萱草根的研究 Ⅲ.治疗血吸虫病有效成分的初步分离和鉴定

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百合科萱草属萱草根(Hemerocallis thunbergii Baker),系一种治疗血吸虫病的中药。經过氯仿提取,通过氧化鋁色层分离,能获得一种黄色粉末(萱草根成分Ⅰ),在243℃时变棕色,266—269℃时熔融(分解)。經用小白鼠測毒試驗,LD_(50)为0.95毫克/20克,同时出現疗效。用甲酰二甲胺重結晶,得橘紅色結晶(萱草根成分Ⅱ),在240℃时变棕色,268—269℃时熔融(分解),毒性与疗效却大大降低,但当剂量增大时,毒性与疗效又同时出現。继以碱液溶解結晶,加酸酸化,又得黄色粉末(萱草根成分Ⅲ),在240℃时变棕色,268—269℃时熔融(分解),LD_(50)为0.34毫克/20克。萱草根成分Ⅰ,Ⅱ,Ⅲ虽然毒性大小有差別,但是,在化学上均为弱酸性物貭,它們的溶解情况、显色反应和熔点等都相同;而且,相互間的混合熔点也不降低;在紅外綫吸收光譜上,所呈現的吸收峯也相一致;紙上层析試驗,在三种不同的溶解系統中,均得相似的一个斑点;它們在相同条件下进行乙酰化,分別获得熔点为240—241℃的白色板状結晶,相互間的混合熔点也不降低,紅外綫吸收光譜也相一致。根据上述結果,从化学上看来,萱草根成分Ⅰ,Ⅱ,Ⅲ可能是同一种物貭,这种物貭系治疗血吸虫病的有效成分。經药理試驗証明,成分Ⅰ,Ⅱ,Ⅲ的药理作用尚有程度上的不同,这种現象可能与化学結构有关,尚待更多实驗闡明。这个化合物暫定名为萱草根素(hemerocallin),分子式为C_(16)H_(14)O_4。 Hemerocallis thunbergii Baker is a traditional Chinese medicine for the treatment of schistosomiasis. After chloroform extraction, through a layer of aluminum oxide separation, a yellow powder (Compositae root component I) was obtained, which turned brown at 243°C and melted (decomposed) at 266-269°C. After the mice were tested for toxicity, LD_(50) was 0.95 mg/20 g, and the curative effect was observed. Recrystallization from formamide dimethylamine gives orange-red crystals (grassroot component II) that turns brown at 240°C and melts (decomposes) at 268-269°C. The toxicity and efficacy are greatly reduced, but as the dose increases , Toxicity and efficacy appear at the same time. Subsequent to lye dissolution, crystallization, acidification and acidification, the yellow powder (Hemachrum root component III) was obtained. It turned brown at 240°C and melted (decomposed) at 268-269°C. LD_(50) was 0.34 mg/20 g. Although there are differences in the toxicity of the valerian root components I, II, and III, they are chemically weakly acidic, and their dissolution, color reaction, and melting point are the same, and the melting point of the mixture does not decrease. In the infrared absorption spectrum, the absorption peaks presented are also consistent; in the paper chromatography test, similar spots are obtained in three different dissolution systems; they are acetylated under the same conditions and the melting points are obtained respectively. 240-241°C white plate crystals, the melting point of their mixing does not decrease, and the infrared absorption spectrum is also consistent. Based on the above results, chemically, the root component I, II, and III of valerian root may be the same substance, which is an effective component of schistosomiasis treatment. The pharmacological tests have shown that the pharmacological effects of the components I, II, and III are still different. This phenomenon may be related to the chemical structure, and it needs further experiments to clarify. This compound is tentatively named hemerocallin and its molecular formula is C_(16)H_(14)O_4.
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