盐酸小檗碱-环糊精包合物的体外溶出度研究

目的探讨包合技术对中药制剂体外溶出度以及缓释作用的影响。方法选用饱和溶液法生成包合物 ,用DSC证明包合物的生成 ;采用分光光度法 ,考察盐酸小檗碱包合物的体外溶出度和缓释作用。结果 β CD·BH、RM β CD·BH和BH的T50 、Td分别为 5 69.8,740 .2min ;73 .7,10 7.0min和 19.6,2 5 .5min ,包合物的释药数据与t作线性回归方程为 :Y =0 .0 63 9t -0 .473 8,Y =0 .5 5 64t+5 .65 8。结论RM β CD·BH和 β CD·BH的溶出速率明显慢于BH ,具有一定的缓释作用 ,同时RM β CD·BH较β CD·BH具有更好的生物利用度 ;β CD·BH和β CD·BH的体外溶出度与t为一相关性良好的线性方程 ,符合零级释药方程。     

反相胶束增稳室温荧光法测定痕量中药有效成分盐酸小檗碱的研究——兔血浆中痕量盐酸小檗碱的测定

研究了双［２－乙基己基］－磺酸基琥珀酸／环己烷／水（ＡＯＴ／Ｃ６Ｈ１２／Ｈ２Ｏ）反相胶束介质中中药有效成分盐酸小檗碱的荧光性质．并将该法应用于兔血浆中痕量盐酸小檗碱的测定，绘制了药时曲线．该法的线性范围（ｇ／ｍＬ）为：６．０×１０－８～６．０×１０－５，检出限（ｇ／ｍＬ）为：７．２×１０－８，相对标准偏差（％）为：１．１     

Binding Properties of RNA Quadruplex of SARS-CoV-2 to Berberine Compared to Telomeric DNA Quadruplex

Previous studies suggest that berberine, an isoquinoline alkaloid, has antiviral potential and is a possible therapeutic candidate against SARS-CoV-2. The molecular underpinnings of its action are still unknown. Potential targets include quadruplexes (G4Q) in the viral genome as they play a key role in modulating the biological activity of viruses. While several DNA-G4Q structures and their binding properties have been elucidated, RNA-G4Qs such as RG-1 of the N-gene of SARS-CoV-2 are less explored. Using biophysical techniques, the berberine binding thermodynamics and the associated conformational and hydration changes of RG-1 could be characterized and compared with human telomeric DNA-G4Q 22AG. Berberine can interact with both quadruplexes. Substantial changes were observed in the interaction of berberine with 22AG and RG-1, which adopt different topologies that can also change upon ligand binding. The strength of interaction and the thermodynamic signatures were found to dependent not only on the initial conformation of the quadruplex, but also on the type of salt present in solution. Since berberine has shown promise as a G-quadruplex stabilizer that can modulate viral gene expression, this study may also contribute to the development of optimized ligands that can discriminate between binding to DNA and RNA G-quadruplexes.     

黄连素对2型糖尿病大鼠血清、肾脏的保护作用

目的:观察黄连素对实验性2型糖尿病大鼠血清、肾脏中羟自由基(.OH)能力的影响。方法:采用小剂量链脲佐菌素加高糖高脂饲料喂养的方法建立Wistar大鼠2型糖尿病模型,成模后给予黄连素0.1g/(kg.d)灌胃治疗8周,检测血清、肾脏羟自由基能力的变化。结果:与糖尿病组相比,黄连素组肾脏、血清中羟自由基能力下降,各观察值均与糖尿病组存在显著性差异(P<0.05)。结论:黄连素可保护大鼠的血清和肾脏,降低羟自由基能力,减少自由基对机体细胞的损伤。     

生物酶法黄檗小檗碱染料提取及其染色性能

为了提高黄檗小檗碱染料的提取率,利用纤维素酶酶解黄檗中的纤维素,降低色素从细胞中被萃取出来的阻力,提高黄檗染料的提取率,加快提取速率。通过单因素分析探讨了提取温度、提取时间、pH值以及浓度对黄檗小檗碱色素提取率的影响,确定了利用纤维素酶提取黄檗中小檗碱染料的最佳提取工艺;同时对棉织物进行染色处理,对其染样进行了耐摩擦牢度和水洗牢度的测试。实验结果表明,纤维素酶受温度、pH值、浓度的影响较大,且生物酶法与传统水浸煎煮法相比,其染料萃取率可提高21%~23%。最佳工艺条件为:提取温度50℃,提取时间为60 min,提取介质pH=4.5,纤维素酶与黄檗的配料比为1∶100。     

Pharmacokinetic Comparison of Berberine in Rat Plasma after Oral Administration of Berberine Hydrochloride in Normal and Post Inflammation Irritable Bowel Syndrome Rats

In the present study, post inflammation irritable bowel syndrome (PI-IBS) rats were firstly established by intracolonic instillation of acetic acid with restraint stress. Then the pharmacokinetics of berberine in the rat plasma were compared after oral administration of berberine hydrochloride (25 mg/kg) to normal rats and PI-IBS rats. Quantification of berberine in the rat plasma was achieved by using a sensitive and rapid UPLC-MS/MS method. Plasma samples were collected at 15 different points in time and the pharmacokinetic parameters were analyzed by WinNonlin software. Compared with the normal group, area under the plasma concentration vs. time curve from zero to last sampling time (AUC_0–t) and total body clearance (CL/F) in the model group significantly increased or decreased, (2039.49 ± 492.24 vs. 2763.43 ± 203.14; 4999.34 ± 1198.79 vs. 3270.57 ± 58.32) respectively. The results indicated that the pharmacokinetic process of berberine could be altered in PI-IBS pathological conditions.     

正交实验法优选黄连中盐酸小檗碱醇提工艺的研究

用乙醇提取黄连中盐酸小檗碱,采用正交实验法优化工艺条件.结果表明,优选的醇提工艺条件为：50％乙醇提取3次,每次提取时间1.5h,3次加醇量分别8,6,6倍.该醇提工艺重现性和稳定性良好.     

Diabetes Mellitus and Cardiovascular Diseases: Nutraceutical Interventions Related to Caloric Restriction

Type 2 diabetes (T2DM) and cardiovascular disease (CVD) are closely associated and represent a key public health problem worldwide. An excess of adipose tissue, NAFLD, and gut dysbiosis establish a vicious circle that leads to chronic inflammation and oxidative stress. Caloric restriction (CR) is the most promising nutritional approach capable of improving cardiometabolic health. However, adherence to CR represents a barrier to patients and is the primary cause of therapeutic failure. To overcome this problem, many different nutraceutical strategies have been designed. Based on several data that have shown that CR action is mediated by AMPK/SIRT1 activation, several nutraceutical compounds capable of activating AMPK/SIRT1 signaling have been identified. In this review, we summarize recent data on the possible role of berberine, resveratrol, quercetin, and L-carnitine as CR-related nutrients. Additionally, we discuss the limitations related to the use of these nutrients in the management of T2DM and CVD.     

小檗碱对局灶性脑缺血大鼠原癌基因c-fos 表达的影响

目的 研究大鼠局灶性脑缺血过程中c-fos mRNA 表达的动态变化, 并观察小檗碱(Ber)对其作用。方法 运用斑点杂交技术, 观察Ber 对局灶性脑缺血再灌注大鼠大脑皮质及海马组织c-fos mRNA 表达的影响。结果 大鼠局灶性脑缺血2 h 再灌注0.5～4 h, 脑皮质及海马组织c-fos mRNA 出现一过性高表达, 2 h 达高峰, 分别为对照组的4.5 和4.7 倍。Ber 20 mg/(kg·d)ip 显著抑制大鼠脑缺血诱导的c-fos 高表达, 降低病灶侧海马和皮层组织水、钙含量。结论 脑缺血过程中c-fos 原癌基因呈现一过性高表达, Ber 可降低c-fos mRNA 水平, 该作用可能是其抗脑缺血机理之一。     

黄连素提取工艺研究

分别介绍了以黄连、黄柏、三棵针3种中草药提取黄连素的具体工艺流程,给出了多种的不同的传统提取工艺和技术参数;进一步介绍了液膜法,微波萃取和超声波萃取的新技术在黄连素提取中的工艺研究,给出了相应的工艺流程。