木芙蓉叶有效组分抗非特异性炎症的实验研究

目的观察木芙蓉叶有效组分(MFR-C)的抗非特异性炎症作用.方法通过大鼠鹿角菜致肿实验、大鼠蛋清致肿实验、小鼠腹腔毛细血管通透性实验和小鼠耳肿胀实验,对木芙蓉叶有效组分抗非特异性炎症的作用进行评定.结果 MFR-C和盐酸青藤碱对鹿角菜及蛋清所致的大鼠足肿胀具有良好的抑制作用,与空白对照组相比差异有显著性(P＜0.05);与空白组相比,MFR-C对乙酸引起的小鼠腹腔毛细血管通透性也具有良好的抑制作用,两者之间差异有显著性意义(P＜0.05);小鼠耳肿胀实验显示MFR-C有抑制二甲苯造成的非特异性耳肿胀作用,与空白组相比P＜0.05,与阳性对照组(盐酸青藤碱)相比有同样的抗炎消肿作用.结论木芙蓉叶有效组分(MFR-C)对鹿角菜、蛋清、乙酸及二甲苯引起的非特异性炎症具有良好的抑制作用.     

灯盏花对自发性高血压大鼠肾脏保护作用的实验研究

目的 :观察蛋白激酶 C ( PKC)抑制剂——灯盏花对自发性高血压大鼠 ( SHR)肾脏的保护作用。方法 :将 12只 10月龄 SHR随机分为灯盏花 ( SHRD)和生理盐水 ( SHRC)组 ,均以 10 m g/ ( kg· d)腹腔内注射 ,连续8周。测定血压、心率 ,用光镜、电镜观察肾脏结构改变。图像分析仪计算肾小球间质胶原面积、含量。结果 :SHRD组肾脏组织结构均有明显改善 ,肾小球面积校正后的胶原面积 ( GCA/ GA) ,SHRD 组较 SHRC 组降低 14 .87%〔( 14 .66± 1.74 ) % vs( 17.2 2± 2 .0 1) % ,差异有显著性意义 ( P <0 .0 5 )〕。结论 :SHRD 能在降低 SHR血压的同时延缓肾小球硬化发展的作用     

5种黄酮类化合物对凋亡心肌细胞Bcl-2家族蛋白表达的影响

目的 观察5种黄酮类化合物芦丁(RU)、二氢杨梅素(DMY)、陈皮素(HP)、大豆黄素(DA)、红花黄色素A(HYSA)对H2O2诱导的心肌细胞凋亡的作用,探讨其与克山病的关系及可能的作用机制.方法 培养新生Wistar仔鼠心肌细胞,分为对照组、模型组、药物孵育组,用荧光染色法观察心肌细胞凋亡情况,流式细胞仪检测细胞凋亡率,Western blot法观察凋亡相关基因Bcl-2家族蛋白表达.结果 与模型组[(24.33±6.51)%]比较,RU[(13.95±3.80)%]、DA[(11.82±3.50)%]、HYSA[(12.33±3.78)%]能有效降低心肌细胞凋亡率(P＜0.05).5种黄酮类化合物能不同程度地上调Bcl-2蛋白表达,下调Bax蛋白表达,使Bcl-2/Bax比值增力口[RU(0.989±0.094)、DMY(0.931±0.280)、HP(0.980±0.095)、DA(1.049±0.092)、HYSA(1.031±0.039)],与模型组(0.490±0.046)比较,差异均有统计学意义(P＜0.05);而Bcl-xl表达无明显变化(P＞0.05).结论 RU、DMY、HP、DA、HYSA可以通过Bcl-2、Bax途径调节细胞凋亡过程,发挥抗氧化作用,抑制细胞凋亡,为克山病防治提供了一种思路.     

Contents of major bioactive flavones in proprietary traditional Chinese medicine products and reference herb of Radix Scutellariae

A simple and efficient HPLC/UV method for the simultaneous determination of six bioactive flavones, namely baicalein, baicalin, wogonin, wogonoside, oroxylin A and oroxylin A-7-O-glucuronide, has been developed and applied for their content determination in reference herb and proprietary traditional Chinese medicine (PTCM) products of Radix Scutellariae. The chromatographic separation was carried out on a Thermo C₁₈ column and linear gradient elution was employed with a mobile phase containing acetonitrile and 20 mM sodium dihydrogen phosphate buffer (pH 4.6). All the analytes were detected by PDA detector at a wavelength of 270 nm. Contents of the analytes in Radix Scutellariae containing PTCM products in forms of capsule, soft capsule, tablet and dripping pill and the reference herb of Radix Scutellariae were analyzed by sonicator extraction with methanol and water mixture (80:20) containing 1 mM HCl for 30 min followed by HPLC analysis. Separation of the six analytes was achieved within 25 min with good linearity (R² > 0.99). The R.S.D. of both the intra-day and inter-day precision for all the six analytes was below 10.14%. The accuracy at different concentrations was within the range of −7.83 to 4.06%. The extraction recovery was within the range of 89.22–107.33% for all the analytes. Contents of the six flavones were found to vary significantly among different products with glycosides, such as baicalin, wogonoside and oroxylin A-7-O-glucuronide, in much greater quantity than their corresponding aglycones. In addition to baicalin (18.54 ± 0.71%, w/w), the commonly used marker compound for Radix Scutellariae, wogonoside (3.54 ± 0.18%, w/w) and oroxylin A-7-O-glucuronide (2.84 ± 0.14%, w/w) also existed in abundant amount in the reference herb. Our findings suggested that wogonoside and oroxylin A-7-O-glucuronide should also be served as the chemical markers together with baicalin for the quality control of herbs and PTCM products of Radix Scutellariae.     

微粒化纯化的黄酮成分治疗下肢慢性静脉功能不全133例的疗效评价

目的：前瞻性评估微粒化纯化的黄酮成分(爱脉朗)治疗慢性静脉功能不全(chronic venous insufficiency，CVI)的疗效。方法：按预先制定的标准，随机选择133例CVI患者。其中，研究前曾用其他药物治疗者34例(27．6％)，有合并症者38例(28．8％)。对入选患者进行CVI分级、临床症状和体征的治疗前评估，然后予以口服微粒化纯化的黄酮成分500mg／次，2次／d治疗。在治疗后15、30和60d进行测定和记录，最后进行统计学分析。结果：治疗前后患者的肢体肿胀、沉重、痉挛和疼痛程度等症状和体征有明显的改善并具有统计学意义。结论：微粒化纯化的黄酮成分能有效地改善CVI的临床症状和体征。     

淫洋藿总黄酮对大鼠血清中ACE,NO及ET含量的影响

目的　观察淫洋藿总黄酮对大鼠血清中血管紧张素转化酶 (ACE)、一氧化氮 (NO)及内皮素 (ET)含量的影响。方法　用紫外分光光度法和放射免疫学方法 ,测定淫洋藿总黄酮 (大剂量组 2 0 0mg kg·d ;小剂量组10 0mg kg·d ;腹腔注射 ,用药 7d后 )对大鼠血清中ACE ,ET的活性及NO含量的影响。结果　淫洋藿总黄酮对ACE活性无影响 (P >0 .0 5 ) ;对ET有抑制作用 (P <0 .0 1) ;NO含量明显降低 (P <0 .0 1)。结论　淫洋藿总黄酮的降压作用与其降低血浆内皮素的含量有关。     

气相色谱-质谱联用分析莳萝子中挥发油和油脂的化学成分及其抗氧化活性研究

目的 提取莳萝子的挥发油和油脂,并对其组成进行分析,筛选出活性成分,为莳萝子挥发油、油脂的临床应用研究提供依据。方法 2021年6月至2022年2月采用水蒸气蒸馏法提取挥发油,经石油醚索氏提取油脂,用气相色谱-质谱联用（GCMS）联用仪分析鉴定其组分,并通过检测清除自由基能力评价抗氧化活性。结果 莳萝子挥发油提取率为（5.850±0.141）%,共鉴定出19种化合物,主要含有黄酮类化合物（61.418%）及萜类化合物（29.471%）;莳萝子油脂提取率为（13.168±0.117）%,共鉴定出16种化合物,主要包括亚油酸甲酯（5.58%）、顺式亚油酸（5.58%）、十八碳六烯酸甲酯（56.73%）等。1,1-二苯基-2-三硝基苯肼（DPPH）自由基清除率结果是挥发油的IC50值（半抑制浓度）为42.963 mg/L,油脂的IC50值为28.430 mg/L;2’-联氨-双（3-乙基苯并噻唑啉-6-磺酸）二胺盐（ABTS）自由基清除率结果是莳挥发油的IC50值为21.129 mg/L,油脂的IC50值为9.722 mg/L。结论 莳萝子挥发油、油脂均具有较强的抗氧化能力。     

一测多评法测定止血化痔合剂中6种黄酮类成分的含量

目的 建立一种一测多评法（QAMS）同时测定止血化痔合剂中6种黄酮类成分的含量。方法 采用高效液相色谱法,以黄芩苷为内参物,建立黄芩苷与芦丁、甘草苷、槲皮素、黄芩素、汉黄芩素的相对校正因子（f）,再通过f计算出止血化痔合剂中6种黄酮类成分的含量。同时采用外标法（ESM）测定6种黄酮类成分的含量,并比较二者的差异,以验证一测多评法的准确性和可行性。结果 芦丁、甘草苷、黄芩苷、槲皮素、黄芩素、汉黄芩素在一定范围内浓度与峰面积呈良好的线性关系（r>0.997）;精密度、稳定性、重复性均符合方法学要求;平均加样回收率范围为95.72%～100.43%,RSD范围为1.97%～3.22%。芦丁、甘草苷、槲皮素、黄芩素、汉黄芩素的相对校正因子分别为6.426、3.939、3.215、41.140、0.555,且重现性良好。一测多评法的计算结果与外标法测定结果差异无统计学意义（P>0.05）。结论 以黄芩苷为内参物建立的一测多评法,同时测定止血化痔合剂中6种黄酮类成分的含量,方法操作简便,准确可靠,可用于止血化痔合剂的质量评价。     

Flavonoids diosmetin and luteolin inhibit midazolam metabolism by human liver microsomes and recombinant CYP 3A4 and CYP3A5 enzymes

We evaluated the effects of increasing concentrations of the flavonoids salvigenin, diosmetin and luteolin on the in vitro metabolism of midazolam (MDZ), a probe substrate for cytochrome P450 (CYP) 3A enzymes, which is converted into 1'-hydroxy-midazolam (1'-OH-MDZ) and 4-hydroxy-midazolam (4-OH-MDZ) by human liver microsomes. Salvigenin had only a modest effect on MDZ metabolism, whereas diosmetin and luteolin inhibited in a concentration-dependent manner the formation of both 1'-OH-MDZ and 4-OH-MDZ, with apparent K(i) values in the 30-50mumol range. Both diosmetin and luteolin decreased 1'-OH-MDZ formation by human recombinant CYP3A4, but not CYP3A5, whereas they decreased 4-OH-MDZ formation by both recombinant enzymes. To assess whether any relationship exists between the physico-chemical characteristics of flavones and their effects on MDZ metabolism, we tested the effects of three other flavones (flavone, tangeretin, chrysin) on MDZ metabolism by human liver microsomes. Whereas flavones possessing more than two hydroxyl groups (luteolin, diosmetin) inhibited MDZ biotransformation, flavones lacking hydroxyl groups in their A and B rings (flavone, tangeretin) stimulated MDZ metabolism. We also found close relationships between the maximum stimulatory or inhibitory effects of flavones on 1'-OH-MDZ and 4-OH-MDZ formation rates and their log of octanol/water partition coefficients (logP) or their total number of hydroxyl groups. The results of the study may be of clinical relevance since they suggest that luteolin and diosmetin may cause pharmacokinetic interactions with co-administered drugs metabolized via CYP3A.     

建立凤尾草中总黄酮和木犀草素的含量测定方法

目的 建立凤尾草中木犀草素及总黄酮的含量测定方法.方法 采用D101大孔树脂分段洗脱,并采用紫外分光光度法测定总黄酮含量;采用HPLC法测定木犀草素含量.色谱柱为RP-C18柱(4.6 mm×250 mm,5μm);流动相为乙腈-0.2%磷酸(35:65),检测波长349 nm,流速1.0 ml/min,柱温30℃.结果 3批凤尾草药材中木犀草素含量依次为0.015%、0.019%、0.016%;总黄酮含量依次为0.55%、0.66%、0.59%.结论 所建立的分析方法准确、简便,可为定量评价凤尾草药材的质量提供依据.