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Planta Med 2002; 68(2): 111-114
DOI: 10.1055/s-2002-20256
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

In vitro Anti-HIV Activity of Oleanolic Acid on Infected Human Mononuclear Cells

Fabio Mengoni1 , Miriam Lichtner1 , Lucia Battinelli2 , Monica Marzi1 , Claudio Maria Mastroianni1 , Vincenzo Vullo1 , Gabriela Mazzanti2
  • 1Department of Infectious and Tropical Diseases, University ”La Sapienza”, Rome, Italy
  • 2Department of Pharmacology of Natural Substances and General Physiology, University ”La Sapienza”, Rome, Italy
Further Information

Publication History

February 2, 2001

June 24, 2001

Publication Date:
22 February 2002 (online)

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Abstract

Oleanolic acid is a triterpenoid which is quite common in nature in the form either of free acid or in triterpenoid saponin glycosides. This study describes the effect of oleanolic acid on the growth of human immunodeficiency virus-1 (HIV-1) in cultures of human peripheral mononuclear cells (PBMC) and of monocyte/macrophages (M/M). Its inhibitory activity was also evaluated on PBMC obtained from HIV-1 infected patients. Results obtained show that oleanolic acid inhibits the HIV-1 replication in all the cellular systems used (EC50 values: 22.7 μM, 24.6 μM and 57.4 μM for in vitro infected PBMC, naturally infected PBMC and M/M, respectively). As regards the mechanism of action, oleanolic acid inhibits in vitro the HIV-1 protease activity.

Key words

Oleanolic acid - anti HIV-1 activity - HIV-1 protease - PBMC - M/M

References

  • 1 Wang B, Jiang Z H. Studies on oleanolic acid.  Chinese Pharmaceutical Journal. 1992;  27 393-7
    PubMedGoogle Scholar
  • 2 Liu J. Pharmacology of oleanolic acid and ursolic acid.  Journal of Ethnopharmacology. 1995;  49 57-68
    CrossrefPubMedGoogle Scholar
  • 3 Liu Z, Wang D, Wang S, Ha S, Li P. Oleanolic acid in decreasing hyperglycemia.  Chinese Pharmaceutical Journal. 1994;  29 725-6
    PubMedGoogle Scholar
  • 4 Ma X H, Zhao Y C, Yin L, Han D W, Ji C X. Studies on the effect of oleanolic acid on experimental liver injury.  Acta Pharmaceutica Sinica. 1982;  17 93-7
    PubMedGoogle Scholar
  • 5 Jeong H G. Inhibition of cytochrome P450 2E1 expression by oleanolic acid: hepatoprotective effects against carbon tetrachloride-induced hepatic injury.  Toxicology Letters. 1999;  105 215-22
    CrossrefPubMedGoogle Scholar
  • 6 Liu J, Liu Y P, Parkinson A, Klaassen C D. Effect of oleanolic acid on hepatic toxicant-activating and detoxifying systems in mice.  Journal of Pharmacology and Experimental Therapeutics. 1995;  275 768-74
    PubMedGoogle Scholar
  • 7 Zhang L Z, Li X F. Study on the mechanism of oleanolic acid against experimental liver injury in rats.  Traditional Medicine and Clinical Pharmacology. 1992;  8 24-6
    PubMedGoogle Scholar
  • 8 Singh G B, Singh S, Bani S, Gupta B D, Banerjee S K. Anti-inflammatory activity of oleanolic acid in rats and mice.  Journal of Pharmacy and Pharmacology. 1992;  44 456-8
    PubMedGoogle Scholar
  • 9 Ohigashi H, Takamura H, Koshimizu K, Tokuda H, Ito Y. Search for possible antitumor promoters by inhibition of 12-o-tetradecanoylphorbol-13-acetate-induced Epstein-Barr virus activation: ursolic acid and oleanolic acid from an anti-inflammatory Chinese medicinal plant, Glechoma hederaceae L.  Cancer Letters. 1986;  30 143-51
    CrossrefPubMedGoogle Scholar
  • 10 Oguro T, Liu J, Klaassen C D, Yoshida T. Inhibition effect of oleanolic acid on 12-O-tetradecanoylphorbol-13-acetate-induced gene expression in mouse skin.  Toxicological Science. 1998;  45 88-93
    PubMedGoogle Scholar
  • 11 Muto Y, Ninomiya M, Fujiki H. Present status research on cancer chemoprevention in Japan.  Japanese Journal of Clinical Oncology. 1990;  20 219-24
    PubMedGoogle Scholar
  • 12 Xu L Z, Wan Z X. The effect of oleanolic acid on acute hepatites (70 cases).  Human Medicine. 1980;  7 50-2
    PubMedGoogle Scholar
  • 13 Serra C, Lampis G, Pompei R, Pinza M. Antiviral activity of new triterpenic derivatives.  Pharmacological Research. 1994;  29 359-66
    CrossrefPubMedGoogle Scholar
  • 14 De Tommasi N, Conti C, Stein M L, Pizza C. Structure and in vitro antiviral activity of triterpenoid saponins from Calendula arvensis .  Planta Medica. 1991;  57 250-3
    PubMedGoogle Scholar
  • 15 Sindambiwe J B, Calomme M, Geerts S, Pieters L, Vlietinck A J, Vanden Berghe D A. Evaluation of biological activities of triterpenoid saponins from Maesa lanceolata .  Journal of Natural Products. 1998;  61 585-90
    CrossrefPubMedGoogle Scholar
  • 16 Simões C MO, Amoros M, Schenkel E P, Shin-Kim J S, Rücker G, Girre L. Preliminary studies of antiviral activity of triterpenoid saponins: relationship between their chemical structure and antiviral activity.  Planta Medica. 1990;  56 652-3
    PubMedGoogle Scholar
  • 17 Kashiwada Y, Wang H K, Nagao T, Kitanaka S, Yasuda I, Fujioka T, Yamagishi T, Cosentino L M, Kozuka M, Okabe H, Ikeshiro Y, Hu C Q, Yeh E, Lee K H. Anti-AIDS agents 30. Anti-HIV activity of oleanolic acid, pomolic acid and structurally related triterpenoids.  Journal Natural Products. 1998;  61 1090-5
    PubMedGoogle Scholar
  • 18 Vlietinck A J, De Bruyne T, Apers S, Pieters L A. Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection.  Planta Medica. 1998;  64 97-109
    PubMedGoogle Scholar
  • 19 Perno C F, Yarchoan R. Current protocols in immunology. Vol. 3, New York; John Wiley & Sons 1993: 12.4.1-.11
    Google Scholar
  • 20 Tallarida R, Murray R B. Manual of Pharmacologic Calculation with Computer Programs. 2nd Edn, Springer Verlag New York; 1981
    Google Scholar
  • 21 Hattori T, Ikematsu S, Koito A, Matsushita S, Maeda Y, Hada M, Fujimaki M, Takatsuki K. Preliminary evidence for inhibitory effect of glycyrrhizin on HIV replication in patients with AIDS.  Antiviral Research. 1989;  11 255-61
    CrossrefPubMedGoogle Scholar
  • 22 Ito M, Nakashima H, Baba M, Pauwels R, De Clercq E, Shigeta S, Yamamoto N. Inhibitory effect of glycyrrhizin on the in vitro infectivity and cytopathic activity of the human immunodeficiency virus [HIV (HTLV-III/LAV)].  Antiviral Research. 1987;  7 127-37
    CrossrefPubMedGoogle Scholar
  • 23 Ma C, Nakamura N, Miyashiro H, Hattori M, Shimotohno K. Inhibitory effects of costituents from Cynomorium songaricum and related triterpene derivatives on HIV-1 protease.  Chemical and Pharmacological Bulletin. 1999;  477 141-5
    PubMedGoogle Scholar

Lucia Battinelli

Dipartimento di Farmacologia delle Sostanze Naturali e

Fisiologia Generale

Università ”La Sapienza”

P.le Aldo Moro, 5

00185 Rome

Italy

Phone: +39-06-4991-2903

Fax: +39-06-4991-2480

Email: lucia.battinelli@uniroma1.it

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