Bicyclol, a synthetic dibenzocyclooctadiene derivative, decreases hepatic lipids but increases serum triglyceride level in normal and hypercholesterolaemic mice

Abstract

Bicyclol is used for the treatment of chronic hepatitis B in China. In this study, the effects of bicyclol (100 or 300 mg kg(-1), p.o.) on serum and liver lipid contents were investigated in both normal and experimentally induced hypercholesterolaemic mice. Hypercholesterolaemia was induced by either oral administration of cholesterol/bile salt or feeding a diet containing lard/cholesterol. Daily administration of bicyclol for 7 days dose-dependently increased the serum triglyceride level (29-80%) but slightly decreased the hepatic total cholesterol level (12-17%) in normal mice. Co-administration of bicyclol with cholesterol/bile salt decreased the hepatic triglyceride and total cholesterol levels (7-15% and 25-31%, respectively), when compared with the drug-untreated and cholesterol/bile salt-treated group. Bicyclol treatment for 7 days decreased hepatic triglyceride (5-76%) and total cholesterol (5-48%) levels in mice fed with high-fat/cholesterol diet. In contrast, bicyclol treatment increased the serum triglyceride level (18-77%) in mice treated with cholesterol/bile salt or fed with high-fat/cholesterol diet. Bicyclol treatment also caused an increase in hepatic index of normal and hypercholesterolaemic mice (3-32%). The results indicate that bicyclol treatment can invariably decrease hepatic lipid levels and increase serum triglyceride levels in normal and hypercholesterolaemic mice.

Supplementation with the Extract of Schisandrae Fructus Pulp, Seed, or Their Combination Influences the Metabolism of Lipids and Glucose in Mice Fed with Normal and Hypercholesterolemic Diet

“…Gomisin N, a diastereomer of schisandrin B (Sch B, a major active ingredient of SF), inhibited DNA damage checkpoint signaling by stereospecifically interacting with ataxia telangiectasia and Rad-3-related (ATR) protein kinase [22]. Our previous studies have shown that SF extracts [23, 24], Sch B [25], bicycol [26], and bifendate [27] can reduce hepatic triglyceride (TG) and total cholesterol (TC) levels in hypercholesterolemic (HCL) mice. In the present study, we endeavored to compare the effects of ethanol extracts of SF pulp, seed, or a mixture of pulp/seed on serum and hepatic lipid/glucose (GLU) levels, as well as liver function in mice under the normal and HCL conditions.…”

New Perspectives on Chinese Herbal Medicine (Zhong‐Yao) Research and Development

“…A large number of pharmacological and clinical studies have shown that FS produces a systemic effect in the body [107]. In our laboratory, an ethanol extract of FS [108], its active ingredient schisandrin B [109], as well as its related synthetic derivatives bifendate [110] and bicyclol [111] have been shown to suppress the lipid accumulation in the liver, but without affecting serum lipid levels, in experimental hypercholesterolemic mice. The possible clinical use of FS for the clinical management of fatty liver disease exemplifies the new use of an old herb in CHM.…”

Hepatitis B patients exhibiting mild alanine aminotransferase elevation: A comparative analysis of treatment with and without Bicyclol tablets

“…In addition, Bicyclol may inhibit inflammatory injury, oxidative damage and abnormal apoptosis of hepatocytes caused by generation of reactive oxygen species and NO generation (19)(20)(21)(22), thereby improving the structure and function of the hepatocyte and mitochondrial membranes (23,24). Previous clinical studies indicate that orally administered Bicyclol possesses a good safety profile and is advantageous in the setting of CHB-induced ALT elevation (14,25).…”

“…Its mechanism of action may be closely associated with free radical-scavenging properties, protection against lipid peroxidation, protection of hepatic cell membranes and mitochondrial function (12), and inhibition of inflammatory cytokines (13). It was demonstrated in experimental and clinical studies that Bicyclol decreased serum transaminase levels and resulted in improvements as observed by pathology (14)(15)(16). Although various studies have examined the clinical efficacy of Bicyclol in virus hepatitis patients, none, to the best of our knowledge, have investigated the effectiveness and safety of Bicyclol in a clinical setting.…”