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Biological Activity Topoisomerase-I-Inhibitor

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List of activity chemicals.
Click on column headings to sort table by that column. *Unless otherwise noted all references are to (Duke, 1992)
Chemical Name Dosage Reference
MAKALUVAMINE-G IC50=3 uM Carney, J. R., Scheuer, P. J., Kelly-Gorges, M. 1993. Makaluvamine G, a Cytotoxic Pigment From an Indonesian Sponge Histodermella sp. Tetrahedron, 49: 8483-8486.
MENADIONE 1 ug/mL Frydman, B., et al. 1997. Induction of DNA Topoisomerase II-Mediated DNA Cleavage by Beta-lapachone and Related Naphthoquinones. Cancer Research, 57: 620-627.
MITOMYCIN-C not available Zhang, W. S., Lin, Z. K., Huang, X. T. 1990. Effect of Some Nonintercalative Antitumor Drugs on the Activity of Calf Thymus DNA Topoisomerase I. Yao Hsueh Hsueh Pao, 25: 641-645.
MONOMARGINE 10 ug/ml Mahmood, K., Pais, M., Fontaine, C., Ali, H. M., Hamid, A., Hadi, A., Guittet, E. 1993. Monomargine, a Nitrogenous Cytotoxic Pigment From Monocarpia marginalis. Tetrahedron Letters, 34: 1795-1796.
MORIN IC50=42.1 ug/ml (weak activity) Constantinou, A., Mehta, R., Runyan, C., Rao, K., Vaughan, A., Moon, R. 1995. Flavonoids as DNA Topoisomerase Antagonists and Poisons: Structure-Activity Relationships. J Natural Products, 58: 217-225.
MYRICETIN IC50=11.9 ug/ml Duke, 1992 *
NARINGENIN not available Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
NEOAMPHIMEDINE not available De Guzman, F. S., et al. 1999. Neoamphimedine: A New Pyridoacridine Topoisomerase II Inhibitor Which Catenates DNA. J Org Chem, 64: 1400-1402.
NITIDINE 0.15 uM Duke, 1992 *
NORHARMAN ED50=34.4 ug/ml (weak activity) Funayama, Y., Nishio, K., Kabayashi, K., Nagao, M., Shimoi, K., Ohira, T., Hasegawa, S., Saijo, N. 1996. Effects of Beta- and Gamma-carboline Derivatives on DNA Topoisomerase Activities. Mutat Research, 249: 183-191.
NOVOBIOCIN 150 uM Constantinou, A., Henning-Chubb, C., Huberman, E. 1989. Novobiocin- and Phorbol-12 myristate-13-acetate-Induced Differentiation of Human Leukemia Cells Associated with a Reduction in Topoisomerase II Activity. Cancer Research, 49: 1110-1117.
PEDUNCULAGIN 0.03 ug/ml Ooishi, K., Kato, J., Hayamizu, K. 1994. Topoisomerase Inhibitors Containing Tannins, Especially Pedunculagin, for Treatment of Cancer. Patent, Japan Kokai Tokkyo Koho-06 72,885. 7pp.
QUERCETIN IC50=12.8 ug/ml Duke, 1992 *
QUERCETIN IC50=42 uM Duke, 1992 *
RABDOSIN 50 uM Kashiwada, Y., Bastow, K. F., Lee, K. H. 1995. Novel Lignan Derivatives as Selective Inhibitors of DNA Topoisomerase II. Bioorg Med Chem Lett, 5: 905-908.
RUBRAXANTHONE IC50=60 ug/ml Iinuma, T., Nozaki, H. 1998. Antitumor Agents Containing Xanthones as Topoisomerase Inhibitors. Patent, Japan Kokai Tokkyo Koho-10 203,977. 10pp.
SANGUIIN-H-6 IC50=0.02-5 uM Bastow, K.F., Bori, I.D., Fukushima, Y., Kashiwada, Y., Tanaka, T., Nonaka, G., Nishioka, I., Lee, K.H. 1993. Inhibition of DNA Topoisomerases by Sanguiin H-6, a Cytotoxic Dimeric Ellagitannin From Sanguisorba officinalis. Planta Medica, 59: 240-245.
SANSALVAMIDE-A IC50=124 um Duke, 1992 *
VELUTIN 0.1 ug/ml Zahir, A., Jossang, A., Bodo, B., Provost, J., Cosson, J. P., Sevenet, T. 1996. DNA Topoisomerase I Inhibitors: Cytotoxic Flavones From Lethedon tannaensis. J Natural Products, 59: 701-703.
WAKAYIN 6.7 nM Kokoshka, J. M., Capson, T. L., Holden, J. A., Ireland, C. M., Barrows, L. R. 1996. Differences in the Topoisomerase I Cleavage Complexes Formed by Camptothecin and Wakayin, a DNA-Intercalating Marine Natural Product. Anticancer Drugs, 7: 758-765.
List of Activity Plants.
Click on column headings to sort table by that column.
Plant Name Common Name Chemical Count Total Parts Per Million
Cynara cardunculus Artichoke 4 0
Cypripedium pubescens Ladyslipper 1 0
Cytisus ardoini not available 1 0
Cytisus ingramii not available 1 0
Cytisus multiflorus not available 1 0
Cytisus scoparius Scotch Broom 3 0
Cytisus striatus not available 1 0
Cytisus tribracteolatus not available 1 0
Daphne genkwa Yuan Hua 2 0
Daucus carota Carrot 6 0
Desmodium gangeticum not available 1 16
Dictamnus albus Akgiritotu; Burning Bush; Dittany; Gas Plant; Gazelotu 1 0
Digitalis lanata Grecian Foxglove 1 0
Digitalis purpurea Purple Foxglove 3 0
Dioclea glycinoides not available 1 30
Diospyros virginiana American Persimmon 3 0
Dipogon lignosus not available 1 0
Dodonaea viscosa Hopwood 2 0
Dolichos biflorus not available 1 0
Drimys winteri Winter's Bark 2 0