Reference

Effects of gomisin A on liver functions in hepatotoxic chemicals-treated rats

Effects of gomisin A on liver functions in hepatotoxic chemicals-treated rats. Maeda, Shinya; Takeda, Shigefumi; Miyamoto, Yoshimasa; Aburada, Masaki; Harada, Masatoshi (Tsumura Res. Inst. Pharmacol., Ami 300-11, Japan). Jpn. J. Pharmacol., 38(4), 347-53 (English) 1985. CODEN: JJPAAZ. ISSN: 0021-5198. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effects of gomisin A (I) [58546-54-6], a lignan component of schizandra fruits, on liver function in various exptl. liver injuries and on bile secretion in CCl4-induced liver injury were studied. Gomisin A weakly accelerated the disappearance of plasma indocyanine green (ICG) (a measure of liver function) when given alone at a high dose (100 mg/kg, i.p.). All of the hepatotoxic chem. used in this study inhibited the elimination of ICG from plasma. Gomisin A prevented the delays of the disappearance of plasma ICG induced by CCl4, D-galactosamine and orotic acid, but not that induced by a-naphthylisothiocyanate. Bile flow and biliary output of total bile acids and electrolytes (Na+, K+, Cl- and HCO3-) were decreased in CCl4-treated rats. Gomisin A maintained bile flow and biliary output of each electrolyte at nearly the levels of the vehicle-treated group, but did not affect the biliary output of total bile acids. Apparently, gomisin A possesses a liver function-facilitating activity in normal rats and rats with liver injury and its prevention action on CCl4-induced cholestasis is due to maintaining the function of the bile acid-independent fraction.

Studies on the metabolic fate of gomisin A (TJN-101)

Studies on the metabolic fate of gomisin A (TJN-101). I. Absorption in rats. Matsuzaki, Yutaka; Matsuzaki, Tamae; Takeda, Shuichi; Koguchi, Sachiko; Ikeya, Yukinobu; Mitsuhashi, Hiroshi; Sasaki, Hiromi; Aburada, Masaki; Hosoya, Eikichi; Oyama, Tsutomu (Res. Inst. Pharmacol., Tsumura and Co., Ami 300-11, Japan). Yakugaku Zasshi, 111(9), 524-30 (Japanese) 1991. CODEN: YKKZAJ. ISSN: 0372-7750. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Gomisin A (TJN-101) (I; R + R1 = CH2) is one of the lignan components isolated from Schisandra Fruits and expected to have some efficacies in clin. treatment of hepatitis. The serum concns. of TJN-101 and metabolite B, which was identified as a demethylenated substance and one of the major metabolites of TJN-101 in rats, were investigated. After i.v. administration at doses of 1.6, 4.0 and 10 mg/kg, the serum concn. of TJN-101 decreased biphasically, and the terminal elimination half-life at each dose was about 70 min.Several substances with their cas registry numbers 58546-54-6 and 72551-73-6 may be metioned in this study. Dose-dependency was obsd. for the area under the concn.-time curve (AUC). On the other hand, the serum concn. of TJN-101 increased rapidly and reached max. within 15 to 30 min when administered orally. This result was supported by the in situ roop method. The Cmax and the AUC values were not exactly dose-dependent, but the values increased with a dose-up of TJN-101. The biotransformation of TJN-101 to metabolite B, was very rapid in both i.v. and oral administrations. The AUC value of metabolite B after oral administration of TJN-101 at a dose of 1.6 mg/kg was relatively larger than any other dosages. It suggested that TJN-101 was extensively underwent the 1st pass effect in rats. More than 80% of TJN-101 was bound with rat serum protein in vitro and in vivo. Therefore, it seems to be necessary to pay attention when it was administered concurrently with high protein binding drugs. .