Polygonum multiflorum Thunb. is a commonly used for traditional Chinese medicine. It is prepared from the dried root tuber of Polygonum multiflorum Thunb. It is recorded as Radix Polygoni Multiflori and Radix Polygoni Multiflori Praeparata cum Succo Glycines Sotae in Pharmacopoeia of the People's Republic of China (2010). Polygonum multiflorum Radix is used to counteract toxicity, cure carbuncles, and relax bowels, while Radix Polygoni Multiflori Praeparata cum Succo Glycines Sotae is used to replenish the liver and the kidney with vital essence and blood, blacken hair, and strengthen the tendons and bones. Nevertheless, growing evidents show that Radix Polygoni Multiflori can induce liver toxicity recently. For providing theoretical basis of using Radix Polygoni Multiflori scientifically and reasonably, this study will analyze the different components of the Radix Polygoni Multiflori and investigate their hypatoxic effects by using HPLC, cell materials biospecific extraction and pharmacological analysis. First, Radix Polygoni Multiflori was extracted by water ultrasonic, water reflux and ethanol ultrasonic methods, and we found that the parts of high and medium polarity compounds are similar, while the parts of low polarity compounds are different. Second, the hypatoxic effects of those compounds were evaluated. The result showed that the extracts from water ultrasonic and water reflux don’t have hepatotoxicity, but the ethanol ultrasonic extract has remarkable hepatotoxicity. So it can be speculated that the low polarity compounds exhibt the hepatotoxic effects. Next, the specific binding compounds were colleted and analyzed by using cell materials biospecific extraction and chemical analysis, respectively. We found that these compounds are including cis-2,3,5,4′-tetrahydroxystilbene-2-O-β-Dglucopyranoside, 2,3,5,4′-tetrahydroxystilbene-2,3-di-O-β-D-glucopyranoside (polygonimitin C), trans-2,3,5,4′-tetrahydroxystilbene-2-O-β-D-glucopyranoside, emodin-8-O-β-Dglucopyranoside, physcion-8-O-β-D-glucopyranoside, emodin and physcion. Finally, we confirmed that emodin causes strongly hypatoxic effect. Furthermore, emodin-8-O-β-Dglucopyranoside, physcion-8-O-β-D-glucopyranoside and physcion also exhibit the hypatoxic effects. This study analyzed the conponets of Radix Polygoni Multiflori which cause hypatoxic effect by using chemical and pharmacology method, providing theoretical basis of using Radix Polygoni Multiflori scientifically and quality control. Key words: Radix Polygoni Multiflori; emodin; liver toxicity; cell materials biospecific extraction, comparative chemistry, comparative pharmacology

何首烏為蓼科植物何首烏（Polygonum multiflorum Thunb.）的乾燥塊根，是一種 珍貴的常用中藥材，2010 版《中華人民共和國藥典》分別收載了何首烏和制何首烏。 何首烏有解毒，消癰，截虐，潤腸通便的功效，制何首烏則有補肝腎，益精血，烏 須發，強筋骨，化濁降脂的功效。但是近年來關於何首烏製劑造成肝毒性的報導日 益增多，所以本實驗採用不同何首烏提取物的成分比較和肝毒性比較的方法並結合 細胞固相萃取的方法對何首烏中造成肝毒性的成分進行確定。首先使用水超聲、水 冷凝回流及乙醇超聲提取的方法對何首烏進行提取，對提取物的化學成分進行分析， 發現三種提取物的大極性和中極性成分相似，而小極性成分差異較大；然後對三種 提取物肝毒性強弱進行測定，確定何首烏水超聲提取物和水冷凝回流提取物沒有肝 毒性，而何首烏乙醇超聲提取物則有較強的肝毒性，故推測何首烏造成肝毒性的成 分可能是何首烏乙醇超聲提取物中的小極性成分；接著使用肝細胞固相萃取技術結 合 HPLC 分析的方法對何首烏乙醇超聲提取物進行分析，並對和肝細胞結合的成分 的化學結構進行確定，確定這些與肝細胞結合成分為 2,3,5,4′-四羥基順式二苯乙烯 -2-O-β-D-吡喃葡萄糖苷、2,3,5,4′-四羥基反式二苯乙烯-2,3-二-O-β-D-吡喃葡萄糖苷 （何首烏丙素）、2,3,5,4′-四羥基反式二苯乙烯-2-O-β-D-吡喃葡萄糖苷、大黃素 -8-O-β-D-吡喃葡萄糖苷、大黃素甲醚-8-O-β-D-吡喃葡萄糖苷、大黃素、大黃素甲醚； 最後對以上7種化合物進行藥理實驗測定，確定大黃素是造成肝毒性的最主要成分， 而大黃素-8-O-β-D-吡喃葡萄糖苷、大黃素甲醚-8-O-β-D-吡喃葡萄糖苷及大黃素甲醚 亦有部分肝毒性，但其毒性沒有大黃素顯著。這亦證明瞭推測的正確性。本研究使 用比較化學和比較藥理相結合的方法對何首烏中造成肝毒性的成分進行闡述，為何 首烏的科學合理用藥和品質控制提供理論依據，為今後中藥活性分析提供了參考。 關鍵字：何首烏；大黃素；肝毒性；細胞固相萃取法；比較化學；比較藥理學