• The Korea Journal of Herbology
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• v.23 no.3
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• pp.53-60
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• 2008

Objectives : Oxidative stress has a critical role in neurodegenerative diseases. In this study, we investigated the antioxidant and neuroprotective effects of the ethanolic extract of Banryong-hwan (BRHE) in SH-SY5Y cells and primary rat mesencephalic dopaminergic neurons. Methods : To assess the antioxidant effects, we carried out 1,1-diphenyl-2-picrylhydrazyl(DPPH) free radical scavenging assay, 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid)(ABTS) radical cation decolorization assay, and determination of total polyphenolic content. We evaluated the effect of BRHE treatment on neuroprotection against 6-hydroxydopamine(6-OHDA) toxicity using thiazolyl blue tetrazolium bromide(MTT) assay, nitric oxide(NO) assay, reactive oxygen species(ROS) assay in SH-SY5Y cells and tyrosine hydroxylase(TH) immunocytochemistry in primary rat mesencephalic dopaminergic neurons. Results : BRHE showed IC50 values of 328.10 ${\mu}g/mL$ and 43.12 ${\mu}g/mL$ in DPPH assay and in ABTS assay, respectively. Total polyphenolic content was 180.76 ${\mu}g/mL$. In SH-SY5Y cells, BRHE significantly attenuated the toxicity induced by 6-OHDA at the concentrations of 25-100 ${\mu}g/mL$ pre- and post- treatment in MTT assay. While 6-OHDA increased the NO and ROS contents, BRHE decreased them in a dose dependent manner. Moreover, in primary dopaminergic neuron culture, BRHE significantly protect-ed the dopaminergic cell loss against 6-OHDA toxicity up to 136% at the concentration of 75 ${\mu}g/mL$. Conclusions : These results demonstrate that BRHE has neuroprotective effect against 6-OHDA induced neurotoxicity through decreasing NO and ROS generation.

• Bulletin of the Korean Chemical Society
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• v.34 no.5
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• pp.1421-1424
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• 2013

Two new isoflavanones, (3R) 5,7,3',4'-tetrahydroxy-2'-methoxyisoflavanone (1) and (3R) 5',8-di-(${\gamma}$,${\gamma}$-dimethylallyl)-2',5-dihydroxyl-4',7-dimethoxyl-isoflavanone (2), were isolated from Uraria clarkei, together with two known compounds dalbergioidin (3), 5,7-dihydroxy-2',4'-dimethoxyisoflavanone (4). The structures involving the absolute configuration of the new compounds were well elucidated by MS, IR, UV, CD, 1D and 2D NMR analyses. Cytotoxicity of the four compounds were assessed, results suggested that compound 2 possessed well cytotoxic activity, against the Hela, K562, and HL60 cell lines with $IC_{50}$ values of 28.0, 40.6 and $35.1{\mu}M$, respectively.

• YAKHAK HOEJI
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• v.43 no.5
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• pp.642-651
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• 1999

Nonsedating antihistamines do net cause sedation in therapeutic doses because these drugs hardly cross the blood-brain barrier. Since most of the peripheral side dffects of conventional antihistamines are related to their muscarinic receptor blocking action, the present study was performed to investigate whether nonsedating antihistamines interact with the muscarinic receptors and discriminate the muscarinic receptor subtypes in the rat cerebral microsomal fraction which containes both $M_1,{\;}M_2,{\;}M_3{\;}and{\;}M_4$ receptors. Five nonsedating antihistamines at high concentrations inhibited [$^3H$]QNB binding to the muscarinic receptor in a dose-dependent manner. The inhibition curves of these drugs except loratadine which showed positive cooperativity (nH=1.55) were steep (nH=1), indicating interaction with a single homogenous population of the binding sites. Astemizole, clemizole and mequitazine increased the $K_D$ value for [$^3H$]QNB without affecting the binding site concentrations, and this increase in the $K_D$ value resulted from the ability of these drugs to slow [$^3H$]QNB-receptor association. The Ki values of astemizole, clemizole and mequitazine for the inhibition for the inhibition of [$^3H$]QNB binding to muscarinic receptor were 0.58, 5.99 and $0.007{\;}{\mu}M$, respectively. However, loratadine and terfenadine inhibited noncompetitively [$^3H$]QNB binding with the normalized $IC_50$ value of about $2{\;}{\mu}M$. These results demonstrate that; 1) astemizole, clemizole and mequitazine interact directly with the muscarinic receptor at high concentrations; 2) muscarinic receptor blocking potency of these drugs varies widely among drugs; 3) these drugs do not discriminate between muscarinic receptor subtypes.

• Preventive Nutrition and Food Science
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• v.19 no.4
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• pp.281-290
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• 2014

The aim of the present study was to evaluate the anti-diabetic, anti-inflammatory, antioxidant potential, and total phenolic content (TPC) of green and red kohlrabi cultivars. Anti-diabetic and anti-inflammatory activities were evaluated via protein tyrosine phosphatase (PTP1B) and rat lens aldose reductase inhibitory assays and cell-based lipopolysaccharide (LPS)-induced nitric oxide (NO) inhibitory assays in RAW 264.7 murine macrophages. In addition, scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical, and peroxynitrite ($ONOO^-$) were used to evaluate antioxidant potential and TPC was selected to assess phytochemical characteristics. Between the two kohlrabi cultivars, red kohlrabi (RK) had two times more TPC than green kohlrabi (GK) and showed significant antioxidant effects in DPPH, ABTS, and $ONOO^-$ scavenging assays. Likewise, methanol (MeOH) extracts of RK and GK inhibited LPS-induced NO production in a dose dependent manner that was further clarified by suppression of iNOS and COX-2 protein production. The MeOH extracts of RK and GK exhibited potent inhibitory activities against PTP1B with the corresponding $IC_{50}$ values of $207{\pm}3.48$ and $287{\pm}3.22{\mu}g/mL$, respectively. Interestingly, the RK MeOH extract exhibited significantly stronger anti-inflammatory, anti-diabetic, and antioxidant effects than that of GK MeOH extract. As a result, our study establishes that RK extract with a higher TPC might be useful as a potent anti-diabetic, antioxidant, and anti-inflammatory agent.

• Preventive Nutrition and Food Science
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• v.18 no.3
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• pp.163-168
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• 2013

In this study, we investigated the inhibitory effects of Baechu kimchi added Ecklonia cava on the activities of ${\alpha}$-glucosidase and ${\alpha}$-amylase and its alleviating effect on the postprandial hyperglycemia in STZ-induced diabetic mice. Baechu kimchi added Ecklonia cava (BKE, 15%) was fermented at $5^{\circ}C$ for 28 days. Optimum ripened BKE was used in this study as it showedthe strongest inhibitory activities on ${\alpha}$-glucosidase and ${\alpha}$-amylaseby fermentation time among the BKEs in our previous study. The BKE was extracted with 80% methanol and the extract solution was concentrated, and then used in this study. The BKE extract showed higher inhibitory activities than Baechu kimchi extract against ${\alpha}$-glucosidase and ${\alpha}$-amylase. The $IC_{50}$ values of the BKE extract against ${\alpha}$-glucosidase and ${\alpha}$-amylase were 0.58 and 0.35 mg/mL, respectively; BKE exhibited a lower ${\alpha}$-glucosidase inhibitory activity but a higher ${\alpha}$-amylase inhibitory activity than those of acarbose. The BKE extract alleviated postprandial hyperglycemia caused by starch loading in normal and streptozotocin- induced diabetic mice. Furthermore, the BKE extract significantly lowered the incremental area under the curve in both normal and diabetic mice (P<0.05). These results indicated that the BKE extract may delay carbohydrate digestion and thus glucose absorption.

• Korean Journal of Food Science and Technology
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• v.42 no.6
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• pp.755-761
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• 2010

The quinone reductase (QR) inducing activities of mung bean and soybean solvent extracts were compared using murine hepatoma cells (Hepa 1c1c7). The mung bean extracts (ethylacetate and ethanol) showed higher chemoprevention index values (7.88-8.22) than those of soybean extracts (2.9-5.2) from four different cultivars. The mung bean extracts also had significantly higher inhibitory effects (47-62% at 100 ${\mu}g$/mL) than the soybean extracts (15-42% at 100 ${\mu}g$/mL) against the production of nitric oxide and prostaglandin E2 in lipopolysccharide stimulated macrophage RAW264.7 cells without cytotoxicity. Among seven recovered fractions of mung bean ethanol extract obtained by C 18 silica flash column chromatography, the most non-polar fraction exhibited the highest chemoprevention index of 10.4.

• Journal of Microbiology and Biotechnology
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• v.9 no.6
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• pp.798-803
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• 1999

Prolyl endopeptidase [PEP; EC 3.4.21.26], a serine protease which is known to cleave peptide bonds on the carboxy side of a proline residue, plays an important role in the degradation of proline-containing neuropeptides that have been suggested to participate in learning and memory processes. An abnormal increase in the level of PEP, which can lead to generation of $A{\beta}$, is also suggested to be involved in Alzheimer's type senile dementia. In the course of screening PEP inhibitors from Basidiomycetes, the mushroom Polyozellus multiplex exhibited a high inhibitory activity against PEP. Two active compounds were isolated from the ethyl acetate soluble fraction by consecutive purification, using silica gel, Sephadex LH-20, and Lobar RP-18 chromatography. The chemical structures of these compounds were identified as thelephoric acid and 12-acety1-2,3,7,8-tetrahydroxy-[12H]-12-hydroxymethylbenzobis[I.2b,3.4b'] benzofuran-11-one (kynapcin-9) by spectral data including UV, IR, MS, HR-MS, $^1H-,{\;}^{13}C-$, and 2D-NMR. The $IC_{50}$ values of the thelephoric acid and kynapcin-9 were 0.157 ppm (446nM) and 0.087 ppm (212nM) and their inhibitor constants ($K_i$) were 0.73ppm ($2.09{\;}\mu\textrm{m}$) and 0.060 ppm (146 nM), respectively. Furthermore, they were non-competitive with a substrate in Dixon plots.

• Journal of the Korean Magnetic Resonance Society
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• v.23 no.4
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• pp.87-92
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• 2019

Allium hookeri (Liliaceae) has been received the increasing attention as a bioactive resource due to its potent biological activities including anti-oxidant, anti-obesity, anti-microbial and lipid-regulating activities. The beneficial effects of A. hookeri are known contributed from the high content of organosulfur compounds in A. hookeri. Though a variety of articles demonstrated that A. hookeri contains 'saponin' as a bioactive constituent, the scientific evidence to prove it was limited. In the present study, we have attempted to identify saponin contained in A. hookeri through chromatographic isolation and NMR spectroscopic methods. As a result, a spirostane-type steroidal saponin (1) has been successfully isolated from the methanolic extract of A. hookeri roots. The structure of 1 was elucidated by extensive 1D and 2D spectroscopic methods including ¹H-NMR, ¹³C-NMR, ¹H-¹H COSY, HSQC, HMBC and NOESY; identified as (3β, 22R, 25S)-spirost-5-en-3yl O-6-deoxy-α-L-mannopyranosyl-(1→4)-O-6-deoxy-α-L-mannopyranosyl-(1→4)-O-[6-deoxy-α-L-mannopyranosyl-(1→2)]-β-D-gluco pyranoside. 1 showed the significant inhibitory activity on mushroom tyrosinase with IC₅₀ values of 248.7 μM while the inhibition on alpha-glucosidase was not significant.

• Natural Product Sciences
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• v.16 no.2
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• pp.80-87
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• 2010

High performance liquid chromatography (HPLC) analysis on the MeOH extract of Ligularia stenocephala leaves identified six caffeoylquinic acids, viz. 3,4-di-O-caffeoylquinic acid, 3,5-di-O-caffeoyl-mucoquinic acid, 3,5-di-O-caffeoylquinic acid, 4,5-di-O-caffeoylquinic acid, 5-O-caffeoylquinic acid, and 3-Ocaffeoylquinic acid using standard compounds, and determined the quantity of each extract. Percentage of total caffeoylquinic acids of the MeOH extract and its BuOH fraction were calculated as $67.83{\pm}3.79%$ and $94.52{\pm}1.84%$, respectively. Since the caffeoylquinic acid-rich MeOH extract exhibited a potent peroxynitrite-scavenging effect in vitro ($IC_{50}=0.87{\pm}0.33\;{\mu}g/ml$ (mean $\pm$ SEM)), the experiment was designed to identify whether or not that extract has an anti-obesity effect on rat obesity induced by high fat diet. Oral administration of the MeOH extract and its BuOH fraction abundant in caffeoylquinic acid decreased the rat body weight to the level of untreated group and decreased abdominal fat pad weight. The atherogenic index and thiobarbituric acid-reactive substance (TBARS) values were restored by treatment, indicating that the caffeoylquinic acid-rich extract probably inhibited hyperlipidemia and oxidative stress caused by high fat diet. These results suggest that L. stenocephala in vegetable form or its caffeoylquinic acid-rich fraction (BuOH fraction) as an agent can be used for treatment or prevention of obesity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.1
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• pp.187-192
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• 2006

Herbal medicines have been utilized to treat a variety of diseases, including cancer. Several species of the family rubiaceae have been reported to have antitumor activity. In this study, we report the cytotoxicity and antitumor activity exhibited dy the methanol extracts prepared from Rubia radix (RRME), Uncaria gambir (UGME) and Oldenlandia diffusa (ODME) (family: Rubiaceae) against human promyleloid leukemia cell line, HL-60. The cytotoxicity of RRME (2~20 ${\mu}g/ml$), UGME (20~200 ${\mu}g/ml$) and ODME (20~200 ${\mu}g/ml$) were assessed dy the MTT reduction assay. IC50 values for RRME, UGME and ODME were 11.0, 99.5 and 106.1 ${\mu}g/ml$, respectively. When the HL-60 cells were treated with RRME (10 ${\mu}g/ml$), UGME (120 ${\mu}g/ml$) and ODME (140 ${\mu}g/ml$) for 24 h, several apoptotic characteristics such as DNA fragmentation and morphologic changes were observed. Furthermore, flow cytometric analysis was peformed to determine the percent of apoptotic cells. The poupulation of sub-G1 hypodiploid cells was increased 37.49% in RRME treatment, 12.49% in UGME treatment and 7.21% in ODME treatment compared with untreated control cells (2.64%). To further confirm apoptotic cell death, we assayed caspase-3, -8 and -9 activities in RRME, UGME and ODME-treated cells. After treatment of RRME, UGME and ODME for 12 h, caspase-3, -8 and -9 activities significantly increased.compared to untreated control cells. These results show that RRME, UGME and ODME induced apoptotic cell death in HL-60 cells and may have a possibility of potential antitumor activities.