• Archives of Pharmacal Research
• /
• v.28 no.2
• /
• pp.172-176
• /
• 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.

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.67.1-67.1
• /
• 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
• /
• v.17 no.3
• /
• pp.1399-1404
• /
• 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.

• Journal of Life Science
• /
• v.13 no.2
• /
• pp.206-213
• /
• 2003

This study was conducted to estimate volatile compounds in pericarp of Zanthoxylum piperitum DC (Chopi). Chopi which harvested on lune 2, July 14 and September 11 in 2001 was dried at room temperature for one week. Fifty-two, 47, and 44 volatile compounds were analyzed with GC-MS in pericarp harvested on lune 2, July 14 and September 11, respectively. Eight terpenes including myrcene, ${\gamma}$-terpinene, $\alpha$-terpinolene, $\alpha$-phellandrene and $\beta$-caryophyllene were detected in pericarp harvested on tulle 2 and July 14, but not $\alpha$-phellandrene and $\beta$-caryophyllene in pericarp harvested on September 11. Thirteen alcohols or terpene alcohols including linalool L and citronellol were detected in pericarp harvested on lune 2, and added cis-linallol oxide and piperitol isomer in pericarp harvested on July 14 and September 11. Three aldehydes or terpene aldehydes were not affected by degree of maturation, but citronellal was increased in pericarp harvested on September 11. Five volatile compounds of ketones containing cryptone and piperitone were detected, and their concentration was changed during maturation. Six esters including lavandulyl acetate and $\alpha$-terpinenyl acetate were detected in pericarp harvested on lune 2, and [(E)-6,7-ephoxy-3,7-dimethyl-2-octenyl]ester of acetic acid was added in pericarp harvested on July 14 and September 11. Seven hydrocarbons including $\delta$-cadinene and neopentylidene cyclohexane were detected in pericarp harvested on June 2 and $\alpha$-muurolene was newly added in pericarp harvested on July 14 and September 11. We suggest that kinds and concentration of volatile compounds in pericarp were remarkably different from those in mature stage.

• Food Science and Biotechnology
• /
• v.17 no.5
• /
• pp.1115-1118
• /
• 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.

• Journal of the Korean Chemical Society
• /
• v.31 no.2
• /
• pp.168-177
• /
• 1987

The equilibria of chemical reaction between $\alpha$-Ni(rac-[14]-decane)$^{2+}$ and polar solvents(L; ANT, MFA, DMSO, DMF, and DMA) have been investigated by the spectrophotometric method at $25^{\circ}C$. (The equilibrium constants($K_1$) of) the first step in ANT, MFA, DMSO, DMF, and DMA were 31.0, 27.5, 21.3 15.9, and 6.4, respectively. The smallness of equilibrium constants ($K_2$) of the second step compared with $K_1$, was observed. $\alpha$-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}$L_2$)$^{2+}$ :$K_2$. The relationship between d-d absorption energy and half-wave potential of complex ions at ACT was considered. Macrocyclic ligands increasing d-d transition energy caused half-wave potentials of Ni(II)-macrocycle to be shifted more positively. The half-wave potentials for 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+}$, and Ni(meso-[14]-decane)$^{2+}$ reductions were -1.419, -1.431, -1.450, -1.473, and -1.480 (V vs. SCE), respectively. The d-d transition energies ($\nu_{max},\;cm^{-1}$) of the Ni(meso-[14]-decane)$^{2+}$ isomer were discussed with the dielectric constant (${\varepsilon}/{\varepsilon}_0$) of the various solvents, $\nu_{max}(cm^{-1})$ increased with increasing ${\varepsilon}/{\varepsilon}_0$.

• YAKHAK HOEJI
• /
• v.41 no.4
• /
• pp.498-511
• /
• 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
• /
• v.17 no.5
• /
• pp.323-326
• /
• 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.

• YAKHAK HOEJI
• /
• v.29 no.2
• /
• pp.62-69
• /
• 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
• /
• v.17 no.4
• /
• pp.213-216
• /
• 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 $rHuIFN-{\alpha}A$.