• Archives of Pharmacal Research
• /
• v.15 no.1
• /
• pp.52-57
• /
• 1992

The molecular structure of a natural compound was determined by single crystal X-ray diffraction analysis. The compound was isolated by methanol extraction and repeated chromatography from the stem of Paulownia tomentosa. Yellow prismatic crystals of the compound, which were recrystallized from tetrahydrofuran, are triclinic, with a = 7.310 (6), b = 10.753(6), c = 11.586(5) ${\AA}.\;\alpha= 93.30(6),\;\beta=105.62(10),\;\gamma=109.49(7)^\circ,\;D_x=1.514,\;D_m=1.51 g/cm^3$, space group P1 and Z = 2. The structure was solved by direct method, and refined by least-squares procedure to the final R-value of 0.032 for 1271 independent reflections $(F\le3\sigma{(F))}$. The compound is one of new furanquinone analogue. The molecule has a nearly planar conformation with an intramolecular hydrogen bond. In the crystal, the planar molecules are arranged as a prallel sheet-like pattern, and these stackings are stabilized by the O-H...O type intermolecular hydrogen bonds. The other intermolecular contacts appear to be the normal van der Waals interactions.

• Archives of Pharmacal Research
• /
• v.19 no.3
• /
• pp.197-200
• /
• 1996

6-[(N-2,3-Dichlorophenyl)aminol-7-chloro-5,8-quinolinedione (RCK1 1) was tested for in vivo antifungal activities in the treatment of systemic infection with Canclicla albicans in normal mice compared with ketoconazole. The therapeutic potential of RCK11 had been assessed by evaluating their activities (survival rates) against systemic infections in normal mice. $ED_{50}$ of intraperitoneally administered RCK11 was $0.10\pm0.01 mg/kg$ but that of ketoconazole had $8.00\pm0.73 mg/kg$ respectively. When RCK11 was administered intravenously at the $ED_{50}$(0.10 mg/kg), the colony counts of Canoliola albicans in the liver after 7 days and 14 days were reduced as likely as ketoconazole at the $ED_{50}$ (8.00 mg/kg), and the better survival rates than ketoconazole were achieved after 14 days. The results suggest that RCK11 may be a potent antifungal agent.

• Journal of the Korean Society of Clothing and Textiles
• /
• v.34 no.6
• /
• pp.1042-1052
• /
• 2010

The Degradation of amur cork tree extract is investigated by GC-MS after treating the dye with three thermal degradation systems of, room temperature (RT), $4^{\circ}C$ refrigeration (LT), $100^{\circ}C$ oven (OV), and $H_2O_2$/UV/$O_2$ (PER) degradation system for 0-24 days. It was found that PER degradation system represented the highest intensity of degradation treatment followed by OV treatment among the four degradation parameters. The possible fingerprint products of amur cork tree dye, that yielded 68% (or higher) reliability in the NIST spectral match, were isobenzofuran-1,3-dione,4,5-dimethoxy- (8.37 min, PER only), 1,3-dioxolo[4,5-g]isoquinolin-5(6H)-one,7,8-dihydro (9.41 min, PER only), canthine-6-one (10.24 min, RT, LT, OV only), and dihydroberberine (15.05 min, RT, LT, OV, PER) in the order of higher to lower possibility of detection. Unknown products 7 (13.43 min) and 8 (16.35 min) are two other possible fingerprint products of amur cork tree dye that require future identification.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.5
• /
• pp.1613-1619
• /
• 2011

A hybrid thermosetting maleimido epoxy compound 4-(N-maleimidophenyl) glycidylether (N-MPGE) containing Co(II), Ni(II) and Cu(II) ions was prepared by curing N-MPGE and tetradentate Schiff base Co(II), Ni(II) and Cu(II) complexes. The curing polymerization reaction of N-MPGE with metal complexes as curing agents was studied. The cured samples were studied for thermal stability, chemical (acid/alkali/solvent) and water absorption resistance and homogeneity of the cured systems. The tetradentate Schiff base, 3-[(Z)-2-piperazin-1-yl-ethylimino]-1,3-dihydro indol-2-one was synthesized by the condensation of Isatin (Indole-2, 3-dione) with 1-(2-aminoethyl)piperazine (AEP). Its complexes with Co(II), Ni(II) and Cu(II) have been synthesized and characterized by microanalysis, conductivity, Uv-Visible, FT-IR, TGA and magnetic susceptibility measurements. The spectral data revealed that the ligand acts as a neutral tetradentate Schiff base and coordinating through the azomethine nitrogen, two piperazine nitrogen atoms and carbonyl oxygen.

• Journal of Integrative Natural Science
• /
• v.8 no.1
• /
• pp.19-29
• /
• 2015

In view of the growing medicinal importance of chromene and its derivatives, the single crystal X-ray diffraction study was carried out for the potential active 4,6-dimethyl-9-phenyl-8,12-dioxa-4,6-diazatetracyclo [8.8.0.02,7.013,18]octadeca-2(7),13,15,17-tetraene-3,5,11-trione-2-ethoxyphenyl (2E)-but-2-enoate ($C_{18}H_{20}N_2O_5$). In the title compound are two molecules exist in the asymmetric unit. It crystallizes in the monoclinic space group $P2_1/c$ with unit cell dimension a=14.608(3) ${\AA}$, b=12.845(3) and c= 17.781(4) [alpha & gamma=$90^{\circ}$ beta=$91.233(5)^{\circ}$]. Both pyran and pyran ring of the chromene moiety adopts sofa conformation in the molecule A & B. The crystal structure is stabilized by intramolecular C-H...O hydrogen bond interaction.

• Journal of Microbiology and Biotechnology
• /
• v.4 no.2
• /
• pp.119-125
• /
• 1994

Steroid $\Delta^1$-dehydrogenase purified from hydrocortisone-induced cells of Arthrobacter simplex converted various 3-ketosteroids into their corresponding $\Delta^1$-dehydrogenated products. The transformation efficiencies depend upon the chemical structure of the steroids, especially length of the side chain at 17 position and hydroxyl groups at 11 and 17 positions. The Km values for androstenedione, the most favorable substrate examined, and hydrocortisone were 74 ${\mu}M$ and 294 ${\mu}M$, respectively. The optimum temperature and pH of the enzyme reaction were 35$^{\circ}C$ and pH 9, respectively, and the enzyme was relatively stable at the range from 20 to 35$^{\circ}C$ and from pH 5 to 10 after one hour of incubation. The enzyme activity was markedly inhibited in the presence of $Cu^{2+},\;Fe^{3+},\;Hg^{2+},\;Mo^{6+}$ ions, and somewhat inhibited by $Zn^{2+}$ and $Fe^{2+}$. $\alpha,\alpha'$-Dipyridyl that inhibits 9$\alpha$-hydroxylase and accumulates 1,4-androstadiene-3,17-dione from sterols revealed no inhibitory effect on this enzyme. EGTA showed inhibitory effect. $\beta$-Estradiol competitively inhibited the enzyme activity. Chemical modifications of the enzyme were attempted with several reagents. p-Hydroxymer-curibenzoate showed inhibition of the enzyme activity and protection of the substrate. This suggests that cysteine residue may be involved in the active site of the enzyme.

• Journal of Microbiology and Biotechnology
• /
• v.27 no.6
• /
• pp.1065-1070
• /
• 2017

This study aimed to examine the anti-candidal efficacy of a novel ketone derivative isolated from Diaporthe sp. ED2, an endophytic fungus residing in medicinal herb Orthosiphon stamieus Benth. The ethyl acetate extract of the fungal culture was separated by open column and reverse phase high-performance liquid chromatography (HPLC). The eluent at retention time 5.64 min in the HPLC system was the only compound that exhibited anti-candidal activity on Kirby-Bauer assay. The structure of the compound was also elucidated by nuclear magnetic resonance and spectroscopy techniques. The purified anti-candidal compound was obtained as a colorless solid and characterized as 3-hydroxy-5-methoxyhex-5-ene-2,4-dione. On broth microdilution assay, the compound also exhibited fungicidal activity on a clinical strain of Candida albicans at a minimal inhibitory concentration of $3.1{\mu}g/ml$. The killing kinetic analysis also revealed that the compound was fungicidal against C. albicans in a concentration- and time-dependent manner. The compound was heat-stable up to $70^{\circ}C$, but its anti-candidal activity was affected at pH 2.

• Journal of Microbiology and Biotechnology
• /
• v.19 no.11
• /
• pp.1333-1341
• /
• 2009

Haematococcus pluvial is, a green alga, accumulates astaxanthin (3,3'-dihydroxy-$\beta$,$\beta$'-carotene-4,4'-dione) upto 2-3% on a dry weight basis. In the present study, identification of carotenoids from Haematococcus cyst cell extract by HPLC and LC-MS (APCI) and their antioxidant properties were evaluated in in vitro model systems. The extract exhibited 89% and 78% antioxidant activities in the $\beta$-carotene linoleate model and the hydroxyl radical scavenging model, at 9 ppm of total carotenoid, respectively. The extract also showed 80%, 85%, and 79% antioxidant activities against lipid peroxidation in the kidney, brain, and liver of rats. Low-density lipoprotein oxidation induced by $Cu^{2+}$ ions was also protected (45%, 64%, and 75%) by the extract in a dose-dependent manner with different carotenoid levels. Thiobarbituric acid reactive substances concentration in the blood, liver, and kidney of rats were also significantly (p<0.005) decreased in H. pluvialis-treated rats. The potent antioxidant activity is attributable to various carotenoids present in the extract.

• Archives of Pharmacal Research
• /
• v.28 no.10
• /
• pp.1147-1151
• /
• 2005

A new naturally occurring sterol, compound 5, and six known stigmasterols were isolated from fruits of Ailanthus altissima Swingle by repeated column chromatography and RP-HPLC. Their structures were identified as, 5${\alpha}$-stigmastane-3,6-dione (1), 3${\beta}$-hydroxystigmast-5-en-7-one (2), stigmast-5-ene-3${\beta}$, 7${\alpha}$-diol (3), 6${\alpha}$-hydroxystigmast-4-en-3-one (4), 5${\alpha}$-stigmastane-3${\beta}$, 6${\beta}$-diol (5), stigmast-4-ene-3${\beta}$, 6${\alpha}$-diol (6), stigmast-5-ene-3${\beta}$, 7${\alpha}$, 20$\xi$-triol (7) by spectral analysis and comparison with the published data. These compounds have not been reported from genus Ailanthus, whereas compound 7 was identified by NMR for the first time. In addition, the $95\%$ ethanol extract and compounds from the fruits of Ailanthus altissima SWINGLE were assayed for in vitro antimicrobial activity. The extract was potent active against the assayed bacteria while compounds 3 and 7 exhibited moderate activity.

• Bulletin of the Korean Chemical Society
• /
• v.34 no.8
• /
• pp.2381-2386
• /
• 2013

A new series of Mn(II) and Mo(VI) complexes containing the Schiff bases hydrazinecarbothioamide and hydrazinecarboxamide of 5,6-dimethyl-1H-indol-2,3-dione have been synthesized. The nature of bonding and the stereochemistry of the complexes have been deduced from elemental analyses, molecular weight determinations and spectral studies viz. electronic IR, ESR, $^1H$ NMR and $^{13}C$ NMR and X-ray diffraction spectral studies. The magnetic moment values of the manganese(II) complexes are in the range of 5.80-6.15 B.M. suggesting a high spin state of manganese in these complexes. The spectral data are consistent with a tetrahedral geometry around Mn(II) and an octahedral geometry for Mo(VI), in which the ligands act as bidentate chelating agents, coordinated through the nitrogen and sulfur/oxygen atoms. The ligands and their metal complexes have been tested against a number of pathogenic fungi and bacteria at different concentrations and were found to possess sufficient fungicidal and bactericidal properties. Further, the complexes were also tested for their antifertility activity in male albino rats and the results were indeed positive.