• 제목/요약/키워드: .Antitumor activity

검색결과 1,046건 처리시간 0.035초

The 3-D QSAR study of antitumor arylsulfonylimidazolidinone derivatives by CoMFA and COMSIA

  • ParkChoo, Hea-Young;Choi, Su-Young;Jung, Sang-Hun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.357.1-357.1
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    • 2002
  • Three-dimensional quantitative activity relationship (3D-QSAR) study for a series of arylsulfonylimidazolidinone derivatives with antitumor activity was conducted using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices anaysis (CoMSIA). The in vitro cytotoxicity against human lung carcinoma (A549) exhibited a strong correlation with steric and electrostatic factors of the molecules. (omitted)

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Molecular modeling study of indeno[1,2-c]isoquinolines and 3-arylisoquinolines using CoMFA

  • Kang, Sung-Kyung;Manhk, Le-Quynh;Cho, Won-Jea
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.171.1-171.1
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    • 2003
  • ·The potent antitumor activities of 3-arylisoquinolines promoted us to explore the structure-activity relationship of these compounds. A series of 3-arylisoquinoline derivatives were evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). For the next stage, we decided to prepare the constrained form of 3-arylisoquinolines as indeno[1,2-c]isoquinolines. As a result, diverse spectrum against human tumor cell lines was obtained. In order to study structure-activity relationship (SAT) of these compounds the comparative molecular field analysis (CoMFA) was carried out. (omitted)

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Total Synthesis of New Apicidin Derivatives as Potent Antitumor Agents

  • kim, hyung-Kyo;Jin, Cheng-Hua;Han, Jeong-Whan;Lee, Hyang-Woo;Lee, Yin-Won;Zee, Ok-Pyo;Jung, Young-Hoon
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.188.1-188.1
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    • 2003
  • The antiparasitic agent apicidin, which was recently isolated from cultures of Fusarium Pallidoroseum, belongs to a rare group of cyclictetrapeptide fungal metabolites. Apicidin inhibits protozoal HDAC and is orally active against Plasmodium berghei malaria in mice. The biological activity of apicidin appears to be attributable to inhibition of apicomplexan HDAC at low nanomolar concentrations. In the present, we have worked about the synthesis of new apicidin derivatives and discovered that apicidin and some derivatives have mild antitumor activity. (omiited)

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DESIGN, SYNTHESIS AND IN VITRO EVALUATION OF APIO ANALOGUE OF NEPLANOCIN A

  • Moon, Hyung-Ryong;Lee, Jeong-Ah;Yoo, Byul-Nae;Shin, Dae-Hong;Jeong, Lak-Shin
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.233.2-233.2
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    • 2002
  • Apio nucleosides whose 4'-hydroxymethyl group moves to 3'-position exhibit interesting biological activity such as antitumor or antiviral activity. On the other hand. neplanocin A is the representative of the carbocyclic nucleosides and has been recognized as a potent antitumor and antiviral agent. Based on these findings. it was of great interest to design apio neplanocia A which combined the properties of apio nucleosides and neplanocin A. (omitted)

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Synthesis of 2,6-Diaromatic Substituted Pyridine Derivatives and Their Antitumor Activities

  • Moon, Yoon-Soo;Lim, Hyun-Tae;Zhao, Long-Xuan;Basnet-Arjun;Lee, Eung-Seok
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.345.1-345.1
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    • 2002
  • ${\alpha}$-terthienyl the first isolated from natural products shows potent antitumor activity, which encouraged us to study terpyridine and its biological properties. Terpyridine has also been reported as having carcinogenicity, and it's erivatives showed high cytotoxic activities against several human cancer cell lines and topoisomerase I inhibitory ctivity. Mannich free base from condensation reaction was allowed to react with pyridinum salts to give activity. (omitted)

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Studies on Constituents of the Higher Fungi of Korea (XLVI) -Antitumor Components Extracted from the Cultured Mycelia of Lyophyllum decastes-

  • Kim, Hye-Ryoung;Shim, Mi-Ja;Kim, Jung-Woo;Kim, Ha-Won;Lee, Chong-Ock;Choi, Eung-Chil;Kim, Byong-Kak
    • 생약학회지
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    • 제15권2호
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    • pp.61-73
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    • 1984
  • To investigate antitumor component of Lyophyllum decastes, the aqueous extract of its shake-cultured mycelia was subjected to antitumor test against sarcoma 180 cells implanted in ICR mice. The extract showed an inhibition ratio of 65.4% and was found to consist of a polysaccharide moiety and a protein moiety. After purification with DEAE-Sephadex A-50 ion exchange chromatography, Fraction D showed the highest inhibition ratio of 75.7%. The antitumor constituent was examined for immunoaccelerating activity and was found to increase macrophage accumulation in the peritoneal cavity and plaque forming cells of the spleen cells. It was named lyophyllan after the genus name.

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키틴 ${\cdot}$키토산 및 그 올리고당의 면역작용에 의한 항종양 활성 (Antitumor Activities by lmmunological Function of Chitin, Chitosan and Their Oligosaccharides)

  • 전유진;김세권
    • 생명과학회지
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    • 제7권2호
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    • pp.149-159
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    • 1997
  • Chitin, a linked polysaccharide composed of 2-acetamido-2-deoxy-$\beta$-D-glucopytanose residues, is distributed widely in nature. It has been utilized on various application field due to the development of chitin derivatives such as chitosan, partial deacetylated chitin, carboxylmethyl chitin, sulfated chitin, and so on. Chitin and chitosan have been recently interested in antitumor and antimicrobial activities, because of a powerful tumor inhibitory effect against experimental mouse tumors. Especially, the oligosaccharides obtained by partial degradation of them exhibited a remarkable antitumor effect against sarcoma 180, MM 48 and Meth Asolid tumors and antimetastatic effect against Lewis lung carcinoma in mice. This review describes on antitumor effects of chitin, chitosan and their oligosaccharides by their mechanism of action involving enhancement of immunological system.

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젓갈에서 분리한 Bacillus subtilis SW-1의 항암활성 (Antitumor activity of Bacillus subtilis SW-1 isolated from Jeotgal)

  • 박종기;조용운;최영우;정영기;갈상완
    • 생명과학회지
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    • 제14권5호
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    • pp.815-820
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    • 2004
  • 본 연구에서 미생물유래의 종양 예방 및 억제제 개발을 목적으로 우리나라 전통 발효식품인 젓갈에서 항암 활성이 우수한 미생물을 분리, 동정 하였다. 젓갈로부터 항암물질을 생산하는 균주 SW-1을 분리하여 형태학적, 생리학적 특성을 검토한 결과, 본 균주는 Bacillus subtillis SW-1으로 동정되었다. 본 균주로부터 항암물질은 실험에 사용한 두가지의 암세포에 강한 활성을 나타내었다. 그 중에서 폐암 세포인 A549에 가장 강한 활성을 나타내었다. 항암물질 생산을 위한 최적 배양조건을 검토한 결과, 3.0% soluble starch, 1.0% yeast extract 였다. 무기염의 경우는 활성에는 그다지 영향을 미치지 않았다. 배지의 초기 pH 및 배양온도에 따른 항암물질의 생산성을 검토한 결과 초기 pH 5.0배양온도 3$0^{\circ}C$에서 25시 간배양 했을 때 최대 활성을 보였다. Chromosomal DNA단편화 실험에서 Bacillus subtilis SW-1의 배양상등액을 처리했을 때 DNA가 사닥다리모양으로 분해되는 Apoptosis(계획된 세포죽임)를 일으키는 것으로 확인되었다. 이 미생물이 생성하는 물질을 현재 HPLC, GC등을 이용하여 분리 중에 있으며 현재까지의 결과로는 당 중합체 인 것으로 분석된다.

Cytotoxic and Apoptotic Activites of Echinomycin Derivative (Echinomycin-7) on P388 Murine Leukemia Cells

  • Jeon, Hyang;Kim, Sung-Su;Kim, Yoon-Suk;Park, Yil-Sung;Kim, Yong-Hae;Choi, Sun-Ju;Kim, Soo-Kie;Kim, Tae-Ue
    • BMB Reports
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    • 제31권6호
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    • pp.560-564
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    • 1998
  • Echinomycin-7 is an echinomycin derivative, Smethylated sulfonium perchlorate of echinomycin. We studied the in vitro cytotoxicity and in vivo antitumor activity of echinomycin-7 against P388 leukemia cells and compared the results with echinomycin. With respect to the cytotoxic effects, echinomycin-7 had cell line-dependent $IC_{50}$ values while echinomycin had similar values to several tumor cell lines. Also, in vivo antitumor activities were observed in tumor-bearing mice treated with both agents, which showed that echinomycin-7 had a broad therapeutic dose range. We also observed the apoptosis on leukemia cells treated with echinomycin-7 which exihibited the ladder pattern of DNA on electrophoresis. In addition to apoptosis, echinomycin-7 arrested $G_1/S$ phases of the cell cycle at the same time. We then examined the signaling pathway of echinomycin-7-induced apoptosis and showed that ERK of the MAP kinase family was activated and translocated into the nucleus by echinomycin-7 stimulation. This study suggests that echinomycin-7 acts as an antitumor agent through in vitro cytotoxicity and has in vivo antitumor activity against leukemia cells, and that the echinomycin-7- induced apoptosis might involve signal transduction via MAP kinases.

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Effects of the Antitumor Component, F-D-P, Isolated from Elfvingia applanata on the Immune Response

  • Kim, Young-So;Ryu, Ku-Hyun;Mo, Young-Keun;Lee, Chong-Kil;Han, Seong-Sun
    • 생약학회지
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    • 제25권4호통권99호
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    • pp.348-355
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    • 1994
  • An antitumor component, F-D-P, was purified from the hot water extract of the carpophores of Elfvingia applanata by precipitation with ethanol, dialysis, and passage through a column of DEAE-cellulose ion exchange. F-D-P inhibited the growth of Sarcoma 180 in mice showing the tumor inhibition ratio of 88.3% in doses of 20 mg/kg for ten days. Chemical analysis of F-D-P showed that it was composed of polysaccharide(65.3%) and protein(6.5%0, and that the monosaccharides consisting of the polysaccharide was glucose(89.1%) and mannose(10.9%). The immunomodulatory activities of F-D-P were explored by determining its effect on the proliferation of the whole and subpopulations of lymphocytes, and on the generation of natural killer(NK) cell activity in vitro. F-D-P was mitogenic to total lymphocytes and B cells, but not to purified T cells, even in the presence of accessory cells. F-D-P did not increase NK cell activity when added to cultures of resting lymphocytes. From these results, it is clear that F-D-P modulates primarily the humoral immune responeses.

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