Lauraceae plants are diverse in species and rich in volatile components, which possess functions such as insect repellency, antioxidant activity, and antibacterial properties. However, currently, the methods for analyzing the volatile components of Lauraceae plants are relatively single. The essential oils are mainly extracted by steam distillation, but the pretreatment is relatively complex and cumbersome. Therefore, it is essential to find a simple and cost-effective method. By comparing different extraction methods, HS-SPME-GC-MS was selected as the optimal extraction condition. Regarding Head-space Solid-Phase Microextraction and Gas Chromatography-Mass Spectrometry (HS-SPME-GC-MS), single-factor condition optimization and response surface analysis were carried out for different fiber coatings, equilibrium time, extraction temperature, and extraction time. Eventually, 75-μm CAR/PDMS fiber head was chosen, with an equilibrium time of 15 min, and extraction was conducted at 70°C for 57 min as the optimal HS-SPME extraction conditions. Furthermore, a differential analysis of the volatile components of five Lauraceae plants from different genera was performed, and differential metabolites were screened out respectively. This can effectively separate Cinnamomum and Litsea from the other three genera, providing certain assistance for the chemotaxonomy of the volatile components of Lauraceae plants and the subsequent development of medicinal plant resources.
2,2′,4,4′-Tetrabrominated biphenyl ether (BDE-47) is a polybrominated diphenyl ether (PBDE) homologue that is ubiquitous in biological samples and highly toxic to humans and other organisms. Prior research has confirmed that BDE-47 can induce oxidative damage in RAW264.7 cells, resulting in apoptosis and impaired immune function. The current study mainly focused on how Isoliquiritigenin (ISL) and Licochalcone B (LCB) might protect against BDE-47’s immunotoxic effects on RAW264.7 cells. The results show that ISL and LCB could increase phagocytosis, increase the production of MHC-II, and decrease the production of inflammatory factors (TNF-α, IL-6, and IL-1β) and co-stimulatory factors (CD40, CD80, and CD86), alleviating the immune function impairment caused by BDE-47. Secondly, both ISL and LCB could reduce the expressions of the proteins Bax and Caspase-3, promote the expression of the protein Bcl-2, and reduce the apoptotic rate, alleviating the apoptosis initiated by BDE-47. Additionally, ISL and LCB could increase the levels of antioxidant substances (SOD, CAT, and GSH) and decrease the production of reactive oxygen species (ROS), thereby counteracting the oxidative stress induced by BDE-47. Ultimately, ISL and LCB suppress the NF-κB pathway by down-regulating IKBKB and up-regulating IκB-Alpha in addition to activating the Nrf2 pathway and promoting the production of HO-1 and NQO1. To summarize, BDE-47 causes oxidative damage that can be mitigated by ISL and LCB through the activation of the Nrf2 pathway and inhibition of the NF-κB pathway, which in turn prevents immune function impairment and apoptosis. These findings enrich the current understanding of the toxicological molecular mechanism of BDE-47 and the detoxification mechanism of licorice.
Alzheimer's disease (AD) is a progressive neurodegenerative disease that primarily develops in old age. The main clinical symptom of the disease is memory loss. Therefore, the treatment of learning and memory dysfunction is an important research direction for prevention and treatment of AD. Studies have shown that scopolamine hydrobromide (SCOP), sodium nitrite (NaNO2) and ethanol impair memory acquisition, memory consolidation and memory retrieval in mice, respectively. Safflower yellow (SY) can effectively improve the memory function of AD mice, but the specific mechanism needs further exploration. In the present study, mice were injected with SCOP, NaNO2 and 40% ethanol to establish models of memory acquisition, memory consolidation and memory retrieval impairment. This study investigated the mechanism of SY treatment of AD from the perspectives of oxidative stress, the cholinergic system, the CREB/BDNF/TrkB signaling pathway and synaptic protein expression. We conducted several studies that have shown that after SY treatment, the memory ability of three memory impairment mice models improved, the pathological changes in brain tissue were reduced, the activity of cholinergic system-related enzymes were changed, the level of oxidative stress in the brain of mice was reduced, and the CREB/BDNF/TrkB pathway was activated. In addition, SY can also upregulate the expression of synapse-associated proteins and exert neuroprotective effects.
Postoperative abdominal adhesion is one of the most common complications after abdominal surgery. A single drug or physical barrier treatment does not achieve the ideal anti-adhesion effect. We developed a thermosensitive hydrogel (PPH hydrogel) consisting of poloxamer 407 (P407), poloxamer (P188), and hydroxypropyl methylcellulose (HPMC) co-blended. An injectable thermosensitive TA/MMC-PPH hydrogel was obtained by loading tannic acid (TA) with an anti-inflammatory effect and mitomycin C (MMC), which inhibits fibroblast migration or proliferation. The optimal prescriptions of PPH hydrogels with a suitable gelling time (63 s) at 37 °C was 20% (w/v) P407, 18% (w/v) P188, and 0.5% (w/v) HPMC. The scanning electron microscopy (SEM) revealed that the PPH hydrogel had a three-dimensional mesh structure, which was favorable for drug encapsulation. The PPH hydrogel had a suitable gelation temperature of 33 °C, a high gel strength, and complicated viscosity at 37 °C, according to the rheological analysis. In vitro release studies have shown that the PPH hydrogel could delay the release of TA and MMC and conform to the first-order release rate. Anti-adhesion tests performed on rats in vivo revealed that TA/MMC-PPH hydrogel significantly reduced the risk of postoperative adhesion. In conclusion, the TA/MMC-PPH hydrogel prepared in this study showed an excellent performance in both controlled drug release and anti-adhesive effects. It can be used as a protocol to prevent or reduce postoperative abdominal adhesion.
药品作为一种特殊的商品,与人民群众的生命安全息息相关.课程组教师在药学专业学生培养过程中,将思政理论与专业知识相结合,通过目标设置、环节设计等开展教学改革,达到了很好的课程育人效果.
药物分析课程是药学专业核心课程,也是一门理论和实践联系非常紧密的学科.近年来,通过探索,开展在线课程建设,作者制作完成了药物分析慕课,2018年该课程被评为第二批国家精品在线开放课程,也是新疆目前唯一获评课程.该门课程作为混合式教学改革的组成部分,被应用在药学专业本科教学当中,取得较好的教学效果.
药学英语是将基础英语与专业英语相结合的一门专业个性选修课程,随着应用型专业英语人才需求不断增加,逐渐发展成各大医药院校英语教学的重要组成部分.课程目标是培养学生掌握必要词汇、具备药学专业知识并且能理解掌握药学专业英文文献的能力等.通过自身的教学体会,针对我校药学英语课程的特点及教学现状,例如存在药学专业英语词汇繁多、学生学习兴趣低、教学形式单一及教学效果差等问题,提出了改革方式,将教学的改革应用到实际的教学过程中,以期提升药学英语课程的教学质量,为社会培养出更优秀的药学复合型专业人才.
目的 更好地发挥天山堇菜的药用功效,将其制成凝胶剂进行研究和质量评价.方法 用正交设计-效应面优化法优选天山堇菜微乳凝胶剂的基质,并用失水率、成型性作为评价指标,最终制成成型性较好,失水率较低的凝胶基质.结果 最优配方为黄原胶0.89%、甘油7.7%、羟丙甲基纤维素为1.79%、蒸馏水为90.42%、尼泊金乙酯0.2%、三乙醇胺适量.结论 由此基质制备的天山堇菜凝胶剂安全稳定.
在疫情防控常态化的背景下,线上线下的混合式教学日益受到高校的重视,成为传统教学方式的有益补充.文章将超星"一平三端"应用于药学专业课程的教学过程当中,在课前、课中、课后三个阶段实施教学改革,提升了授课质量,取得了较好的教学效果.
目的 采用网络药理学方法,筛选天山花楸Sorbus tianschanica叶抗心肌缺血再灌注损伤(MIRI)的活性成分及主要靶点,验证天山花楸叶黄酮化合物对离体心脏缺血再灌注损伤的保护作用及其作用机制.方法 通过TCMSP等数据库辅助,筛选出天山花楸叶中具有保护MIRI作用的化合物;构建化合物-靶点-疾病网络及蛋白互作网络,定位关键靶点;建立Langendorff离体大鼠MIRI模型,给予黄酮提取物高剂量组(1.5 mg/L)、低剂量组(0.5 mg/L)与4'-chlorodiazepam (CDZ,1 μmol/L)预处理,观察缺血再灌注过程中心功能指标的变化情况,对新鲜的心肌组织进行TTC染色,测定心肌梗死面积;石蜡包埋切片HE染色;心肌组织超氧化物歧化酶(SOD)、丙二醛(MDA)、过氧化氢酶(CAT)、还原性谷胱甘肽/氧化型谷胱甘肽(GSH/GSSG)、总抗氧化能力(T-AOC)和mPTP孔的开放程度.结果 网络药理学方法筛选得到天山花楸抗心肌缺血再灌注损伤活性成分主要为黄酮类化合物,核心靶点为TSPO,与线粒体膜通透性转换孔mPTP密切相关;各给药组均能显著增强心功能指标,减小心肌梗死面积(P<0.01),减轻心肌组织病理损伤,增强心肌组织抗氧化能力(P<0.01),抑制mPTP孔的开放(P<0.01),减轻线粒体水肿;其中,高剂量组作用最强.结论 天山花楸叶黄酮提取物可增强心肌舒缩功能,减小心肌梗死面积,减轻心肌组织氧化应激损伤,通过作用于TSPO靶点,抑制mPTP孔开放,减轻心肌细胞线粒体水肿从而保护心肌组织.
对慕课应用于传统公选课教学进行论述,分析不同类型教学资源的实际应用,对于发现的突出问题进行归纳并提出解决方法,总结与展望慕课在医学教育中的应用前景.
硝酸甘油除了治疗心绞痛,还可以降低高血压,治疗充血性心力衰竭.因为硝酸甘油有扩张动脉血管、降低血压的作用,如果服用方法错误,可能会导致低血压、昏厥,严重还可能会危及生命. 1.不能多吃:硝酸甘油可以用于预防和治疗心绞痛,当疾病发生时,取出一片,大约0.5毫克,舌下含服,等1到2分钟,就可发挥药效,缓解疼痛.一般来说,药效可以保持30分钟.如果第一片服用后过了5分钟,没有起效,可以再服用一片,但是一定要牢记,最多三片,如果依然无效,必须立刻拨打120.
目的 以天山堇菜总黄酮含量为考察指标,研究大孔吸附树脂分离纯化天山堇菜总黄酮工艺.方法 以亚硝酸钠比色法检测天山堇菜中总黄酮含量,用大孔吸附树脂及柱层析法,考察总黄酮分离纯化的影响因素.结果 AB-8型大孔吸附树脂是纯化天山堇菜总黄酮的最佳大孔吸附树脂.最佳工艺参数为上柱液浓度0.0667mg·mL-1,洗脱剂为60%乙醇,最大上样体积为13BV,解吸液体积用量为10BV.结论 该方法操作简单,有效,可作为天山堇菜总黄酮纯化的工艺条件.
随着信息技术的广泛应用,慕课成为新的学习方式并得以快速发展.本文介绍药物分析慕课的制作及在教学过程中的应用,分析慕课发展现状,指出需要注意的问题,从而帮助高校教师更好地应用慕课,为教学服务.
目的 以天山堇菜总黄酮含量为考察指标,优化天山堇菜总黄酮提取工艺.方法 以亚硝酸钠比色法检测天山堇菜中黄酮含量,采取正交试验对影响因素进行优化,考察总黄酮的提取影响因素.结果 天山堇菜最佳提取工艺条件为料液比1:15,提取时间60min,乙醇浓度70%,提取温度90℃.结论 该方法准确,简便,可作为天山堇菜总黄酮提取工艺条件.
Objective To explore the hypoglycemic effects of Viola tianshanica Maxim.Methods Extraction conditions by orthogonal design research,in total flavonoids as index by reflux extraction for Viola tianshanica Maxim extracted.Established mouse model of diabetes with streptozotocin(STZ),reused Viola tianshanica Maxim extract for hypoglycemic experiment.The mice were divided into high dose group,middle dosage group,low dose group,blank control group,positive control group and normal mice group,15 mice in each group.The mice blood glucose and body weight of the different groups were observed.Results Viola tianshanica Maxim in a high concentration had significantly hypoglycemic effect in diabetic mice,average blood glucose level decreased from (18.4±5.8)mmol/L to (11.6±3.4)mmol/L,and the concentration of the extract could reduce the level of blood glucose in diabetic mice,average blood glucose level decreased from (24.8±5.6)mmol/L to (18.5±4.6)mmol/L,the differences were statistically significant(all P<0.05).Conclusion Viola tianshanica Maxim crude extract has a certain hypoglycemic effect.
采用响应面法优化超声波提取新疆天山堇菜中总黄酮的工艺条件.采用Box-Behnken中心组合设计及响应面法分析提取时间、 料液比、 乙醇浓度、 超声次数对天山堇菜中总黄酮的超声提取工艺的影响,筛选最佳条件.提取最优条件为超声70 min,液料比27:1,乙醇浓度为55%,超声次数为3次,总黄酮提取率预测值为6.27%.在最优条件下进行三次验证试验,总黄酮的平均得率为6.29%.响应面回归方程与试验结果拟合性好,可用于天山堇菜中总黄酮的提取工艺优化.
This study was designed to investigate the inhibitory effects of regorafenib (REG) on the catalytic activities of 12 kinds of human UGT isoforms and human liver microsomes (HLM) in vitro.The broader potential of REG to perpetrate drug-drug interactions (DDI) arising from UGT enzyme inhibition is predicted by in vitro-vivo extrapolation (IV-IVE).Fifty mixed HLM and 12 kinds of recombinant UGTs were utilized as enzyme sources to evaluation the inhibitory effects of REG against UGTs.4-Methylumbelliferone (4-MU)as a nonselective substrate of UGTs except for UGT1A4,N-(3-carboxypropyl)-4-hydroxy-l,8-napht-halimide (NCHN) and N-butyl-4-(4-hydroxyphenyl)-l,8-naphthalimide (NPHN) as the specific fluorescent substrate of UGT1A1,and trifluoperazine (TFP) as the specific substrate of UGT1A4.The half maximal inhibitory concentration (IC50) was calculated via the nonlinear regression analysis using Graphpad Prism 6.0,the inhibition kinetic types were selected and evaluated based on the intersection location of Lineweaver-Burk plot and Dixon plot,and Ki values were determined by the second plot of slopes.The potential DDI risk based on UGT1A1 inhibition was also evaluated through the in vitro parameters.The results demonstrated that REG displayed strong inhibitory effects against UGT1A1,1A7,1A9,and 2B7.The IC 50 values were from 0.15 to 6.6 μmol.L-1and Ki values from 0.027 to 14 μmol.L-1.The REG exerted competitive inhibition against UGT1A1-mediated 4-MU-O-glucuronidation and UGT1A1-mediated NPHN-O-glucuronidation,while the inhibition of NCHN-4-O-glucuronide by REG was suited to noncompetitive inhibition in both HLM and recombinant UGT1A1.Likewise,REG exhibited a mixed efficacy in inhibition of UGT1A7-,UGT1A9-,and UGT2B7-catalyzed 4-MU-O-glucuronidation.The AUC ratio of UGT1A1 specific substrates NPHN and NCHN can be increased by 101% to 302% and 13% to 109%,respectively.These results suggest that much caution should be exercised when REG is co-administered with UGT1A1 substrates.
目的 探讨新形势下药物分析课程的创新培养模式.方法 建立药物分析科技创新团队,引导学生参与科研,提高综合能力.结果 学生的科技创新能力得到提高,取得了较好成绩.结论 科技创新团队的建立是创新培养模式的体现.