• Journal of Life Science
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• v.10 no.6
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• pp.584-590
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• 2000

Natural products are one of the useful source of cardiovascular drugs, in particular, when they have antioxidant activity. Gagaminine, an alkaloid isolated from the roots of Cynanchum wilfordi Hemsley, has been reported to potently inhibit the aldehyde oxidase activity ({TEX}$IC_{50}${/TEX}=0.8$\mu$M) and reduce lipid peroxidation. However, the effect of gagaminine on vascular smooth muscle has not yet been investigated. In the present study, we examined whether gagaminine relaxes vascular smooth muscle by isometric tension study. In order to observe its relaxation effect on the arteries, conductivel vessel (rat thoracic aorta) and resistance vessel (pig coronary artery) were purposely used. Results indicated that gagaminine relaxed in a concentration-dependent manner $\alpha$-adrenoceptor agonist, phenylephrine (PE)-induced contraction of rat aorta. Pretreatment with gagaminine inhibited PE-induced contraction, noncompetitively. {TEX}$Ca^{2+}${/TEX}-induced contraction was significantly diminished by gagaminine. In pig coronary artery, gagaminine relaxed thromboxane receptor (U 46619)-mediated contraction in dose-dependent manner. Pretreatment with gagaminine also reduced the maximum contraction induced by KCl. These observations strongly suggest that agagminnine relaxes vascular smooth muscle, irrespective of both resistance and conductive artery. We demonstrate that gagaminine, a potent natural antioxidant, has a significant vasodilatory effect and its action mechanism van be ascribed at least in part to {TEX}$Ca^{2+}${/TEX} antagonistic action as evidenced by inhibition {TEX}$Ca^{2+}${/TEX}-induced contraction (rat aorta) and KCl-induced contraction (porcine artery). Furthermore, neither $\alpha$ -adrenoceptor nor thromboxane receptor seems responsible for the relaxation of gagaminine.

• YAKHAK HOEJI
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• v.41 no.5
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• pp.554-558
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• 1997

Two alkaloidal components were isolated from the ether soluble part of the MeOH extract of the root bark of Euonymus japonica. Their structures were elucidated by the spe ctroscopic analylses as the sesquiterpene pyridine alkaloids derived from polyester sesquiterpenes which are characteristically detected in Celastraceae plants. These include macrocycle formed by two ester linkages between dihydro-${\beta}$-agarofuran nucleus and pyridinic dibasic acid(compound 1:evoninic acid, compound 2:wilfordic acid). The structure of compound $1[C_{47}H_{50}N_2O_{17},\;mp\;161{\sim}163^{circ}C$. $[{\alpha}]_D^{28}=+31.6^{\circ}$(c, 0.1 in EtOH)] was determined as novel structure named as euojaponine N, and compound $2[C_{48}H_{57}NO_{18},\;mp\;142{\sim}145^{circ}C,\;[{\alpha}_D^{27}=+27.0^{\circ}$(c, 0.1 in EtOH)] was identified as ebenifoline W-I reported from Maytenus ebenifolia.

• Journal of the Korean Wood Science and Technology
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• v.24 no.1
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• pp.87-94
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• 1996

한국산 동백나무겨우살이(Pseudixus japonicus) 추출물의 암치료를 위한 생약으로서 활성 유효성을 검증하기 위하여 메탄올, 석유에테르, 클로로포름, 초산 에틸 용매로 순차적으로 추출하여 겨우살이 추출물의 다섯 가지 분획을 얻어, 이에 대하여 in vitro로 1차와 2차 검색 시스템을 사용해 항암활성 성분을 체계적으로 검색하였다. 다섯 가지 분획 중 클로로포름 가용성 분획이 1차 검색 세포인 $P388D_1$에 대해 가장 높은 항암활성을 나타내어 MSB1, NIH/3T3, SNU-1, SNU-C2A 등 2차 검색 시스템에 대해 클로로포름 가용성 분획의 항암활성을 다양한 농도하에서 비교 검색하였다. 혈액암 세포중 특히 $P388D_1$의 생장이 클로로포름 추출물에 의해 강하게 저해되었으며, 형질전환된 생쥐의 태아 섬유아세포와 사람의 대장암, 위암세포들도 어느 정도의 생육저해를 나타내었다. 이 클로로포름 가용성 분획의 주성분은 원소분석, 발색시약과의 반응, IR, GC-MS, $^{13}C$-NMR의 스펙트럼의 결과로 세 종류의 알칼로이드 화합물로 확인되었고, 부성분으로는 지방산 메틸 에스테르와 프탈라이드 화합물이 MS 스펙트럼을 통해 동정되었다.

• YAKHAK HOEJI
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• v.47 no.4
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• pp.230-233
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• 2003

Previously, protoberberine alkaloids such as berberine and palmatine have been found to lower dopamine content in PC12 cells (Shin et at., 2000). In this study, the effects of berberine and palmatine on L-DOPA-induced increase in dopamine level and cytotoxicity in PC12 cells were investigated. Treatment of PC12 with L-DOPA at concentration ranges of 20∼50 $\mu$M increased dopamine content and the increase in dopamine levels by L-DOPA was inhibited by 10∼40 $\mu$M berberine and 10∼80 $\mu$M palmatine, which the concentration ranges did not show a cytotoxicity. However, berberine and palmatine at concentrations higher than 50 $\mu$M and 100 $\mu$M caused a cytotoxicity, respectively. In addition, berberine (10∼20 $\mu$M) and palmatine (10∼50 $\mu$M) at non-cytotoxic concentration ranges aggravated L-DOPA-induced cytotoxicity in PC12 cells (L-DOPA concentration ranges, 20∼50 $\mu$M). The L-DOPA-induced cytotoxicity was also significantly potentiated by berberine (50 $\mu$M) and palmatine (100 $\mu$M) with cytotoxic ranges. These data demonstrate that berberine and palmatine inhibit L-DOPA-induced increase in dopamine content and stimulate L-DOPA-induced neurotoxicity. Therefore, the possibility that the long-term L-DOPA treated patients with berberine and palmatine could be checked the adverse symptoms.

• YAKHAK HOEJI
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• v.37 no.2
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• pp.143-148
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• 1993

The objective of this study was to evaluate the sedative activity of four aporphine alkaloids (APA) and nine cyclopeptide alkaloids(CPA), which had been isolated from the seeds (sanjoin) of Zizyphus vulgaris var. spinosus, and the fruits and stem bark of Zizyphus jujuba var. inermis. The assessment of sedative activity was carried out, employing a hexobarbital-induced sleeping time method in mice. When the relative sedative potency of sanjoinine-A(CPA) was given as one unit, those of nuciferine (APA), lysicamine (APA), chlorpromazine (positive control), and sanjoinine -Ahl (an epimer of sanjoinine-A) were 13, 6.5, 5, and 3, respectively. The sedatvie activities of other CPAs were much lower than those of sanjoinine-A and -Ahl, and other APAs were not active. On heat treatment, nuciferine and lysicamine were degraded into some artifacts which exhibited no sedative activity, while sanjoinine-A was converted into sanjoinine-Ahl which showed more potent sedative activity. These results suggested that nuciferine and sanjoinine-A were major sedative components of native sanjoin, and that sanjoinine-A and its epimeric artifact, sanjoinineAhl were the active principles of roasted sanjoin. It provides a scientific basis for heat-processing (roasting) of this Oriental medicine.

• Proceedings of the Korean Society of Tobacco Science Conference
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• 2001.05a
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• pp.35-43
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• 2001

일대잡종육종이란 현대의 다양한 육종기술 중 하나로 교배 제1세대의 잡종강세현상을 곧바로 이용하는 것으로 여러 작물에서 실용적으로 이용되고 있다. F$_1$잡종종자를 생산하려면 자가수분을 통제해야 하는데 웅성불임을 이용하면 자친의 화분제거 노력이 생력되어 경제적인 종자생산이 가능하다. 연초는 자식성 작물로 잡종강세는 높지 않으나 종간 교잡에 의한 cms가 만들어진 이후 버어리종 등에서는 60년대부터 직적형질에 가깝게 유전되는 우성 단일유전자의 지배를 받는 N. logniflora의 역병(race 0)저항성을 도입한 웅성불임(cms) F$_1$잡종이 활발하게 이용되어 왔다. 최근에는 cms F$_1$잡종의 이용영역이 넓어져 우리나라의 경우 N. glutinosa에서 유래한 우성 단일인자 TMV저항성을 도입한 황색종 cms F$_1$잡종 KF 114가 주 재배품종이 되었고 버어리종에서는 VAM에서 유래한 열성단일유전자의 지배를 받는 PVY저항성이 도입된 KB 111의 확대재배가 예상되고 있다. 본 글에서는 cms F$_1$잡종의 국내외 이용 사례를 살펴보고 cms F$_1$잡종의 육성과 이용방향, cms F$_1$잡종 종자생산에 관하여 기술하였다. 그리고 병저항성뿐 아니라 알칼로이드함량, 염록소함량, DVT나 챤-abienol 및 SE함량 등 질적형질에 가깝게 유전되고 유전양식이 명확하게 밝혀진 화학성분에 대해서도 F$_1$잡종 육성의 대상 형질로 논의하였다.

• Korean Journal of Pharmacognosy
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• v.34 no.3 s.134
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• pp.206-209
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• 2003

The fruit of Evodia officinalis (Rutaceae) is known for containing a number of indoloquinazoline and quinoline type alkaloids. Evodiamine, evocarpine and rutaecarpine are the major constituents of Evodiae Fructus. These alkaloids were isolated and determined by forming complex compounds from Evodiea Fructus. For the determination of these alkaloids, a new spectrophotometric method was developed with a simple and selective sample clean-up using thiocyanatocobaltate [II] complex ion. The absorbance of alkaloidal complex in 1.2-dichloroethane solution was measured at 625 nm. A calibration curve for the alkaloids isolated from Evodia Fruit was linear over the concentration range of $1.0{\sim}6.0\;mg/ml$. The method proved to be rapid, simple and reliable for the isolation and the determination of the alkaloids in Evodiae Fructus.

• Biomolecules & Therapeutics
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• v.7 no.3
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• pp.278-284
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• 1999

DK1001 is a thebain derivative, which is newly synthesized as an alkaloid analgesic. This study was designed to study effects of DK1001 on the ligands binding to the opioid receptor subtypes, and general pharmacology of DK1001. DK1001 inhibited the binding of [$^3H$]DAMGO, a selective mu-subtype agonist, to the opioid receptor of rat forebrain in a concentration-dependent manner. $EC_{50}$ of DK1001 was significantly lower than that of morphine. DK1001 inhibited the binding of 〔$^3$H〕DPDPE, a selective delta-subtype agonist concentration-dependently. DK1001(0.5 mg/kg) had no effects on behavior, body temperature, blood pressure. respiratory rate, and intestinal charcoal propulsion of mice. In addition, DK1001 did not affect on the contractilities of isolated muscle strips of aorta, ileum, and trachea of rats. These results suggest that DK1001 might be a potent analgesic without serious side effects.

• Korean Journal of Pharmacognosy
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• v.5 no.3
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• pp.159-166
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• 1974

The Yellow needle crystal was isolated from Atractylis Rhizoma, having mp $124{\sim}126^{\circ}C$(decomp.), the chemical composition $C_{16}H_{21}N_{3}O_{6}$, and its m.w. 251. The pharmacological actions of this alkaloid were studied by various psycopharmacological experiments. 1) In order to see the effect of this Atractylis(=At.) alkaloid on gross general behaviors in mice, a behavioral analysis experiment was adapted. The occurrence number of sleep and lying in At. alkaloidal animals with the doses 10mg/kg or 20mg/kg was increased but the number of jumping, exploration, rearing and defecation was significantly decreased than those of placebo. 2) The effect of the At. alkaloid on unlearned emotional behaviors of mice was studied with an open-field method. The At. alkaloidal groups with the doses 20mg/kg or 30mg/kg showed less often the frequency of locomotion than that of placebo. 3) To know the effect of the At. alkaloid on the learning, a standard water maze experiment and conditioned avoidance response were conducted. As compared to placebo control, the aquisition rate of the maze learning in the alkaloidal mice with the dose of 10mg/kg or 20mg/kg was significantly impaired and the speed of swimming was also signficantly delayed. In the conditioned avoidance response, the extinction performances of the alkaloidal rats with doses of 20mg/kg or 30mg/kg did not differ significantly than that of placebo.

• YAKHAK HOEJI
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• v.44 no.2
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• pp.135-140
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• 2000

Determination of Aconitum alkaloids in processed Buza (Cho-0, Salted Buza, Moist-heating Buza, Limed Buza), which had been prepared from the raw tubers of Aconitum chiisanenseb(Ranunculaceae), was established using visible spectrophotometry and high-performance liquid chromatography (HPLC) method especially for Aconitine analysis. Aconitum alkloids were reacted with tetra- thiocy-anatocobalt[II] complex ion to form a stable ion pair. The reaction product was insoluble in water but freely soluble in several organic solvents. 1.2-Dichloroethane was the best extracting solvent among the examined solvents. Spectrophotometry of Aconitum alkaloids at nax. 625 was carried out. The HPLC method for aconitine was carried out using Radial PAK-CN column with gradient solvent system by solvent mixture of acetonitrile and phosphate buffer (pH 3.0) at 4$0^{\circ}C$ and 254 nm. Linear relationship was found between absorbance response and concentration of aconitine in range of 0.45 mM~0.9 mM ($r^2$=0.9949) by spectrophotometry and 0.3 mM~1.2mM($r^2$=0.9983) by HPLC method. These methods have been found to be suitable and reproducible for routine analysis of Aconitum alkaloids and its pharmaceutical preparations.