微波法与传统法煎煮葛根芩连汤有效成分含量的比较

目的：研究微波法与传统法煎煮中药效果。方法：用微波法与传统法分别制取供试汤剂，用紫外分光光度法测定葛根芩连汤中有效成分盐酸小檗碱、总黄酮含量，以此含量及总固体量为考察指标，比较两种方法煎煮中药效果。结果：微波法与传统法煎煮效果相同（P〉0．05），但微波法与传统法相比有高效、节能、省时的优势。结论：微波煎煮法可代替传统煎煮法煎煮中药。     

Antiproliferative activity of three methoxylated flavonoids isolated from Zeyheria montana Mart. (Bignoniaceae) leaves

The present study isolated three major active flavonoids, two flavones named 4',5,7-trimethoxy-luteolin (1) and 6-hydroxy-5,7-dimethoxyflavone (2) and the flavanone 5-hydroxy-6,7-dimethoxyflavanone (3) from Zeyheria montana dichloromethane leaf extract. Isolation and purification were conducted with the application of column chromatography and structures were assigned by spectral analysis. All compounds were evaluated for cytotoxic activities against human tumor cell lines UACC-62 (melanoma), MCF-7 (breast), NCI-ADR/RES (breast expressing phenotype multiple drug resistance), 786-0 (renal), NCI-H460 (lung, non-small cells), PC-3 (prostate), OVCAR-3 (ovarian), HT-29 (colon) and K562 (leukemia) in vitro. All compounds were active in different degrees on several tumor cell lines and flavanone 3 showed cytotoxicity against almost all cell lines, particularly against human NCI-ADR/RES and K562 cell lines. In conclusion, three antiproliferative compounds were isolated for the first time from Zeyheria montana and its leaves were characterized as an important source of methoxylated flavones and flavanone as potential antitumor compounds.     

东方荚果蕨的化学成分研究

目的 研究东方荚果蕨Matteuccia orientalis干燥根茎60%乙醇提取物的化学成分。方法 采用大孔树脂Diaion HP-20柱色谱、反相ODS柱色谱、Sephadex LH-20柱色谱、高效液相色谱等多种色谱学方法对东方荚果蕨干燥根茎60%乙醇提取物中的化学成分进行分离,利用光谱学方法鉴定化合物的结构。结果 从该植物中分离得到11个化合物,分别鉴定为(±)-thunberginol C（1）,(2S)-5, 7, 3', 5'-四羟基-二氢黄酮（2）,柚皮素（3）,strobopinin（4）,杜鹃素（5）,leptorumol（6）,顺-3, 5-二羟基二苯乙烯（7）,dihydropinosylvin（8）,丹皮酚（9）,3, 4-dihydroxy-benzalacetone（10）,咖啡酸甲酯（11）。结论 化合物1～11均为首次从该属植物中分离得到。     

Association between dietary flavonoids intake and obesity in a cohort of adults living in the Mediterranean area

Abstract

Dietary polyphenols, including flavonoids, are abundantly present in a healthy and balanced diet. Evidence for their role in preventing non-communicable diseases is emerging. We examined the association between estimated habitual intake of dietary flavonoid and obesity in a cohort study. After adjusting for potential confounding factors, inverse association between total flavonoid intake and excess weight (BMI?≥25) was found (OR?=?0.66, 95% CI: 0.45, 0.99); among individual classes of flavonoids, only flavanones were inversely associated with excess body weight (OR?=?0.68, 95% CI: 0.48, 0.97). However, when considering adjustment for dietary factors (adherence to the Mediterranean diet), the associations were no more significant. When considering obesity as the outcome (BMI?≥30), individuals with high intake of total flavonoids and flavonols resulted less likely to be obese (OR?=?0.38, 95% CI: 0.21, 0.66 and OR?=?0.63, 95% CI: 0.39, 0.99, respectively), even after adjustment for confounding factors. The results of the present study add to the current literature further evidence of the association between higher flavonoid intake and decreased body weight. Further studies are needed to confirm retrieved association.     

Evaluation of First‐Pass Cytochrome P4503A (CYP3A) and P‐glycoprotein Activities Using Felodipine and Hesperetin in Combination in Wistar Rats and Everted Rat Gut Sacs in Vitro

The effects of hesperetin on the pharmacokinetics and the role of P‐glycoprotein (P‐gp) in the transport of felodipine were investigated in rats and in vitro. Felodipine was administered orally (10 mg/kg) without or with hesperetin (25, 50 and 100 mg/kg) to rats for 15 consecutive days. Blood samples were collected at different time intervals on 1^st day in single dose pharmacokinetic study (SDS) and on 15^th day in multiple dose pharmacokinetic study (MDS). The area under the plasma concentration–time curve (AUC_0–∞) and the peak plasma concentration (C_max) of felodipine were dose‐dependently increased in SDS and MDS with hesperetin compared to control ( p < 0.001). The half‐life (t_1/2) and mean residence time was longer than the control group in both studies. The role of P‐gp determined using everted rat gut sacs in vitro by incubating felodipine with or without hesperetin and verapamil (typical P‐gp and CYP3A4 inhibitor). The in vitro experiments revealed that the verapamil and hesperetin increased the intestinal absorption of felodipine (p < 0.01). Concurrent use of hesperetin dramatically altered the pharmacokinetics of felodipine leading to an increase in systemic exposure. The likely mechanism is inhibition of CYP3A4‐mediated first‐pass metabolism and P‐gp in the intestine and the liver. Copyright © 2013 John Wiley & Sons, Ltd.     

垂盆草总黄酮影响肝星状细胞凋亡的作用机制研究

目的:研究垂盆草总黄酮(SSTF)对大鼠肝星状细胞(HSC-T6)凋亡的影响及其作用机制。方法:将不同质量浓度的SSTF与HSC-T6细胞共培养不同时间后,MTT法检测SSTF对HSC-T6细胞的增殖抑制作用;流式细胞仪Annexin-V/PI双染方法检测SSTF对HSC-T6细胞凋亡的影响;应用Western blotting和Real-time PCR方法观察药物对凋亡相关细胞因子Bcl-2,Bax和Caspase-3蛋白及mRNA表达的影响。结果:SSTF能显著抑制HSC-T6细胞增殖、诱导细胞凋亡,且呈剂量和时间依赖;Western blotting结果显示,SSTF通过抑制Bcl-2,促进Bax和Caspase-3蛋白表达促进细胞凋亡;进一步采用Real-time PCR研究发现,Bcl-2能够从mRNA水平抑制Bcl-2、促进Bax和Caspase-3表达。结论:SSTF具有促进HSC-T6凋亡的作用,这种作用的发挥主要是通过抑制Bcl-2、促进Bax和Caspase-3蛋白和mRNA的表达实现的。     

艾纳香二氢黄酮对脂质过氧化及活性氧自由基的作用

目的研究5种艾纳香二氢黄酮化合物的抑制脂质过氧化及其对超氧阴离子自由基（O）、羟自由基（·OH）的清除作用。方法：不同浓度的艾纳香二氢黄酮化合物与大鼠组织匀浆或自由基发生系统共治后，比色法测定丙二醛、、·OH生成量。结果：10(－5)～10(－4)mol·L(-1)浓度下，5种艾纳香二氢黄酮类化合物，能够抑制大鼠组织匀浆自氧化及FeSO4／半胱氨酸激发的脂质过氧化，10(－6)～10(－5)mol·L(-1)浓度下能够清除黄嘌呤／黄嘌呤氧化酶系统产生的O，以及抗坏血酸／硫酸铜自由基系统产生的·OH。结论：艾纳香二氢黄酮具有较强的抗氧化作用。     

Effects of chalcones isolated from licorice roots on leukotriene biosynthesis in human polymorphonuclear neutrophls

The effects of chalcones and flavanones isolated from Sinkiang Licorice (Glycyrrhiza inflata Bat.) on leukotriene B₄(LTB₄) and C₄(LTC₄) formation in human polymorphonuclear neutrophils (PMNs) were investigated. Licochalcone A (2-methoxy-4,4′-dihydroxy-5-α,α-dimethyl-allylchalcone) and licochalcone B (2-methoxy-3,4,4′-trihydroxychalcone), at concentrations of 10^?3 to 10^?6 M, inhibited calcium ionophore A 23187 (A 23187)-induced LTB₄ and LTC₄ formation in human PMNs. The concentration of licochalcones A required for 50% inhibition (LC₅₀) of LTB₄ and LTC₄ formation was 4.6 × 10^?7 and 4.2×10^?6 M, respectively, using 2 μM A 23187. The IC₅₀ values of licochalcone B for LTB₄ and LTC₄ formation were also 1.2 × 10^?6 and 2.0×10^?6 M, respectively. In addition, licochalcones A and B significantly increased cyclic AMP level in human PMNs at concentrations of 10^?4 to 10^?3 M. Licochalcones A and B were found to reduce the elevation of the cytosolic free calcium concentration induced by calcium ionomycine, dose-dependently, in the presence of 1 mM Ca²⁺ or 1 mM EGTA.     

Flavonoids, vitamin C and adenocarcinoma of the stomach

OBJECTIVE: To examine the role of six flavonoid classes (flavanones, flavan-3-ols, flavonols, flavones, anthocyanidins and isoflavones) and vitamin C in the aetiology of stomach cancer. METHODS: Case-control study undertaken in Greece in the 1980s. Dietary information was obtained from 110 patients with incident stomach adenocarcinoma and 100 control patients. Flavonoid estimates were based on the recently released database of the US Department of Agriculture. RESULTS: In models including sociodemographic variables, energy intake, vegetables, fruits and, alternatively, vitamin C the six flavonoid classes, only flavanones and vegetables remained significantly inversely associated with stomach cancer risk. The odds ratio (95% confidence intervals) per one standard deviation increase of intake of flavanones was 0.55 (0.31-0.96) whereas for vitamin C it was 1.05 (0.46-2.41). When fruits and vegetables were not adjusted for, both vitamin C and several flavonoid categories were inversely associated with stomach cancer risk, but these associations could be attributed to other compounds in these foods. CONCLUSIONS: Among the major flavonoid classes studied, only flavanone intake is inversely associated with stomach cancer risk and could account for the apparent protective effect of fruit intake against this form of cancer. Additional factors, however, are likely to be involved in the consistent protection conveyed by vegetables.     

竹叶中总黄酮的提取及鉴别

目的为充分利用竹叶植物资源,避免资源的浪费,探讨竹叶总黄酮的提取及鉴别方法。方法采用纯物理的工艺流程过程和分光光度法从竹叶中提取黄酮类物质,对所提取的黄酮类物质进行验证。结果通过上述的方法测得样品中总黄酮的含量C=1.56%。回收率为99.4%,其纯度和产率均较高。结论该方法采用全物理过程,无任何化学变化及污染,是提取竹叶黄酮类物质的有效途径。