黃連及其炮炙品對大鼠胃腸道的藥理作用

Gastrointestinal Effects of Various Processed Forms of Coptidis Rhizoma on the Rat

黃連是常用中藥之一，其有多種不同的炮炙方法，其中生黃連、薑黃連、萸黃連、酒黃連、炒黃連一直沿用至今。為探討炮炙的意義，本研究比較了炮炙黃連的藥理作用及化學成分。獲得如下結果：1.除酒黃連的小檗鹼及炒黃連的黃連鹼抽出率較高外，其他炮炙黃連的小檗鹼、黃連鹼及巴馬亭抽出率與生黃連約略相等。2.口服各種炮炙黃連其一半致死量皆大朴每公斤二公克。腹腔注射給藥以妙黃連的一半致死劑量最高(213mg/kg)。3.對幽門結紮大鼠，十二指腸投與各種炮炙黃連(1500mg/kg)皆具胃酸分泌抑制作用，以生黃連及萸黃連的作用較強。又提高萸黃連炮炙時吳茱萸的含量，可增強萸黃連的胃酸分泌抑制作用。4.薑黃連(125mg/kg)口服可抑制酒精胃損傷。薑黃連(250mg/kg)及萸黃連(250mg/kg)口服可抑制酸化阿斯匹林胃損傷。又提高薑黃連炮炙時生薑的比率，可增強薑黃連的胃黏膜保護作用。5.口服各種炮炙黃連(500mg/kg)，皆可使胃內殘留體積增加，以薑黃連效果較強。6.口服各種炮炙黃連(1000mg/kg)，皆可使腸道運動減慢，以生黃連作用較強。7.各種炮炙黃連(0.005~0.08mg/kg)皆能使carbachol引起收縮的胃條片鬆弛，以薑黃連的效果較強。以上結果顯示，各種炮炙黃連的化學組成及藥理作用大體類似，除了萸黃連的酸分泌抑制作用及薑黃連的胃黏膜保護作用稍強外。至於各種炮炙黃連在臨床上的意羲仍有待進一步探討。

In recognition of the fact that different ways of processing may affect the pharmacological effects of herbal drugs, the present study was initiated to compare the gastrointestinal effects of various processed forms of Coptidis Rhizoma (CR), a commonly used Chinese herbal drug, on the rat. The various processing methods employed included stir-roasting in juice of Zingiberis Rhizoma (ZCR), stir-roasting in water of Evodia Fructus (ECR), stir-roasting in wine (ACR) and simple stir-roasting (FCR). Results indicated that: (1) With the exception of higher yield of berberine by ACR, extraction efficiency of berberine, coptisine and palmatine from CR were almost equivalent by all other means. (2) LD50 values for oral administration for all processed forms of CR were greater than 2 g/kg. For intraperitional administration, FCR's LD50 at 213 mg/kg was lower than other processed forms. (3) Intraduodenal administration of all forms of processed CR (1500 mg/kg) inhibited gastric acid secretion in pylorus-ligated rats with both raw CR and ECR showing higher efficacies. In addition, the antisecretory action of ECR rose with increased proportions of Evodiae Fructus. (4) Oral administration of ZCR (125 mg/kg) inhibited the gastric lesions induced by ethanol. Both ZCR (250 mg/kg, p. o.) and FCR (250 mg/kg, p. o.) also prevented the gastric lesions induced by acidified aspirin. In additions, the gastric cytoprotection potency of ZCR rose with increased proportions of Zingiberis Rhizoma. (5) Oral administration of all processed forms of CR (500 mg/kg) increased gastric contents, with ZCR showing the best efficacy. (6) Oral administration of all forms of CR (1000 mg/kg) depressed intestinal transition with raw CR showing the best efficacy. (7) All processed forms of CR (0.005-0.08 mg/ml) concentration dependently relaxed carbachol-contracted gastric fundus strip of the rat with ZCR showing the best efficacy. These results indicated that with the exception of ECR and ZCR exhibiting greater efficacies in gastric acid secretion inhibition and gastric protection respectively, pharmacological actions and chemical composition of all processed forms were almost identical. The significance of processing of CR in clinical uses awaits further investigations.