红花化学成分的研究

目的：为进一步揭示红花Carthamus tinctorius L.药理活性的化学物质基础,开发其活性成分,我们对其进行了较为深入系统的化学成分研究。方法;经大孔树脂,硅胶和Sephadex LH-20反复柱层分得并通过波波谱分析鉴定了12个化合物。结果：它们分别为2,3,4,9－tetrahydro-1-methyl-1-H-pyrido[3,4-b]indole-3-carboxylicacid(Ⅰ）;thymine-2-desoxyribofuranoside(Ⅱ）;ethyl-α-D-lyxofuranoside(Ⅲ）;kaempferol-3-O-rutinoside(Ⅳ）;syringin(Ⅴ）;quercetin-3-O-β-D-galactoside(Ⅵ）;safflor yellow-A(Ⅶ）;carthamin(Ⅷ）和阿魏酸,对羟基玻酸,胡萝卜苷,β－谷甾醇。结论：化合物Ⅰ,Ⅱ和Ⅲ为首次从该植物中分得。化合物Ⅶ对ADP诱导的大鼠血小板聚集有较好的抑制活性。     

红花水煎剂对家兔离体主动脉血管的舒张作用

目的　观察红花Carthamustinctorius (DFCT)水煎剂对血管肌条的舒张作用及机制。方法　将家兔离体主动脉肌条放置于灌流肌槽中 ,记录其等长收缩。结果　DFCT对血管肌条静息张力无明显影响 ,但 2 0mg/mLDFCT水煎剂与 10 -5mol/L乙酰胆碱相似 ,可使 10 -6mol/L去甲肾上腺素预收缩血管肌条产生明显的舒张作用。去除内皮细胞、10 -4mol/LL NNA或 10 -5mol/L甲烯蓝可减弱DFCT的舒张血管作用 ,但前列腺素合成抑制剂和 β肾上腺素能受体阻断无明显影响。另外 ,4 0mg/mLDFCT水煎剂可明显抑制去内皮血管肌条去甲肾上腺和KCl的量效收缩反应 ,使其PD2 值分别由对照组 6 0 6± 0 0 9和 1 71± 0 33变为 5 0 7± 0 0 8和 1 35± 0 2 0。结论DFCT水煎剂可通过受体操纵Ca2 + 通道和电压依赖性Ca2 + 通道抑制外Ca2 + 内流 ,使血管肌条舒张 ,其作用与内皮释放的NO有关。     

红花对大鼠心脏功能的影响

红花５０、５００、２００ｍｇ生药／ｋｇｉｖ，均能使大鼠心率显著减慢（ｐ＜０．０５），左室内压（ＬＶＰ）、左室内压最大变化速率（±ｄｐ／ｄｔｍａｘ）、等容收缩和零负荷情况下心肌收缩成分缩短速度（ｄｐ／ｄｔ／ＣＰＩＰ、Ｖｍａｘ）呈现不同程度的抑制效应。红花５０、２５０ｍｇ生药／Ｌ灌流大鼠离体心脏能使冠脉流量（ＣＦ）明显增加（ｐ＜０．０５），结果提示红花有益于心脏缺血疾病的防治。     

HPLC法测定红花微乳中羟基红花黄色素A的含量

目的:建立HPLC法测定红花微乳中羟基红花黄色素A的含量。方法:采用色谱柱:Diamonsil C18(2)5μm,250mm×4.6mm;流动相:甲醇-0.4%的磷酸水溶液(三乙胺调至pH=3.3)为30∶70;检测波长:402nm;柱温:室温。结果:羟基红花黄色素A在0.3128～3.128μg的范围内呈良好的线性关系(r=0.9990)。结论:本测定方法快捷,简便,准确,重现性好。     

复方红花微乳组方配比关系研究

目的:确定复方红花微乳中2种成分的最佳配比用量。方法:采用均匀设计法,以镇痛抑制率和出血时间延长率为药效学指标,运用统计学软件处理数据和药效分析相结合筛选组方。结果:联合使用红花提取物剂量20mg/20g和利多卡因剂量2.0mg/20g能明显减少冰醋酸所致小鼠扭体反应次数,延长小鼠全血出血时间。结论:均匀设计法可用于药物联用的配比用量分析,但存在有一定局限,还需对结果进行实验验证。     

Effect of Honghua （Flos Carthami） on nitric oxide production in RAW 264.7 cells and a.glucosidase activity

OBJECTIVE： To study the effects of extracts from Honghua （Flos Carthaml~ on lipopolysaccharide in- duced nitric oxide （NO） production in RAW 264.7 cells and the influence of the extracts on yeast a-glucosidase activity. The total flavonoid content of the extracts was also determined. METHODS： Cytotoxicity of the extracts to RAW 264.7 cells was evaluated by the ATPliteTM method. Inhibitory effects of the extracts on NO production were evaluated by Griess assay. Curcumin was used as a positive control. Screening of extracts for po- tential a-glucosidase inhibitors was done by a fiuo- rometric assay. The assay was based on the hydroly- sis of 4-methylumbelliferyl-a-D-glucopyranoside toform the fluorescent product, 4-methylumbellifer- one. Acarbose was used as a positive control. The total t3avonoid content was tested using kaempfer- ol as the standard. RESULTS： There were significant inhibitory effects on NO production when the extracts were 25-100 μg/ mL （P〈0.05） and curcumin was 2-4 μg/mL （P〈 0.001）. The extracts showed an inhibitory effect on a-glucosidase activity at the concentrations of 15.6-125 μg/mL with a half maximal （50%）inhibito- ry concentration （ICs0） of （32.8± 5.7） μg/mL, com- pared with the ICs0 of acarbose at （1.8±0.4） μg/mL. There was a significant difference between the two IC50 values （P〈0.001）. The total content of flavo- noids per gram of dried herb was 1.14 mg. CONCLUSION： Honghua （Flos Carthami） showed in- hibitory effects on NO production in activated RAW 264.7 macrophage cells and an inhibitory effect on yeast a-glucosidase. There might be a relationship between these pharmacological effects and its fla- vonoid content.     

Carthamus tinctorius L. extract activates insulin‐like growth factor‐I receptor signaling to inhibit FAS‐death receptor pathway and suppress lipopolysaccharides‐induced H9c2 cardiomyoblast cell apoptosis

Carthamus tinctorius L. (Compositae) is used in Chinese medicine to treat heart disease and inflammation. In our previous study, we found that C. tinctorius L. inhibited lipopolysaccharides (LPS)‐induced tumor necrosis factor‐alpha (TNF‐α) activation, JNK expression, and apoptosis in H9c2 cardiomyoblast cells. The present study was performed to investigate the protective effect of C. tinctorius extract (CTF) on LPS‐challenged H9c2 myocardioblast cell and to explore the possible underlying mechanism. Cell viability assay showed that LPS treatment decreased the cell viability of H9c2 cell, whereas CTF treatment reversed LPS cytotoxicity in a dose‐dependent manner, especially in the LPS + CTF 25 (μg/mL) group. LPS treatment‐induced apoptosis was determined by transferase‐mediated dUTP nick end labeling assay, and by Western blot. LPS‐induced apoptotic bodies were decreased following CTF treatment. Expression of TNF‐α, FAS‐L, FAS, FADD, caspase‐8, BID, and t‐BID was significantly increased in LPS‐treated H9c2 cells. In contrast, it was significantly suppressed by the administration of CTF extract. In addition, CTF treatment activates antiapoptotic proteins, Bcl‐2 and p‐Bad, and downregulates Bax, cytochrome‐c, caspase‐9, caspase‐3, and apoptosis‐inducing factor expression. Furthermore, CTF exerted cytoprotective effects by activating insulin‐like growth factor‐I (IGF‐I) signaling pathway leading to downregulation of the apoptotic proteins involved in FAS death receptor pathway. In addition, AG1024 and IGF‐I receptor (IGF‐IR) inhibitor and siRNA silencing reverses the effect of CTF implying that CTF functions through the IGF‐IR pathway to inhibit LPS‐induced H9c2 apoptosis. These results suggest that treatment with CTF extract prevented the LPS‐induced apoptotic response through IGF‐I pathway.     

高效毛细管电泳法同时测定红花中腺苷、芦丁和槲皮素的含量

目的 用高效毛细管电泳法对红花中的有效成分腺苷、槲皮素和芦丁同时进行含量测定。方法 采用熔融石英毛细管柱（66.5 cm×50 μm ID，有效长度58 cm）作为分离通道；以50 mmol·L^-1硼砂其中含18%甲醇的溶液（pH 9.7）为运行缓冲液；运行电压: 24 kV；毛细管柱温: 20 ℃；检测波长： 210 nm。结果 以利福平为内标，腺苷、芦丁和槲皮素分别在10～160 mg·L^-1，100～2 000 mg·L^-1和100～1 600 mg·L^-1 线性关系良好（R>0.998）；平均回收率分别为98.5%～100.5%， 96.9%～99.5%和99.1%～99.5%； RSD分别为6.5%，5.2%和5.6%(N=5)。结论 此法操作简便快速，回收率及重现性好，可作为红花质量控制的方法。     

红花多糖对H22荷瘤小鼠的免疫调节和抗氧化功能的影响

目的：探讨红花多糖的抗肿瘤作用及其机制。方法：采用移植H22荷瘤小鼠模型,分别设置阴性对照组、阳性对照组和红花多糖低、中、高三个剂量组（15mg/kg、45mg/kg和135mg/kg）,对模型小鼠进行效果处理,观察各组的抑瘤效果、碳廓清能力、耳肿胀度,并对血清GR、GSH-PX、CAT、SOD和MDA含量等进行检测。结果：红花多糖高剂量可明显抑制小鼠H22实体瘤生长（P<0.05）,抑瘤率为66.8%;高剂量组小鼠血清MDA水平明显降低（P<0.05）,GR、GSH-PX、CAT、SOD活性较阴性对照组明显升高,还可降低肿瘤细胞中ROS水平（P<0.05）。结论：红花多糖可明显增强H22荷瘤小鼠的免疫功能,清除自由基、减轻活性氧造成的损伤,从而起到抗肿瘤的作用。     

红花化学成分的研究

红花为菊科植物红花（ＣａｒｔｈａｍｕｓｔｉｎｃｔｏｒｉｕｓＬ．）的干燥花，是重要的活血化瘀中药之一［１］。红花有降血压、降血脂等作用，临床上用于治疗冠心病、高血压等疾病［２］。为阐明红花的活性成分，我们曾以药理活性为指标，对其化学成分进行研究，报道...