Recently, we have shown that green tea extract (GTE) intake markedly lowers the lymphatic absorption of lipid-soluble compounds (eg. cholesterol, benzo[a]pyrene) and enhances its secretion into the biliary route in rats. Dioxin is a persistent lipophilic organic pollutant. The present serial studies were designed to examine the effect of enteral infusion of GTE on the lymphatic absorption, metabolism and biliary secretion of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in rats. In study 1 was conducted to examine whether enteral infusion of GTE would affect the lymphatic absorption of TCDD in rats. Male Sprague-Dawley rats with lymph cannulae were infused at 3.00 mL/h for 8 h via a duodenal catheter with a lipid emulsion containing TCDD labeled with 3H (3H-TCDD), 10.00 pg TCDD, 452.00 μmol triolein, 20.70 μmol cholesterol, 3.10 μmol α-tocopherol and 396.00 ?mol Na-taurocholate without (control) or with 76.10 mg GTE in PBS buffer (pH, 6.4). Lymph was collected hourly for 8 h. No significant difference was noted in lymph flow (19.13 ± 6.02 mL in GTE-infused vs. 20.78 ± 4.71 mL in control rats). However, the infusion of GTE markedly lowered the lymphatic absorption of 3H-TCDD (17.89 ± 2.53% dose/8 h) compared with controls infused with the lipid emulsion alone (23.09 ± 1.66% dose/8 h). Likewise, GTE significantly decreased the lymphatic output of cholesterol, α-tocopherol and total fatty acids. Also the 3H-radioactivities in the small intestinal lumen, mucosa and cecum were markedly increased in rats infused with GTE. The results indicate that GTE has a profound inhibitory effect on the intestinal absorption of dioxin in rats. Study 2 was conducted to examine whether GTE affects the luminal uptake of TCDD into the intestinal mucosa. Male Sprague-Dawley rats were fed an AIN-93G diet with or without (control) GTE at 5 g/kg diet (GTE1) and 20 g/kg diet (GTE2) for 3 week. At 3 weeks, a 10cm long jejunal segment of the small intestine was ligated in situ. Then, micellar solutions were injected into the ligated jejunal segments and incubated for 10 min. The micellar solution contained 1.00 μCi 3H-TCDD, 1.00 μCi 14C-oleic acid, 133.00 μM unlabelled oleic acid, 66.70 μM 2-monooleoyl-glycerol, 2.20 mM glucose, 50.00 μM albumin, 66.70 μM lysoPC, 8.30 pg TCDD, 16.50 mM sodium taurocholate in PBS buffer (pH, 6.4). At 10 min, the segment was removed. GTE dose-dependently reduced the luminal uptake of 3H-TCDD into the intestinal mucosa. Also, GTE significantly lowers the rate of 14C-oleic acid esterification into triglycerides and phospholipids fraction. Lastly study 3 was conducted to examine if an enteral infusion of GTE would infulence the biliary secretion of TCDD. Additionally, the effect of GTE on the expression of CYP1A1, SULT and MRP3 was investigated in hepatic tissue. Male Sprague-Dawley rats were fed an AIN-93G diet with or without (control) GTE at 5 g/kg diet for 2 week. Rat with bile duct cannulae were infused at 3.00 mL/h for 8 h via a duodenal catheter with a lipid emulsion containing TCDD labeled with 3H (3H-TCDD), 10.00 pg TCDD, 452.00 μmol triolein, 20.70 μmol cholesterol, and 3.10 μmol α-tocopherol and 396.00 ?mol Na-taurocholate without (control) or with 76.10 mg GTE in PBS buffer (pH, 6.4).Bile was collected hourly via bile cannulae for an 8 h period. No significant difference was noted in bile flow (7.67 ± 0.51 mL in GTE-infused vs. 7.33 ± 0.45 mL in control rats). However, the biliary secretion of 3H-TCDD was significantly enhanced by GTE infusion (7.19 ± 0.40% dose/8 h), compared with those infused with the lipid emulsion alone (6.50 ± 0.15% dose/8 h). Likewise, GTE significantly increased the biliary output of cholesterol and phospholipid. Also, GTE significantly increased SULT and MRP3 expression of hepatic tissue. These findings indicate that GTE has a profound stimulatory effect on the biliary excretion of TCDD in rats. In summary, the findings provide evidence that GTE effectively lowers the lymphatic absorption of TCDD, inhibits the luminal uptake and increases its biliary secretion. All these studies are closely related each other, which provides the first conclusive data that green tea is a dietary means to reduce dioxin contamination from the body. These findings indicate that GTE inhibits the lymphatic absorption and simultaneously enhances the biliary secretion of TCDD, suggesting a possible use as an effective dietary means of mitigating its toxicity.