A Screening strategy for selection of Anti-HIV-1 Integrase and anti-HIV- 1 Protease Inhibitors from extracts of Indian Medicinal plants
Keywords:
AIDS, HIV-1 protease, HIV-1 integraseAbstract
Ethanolic and water extracts from six species of Indian medicinal plants mainly distributed in the region of Western Ghats, India such as Morinda citrifolia (leaf), Garcinia indica (leaf), Garcinia cambogia (leaf), Salacia oblonga (leaf), Coccinium fenestratum (stem bark) and Calophyllum inophyllum (bark) were tested for their inhibitory activities against two prime enzymes of HIV which are HIV-1 protease (HIV-PR) and HIV-1 integrase (HIV-IN). The results revealed that the ethanolic and water extract of the bark extract of Calophyllum inophyllum exhibited potent anti-HIV-IN activity with IC50 values of 9.8 and 5.6 μg/ml, respectively. Whereas those for anti-HIV-1 PR effect were found to be 63.8 and 16.3 μg/ml, respectively. This result strongly supports the basis for the use of C. inophyllum for AIDS treatment by local traditional practitioners of Ayurveda and Unani system of Indian medicine and it is the first report on HIV-1 Protease and HIV-1 Integrase enzyme inhibition by this plant extract.
References
. Tewtrakul, S., Nakamura, N., Hattori, M.,
Fujiwara, T., and Supavita, T. Flavanone
and Flavonol Glycosides from the leaves of
Thevetia peruviana and their HIV-1
Reverse Transcriptase and HIV-1 Integrase
Inhibitory Activities. Chem and
Pharmaceutical Bull. 2002; 50(5) : 630-
. Peter, P.I. Clinical Research of Morinda
citrifolia L.-Noni. Noni Clinical Res J.
; 1 (1-2).
. Mishra, A., Bapat, M.M ., Tilak, J.C., and
Thomas, P. A., Devasagayam. Antioxidant
activity of Garcinia indica (kokam) and its
syrup. Curr Sci. 2006; 91 (1).
. Magadula, J.J., and Tewtrakul, S. AntiHIV-1 protease activities of crude
extracts of some Garcinia species growing
in Tanzania. African J of Biotechnol. 2010;
(12) : 1848-1852.
. Heymsfield, S.B., Allison, D.B., Vasselli,
J.R., Pietrobelli, A., Greenfield, D., Nunez,
C. Garcinia cambogia (hydroxycitric acid)
as a potential antiobesity agent: a
randomized controlled trial. J of Amer
Med Ass. 1998; 280 (18) : 1596-600.
. Mahendran, P., Vanisree, A.J., Devi, C.S2.
The antiulcer activity of Garcinia
cambogia extract against indomethacininduced gastric ulcer in rats. Phytother.
Res. 2002; 16 (1) : 80–83.
. Rao T.M., Prayaga Murty P. In-vitro
antibacterial activity of Salacia oblonga
Wall. Recent Res in Sci and Technol, 2010;
(6).
. Wattanathorn, J ., Uabundit, N ., Itarat, W .,
Mucimapura, S., Laopatarakasem, P.,
Sripanidkulchai, B. Neurotoxicity of
Coscinium fenestratum stem, a medicinal
plant used in traditional medicine. Food
and Chem Toxicol. 2006; 44(8) : 1327-
. Shirwaikar, A., Rajendran, K., and Punitha,
I.S.R. Antidiabetic activity of alcoholic
stem extract of Coscinium fenestratum in
streptozotocin-nicotinamide induced type 2
diabetic rats. J of Ethnopharmacol. 2005;
: 369-374.
. Patil, A.D., Freyer, A.J., Eggleston, D.S.,
Haltwanger, R.C., Bean, M.F., Taylor,
P.B., Caranfa, M.J., Breen, A.L., Bartus,
H.R., Johnson, R.K. The inophyllums,
novel inhibitors of HIV-1 Reverse
Transcriptase isolated from the Malaysian
tree, Calophyllum inophyllum Linn. J of
Med Chem. 1993; 36 (26) : 4131- 4138.
. Claude Spino, Marco Dodier,
Subramaniam Sotheeswaran. Anti-HIV
coumarins from calophyllum seed oil.
Bioorg and Med Chem Let. 1998; 8 : 3475
– 3478.
. Jenkins,T.M., Engelman, A., Ghirlando, R.,
Craigie, R. A soluble active mutant of
HIV-1 integrase. J of Biol Chem. 1996;
: 7712-7718.
. Tewtrakul, S., Subhadhirasakul, S.,
Kummee, S. HIV-1 protease inhibitory
effects of medicinal plants used as self
medication by AIDS patients.
Songklanakarin J of Sci and Technol.
; 25 : 239-243.
. Tewtrakul, S., Miyashiro, H., Hattori, M.,
Yoshinaga, T., Fujiwara, T., Tomimori, T.,
Kizu, H., Miyaichi, Y. Inhibitory effects of
flavonoids on human immunodeficiency
virus type-1 integrase. J of Trad Med.
; 18 (6) : 229-238.
. Laurea, F., Raharivelomananaa, P.,
Butauda, J., Bianchinia, J., Gaydou, E.M.
Screening of anti-HIV-1 inophyllums by
HPLC–DAD of Calophyllum inophyllum
leaf extracts from French Polynesia
Islands. Analytica chimica acta . 2008; 624
: 147–153.
