• Title/Summary/Keyword: Cytotoxic agents

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Development of Anticancer Agents from Korean Medicinal Plants (Part 8). - Cytotoxic Activity of Taraxaci Herba Extract against Human Skin Melanoma Cells - (한국산 생약으로부터 항암물질의 개발(제 8보) - 포공령 추출물이 인체 피부흑색종세포에 미치는 세포독성작용 -)

  • Oh, In-Kio;Yoo, Eun-Ah;Han, Du-Seok;Kang, Kil-Ung;Baek, Seung-Hwa
    • Korean Journal of Pharmacognosy
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    • v.29 no.3
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    • pp.198-203
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    • 1998
  • In the present study, we have evaluated cytotoxic effects of Taraxaci herba extract on human skin melanoma cells. The light microscopic study showed morphological changes of the treated cells. Disruptions in cell organelles were determined by calorimetric methods: MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide), NR (Neutral red) and SRB (Sulforhodamine B protein) assay. These results suggest that Taraxaci herba retains a potential antitumor activity.

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Induction of Apoptosis with Moringa oleifera Fruits in HCT116 Human Colon Cancer Cells Via Intrinsic Pathway

  • Guon, Tae-Eun;Chung, Ha Sook
    • Natural Product Sciences
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    • v.23 no.4
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    • pp.227-234
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    • 2017
  • Moringa oleifera Lam (M. oleifera, Moringaceae) is a tree of the Moringaceae family that can reach a height of between 5 and 10 m. The current paper presents cytotoxic effect of M. oleifera fruits and its flavonoids 1 and 2. The viability of HCT116 human colon cancer cells were 38.5% reduced by $150{\mu}g/mL$ of ethanolic extracts in a concentration-dependent manner; in addition, we observed the apoptotic features of cell shrinkage and decreased cell size. Bcl-2 family proteins were regulated as determined by Western blotting analysis, suggesting that M. oleifera fruits and their flavonoids 1 and 2 induced apoptosis through an intrinsic pathway. Based on our findings, 70% ethanolic extracts of M. oleifera fruits and flavonoids 1 and 2 might be useful as cytotoxic agents in colorectal cancer therapy.

DISCOVERY OF NEW ANTITUMOR AGENTS FROM MEDICINAL PLANTS (항종양활성천연약물연구의 전망)

  • 히데치
    • Korean Journal of Plant Resources
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    • v.5 no.2
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    • pp.73-84
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    • 1992
  • Many types of compounds have been isolated from higher plants till now, that is, alkaloids, terpenes, lignans, steroids and so on. One of them, named as RA series Cyclic hexapeptides isolated from Rubia akane and R. cordijofia also have strong antineoplastic activity against various types of tumors. Till now 10 kinds ofRA series compounds were isolated and named as RA - I, II, III, IV, V, VI, VII, VIII, IX and X. Moreover,monogl-ucoside of RA - V newly Isolated from same plant. Many kinds of derivatives including natural RAcompounds were tested for QSAR, and one of them, RA - VII was screened up as a most suitable substance asan antitumor agent. RA - VII(=RA-700) has strong cytotoxic activity against KB cells, P388 Iymphocyticleukemia and MM2 mammary carcinoma cells. RA - VII has been under investigation for Phase I clinical trials.

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Cytotoxic Activity of Several Extracts from Chinese Medicinal Plants (중국산 천연자원의 세포독성 검색)

  • Yoo, Young-Jin;Lee, You-Hui;Kim, Young-Sook;Park, Jong-Dae;Kim, Shin-Il
    • Korean Journal of Pharmacognosy
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    • v.28 no.4
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    • pp.192-197
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    • 1997
  • As a part of searching for new antitumor agents from natural products, 94 kinds of Chinese plants were extracted with petroleum ether/ether (1:1), ethyl acetate and methanol, successively and their cytotoxicities were evaluated against A549 (human lung carcinoma) cell line. Among them, six kinds of ether extracts, seven kinds of ethyl acetate extracts and one kind of methanol extracts showed significant cytotoxic activities (above 70% inhibition) at a concentration of $50\;{\mu}g/ml$. These results surest that they may be involved in natural sources with possible anticancer activities.

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Cytotoxicity of Cratoxylum Formosum Subsp. Pruniflorum Gogel Extracts in Oral Cancer Cell Lines

  • Promraksa, Bundit;Daduang, Jureerut;Chaiyarit, Ponlatham;Tavichakorntrakool, Ratree;Khampitak, Tueanjit;Rattanata, Narintorn;Tangrassameeprasert, Roongpet;Boonsiri, Patcharee
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.16
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    • pp.7155-7159
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    • 2015
  • Background: Oral cancer is a health problem in Thailand. Cratoxylum formosum subsp. pruniflorum Gogel (Teawdang), normally consumed in northeast Thailand, has proven cytotoxic to cervical cancer cell lines including HeLa, SiHa and C-33A. Recently, Asian oral cancer cell lines, ORL-48 and ORL-136, were established. Therefore, we aimed to study cytotoxicity of Teawdang in these. Total phenolic (TPC) and flavonoid content (TFC), and antioxidant activity of Teawdang were also determined. Materials and Methods: Teawdang was purchased from Khon Kaen market during June-October 2013. Hexane (CHE), ethyl acetate (CEE) and methanol (CME) extracts of its edible part were analyzed for TPC by the folin-ciocalteau method and for TFC by an aluminium colorimetric method. Antioxidant activity and cytotoxicity in normal Vero cells and oral cancer cells were investigated. Cell viability was assessed using 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT) assays. Results: CME and CEE had higher TPC and TFC and antioxidant activity than CHE. Both CME and CEE, at $200{\mu}g$ dry wt/mL, were cytotoxic to the studied oral cancer cell lines. However, CME was cytotoxic to Vero cells whereas CEE was not. Compared to Vero cells, CEE significantly inhibited ORL-48 and ORL-136 growth (p=0.03 and p=0.02, respectively). Conclusions: CEE exhibited cytotoxic effects on the studied oral cancer cell lines but not normal Vero cells. The bioactive compounds in CEE should be further purified and elucidated for their mechanisms of action for development as anticancer agents.

Synthesis of Hydrazone Derivatives of 4-(2-Chloroethyl) semicarbazide : A New Class of Cytotoxic Agents (4-(2-Chloroethyl) semicarbazide의 히드라존 유도체 합성:새로운 종류의 세포독성요법제)

  • El-Sabbagh, O.I.;El-Sadek, M.E.;Aboukull, M.E.;Shallal, H.M.
    • Journal of the Korean Chemical Society
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    • v.53 no.1
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    • pp.34-41
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    • 2009
  • A new series of hydrazone derivatives were synthesized from 4-(2-chloroethyl)semicarbazide and their antiproliferative activity against human brain (U251) and liver (Hepg2) carcinoma cell lines were evaluated. The hydrazone compounds are benzaldehyde (2a-2g), acetophenone (3a-3f), and 3-formylindole derivatives (4a-4d). Among the acetophenone derivatives, 3e (p-methoxy substituted) and 3f (p-nitro substituted) showed the highest cytotoxic activity against Hepg2 cell line (I$C_{50}$ = 6 and 8 $\mu$g/ml, respectively). Among the 3-formylindole derivatives, 4a (hydrazone of 3-formylindole itself) showed a pronounced cytotoxic activity against both U251 (I$C_{50}$ = 21 $\mu$g/ml) and Hepg2 (I$C_{50}$ = 7 $\mu$g/ml).

Synthesis and In Vitro Cytotoxicity of 4-Alkyl- or 4-Arylaminosubstituted Cyclopenta[c]quinoline Derivatives

  • Lee, Hee-soon;Lee, Jee-man;Yang, Sung-Il
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.385-389
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    • 2001
  • Twelve 4-substituted cyclopenta[c]quinoline derivatives were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, MD-MB-468 and T-47D). The compounds 6c and 6e bearing p-anisidine and pyrrolidine side chain were more active than the others.

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Synthesis and In Vitro Cytotoxicity of 1,3-Dioxoindan-2-Carboxylic Acid Arylamides

  • Jung, Jae-Kyung;Ryu, Jin-Hyeong;Yang, Sung-Il;Cho, Jung-Sook;Lee , Hee-Soon
    • Archives of Pharmacal Research
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    • v.27 no.10
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    • pp.997-1000
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    • 2004
  • A series of 1,3-dioxoindan-2-carboxylic acid arylamides were synthesized and evaluated for in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, MD-MB-468 and T- 47D). The most active was compound 3e (1.2 ${\mu}M$ against SK-OV-3 cell line) bearing a 4- methyl substituent.

Pharmacodynamics of anticancer activity of tirapazamine and paclitaxel against human NSCLC

  • Park, Jong-Kook;Kang, Jin-Hyoung;Kuh, Hyo-Jeong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.228.1-228.1
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    • 2002
  • Hypoxia in solid tumors is known to contribute to intrinsic chemoresistance. Tirapazamine(TPZ). a hypoxia-selective cytotoxin. showed synergism with radiation or cytotoxic agents. Paclitaxel(PTX) is a highly active anti-cancer agent against Non small cell lung cancer(NSCLC), however. due to poor penetration into central hypoxic region of tumor tissue. combination with TPZ has been suggested to enhance its efficacy. (omitted)

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Novel Benzoylurea Derivatives as Potential Antitumor Agents; Synthesis, Activities and Structure-Activity Relationships

  • Hwang, Ki-Jun;Park, Kyung-Ho;Lee, Chong-Ock;Kim, Beom-Tae
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.781-785
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    • 2002
  • A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.