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

Abstract

Pistagremic acid (PA) is a bioactive triterpenoid isolated from various parts of Pistacia integerrima plants. The aim of this research was to investigate PA for reversion of multidrug resistant (MDR) mediated by P-glycoprotein using rhodamine-123 exclusion study on a multidrug resistant human ABCB1 (ATP-binding cassette, sub-family B, member 1) gene-transfected mouse T-lymphoma cell line in vitro. Results were similar to those with verapamil as a positive control. Docking studies of PA and standard Rhodamine123 were carried out against a P-gp crystal structure which showed satisfactory results. Actually, PA cannot bind exactly where co-crystallized ligand of P-gp is already present. However, the docking study predicted that if a compound gives a lesser score then it may have some potency. The docking scores of PA and Rhodamine were similar. Therefore, we can conclude that there are certain important chemical features of PA which are responsible for the inhibiting potency of P-gp.

Reversal of multidrug resistance and antitumor promoting activity of 3-oxo-6β-hydroxy- β-amyrin isolated from Pistacia integerrima

“…2, compound 1 exhibited significantly modulated the efflux pump activity (FAR: 125, 4 µg/ml). Similar results were obtained in study conducted on Pistagremic acid (PA), a triterpenoid, present in Pistacia integerrima on reversal of MDR (Rauf et al, 2016c). They concluded that there might be certain important chemical features of Pistagremic acid responsible for its inhibitory potential of P-glycoprotein (Pgp).…”

Antifungal and Antiproliferative Activity of Pistagremic Acid and Flavonoids Extracted from the Galls ofPistacia chinensissubsp.integerrima

“…Indeed, these observations are in line with previous findings that showed that pistagremic acid (1) is a broad spectrum cytotoxic compound. [19] It must be also taken into account that pistagremic acid (1) was already reported to revert multidrug resistance mediated by Pglycoprotein, [11] thus suggesting that this compound could act as a multitarget anticancer agent.…”

“…The triterpene pistagremic acid ( 1 ) is one of the main components extracted from P. chinensis galls, but it can also be retrieved in its roots and barks [10] . P. chinensis galls also contain flavonoids, such as apigenin ( 2 ) and sakuranetin ( 3 ) that we studied in the current report, and which contribute in conferring antiproliferative, anti‐infective and antioxidant potential to the plant and to its extracts [11,12] …”

“…[10] P. chinensis galls also contain flavonoids, such as apigenin (2) and sakuranetin (3) that we studied in the current report, and which contribute in conferring antiproliferative, anti-infective and antioxidant potential to the plant and to its extracts. [11,12] The aim of this study is to evaluate, by means of in vitro tests, the antifungal properties of the defatted methanolic extract of P. chinensis galls and of the 3 cited molecules, consisting in a triterpene and 2 flavonoids, isolated by column chromatography. The samples were tested against a panel of 6 different, biologically relevant fungal strains, namely Aspergillus flavus, Candida albicans, Candida glabrata, Fusarium solani, Microsporum canis and Trichoderma longibrachiatum.…”