• Biomolecules & Therapeutics
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• v.15 no.2
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• pp.95-101
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• 2007

Resveratrol (3,5,4’-trihydroxy-trans-stilbene), a naturally occurring phytoallexin abundant in grapes and several plants, has been shown to be active in inhibiting proliferation and inducing apoptosis in several human cancer cell lines. On the line of the biological activity of resveratrol, a variety of resveratrol analogs were synthesized and evaluated for their growth inhibitory effects against several human cancer cell lines. In the present study, we found that one of the resveratrol analogs, 3,4,5-trimethoxy-4’-bromo-cis-stilbene, markedly suppressed human colon cancer cell proliferation (EC$_{50}$ = 0.01 ${\mu}$g/ml), and the inhibitory activity was superior to its corresponding trans-isomer (EC$_{50}$ = 1.6 ${\mu}$g/ml) and resveratrol (EC$_{50}$ = 18.7 ${\mu}$g/ml). Prompted by the strong growth inhibitory activity in cultured human colon cancer cells (Col2), we investigated its mechanism of action. 3,4,5-Trimethoxy-4’-bromo-cis-stilbene induced arrest of cell cycle progression at G2/M phase and increased at sub-G1 phase DNA contents of the cell cycle in a time- and dose-dependent manner. Colony formation was also inhibited in a dose-dependent manner, indicating the inhibitory activity of the compound on cell proliferation. Moreover, the morphological changes and condensation of the cellular DNA by the treatment of the compound were well correlated with the induction of apoptosis. These data suggest the potential of 3,4,5-trimethoxy-4’-bromo-cis-stilbene might serve as a cancer chemotherapeutic or chemopreventive agent by virtue of arresting the cell cycle and inducing apoptosis for the human colon cancer cells.

• Natural Product Sciences
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• v.8 no.4
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• pp.170-172
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• 2002

In continuous efforts for discovery of novel potent antitumor agents from natural products, fifty-seven methanolic extracts derived from indigenous Korean plants were primarily evaluated for in vitro cytotoxic activity in cultured human lung (A549) and colon (Col2) cancer cells. As a result, 16 plant extracts were found to be active against A549 cells and 15 extracts were active against Col2 cells in the criteria of $IC_{50}$<$50\;{\mu}g/ml$. In particular, the extracts of Calystegia soldanella $(IC_{50}$<$8.0\;{\mu}g/ml\;in\;A549;IC_{50}=27.4\;{\mu}g/ml\;in\;Col2)$, Heloniopsis orientalis $(IC_{50}=4.6\;{\mu}g/ml\;in\;A549; IC_{50}=4.5\;{\mu}g/ml\;in\;Col2)$, and Thuja koraiensis $(IC_{50}=1.2\;{\mu}g/ml\;in\;A549;IC_{50}=0.6\;{\mu}g/ml\;in\;Col2)$ showed a potent cytotoxic activity. Further study for the identification of active compounds from these lead extracts might be warranted.

• Natural Product Sciences
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• v.6 no.4
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• pp.183-188
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• 2000

In order to discover novel potent antitumor agents, methanolic extracts of approximately 180 herbal medicines were prepared and primarily evaluated for cytotoxic activity in cultured human lung (A549) and colon (Col 2) cancer cells. As a result, 17 natural product extracts were found to be active in the criteria of $IC_{50}$<$20\;{\mu}g/ml$. Especially, the extracts of Aristolochia debilis, Cynanchum ascyrifolium, Cynanchum paniculatum, Daphne genkwa, Euphorbia lathyris, Ipomoea hederacea, Magnolia officinalis, Melia azedarach var. japonica, Solanum nigrum, Thuja orientalis, and Trichosanthes kirilowii showed a strong cytotoxic potential. The flower extract of Daphne genkwa was more selective cytotoxic activity against lung cancer cells $(IC_{50};\;0.2\;{\mu}g/ml)$ compared to colon cancer cells $(IC_{50}>20\;{\mu}g/ml)$. In addition, based on the cytotoxic potential of the root extract of Cynanchum paniculatum, the further fractionation of methylene chloride partition with silica gel column chromatography was performed. Several subfractions were considered to be active, and thus indicating that further studies for the identification of active principles from these fractions might be warranted.

• Archives of Pharmacal Research
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• v.24 no.5
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• pp.441-445
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• 2001

Resveratrol, a trihydroxystilbene found in grapes and several plants, has been shown to be active in inhibiting multistage carcinogenic process. Using resveratrol as the prototype, we synthesized several analogs and evaluated their growth inhibitory effect using cultured human cancer cells. In the present report we show that one of the resveratrol analogs, 3, 5,2',4'-tetramethoxy-trans-stilbene, potentiated the inhibition of cancer cell growth. Prompted by the strong growth Inhibitory activity of the compound ($IC_{50}$; $0.8{\mu}$ g/ml) compared to resveratrol ($IC_{50}$; $18{\mu}$ug/ml) in cultured human colon cancer cells (Col2), we performed an action mechanism study using the compound. The compound induced the accumulation of cellular DNA contents in the sub-CO phase DNA contents of the cell cycle by in a time-dependent manner. The morphological changes were also consistent with an apoptotic process. This result indicated that the compound induced apoptosis of cancer cells, and may be a candidate for use in the development of potential cancer chemotherapeutic or cancer chemopreventive agents.

• Korean Journal of Human Ecology
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• v.7 no.3
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• pp.49-58
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• 2004

The purpose of the study was to verify if or not as funtional food by estimating antitumor activity and antimicrobial activity of Coriolus versicolor(Fr.)Quel and Ganoderma Lucidum (Fr.)Karst. 1. The contents of moisture. crude fiber and crude protein of GL were higher $(18.28\%,\;10.3\%,\;78.4\%)$ than that of CV, but the content of crude lipid GL was higher than that of CV. 2. Inhibitory effects of on the growth of AGS human gastric adenocarcinoma cells and HT-29 human colon adenocarcinoma cell were increased by increasing of concentration in added methanol extracts of CV and GL. 3. Antimicrobial activity on Escherichia col1; Staphylococcus aureus, Salmonella typhimurium existed methanol extracts of CV. Therefore. it is suggested that CV is worth as functional food.

• Natural Product Sciences
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• v.8 no.4
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• pp.165-169
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• 2002

One-hundred and twenty plant extracts were prepared from 29 Indonesian plants and were primarily tested in vitro cytotoxicity in cultured human lung (A549), colon (Col2), and stomach (SNU-638) cancer cells. As a result, the 23 extracts were found to be active in the criteria of $ED_{50}$<$20\;{\mu}g/ml$. Remarkable cytotoxicity was observed for chloroform and n-butanol extracts of Calotropis gigantea, with $ED_{50}$ values ranging from 0.25 to $0.46\;{\mu}g/ml$. Five extracts derived from Eclipta alba and Excoecaria cochinchinensis displayed potent cell-line selective cytotoxicity, while the rest of 15 extracts showed modest cytotoxic activity against all of three cancer cells. In addition, the cytotoxic potential of subfractions of Zingiber cassumunar against a panel of human cancer cell lines is presented.