紫荆属植物紫荆地上部分的化学成分及生物活性研究

紫荆Cercis chinens &Bunge，又名满条红，为豆科(Leguminosae)紫荆属(Cercis)植物，产于我国东南部大部分省区。分布于黄河流域以南各地。树皮和木材可入药，具有活血行气，清热解毒，消肿止痛等功效。紫荆花可用于治疗风湿骨痛、鼻中疳疮；紫荆果可以治疗咳嗽。紫荆属植物化学成分以黄酮类成分为主，生物活性主要是抗炎、抗氧化。日本大正制药公司对紫荆95％乙醇提取物进行筛选后，发现提取物浓度为0.5μg/ml时，对肝细胞生长因子(HGF)的酪氨酸激酶(Tyrosine kinase)受体抑制率为103％；对前列腺素E合成酶(mPGES)的抑制率为92％。为了更好地开发利用该药用植物资源，我们对紫荆属植物紫荆的化学成分和生物活性展开研究。紫荆地上部分经95％乙醇回流提取，硅胶拌样，干燥后将硅胶装入索氏提取器中，分别用石油醚、氯仿、醋酸乙酯、丙酮、95％乙醇和甲醇回流提取，得到6个洗脱部分。 　　本文对氯仿、醋酸乙酯和丙酮部分进行了系统的化学成分研究，从中分离并鉴定了24个化合物，并通过1D、2D NMR，IR，UV，MS及化学方法鉴定了它们的结构。包括5个二苯并氧杂卓类成分：6-methoxy-7-methyl-8-hydroxydibenz 　　药理筛选结果：对整体动物实验结果显示，在给巴豆油耳部炎症小鼠皮下注射相应受试物后，紫荆氯仿和甲醇粗提部分有明显的抗炎作用(给药量50 mg/kg时，抑制率分别为30.58％，46.36％)。紫荆95％乙醇提取物以及氯仿、丙酮和乙醇洗脱部分对D-GalN引起的肝细胞损伤有保护作用(给药量50 μg/ml时，有效率分别为35％，41％，41％和38％)。化合物4、6、10和11对D-GalN引起的肝细胞损伤有明显的保护作用(浓度为1×10<'-4>M时，有效率分别为37％，38％，67％和31％)。化合物13对贫血症中的PHD2有明显的抑制作用(抑制率为79.3％)。

Cercis chinensis Bunge, also known as Mantiaohong, is a plant of the genus Cercis in the family Leguminosae, native to most provinces in southeastern China and distributed in areas south of the Yellow River. Its bark and wood can be used as medicines, with effects including promoting blood circulation and regulating qi, clearing heat and detoxifying, reducing swelling and relieving pain. The flowers of Cercis chinensis are used to treat rheumatic arthralgia and nasal aphthous ulcers, while its fruits can alleviate cough. The chemical constituents of Cercis plants are mainly flavonoids, and their main biological activities are anti-inflammatory and antioxidant effects. Taisho Pharmaceutical Co., Ltd. screened the 95% ethanol extract of Cercis chinensis, and found that when the extract concentration was 0.5 μg/ml, the inhibition rate against the tyrosine kinase receptor of hepatocyte growth factor (HGF) was 103%, and the inhibition rate against microsomal prostaglandin E synthase (mPGES) was 92%.

To better develop and utilize this medicinal plant resource, we conducted research on the chemical constituents and biological activities of Cercis chinensis. The aerial parts of Cercis chinensis were extracted via reflux with 95% ethanol, mixed with silica gel, dried, and then loaded into a Soxhlet extractor. Reflux extractions were performed sequentially with petroleum ether, chloroform, ethyl acetate, acetone, 95% ethanol and methanol, yielding six elution fractions.

This study systematically investigated the chemical constituents of the chloroform, ethyl acetate and acetone fractions, from which 24 compounds were isolated and identified. Their structures were elucidated via 1D and 2D NMR, IR, UV, MS and chemical methods, including 5 dibenzoxepin components: 6-methoxy-7-methyl-8-hydroxydibenz

Pharmacological screening results: Whole animal experiments showed that after subcutaneous administration of the corresponding test substances to croton oil-induced ear inflammation mice, the crude chloroform and methanol fractions of Cercis chinensis exhibited significant anti-inflammatory effects, with inhibition rates of 30.58% and 46.36% respectively at a dosage of 50 mg/kg. The 95% ethanol extract, as well as the chloroform, acetone and ethanol elution fractions, showed protective effects against D-galactosamine (D-GalN)-induced hepatocyte injury, with effective rates of 35%, 41%, 41% and 38% respectively at a concentration of 50 μg/ml. Compounds 4, 6, 10 and 11 also exhibited significant protective effects against D-GalN-induced hepatocyte injury, with effective rates of 37%, 38%, 67% and 31% respectively at a concentration of 1 × 10^-4 M. Compound 13 showed significant inhibitory activity against PHD2 in anemia, with an inhibition rate of 79.3%.

搜集汇总

背景与挑战

背景概述

该数据集聚焦于紫荆属植物紫荆地上部分的化学成分研究，分离鉴定了24个化合物，并发现其具有显著的抗炎和肝细胞保护活性。研究结果为该药用植物的开发利用提供了科学依据。