• Archives of Pharmacal Research
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• 제28권2호
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• pp.172-176
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• 2005

Phytochemical investigation of the whole plant of Amberboa ramosa led to the isolation of six sesquiterpene lactones which could be identified as $8{\alpha}$-hydroxy-$11{\beta}$-methyl-$1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\alpha}H-guai-10(14)$, 4(15)-dien-6, 12-olide(2), $3{\beta},\;8{\alpha}-dihydroxy-11{\alpha}-methyl-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\beta}H-guai-10(14)$, 4(15)-dien-6, 12-olide (2), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide (3), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}-(chloromethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide(4), $3{\beta},\;4{\alpha},\;dihydroxy-4{\beta}-(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide(5), $3{\beta},\;4{\alpha}-dihydroxy-4{\beta}-(chloromethyl)-8{\alpha}-(4-hydroxymethacrylate)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide (6) by spectroscopic methods. All of them showed inhibitory potential against butyrylcholinesterase.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.67.1-67.1
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• 2003

Three new guaianolide type of sesquiterpene lactones, 8${\alpha}$-angeloyloxy-1${\alpha}$-hydroxy-3${\alpha}$,4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14), 11(13)-guaiadien-12,6${\alpha}$-olide (1), 8${\alpha}$-methylbutyryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11(13)-guaiadien-12,6${\alpha}$-olide (2), and 8${\alpha}$-isovaleryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11 (13)- guaiadien-12,6${\alpha}$-olide (3), together with six known sesquiterpenes, artemisolide (4), 3-methoxytanapartholide (5), deacetyllaurenobiolide (6), moxartenolide (7), arteminolide B (8), and arteminolide D (9) were isolated by bioassay-guided fractionation using the NF-kB mediated reporter gene assay system. (omitted)

• Asian Pacific Journal of Cancer Prevention
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• 제17권3호
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• pp.1399-1404
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• 2016

We investigated the urinary levels of 14-3-3 protein beta/alpha to evaluate their diagnostic significance with regard to clear cell renal cell carcinoma (ccRCC) and angiomyolipoma (AML). Urine samples from 91 patients with ccRCC, 16 patients with AML and 24 healthy volunteers were assessed. We used an enzyme-linked immunosorbent assay (ELISA) to quantify 14-3-3 protein beta/alpha levels in urine. Values were higher in patients with ccRCC than in those with AML and in healthy volunteers. High levels were associated with pathologic stage, lymph node status, distant metastasis and poor survival. Urinary levels of 14-3-3 protein beta/alpha were significantly increased in patients with small-sized carcinoma, irrespective of being less than 4.0 cm and 2.0 cm, compared with levels in patients with AML. This study is the first to report that increased expression of 14-3-3 protein beta/alpha in urine is associated with advanced stage and poor survival in patients with ccRCC. In addition, urinary 14-3-3 protein beta/alpha may differentiate AML from RCC, even when small sized. These results suggest that examination of urinary 14-3-3 protein beta/alpha could serve as a diagnostic and prognostic marker in patients with ccRCC.

• 생명과학회지
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• 제13권2호
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• pp.206-213
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• 2003

초피의 성숙과정중 향기성분을 조사하고자, 경상남도 밀양시 제약산 일대에서 2001년 6월 2일, 7월 14일 및 9월 11일에 채취한 초피 과피의 향기성분을 CC-MS로 분석한 결과, 6월 2일에는 52종, 7월 14일에는 47종 및 9월 11일에는 44종이 확인되었다. 각각의 채취시기에 대한 구성성분의 종류를 비교하면 terpene류는 6월 2일과 7월 14일에는 myrcene, ${\gamma}$-terpinene, $\alpha$-terpinolene, $\alpha$-phellandrene, $\beta$-caryophyllene 등 8종이 검출되었으나, 9월 11일에는 $\alpha$-phellandrene과 $\beta$-raryophyllene이 검출되지 않았다. Alcohol류는 6월 2일 채취시에는 linalool L, citronellol 등 13종이, 7월 14일과 9월 11일에는 cis-linalool oxide와 piperitol isomer가 추가되어 15종이 검출되었다. Aldyhyde류는 채취시기에 관계없이 citronellal 등 3종이 검출되었으나, 9월 11일에는 citronellal의 함량이 현저히 증가하였으며, ketone류도 cryptone, piperitone 등 5종이 검출되었는데 구성성분의 종류는 채취시기에 관계없이 동일하였으나, 함량의 차이는 있었다. Ester류는 6월 2일에 채취하였을 경우에는 lavandulyl acetate, $\alpha$-terpinenyl acetate 등 6종이 검출되었으나, 7월 14일과 9월 11일에 채취한 과피에서는 [(E)-6,7-ephoxy-3,7-dimethyl-2-octenyl]ester of acetic acid 가 새로이 검출되어 7종이었다. Hyrocarbon류는 $\delta$-cadinene, neopentylideneclohexane 등 7종이었는데, 7월 14일과 9월 11일에는 $\alpha$-muurolene이 추가되어 8종이 검출되었다 초피 과피의 향기성분은 채취시기에 따라서 구성성분의 종류는 물론 농도의 변화가 현저하였다.

• Food Science and Biotechnology
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• 제17권5호
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• pp.1115-1118
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• 2008

${\alpha}$-Galactosidase gene (aga) from Leuconostoc mesenteroides SY1 was expressed in a heterologous host, Lactobacillus brevis 2.14 using an Escherichia coli-Leuconostoc shuttle vector, pSJE. pSJEaga (pSJE carrying aga) was introduced into Lactobacillus brevis 2.14 by electroporation and transformation efficiency was $1.1{\times}10^3$ per ${\mu}g$ DNA. L. brevis transformants (TFs) showed higher ${\alpha}$-galactosidase (${\alpha}$-Gal) activities than cells containing pSJE. Transcription levels of aga in L. brevis 2.14 grown on different carbon sources (1%, w/v) were examined by slot blot analysis. Aga transcript levels and ${\alpha}$-Gal activities were higher in cells grown on melibiose, raffinose, and galactose than cells on glucose, sucrose, and fructose. Western blot result showed that L. brevis 2.14 harboring pSJEaga produced much more ${\alpha}$-Gal when grown on melibiose than on glucose.

• 대한화학회지
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• 제31권2호
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• pp.168-177
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• 1987

극성용매(L; ANT, MFA, DMSO, DMF, DMA)에서 $\alpha$-Ni(rac-[14]-decane)$^{2+}$의 화학평형 관계를 상온에서 분광광도법으로 연구하였다. ANT, MFA, DMSO, DMF, DMA일 때 평행상수 $K_1$은 각각 31.0, 27.5, 21.3 15.9, 6.4이었으며 $K_2$는 $K_1$보다 적은 값이었다. $\alpha$-Ni(rac-[14]-dacane)$^{2+}$ + L $\leftrightharpoons$ [$\alpha$-Ni(rac-[14]-decane){\cdot}L]$^{2+}$ : $K_1$[$\alpha$-Ni(rac-[14]-decane){\cdot}L)$^{2+}$ + L $\leftrightharpoons$ [$\alpha$-Ni(rac-[14]-decane){\cdot}$L_2$)$^{2+}$; $K_2$.ACT에서 Ni(II)-macrocycle 착이온의 d-d흡수에너지 ($cm^{-1}$와 환원 반파전위 ($E_{1/2}$, V vs. SCE)사이의 상관성을 조사하였다. d-d 전이에너지를 크게하는 거대고리 리간드일수록 착이온의 반파전위는 좀더 양의 값으로 이동하였다. Ni(rac-1[14]7-diene)$^{2+}$, Ni(meso-1[14]7-diene)$^{2+}$, Ni(1[14]4-diene)$^{2+}$, $\alpha$-Ni(rac-[14]-decane)$^{2+}$, $\beta$-Ni(rac-[14]-decane)$^{2+}$, Ni(meso-[14]-decane)$^{2+}$ 착이온의 환원반파전위는 각각 -1.419, -1.431, -1.450, -1.473, -1.480 (V vs. SCE)이었다. 몇 가지 용매에서 Ni(meso-[14]-decane)$^+$ 이성질체의 d-d전이에너지($\nu_{max},\;cm^{-1}$) 변화와 용매의 유전상수(${\varepsilon}/{\varepsilon}_0$) 관계를 고찰하였으며 ${\varepsilon}/{\varepsilon}_0$가 클수록 $\nu_{max}(cm^{-1})$는 증가하였다.

• 약학회지
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• 제41권4호
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• pp.498-511
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• 1997

The effects of UK 14,304, an ${\alpha}_2$-adrenergic agonist, on renal function were investigated in dogs. UK 14,304, when given intravenousely($15.0{\mu}g/kg,\;50{\mu}g/kg$), produced the increase of urine flow accompanied with the marked augmentation of free water clearance ($C_{H_2O}$) and reabsorption rates of sodium in renal tubules ($R_{Na}$), and the remarkable decrease of osmolar clearance ($C_{osm}$) and the amounts of sodium excreted in urine ($E_{Na}$). UK 14,304 given into a renal artery($1.5{\mu}g/kg,\;5.0{\mu}g/kg$) elicited the increase of urine flow with the augmentation of $C_{H_2O}$ in both kidney. UK 14,304, when administered into carotid artery($3.0{\mu}g/kg,\;10.0{\mu}g/kg$). exhibited the same aspect as shown in intravenous UK 14.304 at smaller dose than the intravenous dose. Diuretic action of intravenous UK 14,304 were produced together with increase of $C_{H_2O}$ in situation of water diuresis too, changes of renal function in this state were the increase of $C_{osm},\;E_{Na},\;and\;E_K$ (excreted amounts of potassium in urine), and the decrease of $R_{Na}\;and\;R_K$, these were different appearances from situation of saline diuresis. Diuretic action of intravenous UK 14,304 were blocked completely by post or pretreatment of yohim-bine, ${\alpha}_2$-adrenergic blocking agents, and inhibited by pretreatment of vasopressin, antidiuretic hormone. Above results suggest that UK 14,304 produces the diuretic action by the inhibition of vasopressin secretion and suppression of electrolytes reabsorption of electrolytes in renal tubules mediated with central ${\alpha}_2$-adrenoceptor in dog.

• Archives of Pharmacal Research
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• 제17권5호
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• pp.323-326
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• 1994

Three new sesquiterpene lactone glucosides named dentatins A, B and C were isolated from lxeris dentata and the structures were elucidated as $3{\betha}, {\;}8{\betha}-dihydroxy-(1{\alpha}, 5{\alpha})guainan-10(14)-ene-6{\alpha}, {;\}12-olide-3-O-{\betha}-D-giucopyuranoside{\;}(1), {\;}3{\betha}, {\;}8{\betha}-dihydroxy-(1{\alpha}, {\;}5{\alpha})-guaian-4(15), {\;}10(14)-diene-6{\alpha}, {\;}12-plide-3-O-{\betha}-D-glucopyranoside{\;}(3)$, respectively, on the basis of spectral evidence.

• 약학회지
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• 제29권2호
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• pp.62-69
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• 1985

The isomeric intermediates, $3{\alpha}$and $3{\beta}-amino-5{\alpha}-cholestane required for the synthesis of N-nitrosoureas, N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{\alpha}-amino-5{\alpha}$-cholestane (9), N-methyl-N-nitrosocarbamoyl-3${\alpha}-amino-5{\alpha}-cholestane$ (10), N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{\beta}-amino-5{\alpha}-cholestane$: (7), and N-methyl-N-nitrosocarbamoyl-$3{\beta}-amino-5{\alpha}-cholestane$ (8) were obtained through the $LiAlH_{4}$ reduction of $5{\alpha}$-cholestan-3-one oxime, followed by the chromatographic separation: the assignment of the stereochemistry of both isomers were based on the shape and chemical shift of $C_{3}$-proton resonances on their NMR spectra and on the elution mobility on the TLC. The urea intermediates, N-(2-chloroethyl) carbamoyl-3.alpha.-amino-5.alpha.-cholestane (13), N-methylcarbamoyl-$3{\alpha}-amino-5{\alpha}-cholestane$ (14), N-(2-chloroethyl) carbamoyl-$3{\beta}-amino-5{\alpha}-cholestane (11) and N-methyl-$3{\beta}-amino-5{\alpha}$-cholestane (12) were prepared by the treatment of each isomers ($3{\alpha}$-amino-and $3{\beta}-amino-5{\alpha}$-cholestane) with alkyl isocyanates in anhydrous $CHCl_{3}$, and the corresponding nitrosoureas, 7-10 were obtained by the nitrosation of the ureas, 11-14, with AcOH (or HCOOH)/$NaNO_{2}$ in ice-cold condition. The inhibitory activity of the nitrosoureas, 7-10, and their intermediates, 12-14 towards the growth of L1210 murine leukemia cells, were examined. Among them, the compounds 9 and 10 exhibited high activity having $ED_{50}$ to be 5.5g/ml and 6.1g/ml, respectively.

• Journal of Pharmaceutical Investigation
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• 제17권4호
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• pp.213-216
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• 1987

The distribution features of recombinant human $alpha-interferon(rHuIFN-{\alpha}A)$ and $^{14}C-radiolabeled\;rHuIFN-{\alpha}A\;(^{14}C-rHuIFN-{\alpha}A)$ were investigated in ICR mice after i.v. injection. The level of $rHuIFN-{\alpha}A$ in the kidney was significantly higher than those in lung and liver at 10min after the injection. But the level was reduced significantly at 60min. The level of radioactivity in the kidney was also significantly higher than those in other organs after i.v. injection of $^{14}C-rHuIFN-{\alpha}A$, but it was reduced at much slower speed than was $rHuIFN-{\alpha}A$. These results show that interferon is distributed repidly and the kidney is the main site of distribution and metabolism of $rHuIFN-{\alpha}A$.