Disease relevance of Benzylidene glucose

• In vivo pharmacokinetics of 4,6-benzylidene-D-glucose (BG) was investigated in rats following an i.v. bolus injection of 85 mg BG/kg body weight [1].
• There was no indication of systemic toxicity in mice receiving P-1013 [2].
• Antitumour effect of benzylidene-glucose (BG) in rats with chemically induced hepatocellular carcinoma [3].
• P-1013 at 90 mg/kg for 49 days was effective against SK-OV-3 human ovarian carcinoma (T/C 47% at day 40 and 50% increase in TD) [2].

High impact information on Benzylidene glucose

• In vivo and in vitro pharmacokinetics of 4,6-benzylidene-D-glucose (BG) in rats [1].
• In this study we compared the bioavailability of BG and P-1013, since both intraperitoneal and, especially, oral administration of the drugs would be a great advantage [4].
• The results also indicate that P-1013 shows linear pharmacokinetics, with no change being observed in the half-life (t1/2) with increasing dose and only a slightly more than proportional increase in the area under the concentration-time curve (AUC) occurring with increasing dose [4].
• P-1013 induced significantly greater cell inactivation than BG in mammalian cells of 10 different cell lines, implying that the deuteration of BG leads to increased cellular effects [5].
• 4,6-Benzylidene-d1-D-glucose, P-1013, a deuterated benzaldehyde derivative which acts as a reversible protein synthesis inhibitor in vitro, was evaluated for antitumor effects in two human tumor xenografts implanced s.c. in nude mice [2].

Biological context of Benzylidene glucose

• Testing loss of colony forming ability following a 24 h exposure, the IC50 values, i.e. inhibitory doses that reduced the number of surviving treated cells by one half, were found to range from 3.2 to 10.8 mM BG and from 1.3 to 7.7 mM P-1013 [5].
• Effect on cell survival and protein synthesis of benzylidene-glucose (BG) and the deuterated analogue P-1013 in cultured cells [5].

Anatomical context of Benzylidene glucose

• The effect of 4,6-benzylidene-D-glucose (BG) on chemically induced primary hepatocellular carcinomas in rats was tested after daily single injections of 85 mg per kg body weight into the aorta through a canula implanted through the right carotid artery [3].

Analytical, diagnostic and therapeutic context of Benzylidene glucose

• Histological examinations of each tumor showed that P-1013 treatment of pancreatic xenografts reduced tumor volume without inducing greater necrosis than that comparable to respective control tumors [2].
• For the ovarian xenograft, the histological examination indicated a higher fraction of tumors with more than 50% necrotic tissue in two of the P-1013-treated groups compared with the control group (Fisher exact test, p = 0.12) [2].

References