• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.310.1-310.1
• /
• 2003

SD-2007 ia an apicidin analogue, possessing a potent histone deacetylase inhibiting activity. A rapid and senstive LC/MS method was developed for the determination of SD-2007 and its major active metabolite. apicidin. in rat serum. SD-2007 and apicidin was extracted by liquid-liquid extraction using methyl t-butyl ether. SD-2007 and apicidin were monitored in a SIM mode at m/z of 679 and 622, respectively. (omitted)

• Journal of the Korean Applied Science and Technology
• /
• v.32 no.2
• /
• pp.302-311
• /
• 2015

To better investigate the antioxidative property of thermal treatment yam (Dioscorea batatas DECNE.) in Korea, some established methods were used. 70% Methanol, 70% ethanol and chloroform-methanol (CM, 2:1, v/v) extracts were collected. 70% Methanol extract exhibited stronger antioxidative activity evaluated by ferrous ion chelating activity, NO radical scavenging activity and ${\beta}$-carotene bleaching assays. On the contrary, CM extract was the most effective in inhibiting linoleic acid peroxidation. Yam available in Korea was also analyzed for its bioactive compounds such as lycopene, chlorophyll a, b, tannin, phytic acid and total saponin contents. Total saponin was abundant in thermal treatment, which determined to be $42.52{\pm}1.88mg/g$. Based on the results obtained from this study, thermal treatment yam could be used as natural antioxidant source due to its high antioxidant activity and bioactive compound contents.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.22 no.6
• /
• pp.1532-1536
• /
• 2008

Quercetin which isolated form the roots of Houttuynia cordata. was determined on the basis of IR, ID and 2D NMR specta by direct comparison with authentic compounds. Protein tyrosine phophatase 1B (PTP1B) is thought to be a negative regulator in insulin signal-transduction pathway. Insulin-resistance by the activation of PTP1B is a hallmark of both type 2 diabetes and obesity. Thus, the compound inhibiting PTP1B can improve insulin resistance and can be effective in treating type 2 diabetes and obesity. Quercetin which measured the inhibitory activity against PTP1B was 92.1% inhibition in the 30 ${\mu}g$/mL, 83.4% inhibition in the 6 ${\mu}g$/mL and 76.5% inhibition in the 3 ${\mu}g$/mL. These results suggest that quercetin retains a potential PTP1B activity.

• BMB Reports
• /
• v.43 no.4
• /
• pp.245-249
• /
• 2010

GDH has been known to be related with hyperinsulinism-hyperammonemia syndrome. We have screened new drugs with a view to developing effective drugs modulating GDH activity. In the present work, we investigated the effects of a new drug, KHG26377 on glutamate formation and GDH activity in cultured rat islets. When KHG26377 was added to the culture medium for 24 h prior to kinetic analysis, the $V_{max}$ of GDH was decreased by 59% whereas $K_m$ is not significantly changed. The concentration of glutamate decreased by 50% and perfusion of islets with KHG26377 reduced insulin release by up to 55%. Our results show that KHG26377 regulates insulin release by inhibiting GDH activity in primary cultured islets and support the previous studies for the connection between GDH activity and insulin release. Further studies are required to determine in vivo effects and pharmacokinetics of the drug.

• The Plant Pathology Journal
• /
• v.24 no.3
• /
• pp.328-336
• /
• 2008

Out of various fungi and bacteria tested for inhibition of Tobacco mosaic virus(TMV) infection using Nicotiana tabacum cv. Xanthi-nc, a bacterial isolate JB-l, identified as Pseudomonas putida had a strong direct inhibitory activity against the TMV infection. Its systemic or indirect activity was also noted at more than a half level of the direct control efficacy. Disease severity was reduced significantly in the susceptible tobacco N. tabacum cv. NC 82 by the treatment of the bacterial culture filtrate, somewhat more by the pretreatment than by simultaneous treatment, probably by inhibiting the TMV transmission and translocation in the plants, showing negative serological, which responses in the viral detection by DAS-ELISA. TMV-inhibitory substances from P. putida JB-1 were water-soluble, stable to high temperature(even boiling), and to a wide range of pH. As proteinase K nullified their antiviral activity, the TMV inhibition activity of P. putida may be derived from proteinaceous materials. In electron microscopy, TMV particles treated with the JB-1 culture were shown to be shrunken with granule-like particles attached on them. All of these aspects suggest that P. putida JB-1 may be developed as a potential agent for the control of TMV.

• Korean Journal of Environmental Agriculture
• /
• v.15 no.3
• /
• pp.316-324
• /
• 1996

The four tolerant and one susceptible plant to oxyfluorfen were selected from 26 species and investigated for the inhibition of protox activity, the PPIX accumulation, and the activity of antioxidative enzymes by oxyfluorfen treatment. When treated, the oxyfluorfen-tolerant plant species showed a less decrease in fresh weight and height than the susceptible one. The susceptible barnyardgrass showed more inhibition of protox activity due to the treatment of oxyfluorfen than the tolerant species. Especially at the concentration of $10^{-6}M$, protox activity of the susceptible barnyardgrass was inhibited completely, but tolerant species maintained $25{\sim}45%$ of the activity. Under the light and dark condition, the susceptible barnyardgrass showed more PPIX accumulation than the tolerant.

• Current Research on Agriculture and Life Sciences
• /
• v.31 no.4
• /
• pp.227-232
• /
• 2013

We studied antioxidant activity and inhibitory effect of ${\alpha}$-glucosidase from aqueous, ethanolic and methanolic fractions of Galla rhois. In FRAP and ORAC assay for measuring antioxidant activity, we confirmed that Galla rhois extracts had strong antioxidant activity and ethanolic and methanolic extracts were relatively stronger than aqueous extract. We used trolox as a positive control. In order to measure the inhibitory effect of ${\alpha}$-glucosidase, we compared acarbose and Galla rhois extracts. As a result of ${\alpha}$-glucosidase inhibitory assay, aqueous, ethanolic and methanolic extracts of Galla rhois showed high inhibitory activitity and ethanolic and methanolic extracts were relatively stronger than aqueous extract. The 50% inhibitory concentrations (IC50s) of acarbose, aqueous, ethanolic and methanolic fractions were 0.45 mM, $0.53{\mu}g/ml$, $0.415{\mu}g/ml$ and $0.37{\mu}g/ml$, respectively. These results suggest that Galla rhois extracts can be a clinically useful anti-diabetic ingredient, indicating that it needs to be fractionated and isolated and should be further investigated.

• Biomolecules & Therapeutics
• /
• v.19 no.1
• /
• pp.97-101
• /
• 2011

Cirsium japonicum var. ussuriense is known to have a variety of biological activities, including anti-inflammatory, analgesic activity and antipyretic activity. In this study we investigated the role of polyacetylene compound, 1-Heptadecene-11, 13-diyne-8, 9, 10-triol (PA) from the root of Cirsium japonicum var. ussuriense as an immune-modulator. PA was evaluated as inhibitors of some macrophage functions involved in the inflammatory process. We tested the effect of PA on the production of pro-inflammatory cytokines, interleukin-1beta (IL-$1{\beta}$) and tumor necrosis factor-alpha (TNF-$\alpha$), and nitric oxide (NO) in murine macrophage cell line, RAW264.7. There was no effect on cytokine production of macrophages by PA itself. However, PA inhibited lipopolysaccharide (LPS)-induced IL-$1{\beta}$ and TNF-$\alpha$ production by macrophages at a dose dependent manner. PA also suppressed the NO production of macrophages by LPS. LPS-induced NF-${\kappa}B$ activity was decreased by treatment of PA. Therefore, these results suggest that PA has anti-inflammatory effect by inhibiting the NF-${\kappa}B$ activation.

• Fisheries and Aquatic Sciences
• /
• v.17 no.1
• /
• pp.155-158
• /
• 2014

The objective of this study was to evaluate the antiviral activity of Phaeophyta extracts against feline calicivirus (FCV), used as a norovirus surrogate. A bioassay-guided cytotoxicity and virus infectivity assay revealed that methanolic extracts of Phaeophyta possessed significant antiviral activity against FCV. Among them, Eisenia bicyclis extract exhibited the highest antiviral activity against FCV. The 50% effective concentration of the extract ($EC_{50}$) inhibiting FCV viral replication by 50% was $80{\mu}g/mL$. The extract also showed the highest selectivity index, calculated from the ratio of the median cellular cytotoxicity concentration ($CC_{50}$) and $EC_{50}$, indicating antiviral efficacy against FCV. In addition, significant interruption of FCV infection was observed by pretreatment of host Crandall-Reese feline kidney cells with the E. bicyclis extract ($200{\mu}g/mL$) prior to virus infection, in a dosedependent manner.

• Archives of Pharmacal Research
• /
• v.28 no.2
• /
• pp.180-185
• /
• 2005

In the process of investigating anti-obesity effect of Platycodi Radix, we found that aqueous extract of Platycodi Radix might inhibit intestinal absorption of dietary fat by inhibiting pancreatic lipase (PL) activity. In order to clarify the anti-obesity mechanism of Platycodi Radix, activity-guided isolation was performed to find active components. The total saponin fraction of Platycodi Radix appeared to have a potent inhibitory activity against the hydrolysis of triolein emulsified with phosphatidycholine by pancreatic lipase in vitro. Based on these results, further purification of active components yielded 10 known triterpenoidal saponins, among these compounds, platycodin A, C, D, and deapioplatycodin D exhibited significant inhibitory effects on PL at the concentration of $500\;{\mu}g/mL$ with 3.3, 5.2, 34.8, and $11.67\%$ pancreatic lipase activity vs control, respectively. Platycodin D was found to inhibit the PL activity in a dose-dependent manner. Therefore, the anti-obesity effect of Platycodi Radix might be due to the inhibition of pancreatic lipase by its saponins.