Abstract
We have been screening anti-HIV integrase compounds from Korean medicinal plants by using anin vitro assay system which is mainly composed of recombinant human immunodeficency virus type 1 integrase and radiolabeled oligonucleotides. From the above screening, the aqueous methanolic extract of the roots ofAgastache rugosa exhibited a significant activity. Bioactivity-guided chromatographic fractionation of the methanolic extract resulted in the isolation of rosmarinic acid. The structure of the compound was determined by spectroscopic data and by the comparison with the reported values. The IC50 of the rosmarinic acid was approximately 10 μ/ml against HIV integrase.
Similar content being viewed by others
References Cited
Fesen, M. R., Kohn, K. W., Leteurtre, F. and Pommier, Y., Inhibitors of human immunodeficiency virus integrase.Proc. Natl. Acad. Sci. USA. 90, 2399–2403 (1993).
Fesen, M. R., Pommier, Y., Leteurtre, F., Hiroguchi, S., Yung, J. and Kohn, K. W., Inhibition of HIV-1 integrase by flavones, caffeic acid phenethyl ester (CAPE) and related compounds. Biochem.Pharmacol. 48, 595–608 (1994)
Han, D. S., Kim, Y. C., Kim, S. E., Ju, H. S. and Byun, S. J., Studies of the diterpene constituent of the root ofAgastache rugosa O. Kuntze,Kor. J. Pharmacogn. 18, 99–102 (1987).
Han, D. S., Triterpenes from the root ofAgastache rugosa, Kor. J. Pharmacogn. 18, 50–53 (1987).
Kelly, C. J., Harruff, R. C. and Carmack, M., The poly-phenolic acids ofLithospermum ruderale. II. Carbon-13 nuclear magnetic resonance of lithospermic and rosmarinic acids,J. Org. Chem. 41, 449–455 (1976).
Kelly, C. J., Mahajan, J. R., Brooks, L. C., Neubert, L. A., Breneman W. R. and Carmack, M., Polyphenols acids fromLithospermum ruderale Dougl. ex Lehm. (Bora-ginaceae). 1. Isolation and structure determination of lithospermic acid,J. Org. Chem. 40, 1804–1815 (1975).
Kim, H. J., Woo, E-R., Shin, C-G. and Park, H., A new flavol glycoside gallate ester fromAcer okamotoanum and its inhibitory activity against human immunodeficiency virus (HIV-1) integrase,J. Nat. Prod. 61, 145–148 (1998).
Kuhnt, M., Rimpler, H. and Heinrich, M., Lignans and other compounds from the mixture Indian medicinal plantHyptis verticillata, Phytochem. 36, 485–489 (1994).
Lee, H. K., Oh, S. R., Kim, J. I., Kim, J. and Lee, C., Agastaquinone, a new cytotoxic diterpenoid quinone fromAgastache rugosa, J. Nat. Prod., 58, 1718–1721 (1995).
Lee, S. J., Korean Folk Medicine, Seoul Prints, Seoul, p 113 (1976).
Mazumder, A., Neamati, N., Sunder, S., Schulz, J., Pertz, H., Leteurtre, E. and Pommier, Y., Curcumin analogs with altered potencies against HIV-1 integrase as probes for biochemical mechanisms of drug action.J. Med. Chem. 40, 3057–3063 (1997)
Mazumder, A., Raghavan, K., Weinstein, J., Kohn, K. W. and Pommier, Y., Inhibition of human immunodeficiency virus type-1 integrase by curcumin.Biochem. Pharmacol. 49, 1165–1170 (1995)
Oh, J. -W. and Shin, C. -G., Purification and characterization of the human immunodeficiency virus type 1 integrase expressed in Escherichia coli,Mol. Cell, 6, 96–100 (1996).
Oh, Y. -T. and Shin, C. -G., Comparison of enzymatic activities of the HIV-1 and HFV integrases to their U5 LTR substrates.Biochem. Mol. Biol. Int., 47, 621–629 (1999).
Pearson, D. A., Frankel, E. N., Aeschbach, R. and German, J. B., Inhibition of endothelial cell-mediated oxidation of low-density lipoprotein by rosmary and plant phenolics,J. Agric. Food Chem. 45, 578–582 (1997).
Sherman, P. A. and Fyfe, J. A., Human immunodeficiency virus integrase protein expressed inEscherichia coli possesses selective DNA cleavaging activity.Proc. Natl. Acad. Sci. USA 87, 5119–5123 (1990).
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Kim, H.K., Lee, HK., Shin, CG. et al. HIV integrase inhibitory activity ofAgastache rugosa . Arch Pharm Res 22, 520–523 (1999). https://doi.org/10.1007/BF02979163
Received:
Issue Date:
DOI: https://doi.org/10.1007/BF02979163