• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1998.11a
• /
• pp.170-170
• /
• 1998

In order to discover new types of 5-hydroxytryptamine antagonists, we have devoted our attention to investigating naturally occurring compounds having anti-5HT activity in vitro. Recently, ${\gamma}$-mangostin [1,3,6,7-tetrahydroxy-2,8-bis(3-methyl-2-bytenyl)-9H-xanthen-9-one] from the fruit hull of Garcinia mangostana Linn has been shown to be a selective antagonist for 5-hydroxytryptamine$_{2A}$ receptors in smooth muscle and platelets. It is of interesting that y-mangostin which does not have a nitrogen atom, possesses marked 5-$HT_{2A}$ receptor blocking activity. The present study was undertaken to investigate the effects of ${\gamma}$-mangostin on central 5-HT receptors by using animal behavioural models. Intracerebronventricular injection of ${\gamma}$-mangostin (10-40n mol/mouse) inhibited 5-fluoro-${\alpha}$-methyltryptamin (5-FMT) (45 mg kg$^{-1}$, i.p.)-induced head-twitch response in mice in the presence or absence of citalopram (5-HT-uptake inhibitor). Neither the 5-FMT- nor the 8-hydroxy-2-( di-n-propylamino )tetralin (5-HT$_{1A}$-agonist)-induced 5-HT syndrome (head weaving and hindlimb abduction) was affected by ${\gamma}$-mangostin. The locomotor activity stimulated by 5-FMT through the activation of at-adrenoceptors did not alter in the presence of ${\gamma}$-mangostin. 5-HT-induced inositol phosphates accumulation in mouse brain slices was abolished by ketanserin. ${\gamma}$-Mangostin caused a concentration-dependent inhibition of the inositol phosphates accumulation and the binding of [$^3H$]-spiperone, a specific 5-$HT_{2A}$ receptor antagonist, to mouse brain membranes. Kinetic analysis of the [$^H3$]-spiperone binding revealed that ${\gamma}$-mangostin increased the $_{d}$ value without affecting the $B_{max}$ value, indicating the mode of the competitive nature of the inhibition by ${\gamma}$-mangostin. These results suggest that ${\gamma}$-mangostin inhibits 5-FMT-induced head-twitch response in mice by blocking 5-$HT_{2A}$ receptors not by blocking the release of 5-HT from the central neurone. ${\gamma}$-Mangostin is a promising 5-$HT_{2A}$ receptors antagonist in the central nervous system.m.

• 한국신재생에너지학회:학술대회논문집
• /
• 2005.06a
• /
• pp.150-153
• /
• 2005

반도체성 고분자인 poly(3-hexylthiophene) (P3HT)과 $C_{60}$ 유도체인 PCBM의 복합재를 이용하여 유기태양전지를 제작하였다. 열처리 온도론 중심으로 다양한 제조조건 하에서의 태양전지 특성을 조사하였다. 열처리 온도를 높임에 따라, P3HT/PCBM 복합재 박막은 뚜렷한 색변화와 함께 가시광 영역에서의 광흡수가 증가됨이 관찰되었고, 소자 성능도 크게 향상되었다. 결과적으로, 본 P3HT/PCBM bulk 이종접합형 구조의 유기 태양전지는 최적화된 제조 조건에서 $2.8\%$의 에너지 전환 효율을 나타내었다($100mW/cm^2$, 백색광).

• Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
• /
• 2006.11a
• /
• pp.9-10
• /
• 2006

The patterning for the active layer of organic semiconductors is important to attain completely organic-based OTFTs(Organic Thin Film Transistors). We studied on possibility of the application of the conventional photolithography technique to pattern the organic active layer poly(3-hexylthiophene)(P3HT). Patterned P3HT-based OTFTs with Bottom Contact(BC) configuration were fabricated using the conventional photolithography. We achieved field-effect mobilities in the saturation regime ${\sim}1.2{\times}10^{-3}cm^2/V{\cdot}s$, $I_{on/off}$ ratios ${\sim}10^5$ in the subtractive method, ${\sim}8{\times}10^{-4}cm^2/V{\cdot}s$, $I_{on/off}$ ratios ${\sim}10^3$ in the additive one.

• Journal of Ginseng Research
• /
• v.29 no.1
• /
• pp.37-43
• /
• 2005

We performed in vitro and in vivo studies to know whether the inhibitory effects of ginsenosides on $5-HT_{3A}$ receptor channel acctivity are coupled to anti-nausea and anti-vomiting action. In vitro study, we investigated the effect of compound K (CK) and M4, which are ginsenoside metabolites, on human $5-HT_{3A}$ receptor channel activity expressed in Xenopus oocytes using two-electrode voltage clamp technique. Treatment of CK or M4 themselves had no effect in both oocytes injected with $H_2O\;and\;5-HT_{3A}$ receptor cRNA. In oocytes injected with $5- HT_{3A}$ receptor cRNA, M4 treatment inhibited more potently 5-HT-induced inward peak current $(I_{5-HT})$ than CK with dose-dependent and reversible manner. The half-inhibitory concentrations $(IC_{50})$ of CK and M4 were $36.9\;\pm\;10.1\;and\;7.3\;\pm\;2.2\;{\mu}M$, respectively. The inhibition of $I_{5-HT}$ by M4 was non-competitive and voltage-independent. These results indicate that M4 might regulate $5-HT_{3A}$ receptors. In vivo experiments, injection of cisplatin (7.5 mg/kg, i.v.) induced both nausea and vomiting with 1 h latency. These episodes reached to peak after 2 h and persisted for 4 h. Pre-treatment of GTS (500 mg/kg, p.o.) significantly reduced cisplatin-induced nausea and vomiting by $51\;\pm\;8.4\;and\;48.8\;\pm\;6.4\%$ during 4 h compared to GIS­untreated group, respectively. These results show the possibility that in vitro inhibition of $5-HT_{3A}$ receptor channel activity by ginsenosides might be coupled to in vivo anti-emetic activity.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.39 no.1
• /
• pp.31-35
• /
• 2010

This study was designed to evaluate anti-diabetes effect of Helianthus tuberosus extract (HT) in HIT-T15 cells. There were 5 experimental groups according to treatment NC (0 ${\muL/mL$), HT2 (1.1 ${\muL/mL$), HT3 (1.5 ${\muL/mL$), IN2 (1.8 ${\muL/mL$), IN3 (2.5 ${\muL/mL$). Inulin (IN) was used as a positive control for the Helianthus tuberosus extract groups. Cell viability was significantly increased in the HT3 (1.5 ${\muL/mL$), IN2 (1.8 ${\muL/mL$), IN3 (2.5 ${\muL/mL$) groups, compared with the NC group. There was no significant difference in cytotoxicity among all groups. Cell survival by MTT assay with alloxan was significantly increased in the HT2 (1.1 ${\muL/mL$), HT3 (1.5 ${\muL/mL$) groups, compared with the NC group. Insulin secretion and NAD+/NADH ratio were significantly increased in the HT3 group, compared with the NC group. We found that Helianthus tuberosus extract increased cell viability, had a protective effect on $\beta$-cells, and increased insulin secretion level and $NAD^+$/NADH ratio in HIT-T15 cells. These results suggest that Helianthus tuberosus extract improves the diabetes-related factors.

• The Korean Journal of Pharmacology
• /
• v.28 no.1
• /
• pp.19-25
• /
• 1992

The effect of the nonbenzodiazepine anxiolytic, buspirone $(Buspar^R)$, a serotonin $(5-HT)_{1A}$ partial agonist, which also has dopamine $(DA)_2$ receptor antagonist properties, on prolactin and cortisol secretion was examined in eight normal male volunteers. The oral administration of buspirone (30 mg) significantly increased plasma prolactin concentrations but did not significantly increase plasma cortisol concentrations in this study. The oral administration of pindolol (30 mg), a beta adrenoceptor antagonist which is also a $5-HT_{1A}$ receptor antagonist, had no significant effect on basal prolactin or cortisol levels. Moreover, pretreatment with pindolol did not significantly inhibit the buspirone-induced increase in prolactin secretion. These preliminary data are suggestive that buspirone-induced prolactin secretion is not mediated via $5-HT_{1A}$ receptor activation.

• Korean Journal of Community Nutrition
• /
• v.2 no.2
• /
• pp.179-186
• /
• 1997

A new bioelectrical impedance method has been developed and evaluated. The electrodes; were made of stainless steel and electrical interfaces were created by an upright subject gripping hand electrodes and stepping onto foot electrodes. Eight tactile electrodes were in contact with surfaces of both hands and feet; thumb, palm and fingers, front sole, and rear sole. Automatic on-off switches were used to change current pathways and to measure voltage differences for target segments. Segmental body resistances and whole body resistance(RWHOLE)were measured in 60 healthy subjects. Segmental resistances of right arm(RRA), left arm(RLA), trunk(RT), right leg(RRL) and left leg(RLL)were310.0$\pm$61.6$\Omega$, 316.9$\pm$64.6$\Omega$, 25.1$\pm$3.4$\Omega$, 236.8$\pm$31.2$\Omega$ and 237.6$\pm$30.4$\Omega$, respectively. Individual segmental impedance indexes(Ht2/RRA, Ht2/RT, and Ht2 /RLA) were closely related to lean body mass(LBM)as measured by densitometry ranged from r=0.925 to 0.960. Ht2/(RRA+RT+RLA) predicted LBM slightly better(r=0.969) than the traditional index, Ht2/RWHOLE(r=0.964), supporting the accuracy of the segmental measurement. A multiple regression equation utilizing Ht2/RRA, Ht2/RT and Ht2/RRL predicted LBM with r=0.971. Ht2/RRA term of the regression contributed to more than 40$\%$ of the LBM prediction, indicating that lean mass of arm represented whole body LBM more closely than other body segments. The new bioimpedance method was characterized by upright posture, eight tactile electrodes, segmental measurements and utilization of electronic switches in comparison with the traditional method. The measurement with this new method was extremely reproducible, quick and easy to use.

• Korean Journal of Veterinary Research
• /
• v.34 no.3
• /
• pp.447-456
• /
• 1994

In order to elucidate the characterization of receptors involved in inestinal motility of Israeli carp, spontaneously contracting Israeli carp intestinal preperations were prepared and mounted in the organ chambers for contraction traicings using a polygraph. Various contractile agonists were treated and their dose-response curves were constructed. $EC_{50}$ values$(pD_2)$ of each agonist on specific receptors, $pA_2$ values of competitive antagonists against some agonists, and $K_1$, values of noncompetitive antagonists against some agonists were analyzed for characterization of receptors related with the intestinal contraction. Results obtained through the experiments were summarized as follows: 1. Acetylcholine(ACh) exhibited biphasic dose-response curves: initial ACh-induced dose dependent contractions were observed in pM levels but followed by decreased response in in-between concentration levels. Dose dependent contractions reappeared in ${\mu}M$ level. The peaks in pM and ${\mu}M$ levels appeared in $10^{-13}M$ and $3{\times}10^{-5}M$, respectvely. 2. Carbachol(CaCh) exhibited dose dependent contractions from $10^{-9}M$ to $10^{-5}M$, and its $pD_2$ values were higher than those of ACh($5.60{\pm}0.11$). ACh and CaCh exhibited equiactive contractions. Nicotine had no effects on contractile responses of Israeli carp intestine. 3. ACh-induced responses were inhibited by atropine($K_1:7{\times}10^{-8}M$), a muscarinic antagonist, in a non-competitive manner. But CaCh-induced responses were inhibited by both antimuscarinic atropine($pA_2:9.52{\pm}0.14$) and selective $M_2$ antagonistic 4-DAMP($pA_2:8.16{\pm}0.09$), in competitive manners. Nicotine receptor antagonistic decamethonium and hexamethonium had no effects on ACh-and CaCh-induced contractions. Therefore, the cholinergic receptor related to intestinal motility of Israeli carp was assumed as $M_2$ type. 4. In Israeli carp intestine, 5-HT (serotonin) exhibited dose dependent contractions in concentration range from $10^{-8}M$ to $10^{-5}M$. The maximal responses, however, were corresponded to about 50% of those of ACh or CaCh. 5-HT induced contractions were inhibited by $5-HT_2$ antagonistic ketanserin ($K_1: 7.8{\times}10^{-4}M$) in a non-competitive manner, but not by both of anti $5-HT_1$, spiperone and anti $5-HT_3$, MDL-72222. Hence, $5-HT_2$ receptors are suggested to be existed in Isreli carp intestine.

• Radiation Oncology Journal
• /
• v.29 no.4
• /
• pp.219-227
• /
• 2011

Purpose: This study evaluated the treatment effectiveness and proper radiation dose of helical tomotherapy (HT) in spine oligometastases from gastrointestinal cancers. Materials and Methods: From 2006 to 2010, 20 gastrointestinal cancer patients were treated with HT for spine oligometastases (31 spine lesions). The gross tumor volume (GTV) was the tumor evident from magnetic resonance imaging images fused with simulation computed tomography images. Clinical target volume (CTV) encompassed involved vertebral bodies or dorsal elements. We assumed that the planning target volume was equal to the CTV. We assessed local control rate after HT for 31 spine metastases. Pain response was scored by using a numeric pain intensity scale (NPIS, from 0 to 10). Results: Spine metastatic lesions were treated with median dose of 40 Gy (range, 24 to 51 Gy) and median 5 Gy per fraction (range, 2.5 to 8 Gy) to GTV with median 8 fractions (range, 3 to 20 fraction). Median biologically equivalent dose (BED, ${\alpha}/{\beta}$ = 10 Gy) was 52 $Gy_{10}$ (range, 37.5 to 76.8 $Gy_{10}$) to GTV. Six month local control rate for spine metastasis was 90.3%. Overall infield failure rate was 15% and outfield failure rate was 75%. Most patients showed pain relief after HT (93.8%). Median local recurrence free survival was 3 months. BED over 57 $Gy_{10}$ and oligometastases were identified as prognostic factors associated with improved local progression free survival (p = 0.012, P = 0.041). Conclusion: HT was capable of delivering higher BED to metastatic lesions in close proximity of the spinal cord. Spine metastases from gastrointestinal tumors were sensitive to high dose radiation, and BED (${\alpha}/{\beta}$ = 10 Gy) higher than 57 $Gy_{10}$ could improve local control.

• Korean Journal of Clinical Laboratory Science
• /
• v.51 no.2
• /
• pp.214-220
• /
• 2019

Hwangryunhaedok-tang (HT) is prescribed in oriental medicine to treat inflammation-related diseases. This study examined the anti-bacterial effect to select the index components of Traditional Chinese Medicine (TCM) HT. The disc diffusion method and minimum inhibition concentrations (MIC) tests were conducted to measure the antibacterial activity of HT. The strains were Staphylococcus aureus ATCC 25923 and Escherichia coli 23724. Berberine and geniposide were selected as the index components of HT and were analyzed quantitatively by high-performance liquid chromatography (HPLC). As a result, the inhibition ring was formed at $11.7{\pm}1.3mm$ and $8.7{\pm}0.7mm$ at HT 20 mg and 10 mg on S.aureus ATCC 25923, respectively; and $8.0{\pm}0.0mm$ at HT 20 mg on E.coli ATCC 23724. The MIC were 31.25 mg/mL in S.aureus ATCC 25923 and 125.0 mg/mL in E.coli ATCC 23724. In quantitative analysis for standardization, HT contained 16.55 mg/g of berberine and 81.85 mg/g of geniposide. Overall, when antibiotics are developed using natural products, they may reduce the side effects and inhibit resistant bacteria. If research on HT continuously proceeds, positive developments are expected to be made in oriental medicine as well as in various other industries.