Tyrosinase inhibitors from Rhododendron collettianum and their structure-activity relationship (SAR) studies |
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Authors: | Ahmad Viqar Uddin Ullah Farman Hussain Javid Farooq Umar Zubair Muhammad Khan Mahmud Tareq Hassan Choudhary Muhammad Iqbal |
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Affiliation: | HEJ Research Institute of Chemistry, University of Karachi, Karachi, Pakistan. vuahmad@cyber.net.pk |
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Abstract: | A new coumarinolignoid 8'-epi-cleomiscosin A (1) together with the new glycoside 8-O-beta-D-glucopyranosyl-6-hydroxy-2-methyl-4H-1-benzopyrane-4-one (2) have been isolated from the aerial parts of Rhododendron collettianum and their structures determined on the basis of spectroscopic evidences. Tyrosinase inhibition study of these compounds and their structure-activity relationship (SAR) were also investigated. The compounds exhibited potent to mild inhibition activity against the enzyme. Especially, the compound 1 showed strong inhibition (IC50=1.33 microM) against the enzyme tyrosinase, as compared to the standard tyrosinase inhibitors kojic acid (IC50=16.67 microM) and L-mimosine (IC50=3.68 microM), indicating its potential used for the treatment of hyperpigmentation associated with the high production of melanocytes. |
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