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

Abstract

In this study, the anti-tumour-promoting and thermal-induced protein denaturation inhibitory activities of β-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 (20 ng/32 pmol)-induced Epstein-Barr virus early antigen activation in Raji cells with IC50 of 270 μg/ml, without significant toxicity (70% viability). Compound 2 showed significant anti-tumour-promoting effect with IC50 of 412 μg/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 500 μg/ml with EC50 of 117 μg/ml, while compound 2 exhibited a maximum effect of 59.2% at 500 μg/ml with EC50 of 355 μg/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.

Chemical constituents and medical function of leaves of Diospyros lotus L.

“…Diospyros lotus L. is a species of tree in the genus Diospyros and the family Ebenaceae and widely distributed in China. It has been cultivated in several countries for its edible fruits and used as traditional medicines for various medicinal purposes [10][11][12][13][14][15][16][17]. Diospyros lotus L. has more economic importance with yielding edible fruits and valuable timbers.…”

Reversal of Multidrug Resistance and Computational Studies of Pistagremic Acid Isolated from Pistacia integerrima

“…Furthermore, all the default parameters were used for both Autodock Vina and i-GEMDOCKv 2.1 software's (Rauf et al, 2015a;Rauf et al, 2015b;Rauf et al, 2015c). The docking analysis was carried out through LIGPLOT+ version v.1.4.5 (Wallace et al, 1995), PyMOL (DeLano, 2002) and Discovery studio visualizer softwares (Visualizer, 2005).…”

Molecules and medical function of Diospyros lotus L.

“…The Diospyros lotus L. is the deciduous tree and the important fruit yielding species of genus Diospyros. The fruit is used usually as a sedative, astringent, nutritive, antiseptic, antidiabetic, antitumor, laxative, antipyretic and for the treatment of constipation [8]. The fruit extract has a high amount of total phenolic and flavonoid contents and showed the strong antioxidant and free-radical scavenging activity [9][10][11][12][13][14][15][16].…”