全球每年約有 65.5 萬人死於結直腸癌。流行病學研究顯示,飲食中攝取含有大量類黃酮物質的水果與蔬菜,可能有助於預防人類結直腸癌的發生。根據研究,海巴戟天葉乙醇萃取物(LES)及其分劃物(F I-V)、香蓼嫩枝甲醇 (PoM) 或水(PoW)萃取物,除了富含高多酚類化合物之外,更擁有良好抗氧化活性。因此,本研究進一步探討LES、F I-V、PoM 及 PoW 對結直腸癌細胞(HT-29) 的抗癌活性,是否可藉由活化caspase-3,以及調節細胞核轉錄因子NF-kappa B 或 AP-1 的表現而達成。研究結果顯示 LES、F I、F III (Rutin) PoM 及 PoW 皆可抑制 HT-29的細胞增生,以及增加與凋亡機制相關的蛋白質 AP-1 及 caspase-3 的表現。此外,F I 在細胞存活率及基因毒性試驗中,誘導 HT-29 細胞凋亡及細胞週期之影響的結果與 LES 結果類似;然而,PoW 在抑制HT-29 細胞的增生、NF-kappa B 的表現以及 caspase-3 的活化較優於 PoM 。因此,F I 與 PoW 可為抗癌活性的重要來源,值得進一步純化與鑑定其生物活性成分,並深入探討其抗癌機制。此外,清楚了解 F I 與 PoW 的生物活性機制,有助於發展成為保健食品或治療藥物。 With 655,000 deaths in worldwide is due to colorectal carcinoma per year. Epidemiological studies suggest that ingesting a lot of dietary flavonoids with fruits and vegetables may prevent the incidene of colorectal carcinoma in humans. Based on our researches, ethanolic extracts from Morinda citrifolia leaf (LES), methanolic (PoM) or aqueous (PoW) extracts from Polygonum odoratum young shoots (Po) exhibited higher polyphenolic contents and revealed that these compounds played a part in antioxidative activities. LES, sub-fractions from LES (F I-V), PoM and PoW were used to study anti-cancer activity by acting through caspase-3 and modulating the expressions of NF-kappa B or AP-1 in colorectal carcinoma cells (HT-29), respectively. Results suggested that LES, F I, F III (rutin), PoM and PoW inhibited the proliferation of HT-29 and was associated with an apoptotic mechanism involving increasing in AP-1 expression and caspase-3 activation. Moreover, effects of F I on cell viability, genotoxicity, induction of apoptosis and cell cycle arrest were all similar to those of LES in HT-29. However, inhibition of HT-29 proliferation, and NF-kappa B expression as well as caspase-3 activation of PoW were better than PoM. Therefore, F I and PoW should be significant sources of anti-cancer activity. It was worth further research in purification and identification of active compounds, and deeply investigation for anti-cancer effects. Moreover, a clear understanding of the molecular mechanisms of action of F I and PoW are crucial in the valuation of these potent molecules as potential prophylactic and therapeutic agents.