| 摘要: | 台灣馬桑 (Coriaria intermedia MATSUM) 為馬桑科 (Coriariaceae) 馬桑屬 (Coriaria LINN.) 植物。台灣民間用其葉治腹痛，根治子宮癌，在近年的研究中，發現馬桑屬植物中所含倍半?內酯 (sesquiterpene -lactones)，具有治療精神分裂症的效果，進一步研究倍半?類的結構與活性的關係發現，馬桑所含的倍半?類化合物對 GABAA 接受器具拮抗作用，且與其中的氯離子通道 (chloride channel) 有關。本實驗室對台灣馬桑進行成分及生物活性研究中，在台灣馬桑根部及葉部進行成分分離，得到七個化合物，分別為 phytosterol, ellagic acid 3,3''-dimethyl ether, coriamyrtin, b-tutin, naringenin, ursolic acid 及 20-epibryonolic acid 其中 20-epibryonolic acid 為天然物首次所分離得到，接著繼續對台灣馬桑根部及果實部位進行成分分離，分別由根部得到 corianin 及 7-hydroxycoumarin，由果實部位得到 ursolic acid, coriamyrtin, tutin, angustifolin, quercetin 及 kaempferol 八個化合物，其中 7-hydroxycoumarin 及 angustifolin 首次由馬桑屬植物中分離得到。 在臺灣馬桑成分分離中所得到的倍半?類化合物 coriamyrtin, 及 tutin，誘發鼷鼠陣發性痙攣及陣發性痙攣至強直性痙攣的時間及死亡時間。發現 coriamyrtin 在 2mg/kg 引起鼷鼠陣發性痙攣，3mg/kg 引起鼷鼠強直性痙攣並造成鼠死亡；tutin 在 3mg/kg 引起鼷鼠陣發性痙攣，5mg/kg 引起鼷鼠強直性痙攣並造成鼠死亡。以治療大發作藥物 pentobarbital 及 diazepam 來拮抗其中樞興奮作用，coriamyrtin, 及 tutin 的致痙攣作用，都可以被有效的抑制，此果可以提供臺灣馬桑中毒的治療方法。 由抗腫瘤試驗顯示臺灣馬桑中 coriamyrtin 及 tutin 對人類胃癌細胞有抑制的活性。 五味子為中醫常用藥材，其成分與藥理作用均被廣泛研究。本研究以水、50% 酒精及 95% 酒精三種不同溶媒分別抽取五味子並以高效液相層析分析，比較得知以95% 酒精抽取五味子其中 schizandrin 及 gomisin A 含量最高，50% 酒精抽取液次之，以水抽取者含量最低。由抗肝損傷藥理試驗顯示 95% 酒精抽取物亦具有較高的生物活性，水抽出物活性低，可提供五味子萃取及入藥時的參考。 此外，急性毒性試驗結果亦發現五味子水、50% 酒精及 95% 酒精三種抽取物對鼷鼠之半數致死劑量 (LD50) 分別為 1.60 g/kg, 1.75 g/kg 及 1.00 g/kg，可見五味子具有一定的毒性，使用時應注意其劑量之控制。; Coriaria intermedia MATSUM （Coriariaceae）is a folk medicine in Taiwan for the treatment of gastrointestinal and uterus cancer. It is also reported that the sesquiterpenes from Coriaria genus were used for schizophrenia in the southwest area of China. The structure-activity relationship of these sesquiterpene-lactones showed non-competitive antagonist of GABAA receptors. The site of action is thought the related to the GABA-gated chloride channel. Our previous studies resulted in the isolation of seven components from the leaves and roots of C. intermedia. Those components were identified as phytosterol, ellagic acid 3,3''-dimethyl ether, coriamyrtin. β-tutin, narigenin, ursolic acid and 20-epibryonolic acid. Further isolation and purification from roots and fruits of this plant, we obtained corianin, 7-hydroxycoumarin, ursolic acid, coriamyrtin, tutin, angustifolin, quercetin and kaempferol. Among them, 7-hydroxycoumarin and angustifolin were found from the coriaria genus for the first time. Two sesquiterpene-lactones coriamyrtin and tutin, isolated from Coriaria intermedia, produced convulsion effect in mice. Intraperitoneal administration coriamyrtin (3mg/kg) or tutin (5mg/kg) produced clonic convulsion and tonic convulsion. Intraperitoneal administration pentobarbital (30mg/kg-15mg/kg) or diazepam (2.5mg/kg-0.5mg/kg) significantly prolonged the onset of clonic convulsion and tonic convulsion which produced by coriamyrtin (3mg/kg) and tutin (5mg/kg). It showed a good therapeutic in Coriaria intermedia poisoning. The results of pharmacological experiment show that the coriamyrtin and tutin had obvious inhibition of the tumor cell, SCM-1. Schisandrae Fructus, the fruit of Schisandra chinensis (TURCZ.) BAILL. is a traditional Chinese medicine. Its constituents and pharmacological activities had been extensively studied. Schisandrae Fructus was extracted by water, 50% alcohol and 95% alcohol respectively and were quantitatively analyzed by high performance liquid chromatography (HPLC). The content of schizandrin and gomisin A in 95% alcohol extracts was highest followed by 50% alcohol extract and water extract. The 95% alcohol extracts also showed higher liver protective activity. The acute toxicity study of Schisandrae Fructus extract was evaluated in mice and the LD50 was 1.0~1.75 g/kg (95% confidence 0.67~2.43 g/kg ). Therefore ,we must be cautious with the dose of Schizandrae Fructus.
台灣馬桑 (Coriaria intermedia MATSUM) 為馬桑科 (Coriariaceae) 馬桑屬 (Coriaria LINN.) 植物。台灣民間用其葉治腹痛，根治子宮癌，在近年的研究中，發現馬桑屬植物中所含倍半?內酯 (sesquiterpene -lactones)，具有治療精神分裂症的效果，進一步研究倍半?類的結構與活性的關係發現，馬桑所含的倍半?類化合物對 GABAA 接受器具拮抗作用，且與其中的氯離子通道 (chloride channel) 有關。本實驗室對台灣馬桑進行成分及生物活性研究中，在台灣馬桑根部及葉部進行成分分離，得到七個化合物，分別為 phytosterol, ellagic acid 3,3''-dimethyl ether, coriamyrtin, b-tutin, naringenin, ursolic acid 及 20-epibryonolic acid 其中 20-epibryonolic acid 為天然物首次所分離得到，接著繼續對台灣馬桑根部及果實部位進行成分分離，分別由根部得到 corianin 及 7-hydroxycoumarin，由果實部位得到 ursolic acid, coriamyrtin, tutin, angustifolin, quercetin 及 kaempferol 八個化合物，其中 7-hydroxycoumarin 及 angustifolin 首次由馬桑屬植物中分離得到。 在臺灣馬桑成分分離中所得到的倍半?類化合物 coriamyrtin, 及 tutin，誘發鼷鼠陣發性痙攣及陣發性痙攣至強直性痙攣的時間及死亡時間。發現 coriamyrtin 在 2mg/kg 引起鼷鼠陣發性痙攣，3mg/kg 引起鼷鼠強直性痙攣並造成鼠死亡；tutin 在 3mg/kg 引起鼷鼠陣發性痙攣，5mg/kg 引起鼷鼠強直性痙攣並造成鼠死亡。以治療大發作藥物 pentobarbital 及 diazepam 來拮抗其中樞興奮作用，coriamyrtin, 及 tutin 的致痙攣作用，都可以被有效的抑制，此果可以提供臺灣馬桑中毒的治療方法。 由抗腫瘤試驗顯示臺灣馬桑中 coriamyrtin 及 tutin 對人類胃癌細胞有抑制的活性。 五味子為中醫常用藥材，其成分與藥理作用均被廣泛研究。本研究以水、50% 酒精及 95% 酒精三種不同溶媒分別抽取五味子並以高效液相層析分析，比較得知以95% 酒精抽取五味子其中 schizandrin 及 gomisin A 含量最高，50% 酒精抽取液次之，以水抽取者含量最低。由抗肝損傷藥理試驗顯示 95% 酒精抽取物亦具有較高的生物活性，水抽出物活性低，可提供五味子萃取及入藥時的參考。 此外，急性毒性試驗結果亦發現五味子水、50% 酒精及 95% 酒精三種抽取物對鼷鼠之半數致死劑量 (LD50) 分別為 1.60 g/kg, 1.75 g/kg 及 1.00 g/kg，可見五味子具有一定的毒性，使用時應注意其劑量之控制。; Coriaria intermedia MATSUM （Coriariaceae）is a folk medicine in Taiwan for the treatment of gastrointestinal and uterus cancer. It is also reported that the sesquiterpenes from Coriaria genus were used for schizophrenia in the southwest area of China. The structure-activity relationship of these sesquiterpene-lactones showed non-competitive antagonist of GABAA receptors. The site of action is thought the related to the GABA-gated chloride channel. Our previous studies resulted in the isolation of seven components from the leaves and roots of C. intermedia. Those components were identified as phytosterol, ellagic acid 3,3''-dimethyl ether, coriamyrtin. β-tutin, narigenin, ursolic acid and 20-epibryonolic acid. Further isolation and purification from roots and fruits of this plant, we obtained corianin, 7-hydroxycoumarin, ursolic acid, coriamyrtin, tutin, angustifolin, quercetin and kaempferol. Among them, 7-hydroxycoumarin and angustifolin were found from the coriaria genus for the first time. Two sesquiterpene-lactones coriamyrtin and tutin, isolated from Coriaria intermedia, produced convulsion effect in mice. Intraperitoneal administration coriamyrtin (3mg/kg) or tutin (5mg/kg) produced clonic convulsion and tonic convulsion. Intraperitoneal administration pentobarbital (30mg/kg-15mg/kg) or diazepam (2.5mg/kg-0.5mg/kg) significantly prolonged the onset of clonic convulsion and tonic convulsion which produced by coriamyrtin (3mg/kg) and tutin (5mg/kg). It showed a good therapeutic in Coriaria intermedia poisoning. The results of pharmacological experiment show that the coriamyrtin and tutin had obvious inhibition of the tumor cell, SCM-1. Schisandrae Fructus, the fruit of Schisandra chinensis (TURCZ.) BAILL. is a traditional Chinese medicine. Its constituents and pharmacological activities had been extensively studied. Schisandrae Fructus was extracted by water, 50% alcohol and 95% alcohol respectively and were quantitatively analyzed by high performance liquid chromatography (HPLC). The content of schizandrin and gomisin A in 95% alcohol extracts was highest followed by 50% alcohol extract and water extract. The 95% alcohol extracts also showed higher liver protective activity. The acute toxicity study of Schisandrae Fructus extract was evaluated in mice and the LD50 was 1.0~1.75 g/kg (95% confidence 0.67~2.43 g/kg ). Therefore ,we must be cautious with the dose of Schizandrae Fructus. |
