• Journal of Applied Biological Chemistry
• /
• v.61 no.2
• /
• pp.187-190
• /
• 2018

Two curcumin derivatives, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), isolated from Curcuma longa were analyzed for their inhibitory activities against two isoforms of monoamine oxidase (MAO), which is involved in the catalysis of neurotransmitting monoamines. In the study, DMC and BDMC potently inhibited human MAO-B, with $IC_{50}$ values of 2.45 and $2.59{\mu}M$, respectively, and both compounds showed effective inhibitory activities against human MAO-A, with $IC_{50}$ values of 3.24 and $3.09{\mu}M$, respectively. The inhibitory activities of the two compounds were higher than those of curcumin. The removal of the methoxy or dimethoxy groups in curcumin might increase the inhibitory activities against human MAO-A and MAO-B. The inhibited activities were recovered to almost the values of the reversible references in the dialysis experiments with DMC and BDMC. DMC and BDMC showed competitive inhibition for MAO-A and MAO-B, respectively, with $K_i$ values of 0.91 and $0.80{\mu}M$, respectively. These results suggest that the two curcumin derivatives may be useful or lead compounds in the treatment of related disorders as potent reversible MAO inhibitors.

• Preventive Nutrition and Food Science
• /
• v.16 no.1
• /
• pp.89-94
• /
• 2011

The potential biological activities of water and ethanol extracts from two varieties of Rubus coreanus Miquel fruits produced in the Gochang-gun (GR) and Hoengseong-gun (HR) regions of Korea were examined. The hydroxyl radical ($\cdot$OH) scavenging activity, reducing power, lipid peroxidation inhibitory activity, and antiproliferative activity on cancer cells by these extracts were examined, and $\alpha$-amylase and $\alpha$-glucosidase inhibition assays were also performed. The EtOH extract from GR showed high hydroxyl radical scavenging activity ($EC_{50}=119.47{\pm}5.13\;{\mu}g/mL$), lipid peroxidation inhibitory activity ($EC_{50}=213.45{\pm}3.14\;{\mu}g/mL$) and a concentration dependence, with OD values ranging from 0.15 to 0.56 (50 to 200 ${\mu}g/mL$), for reducing power. The EtOH extract from GR has the highest antiproliferative activities on MDA-MB-231 and HepG2 cancer cells among four extracts. Meanwhile, all extracts showed certain $\alpha$-amylase and $\alpha$-glucosidase inhibition activities. These results indicate that extracts from two varieties of R. coreanus fruits have significant antioxidant, anti-diabetic and anti-tumorigenic activities, which suggest these extracts could be a potential source for pharmaceutical.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.8
• /
• pp.2593-2598
• /
• 2011

Polyphenols (PPs) are known as antioxidant compounds having benign biological activities. In this paper, a series of hybrid molecules between the free or acetyl protected polyphenol compounds were synthesized and their in vitro antioxidant activity (DPPH assay) and cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were evaluated. As expected, free phenolic hybrid compounds (6 and 8) showed better antioxidant activity than acetyl protected hybrid compounds (5 and 7) from DPPH assay. But the contrast result was obtained from BuChE inhibition assay. Acetyl protected hybrid compounds (5 and 7) showed better inhibition activity for BuChE than free phenolic hybrid compounds (6 and 8). Specifically, 10 (AcFA-AcFA) were shown as an effective inhibitor of BuChE ($IC_{50}=2.3{\pm}0.3{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 170 fold). Inhibition kinetic studies with acetyl protected compounds (5, 7, 9, and 10) indicated that 5, 7 and 10 are a hyperbolic mixed-type inhibition and 10 is a competitive inhibition type. The binding affinity (Ki) value of 10 to BuChE is $2.32{\pm}0.15{\mu}M$.

• Asian Pacific Journal of Cancer Prevention
• /
• v.15 no.13
• /
• pp.5455-5461
• /
• 2014

Background: Saponins are a major active component for the traditional Chinese medicine, Rubus parvifolius L., which has shown clear antitumor activities. However, the specific effects and mechanisms of saponins of Rubus parvifolius L. (SRP) remain unclear with regard to human chronic myeloid leukemia cells. The aim of this study was to investigate inhibition of proliferation and apoptosis induction effects of SRP in K562 cells and further elucidate its regulatory mechanisms. Materials and Methods: K562 cells were treated with different concentrations of SRP and MTT assays were performed to determine cell viability. Apoptosis induction by SRP was determined with FACS and DAPI staining analysis. Western blotting was used to detect expression of apoptosis and survival related genes. Specific inhibitors were added to confirm roles of STAT3 and AMPK pathways in SRP induction of apoptosis. Results: Our results indicated that SRP exhibited obvious inhibitory effects on the growth of K562 cells, and significantly induced apoptosis. Cleavage of pro-apoptotic proteins was dramatically increased after SRP exposure. SRP treatment also increased the activities of AMPK and JNK pathways, and inhibited the phosphorylation expression level of STAT3 in K562 cells. Inhibition of the AMPK pathway blocked the activation of JNK by SRP, indicating that SRP regulated the expression of JNK dependent oon the AMPK pathway. Furthermore, inhibition of the latter significantly conferred resistance to SRP pro-apoptotic activity, suggesting involvement of the AMPK pathway in induction of apoptosis. Pretreatment with a STAT3 inhibitor also augmented SRP induced growth inhibition and cell apoptosis, further confirming roles of the STAT3 pathway after SRP treatment. Conclusions: Our results demonstrated that SRP induce cell apoptosis through AMPK activation and STAT3 inhibition in K562 cells. This suggests the possibility of further developing SRP as an alternative treatment option, or perhaps using it as adjuvant chemotherapeutic agent for chronic myeloid leukemia therapy.

• The Korea Journal of Herbology
• /
• v.20 no.3
• /
• pp.83-92
• /
• 2005

Objectives : The physiological activities of Coptidis Rhizoma investigated for application as a cosmetic ingredients. Methods : We were experimented anti-oxidation effect, growth inhibition ability on cancer cells, antibacterial activity on various kinds of bacteria of skin. Results : The results were obtained as follows : Electron-donating ability(EDA) shows that Coptidis Rhizoma extracted with ethanol(94.51%) gives higher EDA in comparison to that extracted with water in 1000 ppm(63.24%). In the test of SOD-like activity, ethanol extract showed quite more activity with 81.01% in 1000 ppm, while water extract was low in 18.22%. In the inhibition activity of Xathine oxidase, ethanol extract showed higher inhibition activity compared to water extract. In measuring lipid oxidation inhibition ability using fish oil, ethanol extract in 100 ppm showed prominent ability. In the oxidation inhibition effect added with $Cu^{2+}\;ion\;and\;Fe^{2+}$ ion as a oxidation promoter, ethanol extract in 1000 ppm, each in the proportion of 90% and 92%, showed high oxidation inhibition effect compared with water extract. Conclusions : The results indicated that, ethanol extract which is superior in its anti-oxidation and antibacterial effect is useful to be applied in cosmetic industry.

• Biomolecules & Therapeutics
• /
• v.7 no.1
• /
• pp.54-58
• /
• 1999

The pharmacological activities and pharmacokinetic aspects of a topical microemulsion (KDPM) containing 0.5% piroxicam were evaluated after its topical application compared with a commercially available 0.5% piroxicam gel (R gel). When the pharmacological activities were evaluated with the carrageenan-induced paw edema model, KDPM showed 55.6% edema inhibition, while R gel resulted in 37.1%. With the adjuvant-induced arthritis model, KDFM also resulted in the better pharmacological activities than R gel. The relative bioavailability of KDPM based on R gel was 176% in rabbits.

• Bulletin of the Korean Chemical Society
• /
• v.14 no.6
• /
• pp.717-722
• /
• 1993

N-Phenyl oxadiazolidinedione derivatives II were synthesized and their herbicidal activities were measured against grass weeds. A parabolic relationship between molar refractivity (MR) of meta substituents of dione Ⅱ and their herbicidal activities was observed. With the substituents having MR value=${\sim}15$, the higher activities were obtained. Especially, the highest herbicidal activity (97% inhibition of weeds at 0.25 kg/ha) was observed by propyne IIr containing propargyloxy group as meta substituent.

• Korean Journal of Child Studies
• /
• v.27 no.3
• /
• pp.81-100
• /
• 2006

This study explored the relationship of behavioral inhibition to narrative representations. Narratives of 96 four-year-old children were recorded and analyzed by the scoring system of Robinson, Holmberg and Klute(in press). Six clusters were found : Constrained(47.9%), Anxious/Restricted(23.9%), Emotional Integrated/Empathic(12.5%), Empathic/Avoidant(6.3%), Dysregulated(5.2%) and Anxious/Avoidant(4.2%) clusters. Behavioral inhibition was determined by observations using "Play with Unfamiliar Peers(Rubin et al., 2002)". Behavioral inhibition differences corresponded to the children's narrative representation clusters; The Anxious/Restricted Cluster was related to more and the Emotional Integrated/Empathic Cluster to less inhibited behavior. In context-specific differences, more inhibited behavior was related to Anxious/Avoidant Clusters during show-and-tess and to Empathic/Avoidant Clusters during card-sorting activities, respectively.

• YAKHAK HOEJI
• /
• v.54 no.5
• /
• pp.398-402
• /
• 2010

[ ${\alpha}$ ]Glucosidase inhibitor is a target in the treatment of type II diabetes through the mainly inhibition of glucose levels after meals. In this study, we purified steppogenin and oxyresveratrol from the stem of Morus alba L. and examined their inhibitory activity against yeast ${\alpha}$-glucosidase. Steppogenin and oxyresveratrol were inhibited yeast ${\alpha}$-glucosidase in a dose dependent manner. The $IC_{50}$ activities (50% inhibition) were 34.4 and 9.3 ${\mu}M$, respectively. The kinetic inhibition of steppogenin showed noncompetitive inhibition ($K_m:1.1{\times}10^{-3}M$; $K_i:1{\times}10^{-5}M$), meanwhile oxyresveratrol showed competitive inhibition ($K_m:4.3{\times}10^{-3}M$; $K_i:3.4{\times}10^{-6}M$) against yeast ${\alpha}$-glucosidase. These results indicate that steppogenin and oxyresveratrol are noncompetitive and competitive inhibitors, respectively, against yeast ${\alpha}$-glucosidase.

• Journal of Applied Biological Chemistry
• /
• v.54 no.1
• /
• pp.33-40
• /
• 2011

Ionizing radiation can be used to improve the color of green tea extract to brighter. As a result, the irradiated green tea extract can be applied easier and broader in food or cosmetic industry. To confirm the retention of the biological activities of the cosmetic products added with green tea polyphenols (PPs), the real cosmetic products including a skin lotion (PS) and an essence (PE) cream were manufactured. Irradiation also applied to the manufactured cosmetic products to see their improvement of color and changes of biological activity. The PP showed 72% of electron donating ability (EDA) at a 5 ppm concentration and the PS and PE containing 2% PP showed higher than 60%, which was similar inhibition activity to vitamin C. The inhibition of superoxide dismutase (SOD)-like activity of PP, PS, and PE were higher than 55% at a 500 ppm concentration and the inhibition of xanthine oxidase (XOase) were also higher than 65% at a 200 ppm concentration. The measurement of lipid oxidation by addition of $Cu^{2+}$ and $Fe^{2+}$ as prooxidants showed that PP and PS had higher metal chelating ability for $Fe^{2+}$ than that of PE and the ability increased by increase of polyphenol concentration isolated from green tea. The $Cu^{2+}$ chelating ability of PP and PS showed higher than 90% at a 200 ppm concentration. Therefore, it is concluded that addition of PP in manufacturing PS and PE retains its biological activities including EDA, inhibition of XOase and SOD-like activity, and metal chelating ability in the manufactured cosmetic products. In addition, irradiation of PS and PE improved color of the products containing PP brighter without any adverse changes in biological activity of the products.