Anti-malarial activity of some xanthones isolated from the roots of Andrographis paniculata

• Published in: Journal of ethnopharmacology 2004-12, Vol.95 (2), p.247-251
• Main Authors: Dua, V.K., Ojha, V.P., Roy, R., Joshi, B.C., Valecha, N., Devi, C. Usha, Bhatnagar, M.C., Sharma, V.P., Subbarao, S.K.
• Format: Article
• Language: English
• Subjects: Andrographis; Andrographis paniculata; Animals; Anti-malarial activity; antimalarials; Antimalarials - chemistry; Antimalarials - isolation & purification; Antimalarials - pharmacology; antimicrobial properties; Biological and medical sciences; cytotoxicity; General pharmacology; Humans; malaria; Medical sciences; medicinal plants; Mice; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Plant Roots; Plasmodium berghei; Plasmodium falciparum; Plasmodium falciparum - drug effects; Plasmodium falciparum - physiology; roots; Xanthones; Xanthones - chemistry; Xanthones - isolation & purification; Xanthones - pharmacology
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2004.07.008

Four xanthones were isolated from the roots of Andrographis paniculata using a combination of column and thin-layer chromatographic methods. They were characterized as (i) 1,8-di-hydroxy-3,7-dimethoxy-xanthone, (ii) 4,8-dihydroxy-2,7-dimethoxy-xanthone, (iii)1,2-dihydroxy-6,8-dimethoxy-xanthone and (iv) 3,7,8-trimethoxy-1-hydroxy xanthone by IR, MS and NMR spectroscopic methods. In vitro study revealed that compound 1,2-dihydroxy-6,8-dimethoxy-xanthone possessed substantial anti-plasmodial activity against Plasmodium falciparum with its IC 50 value of 4 μg ml −1. Xanthones bearing hydroxyl group at 2 position demonstrated most potent activity while xanthones with hydroxyl group at 1,4 or 8 position possessed very low activity. In vivo anti-malarial sensitivity test of this compound on Swiss Albino mice with Plasmodium berghei infection using Peters’ 4-day test gave substantial reduction (62%) in parasitaemia after treating the mice with 30 mg kg −1 dose. In vitro cytotoxicity against mammalian cells revealed that 1,2-dihydroxy-6,8-dimethoxy-xanthone is non-cytotoxic with its IC 50 > 32 μg ml −1.