Artemisinin Endoperoxide Biological Data Literally thousands of pre/clinical studies (in vitro, in vivo and human) have been conducted with artemisinin endoperoxides and derivatives during the past three decades in the treatment of malaria. In the past 10 years, however, nearly 300 studies have been published regarding artemisinin-based therapies in the treatment of cancer, proliferative and inflammatory diseases, and infectious diseases. Summaries of studies conducted with the Company's compounds can be found below.
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Cancer Cell Growth Inhibition Several of the Company's compounds have been tested in vitro against 60 human cancer cell lines in the US National Cancer Institute's Developmental Therapeutics Program. In nearly all cancers, the novel artemisinin compounds have demonstrated growth inhibition activity towards cancer cells comparable to or better than gold standard anti-cancer drugs. Based on in vivo toxicity studies and the established safety profiles of artemisinin compounds in humans, the Company's compounds should offer an effective and safer chemotherapy.
The following charts compare the GI50 values of artemisinin-based compounds and standard chemotherapy in 60 human cancer cell lines. A GI50 value is the concentration of a drug that causes 50% Growth Inhibition and is a measure of the growth inhibitory power of the test agent. The lower the GI50 value (to left on graphs), the more potent the drug.
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Company In Vitro Test Data
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Therapy
| Disease
| Cell Line
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ART Trioxane Dimers
| Multiple Cancers Prostate Cancer Cervical Cancer Medulloblastoma Breast Cancer Leukemia Lymphoma Multiple Myeloma Melanoma
| 60 NCI Cancer Cell Lines Transgenic Adenoarcinoma of Mouse Prostate HeLa, C33A, HCX-HPV16 Cells DAOY Cells MCF-7 Cells HL-60 Cells U-937 Cells MM1.S, U266 Cells UACC-62 Cells
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ART-Iron Chelators
| Multiple Cancers Medulloblastoma Neuroblastoma Leukemia Breast Cancer Prostate Cancer Multiple Myeloma
| 60 NCI Cancer Cell Lines DAOY Cells SMS-KCNR, SK-N-BE(2)c, SH-SY5Y Cells Molt-4 Cells MCF-7 Cells C4-2, DU-145, LNCaP, PC-3 Cells MM1.S, U266 Cells
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ART-Peptides
| Medulloblastoma Leukemia Neuroblastoma Liver Cancer Multiple Cancers
| DAOY Cells Molt-4 Cells IMR-32 Cells HepG2 Cells, Hepatocytes 60 NCI Cancer Cell Lines
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ART-Transferrin
| Leukemia Benign Prostatic Hyperplasia
| Molt-4 Cells, Lymphocytes Prostate Stromal, Epithelial Cells
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ART plus Transferrin
| Leukemia Breast Cancer Neuroblastoma
| Molt-4 Cells HTB27, HTB125 Cells IMR-32 Cells
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ART plus Butyrate
| Leukemia
| Molt-4 Cells, Lymphocytes
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Company In Vivo Test Data
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Therapy
| Disease
| Disease Model
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ART Trioxane Dimers
| Breast Cancer Brain Cancer Brain Cancer
| MTLn3 Model in Rats Toxicity Study in Mice Intracranial Glioma Xenografts in Mice
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ART-Peptides
| Breast Cancer
| MTLn3 Model in Rats
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Artemisinin
| Breast Cancer Prevention
| DMBA-Induced Breast Cancer in Rats
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DHA plus Ferrous Sulfate
| Fibrosarcoma
| Fibrosarcoma in Rats
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