• Korean Journal of Pharmacognosy
• /
• v.31 no.2
• /
• pp.125-129
• /
• 2000

Three sesquiterpene lactones (1, 2 and 5) and two lipid glycerols (3 and 4) were isolated from MeOH extract of Ainsliaea acerifolia (Compositae). Based on spectral data, their chemical structures were determined as estafiatone (1), zaluzanin C (2), 3-O-(9Z, 12Z, 15Z-octadecatrienoyl) glycerol (3), 3-O-(9Z, 12Z-octadecadienoyl) glycerol (4) and glucozaluzanin C (5). Compounds 1, 3 and 4 were previously not reported from Ainsliaea species.

• Asian Pacific Journal of Cancer Prevention
• /
• v.16 no.15
• /
• pp.6317-6325
• /
• 2015

Ginkgo biloba extract (GBE) is a popular phytomedicine and has been used for disorders of the central nervous system, cardiovascular, renal, respiratory, and circulatory diseases. Although GBE is a complex mixture of over 300 compounds, its major components are 24% flavonoids and 6% terpene lactones. In this study, we tested the inhibitory effects of the three major flavonoids (kaempferol, quercetin, and isorhamnetin) from GBE, independently and as mixtures, on aromatase activity using JEG-3 cells (human placental cells) and recombinant proteins (human placental microsome). In both systems, kaempferol showed the strongest inhibitory effects among the three flavonoids; the flavanoid mixtures exerted increased inhibitory effects. The results of exon I.1-driven luciferase reporter gene assays supported the increased inhibitory effects of flavonoid mixtures, accompanied by suppression of estrogen biosynthesis. In the RT-PCR analysis, decreased patterns of aromatase promoter I.1 mRNA expressions were observed, which were similar to the aromatase inhibition patterns of flavonoids and their mixtures. The present study demonstrated that three flavonoids synergistically inhibit estrogen biosynthesis through aromatase inhibition, decrease CYP19 mRNA, and induce transcriptional suppression. Our results support the usefulness of flavonoids in adjuvant therapy for breast cancer by reducing estrogen levels with reduced adverse effects due to estrogen depletion.

• YAKHAK HOEJI
• /
• v.56 no.3
• /
• pp.173-179
• /
• 2012

Saussurea lappa (SL) and major compounds, sesquiterpene lactones, have been suggested to possess various biological effects, including anti-tumor, anti-ulcer, anti-inflammatory, anti-viral and cardiotonic activities. Therefore, the ethanol extract of Saussurea lappa root (ESL) is studied for the mechanism of its action in apoptotic pathway. ESL-treated cells manifested nuclear condensation, and fragmentation. ESL also triggered the mitochondrial apoptotic pathway, as indicated by a change in Bax/Bcl2 ratio and caspase-9/-3 activation. ESL induced p38 MAPK/JNK, p53, and ASK1 phosphorylation. ROS scavenger reversed ESL-induced apoptotic cell death via inhibition of caspase-3 and p38 MAPK/JNK phosphorylation. These results suggest that ESL induced apoptosis in HepG2 cells through the ROS-p38/JNK pathway.

• Proceedings of the KOSOMBE Conference
• /
• v.1998 no.11
• /
• pp.229-230
• /
• 1998

Triblock copolymers from poly(ethylene glycol) (PEG) and D,L-lactide or $\varepsilon$-carprolactone were synthesized to prepare semi-interpenetrating polymer network (semi-IPN) with chitosan by U.V. irradiation method. Then, solute permeation through these semi-IPNs hydrogels were investigated. The structures of semi-IPNs were confirmed by FT-IR spectroscopy and wide angle X-ray diffractometer (WAXD). Equilibrium water content (EWC) of these hydrogels was in the range of 67-75%. The crystallinity, thermal properties and mechanical properties of semi-IPNs hydrogels were studied. All the hydrogels revealed a remarkable decrease in crystallinity as compared with PEG macromer itself. The tensile strengths of semi-IPNs hydrogels in dry state were rather high, but those of hydrogels in wet state decreased drastically. The permeabilities of solutes of hydrogels followed the swelling behaviors and were regulated by solute size.

• Research in Plant Disease
• /
• v.24 no.2
• /
• pp.162-169
• /
• 2018

The GacS/GacA system in the root colonizer Pseudomonas chlororaphis O6 is a key regulatory system of many traits relevant to the plant probiotic nature of this bacterium. The work in this paper elucidates proteins using proteomics approach in P. chlororaphis O6 under the control of the cytoplasmic regulatory protein, GacA. A gacA mutant of P. chlororaphis O6 showed loss in production of phenazines, acyl homoserine lactones, hydrogen cyanide, and protease, changes that were associated with reduced in vitro antifungal activity against plant fungal pathogens. Production of iron-chelating siderophore was significantly enhanced in the gacA mutant, also paralleling changes in a gacS mutant. However, proteomic analysis revealed proteins (13 downregulated and 7 upregulated proteins in the mutant compared to parental strain) under GacA control that were not apparent by a proteomic study of a gacS mutant. The putative identity of the downregulated proteins suggested that a gacA mutant would have altered transport potentials. Notable would be a predicted loss of type-VI secretion and PEP-dependent transport. Study of mutants of these GacA-regulated proteins will indicate further the features required for probiotic potential in this rhizobacterium.

• Korean Journal of Soil Science and Fertilizer
• /
• v.30 no.3
• /
• pp.295-300
• /
• 1997

Flavor components of natively grown tea plant(Camellia sinensis O. kuntze) in Korea, collected from 12 locations, were analyzed by gas chromatograph and mass spectrometer. Seventy to eighty flavor components in tea leaves were separated by GC. Total 52 flavor components were identified by comparing gas chromatograhp retention time and mass spectral date. They were classified as 19 alcohols, 5 aldehydes, 2 hydrocarbons, 6 ketones, 4 esters, 3 lactones, 2 acids, 3 phenols, 4 pyrazines, and 4 nitrogenous compounds. Major compounds identified were geraniol, linalool oxide, 1-hexanol and ethanol.

• Korean Journal of Medicinal Crop Science
• /
• v.9 no.4
• /
• pp.269-274
• /
• 2001

Two sesquiterpene lactones were isolated from the flowers of Chrysanthemum coronarium L. by silica gel chromatography and recrystalization. Their structures were determined using various spectroscopic data, and were identified as eudesmanolide derivatives douglanine and reynosin, respectively. This is reported for the first time in this plant. The cytotoxic activity of two compounds showed strong activities against human cancer cell lines such as A549, PC-3 and HCT 116.

• Archives of Pharmacal Research
• /
• v.21 no.4
• /
• pp.452-457
• /
• 1998

Three compounds, 5-(acetoxymethyl)-5-(hydroxymethyl)-3-tetradecyl-2,5-dihydro-2-furanone (3), 5-(acetoxymethyl)-5-(hydroxymethyl)-3,3-dihexyltetrahydro-2-furanone (4) and 5-(acetoxymethyl)-5-(hydroxymethyl)-3,3-dioctyltetrahydro-2-furanone (5), were designed and synthesized as surrogates of the ultrapotent DAG analogue, 5-(acetoxymethyl)-5-(hydroxymethyl) 3-[(Z)-tetradecylideneltetrahydro-2-furanone (1), a compound that showed high affinity for PKC-$\alpha$ ($K_1$=35 nM) in a competition binding assay with [$^3H$-20]phorbol-12,13-dibutyrate (PDBU). In an attempt to overcome the problem of generating geometrical E- and Z- isomers, as encountered with 1, the double bond was moved to an endocyclic location as in 3, or an additional alkyl chain was appended to C3 to give the corresponding 3,3-dialkyl saturated lactones (4 and 5). The lactone was constructed from glycidyl-4-methoxyphenyl ether in 5 steps. The target compounds showed reduced binding affinities for PKC-.alpha. with $K_{i}$ values of 192 nM (3), 4,829 nM (4), and 2,812 nM (5), respectively. These results indicate that constrained DAG analogues having a tetrahydro-2-furanone template are effectively discriminated by PKC-(X in terms of the direction of the long alkyl chain connected to the 3-position.n.

• Bulletin of the Korean Chemical Society
• /
• v.18 no.3
• /
• pp.274-280
• /
• 1997

The rates and stoichiometry of the reaction of gallane-trimethylamine with selected organic compounds containing representative functional groups were examined in tetrahydrofuran solution under standardized conditions (THF, 0 ℃). And its reducing characteristics were compared with those of aluminum hydride-triethylamine(AHTEA). The rate of hydrogen evolution from active hydrogen compounds varied considerably with the nature of the functional group and the structure of the hydrocarbon moiety. Alcohols, phenol, amines, thiols evolved hydrogen rapidly and quantitatively. Aldehydes and ketones were reduced moderately to the corresponding alcohols. Cinnamaldehyde was reduced to cinnamyl alcohol, which means that the conjugated double bond was not attacked by gallane-trimethylamine. Carboxylic acids, esters, and lactones were stable to the reagent under standard conditions. Acid chlorides also were rapidly reduced to the corresponding alcohols. Epoxides and halides were inert to the reagent. Caproamide and nitrile were stable to the reagent, whereas benzamide was rapidly reduced to benzylamine. Nitropropane, nitrobenzene and azoxybenzene were stable to the reagent, whereas azobenzene was reduced to 1,2-diphenylhydrazine. Oximes and pyridine N-oxide were reduced rapidly. Di-n-butyl disulfide and dimethyl sulfoxide were reduced only slowly, but diphenyl disulfide was reduced rapidly. Finally, sulfones and sulfonic acids were inert to the reagent under the reaction.

• 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)