lignans and kadsurin

The progress in the research of the chemical constituents and their pharmacological activities of Kadsura was summarized. These chemical constituents mainly contain lignanoids and triterpnoids, much of which are characteristic ingredients of the plant and have such activities as anti-oxidation, anti-HIV, and platelet active factor antagonists.

Topics: Anti-HIV Agents; Antioxidants; Cyclooctanes; Dioxoles; Drugs, Chinese Herbal; Kadsura; Lactones; Lignans; Molecular Structure; Plants, Medicinal; Platelet Activating Factor; Triterpenes

This study is to investigate the effects of aqueous extract of Schisandra chinensis Baill (WWZ), kadsurin, schisandrin A, schisandrin B and schisandrol B on rat hepatic CYP3A. Rats received a daily gavage of aqueous extract of WWZ for different times. The livers were harvested after gavage and subjected to microsome preparation. Microsomal CYP3A activity was determined by measuring the amount of the metabolite of testosterone (6 beta-hydroxytestosterone) with HPLC. Aqueous extract of WWZ, kadsurin and schisandrin A were incubated with microsomes obtained from rat. Microsomal CYP3A activity was determined by HPLC. Primary hepatocytes were separated and extracted from rat, then were treated with aqueous extract of WWZ, schisandrin A, schisandrin B and schisandrol B. Then, the expression of CYP3A1 mRNA was analyzed by RT-PCR. As for the in vivo assay, aqueous extract of WWZ significantly inhibited the enzyme activity of CYP3A after 12 h gavage. The inhibitory effect was converted to inductive effect after 3-day gavage. Aqueous extract of WWZ could induce the enzyme activity of CYP3A after 6-day gavage. Aqueous extract of WWZ and kadsurin showed a dose-dependent inhibition of CYP3A (IC50 of 487.8 microg mL(-1) and 6.2 micromol L(-1), separately). In rat primary hepatocytes, aqueous extract of WWZ (2.5 mg mL(-1)), schisandrin A (0.1 micromol L(-1)), schisandrin B (0.1 micromol L(-1)) and schisandrol B (10 micromol L(-1)) increased significantly the expression of CYP3A1 mRNA by 23%, 55%, 42% and 27%, respectively. Aqueous extract of WWZ could show dual effect on the enzyme activity of CYP3A in rat in vivo. Meanwhile, kadsurin showed a dose-dependent inhibition of the enzyme activity of hepatic CYP3A in vitro. And schisandrin A, schisandrin B and schisandrol B showed significant inductive effect on the expression of rat CYP3A1 mRNA.

Topics: Animals; Cyclooctanes; Cytochrome P-450 CYP3A; Dioxoles; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Hepatocytes; Inhibitory Concentration 50; Lignans; Male; Microsomes, Liver; Plants, Medicinal; Polycyclic Compounds; Rats; Rats, Sprague-Dawley; RNA, Messenger; Schisandra

Three-days successive p.o. administration of an EtOH extract of the stems of Kadsura heteroclita (Schizandraceae) or its major constituent, kadsurin, resulted in significant decreases of CCl4-induced lipid-peroxidation products, such as thiobarbituric acid reactive substances (TBA-RS), conjugated dienes and fluorescent products in the liver of mice. In contrast, a significant restoration of superoxide dismutase (SOD) activity reduced by CCl4-intoxication was observed in the administered groups, suggesting that the subchronic treatment of mice with the EtOH extract or kadsurin induce enzymes capable of scavenging oxygen radical species in the liver, though the extract and kadsurin themselves may have an anti-oxidant property.

Topics: Animals; Antioxidants; Carbon Tetrachloride; Cyclooctanes; Dioxoles; Drugs, Chinese Herbal; Glutathione; Lignans; Lipid Peroxidation; Liver; Male; Mice; Superoxide Dismutase