Planta Med 2002; 68(1): 86-87
DOI: 10.1055/s-2002-20058
Letter

© Georg Thieme Verlag Stuttgart · New York

Inhibition of HIV-1 Reverse Transcriptase and HIV-1 Replication by Calophyllum Coumarins and Xanthones

H. R.W. Dharmaratne1 , G. T. Tan2 , G. P.K. Marasinghe1 , J. M. Pezzuto2
  • 11 Natural Products Programme, Institute of Fundamental Studies, Kandy, Sri Lanka
  • 22 Programme for Collaborative Research in the Pharmaceutical Sciences, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Chicago, Illinois, U.S.A.
Further Information

Publication History

January 19, 2001

July 7, 2001

Publication Date:
31 January 2002 (online)

Abstract

As part of our continuing study on the Calophyllum species, a number of coumarins, xanthones and chromene acids from different Calophyllum species of Sri Lanka were tested for inhibitory activity against the HIV-1 and its virally-encoded reverse transcriptase (RT). These compounds were found to be inactive in both the HIV-1 RT and whole virus systems. In contrast, cordatolide A and B demonstrated IC50 values of 19.3 and 11.7 μM, respectively, against HIV-1 replication in a novel green fluorescent protein (GFP)-based reporter cell assay (HOG.R5).

References

  • 1 Dharmaratne H RW, Perera D SC, Jamie J, Marasinghe G PK. A chromene acid from Calophyllum cordato-oblongum .  Phytochemistry. 1999;  51 111-3
  • 2 Dharmaratne H RW, Wanigasekera W MAP, Mata-Greenwood E, Pezzuto J M. Inhibition of human immuno-deficiency virus type 1 reverse transcriptase activity by cordatolides isolated from Calophyllum cordato-oblongum .  Planta Medica. 1998;  64 460-1
  • 3 Tan G T, Honnen W J, Kayman S C, Pinter A. A sensitive microtiter infectivity assay for macrophage-tropic and primary isolates of HIV-1 based on the transactivation of a stably integrated gene for the green fluorescent protein. The 9th National Cooperative Vaccine Development Group (NCVDG) Meeting: Advances in AIDS Pathogenesis and Preclinical Vaccine Development NIH, Bethesda, Maryland; May 4 - 7, 1997
  • 4 Kashman Y, Gustafson K R, Fuller R W, Cardellina II J H, McMahon J B, Currens M J, Buckheit Jr R W, Hughes S H, Cragg G M, Boyd M R. Journal of Medicinal Chemistry 1992 35: 2735-43
  • 5 McKee T C, Covington C D, Fuller R W, Bokesch H R, Young S, Cardellina II J H, Kadushin M R, Soejarto D D, Stevens P F, Cragg G M, Boyd M R. Pyranocoumarins from tropical species of the genus Calophyllum: a chemotaxonomic study of extracts in the National Cancer Institute collection.  Journal of Natural Products. 1998;  61 1252-6
  • 6 Tan G T, Pezzuto J M, Kinghorn A D, Hughes S H. Evaluation of natural products as inhibitors of human immunodeficiency virus type-1 (HIV-1) reverse transcriptase.  Journal of Natural Products. 1991;  54 143-54

Dr. H. R. W. Dharmaratne

Natural Products Propgramme

Institute of Fundamental Studies

Kandy

Sri Lanka

Email: hrwd13@hotmail.com

Fax: 94 - 8 232131