Bok Hee Kim

Synthesis and evaluation of antitumor activity of novel 1,4-Naphthoquinone derivatives (IV)

Abstract1,4-Naphthoquinones are widely distributed in nature and many clinically important antitumor drugs containing a quinone moiety, such as anthracyclines, mitoxantrones and saintopin, show excellent anticancer activity. In this study, 2- or 6-substituted 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) and 5,8-dihydroxy-1,4-naphthoquinone (DHNQ) derivatives were synthesized, and their cytotoxic activity against L 1210 and P388 cancer cells was examined. Their antitumor activity was also assessed in mice bearing S-180 cells in the peritoneal cavity. In comparison with the DMNQ derivatives, the DHNQ derivatives exhibited more potent bioactivities than the DMNQ derivatives against both L 1210 and P388 cellsin vitro and S-180 cellsin vivo. The ED50 values of the DHNQ derivatives against P388 cells were in the range of 0.18–1.81 μg/mL whereas those of the DMNQ derivatives were in the range of 0.26–40.41 μg/mL. The T/C (%) values of the DHNQ derivatives,8, 17, 18, 19, and20, were found to be comparable to or even better than that of adriamycin. It was also observed that the 2-substituted derivatives (8, 19, 20) showed better antitumor activity than the 6-substituted derivatives (7, 17, 18) in the mice bearing S-180 cells in the peritoneal cavity.

Under-reporting of Energy Intake from 24-hour Dietary Recalls in the Korean National Health and Nutrition Examination Survey

Objectives Chronic degenerative diseases are closely related to daily eating habits, nutritional status, and, in particular, energy intake. In clarifying these relationships it is very important for dietary surveys to report accurate information about energy intake. This study attempted to identify the prevalence of the under-reporting of energy intake and its related characteristics based on the Korean National Health and Nutrition Examination Survey conducted in the years 2007–2009. Methods The present study analyzed dietary intake data from 15,133 adults aged ≥19 years using 24-hour dietary recalls. Basal metabolic rates were calculated from the age- and gender-specific equations of Schofield and under-reporting was defined as an energy intake <0.9, represented by the ratio of energy intake to estimated basal metabolic rate. Results Under-reporters (URs) accounted for 14.4% of men and 23.0% of women and the under-reporting rate was higher in the age group 30–49 years for both men and women. The results from an analysis of the age-specific socioeconomic characteristics of participants classified as URs showed that under-reporting was high in women living alone and in women with only elementary school education or no education. The results from an analysis of the health-specific characteristics of URs showed that a large proportion of URs had poor self-rated health or were obese, or both, compared with non-URs. The proportion of participants who consumed less than the estimated average requirements for nutrients was significantly higher in URs compared with non-URs. Conclusion The under-reporting of energy intake was associated with age, gender, education level, income level, household status (single-person or multi-person), self-rated health, physical activity, and obesity.

Comparative study on the antioxidant and nitrite scavenging activity of fruiting body and mycelium extract from Pleurotus ferulae

We investigated the effects of the antioxidant and the nitrite scavenging activities of the extracts from Pleurotus ferulae fruiting body grown on the solid state using corn cob and activated bleaching earth (CCABE media) and its mycelium grown in the liquid state. The total phenol and polysaccharide concentrations in hot water extract of fruiting body were approximately 3.6- and 4.3-fold higher than those of the mycelium. Using the hot water extract of fruiting body, the maximum DPPH radical scavenging activity at 9 mg/mL, hydroxyl radical scavenging activity at 12mg/mL, reducing power at 12 mg/mL, and chelating ability at 12 mg/mL were obtained, 80.5%, 72.4%, 0.99 OD (700 nm), and 77.0%, respectively. However, in the case of hydrogen peroxide scavenging activity, the ethanol extract was the highest, 78.7% at 12 mg/mL. The maximum nitrite scavenging activity was obtained, 89.7% at 6 mg/mL of hot water extract from fruiting body. Hot water extracts were more effective than ethanol extracts in scavenging activity on DPPH radicals and hydroxyl radical scavenging, reducing power, and chelating activity of ferrous, whereas ethanol extracts were more effective in hydrogen peroxide scavenging activity as evidenced by their lower EC50 values. These results indicate that the hot water extract of P. ferulae fruiting body using CCABE media has good potential to be used as a source of materials or additives for oxidation suppressant in food, cosmetics and drug compositions.

Effects of water-soluble tacrolimus-PEG conjugate on insulin-dependent diabetes mellitus and systemic lupus erythematosus

The effects of a water-soluble tacrolimus-PEG conjugate (KI-102) on insulin-dependent diabetes mellitus and systemic lupus erythematosus were investigated. KI-102 was stable at pH 4.0–4.5 and 4°C. The area under the concentration-time curve, the time of maximum concentration, and the maximum concentration were 43.4 ng·h/mL, 0.85 h, and 8.1 ng/mL, respectively, similar to those of FK506. Mice that administered KI-102 at 4.32 mg/kg had the plasma glucose concentrations that decreased to 7.5 mmol/L after 170 days, similar to that of mice administered FK506 at 0.6 mg/kg. There were no incidences of diabetes when KI-102 was administered at 86.4 mg/kg after 24 weeks. The group that administered 43.2 mg/kg had decreases in the concentrations of β-hydroxybutyrate (60%), triglyceride (24%), and cholesterol (30%). KI-102 administered at 180 mg/kg reduced serum anti-dsDNA antibody activity by 64% compared with a control. Urinary albumin concentration in the same group decreased 81% compared with the control. These results indicate that KI-102 may be practically applicable as prodrug of FK506.