• Title/Summary/Keyword: Anti-neoplastic agents

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Comparative Reverse Screening Approach to Identify Potential Anti-neoplastic Targets of Saffron Functional Components and Binding Mode

  • Bhattacharjee, Biplab;Vijayasarathy, Sandhya;Karunakar, Prashantha;Chatterjee, Jhinuk
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.11
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    • pp.5605-5611
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    • 2012
  • Background: In the last two decades, pioneering research on anti-tumour activity of saffron has shed light on the role of crocetin, picrocrocin and safranal, as broad spectrum anti-neoplastic agents. However, the exact mechanisms have yet to be elucidated. Identification and characterization of the targets of bioactive constituents will play an imperative role in demystifying the complex anti-neoplastic machinery. Methods: In the quest of potential target identification, a dual virtual screening approach utilizing two inverse screening systems, one predicated on idTarget and the other on PharmMapper was here employed. A set of target proteins associated with multiple forms of cancer and ranked by Fit Score and Binding energy were obtained from the two independent inverse screening platforms. The validity of the results was checked by meticulously analyzing the post-docking binding pose of the picrocrocin with Hsp90 alpha in AutoDock. Results: The docking pose reveals that electrostatic and hydrogen bonds play the key role in inter-molecular interactions in ligand binding. Picrocrocin binds to the Hsp90 alpha with a definite orientation appropriate for nucleophilic attacks by several electrical residues inside the Hsp90-alpha ATPase catalytic site. Conclusion: This study reveals functional information about the anti-tumor mechanism of saffron bioactive constituents. Also, a tractable set of anti-neoplastic targets for saffron has been generated in this study which can be further authenticated by in vivo and in vitro experiments.

Experimental Studies on the Anti-tumor and the Immuno-modulatory Effects of Jiaweicitaowan (수종항암제(數種抗癌劑)와 한약병용효과(韓藥倂用效果)에 관한 실험적(實驗的) 연구(硏究))

  • Yoon Hong-Rho;Kim Kwang-Ho;Seung Hyun-Jea
    • Journal of Society of Preventive Korean Medicine
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    • v.2 no.1
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    • pp.1-11
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    • 1998
  • This experimental study was carried out to evaluate the effort of Lulianwendang on number of white blood cells and blood platelets in anti-neoplastic agents treated mice. The results were as follows; 1. The group of adriamycine treated and Lulianwendang administered mice were increased significantly in WBC as compared with control group.: 2. The group of cyclophosphamide injected and Lulianwendang administered mice were increased significantly in WBC as compared with control group. 3. The group of vincristin injected and Lulianwendang administered mice were increased significantly in W5C as compared with control group. 4. The group of adriamycine treated and Lulianwendang administered mice were increased significantly in blood platelets as compared with control group. 5. The group of cyclophosphamide injected and Lulianwendang administered mice were increased significantly in blood platelets as compared with control group. 6. The group of vincristin injected and Lulianwendang administered mice were increased significantly in blood platelets as compared with control group. According to the results, we can suggest that Lulianwendang has the hematopoiesis effects against anti-neoplastic agents treated mice.

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Preferential Cytotoxic Effect of Genistein on G361 Melanoma Cells Via Inhibition of the Expression of Focal Adhesion Kinase

  • Park, Sang Rye;Kwak, Hyun-Ho;Park, Bong-Soo;Kim, Gyoo Cheon
    • International Journal of Oral Biology
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    • v.37 no.4
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    • pp.189-195
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    • 2012
  • Resistance to the induction of apoptosis is a possible mechanism by which tumor cells can survive anti-neoplastic treatments. Melanoma is notoriously resistant to anti-neoplastic therapy. Previous studies have demonstrated focal adhesion kinase (FAK) overexpression in melanoma cell lines. Given its probable role in mediating resistance to apoptosis, many researchers have sought to determine whether the downregulation of FAK in melanoma cells would confer a greater sensitivity to anti-neoplastic agents. Genistein is a known inhibitor of protein-tyrosine kinase (PTK), which may attenuate the growth of cancer cells by inhibiting the PTK-mediated signaling pathway. This present study was undertaken to investigate the effect of genistein on the expression of FAK and cell cycle related proteins in the G361 melanoma cell line. Genistein was found to have a preferential cytotoxic effect on G361 melanoma cells over HaCaT normal keratinocytes. Genistein decreased the expression of 125 kDa phosphotyrosine kinase and the FAK protein in particular. Genistein treatment did not affect the expression of p53 in G361 cells in which p21 is upregulated. The expression of cyclin B and cdc2 was downregulated by genistein treatment. Taken together, our data indicate that genistein induces the decreased proliferation of G361 melanoma cells via the inhibition of FAK expression and regulation of cell cycle genes. This suggests that the use of genistein may be a viable approach to future melanoma treatments.

Rutin Suppresses Neoplastic Cell Transformation by Inhibiting ERK and JNK Signaling Pathways (Rutin의 ERK 및 JNK 신호전달체계 억제를 통한 암예방 효능)

  • Kang, Nam Joo
    • The Korean Journal of Food And Nutrition
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    • v.28 no.4
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    • pp.579-585
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    • 2015
  • Rutin is a well-known flavonoid found in buckwheat. Recent studies have demonstrated that the biological actions of rutin include anti-inflammatory and anti-cancer effects, but the underlying molecular mechanisms of these actions are not yet fully understood. Neoplastic cell transformation is considered a major event that contributes to carcinogenesis, and the present study aimed to determine whether rutin would exert anti-tumor effects via the results suggest that rutin exerted a potent inhibitory influence on the molecular activity of the MEK/ERK and MKK4/JNK pathways and strongly attenuated EGF-induced neoplastic cell transformation. These findings provide insight into the biological actions of rutin and the molecular basis for the development of new chemoprotective agents.

Exogenous Natural Glycoprotein Multiple Mechanisms of Anti-tumor Activity

  • Yuan, Hong-Liang;Liu, Xiao-Lei;Dai, Qi-Chang;Song, Hui
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.4
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    • pp.1331-1336
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    • 2015
  • Natural glycoproteins can induce apoptosis of tumor cells and exert anti-tumor activity by immunomodulatory functions, cytotoxic and anti-inflammation effects, and inhibition of endothelial growth factor. Given their prospects as novel agents, sources of natural antitumor glycoproteins have attracted attention and new research directions in glycoprotein biology are gradually shifting to the direction of cancer treatment and prevention of neoplastic disease. In this review, we summarize the latest findings with regard to the tumor suppressor signature of glycoproteins and underlying regulatory mechanisms.

Studies on Anti-cancerous and Anti-malarial Substances from Simaroubaceae Plants

  • Takeya, Koichi
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2000.10a
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    • pp.64-65
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    • 2000
  • Cancer is a general term subjected to a series of malignant tumor diseases which may affect many different parts of the human body. These cancer diseases are characterized by a rapid and uncontrolled formation of abnormal cells in the body. Cancer chemotherapeutic agents can often provide the prolongation of life and occasionally cures. To date many kinds of compounds have been obtained from plants kingdom as anti-neoplastic and anti-cancerous agents. However, there is no special type of compounds for cancer therapy. In our laboratory, anti-tumor and cytotoxic screenings on higher plants collected in Japan, China, Korea, Southeast Asia and South America have been done by using Sarcoma 180 ascites in mice, P388 lymphocytic leukemia in mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma (KB) cells. The family, Simaroubaceae consists of about 20 genera and 120 species, mainly shrubs and trees, distributed in tropical and subtropical country. Simaroubaceae is classified as RUTALES, together with Rutaceae, Burseraceae, Meliaceae, Malpighiaceae and Polygalaceae. The members differ from the Rutaceae in not containing oil glands. Bitter principles are a characteristic of the family, Simaroubaceae. The genera include Quassia (Simarouba) (40 spp.), Picrasma (Aeschrion) (6 spp.), Brucea (10 spp.), Soulamea (10 spp.), Ailanthus (10 spp.) and Perriera (1 spp.) etc.. Surinam quassia derived from Quassia amara growing in Guianas, north Brazil and Venezuela is used in traditional medicines for stomachic, anti-amoebic, anti-malarial and anti-anaemic properties. Also, various parts of a number of plants of the family Simaroubaceae have been used in traditional medicine for the treatment of a variety oi diseases including cancer, amoebic, dysentery and malaria. Then, the research has established that it is the quassinoid content of these plants that is responsible for above activities. In this meeting, I will present on anti-tumor and anti-malarial activities and their active principles of Simaroubaceae plants, Eurycoma longifolia, Ailanthus vilmoriniana, Simaba cedron and Brucea mullis which have been studied in our laboratory.

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Studies on Anti-cancerous and Anti-malarial Substances from Simaroubaceae Plants

  • Takeya, Koichi
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2000.10b
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    • pp.11-13
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    • 2000
  • Cancer is a general term subjected to a series of malignant tumor diseases which may affect many different parts of the human body. These cancer diseases are characterized by a rapid and uncontrolled formation of abnormal cells in the body. Cancer chemotherapeutic agents can often provide the prolongation of life and occasionally cures. To date many kinds of compounds have been obtained from plants kingdom as anti-neoplastic and anti-cancerous agents. However, there is no special type of compounds for cancer therapy. In our laboratory, anti-tumor and cytotoxic screenings on higher plants collected in Japan, China, Korea, Southeast Asia and South America have been done by using Sarcoma 180 ascites in mice, P388 lymphocytic leukemia in mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma (KB) cells. The family, Simaroubaceae consists of about 20 genera and 120 species, mainly shrubs and trees, distributed in tropical and subtropical country. Simaroubaceae IS classified as RUTALES, together with Rutaceae, Burseraceae, Meliaceae, Malpighiaceae and Polygalaceae. The members differ from the Rutaceae in not containing oil glands. Bitter principles are a characteristic of the family, Simaroubaceae. The genera include Quassia (Simarouba) (40 spp.), Picrasma (Aeschrion) (6 spp.), Brucea (10 spp.), Soulamea (10 spp.), Ailanthus (10 spp.) and Perriera (1 spp.) etc.. Surinam quassia derived from Quassia amara growing in Guianas, north Brazil and Venezuela is used in traditional medicines for stomachic, anti-amoebic, anti-malarial and anti-anaemic properties. Also, various parts of a number of plants of the family Simaroubaceae have been used in traditional medicine for the treatment of a variety of diseases including cancer, amoebic, dysentery and malaria. Then, the research has established that it is the quassinoid content of these plants that is responsible for above activities. In this meeting, I will present on anti-tumor and anti-malarial activities and their active principles of Simaroubaceae plants, Eurycoma longifolia, Ailanthus vilmoriniana, Simaba cedron and Brucea mollis which have been studied in our laboratory.

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Anti-neoplastic and Anti-inflammatory Effects of Single and Mixed Extracts of Ulmus Davidiana and Oldenlandia Diffusa on Azoxymethane/dextran Sodium Sulfate-induced Colonic Neoplasms (AOM/DSS 유발 대장암에 대한 유근피(楡根皮)와 백화사설초(白花蛇舌草) 단일 및 배합 추출물의 항암 및 항염 효과)

  • Lee, Seon-a;Baek, Dong-gi;Moon, Goo
    • The Journal of Internal Korean Medicine
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    • v.38 no.6
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    • pp.863-876
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    • 2017
  • Objectives: The aim of this experimental study was to evaluate the anti-neoplastic and anti-inflammatory effects of single and mixed extracts of Ulmus davidiana (UD) and Oldenlandia diffusa (OD) on azoxymethane/dextran sodium sulfate (AOM/DSS)-induced colonic neoplasms in mice. Methods: AOM/DSS induces colitis-associated colonic neoplasms in mice. Mice were divided into seven groups: normal-no inducement and no treatment; control-colonic neoplasms with no treatment; UD-colonic neoplasms and treatment with UD; OD-colonic neoplasms and treatment with OD; UD1+OD1-colonic neoplasms and treatment with UD1 and OD1. UD1+OD2-colonic neoplasms and treatment with UD1 and OD2; UD2+OD1-colonic neoplasms and treatment with UD2 and OD1. Single and mixed preparations of UD and OD were applied to mice for six weeks. The colon length and weight and histopathologic changes of colon tissue were observed. Serum pro-inflammatory cytokines, including tumor necrosis factor-alpha ($TNF-{\alpha}$) and interleukin-6 (IL-6), were determined by enzyme-linked immunosorbent assay. The mRNA expression levels of Bax, Bcl-2, and interferon-gamma ($INF-{\gamma}$) were measured by RT-PCR. Results: The colon length was significantly increased in OD, UD1+OD2, and UD2+OD1 mice, and the colon weight was significantly decreased in OD and UD1+OD2 mice. The morphological change of colon epithelial cells was more suppressed in complex-treatment groups than in single-treatment groups. The inhibitory effect on inflammatory cell invasion was especially shown in UD1+OD2 mice. The serum level of the pro-inflammatory $TNF-{\alpha}$ was decreased in all complex-treatment groups, and the IL-6 level was decreased in UD1+OD1 mice. Single-treatment groups had an increase in the mRNA expression of the pro-apoptosis regulator Bax, and UD2+OD1 decreased the mRNA expression of the anti-apoptosis regulator Bcl-2. The mRNA expression of $INF-{\gamma}$ associated with inflammation was decreased in OD and UD1+OD2 mice. Conclusions: This study suggests that single and mixed extracts of Ulmus davidiana and Oldenlandia diffusa have anti-neoplastic and anti-inflammatory effects on AOM/DSS-induced colonic neoplasms in mice. Therefore, we conclude that UD, OD, and a mixture of UD and OD are potential therapeutic agents for colitis-associated colonic neoplasms.

Cancer Chemoprevention by Dietary Phytochemicals: Rationale and Mechanisms (Dietary Phytochemical을 이용한 화학적 암에방과 그 작용 기전)

  • Surh, Young-Joon;Lee, Jong-Min
    • Environmental Mutagens and Carcinogens
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    • v.18 no.1
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    • pp.1-8
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    • 1998
  • Chemoprevention refers to the use of non-toxic chemical agents to prevent the neoplastic development by inhibiting, delaying, or reversing a multi-stage carcinogenesis. The primary goal of chemoprevention research is to identify or produce effective agents and strategies for clinical trials for applications to normal or high risk human populations. A large number of compounds have been tested for their possible chemopreventive activities, and it is of interest to note that many of them are naturally occurring substances. Thus, a variety of plant and vegetable constituents, particularly those included in our daily diet, have been found to possess substantial protective properties against experimental carcinogenesis. These substances, collectively known as dietary phytochemicals, exert their chemopreventive effects by influencing specific step(s) of multi-stage carcinogenesis: some inhibit metabolic activation or enhance detoxification of carcinogens, others interfere with covalent interactions between ultimate eloctrophilic carcinogens and the target cell DNA and still others may exert anti-promoting or anti-progressing effects. Mechanism-based interventions by use of safe dietary phytochemicals may provide one of the most practical and promising cancer chemopreventive strategies.

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Aloe vera Inhibits Proliferation of Human Breast and Cervical Cancer Cells and Acts Synergistically with Cisplatin

  • Hussain, Arif;Sharma, Chhavi;Khan, Saniyah;Shah, Kruti;Haque, Shafiul
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.7
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    • pp.2939-2946
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    • 2015
  • Many of the anti-cancer agents currently used have an origin in natural sources including plants. Aloe vera is one such plant being studied extensively for its diverse health benefits, including cancer prevention. In this study, the cytotoxic potential of Aloe vera crude extract (ACE) alone or in combination with cisplatin in human breast (MCF-7) and cervical (HeLa) cancer cells was studied by cell viability assay, nuclear morphological examination and cell cycle analysis. Effects were correlated with modulation of expression of genes involved in cell cycle regulation, apoptosis and drug metabolism by RT-PCR. Exposure of cells to ACE resulted in considerable loss of cell viability in a dose- and time-dependent fashion, which was found to be mediated by through the apoptotic pathway as evidenced by changes in the nuclear morphology and the distribution of cells in the different phases of the cell cycle. Interestingly, ACE did not have any significant cytotoxicity towards normal cells, thus placing it in the category of safe chemopreventive agent. Further, the effects were correlated with the downregulation of cyclin D1, CYP 1A1, CYP 1A2 and increased expression of bax and p21 in MCF-7 and HeLa cells. In addition, low dose combination of ACE and cisplatin showed a combination index less than 1, indicating synergistic growth inhibition compared to the agents applied individually. In conclusion, these results signify that Aloe vera may be an effective anti-neoplastic agent to inhibit cancer cell growth and increase the therapeutic efficacy of conventional drugs like cispolatin. Thus promoting the development of plant-derived therapeutic agents appears warranted for novel cancer treatment strategies.