• Title/Summary/Keyword: $P_388$

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Synthesis and Antitumor Activity of 2',3'-Didehydro-3'-Didehydro-3'-deoxy-thymidine and Its Derivative

  • 이봉훈;임미경;신정희;장태식;박장수;강신원
    • Bulletin of the Korean Chemical Society
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    • v.18 no.7
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    • pp.711-714
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    • 1997
  • In an effort to enhance the lipophilicities, thereby, the penetration into the cell membrane and to increase the antitumor activities of modified derivatives of 2',3'-didehydro-3'-deoxythymidine (d4T, 1), derivatives of 1 were designed and synthesized. Starting from thymidine, 1, 2',3'-didehydro-3'-deoxythymidine-5'-phosphate, disodium salt (d4T-p, 7), and two nicotinate esters of 1; 2',3'-didehydro-3'-deoxy-5'-O-(3-pyridinylcarbonyl)thymidine (d4T-NA, 5) and 2',3'-didehydro-3'-deoxy-5'-phosphoryl-O-(3-pyridinylcarbonyl)thymidine (d4T-p-NA, 8) were synthesized. The lipophilicities of the synthesized compounds were measured by P-values and antitumor activities of those were estimated against mouse leukemia P388, murine mammary carcinoma FM3A, and human histiocytic lymphoma U937 tumor cells in vitro. Although the lipophilicities of the nicotinate esters, 5 and 8 were increased 2.75- and 9.71-fold relative to that of 1 and 7, respectively, the synthesized compounds, 1, 5, 7, and 8 were found to be inactive against P388 and FM3A cells except weak antitumor activity against U937 cell.

Meliglabrin, A New Flavonol Derivative from the leaves of Melicope glabra (Blume) T.G. Hartley

  • Saputri, Ratih Dewi;Tjahjandarie, Tjitjik Srie;Tanjung, Mulyadi
    • Natural Product Sciences
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    • v.24 no.3
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    • pp.155-158
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    • 2018
  • A new flavonol derivative, meliglabrin (1) along with three known flavonols, ternatin (2), meliternatin (3), and 5,4'-dihydroxy-3,7,3'-trimethoxyflavon (4) were isolated from the leaves of Melicope glabra (Blume) T.G. Hartley. Their structures were determined using extensive spectroscopic methods, including UV, IR, HRESIMS, 1D and 2D NMR. Compounds 1 - 4 were evaluated for their cytotoxicity against murine leukemia P-388 cells, compound 4 showed moderate activity.

Synthesis and Antitumor Activity of Pt(ll) Complexes Containing Ethylenediamine (에칠렌디아민을 배위자로 한 백금(II) 착체의 합성과 항암효과)

  • Lee, Kyung-Tae;Jung, Jee-Chang;Roh, Young-Soo
    • Journal of Pharmaceutical Investigation
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    • v.24 no.4
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    • pp.245-250
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    • 1994
  • An attempt was made to develop new water-soluble antitumor Pt(ll) complexes containing ethylenediamine, and their structures were determined by infrared spectroscopy, $^{13}C$ nuclear magnetic resonance and elemental analysis. Their antitumor activities in vitro against L-1210, p-388 leukemia cells and M-14 melanoma cells were investigated and acceptable antitumor activity was found as compared with cisplatin.

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Isolation and Evaluation of an Antitumor Constituent from Pyrolae Herba (녹수초의 항암활성물질의 분리 및 항암력 평가)

  • Bae, Ki-Hwan;Kim, Hwan-Mook;Lee, Sang-Myung
    • YAKHAK HOEJI
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    • v.40 no.2
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    • pp.225-229
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    • 1996
  • The cytotoixic effect of Pylorae Herba (Pyrola japonica Klenze) against L1210 and K-562 cells was studied in vitro. The methanolic extract of Pylorae Radix was add ed to the culture of L1210 cells and K-562 cells for the cytotoxic activity and the ED50 values of hexane, ethylacetate, buthanol and water fractions from methanolic extract were determined using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazoliumbromide) assay. The active constituent isolated by bioassay guided fractionation followed by purification gave rise to a yellow needle crystal and was clarified to be chimaphilline by the comparison with the published data. The average life spans with it were not prolonged significantly on tumor growth in hybrid female mouse (BDF1-KIST) inoculated subcutaneously with P388 cells.

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Screening of Antitumor Activity from the Crude Drugs in Korea (국내 생약자원으로부터의 항종양효과의 검색)

  • Ryeom, Kon;Choi, Byung-Don
    • Korean Journal of Pharmacognosy
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    • v.31 no.1
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    • pp.16-22
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    • 2000
  • These studies were designed to determine the potential cytotoxic activity of MeOH extracts of 65 crude drugs against leukemia L1210 and $P388D_1$, cell line in vitro, of which 25 samples were selected. The n-BuOH extracts of 25 samples were measured using the same method and nine were selected. These samples were measured for the potential antitumor activity against $P388D_1$, for life span in vivo, and against sarcoma 180 for tumor weight. On the basis of results, Notoginseng Radix, Anemarrhenae Rhizoma, Albizziae Cortex, Portulacae Herba, Bupleuri Radix were evaluated the effective plant on the antitumor activity. In addition, the mixture of Notoginseng Radix and Albizziae Cortex was evaluated to enhance the antitumor activity in vivo.

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Biological Activity of Water Extract from Atractylodes macrocephala

  • Chun Ju Yeon;Lee Hyun Ok;Baek Seung Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.2
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    • pp.596-598
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    • 2004
  • The effects of water extract from Atractylodes macrocephala Koidz on biological activity were investigated. The crude water extract of A. macrocephala inhibited the growth of the dermatophytic fungus Trichophyton mentagrophytes ATCC 28185, (3 mm inhibition zone at 300 ㎍/disc). However, it did not show growth inhibition activity against Sreptococcus mutans JC-2 (MIC >1,000 ㎍/mL). This extract was cytotoxic to P388 murine leukaemia cells ATCC CCL 46 P388D1, (IC/sub 50/ 62.24 ㎍/mL at 150 ㎍/disc). These results suggest that water extract of A. macrocephala possesses antitumoral, and antimicrobial activities.

Isolation and Biological Activity of Sesquiterpene Lactone

  • Kim Myung-Ju;Oh Hyun-Ju;Baek Seung-Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.19 no.5
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    • pp.1375-1378
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    • 2005
  • Sequiterpene lactone (1) has determined by spectroscopic analysis. This compound (1) inhibited the growth of the dermatophytic fungus Trichophyton mentagrophytes (ATCC 28185, 2 mm zone at $15{\mu}g/disk$), cytotoxic to murine leukaemia cell lines ATCC CCL 46 P388Dl, ($IC_{50}$ 1,125 ng/mL at $7.5{\mu}g/disk$) and BSC monkey kidney cell lines (100% of well at $15{\mu}g/disk$).

Synthesis and Biological Activity of Geranyloxy Compounds

  • Oh, Hyun-Ju;Oh, In-Kio;Na, Young-Soon;Kim, Myung-Ju;Baek, Seung-Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.19 no.3
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    • pp.792-796
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    • 2005
  • Disk assays on the compounds (10 and 12) showed both to have antifungal activity against the dermatophytic fungus Trichophyton mentagrophytes ATCC 28185, (1 and 3 mm inhibition zones at $60\;{\mu}g/disc$), but not against the Gram-positive bacterium B. subtilis or the Gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa or fungi Cladosporium resinae and Candida albicans. However, the compound (13) did not show against antifungal activity. The geranyloxy compounds (10, 12, and 13) were cytotoxic to P388 murine leukaemia cells ATCC CCL 46 P388D1, ($IC_50$ >6,250 ng/mL at $7.5\;{\mu}g/disc$). These results suggest that The geranyloxy compounds possesses antimicrobial and antitumor activities.

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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Differential Antitumor Activities of the Proteoglycans from the Mycelium of Lentinus Lepideus (잣버섯 균사체로부터 분리한 단백다당체의 암종에따른 선별적 항암작용)

  • Jin, Mi-Rim;Jung, Kyu-Sun;Kim, Byong-Kak
    • YAKHAK HOEJI
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    • v.42 no.5
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    • pp.480-486
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    • 1998
  • Many antitumor and immune modulating components have been isolated from fungal extracts. In this study, the authors isolated the proteoglycans from cultured mycelia of Lentin us lepideus, including especially the acidic polysaccharide fraction, named lepidan. It was obtained by extraction with hot water followed by purification using DEAE cellulose anion exchange. To elucidate antitumor effects against different type of tumor, the proteoglycans were tested on sarcoma 180, C3H MCA clone 16 and P388 leukemia in vivo. Lepidan showed 58.3% of tumor inhibition against solid form of sarcoma 180 and 58.6% against MCA clone 16. But lepidan did not affect life span of mice against P388 leukemia. Also when Lepidan was applicated to MTT assay, it did not show any direct cytotoxicity against various tumor cells in vitro.

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