Drug Screening Assays, Antitumor

Publication Title: 
Hematology. American Society of Hematology. Education Program

Integrative medicine (IM) has become a major challenge for doctors and nurses, as well as psychologists and many other disciplines involved in the endeavor to help patients to better tolerate the burden of toxic therapies and give patients tools so they can actively participate in their "salutogenesis." IM encompasses psycho-oncology, acupuncture, and physical and mental exercises to restore vital capacities lost due to toxic therapies; furthermore, it aims to replenish nutritional and metabolic deficits during and after cancer treatment.

Author(s): 
Diehl, Volker
Publication Title: 
Medicinal Chemistry (Shariqah (United Arab Emirates))

Non-steroidal anti-inflammatory drugs (NSAIDs) and cyclooxygenase-2 (COX-2) specific inhibitors are anti-inflammatory agents that have also shown to be useful in anticancer therapy. The effects of chebulagic acid (CA), a benzopyran tannin from Terminalia chebula having COX-2/5-LOX dual inhibitory properties, on the sensitivity of doxorubicin (Dox) in human hepatocellular carcinoma cell line HepG2 were studied in the present investigation. CA increased the accumulation of Dox in a concentration dependant manner and also enhanced the cytotoxicity of Dox in HepG2 cells by 20 folds.

Author(s): 
Achari, Chandrani
Reddy, Gorla V.
Reddy, T. C. M.
Reddanna, Pallu
Publication Title: 
Journal of Medicinal Chemistry

With the aim of up-regulating antitumor efficacy and down-regulating adverse effects, three types of aromatic imide and diimides were designed to couple with different polyamines. The in vitro assays revealed that two naphthalene diimide-polyamine conjugates could inhibit the growth of multiple cancer cell lines more potently than amonafide. 9f, the most potent compound, was verified to efficiently induce apoptosis via a ROS mediated mitochondrial pathway in a preliminary mechanistic study.

Author(s): 
Wang, Yuxia
Zhang, Xingbo
Zhao, Jin
Xie, Songqiang
Wang, Chaojie
Publication Title: 
Molecular Biology of the Cell

Forkhead box O (FOXO) transcription factors control diverse cellular functions, such as cell death, metabolism, and longevity. We analyzed FOXO3/FKHRL1 expression and subcellular localization in tumor sections of neuroblastoma patients and observed a correlation between nuclear FOXO3 and high caspase-8 expression. In neuroblastoma caspase-8 is frequently silenced by DNA methylation. Conditional FOXO3 activated caspase-8 gene expression but did not change the DNA-methylation pattern of regulatory sequences in the caspase-8 gene.

Author(s): 
Geiger, Kathrin
Hagenbuchner, Judith
Rupp, Martina
Fiegl, Heidi
Sergi, Consolato
Meister, Bernhard
Kiechl-Kohlendorfer, Ursula
M¸ller, Thomas
Ausserlechner, Michael J.
Obexer, Petra
Publication Title: 
Scientific Reports

Inhibition of cancer-promoting kinases is an established therapeutic strategy for the treatment of many cancers, although resistance to kinase inhibitors is common. One way to overcome resistance is to target orthogonal cancer-promoting pathways. Bromo and Extra-Terminal (BET) domain proteins, which belong to the family of epigenetic readers, have recently emerged as promising therapeutic targets in multiple cancers.

Author(s): 
Allen, Bryce K.
Mehta, Saurabh
Ember, Stewart W. J.
Schonbrunn, Ernst
Ayad, Nagi
Sch¸rer, Stephan C.
Publication Title: 
Molecular Pharmacology

A profound cytotoxic action of the antimalarial, artesunate (ART), was identified against 55 cancer cell lines of the U.S. National Cancer Institute (NCI). The 50% inhibition concentrations (IC50 values) for ART correlated significantly to the cell doubling times (P = 0.00132) and the portion of cells in the G0/G1 (P = 0.02244) or S cell cycle phases (P = 0.03567). We selected mRNA expression data of 465 genes obtained by microarray hybridization from the NCI data base.

Author(s): 
Efferth, Thomas
Sauerbrey, Axel
Olbrich, Armin
Gebhart, Erich
Rauch, Pia
Weber, H. Oliver
Hengstler, Jan G.
Halatsch, Marc-Eric
Volm, Manfred
Tew, Kenneth D.
Ross, Douglas D.
Funk, Jens Oliver
Publication Title: 
Anticancer Research

BACKGROUND: Artemisinin is a chemical compound extracted from the wormwood plant, Artemisia annua L. It has been shown to selectively kill cancer cells in vitro and retard the growth of implanted fibrosarcoma tumors in rats. In the present research, we investigated its mechanism of cytotoxicity to cancer cells. MATERIALS AND METHODS: Molt-4 cells, in complete RPMI-1640 medium, were first incubated with 12 microM of human holotransferrin at 37 degrees C in a humid atmosphere of 5% CO2 for one hour. This enhanced the iron supply to the cells.

Author(s): 
Singh, Narendra P.
Lai, Henry C.
Publication Title: 
PloS One

BACKGROUND: A major obstacle for successful cancer treatment often is the development of drug resistance in cancer cells during chemotherapy. Therefore, there is an urgent need for novel drugs with improved efficacy against tumor cells and with less toxicity on normal cells. Artesunate (ART), a powerful anti-malarial herbal compound, has been shown to inhibit growth of various tumor cell lines in vitro and of xenografted Kaposi's sarcoma in mice in vivo. However, the molecular mechanisms by which ART exerts its cytotoxicity have not been elucidated.

Author(s): 
Efferth, Thomas
Giaisi, Marco
Merling, Annette
Krammer, Peter H.
Li-Weber, Min
Publication Title: 
Journal of Cellular and Molecular Medicine

The present study was designed to determine the effects of artemisinin (ARS) and its derivatives on human ovarian cancer cells, to evaluate their potential as novel chemotherapeutic agents used alone or in combination with a conventional cancer chemotherapeutic agent, and to investigate their underlying mechanisms of action. Human ovarian cancer cells (A2780 and OVCAR-3), and immortalized non-tumourigenic human ovarian surface epithelial cells (IOSE144), were exposed to four ARS compounds for cytotoxicity testing.

Author(s): 
Chen, Tao
Li, Mian
Zhang, Ruiwen
Wang, Hui
Publication Title: 
Journal of Medicinal Chemistry

A new series of 6 dimeric trioxane sulfones has been prepared from the natural trioxane artemisinin in five or six chemical steps. One of these thermally and hydrolytically stable new chemical entities (4c) completely cured malaria-infected mice via a single oral dose of 144 mg/kg. At a much lower single oral dose of only 54 mg/kg combined with 13 mg/kg of mefloquine hydrochloride, this trioxane dimer 4c as well as its parent trioxane dimer 4b also completely cured malaria-infected mice. Both dimers 4c and 4b were potently and selectively cytotoxic toward five cancer cell lines.

Author(s): 
Rosenthal, Andrew S.
Chen, Xiaochun
Liu, Jun O.
West, Diana C.
Hergenrother, Paul J.
Shapiro, Theresa A.
Posner, Gary H.

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