• Title/Summary/Keyword: Antitumor action

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Free Radical Scavenging Activities of Chitosan Oligosaccharides Produced by Bioreactor

  • Park, Pyo-Jam;Byun, Hee-Guk;Kim, Se-Kwon
    • Proceedings of the Korean Society of Fisheries Technology Conference
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    • 2001.10a
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    • pp.241-242
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    • 2001
  • Chitosan, a deacetylated derivative of chitin, is one of the abundant resources, and its biological properties such as antibactierial activity, hypocholesterolemic activity, and hypertensive action are remarked. However, increasing attention has recently been yen to converting chitosan to its oligosaccharides because they possess various functional properties like antitumor activity, immune-enhancing effects, enhancing protective effects against infection with some pathogens in mice, antifungal activity, and antimicrobial activity (Jeon et al., 2001). (omitted)

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Molecular Mechanisms of Casticin Action: an Update on its Antitumor Functions

  • Rasul, Azhar;Zhao, Bin-Ji;Liu, Jun;Liu, Bao;Sun, Jia-Xin;Li, Jiang;Li, Xiao-Meng
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.21
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    • pp.9049-9058
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    • 2014
  • Casticin (3', 5-dihydroxy-3, 4', 6, 7-tetramethoxyflavone) is an active compound isolated from roots, stems, leaves, fruits and seeds of a variety of plants. It is well known for its pharmacological properties and has been utilized as an anti-hyperprolactinemia, anti-tumor, anti-inflammatory, neuroprotetective, analgesic and immunomodulatory agent. Recently, the anticancer activity of casticin has been extensively investigated. The resulkts showed that it exerts protective potential by targeting apoptosis, considered important for cancer therapies. In this article, our aim was to review the pharmacological and therapeutic applications of casticin with specific emphasis on its anticancer functions and related molecular mechanisms. Chemotherapeutic effects are dependent on multiple molecular pathways, which may provide a new perspective of casticin as a candidate anti-neoplastic drug. This review suggests that additional studies and preclinical trials are required to determine specific intracellular sites of action and derivative targets in order to fully understand the mechanisms of its antitumor activity and validate this compound as a medicinal agent for the prevention and treatment of various cancers.

Marine Sponges as a Drug Treasure

  • Anjum, Komal;Abbas, Syed Qamar;Shah, Sayed Asmat Ali;Akhter, Najeeb;Batool, Sundas;Hassan, Syed Shams ul
    • Biomolecules & Therapeutics
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    • v.24 no.4
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    • pp.347-362
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    • 2016
  • Marine sponges have been considered as a drug treasure house with respect to great potential regarding their secondary metabolites. Most of the studies have been conducted on sponge's derived compounds to examine its pharmacological properties. Such compounds proved to have antibacterial, antiviral, antifungal, antimalarial, antitumor, immunosuppressive, and cardiovascular activity. Although, the mode of action of many compounds by which they interfere with human pathogenesis have not been clear till now, in this review not only the capability of the medicinal substances have been examined in vitro and in vivo against serious pathogenic microbes but, the mode of actions of medicinal compounds were explained with diagrammatic illustrations. This knowledge is one of the basic components to be known especially for transforming medicinal molecules to medicines. Sponges produce a different kind of chemical substances with numerous carbon skeletons, which have been found to be the main component interfering with human pathogenesis at different sites. The fact that different diseases have the capability to fight at different sites inside the body can increase the chances to produce targeted medicines.

Inhibitive Effect of KH against Toxicity Induced by 5-Flurouracil(FU) (화학요법제 5-flurouracil의 조혈 및 면역독성 억제를 위한 조성물 개발 연구)

  • Yang, Dong-Sik;Hong, Min-Young;Sung, Hyun-Jea;Yoon, Yoo-Sik
    • Korean Journal of Oriental Medicine
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    • v.8 no.2 s.9
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    • pp.109-119
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    • 2002
  • The objective on this study was to investigate effect of KH, which was composed of 9 kinds of oriental herbs tonifing the blood, against toxicity of 5-flurouracil(FU) through animal study. Reduction of WBC and platelet after treating S-FU was significantly recovered by KH. KH also rehabilitated immune gene expression of interleukin-2(IL2) and $Interferon-{\gamma}\;(IFN-{\gamma})$ by RT-PCR. In addition, in situ hybridization of spleen showed that KH treatment increased mRNA expression of IL2. In addition to the immune action, antitumor activity on 5-FU was not affected by KH treatment. In conclusion, our study demonstrated that KH alleviated damage of hematopoiesis system induced by f-FU without toss of antitumor activity.

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Antitumor activities of hypericin as a protein tyrosine kinase blocker

  • Kil, Kwang-Sup;Yum, Young-Na;Seo, Seung-Hoon;Lee, Kyung-Tae
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.490-496
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    • 1996
  • Naphtodianthrone hypericin produced a potent antitumor activity in vitro against several tumor cells. However, it did not show any cytotoxicity on normal cells such as Macaccus rheus monkey kidney cells (MA-104) and primary cultured rat hepatocytes up to $500{\mu}M$ concentration. Hypericin added to A431 human epidermoid carcinoma cell membrane inhibited the autophosphorylation of the epidermal growth factor (EGF) receptor and the tyrosine phosphorylation of RR-SRC peptide catalyzed by an EGF-receptor. Similarly, treatment of the A431 cells with hypericin inhibited the tyrosine phosphorylation of EGF-dependent endogenous EGF-receptor by western blotting analysis. Hypericin also inhibited the T cell PTK, $P56^{lck}$, in a dose-dependent fashion with an $IC_{50}=5{\mu}M$. The tyrosine phosphorylation, on RR-SRC peptide and EGF-induced receptor autophosphorylation, either in vitro or in intact cells was inhibited by hypericin at the same concentration as that in A431 cell proliferation. These data suggest that hypericin directly inhibits EGF-receptor and $P56^{lck}$ PTK activity in vitro and can mediate such action in vivo.

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Modulation of Cytotoxicity by Nitric Oxide Donors during Treatment of Glioma with Anticancer Drugs

  • Park, Jeong-Jae;Kang, Jong-Sool;Lee, Hyun-Sung;Lee, Jong-Soo;Lee, Young-Ha;Youm, Jin-Young
    • Journal of Korean Neurosurgical Society
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    • v.38 no.5
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    • pp.366-374
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    • 2005
  • Objective : Nitric oxide[NO] is implicated in a wide range of biological processes in tumors and is produced in glioma. To investigate the role of NO and its interaction with the tumoricidal effects of anticancer drugs, we study the antitumor activities of NO donors, with or without anticancer drugs, in human glioma cell lines. Methods : U87MG and U373MG cells were treated with the NO donors sodium nitroprusside[SNP] and S-nitroso-N-acetylpenicillamine[SNAP], alone or in combination with the anticancer drugs 1,3-bis[2-chloroethyl]-1-nitrosourea[BCNU] and cisplatin. Cell viability, cell proliferation, DNA fragmentation, nitrite level, and the expression of Bcl-2 and Bax were determined. Results : NO was markedly increased after treatment with SNP or SNAP; however, the addition of the anticancer drugs did not significantly affect NO production NO donors or anticancer drugs reduced glioma cell viability and, in combination, acted synergistically to further decrease cell viability in a dose- and time-dependent manner. Cell proliferation was inhibited and apoptosis were enhanced by combined treatment. Bax expression was increased by combined treatment, whereas Bcl-2 expression was reduced. The antitumor cytotoxicity of NO donors and anticancer drugs differed according to cell type. Conclusion : BCNU or cisplatin can inhibit cell viability and proliferation of glioma cells and can induce apoptosis. These effects are further enhanced by the addition of a NO donor which modulates the antitumor cytotoxicity of chemotherapy depending on cell type. Further biological, chemical, and toxicological studies of NO are required to clarify its mechanism of action in glioma.

Radical Intermediate Generation and Cell Cycle Arrest by an Aqueous Extract of Thunbergia Laurifolia Linn. in Human Breast Cancer Cells

  • Jetawattana, Suwimol;Boonsirichai, Kanokporn;Charoen, Savapong;Martin, Sean M
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.10
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    • pp.4357-4361
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    • 2015
  • Thunbergia Laurifolia Linn. (TL) is one of the most familiar plants in Thai traditional medicine that is used to treat various conditions, including cancer. However, the antitumor activity of TL or its constituents has never been reported at the molecular level to support the folklore claim. The present study was designed to investigate the antitumor effect of an aqueous extract of TL in human breast cancer cells and the possible mechanism(s) of action. An aqueous crude extract was prepared from dried leaves of TL. Folin-Ciocalteu colorimetric assays were used to determine the total phenolic content. Antiproliferative and cell cycle effects were evaluated in human breast adenocarcinoma MCF-7 cells by MTT reduction assay, cell growth inhibition, clonogenic cell survival, and flow cytometric analysis. Free radical generation by the extracts was detected using electron paramagnetic resonance spectroscopy. The exposure of human breast adenocarcinoma MCF-7 cells to a TL aqueous extract resulted in decreases in cell growth, clonogenic cell survival, and cell viability in a concentration-dependent manner with an $IC_{50}$ value of $843{\mu}g/ml$. Treatments with extract for 24h at $250{\mu}g/ml$ or higher induced cell cycle arrest as indicated by a significant increase of cell population in the G1 phase and a significant decrease in the S phase of the cell cycle. The capability of the aqueous extract to generate radical intermediates was observed at both high pH and near-neutral pH conditions. The findings suggest the antitumor bioactivities of TL against selected breast cancer cells may be due to induction of a G1 cell cycle arrest. Cytotoxicity and cell cycle perturbation that are associated with a high concentration of the extract could be in part explained by the total phenolic contents in the extract and the capacity to generate radical intermediates to modulate cellular proliferative signals.

In Vitro Antitumor Properties of an Isolate from Leaves of Cassia alata L

  • Olarte, Elizabeth Iglesias;Herrera, Annabelle Aliga;Villasenor, Irene Manese;Jacinto, Sonia Donaldo
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.5
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    • pp.3191-3196
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    • 2013
  • Leaf extracts of Cassia alata L (akapulko), traditionally used for treatment of a variety of diseases, were evaluated for their potential antitumor properties in vitro. MTT assays were used to examine the cytotoxic effects of crude extracts on five human cancer cell lines, namely MCF-7, derived from a breast carcinoma, SK-BR-3, another breast carcinoma, T24 a bladder carcinoma, Col 2, a colorectal carcinoma, and A549, a nonsmall cell lung adenocarcinoma. Hexane extracts showed remarkable cytotoxicity against MCF-7, T24, and Col 2 in a dose-dependent manner. This observation was confirmed by morphological investigation using light microscopy. Further bioassay-directed fractionation of the cytotoxic extract led to the isolation of a TLC-pure isolate labeled as f6l. Isolate f6l was further evaluated using MTT assay and morphological and biochemical investigations, which likewise showed selectivity to MCF-7, T24, and Col 2 cells with $IC_{50}$ values of 16, 17, and 17 ${\mu}g/ml$, respectively. Isolate f6l, however, showed no cytotoxicity towards the non-cancer Chinese hamster ovarian cell line (CHO-AA8). Cytochemical investigation using DAPI staining and biochemical investigation using terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL)-a method used to detect DNA fragmentation-together with caspase assay, demonstrated apoptotic cell death. Spectral characterization of isolate f6l revealed that it contained polyunsaturated fatty acid esters. Considering the cytotoxicity profile and its mode of action, f6l might represent a new promising compound with potential for development as an anticancer drug with low or no toxicity to non-cancer cells used in this study.

Cytotoxic Effect of Urushiol on Human Ovarian Cancer Cells

  • Choi, Ju-Youn;Park, Chang-Soo;Choi, Jong-Oh;Rhim, Hyang-Shuk;Chun, Heung-Jae
    • Journal of Microbiology and Biotechnology
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    • v.11 no.3
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    • pp.399-405
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    • 2001
  • Urushiol, a natural pro-electrophilic quinone compound, has potential structural characteristics as antitumor chemotherapeutic agents. However, urushiol's use as an antitumor drug has some problems, because it is hardly miscible with an aqueous solution. Purified urushiol is highly viscous and soluble only in strong solvents. for this study, we prepared an urushiol-ethanol micro-emulsion with a unimodal size distribution by high-speed homogenization. This generated effective delivery of urushiol to its action wites, so that we could investigate its cytotoxic activity against cancer cells. Using a colony-forming assay, we were able to show that urushiol selectively inhibited the growth of the ovarian cancer cells PA-1 and 2774 at a concentration of $10^{-6}$, whereas it had only a negligible effect on normal CHO cells at the same concentration. The data suggest that urushiol may have potential as an effective antitumor agent in the treatment of ovarian cancer. In addition, we addressed the question of whether the specific cytotoxic effect of urushiol is linked to apoptosis, by DNA fragmentation and DAPI staining assays. The inhibitory effects of urushiol on the growth of ovarian cancer cells was found to be associated with DNA fragmentation and the fragmented nuclei formation, both of which represent markers for the induction of apoptosis. Therefore, the results suggested that urushiol affected its profound cytotoxicity by triggering apoptosis in ovarian cancer cells.

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Effects of Wekyungtang and Kami-Wekyungtang on Pulmonary Tumor Cells and the Changes of Tissues (위경탕(葦莖湯).가미위경탕(加味葦莖湯)의 B16-Fo에 대(對)한 항종양(抗腫瘍) 효과(效果)와 조직(組織) 변화(變化))

  • Kim, Hyeon-Su;Kim, Seong-Hun
    • The Journal of Korean Medicine
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    • v.16 no.2 s.30
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    • pp.365-385
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    • 1995
  • In order to prove the antitumor effect of Wekyungtang(WKT) that was originated in Bigeubchunkeumyobang(備急千金要方), Wekyungtang with Houttuyniae Herba(WKT-I) and Wekyungtang with Oldenlandiae diffusae Herba(WKT-II) experimentally, the studies were done, We evaluated the cytotoxic activity against B16- Fo as well as the synergistic effects with anticancer drugs such as cyclophophamide (CPM), cisplatin(CPT) and 5-fluorouracil (5-FU) in vitro and measured body weight, survival time, hematological changes, changes of tissues in G57BL/6 implanted with B16-Fo. The results were obtained as follows: 1. In vitro cytotoxic effect against B16-Fo was shown in all groups as compared with control group, but the concentrations showing inhibitory growth rate below 55% of control was recognized in all concentrations of Wekyungtang(WKT) against B16-Fo and also concentration of $10^4$g/ml above in all group with cyclophophamide (CPM), concentration of $10^3$g/ml in Wekyungtang(WKT-l) with cisplatin(CPT) in synergistic effect, 2. In vivo body and tumor weight were significantly suppressed in all groups as compared with control group 3. The number of platelet, WBC, RBC were significantly increased in all groups, platelet aggregation was significantly increased in WKT-I and WKT-II as compared with control group. 4. In changes of tissues heavy infiltration oh cancer was shown in portal vein, pulmonary tissue, vein, peribronchiole, aveoli, while WKT-I was effective in antihepatic metastasis and WKT-II in pulmonary matastasis. From above results it was concluded that wekyungtang(WKT), wekyungtang with Houttuyniae Herba(WKT-I) and wekyungtang with Oldenlandiae diffusae Herba(WKT -II) had antitumor effect, and also wekyungtang combined with Houttuyniae Herba or Oldenlandiae diffusae Herba were more effective than wekyungtang only and also cyclophophamide (CPM), cisplatin(CPT) showed the more synergistic effect which suggests the necessity of continuous study on the mechanism of antitumor action of Houttuyniae Herba or Oldenlandiae diffusae Herba.

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