Seung Yu Kim

Anti-inflammatory Activity of Medicinal Plant Extracts

The study was conducted to investigate candidate materials as anti-inflammation agent from plant resources. Activities of 33 plant parts extracts with the final concentration of 5μg/ml were evaluated on the several inflammationrelated markers such as the release of proinflammatoty cytokine [tumor necrosis factor-alpha (TNF-α) & interleukin-6 (IL6)], nitric oxide (NO), the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and inhibitor of nuclear factor kappa-B alpha (Iκ-Bα) in lipopolysaccharide (LPS)-treated RAW 264.7 cells. The extracts in the final concentration of 10μg/ml were also screened on peroxynitrite (ONOO−) scavenging activity. Eleven extracts selected from the screening assay were verified on the inhibition activity on peroxynitrite and total reactive species oxygen (ROS) in the several concentrations. As results, Alpinia officinarum Hance (rhizome), Inula britannica var. chinensis Regel (flower), Ulmus arvifolia Jacq (trunk peel) and Aster scaber Thunb. (aerial part) showed comparatively potent anti-inflammatory activities in vitro cells or chemical level systems, and then these four plant parts should be studied on the antiinflammatory mechanism by further studies.

A direct protein kinase B-targeted anti-inflammatory activity of cordycepin from artificially cultured fruit body of Cordyceps militaris.

Background: Cordyceps militaris is one of well-known medicinal mushrooms with anti-inflammatory, anti-cancer, anti-diabetic, and anti-obesity activities. Objective: The objective of the following study is to isolate chemical components from the ethanol extract (Cm-EE) from Cordyceps militaris and to evaluate their anti-inflammatory activities. Materials and Methods: Column chromatographic separation was performed and anti-inflammatory roles of these compounds were also examined by using NO production and protein kinase B (AKT) activity assays. Results: From Cm-EE, 13 constituents, including trehalose (1), cordycepin (2), 6-hydroxyethyladenosine (3), nicotinic amide (4), butyric acid (5), β-dimorphecolic acid (6), α-dimorphecolic acid (7), palmitic acid (8), linoleic acid (9), cordycepeptide A (10), 4-(2-hydroxy-3-((9E,12E)-octadeca-9,12-dienoyloxy)propoxy)-2-(trimethylammonio)butanoate (11), 4-(2-hydroxy-3-(palmitoyloxy)propoxy)-2-(trimethylammonio)butanoate (12), and linoleic acid methyl ester (13) were isolated. Of these components, compound 2 displayed a significant inhibitory effect on NO production in lipopolysaccharide (LPS)-activated RAW264.7 cells. Furthermore, this compound strongly and directly suppressed the kinase activity of AKT, an essential signalling enzyme in LPS-induced NO production, by interacting with its ATP binding site. Conclusion: C. militaris could have anti-inflammatory activity mediated by cordycepin-induced suppression of AKT.

Chemical constituents of Hericium erinaceum associated with the inhibitory activity against cellular senescence in human umbilical vascular endothelial cells

Abstract Hericium erinaceum is an edible and medicinal mushroom widely used in Korea, Japan, and China. On the search for biologically active compounds supporting the medicinal usage, the MeOH extract of the fruiting bodies of H. erinaceum was investigated for its chemical constituents. Six compounds were isolated and identified as hericenone D (1), (22E,24R)-5α,8α-epidioxyergosta-6,22-dien-3β-ol (2), erinacerin B (3), hericenone E (4), hericenone F (5) and isohericerin (6) by comparing their spectroscopic data with previously reported values. The inhibitory effects on adriamycin-induced cellular senescence in human dermal fibroblasts (HDFs) and human umbilical vein endothelial cells (HUVECs) of the isolates (1–6) were studied. Among the isolated compounds, ergosterol peroxide (2) reduced senescence associated β-galactosidase (SA-β-gal) activity increased in HUVECs treated with adriamycin. According to experimental data obtained, the active compound may inspire the development of a new pharmacologically useful substance to be used in the treatment and prevention of age-related diseases.

Investigation of Shikonin Pigments and Antioxidant activity of the Roots from Lithospermum erythrorhizon according to the Different Growth Stages and Areas of Cultivation

This study was conducted to evaluate the quality variation of Lithospermum radix on the pigment contents and antioxidant activities according to different growth stages and areas of cultivation. Acetylshikonin contents showed the tendency to decrease gradually from the middle of July (0.28%) to the end of August (0.05%) and then the content was increased again to the end of October (0.25%). Shikonin content was detected as small amount of about 0.009% during the period. The weight of plants was increased from the end of September to the end of October and showed the highest value as 19.8 g on October 25. ROS scavenging activity was the highest in the early of October as IC50 value of 0.11 ㎍/mL. Lithosper- mum radix of September showed lower ROS scavenging activities than those of other growth stages as IC50 value of 1.02 and 0.49 ㎍/mL on September 9 and September 27, respectively. Among 17 areas cultivated Lithospermum radix, 10 areas (59%) showed 0.05-0.10% of acetylshikonin contents and 3 areas (18%) were measured to contain 0.16-0.26% of acetylshikonin.

Benzyl alcohol derivatives from the mushroom Hericium erinaceum attenuate LPS-stimulated inflammatory response through the regulation of NF-κB and AP-1 activity

Abstract On the search for anti-inflammatory compounds from natural Korean medicinal sources, a bioassay-guided fractionation and chemical investigation of the MeOH extract from the fruiting bodies of Hericium erinaceum resulted in the isolation and identification of five benzyl alcohol derivatives (1–5). In this study, their anti-inflammatory effects on lipopolysaccharide (LPS)-induced production of pro-inflammatory mediators were examined using RAW 264.7 macrophage cells. The structures of isolates were identified by comparing their spectroscopic data with previously reported values. The analysis of their inhibitory activities on LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production in RAW 264.7 macrophage cells showed that erinacerin B (2) and hericenone E (4) decreased the levels of NO and PGE2 production in a concentration-dependent manner. Next, this study was performed to examine their mechanism of action on the regulation of NO and PGE2 production. Compounds 2 and 4 were found to block the LPS-induced phosphorylation of two major inflammatory transcription factors, NF-κB (p65/p50) and AP-1 (c-Jun and c-Fos). Taken together, these results suggest that down-regulation of LPS-induced NO and PGE2 production by compounds 2 and 4 is mediated through the modulation of NF-κB and AP-1 activation in macrophage cells. These results impact the development of potential health products for preventing and treating inflammatory diseases.

The Neuroprotective Effect of White Ginseng (Panax ginseng C. A. Meyer) on the Trimethyltin (TMT)-Induced Memory Deficit Rats

The present study examined the effects of Korean white ginseng (WG, Panax ginseng C. A. Meyer) on the learning and memory function and the neural activity in rats with trimethyltin (TMT)-induced memory deficits. The rats were administered with saline or WG (WG 100 or 300 ㎎/㎏, p.o.) daily for 21 days. The cognitive improving efficacy of WG on the amnesic rats, which was induced by TMT, was investigated by assessing the Morris water maze test and by perform- ing immunohistochemistries on choline acetyltransferase (ChAT), acetylcholinesterase (AchE), cAMP responsive element binding protein (CREB) and brain derived neurotrophic factor (BDNF). The rats treated with TMT injection (control group) showed impaired learning and memory of the tasks, but the rats treated with TMT injection and WG administration produced significant improvement of the escape latency to find the platform in the Morris water maze at the 2nd and 4th days compared to that of the control group. In the retention test, the WG 100 and WG 300 groups showed significantly increased crossing number around the platform compared to that of the control group (p < 0.001). Consistently with the behavioral data, result of immunohistochemistry analysis showed that WG 100 ㎎/㎏ significantly alleviated the loss of BDNF-ir neurons in the hippocampus compared to that of the control group (p < 0.01). Also, treatment with WG has a trend to be increased the cholinergic neurons in the hippocampal CA1 and CA3 areas as compared to that of the control group. These results suggest that WG may be useful for improving the cognitive function via regulation of neurotrophic activity.

1H and 13C NMR spectral assignments of 18 novel polymethoxylated hydroxynaphthopyrazolylchalconoids

Among plant-derived polyphenols produced via phenylpropanoids pathway, chalcones are biosynthesized by a combination of 4-coumaroyl-CoA with malonyl-CoA. Chalcones are known as chalconoids (Figure 1A). They consist of two benzene rings connected via the α,β-unsaturated carbonyl group, which may close to form another ring, to give flavonoids with three rings. It was known that chalconoids act as potassium channel blockers and aromatase inhibitors. As reported previously, some chalconoids can be converted to flavonoids easily (Fig. 1B). Therefore, their stabilities remained to be solved to develop as biological active compounds. A substitution of α,β-unsaturated carbonyl group with pyrazoline group (pyrazolylchalconoids) can prevent the conversion of chalconoids to flavonoids (Fig. 1C). Methoxylation increases the cell permeability and stability of many plant-derived polyphenols. We designed hydroxynaphthopyrazolylchalconoids with hydroxynaphthyl A-ring and trimethoxylated B-ring (Fig. 1D), and synthesized 18 derivatives. Their NMR data and mass spectrometric (MS) data can help us to identify plant-derived polyphenols newly synthesized or isolated from natural sources in the future, thus, we report here the complete H and C NMR data and high-resolution MS data.

The Effect of Cosmetic on Anti-Wrinkle of Acer mono Sap

Department of Herbal Crop Research, NIHHS, RDA, Eumseong 369-873, Korea.ABSTRACT : The purpose of this study was to research for anti-oxidation and anti-wrinkle effects of Acar mono Sap (AM).To cosmetic effect of AM, safety effect (MTT assay), anti-wrinkle effect (elastase, MMP-1 inhibition assay) and anti-oxidanteffect (DPPH assay) were measured. When water extract of AM was used for cell viability, it was over 100% at 6% (6 ml/100 ml in phosphate buffer) concentration. AM showed 45.7% elastase inhibition and 23.7% MMP-1 inhibition at 50% (50 ml/100 ml in phosphate buffer) concentration so that it had good anti-wrinkle characteristic. And AM showed 68.9% antioxida-tion capacity at 50% concentration by using a DPPH assay. Consequently, AM can be used as natural materials or additives forhuman skin owing to their beneficial biologic functions, including the anti-wrinkle effect, for cosmetic compositions.Key Words : Acer mono Sap, Anti-Wrinkle, Elastase

Evaluation on Extraction Conditions and HPLC Analysis Method for Bioactive Compounds of Astragali Radix

This study has been conducted to establish the optimal extraction process and HPLC analysis method for the determination of marker compounds as a part of the materials standardization for the development of health functional food materials from Astragali radix. Five extraction conditions including the shaking extraction at room temperature and the reflux extraction at 85°C with 30%, 50% and 95% ethanol were evaluated. Reflux extraction with 50% ethanol showed the highest extraction yield as 27.27 ± 2.27%, while the extraction under reflux with 95% ethanol showed significantly the lowest yield of 10.55 ± 0.24%. The quantitative determination methods of calycosin-7-O-β-D-glucoside and calycosin as marker compounds of Astragali radix extracts were optimized by HPLC analysis using a Thermo Hypersil column (4.6 × 250 mm, 5 μm) with the gradient elution of water and acetonitrile as the mobile phase at the flow rate of 0.8 mL min and a detection wavelength of 230 nm. The HPLC/UV method was applied successfully to the quantification of two marker compounds in Astragali radix extracts after validation of the method with the linearity, accuracy and precision. The contents of calycosin-7-O-β-D-glucoside and calycosin in 50% ethanol extracts by reflux extraction were significantly higher as 1,700.3 ± 30.4 and 443.6 ± 8.4 μg g-1, respectively, comparing with those in other extracts. The results indicate that the reflux extraction with 50% ethanol at 85°C is optimal for the extraction of Astragali radix, and the established HPLC method are very useful for the evaluation of marker compounds in Astragali radix extracts to develop the health functional material from Astragali radix.

Evaluation on Extraction Conditions and HPLC Analysis Method for Ginsenosides in Panax ginseng

Background : A new extraction method-heated ultrasonic extraction was qualitatively and quantitatively analyzed for the extraction of major ginsenosides from ginseng extract; this new high-performance liquid chromatography (HPLC) method was compared with the official extraction method of Korean industrial standards and standard for health functional food. Methods and Results : Ginsenoside compounds were analyzed for 35 minutes by the new HPLC analysis method using a Halo ® RP-Amide column. The new HPLC analysis method was validated by the measurement of intra-day and inter-day precision, accuracy, limit of detection (LOD), and limit of quantification (LOQ) of each ginsenoside. The correlation coefficients (r2) for the calibration curves of the ginsenoside compounds were over 0.9997 in terms of linearity. The heated ultrasonic extraction method using ultrasonication for 30 minutes at 50℃ yielded higher amount of ginsenosides than the extraction method of the Korean industrial standards owing to the enhancement of extraction efficiency. Conclusions : Compared to the other extraction methods, the heated ultrasonic extraction method yielded a higher amount of ginsenoside Rb1 than Rg1 index compounds for the quality evaluation of ginseng roots.