白木香叶中黄酮类成分结构与抗氧化功能的相关性研究

目的：研究白木香叶中黄酮类成分清除O2^·-,H2O2,·OH的能力,探讨其抗氧化活性与结构的关系。方法：对白木香叶中黄酮类成分进行分离,采用化学发光法,测定所得成分对邻苯三酚-鲁米诺-碳酸缓冲液体系产生的超氧阴离子（O2^·-）,H2O2-鲁米诺-碳酸缓冲液体系产生的过氧化氢（H2O2）,以及邻菲罗啉-Cu2＋-抗坏血酸-H2O2体系产生的羟自由基（·OH）的清除能力。结果：分得6种黄酮类成分,经鉴定分别为：洋芹素-7,4′-二甲醚（Ⅰ）、5-羟基-7,3′,4′-三甲氧基黄酮（Ⅱ）、木犀草素-7,4′-二甲醚（Ⅲ）、芫花素（Ⅳ）、木犀草素（Ⅴ）、羟基芫花素（Ⅵ）。6种黄酮类化合物具有良好的清除自由基活性。构效关系分析显示,其清除超氧阴离子（O2^·-）、过氧化氢（H2O2）、羟自由基（·OH）的活性强弱与母核上连接的酚羟基数目和位置直接相关。结论：白木香叶中的黄酮类成分具有明显的清除自由基活性,可能为白木香叶的主要抗氧化活性成分。     

《中国药典》断血流功能与主治的商榷

目的 探讨综合评价断血流临床功效.方法 2020年10月至2021年5月笔者通过查阅期刊及相关书籍,通过对断血流同属植物的功效和文献典籍记载的断血流功效对比,并对文献报道断血流药理作用及临床应用进行分析,综合评价其临床功效.结果 药典收载的断血流功能与主治不能概括其应有功效.结论 建议应将断血流的功能与主治扩展为:收敛...     

银杏黄酮的体外葡醛酸反应及其药物相互作用

目的:获得银杏黄酮体外代谢情况,预测银杏叶制剂与常用心血管类药物之间的代谢性相互作用的可能性.方法:银杏黄酮与普罗帕酮、硝苯地平、地非三唑和依普黄酮在经β-萘黄酮诱导的鼠肝微粒体中共孵育,以HPLC法测定孵育液中剩余银杏黄酮的浓度,观察共孵育药物对银杏黄酮葡醛酸结合反应的影响,并计算银杏黄酮3个苷元的酶动力学参数.结果:测得银杏黄酮槲皮素、异鼠李素和山奈酚的Vmax值分别为(60±0.21)、(48±0.02)、(34±0.02)μmol·g-1·min-1,Km值分别为(24±0.05)、(148±0.09)、(110±0.03)μmol/L;当银杏黄酮浓度一定时,共孵育药物硝苯地平、普罗帕酮、依普黄酮和地非三唑对银杏黄酮的IC50分别为54～70、69～122、85～98和210～362 μmol.测得地非三唑对银杏黄酮3种苷元的抑制常数Ki值分别为57.6、50.5和33.1 mg/L;普罗帕酮的Ki值分别为33.6、59.5和45.2 mg/L;依普黄酮的Ki值分别为13.7、24.0和15.7 mg/L.普罗帕酮的[I]/[Ki]比值为0.002～0.003.结论:在银杏黄酮的3种苷元中槲皮素的代谢能力最强;硝苯地平、依普黄酮和普罗帕酮等对槲皮素、异鼠李素和山奈酚的葡醛酸反应均有不同程度的抑制作用;根据硝苯地平的IC50值和普罗帕酮的[I]/[Ki]值,表明普罗帕酮与银杏黄酮之间的代谢性相互作用很弱,而硝苯地平与银杏黄酮合用需慎重.     

竹叶提取液抑制小鼠移植性肺癌生长的实验研究

目的 :探讨竹叶提取液对小鼠移植性 ASP- I肺癌生长的抑制作用及其机制。方法 :采用接种 ASP- I肺癌细胞的荷瘤小鼠模型 ,观察灌胃给予不同浓度竹叶提取液对小鼠肿瘤大小和胸腺 (脾 )指数的作用 ,并测定血清中超氧化歧化酶 ( SOD)、丙二醛 ( MDA)的含量。结果 :竹叶提取液能显著减少小鼠瘤体重量 ,提高胸腺和脾指数 ,减少血清 MDA含量 ,提高 SOD水平。结论 :竹叶提取液能明显抑制肿瘤生长 ,其作用机制与清除机体自由基 ,防止脂质过氧化 ,提高机体免疫功能有关。     

山香圆总黄酮对免疫功能低下小鼠免疫功能的影响

目的 探讨山香圆总黄酮（TFS）对免疫抑制小鼠免疫功能的影响。方法 在腹腔注射环磷酰胺（Cy）诱导小鼠免疫低下模型的基础上,采用碳廓清实验检测小鼠巨噬细胞的吞噬功能;分光光度法测定血清及脾细胞中溶血素水平;二硝基氟苯诱导小鼠迟发型变态反应,并用流式细胞仪检测T细胞亚群。结果 TFS（240、480mg／kg,ig）可明显提高Cy诱导免疫功能低下小鼠的吞噬指数a值和校正指数K值、增加Cy诱导免疫功能低下小鼠脾细胞和血清中溶血素水平,增强Cy诱导免疫低下小鼠的迟发性变态反应。进一步研究发现,TFS（240mg／kg,ig）可明显提高CIM＋、CD8＋细胞数,使CIM＋／CD8＋细胞比值上升。结论 TFS能明显改善Cy致免疫功能低下小鼠的免疫功能,其免疫调节作用与调节T细胞亚群有关。     

Pharmacokinetic study of six flavones in rat plasma and tissues after oral administration of 'JiangYaBiFeng' using SPE-HPLC-DAD

In this study, a high performance liquid chromatography (HPLC) coupled with diode array detection (DAD) for simultaneous determination of six flavones including baicalein, sophoricoside, rutin, baicalin, quercetin and genistein in rat plasma and tissues after oral administration of JiangYaBifeng (JYBF) tablets was developed. The investigated analytes in plasma and tissues were extracted and purified with liquid-liquid extraction and solid phase extraction (SPE). Chromatographic separation was accomplished on a DIONEX Acclaim C18 column (250 mm × 4.6 mm, 5.0 μm particle size) with a simple linear gradient elution. The calibration curves for all the flavones had good linearity in the measured range with R² higher than 0.9983. The relative errors (REs) of the intra- and inter-day accuracy at different flavones levels were all less than ±10%. The proposed method enables unambiguous identification and quantification of investigated flavones in vivo. This is the first report on determination of the major flavones in rat plasma and tissues after oral administration of JYBF tablets. The results provided a meaningful basis for evaluating the clinical application of this medicine.     

Isolation and identification of antibacterial and cytotoxic compounds from the leaves of Muntingia calabura L.

Ethnopharmacological relevance

Muntingia calabura (Elaeocarpaceae) is one of the most common roadside trees in Malaysia. Its leaves, barks, flowers and roots have been used as a folk remedy for the treatment of fever, incipient cold, liver disease, as well as an antiseptic agent in Southeast Asia. The aim of this study is to isolate and identify the antibacterial and cytotoxic compounds from the leaves of Muntingia calabura L.

Materials and methods

Antibacterial and cytotoxic activities were determined by micro-broth dilution and MTT assays, respectively. Seven fractions (F1–F7), three flavones and a chalcone were isolated from the active EtOAc extract using bioassay-guided screening. The structures of four compounds were elucidated by spectroscopic methods and compared with published data. The compounds were further tested for their antibacterial and cytotoxic activities.

Results

Three flavones and a chalcone [5,7-dihydroxy-3,8-dimethoxyflavone (1), 2′,4′-dihydroxychalcone (2), 5-hydroxy-3,7-dimethoxyflavone (3) and 3,5,7-trihydroxy-8-methoxyflavone (4)] were isolated from the active fraction F5 of EtOAc extract. Compounds 1 and 3 were isolated for the first time from Muntingia calabura L. Antibacterial activity indicates that compound 2 exhibited the most significant activity with MIC value of 50 μg/mL and 100 μg/mL against MSSA and MRSA, respectively. Cytotoxic activity indicates that compounds 2 and 3 exhibited very strong activity against HL60 with IC₅₀ values of 3.43 μg/mL and 3.34 μg/mL, respectively.

Conclusion

The antibacterial activity of the leaves of Muntingia calabura L. is ascribable to the active compound 2 while the cytotoxic activity is ascribable to the active compounds 2 and 3.     

白花蛇舌草总黄酮对鼻咽癌细胞株CNE1增殖和凋亡的影响

目的：探讨白花蛇舌草总黄酮（FOD）对鼻咽癌细胞株CNE1的增殖和凋亡的影响。方法：体外培养鼻咽癌细胞株CNE1,使用不同质量浓度的FOD作用24、48 h,分别使用CCK-8测定法检测细胞存活率,Annexin V-FITC凋亡检测试剂盒检测细胞凋亡的情况。结果：FOD对鼻咽癌细胞株CNE1具有抑制增殖作用,24 h的半数抑制量（IC50）为（27.0±2.5）mg/L,48 h的IC50为（12.1±1.3）mg/L,在一定质量浓度范围内,呈剂量-效应关系和时间-效应关系。FOD可诱导CNE1细胞凋亡,存在剂量-效应关系和时间-效应关系。结论：FOD对鼻咽癌细胞株CNE1有显著的抑制增殖作用,作用机制可能与诱导细胞凋亡有关。     

丝瓜提取物抗氧化活性的研究

目的: 分离提取丝瓜抗氧化活性成分,观察其抗氧化效应。方法: 应用溶剂萃取法及葡聚糖凝胶柱层析法分离提取丝瓜抗氧化活性物质,通过测定不同提取物的抗氧化能力,筛选出丝瓜的抗氧化活性成分。结果: 由溶剂萃取法获得丝瓜提取物Ⅱ、Ⅲ、Ⅳ、Ⅴ,其中提取物Ⅲ抑制DPPH·和OH·自由基效果显著。提取物Ⅲ经柱层析进一步分离,得到A、B、C、D、E5种组分,其中组分D、E抑制DPPH·和OH·自由基效果最显著,经鉴定提取物符合黄酮类物质特性。结论: 丝瓜具有清除自由基的作用,且主要作用物质为黄酮类物质。     

Antihypertensive effect of total flavones extracted from seed residues of Hippophae rhamnoides L. in sucrose-fed rats

The study was designed to investigate the antihypertensive effect of total flavones extracted from seed residues of Hippophae rhamnoides L. (TFH-SR) and its underlying mechanism in chronic sucrose-fed rats by evaluating its ability to regulate insulin and angiotensin || levels. Feeding of high-sucrose diet (HS: 77% of kcal from carbohydrate, 16% from protein and 6% from lipid, respectively) for 6 weeks resulted in significant rise in systolic blood pressure (SBP) by 25.60%, plasma insulin by 114.24%, triglycerides by 85.14% and activated angiotensin || contents in heart and kidney. However, TFH-SR treatment significantly suppressed the elevated hypertension, hyperinsulinemia and dyslipidemia. Furthermore, TFH-SR (especially at the dose of 150mg/kg/day) increased the circulatory blood angiotensin || level as effective as angiotensin || receptor blocker. These results indicated that TFH-SR exerted its antihypertensive effects at least in part by improving insulin sensitivity and blocking angiotensin || signal pathway. Findings of the present study suggested that TFH-SR might prove to be of potential use in the management of hyperinsulinemia in non-diabetic state with cardiovascular diseases.