Farnesyl protein transferase inhibitory components of Polygonum multiflorum

Abstract

The methanolic extract of the roots of Polygonum multiflorum (Polygonaceae) was found to show inhibitory activity towards farnesyl protein transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two anthraquinone glycosides, as inhibitors of FPTase. These compounds inhibited the FPTase activity in a dose-dependent manner.

Simultaneous Determination of 13 Constituents of Radix Polygoni Multiflori in Rat Plasma and Its Application in a Pharmacokinetic Study

“…RPM extract suspended in an equal volume of 5% CMC-Na solution and orally administered to the six rats at a single dose of 36 g/kg (dose calculated as grams of crude materials used to create the extract per kilogram of rat body weight). e dose was set at a subtoxic level [40,41] to investigate the pharmacokinetic profiles of the constituents of RPM and were approximately 72 times the upper dose (6 g/day) of human recommended by the 2015 edition of Chinese Pharmacopoeia [5] (converted to rat dose based on body 13.0 mg/kg for chrysophanol, emodin, aloe-emodin, rhein, physcion, questin, citreorosein, questinol, TSG, TG, CG, EG, and PG, respectively. Rats were fasted for at least 12 h before the experiments and had free access to water.…”

“…Stilbenes, mainly 2,3,5,4′-tetrahydroxystilbene-2-O-β-D-glucoside (TSG), possessed antioxidative, antitumor, anti-inflammatory, endothelial protective, neuroprotective, and liver-protective activities, etc. [10][11][12][13][14][15][16][17][18][19][20][21]. Anthraquinones were reported to possess many biological activities, including immunomodulating, anticancer, antimutation, antibacterial, anticancer, antioxidant, etc.…”

Pharmacokinetics and tissue distribution of 2,3,5,4′-tetrahydroxystilbene-2-O-β-d-glucoside from traditional Chinese medicine Polygonum multiflorum following oral administration to rats

“…stilbene glycosides, are responsible for its medicinal activities (Yao et al, 2006;Yi et al, 2007;Han et al, 2009). 2,3,5,4 -Tetrahydroxystilbene-2-O-ˇ-d-glucoside (structure in Fig. 1), a major active stilbene glycoside in Polygonum multiflorum, has been reported to possess antioxidative, anti-inflammatory, endothelial protective, and oncogenic enzyme inhibitory activities (Ryu et al, 2002;Li-Shuang et al, 2006;Lv et al, 2007;Wang et al, 2008;Kwon et al, 2009;Liu et al, 2010). These medicinal functions of the Polygonum multiflorum stilbene glycoside (PM-SG) has attracted much attention and generated great interest of researchers for its further investigation and therapeutic application.…”

Nuclear factor kappa B activation and peroxisome proliferator-activated receptor transactivational effects of chemical components of the roots of Polygonum multiflorum

“…Their structures were elucidated by comparing spectroscopic data to published data. The compounds were identified as follows: Physcion (1),[ 23 ] emodin (2),[ 24 ] physcion-8- O - β -D-(6’- O -acetyl)-glucoside (3),[ 25 ] emodin- 8- O - β -D-glucoside (4),[ 26 ] physcion-8- O - β -D-glucoside (5),[ 25 ] torachrysone-8- O - β -D-glucoside (6),[ 27 ] torachrysone-8- O - β -D-glucoside-6’- O -gallate (7),[ 28 ] ( Z )-2,3,5,4’- tetrahydroxystilbene-2- O - β -D-glucoside (8),[ 29 ] ( E )-2,3,5,4’-tetrahydroxystilbene-2- O - β -D-glucoside (9),[ 29 ] ( E )-2,3,5,4’- tetrahydroxystilbene-2- O - β -D-xyloside (10),[ 28 ] ( E )-2,3,5,4’- tetrahydroxystilbene-2- O - β -D-(6’- O -acetyl)-glucoside (11),[ 28 ] (+)- catechin (12),[ 30 ] (+)-catechin-3- O -gallate (13),[ 30 ] β -sitosterol (14),[ 31 ] and β -sitosterol-3- O - β -D-glucoside (15). [ 31 ]…”