Gardenin D has antioxidant, and antiproliferative activities.

METHODS AND RESULTS:In the present study we mined the information on Gardenia lucida (Dikamali) and identified seven polymethoxyflavones from its gum resin. We also investigated its antiproliferative and antioxidant potential. Xanthomicrol (8) found as potent DPPH scavenger (85.86±1.3%) along with strong ferric plummeting ability (53.60±2.0 FSE) and reducing potential (1.07±0.01) as compared to ascorbic acid. Gardenin B (5) strongly inhibit biochemical production of nitric oxide (IC50 10.59±0.4μg/mL) followed by 5-Desmethylnobiletin (7) and Gardenin E (10, IC5011.01±0.7-34.53±2.7μg/mL). Methanol extract, chloroform fraction and Acerosin (11), Gardenin D (9) and Gardenin B (5) exhibited superior antiproliferative activity against lung, breast, colon, hepatic and leukaemia cell lines as well as in keratinocytes (IC50 12.82±0.67-94.63±1.27μg/mL) whereas other fractions and isolated compounds moderately affect the cell proliferation (21.40±0.12-48.12±0.47%) with least and non-specific interaction against succinate dehydrogenase. Except compound 2, 3, 6, 8 and 11, others were found as a significant inhibitor of ODC (IC50 2.36±0.7-8.53±0.32μg/mL) with respect to DFMO (IC50 10.85±0.28μg/mL). In silico analysis also revealed enervated binding energy (-4.30 to -5.02kcal/mol) and inhibition constant (704.18-210.26μM) wherein 5, 7, 8, 9 and 10 showed specific interaction with the receptor while rest were non-specific. Except butanol fraction and Gardenin E, others were potently inhibited the cathepsin D activity with non-specific interaction and better binding energy (-5.78 to -7.24kcal/mol) and inhibition constant (57.87-4.90μM).