• Title/Summary/Keyword: Antitumor activity activity

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Antineoplastic natural products and the analogues V - Antitumor Activity of Skullcapflavon II

  • Ryu, Sung-Ho;Ahn, Byung-Zun;Pack, Moo-Young
    • Archives of Pharmacal Research
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    • v.8 no.4
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    • pp.253-256
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    • 1985
  • The effect of skullcapflavon II, 5, 2'- dihydroxy-6, 7, 8, 6'-tetramethoxyflavone, on the growth of transplantable L 1210 and sarcoma 180 tumors in mice was studied. Intraperitional treatment of skullcapflavon II cased a significant (T/C = 166%) and a moderate (T/C = 122 %) prolongations of the life spans of ICR and $BDF_{1}$ mice respectively, which had been intraperitioneally inoculated with sarcoma 180 and L 1210 cells. Peritumoral injection of skullacapflavon II on the solid form of sarcoma 180 in mice inhibited the tumor growth strongly (Inhibition rate = 71%).

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Immunomodulatory Effects of Hypocrellin A on MHC-restricted Antigen Processing

  • Park, Sun-Im;Im, Sun-A;Kim, Ki-Hyang;Lee, Chong-Kil
    • IMMUNE NETWORK
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    • v.11 no.6
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    • pp.412-415
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    • 2011
  • Hypocrellin A has gained much attention in recent years due to its light-induced antitumor, antifungal and antiviral activities. Here we report that hypocrellin A exerts immunomodulatory effects on MHC-restricted presentation of antigen. Hypocrellin A inhibited class II-MHC restricted presentation of exogenous antigen, but not class I MHC-restricted presentation of exogenous antigen, in dendritic cells. Hypocrellin A also inhibited the cytosolic pathway of endogenous antigen presentation. However, hypocrellin A did not inhibit the expression of class I and class II MHC molecules on dendritic cells (DCs), the phagocytic activity of DCs, or the $H-2K^b$-restricted presentation of a synthetic peptide, SIINFEKL. These results show that hypocrellin A differentially modulates the MHC-restricted antigen presentation pathways.

Reversal of Doxorubicin-induced Cardiotoxicity by Using Phytotherapy: A Review

  • Hosseini, Azar;Sahebkar, Amirhossein
    • Journal of Pharmacopuncture
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    • v.20 no.4
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    • pp.243-256
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    • 2017
  • Doxorubicin as a chemotherapeutic drug is widely used for the treatment of patients with cancer. However, clinical use of this drug is hampered by its cardiotoxicity, which is manifested as electrocardiographic abnormalities, arrhythmias, irreversible degenerative cardiomyopathy and congestive heart failure. The precise mechanisms underlying the cardiotoxicity of doxorubicin are not clear, but impairment of calcium homeostasis, generation of iron complexes, production of oxygen radicals, mitochondrial dysfunction and cell membrane damage have been suggested as potential etiologic factors. Compounds that can neutralize the toxic effect of doxorubicin on cardiac cells without reducing the drug's antitumor activity are needed. In recent years, numerous studies have shown that herbal medicines and bioactive phytochemicals can serve as effective add-on therapies to reduce the cardiotoxic effects of doxorubicin. This review describes different phytochemicals and herbal products that have been shown to counterbalance doxorubicin-induced cardiotoxicity.

Zerumbone, Sesquiterpene Photochemical from Ginger, Inhibits Angiogenesis

  • Park, Ju-Hyung;Park, Geun Mook;Kim, Jin-Kyung
    • The Korean Journal of Physiology and Pharmacology
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    • v.19 no.4
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    • pp.335-340
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    • 2015
  • Here, we investigated the role of zerumbone, a natural cyclic sesquiterpene of Zingiber zerumbet Smith, on angiogenesis using human umbilical vein endothelial cells (HUVECs). Zerumbone inhibited HUVECs proliferation, migration and tubule formation, as well as angiogenic activity by rat aorta explants. In particular, zerumbone inhibited phosphorylation of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1, which are key regulators of endothelial cell function and angiogenesis. In vivo matrigel plug assay in mice demonstrated significant decrease in vascularization and hemoglobin content in the plugs from zerumbone-treated mice, compared with control mice. Overall, these results suggest that zerumbone inhibits various attributes of angiogenesis, which might contribute to its reported antitumor effects.

In vitro cytotoxicity of Chloromethyl-2-dihydroxyphosphinyl-6, 7-dimethoxy-l,2,3,4-tetra hydroisoquinoline on HL60 cells and apoptotic effet

  • Kim, Kun-Jung;Ju, Sung-Min;Yeom, Kee-Bok;Kim, Dae-Geun;Lee, Chai-Ho;Kim, Won-Sin;Han, Dong-Min;Jeon, Byung-Hun
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2003.10b
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    • pp.115-115
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    • 2003
  • The chloromethyl-2-dihydroxyphosphinyl-6, 7-dimethoxy-1,2,3,4-tetrahydro isoquino- line (CDDT) is a newly synthesized agent which is derivated from 1,2,3,4- Tetrahydroiso- quinoline (TIQ). The TIQs include potent cytotoxic agents that display a range of antitumor activities, antimicrobial activity, and other biological properties. (omitted)

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Sarsasapogenin Increases Melanin Synthesis via Induction of Tyrosinase and Microphthalmia-Associated Transcription Factor Expression in Melan-a Cells

  • Moon, Eun-Jung;Kim, Ae-Jung;Kim, Sun-Yeou
    • Biomolecules & Therapeutics
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    • v.20 no.3
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    • pp.340-345
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    • 2012
  • Sarsasapogenin (SAR) is a steroidal sapogenin that is used as starting material for the industrial synthesis of steroids. It has various pharmacological benefits, such as antitumor and antidepressant activities. Since its effect on melanin biosynthesis has not been reported, we used murine melanocyte melan-a cells to investigate whether SAR influences melanogenesis. In this study, SAR significantly increased the melanin content of the melan-a cells from 1 to 10 ${\mu}M$. Based on an enzymatic activity assay using melan-a cell lysate, SAR had no effect on tyrosinase and DOPAchrome tautomerase activities. It also did not affect the protein expression of tyrosinase-related protein 1 and DOPAchrome tautomerase. However, protein levels of tyrosinase and microphthalmia-associated transcription factor were strongly stimulated by treatment with SAR. Therefore, our reports suggest that SAR treatment may induce melanogenesis through the stimulation of tyrosinase and microphthalmia-associated transcription factor expression in melan-a cells.

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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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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Synthesis and Antitumor Activity of New Anthracycline Analogues

  • Young S. Rho;Kim, Wan Jung;Yu, Dong Jin;Gang, Hyeon Su;Jang, Sun Ryang
    • Bulletin of the Korean Chemical Society
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    • v.22 no.9
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    • pp.963-968
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    • 2001
  • New anthracycline analogues 2-9 as potential anticancer agents have been synthesized from daunomycin (1a) and doxorubicin (1b). Compounds 2 and 6 were prepared by the nucleophilic displacement type esterification of 14-bromodaunomycin (1c) with N-benzoyl-(2R,3S)-phenylisoserine and L-pyroglutamic acid in triethyl-amine, respectively. Compounds 3, 7 and 4, 8 were prepared by the reaction of either daunomycin (1a) or doxorubicin (1b) with one equivalent of the corresponding acids in the presence of EDCI/PP. Compounds 5, 9 were obtained from 1b by reaction with 2.2 equivalents of the corresponding acids in the same manner. The cytotoxic activities of the analogues in comparison with adrimycin on cultured SNU-16 and MCF7 cell were described.

The Reaction of 6,7-Dichloro-5,8-quinoxalinedione with Aromatic and Aliphatic Dinucleophiles and Molecular Modeling Study of Their Intercalation Complexes

  • 유희원;서명은;신계중;박상우
    • Bulletin of the Korean Chemical Society
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    • v.18 no.5
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    • pp.484-488
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    • 1997
  • The angular and planar heterocyclic compounds containing nitrogen, sulfur and oxygen were synthesized by reaction of 6,7-dichloro-5,8-quinoxalinedione with aromatic and aliphatic dinucleophiles. Nucleophilic reactivity was somewhat different between 2,3-dichloro-1,4-naphthoquinone and 6,7-dichloro-5,8-quinolinedione with dinucleophiles. The distribution of electron in heterocycle appeared to contribute to this difference. The intercalation comple of planar heterocyclic compound between GC/GC base pairs showed the optimum intercalation but the intercalation of angular heterocyclic compound was not good. Thus, the planar compound was expected to have antitumor activity.