Anti-tumour-promoting and thermal-induced protein denaturation inhibitory activities of beta-sitosterol and lupeol isolated from Diospyros lotus L.

作者：Rauf Abdur; Uddin Ghias; Khan Haroon^*; Raza Muslim; Zafar Muhammad; Tokuda Harukuni

来源：Natural Product Research, 2016, 30(10): 1205-1207.

DOI：10.1080/14786419.2015.1046381

• Diospyros lotus
• beta-sitosterol
• lupeol
• anti-tumour-promoting and inhibitory activities of thermal-induced protein denaturation
• docking studies against the phosphoinositide 3-kinase enzyme

In this study, the anti-tumour-promoting and thermal-induced protein denaturation inhibitory activities of -sitosterol (1) and lupeol (2), isolated from Diospyros lotus L., were explored. Compound 1 showed a marked concentration-dependent inhibition against 12-O-tetradecanoylphorbol-13-acetate (20ng/32pmol)-induced Epstein-Barr virus early antigen activation in Raji cells with IC50 of 270g/ml, without significant toxicity (70% viability). Compound 2 showed significant anti-tumour-promoting effect with IC50 of 412g/ml, without significant toxicity (60% viability). In heat-induced protein denaturation assay, compound 1 exhibited a concentration-dependent attenuation with a maximum effect of 73.5% at 500g/ml with EC50 of 117g/ml, while compound 2 exhibited a maximum effect of 59.2% at 500g/ml with EC50 of 355g/ml. Moreover, in silico docking studies against the phosphoinositide 3-kinase enzyme also show the inhibitory potency of these compounds. In short, both the compounds exhibited a marked anti-tumour-promoting and potent inhibitory effect on thermal-induced protein denaturation.

• 出版日期2016-5-18