• Archives of Pharmacal Research
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• v.28 no.10
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• pp.1156-1160
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• 2005

An iridoid glycoside, oldenlandoside III (5) was isolated from the n-butanol fraction of methanol extracts of the aerial parts of Oldenlandia diffusa Roxb. along with six others previously characterized iridoid glycosides; geniposidic acid (1), scandoside (2), feretoside (3), 10-O-ben-zoylscandoside methyl ester (4), asperulosidic acid (6) and deacetylasperulosidic acid (7). Compounds 1, 2, and 7 inhibited LDL-oxidation, and showed $63.3{\pm}2.0,\;62.2{\pm}1.6,\;and\;63.8{\pm}1.5\%$ inhibition, respectively, at a concentration of 20 ${\mu}g/mL$.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.546-549
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• 2005

A new oleanane-triterpene, 3${\beta}$-acetoxy-11${\alpha}$-benzoyloxy-13${\beta}$-hydroxyolean-1 2-one (1), was isolated along with a known quinone-methide triterpene, pristimerin (2), from the root bark of Siphonodon celastrinneus Griff., a Thai medicinal plant of the family Celastraceae. Their structures were determined based on spectroscopic analysis.

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.640-642
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• 2002

The ethyl acetate fraction of Bupleurum longiradiatum was found to have an inhibitory effect on the tube-like formation of human umbilical venous endothelial (HUVE) cells. The active compounds, isolated from the fraction, were identified as acetylbupleurotoxin (P1) and bupleurotoxin (P2). The compounds P1 and P2 completely inhibited the tube-like formation of HUVE cells at 30 ${\mu}g$/ml, below the cytotoxic concentration. But, they did not exhibit antitumor activity on BDF1 mice bearing Lewis lung carcinoma cells despite their antiangiogenic activity.

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.585-589
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• 2002

Three hairpin polyamides were designed and synthesized by a haloform reaction and DCC/HOBt coupling reaction without amino protection and deprotection. Their anticancer activity were investigated with three kinds of cell lines-hepatic carcinoma, lung carcinoma and gastric carcinoma, and the values of $IC_{50}$ were at range of $10^{-7}~10^{-8}M$.

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.600-607
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• 2002

Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2a∼2f) and 3-aryl-2-(3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a∼3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.625-627
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• 2002

From the leaves of Brassica juncea, an radical scavenging isorhamnetin 7-Ο-glucoside on peroxynitrite and 1,1-diphenyl-2-picrylhydrazyl (DPPH) was isolated and characterized based on the spectroscopic evidence. The compound showed the peroxynitrite and DPPH scavenging activities with $IC_{50}$ values of 2.07$\pm$0.17 and 13.3 $\mu$M, respectively. Penicillamine and L-ascorbic acid as positive control exhibited radical scavenging activities with $IC_{50}$ values of 3.17$\pm$0.39 and 12.78 $\mu$M, respectively.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1211-1215
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• 2004

Ten coumarins were isolated from the root of Angelica dahurica by repeated silica gel column chromatography. Their chemical structures were elucidated on the basic of physicochemical and spectroscopic data. Among them, oxypeucedanin hydrate acetonide (7) was isolated for the first time from this plant. Cytotoxicity of coumarins isolated were determined in vitro against L1210, HL-60, K562, and B16F10 tumor cell lines by MTT method. Pangelin (5) and oxypeucedanin hydrate acetonide (7) showed a potent cytotoxic activity with the $IC_{50}$ values of 8.6 to 14.6 ${\mu}g$ /mL against four kinds of tumor cell lines. Other compounds showed the moderate cytotoxic activity or no activity against the tumor cell lines.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1216-1219
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• 2004

Spinoside, new coumaroyl flavone glycoside was isolated from the n-butanol fraction of the mathanolic extract of the whole plant of Amaranthus spinosus and assigned the structure 7-pcoumaroyl apigenin 4-O-${\beta}$ -D-glucopyranoside (1) on the basis of spectroscopic techniques including 1D and 2D NMR spectroscopy. In addition ${\alpha}$ - xylofuranosyl uracil (2), ${\beta}$ -D-ribofuranosyl adenine (3) and ${\beta}$ -sitosterol glucoside (4) have also been isolated for the first time from this species.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1253-1257
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• 2004

6-Methoxydihydrosanguinarine (6ME), a benzophenanthridine alkaloid derived from the methanol extracts of Hylomecon hylomeconoides, showed a dose-dependent effect at 1-10 ${\mu}M$ on causing apoptotic cell death in HT29 colon carcinoma cells $(IC_{50} = 5.0{\pm}0.2 {\mu}M)$. Treatment of HT-29 cells with 6ME resulted in the formation of internucleosomal DNA fragmentation. Treatment of the cells with 6ME caused activation of caspase-3, -8 and 9 protease and subsequent proteolytic cleavage of poly(ADP-ribose)polymerase. 6ME increased the expression of p53 and Bax and decreased the expression of Bid. These results indicate that p53 and proapoptotic Bcl-2 family proteins might participate in the antiproliferative activity of 6ME in HT29 cells.

• Archives of Pharmacal Research
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• v.26 no.2
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• pp.147-150
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• 2003

To find anticancer agents from higher plants, DNA strand-scission assay method was employed for bioassay-guided fractionation as well as for screening the crude extracts. During the screening, an ethyl acetate extracts of the heartwood of Caesalpinia sappan L. (Leguminosae) exhibited potent DNA strand-scission activity. Therefore, the ethyl acetate extracts of the dried heartwood of C. sappan was subjected to the bioassay-guided fractionation, which led to the isolation of a known compound, brazilin (1) as the active constituent. In addition, caesalpine J (2) was also isolated as an inactive constituent.