基于“药辅合一”理念的厚朴挥发油纳米乳制备及其抗氧化性能研究

目的:采用Box-Behnken响应面法优化厚朴挥发油纳米乳处方的制备工艺并初步评价其稳定性及抗氧化效果。方法:以粒径为评价指标,筛选乳化剂、K_(m)值、厚朴挥发油用量三个因素的最佳比例,考察离心稳定性、稀释稳定性、储存温度稳定性以评价厚朴挥发油纳米乳的稳定性,并用1,1-二苯基-2-三硝基苯肼(1,1-Diphenyl-2-picrylhydrazyl,DPPH)自由基和2,2’-联氮-双(3-乙基苯并噻唑啉-6-磺酸)(2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid),ABTS^(+))阳离子自由基的清除能力为指标评价其抗氧化性能。结果:厚朴挥发油纳米乳的最优处方为厚朴挥发油15.05%,K_(m)值2.5,乳化剂32.9%,所制得的纳米乳外观澄清、透明、微泛蓝光、稳定性良好,厚朴挥发油和纳米乳均具有清除DPPH自由基和ABTS^(+)自由基能力,且厚朴挥发油纳米乳在DPPH和ABTS^(+)自由基的清除能力上更佳。结论:制备所得的厚朴挥发油纳米乳工艺可行、理化性质稳定,具有良好的抗氧化效果,为厚朴挥发油的开发利用提供一种新思路。

平胃散挥发性成分的研究(Ⅱ)——厚朴挥发油的GC/MS分析

利用色质联用 ( GC/MS)技术对复方制剂平胃散中的单味药材厚朴的挥发油成分进行测定 ,基于直观推导式演进特征投影 ( HELP)法对产生的二维色谱 /质谱数据进行分辨 ,得到各个组分的纯色谱曲线和质谱 ,根据色谱保留时间和纯质谱在质谱库中进行相似检索以实现对组分的定性 ,然后采用总体积积分法进行定量 .本文分离出 98个组分 ,其中鉴定了 4 4个组分 ,约占其挥发油总量的 5 8.74 %

厚朴挥发油萃取工艺优化、成分分析及抗氧化性分析

以恩施特色紫油厚朴为原料,采用超临界CO_(2)萃取厚朴挥发油,在单因素试验(夹带剂种类、夹带剂浓度、萃取压力、萃取温度、萃取时间和CO_(2)流量)基础上,借助响应面Box-Behnken设计工具预测厚朴挥发油的最佳萃取参数并重复验证(n=5)。通过气相色谱—质谱(GC-MS)分析其化学成分并测定了挥发油的抗氧化能力。经试验,在夹带剂乙醇用量10%、萃取压力36MPa、萃取温度43℃下,连续萃取1.5h,厚朴挥发油萃取率为(0.205±0.31)%,与模型函数预测值(0.208%)差值小于5%。从厚朴挥发油中鉴别出32种化合物,占全油的86.05%,含量大于10%的成分有伞花烃(28.45%)、β-柠檬烯(18.27%)和桉叶醇(14.15%)。抗氧化试验表明厚朴挥发油对·OH自由基具有较强的清除能力和总还原能力,且与其浓度存在明显的量效关系,可作为天然抗氧化剂的原料来源。

厚朴挥发油纳米乳凝胶的制备及其对溃疡性结肠炎小鼠的药效评价

目的 制备厚朴Magnoliae Officinalis Cortex(MOC)挥发油纳米乳凝胶(MOC volatile oil nanogel,MNG),评价其结肠靶向释放性能,并考察其对葡聚糖硫酸钠(dextran sodium sulfate,DSS)诱导溃疡性结肠炎(ulcerative colitis,UC)小鼠的治疗作用。方法 采用自乳化法制备厚朴挥发油纳米乳(MOC volatile oil nanoemulsion,MN),并对其形貌、粒径、电位等理化性质进行表征;以成胶时间为指标优选透明质酸和海藻酸钠的质量浓度,将最优比的透明质酸和海藻酸钠溶于MN中形成MNG,对得到的MNG进行理化性质表征,并评价其结肠靶向和对DSS诱导的UC小鼠的治疗作用。结果 所制得的MN外观澄清、透明、微泛蓝光,透射电镜观察纳米乳呈球形,平均粒径为(61.56±1.67)nm,ζ电位为(-21.37±0.45)m V,包封率为(85.25±0.50)%;在最佳MN配方的基础上,以海藻酸钠和透明质酸质量浓度分别为30 mg/mL和40mg/mL作为凝胶基质,制得最佳MNG;药效学实验证明MNG对UC小鼠具有较好的治疗作用。结论 成功制备MNG,提高厚朴挥发油稳定性的同时,使其具有结肠靶向释放能力。

中药厚朴产地加工发汗前后所含挥发油抗氧化活性及治疗溃疡性结肠炎药效研究

目的研究厚朴发汗前后挥发油体外抗氧化活性及对溃疡性结肠炎小鼠药效作用。方法采用1,1-二苯基-2-三硝基苯肼(1,1-Diphenyl-2-picrylhydrazyl,DPPH)自由基、2,2’-联氮-双(3-乙基苯并噻唑啉-6-磺酸)[2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid),ABTS^(+)]阳离子自由基、总还原力的清除能力为指标评价厚朴发汗前后挥发油的体外抗氧化活性;将42只雄性ICR小鼠采用葡聚糖硫酸钠(dextran sulfate sodium salt,DSS)建立经典溃疡性结肠炎(ulcerative colitis,UC)小鼠模型,记录正常组、模型组、发汗厚朴挥发油高剂量组、发汗厚朴挥发油低剂量组、未发汗厚朴挥发油高剂量组、未发汗厚朴挥发油低剂量组、柳氮磺吡啶组相关指标差异。结果发汗前后厚朴挥发油均具有一定还原力、清除DPPH自由基和ABTS^(+)自由基能力,且发汗厚朴挥发油在DPPH和ABTS+自由基的清除能力上更佳;发汗前后厚朴挥发油高剂量组及柳氮磺吡啶组均可改善DSS造成的小鼠疾病活动指数(disease activity index,DAI)评分升高,恢复DSS小鼠肠道组织的病理状态,改善脾脏系数和单位长度结肠质量,调节小鼠结肠中白细胞介素-6(interleukin-6,IL-6)、白细胞介素-1β(interleukin-1β,IL-1β)、肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)炎症因子水平,降低结肠黏膜细胞中闭合蛋白(claudin-1)和闭锁蛋白(Occludin)的表达,且发汗后药效更强。结论发汗前后厚朴挥发油均具有抗溃疡性结肠炎及抗氧化作用,且发汗后厚朴挥发油的效果更佳,进一步阐释了厚朴产地加工发汗的科学性。

ANTI-INFLAMMATORY EFFECTS OF MAGNOLIAE FARGESII VOLATILE OIL

Objective To explore the anti-inflammatory effects of magnoliae fargesii volatile oil.Methods Human umbilical vein endothelial cells (HUVECs) were stimulated by TNF-α to express the adhesion molecules. Then the anti-adhesion effects of magnoliae fargesii volatile oil between HUVECs and human peripheral neutrophils were observed. The ischemia-reperfusion animal models were established by 60min renal ischemia followed by 1, 3, 6 and 24h reperfusion. Rats were randomly divided into the following groups: the sham-operation controls, ischemic group only treated with normal saline, and treated group infused magnoliae fargesii volatile oil before reperfusion. Then the renal injury of rats was detected. Results High rate of cell adhesion between HUVECs and neutrophils was observed. Magnoliae fargesii volatile oil could inhibit the adhesion process at the concentration of 0.5μL/mL (191.6±8.6), 1.0μL/mL (158.2±9.0) and 2.0μL/mL (155.2±9.7) (P<0.05). The anti-adhesion effects were strengthened with the increase of volatile oil concentration. Blood urea nitrogen and creatinine levels of the animal models were significantly increased after 24h reperfusion while the increase was remarkably attenuated by the treatment with magnoliae fargesii volatile oil. The renal injury was severe after 1h reperfusion, which was significantly attenuated by the treatment of magnoliae fargesii volatile oil. Conclusion Magnoliae fargesii volatile oil has anti-inflammatory effects.