| Budget Amount *help |
¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
Fiscal Year 2011: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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| Research Abstract |
Thelephora aurantiotincta belonging to the genus Thelephora, grows in symbiosis with pine trees. Several phytochemical investigations have revealed that the genus Thelephora is an abundant source of p-terphenyl derivatives with anti-oxidative and-allergic activities. However, in screening for natural materials with anticancer activity for human hepatocellular carcinoma cells(HepG2), we isolated and identified a new p-terphenyl derivative, thelephantin-O(TO), and a known compound, vialinin-A(VA), as the principal bioactive components using LC-MS/MS and 2-D NMR analysis of deuterium isotope effects on<13>^C chemical shifts. These compounds with adjacent cis-phenolic dihydroxyl group decreased cell viability in HepG2 and human colonic carcinoma cells(Caco2), but not in corresponding to noncancerous human cells. And we investigate its selective biological action mechanism and caspase 3/7 activities, as the results, 10μg/mL of these compounds inhibited completely their activities. These res
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ults showed that anticancer activities of these compounds were not caused by apoptosis and were needed another pathway(will be published somewhere).
Judging from strong anti-oxidative and high caspase inhibitory activity of these compounds, we intended to examine the effects of these compounds on hepatic cirrhosis inflammation occurred with active-oxygen, caused by chronic alcohol consumption. At first, we chemically synthesized VA according to the method of Suzuki-Miyaura novel prize coupling for obtaining need for first trial animal experimental trial. Adult male Wistar rats were fed with a 36% Lieber-DeCarli ethanol-containing liquid diet or pair-fed control diet with or without 0. 0002% and 0. 001% VA(w/v) for 8 weeks. As the results, administration of VA did not show any toxicity and abnormal biochemical parameters, and any difference of food take and body weight provided by pair feeding between ethanol-and VA-fed rats during the study period. However, the TBARS levels were inclined to be higher in the chronic ethanol-fed group than VA-fed group. At present we try to adjust the amounts of oral dose VA. Less
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