Biomaterial Database

Uptake of glycyrrhizin by isolated rat hepatocytes. 1993

S Ishida, and Y Sakiya, and T Ichikawa, and Z Taira

Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Japan.

The mechanism of uptake of glycyrrhizin (GLZ) by isolated rat liver cells was studied. The uptake rate was dependent on the unbound GLZ concentration. The initial uptake rate with respect to the unbound GLZ concentration reflected the operation of both saturable and nonsaturable processes, which followed Michaelis-Menten type kinetics; the process involves a Km of 11.3 microM, Vmax of 0.112 nmol/min/10(6) cells, and a first-order rate constant (Kd) of 0.195 nmol/min/10(6) cells/mM. GLZ adsorption on the cell membrane occurs at two types of binding sites with a linear adsorption coefficient = 2.81 nmol/10(6) cells/mM and a dissociation constant = 18.3 microM and its adsorption capacity = 0.12 nmol/10(6) cells describing specific adsorption. GLZ uptake did not require the presence of Na+ in the incubation medium and was not significantly inhibited by ouabain. The Arrhenius plot of uptake of 10 microM GLZ presented a single straight line in the range of 4-37 degrees C, with an activation energy of 15.9 kcal/mol. An energy requirement was also demonstrated, as all metabolic inhibitors studied (rotenone, antimycin A, 2,4-dinitrophenol, and KCN) significantly reduced the uptake of 10 microM GLZ (p < 0.01). The uptake was competitively inhibited by glycyrrhetinic acid (GLA), taurocholate (TCA), and probenecid (PBC) with inhibition constants, Ki, of 13.7, 48.5, and 115.9 microM, respectively, and it was noncompetitively inhibited by bromosulfophthalein (Ki 9.2 microM) and indocyanine green (Ki 13.5 microM) only at low GLZ concentrations (5 and 10 microM).(ABSTRACT TRUNCATED AT 250 WORDS)

UI	MeSH Term	Description	Entries
D007208	Indocyanine Green	A tricarbocyanine dye that is used diagnostically in liver function tests and to determine blood volume and cardiac output.	Cardio-Green,Cardiogreen,Ujoveridin,Vofaverdin,Vophaverdin,Wofaverdin,Cardio Green,Green, Indocyanine
D008099	Liver	A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.	Livers
D008297	Male		Males
D006034	Glycyrrhetinic Acid	An oleanolic acid from GLYCYRRHIZA that has some antiallergic, antibacterial, and antiviral properties. It is used topically for allergic or infectious skin inflammation and orally for its aldosterone effects in electrolyte regulation.	Enoxolone,Glycyrrhetic Acid,Rhetinic Acid,Uralenic Acid,Arthrodont,Glyciram,Glycyram,Jintan,Po 12,12, Po,Acid, Glycyrrhetic,Acid, Glycyrrhetinic,Acid, Rhetinic,Acid, Uralenic
D000327	Adsorption	The adhesion of gases, liquids, or dissolved solids onto a surface. It includes adsorptive phenomena of bacteria and viruses onto surfaces as well. ABSORPTION into the substance may follow but not necessarily.	Adsorptions
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D000963	Antimetabolites	Drugs that are chemically similar to naturally occurring metabolites, but differ enough to interfere with normal metabolic pathways. (From AMA Drug Evaluations Annual, 1994, p2033)	Antimetabolite
D000998	Antiviral Agents	Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.	Antiviral,Antiviral Agent,Antiviral Drug,Antivirals,Antiviral Drugs,Agent, Antiviral,Agents, Antiviral,Drug, Antiviral,Drugs, Antiviral
D001647	Bile Acids and Salts	Steroid acids and salts. The primary bile acids are derived from cholesterol in the liver and usually conjugated with glycine or taurine. The secondary bile acids are further modified by bacteria in the intestine. They play an important role in the digestion and absorption of fat. They have also been used pharmacologically, especially in the treatment of gallstones.	Bile Acid,Bile Salt,Bile Salts,Bile Acids,Acid, Bile,Acids, Bile,Salt, Bile,Salts, Bile
D012964	Sodium	A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.	Sodium Ion Level,Sodium-23,Ion Level, Sodium,Level, Sodium Ion,Sodium 23