菊苣提取物中的酚类化合物及其护肝活性

Q3 Pharmacology, Toxicology and Pharmaceutics Drug Development and Registration Pub Date : 2021-11-25 DOI:10.33380/2305-2066-2021-10-4-36-45
O. L. Saybel, A. I. Radimich, T. Dargaeva, I. Lupanova, E. V. Ferubko, E. N. Kurmanova, I. A. Martynchik
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引用次数: 4

摘要

介绍。菊苣(chichorium intybus L.)是各国传统医学中广泛应用于肝病治疗的植物;同时也是保肝药理研究的对象。在这方面,全俄药用和芳香植物研究所开发了野生菊苣草本植物(WCHE)干提取物的提取方法。研究的目的是确定酚类化合物的定性组成,鉴定WCHE中普遍存在的物质,并对提取物进行药理筛选。材料和方法。采用HPLC-MS/MS法对其化学成分进行了分析;主要成分采用HPLC-UF法进行定量分析,采用我们早前分离得到的单体化合物,经核磁共振谱鉴定。采用50只雄性大鼠进行WCHE保肝活性药理筛选研究。以每100克体重0.4 ml的剂量皮下注射50%的四氯甲烷(TCM)油溶液,引起动物急性中毒性肝炎。给药前1小时,给药剂量分别为100或500 mg/kg。给药48 h后测定血清谷丙转氨酶(ALT)、天冬氨酸转氨酶(AST)、碱性磷酸酶(ALP)活性及总胆红素含量,初步建立药理活性。采用组织学方法对大鼠肝脏进行病理形态学研究。用苏木精和伊红染色的肝脏切片检查肝脏组织结构。结果和讨论。其主要成分为氧化香豆素、羟基肉桂酸和黄酮类化合物。主要的酚类化合物有槲皮素、菊苣素、菊苣酸、绿原酸和果酸。在急性实验性中毒性肝炎中,初步给药可降低中药对肝细胞的毒性作用。在100 mg/kg和500 mg/kg体重剂量的动物中,观察到ALT活性降低35%和45%,AST降低15%和28%,碱性磷酸酶降低15%和21%;总胆红素含量分别比未使用提取物的动物组的类似指标降低了20%和29%。组织学研究表明,100和500 mg/kg剂量的WCHE可减轻动物肝细胞的营养不良变化,其中500 mg/kg剂量的效果更明显。主要成分为氧化香豆素(橙皮素、菊苣素)、羟基肉桂酸(菊苣酸、绿原酸和肉桂酸)。根据筛选研究结果,确定100 mg/kg和500 mg/kg剂量的WCHE是进一步药理研究的有希望的对象。
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Phenolic Compounds and Hepatoprotective Activity of Chicory Herb Extract
Introduction. Chicory (Cichorium intybus L.) is widely applied for liver disease treatment by traditional medicine of different countries; as well, it is the object for pharmacological research of hepatoprotective activity. In this regard, the method for obtaining dry extract of wild chicory herb (WCHE) is developed in the All-Russian Research Institute of Medicinal and Aromatic Plants.Aim. Aim of the research is determination of the qualitative composition of phenolic compounds, identification of the substances prevailing in WCHE and conducting pharmacological screening of the extract.Materials and methods. WCHE chemical composition has been explored with HPLC-MS/MS method; the main components were determined quantitatively with HPLC-UF method using single compounds that were isolated by us earlier and identified by NMR spectroscopy. WCHE pharmacological screening of hepatoprotective activity research was involving 50 male rats. Acute toxic hepatitis in animals was induced by a single subcutaneous injection of 50 % oily solution of tetrachloromethane (TCM) at a dosage of 0.4 ml per 100 g body weight. One hour before administration TCM, animals received WCHE at the doses of 100 or 500 mg/kg. 48 hours after TCM administration, the activity of serum enzymes alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), as well as the content of total bilirubin were determined for preliminary establishment of pharmacological activity. Pathomorphological studies of rat liver were carried out using histological methods. The liver histological structure was inspected using liver sections stained with hematoxylin and eosin.Results and discussion. The component composition of WCHE is represented by oxycoumarins, hydroxycinnamic acids and flavonoids. The dominant phenolic compounds are esculetin, chicoriin, chicoric, chlorogenic and caftaric acids. It was found under acute experimental toxic hepatitis, that preliminary WCHE administration reduces the toxic TCM effect on liver cells. In animals treated with WCHE at doses both 100 mg/kg and 500 mg/kg body weight, it was observed decreases in ALT activity by 35 % and 45 %, AST by 15 % and 28 %, alkaline phosphatase by 15 % and 21 %; the content of total bilirubin by 20 % and 29 %, respectively, in comparison with similar indicators in the group of animals that were not treated with the extract. The histological study showed that WCHE administration to animals at the doses of 100 and 500 mg/kg reduces dystrophic changes in hepatocytes, this effect is more pronounced at the extract dosage of 500 mg/kg.Conclusion. Main WCHE components are oxycoumarins (esculetin, chicoriin), hydroxycinnamic acids (chicoric, chlorogenic and caftaric). According to the results of screening studies, it was established that WCHE in doses of 100 mg/kg and 500 mg/kg is a promising object for further pharmacological research.
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来源期刊
Drug Development and Registration
Drug Development and Registration Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
1.20
自引率
0.00%
发文量
61
审稿时长
8 weeks
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