正交试验优选甘草制款冬花的炮制减毒工艺

目的:优选甘草制款冬花的炮制减毒工艺,为款冬花的炮制生产工艺提供参考。方法:以总生物碱含量为指标,甘草水煎煮次数、烘制温度及甘草用量(甘草质量/款冬花质量)为考察因素,采用正交试验对甘草制款冬花的减毒工艺进行优选,考察款冬花甘草制品中有效成分含量的变化。结果:款冬花甘草制最佳减毒工艺条件为甘草用量10%,水煎煮数3次,烘制温度90℃;甘草制款冬花中总生物碱、款冬酮及醇浸出物质量分数分别为0.080 3 mg·g-1,0.161%,26.31%。结论:与生品相比,款冬花甘草制品中总生物碱含量显著减少,款冬酮和醇浸出物含量增加。优选的款冬花甘草制减毒工艺稳定可行,提示甘草汁制款冬花有一定的合理性,具有实际应用意义。     

近红外光谱用于甘草中甘草苷、甘草酸及水分测定

目的:运用近红外光谱(NIR)技术检测甘草药材中的甘草苷、甘草酸及水分。方法:采用积分球漫反射扫描近红外光谱,以TQ Analyst软件进行数据分析,建立甘草中甘草苷、甘草酸及水分测定的NIR。结果:甘草苷的预测均方根误差(RMSEP)为0.165,预测集相关系数(Rp)0.986 8;交叉验证均方根误差(RMSECV)为0.393,校正集相关系数(Rv)0.904 6。甘草酸的RMSEP=0.166,Rp=0.995 5;RMSECV=0.575,Rv=0.954 0。水分的RMSEP=0.137,Rp=0.995 2;RMSECV=0.498,Rv=0.931 9。结论:该方法快速、简便。可以用于甘草中甘草苷、甘草酸及水分的含量测定。     

给药剂量对附子总生物碱在大鼠体内药代动力学特征的影响

目的:考察不同剂量附子总生物碱在大鼠体内的药动学特征,并探讨剂量与药动学的关系。方法:将大鼠随机均分为低、中、高剂量组,分别按9.6,19.2,38.4 mg·kg-1灌胃附子总生物碱,在0,5,10,20,30,40,60,120,180,300,420,540,720,1 440 min共14个时间点眼眶内眦静脉取血,采用UHPLC-Q-TOF-MS测定不同时间点血浆中乌头碱、新乌头碱、次乌头碱、苯甲酰乌头原碱、苯甲酰新乌头原碱、苯甲酰次乌头原碱和乌头原碱的血药浓度,绘制药-时曲线,计算药动学参数。结果:与低剂量组比较,中、高剂量组上述7种生物碱类成分的药峰浓度(Cmax)和药时曲线下面积AUC0-∞升高,大部分差异有统计学意义;表观分布容积/生物利用度(Vz/F),清除率(CL)/F,半衰期(t1/2)和达峰时间(Tmax)则大部分无明显变化。结论:剂量对附子总生物碱在大鼠体内的药动学特征有显著影响,从低剂量到高剂量的范围内,附子总生物碱的体内过程基本符合线性动力学特征。     

Melanogenesis inhibitory compounds from Saussureae Radix

Ten compounds were isolated from the EtOAc soluble part of the MeOH extract of Saussureae Radix, with their effects on melanin production also evaluated in B-16 mouse melanoma cell lines stimulated with 3-isobutyl-1-methylxanthine (IBMX), an elevator of cellular cAMP. The compounds were identified as aplotaxene (1), 1β-hydroxy arbusculin A (2), costunolide (3), dehydrocostuslactone (4), 11β,13-dihydrocostunolide (5), reynosin (6), heptadec-(9Z)-enoic acid (7), β-sitosterol (8), linoleic acid methyl ester (9) and betulinic acid methyl ester (10). Compounds 2, 9 and 10 were identified from Saussureae Radix for the first time. Furthermore, compounds 2, 3 and 6 showed potent inhibitory effects on the IBMX-induced melanogenesis, in dose-dependent manners, with IC₅₀ values of 11, 3 and 2.5 μg/mL, respectively. As a positive control, arbutin exhibited an IC₅₀ value of 29 μg/mL.     

Purification and structural analysis of a novel polysaccharide from Rehmannia Radix Praeparata

In this paper, the purification, structure, and antioxidant activity of Rehmannia Radix Praeparata polysaccharide (RRPP) were studied. The RRPP was separated using DEAE-52 cellulose and Sephadex G-100. The RRPP consisted of xylose, glucose, rhamnose, galactose, and mannose in ratios of 10.64:5.58:3.52:1.39:1.0. No protein was detected in the RRPP fraction, and the molecular weight of RRPP was about 1.75 × 10⁶ Da. The basic skeleton information was obtained using periodic acid oxidation—Smith degradation, and RRPP contained 1→, 1 → 2, 1 → 3, 1 → 4, 1 → 2,6, 1 → 4,6 or 1 → 6, 1 → 2,3, 1 → 2,3,4, and other glycosidic bonds. Fourier transform infrared spectroscopy also showed that RRPP has both α- and β-glycosidic bonds. The in vitro antioxidant activity test showed that RRPP could potentialize scavenging effect on ABTS^+· and its scavenging rate was 91.3%.     

板蓝根水提物对糖尿病大鼠早期肝损伤的影响

目的 研究板蓝根水提物（water extract of Radix Isatidis,WERI）对糖尿病大鼠肝功能的影响。方法 采用链脲佐菌素诱导Wistar大鼠糖尿病模型,随机分为模型组、罗格列酮组（0.3 mg·kg^-1）、WERI高、中、低剂量组（100,50,25 mg·kg^-1）,并设正常对照组,均采用灌胃给药。4周后,检测各组大鼠空腹血糖（FBG）、空腹胰岛素（FINS）、肝系数、谷丙转氨酶（ALT）、谷草转氨酶（AST）、游离脂肪酸（FFA）和血清脂联素（ADP）,并观察大鼠肝脏组织病理形态学变化。结果 与正常对照组比较,模型组大鼠FBG、FINS、肝系数、ALT、AST、FFA水平均显著升高（P<0.05或P<0.01）;血清ADP含量显著降低（P<0.05）。与模型组比较,WERI高剂量组大鼠FBG、FINS、肝系数、ALT、AST、FFA水平均显著降低（P<0.05或P<0.01）,血清ADP含量升高（P<0.05）;罗格列酮组与WERI高、中、低剂量组大鼠肝脏病理形态均显著改善。结论 WERI对糖尿病大鼠的肝功能具有保护作用。     

三叶青水提物对慢性阻塞性肺疾病MMP－9和TIMP－1的影响

目的：观察三叶青水提物对慢性阻塞性肺疾病（COPD）大鼠基质金属蛋白酶9（Matrix met alloproteinases－9,MMP－9）和基质金属蛋白酶抑制剂－1（Matrix met alloproteinases inhibitor－1,TIMP－1）的影响,探讨三叶青对大鼠肺组织的作用机制。方法选择烟熏加气管内滴注内毒素（ LPS）法复制COPD模型,将清洁级健康SD雄性大鼠30只,随机分为3组分别为对照组、模型组和三叶青组,每组10只。造模成功后肺组织采用HE染色观察病理改变,采用免疫组织化学方法测定大鼠肺组织中MMP－9和TIMP－1的表达,酶联免疫吸附法测定大鼠血清、支气管肺泡灌洗液和肺匀浆组织中MMP－9和TIMP－1的表达。结果光学显微镜下可见三叶青组大鼠炎症较模型组有所减轻。酶联免疫吸附法检测结果显示,模型组大鼠肺组织、血清和支气管肺泡灌洗液中MMP－9和TIMP－1含量较对照组显著增加（ P＜0．05）,三叶青组的MMP－9和TIMP－1含量较模型组显著下降（P＜0．05）。免疫组织化学检测结果显示,与对照组比较模型组肺组织中的MMP－9和TIMP－1表达明显增多,差异有统计学意义（P＜0．05）。与模型组比较三叶青组肺组织中的MMP－9和TIMP－1表达减少,差异有统计学意义（P ＜0．05）。结论三叶青可能通过下调MMP－9、TIMP－1表达,调节MMP－9／TIMP－1失衡,进而干预气道重塑,延缓病变进展,这可能是其治疗COPD的作用机制之一。     

中药饮片麦冬和芫花中耐热菌的考察

目的 考察中药饮片麦冬和芫花中耐热菌的种类和数量,并探索在冷藏储存过程中的变化情况。方法 采用中国药典2015年版方法测定不同沸水浴时间的耐热菌数,并对120 min沸水浴处理后存活耐热菌采用16S rDNA 基因序列分析方法进行菌种鉴定,同时考察了冷藏储存一定时间后耐热菌数的变化。结果 随着沸水浴时间的增加,耐热菌数不断减少。芫花即使经过120 min沸水浴处理后仍含有较高数量的耐热菌,且经48 h冷藏储存后,耐热菌数量出现明显增加。耐热菌株鉴定结果均为芽孢杆菌属。结论 从用药安全性角度考虑,应控制中药饮片中的耐热菌,并关注中药代煎服务存在的微生物污染问题。     

A subchronic toxicity study of Radix Dipsaci water extract by oral administration in F344 rats

Radix Dipsaci, the dried root of Dipsacus asperoides C.Y. Cheng & T.M.Ai, has therapeutic effects on various disorders, and in particular, bone and joint disease. Despite such ethnomedicinal benefits, there is very little information regarding its in vivo toxicity or adverse effects. This study was conducted to evaluate the potential toxicity of the Radix Dipsaci water Extract (RD-wE) by using F344 rats. The RD-wE was administered orally to rats at doses of 0, 125, 250, 500, 1000, and 2000 mg/kg body weight (bw)/day for 13 weeks. During the treatment period there were no mortalities attributed to RD-wE. Moreover, no toxic effects were observed with regard to body weight, clinical pathology (hematology, clinical biochemistry, and urinalysis), and anatomic pathology (gross findings, organ weight, and microscopic examination). The changes related to the treatment were excessive salivation at the mouth and soft feces, observed in male and female rats at 1000 or 2000 mg/kg bw/day, but these were not accompanied by any microscopic correlate or other pathophysiological changes. Based on these results, the oral no-observed-adverse-effect level of the RD-wE was considered to be 2000 mg/kg bw/day in both genders, although the target organs were not determined under the current experimental conditions.     

HPLC-UV法同时测定羌活酚酸和香豆素类成分含量

[目的]建立同时测定羌活酚酸(新绿原酸、绿原酸和阿魏酸)和香豆素(羌活醇和异欧前胡素)两类成分的高效液相色谱-紫外分析法(HPLC-UV),为羌活药材的质量评价提供技术支撑。[方法]Agilent Zorbax SB-C18反相色谱柱(4.6 mm×250 mm,5μm),流动相为乙腈-0.2%磷酸水,检测波长330 nm,进样量5μL,流速1 m L/min。[结果]两类成分具有良好的线性关系,方法学验证均符合要求。[结论]该方法简单易行,重复性好,专属性强,可用于羌活药材的质量控制。