Trypsin inhibitory activity of artemisinin and its biotransformed product. | [Journal of Chemical Society of Pakistan • 2013]

Author(s):

1. Durr-E-Shahwar: Research Lab. II, Department of Chemistry, Government College University, Lahore, Pakistan

2. Muhammad Asam Raza: Research Lab. II, Department of Chemistry, Government College University, Lahore-54000, Pakistan;Department of Chemistry, University of Gujrat, Hafiz Hayat Campus, Gujrat, Pakistan

3. Viqaruddin Ahmad: HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan

Abstract:

Artemisinin (1), a sesquiterpene lactone is an important constituent of anti-malarial drugs. In the present study, it was extracted from aerial parts of Artemisia roxburghianaBesser. Biotransformation of artemisinin (1) was carried out in the culture of Aspergillusniger GC-4 which yielded 5-hydroxy artemisinin (2) The structures of 1-2 were confirmed through spectral studies. Both compounds were screened against trypsin using colorimetric method. The biotransformed product 2 showed significant protease inhibitory activity with 53.5 ± 1.6% inhibition and IC50 = 0.29 ± 0.02 mM as compared to artemisinin (20.4 ± 0.3% inhibition).

Page(s): 135-138

DOI: DOI not available

Published: Journal: Journal of Chemical Society of Pakistan, Volume: 35, Issue: 1, Year: 2013

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