• Biomolecules & Therapeutics
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• v.23 no.2
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• pp.201-206
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• 2015

Scutellaria baicalensis is one of the most widely used herbal medicines in East Asia. Because baicalein and baicalin are major components of this herb, it is important to understand the effects of these compounds on drug metabolizing enzymes, such as cytochrome P450 (CYP), for evaluating herb-drug interaction. The effects of baicalin and baicalein on activities of ethoxyresorufin O-deethylase (EROD), methoxyresorufin O-demethylase (MROD), benzyloxyresorufin O-debenzylase (BROD), p-nitrophenol hydroxylase and erythromycin N-demethylase were assessed in rat liver microsomes in the present study. In addition, the pharmacokinetics of caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) in baicalin-treated rats were compared with untreated control. As results, EROD, MROD and BROD activities were inhibited by both baicalin and baicalein. However, there were no significant differences in the pharmacokinetic parameters of oral caffeine and its three metabolites between control and baicalin-treated rats. When the plasma concentration of baicalin was determined, the maximum concentration of baicalin was below the estimated $IC_{50}$ values observed in vitro. In conclusion, baicalin had no effects on the pharmacokinetics of caffeine and its metabolites in vivo, following single oral administration in rats.

• Toxicological Research
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• v.17
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• pp.127-133
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• 2001

Together with cytochrome P450 (CYP), flavin-containing monooxygenase (FMO) present in liver microsomes oxidizes various endogenous and exogenous chemicals. In an effort to determine the human FMO activity, we have developed two non-invasive urine analysis methods using caffeine (CA) and ranitidine (RA) as the probe compounds. As the production of theobromine (TB) and ranitidine N-oxide (RANO) from CA and RA is catalyzed primarily by the hepatic FMO, we have assigned the urinary molar ratios of TB/CA and RA/RANO as the in vivo FMO activity. In 200 age-matched Korean volunteers, the obtained TB/CA ratio ranged from 0.4 to 15.2 (38-fold difference) and the RA/RANO ratio from 5.7 to 27.2 (4.8-fold). The FMO activity of 20's, determined by caffeine metabolism, was the highest (2.5$\pm$l.9) and those of 30's, 40's, 50's, 60's and 70's were 40%, 50%, 24%, 39% and 36% of the 20's, respectively. Intake of grapefruit juice, known to contain flavonoids, inhibited the in vivo FMO (TB/CA) activity by 79%. Addition of the flavonoids like naringin, quercitrin and kaempferol, present in grapefruit juice, to the in vitro microso-mal FMO assay, thiobenzamide S-oxidation, produced 75%, 70% and 60% inhibition, respectively. Obtained Ki values of quercitrin, kaempferol and naringin on the in vitro FMO activity were 6.2, 12.0 and 13.9 $\mu\textrm{M}$, respectively. This suggested that the dose of drug should need to be adjusted to suit the individual FMO activities when the drugs metabolized by FMO are given to patients. As the intake of grapefruit juice has been identified to inhibit the FMO as well as CYP3A4 and lA2 activities, patients taking drugs metabolized by these enzymes should not drink grapefruit juice as the carrier.

• Korean Journal of Food Science and Technology
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• v.38 no.1
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• pp.5-9
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• 2006

Method for separation and quantification of methylxanthins, catechins, and theaflavins in Korean commercial teas (green, oolong, and black teas) was developed using reversed phase high-performance liquid chromatography (HPLC). After extraction with hot water, tea compounds were separated on Inertsil ODS-3v $(5\;{\mu}m)$ column, eluted with gradient of 7% acetonitrile and 93% of 20 mM phosphate buffer mixture for 7 min. Column effluent was monitored at 270 nm. This technique was effective for analyses of m methylxanthins, catechins, and theaflavins in teas and biological samples. In green and oolong teas, two kinds of methylxanthins and 7 of catechins were identified, whereas 4 theaflavins were only identified in black tea. Among seven catechins in green and oolong teas, EGCG showed highest amount, whereas ECG was highest in black tea. (theaflavins were found only in black teas) In all teas, theobromine content was lower than that of caffeine.

• Toxicological Research
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• v.13 no.1_2
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• pp.117-125
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• 1997

In order to assess the possibility whether CYP2D is involved in caffeine metabolism, we have purified and characterized the rat liver microsomal cytochrome P4502D1 (CYP2D1), equivalent to CYP2D6 in human liver, and have utilized the reconstituted CYP2D1 in the metabolism of 4 primary caffeine (1, 3, 7-trimethylxanthine) metabolites such as paraxanthine (1, 7-dimethylxanthine), 1, 3, 7-trimethylurate, theophylline (1, 3-dimethylxanthine) and theobromine (3, 7-dimethylxanthine). Rat liver CYP 2D1 has been purified to a specific content of 8.98 nmole/mg protein (13.4fold purification, 1.5% yield) using $\omega$-aminooctylagarose, hydroxlapatite, and DE52 columns in a sequential manner. As judged from sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE), the purified CYP2D1 was apparently homogeneous. Molecular weight of the purified CYP2D1 was found to be 51, 000 Da. Catalytic activity of the purified and then reconstituted CYP2D1 was confirmed by using bufuralol, a known subsFate of CYP2D1. The reconstituted CYP2D1 was found to produce to 1-hydroxylbufuralol at a rate of 1.43$\pm$0.13 nmol/min/nmol P450. The kinetic analysis of bufuralol hydroxylation indicated that Km and Vmax values were 7.32$\mu M$ and 1.64 nmol/min/nmol P450, respectively. The reconstituted CYP2D1 could catalyze the 7-demethylation of PX to 1-methylxanthine at a rate of 12.5 pmol/min/pmol, and also the 7- and 3- demethylations of 1, 3, 7-trimethylurate to 1, 3-dimethylurate and 1, 7-dimethylurate at 6.5 and 12.8 pmol/min/pmol CYP2D1, respectively. The reconstituted CYP2D1 could also 3-demethylate theophylline to 1-methylxanthine at 5 pmol/min/pmol and hydroxylate the theophylline to 1, 3-dimethylurate at 21.8 pmol/min/pmol CYP2D1. The reconstituted CYP2D1, however, did not metabolize TB at all (detection limits were 0.03 pmol/min/pmol). This study indicated that CYP2D1 is involved in 3-and 7-demethylations of paraxanthine and theophylline and suggested that CYP2D6 (equivalent to CYP2D1 in rat liver) present in human liver may be involved in the secondary metabolism of the primary metabolites of caffeine.

• Korean Journal of Food Science and Technology
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• v.43 no.6
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• pp.719-722
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• 2011

The Daecha-12 and Yabukita varieties of powdered green teas were grown under 85% shade-cultivated condition, and their physicochemical properties were analyzed. Total catechin content was not significantly different but, non-gallated catechin content in Daecha-12 was significantly higher than that in Yabukita. Theanine (32%), caffeine (14%), lutein (15%) and total chlorophyll (28%) levels were significantly higher in Daecha-12 than those in Yabukita. The results of a color analysis showed that the lightness L-value of Yabukita was higher than that of Daecha-12 but, that the greenness negative a-value and b-values of Daecha-12 were higher than those of Yabukita. The Daecha-12 cultivar had lower catechin content but higher content of theanine, caffeine, theobromine, lutein, chlorophyll, and a negative a-value than those of the Yabukita cultivar. Thus, the Daecha-12 cultivar is suitable to prepare a high-quality powdered green tea product.

• Korean Journal of Food Science and Technology
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• v.18 no.1
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• pp.16-23
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• 1986

Physico-chemical and sensory characteristics of 28 black tea samples prepared by oaring the mixing ratio of 1 kind of Korean and 9 kinds of foreign black tea were determined, and their relationship was statistically analysed. Korean black tea was found to be lower in bulk density, caffeine, theobromine, crude protein, theaflavin, thearubigin and soluble solids, and higher in Hunter L- and b- value, neutral detergent fiber, calcium and ratio of oxidized matter as compared with foreign black tea. The palatability for 8 kinds of foreign black tea was generally increased by mixing with Korean black tea. The number of black tea whose palatability were higher than that of Korean black tea was 12, which was mostly mixed black tea. Theaflavin. Hunter a-value, soluble solids of the tea infusion, and potassium of the manufactured tea were the major guiding characteristics as a result of stepwise multiple regression analysis, and about 67% of the total variations in the palatability of black tea could be explained by the regression equation formulated by the preceding 4 characteristics.

• Journal of the East Asian Society of Dietary Life
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• v.17 no.3
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• pp.409-416
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• 2007

This study investigated changes in the catechin and alkaloid contents of Bosung green tea during different manufacturing processes and storage periods, using HPLC and UV-VIS spectrophotometer analysis. For changes in the catechin and alkaloid contents by roasting technique, we found that EGCG, CG and GCG decreased just slightly by processes performed before roasting, rather than after roasting. In addition, theobromine, caffeine, and ECG changed minimally throughout all the processes. For changes in the catechin and purine alkaloid contents of the green tea leaves during storage, EGCG, ECG, and CAF decreased considerably in the green tea stored at temperatures of $5^{\circ}C$ and $25^{\circ}C$, and they decreased by $20{\sim}30%$ after storage for 1 year. However, a quantitative difference was hardly observed in the catechin and alkaloid contents regardless of storage temperature.