Archives of Pharmacal Research

, Volume 22, Issue 5, pp 520–523 | Cite as

HIV integrase inhibitory activity ofAgastache rugosa

  • Hye Kyong Kim
  • Hyeong-Kyu Lee
  • Cha-Gyun Shin
  • Hoon Huh
Research Articles Natural Products


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.

Key words

HIV integrase Agastache rugosa Labiatae Rosmarinic acid 


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References Cited

  1. 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).PubMedCrossRefGoogle Scholar
  2. 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)Google Scholar
  3. 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).Google Scholar
  4. Han, D. S., Triterpenes from the root ofAgastache rugosa, Kor. J. Pharmacogn. 18, 50–53 (1987).Google Scholar
  5. 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).CrossRefGoogle Scholar
  6. 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).CrossRefGoogle Scholar
  7. 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).PubMedCrossRefGoogle Scholar
  8. Kuhnt, M., Rimpler, H. and Heinrich, M., Lignans and other compounds from the mixture Indian medicinal plantHyptis verticillata, Phytochem. 36, 485–489 (1994).CrossRefGoogle Scholar
  9. 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).PubMedCrossRefGoogle Scholar
  10. Lee, S. J., Korean Folk Medicine, Seoul Prints, Seoul, p 113 (1976).Google Scholar
  11. 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)PubMedCrossRefGoogle Scholar
  12. 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)PubMedCrossRefGoogle Scholar
  13. 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).Google Scholar
  14. 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).PubMedGoogle Scholar
  15. 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).CrossRefGoogle Scholar
  16. 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).PubMedCrossRefGoogle Scholar

Copyright information

© The Pharmaceutical Society of Korea 1999

Authors and Affiliations

  • Hye Kyong Kim
    • 1
  • Hyeong-Kyu Lee
    • 2
  • Cha-Gyun Shin
    • 3
  • Hoon Huh
    • 1
  1. 1.Research Institute of Pharmaceutical Sciences, College of PharmacySeoul National UniversitySeoulKorea
  2. 2.Korea Research Institute of Bioscience and BiotechnologyKISTTaejonKorea
  3. 3.Department of BiotechnologyChung-Ang UniversityAn-SungKorea

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