Chemical Dosage References
10-HYDROXYCAMPTOTHECIN0.4-1 uM*
17-BETA-ESTRADIOL--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
20(S)-CAMPTOTHECINIC50=0.52 uMWall, M.E., Wani, M.C., Nicholas, A.W., Manikumar, G., Tele, C., Moore, L., Truesdale, A., Leitner, P., Besterman, J.M. 1993. Plant Antitumor Agents. 30. Synthesis and Structure Activity of Novel Camptothecin Analogs. J Med Chem, 36: 2689-2700.
3',5',7-TRI-O-METHYLTRICETIN1 ug/mLZahir, 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.
4-NEROLIDYL-CATECHOLIC50=20 ug/mlMonqelli, E., Aromano, a., Desmarchelier, C., Coussio, J., Ciccia, G. 1999. Cytotoxic 4-nerolidylcatechol From Pothomorphe peltata Inhibits Topoisomerase I Activity. Planta Medica, 65: 376-378.
5,6-DIHYDRO-8-DEMETHYLCORYALYNE0.26 uMPilch, D. S., et al. 1997. Minor Groove-Directed and Intercalative Ligand-DNA Interactions in the Poisoning of Human DNA Topoisomerase I by Protoberberine Analogs. Biochemistry, 36: 12542-12543.
7-HYDROXY-FLAVONE100 ug/ml*
8-DEMETHYLCORALYNE26 uMPilch, D. S., et al. 1997. Minor Groove-Directed and Intercalative Ligand-DNA Interactions in the Poisoning of Human DNA Topoisomerase I by Protoberberine Analogs. Biochemistry, 36: 12542-12543.
ACACETIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
ALNUMYCIM--Bieber, B., Nueske, J. 1998. Alnumycin, a New Metabolite From Streptomyces sp., Procedure For Its Production And Its Biological Effect. Patent, Ger Offen-19,745,914. 10pp.
ALPHA-BOSWELLIC-ACID-ACETATEIC>80=5 uM*
AMAROGENTIN5 uMRay, S., Majumder, H.K., Chakravarty, A.K., Mukhopadhyay, S., Gil, R.R., Cordell, G.A.1996.Amarogentin, a Naturally Occurring Secoiridoid Glycoside and a Newly Recognized Inhibitor of Topoisomerase I From Leishmania donovani. J Natural Products, 59: 27-29
AMPHIMIC-ACID-A--Nemoto, T., Ojika, M., Sakagami, Y. 1997. Amphimic Acids, Novel Unsaturated C28 Fatty Acids as DNA Topoisomerase I Inhibitors From an Australian Sponge Amphimedon sp. Tetrahedron Letters, 38: 5667-5670.
APIGENIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
APIODIONEN83 ug/mlTakahashi, H., Shiraishi, A., Iizuka, Y., Furuya, K., Kagasaki, T. 1992. Manufacture of Anticancer and Anti-Inflammatory Apiodionen With Apiosordaria. Patent, Japan Kokai Tokkyo Koho-04 49,289. 8pp.
BETA-LAPACHONE250 uMLi, C. J., Verboukh, L., Pardee, A. B. 1993. Beta-lapachone, a Novel DNA Topoisomerase I Inhibitor With a Mode of Action Different From Camptothecin. J Biol Chem, 268: 22463-22468.
BETA-LAPACHONEIC50=1 uMWeller, M., et al. 1997. Topoisomerase I Inhibitors For Human Malignant Glioma: Differential Modulation of P53, P21, BAX and BEL-2 Expression and of CD95-Mediated Apoptosis. Int J Cancer, 73: 707-714.
BETA-LAPACHONE1 ug/mLFrydman, B., et al. 1997. Induction of DNA Topoisomerase II-Mediated DNA Cleavage by Beta-lapachone and Related Naphthoquinones. Cancer Research, 57: 620-627.
BIOCHANIN-A--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
BIS-DEMETHOXYCURCUMIN25 ug/ml*
CAFFEINE75 uMShin, C. G., Strayer, J. M., Wani, M., Snapka, R. M. 1990. Rapid Evaluation of Topoisomerase Inhibitors: Caffeine Inhibition of Topoisomerases in vivo. Teratogen Carcinogen Mutagen, 10: 41-52.
CAFFEINE0.1 nMTohda, H., Zhao, J. H., Oikawa, A. 1992. A Possible Involvement of DNA Topoisomerase I in 'Caffeine Effect' After Ultraviolet Irradiation. Tohoku J Exp Med, 168: 129-132.
CAMPTOTHECIN1-50 uM*
CAMPTOTHECINIC50=1 uMWeller, M., et al. 1997. Topoisomerase I Inhibitors For Human Malignant Glioma: Differential Modulation of P53, P21, BAX and BEL-2 Expression and of CD95-Mediated Apoptosis. Int J Cancer, 73: 707-714.
CAMPTOTHECINIC50=670 nMLuzzio, M. J., et al. 1995. Synthesis and Antitumor Activity of Novel Water Soluble Derivatives of Camptothecin as Specific Inhibitors of Topoisomerase I. J Med Chem, 38: 395-401.
CAMPTOTHECINED50=0.8 uMHertzberg, R. P., et al. 1989. Modification of the Hydroxy Lactone Ring of Camptothecin: Inhibition of Mammalian topoisomerase I and Biological Activity. J Med Chem, 32: 715-720.
CHARTREUSIN1 ug/mLYoshida, T., Habuka, N., Takeuchi, M., Ichishima, E. 1986. Inhibition of DNA Topoisomerase I From Alcaligenes sp. by Chartreusin. Agr Biol Chem, 50: 515-516.
CHEBULAGIC-ACIDIC50=50 nM*
CHEBULANINMIC=0.1 ug/mlTokura, K., Kagawa, S. 1993. Anticancer Agents Containing Chebulanin From Terminalia chebula. Patent, Japan Kokai Tokkyo Koho-07 138,165. 4pp.
CHELERYTHRINE--Fang, S. D., Wang, L. K., Hect, S. M. 1993. Inhibitors of DNA Topoisomerase I Isolated From the Roots of Zanthoxylum nitidum. J Org Chem, 58: 5025-5027.
CHRYSIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
CORILAGINIC50=40 uMHecht, S. M., Berry, D. E., MacKenzie, L. J., Busby, R. W., Nasuti, C. A. 1992. A Strategy For Identifying Novel, Mechanistically Unique Inhibitors of Topoisomerase I. J Natural Products, 55: 401-413.
CRYPTOLEPINE5 uMBonjean, K., et al. 1998. The DNA Intercalating Alkaloid Cryptolepine Interferes with Topoisomerase II and Inhibits Primarily DNA Synthesis in B16 Melanoma Cell. Biochemistry, 37: 5136-5146.
CURCUMIN--*
DAIDZEIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
DEMETHOXYCURCUMIN--*
DIHYDRODAIDZEIN250 ppm (weak activity)Chang, Y. C., Nair, M. G., Nitiss, L. J. L. 1995. MEtabolites of Daidzein and Genistein and Their Biological Activities. J Natural Products, 58: 1901-1905.
DIHYDROGENISTEIN250 ppmChang, Y. C., Nair, M. G., Nitiss, L. J. L. 1995. MEtabolites of Daidzein and Genistein and Their Biological Activities. J Natural Products, 58: 1901-1905.
DIHYDROTANSHINONE-I1 uMLee, D. S., Lee, S. H., Kwon, G. S., Lee, H. K., Woo, J. H., Kim, J. G., Hong, S. D. 1999. Inhibition of DNA Topoisomerase I by Dihydrotanshinone I, Components of a Medicinal Herb Salvia miltiorrhiza Bunge. Biosci. Biotech. Biochem., 63: 1370-1373.
DISTAMYCIN--Mortensen, U. H., Stevensner, T., Krogh, S., Olesen, K., Westergard, O., Bonven, B. J. 1990. Distamycin Inhibition of Topoisomerase I-DNA Intercation: A Mechanistic Analysis. Nucleic Acids Res, 18: 1983-1989.
DOTRIACOLIDE2.6 ug/mlOgawara, H., Horikawa, S., Yanagida, T., Nakno, M. M., Andoh, T., Ishii, K., Hori, M., Goto, T. A., Hamada, M., Umezawa, H. 1982. A Novel Deoxyribonuclease Inhibitor From Micromonospora. J Antibiot, 35: 248-250.
EPIBERBERINE250 uMKobayashi, Y, Yamashita, Y., Fujii, N., Takaboshi, K., Kawakami, T., Kawamura, M., Mizukami, T., Nakano, H. 1995. Inhibitors of DNA Topoisomerase I and II Isolated From the Coptis Rhizomes. Planta Medica, 61: 414-418.
EPIMANOALIDE-25-ACETALIC50=25 uMKobayashi,M., Okamoto,T., Hayashi,K., Yokayama,N., Sasaki,T., Kitagawa,I. 1994. Marine Natural Products. XXXII. Absolute Configurations of C-4 of the Manoalide Family, Biologically Active Sesterterpenes From the Marine Sponge. Chem Pharm Bull, 42: 265-270
EQUOLIC50=50 ppmChang, Y. C., Nair, M. G., Nitiss, L. J. L. 1995. MEtabolites of Daidzein and Genistein and Their Biological Activities. J Natural Products, 58: 1901-1905.
FAGARONINE0.15-100 uM*
FISETINIC50=20.6 ug/ml*
FORMONETIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
FORMONONETIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
FREDERICAMYCIN-A4.4 uMLatham, M. D., King, C. K., Gorycki, P., MacDonald, T. L., Ross, W. E. 1989. Inhibition of Topoisomerases by Fredericamycin A. Cancer Chemother Pharmacol, 24: 167-171.
GALANGIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
GALLIC-ACID--Hamada, S. I., Kataoka, T., Woo, J. T., Yamada, A., Yoshida, T., Nishimura, T., Otake, N., Nagai, K. 1997. Immunosuppressive Effects by Gallic Acid and Chebulagic Acid on CTL-Mediated Cytotoxicity. Biol Pharm Bull, 20: 1017-1019.
GENISTEINIC50=250 ppm*
GENISTEIN1-10 ug/mlOkura, A., Arakawa, H., Oka, H., Yoshinari, T., Monden, Y. 1988. Effect of Genistein on Topoisomerase Activity and on the Growth of [VAL 12]HA-RAS-Transformed NIH 3T3 Cells. Biochem Biophys Res Commun, 157: 183-189.
GROENLANDICINE250 uMKobayashi, Y, Yamashita, Y., Fujii, N., Takaboshi, K., Kawakami, T., Kawamura, M., Mizukami, T., Nakano, H. 1995. Inhibitors of DNA Topoisomerase I and II Isolated From the Coptis Rhizomes. Planta Medica, 61: 414-418.
HALENAQUINONE0.3 ug/mlBae, M. A., Tsuji, T., Kondo, K., Hirase, T., Ishibashi, M., Shigemori, H., Kobayashi, J. I. 1993. Inhibition of Mammalian Topoisomerase I by Xestoquinone and Halenaquinone. Biosci. Biotech. Biochem., 57: 330-331.
HARMANED50=23.8 ug/ml (weak)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.
ISORABDOSIIN50 uMKashiwada, 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.
KAEMPFERIDE--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
KAEMPFEROL--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
LUTEOLIN--Santti, R., Makela, S., Strauss, L., Korman, J., Kostian, M. L. 1998. Phytoestrogens: Potential Endocrine Disruptors in Males. Toxicol Ind Health, 14: 223-237.
MAKALUVAMINE-GIC50=3 uMCarney, J. R., Scheuer, P. J., Kelly-Gorges, M. 1993. Makaluvamine G, a Cytotoxic Pigment From an Indonesian Sponge Histodermella sp. Tetrahedron, 49: 8483-8486.
MENADIONE1 ug/mLFrydman, 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--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.
MONOMARGINE10 ug/mlMahmood, 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.
MORINIC50=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.
MYRICETINIC50=11.9 ug/ml*
NARINGENIN--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--De Guzman, F. S., et al. 1999. Neoamphimedine: A New Pyridoacridine Topoisomerase II Inhibitor Which Catenates DNA. J Org Chem, 64: 1400-1402.
NITIDINE0.15 uM*
NORHARMANED50=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.
NOVOBIOCIN150 uMConstantinou, 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.
PEDUNCULAGIN0.03 ug/mlOoishi, 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.
QUERCETINIC50=42 uM*
QUERCETINIC50=12.8 ug/ml*
RABDOSIN50 uMKashiwada, 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.
RUBRAXANTHONEIC50=60 ug/mlIinuma, T., Nozaki, H. 1998. Antitumor Agents Containing Xanthones as Topoisomerase Inhibitors. Patent, Japan Kokai Tokkyo Koho-10 203,977. 10pp.
SANGUIIN-H-6IC50=0.02-5 uMBastow, 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-AIC50=124 um*
VELUTIN0.1 ug/mlZahir, 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.
WAKAYIN6.7 nMKokoshka, 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.
XESTOQUINONEIC50=0.15 ug/mlBae, M. A., Tsuji, T., Kondo, K., Hirase, T., Ishibashi, M., Shigemori, H., Kobayashi, J. I. 1993. Inhibition of Mammalian Topoisomerase I by Xestoquinone and Halenaquinone. Biosci. Biotech. Biochem., 57: 330-331.