• Title/Summary/Keyword: HL-60 cells

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Cytotoxic Activity and Quantitative Structure Activity Relationships of Arylpropyl Sulfonamides

  • Hwang, Yu Jin;Park, Sang Min;Yim, Chul Bu;Im, Chaeuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.3
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    • pp.237-243
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    • 2013
  • B13 is a ceramide analogue and apoptosis inducer with potent cytotoxic activity. A series of arylpropyl sulfonamide analogues of B13 were evaluated for their cytotoxicity using MTT assays in prostate cancer PC-3 and leukemia HL-60 cell lines. Some compounds (4, 9, 13, 14, 15, and 20) showed stronger activities than B13 in both tumor cell lines, and compound (15) gave the most potent activity with $IC_{50}$ values of 29.2 and 20.7 ${\mu}M$, for PC-3and HL-60 cells, respectively. Three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed to build highly reliable and predictive CoMSIA models with cross-validated $q^2$ values of 0.816 and 0.702, respectively. Our results suggest that long alkyl chains and a 1R, 2R configuration of the propyl group are important for the cytotoxic activities of arylpropyl sulfonamides. Moreover, the introduction of small hydrophobic groups in the phenyl ring and sulfonamide group could increase biological activity.

Antitumor Effect of Natural Products, Purified Tannin from Plants and Screening of BRM function (천연물에서 단리한 식물정제 탄닌의 항암효과 및 생물학적 반응 조절 물질로서의 기능 검색)

  • Lee, Do-Ik;Cho, Jang-Hyun;Lee, Min-Won
    • YAKHAK HOEJI
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    • v.42 no.4
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    • pp.345-352
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    • 1998
  • Praecoxin A, an ellagitannin, purified from Alnus hirsuta var.microphlla was evaluated on the antitumor activity. Praecoxin A had the significant cytotoxicity to s ix tumor cell lines: human chronic myelogenous leukemia K-562, human promyelocytic leukemia HL-60, mouse leukemia P388, mouse lymphocytic leukemia L-1210, sarcoma-l8O, mouse lymphoma L5178Y except L-1210. And the most sensitive cell line was K-562 ($ED_{50}=2.43{\mu}g/ml$). The $ED_{50} of praecoxin A against HL-60, P388, L-1210, sarcoma7l8O and L5178Y were 6.28, 8.66, 10.00, 7.01, $9.32{\mu}g/ml$, respectively. Praecoxin A showed the increasing effect in life span by 36.8% on the 1st day after treatment of 10mg/kg in mice bearing sarcoma-180 tumor cells (ascitic form) via NCI (National Cancer Institute, U.S.A.) protocol in vivo assay. As a result, praecoxin A is considered to show the antitumor activity.

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Effect of Thesium Chinese Turczaninow Aqua-acupuncture Solution and Astragail Radix Aqua-acupuncture Solution on Promotion/ progression of Carcinogenesis (하고초와 황기 약침액이 발암 진행과정에 미치는 영향)

  • 손윤희;박신화;류준선;조경희;임종국;남경수
    • Journal of Life Science
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    • v.11 no.4
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    • pp.335-339
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    • 2001
  • Cancer chemoprevention refers to the use of natural or synthetic substances to prevent initiational and promotional events that occur during the process of carcinogenesis. Thesium Chinese Turczaninow aqua-acupuncture solution (TCTAS) and Astragli Radix aqua-acupuncture solution (ARAS) were tested as the cancer chemopreventive agents using biochemical markers of carcinogenesis. The effects on the inhibition of phorbol 12- myristate 13-acetate(TPA)-induced free radical formation in HL-60 cells and the inhibition of polyamine metabolism were measured. There is significant inhibition of TAP-induced free radical formation in human leukemic cells with cells with ARAS. Proliferation of Acanthamoeba castellanii was inhibited by TCTAS and ARAS. TCTAS and ARAS positive in these assays may inhibit the carcinogenesis process and is considered promising cancer-preventing agents.

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Effect of Chungjokupye-tang on the Anti-cancer Property (청조구폐탕의 항암효과에 관한 연구)

  • Park Min Chul;Jeong Han Sol;Lee Kwang Gyu
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.17 no.6
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    • pp.1441-1447
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    • 2003
  • The purpose of this research was to investigate the effects of Chungjokupye-tang(CJKPT) on the anti-carcinogenic action. The cell viability of mouse spienocytes and thymocytes were enhanced by the addition of CJKPT. CJKPT were increased of splenic and thymic T lymphocytes, such as T/sub H/ cells were markedly increased by the treatment of CJKPT in vivo. CJKPT treatment induced the apoptotic cell death of Jurkat and HL60 leukemia cells. CJKPT reduced mitochondrial transmembrane potential and increased the expression of ICE, c-myc and p53 gene in Molt-4cells dose dependant manner. These results suggest that CJKPT have an anti-carcinogenic action via immunoregulatory mechanism.