shoen to exhibit moderate cytotoxicity against cultured human tumor cell lines including A-549, SK-OV-3, Sk-MEL-2, XF-498 and HCT-15 in vitro.

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