麦芽4个化学部位通过多巴胺D2受体对产后缺乳模型大鼠催乳作用研究

目的基于多巴胺D2受体(DRD2),考察小剂量麦芽4个化学部位的催乳作用,初步探讨小剂量麦芽生物碱对产后缺乳模型大鼠泌乳素(PRL)分泌的调节机制。方法采用ig甲磺酸溴隐亭方法制备缺乳大鼠模型,造模成功后,各给药组均ig给予相应的药物,应用ELISA法检测各组大鼠血清PRL、雌二醇(E_2)、孕酮(P)水平;HE染色观察各组大鼠乳腺组织病理改变;采用实时荧光定量PCR(qRT-PCR)法检测各组大鼠脑垂体中泌乳素受体及DRD2 mRNA表达。结果与对照组比较,模型组大鼠血清中PRL、P及E_2水平、脑垂体PRL mRNA表达水平显著降低;脑垂体DRD2 mRNA表达水平显著升高。与模型组比较,麦芽总生物碱组大鼠乳腺小叶体积明显增加,导管明显扩张,且导管及腺泡内含有大量乳汁。麦芽总生物碱明显增加模型大鼠血清中PRL、P、E_2水平及脑垂体PRL mRNA表达水平,降低脑垂体DRD2 mRNA表达水平。结论麦芽催乳的主要药效物质为总生物碱,其作用机制可能与促进PRL分泌,增加脑垂体PRL受体、降低DRD2 mRNA表达水平有关。     

菠萝叶提取物黏附漂浮微丸的制备及评价

采用挤出滚圆法,以壳聚糖为骨架黏附材料,十八醇为漂浮材料,制备菠萝叶提取物(Bolo leaf phenols,BLP)黏附漂浮微丸,评价其体外黏附性、漂浮性及体内滞留情况,并考察药物的体外释放特性。通过体外组织留存量法和直接观察法分别评价微丸的体外黏附性和漂浮性;采用体内组织留存量法和小动物活体成像法考察微丸在大鼠体内的滞留情况;对微丸中指标成分对香豆酸和咖啡酸的体外释放情况进行评价。结果显示,制备的黏附漂浮微丸体外黏附性达(73.2±3.4)%,在人工胃液中可立即起漂,持续漂浮时间在12 h以上;黏附漂浮微丸在大鼠胃内6 h时滞留率达40%以上,而普通参比微丸胃滞留率低于15%,两者相比,滞留效果具有显著性差异(P0.01);药物体外释放时间可达6 h以上,体外释药机制符合Higuchi方程。体内、外研究表明,制备的BLP黏附漂浮微丸具有良好的胃滞留效果和缓释特性。     

区分3种法定基源麻黄的酚类成分HPLC特征图谱中指标成分的确定及4种成分的含量测定

针对麻黄中酚类成分建立HPLC特征图谱,寻找其中指标成分,并对其在草麻黄、中麻黄、木贼麻黄草质茎中的分布及含量规律进行分析。利用HPLC-DAD建立酚类成分特征图谱,采用YMC-Pack ODS-A(4.6 mm×250 mm, 5 μm)色谱柱,以0.01%甲酸水溶液-乙腈为流动相,梯度洗脱,流速1.0 mL·min^-1,柱温40℃,检测波长330, 350 nm。对46批次法定基源麻黄自采样品进行测定,所得图谱可实现基源间有效区分。结合主成分分析、峰面积分布分析,细致探讨图谱中12个主要成分峰对3种法定基源麻黄特征及差异的贡献:其中,10, 11, 12号峰峰面积在木贼麻黄中显著高于另两基源,利用其总峰面积值(木贼麻黄中高于146 mAU),可实现木贼麻黄与另两基源的有效区分;1号峰峰面积在草麻黄、4号峰峰面积在中麻黄中显著高于其他法定基源,分别为两基源麻黄中重要的差异成分峰;8,9号峰为3种基源麻黄中的共有特征成分峰;其余各峰在不同基源麻黄中的分布存在不同程度差异,辅助上述成分,实现3种法定基源麻黄的有效区分。进一步利用上述色谱条件,首次测定了法定基源麻黄中异牡荆素-2"-O-α-L-鼠李糖苷(1)、牡荆素(2)、茶花粉黄酮B(5)、草棉黄素-7-O-β-D-葡萄糖苷(6)4种指标成分的含量,在检测范围内线性良好,平均加样回收率为97.8%~102.5%。所测样品中4种成分的含量范围分别为trace~1.55(1),trace~0.160(2),trace~0.284(5),trace~0.620(6) mg·g^-1,且不同基源麻黄中,各成分含量存在差异。其中,1在草麻黄中质量分数(0.670±0.88) mg·g^-1显著高于另两基源麻黄(除Ei-060630-2-2外低于0.16 mg·g^-1); 6 在木贼麻黄中平均含量水平(0.260±0.039 2) mg·g^-1达草麻黄(0.120±0.270) mg·g^-1与中麻黄(0.136±0.485) mg·g^-1中的2倍,此二成分对法定基源麻黄间区分有重要贡献。所建酚类成分HPLC特征图谱与含量测定方法较为简便、准确,选定指标成分为区分麻黄基源、完善药材质量标准,提供了新的科学依据。     

Pigment identification,antioxidant activity,and nutrient composition of Tinospora cordifolia (willd.) Miers ex Hook. f & Thoms fruit

The stem, leaf, and root of Tinospora cordifolia (willd.) have been highly exploited for medicinal preparations; however, the nutritional and nutraceutical potential of its attractive red berries (fruits) have not so far been studied. Pigments, berberine (107.0 mg/100 g) and lycopene (50.8 mg/100 g), were identified in the deseeded fruit. Total phenol content in the fruit was 3.2 mg gallic acid equivalent/g. The IC₅₀ of DPPH^√ (82, and 468 ppm) and OH^√ (100, and 1,000 ppm) scavenging activity, and the EC₅₀ of reducing power (2,616, and 1,472 ppm) of hexane and methanol extracts, respectively, were observed. Oxygen radical absorbance capacities of the fruit extracts (150 and 300 ppm) were 1,107 and 2,614 μM trolox equivalent/g, respectively. Nutrient composition including carbohydrate (18.4%), proteins (1.5%), lipids (6%) of which ～62% was unsaturated fatty acids, vitamins like ascorbic acid (0.24 μg), niacin (0.7 mg), and tocopherols (2.4 mg) in 100 g fruits were determined. Potassium content was 1.2 g/100 g dry tissue of berries. These findings show that components of T. cordifolia fruit could be bioactive and used in food, pharmaceutical, and cosmetics.     

Effect of plant phenolic compounds on biofilm formation by Pseudomonas aeruginosa

In the natural environment, bacteria predominantly exist in matrix‐enclosed multicellular communities associated with various surfaces, referred to as biofilms. Bacteria in biofilms are extremely resistant to antibacterial agents thus causing serious problems for antimicrobial therapy. In this study, we showed that different plant phenolic compounds, at concentrations that did not or weakly suppressed bacterial growth, increased the capacity of Pseudomonas aeruginosa PAO1 to form biofilms. Biofilm formation of P. aeruginosa PAO1 was enhanced 3‐ to 7‐fold under the action of vanillin and epicatechin, and 2‐ to 2.5‐fold in the presence of 4‐hydroxybenzoic, gallic, cinnamic, sinapic, ferulic, and chlorogenic acids. At higher concentrations, these compounds displayed an inhibiting effect. Similar experiments carried out for comparison with Agrobacterium tumefaciens C58 showed the same pattern. Vanillin, 4‐hydroxybenzoic, and gallic acids at concentrations within the range of 40 to 400 μg/mL increased the production of N–3‐oxo‐dodecanoyl‐homoserine lactone in P. aeruginosa PAO1 which suggests a possible relationship between stimulation of biofilm formation and Las Quorum Sensing system of this bacterium. Using biosensors to detect N‐acyl‐homoserine lactones (AHL), we demonstrated that the plant phenolics studied did not mimic AHLs.     

基于UPLC-Q-TOF/MS的渴络欣胶囊化学成分研究

目的 采用超高效液相色谱-四级杆-飞行时间质谱（UPLC-Q-TOF-MS）技术对中药复方渴络欣胶囊中的化学成分进行研究。方法 采用ACQUITY UPLC HSS T3 C₁₈色谱柱（100 mm×2.1 mm,1.8 μm）,以甲醇-0.1%甲酸水溶液为流动相梯度洗脱,体积流量为0.3 mL/min;采用ESI源在正、负离子模式下分别采集数据。根据化合物精确相对分子质量及二级碎片离子信息,结合参考文献数据,鉴定渴络欣胶囊的主要化学成分。结果 从渴络欣胶囊中分离和鉴定出54个化学成分,包括蒽醌类化合物10个、黄酮类化合物10个、萜类化合物7个、酚类化合物16个等。结论 首次采用UPLC-Q-TOF/MS联用技术研究渴络欣胶囊中化学成分,进一步明确了其物质基础。     

Phenol and para-substituted phenols electrochemical oxidation pathways

The electrochemical behaviour of phenol, catechol, hydroquinone, resorcinol, dopamine, and para-substituted phenolic compounds, 4-ethylphenol, tyrosine, and tyramine, was studied over a wide pH range using a glassy carbon electrode. The oxidation of phenol is pH dependent and irreversible, occurring in one step, and followed by hydrolyse in ortho- and para-positions, leading to two oxidation products, catechol and hydroquinone. The oxidation of phenol oxidation products, ortho-phenol and para-phenol, is reversible and pH dependent. The oxidation potential of para-substituted phenols varies slightly due to their substituent group in position C4, and occurs in one oxidation step corresponding to the oxidation of phenol. The oxidation products of this group of para-substituted phenols are reversibly oxidised and adsorb on the electrode surface.     

基于药物体系的肉桂特征图谱质量表征关联分析研究

目的建立基于药物体系的肉桂特征图谱质量表征关联分析方法,全面评价肉桂饮片质量。方法采用HPLC-PDA法建立肉桂饮片特征图谱,筛选7个特征峰并通过相对保留时间表征其质的关联性;同时测定6个主要有效指标性成分(原儿茶酸、表儿茶素、香豆素、肉桂醇、肉桂酸、肉桂醛)的含量并表征主要酚类成分和主要苯丙素类成分的含量,通过关联度等概念表征其量的关联性。结果以批号13为基准,基于质的表征模式及关联分析,肉桂饮片特征图谱中筛选的7个特征峰中有酚类成分2个、苯丙素类成分5个,15批肉桂饮片色谱图中均含有此7个特征峰。基于量的表征模式及关联分析,批号14有效指标性成分总体含量高于基准批号13,批号4、6、8、10含量与基准批号13关联性较高,综合评价得出批号14、13、4、6、8、10优良度居前。结论在定性的基础上进行定量表征,可全面评价肉桂饮片质量优次,为肉桂饮片资源筛选、药物原料质量控制及应用提供依据,同时为中药质量评价提供新的方法。     

Effects of cooking on in vitro sinigrin bioaccessibility,total phenols,antioxidant and antimutagenic activity of cauliflower (Brassica oleraceae L. var. Botrytis)

Cauliflower (Brassica oleraceae L. var. Botrytis) is a good source of bioactive compounds, such as glucosinolates, phenolic compounds and vitamins. In this study, the effects of some processes (i.e. boiling, steaming) on the sinigrin bioaccessibility as a major glucosinolate found in cruciferous vegetables after in vitro digestion, also in vitro antimutagenic activities, total phenols and total antioxidant capacities of cauliflower were determined. The sinigrin content was reduced by approximately 9.6% and 29.1% in steamed and boiled cauliflower (p > 0.05), respectively. After in vitro simulated digestion, sinigrin content was decreased by 26.4% in raw samples, increased by 29.5% and 114.7% in steamed and boiled samples, respectively. In all samples, mutagenic effect to Salmonella typhimurium TA 100 was not seen. When samples were steamed, phenol content was increased by 14.83%. After boiling total phenol content of cauliflower was decreased by 1.8%. Total antioxidant capacities (TAC) measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3 ethylbenzothiazoline-6-sulfonic acid) (ABTS) methods were increased by 47% and 39%, respectively (p < 0.05) in steamed samples and decreased by 8% and 7% with boiling, respectively (p > 0.05). TAC in raw sample of cauliflower, which was investigated in phosphomolybdenum assays, was determined as 18.7 mg ascorbic acid equivalents (AAE)/100 g. In all cases, the highest antioxidant activity was determined in the steamed samples, while the lowest antioxidant activity was in boiled samples.