丹参与三七对四氯化碳致大鼠急性肝损伤的保护作用

目的　观察丹参与三七配伍对四氯化碳 (CCl4 )化学性急性肝损伤的保护作用。方法　建立CCl4 致大鼠急性肝损伤模型 ,设丹参与三七配伍大、中、小剂量组和正常对照组及模型对照组 ,通过测定各组动物血清谷丙转氨酶 (ALT)、山梨醇脱氢酶(SDH)活性及肝糖原、肝脏系数和观察肝脏组织病理学变化 ,以评价肝脏损伤程度和药物的保护作用。结果　丹参与三七配伍治疗后 ,各剂量组大鼠血清ALT、SDH活性及肝脏系数均降低 (P <0 .0 1) ,肝糖原合成增加 (P <0 .0 1) ,肝脏组织病理损伤得到明显改善 ,且呈明显的量效关系。结论　丹参与三七配伍对损伤肝组织的修复 ,肝细胞再生显示良好的治疗作用     

Compound injection of Radix Hedysari to promote peripheral nerve regeneration in rats

OBJECTIVE: To study the effect of compound injection of Radix Hedysari on peripheral nerve regeneration in rats. METHODS: Seventy-five healthy adult SD male rats, weighing 150 g, were randomized into 5 groups (15 rats in each group). The bilateral sciatic nerves of the rats were exposed and clamped with a smooth clamp to make an injury area of 2 mm. After clamp operation Group 1 was injected with compound injection of radix Hedysari (CIRH) 1.5 ml/day, Group 2 with CIRH 1.0 ml/day, Group 3 with CIRH 0.5 ml/day, Group 4 with nerve growth factor (NGF) 50 U/day, and Group 5 was taken as the control group without any management. The bilateral sciatic nerve was taken out at 3 days, 1, 2 and 4 weeks after clamping, stained with osmic acid and observed microscopically. The myelinated nerve fibers were counted. The nerve conduction velocity was determined 2 and and 4 weeks before sample taking the sciatic nerve function index was measured 4 weeks before sample taking. RESULTS: The results of nerve conduction velocity, the myelinated nerve fiber count and the sciatic functuion index in the CIRH treated groups were better than those in the control group. The results of the nerve conduction velocity and the myelinated nerve fiber count at 2 weeks and the nerve conduction velocity at 4 weeks in Group 1 were better than those of Group 4. Biological observation showed that degenerated and necrotic myelin sheath in CIRH treated Groups at 2 and 4 weeks decreased remarkably compared to the NGF treated group. CONCLUSIONS: CIRH can promote regeneration of peripheral nerves and absorption of degenerated and necrotic injured nerves. It has the same effect as NGF.     

5种中药抑菌效果的测定

黄连、黄芩、大黄提取液对奇异变形杆菌、表皮葡萄球菌、大肠杆菌、绿脓杆菌与金黄色葡萄球菌的抑菌作用多强于黄柏、苦参提取液者。其水煎浓缩液经乙醇提取处理后，所剩物质的抑菌作用减弱。黄连、黄芩、大黄水煎液最小抑菌浓度，随药液ｐＨ升高而增大。     

Paeoniae Radix,a traditional Chinese medicine,and CYP2C9 activity

Paeoniae Radix (PR) is a commonly used traditional Chinese medicine. A slight effect of PR on the pharmacokinetics of phenytoin that is mainly metabolised by CYP2C9 has been reported. The aim of this pilot study was to clarify if PR has an effect on losartan oxidation used as a measure of CYP2C9 activity. Three healthy volunteers received a single oral dose of losartan before and after PR treatment. Losartan and E-3174, an active metabolite of losartan, were analysed in 8 hour urine. PR did not seem to have an effect on CYP2C9 activity when the losartan/E-3174 ratios were compared before and after PR treatment (P = 0.56) although a larger study would need to be undertaken to confirm this finding.     

赤芍、大黄药对提取物中丹皮酚和大黄酸的组织分布研究

目的:建立同时测定大鼠组织中丹皮酚和大黄酸含量的高效液相色谱法。方法:采用Phenomsil BDS C18(4.6 mm×250 mm,5μm),以乙腈-0.1%磷酸(37∶63)为流动相,流速1.0 m L·min-1,以橙黄决明素为内标,在274 nm下进行检测。结果:丹皮酚的线性范围为Y=-0.055+0.03X(r=0.993 2),日内和日间的RSD均4.1%;大黄酸的线性范围为Y=-0.152+0.014X(r=0.993 5),日内和日间的RSD均4.9%。组织样品的稳定性符合要求。结论:所建立的大鼠组织中丹皮酚和大黄酸HPLC测定方法,适用于大鼠体内赤芍、大黄药对的组织分布研究。     

Comprehensive two-dimensional APTES-decorated MCF7-cell membrane chromatographic system for characterizing potential anti-breast-cancer components from Yuanhu–Baizhi herbal medicine pair

Rhizoma corydalis and Radix Angelicae Dahurica (Yuanhu–Baizhi) herbal medicine pair has been used for thousands of years and has been reported to be potentially active in recent cancer therapy. But the exact active components or fractions remain unclear. In this study, a new comprehensive two-dimensional (2D) 3-aminopropyltriethoxysilane (APTES)-decorated MCF7-cell membrane chromatography (CMC)/capcell-C18 column/time-of-flight mass spectrometry system was established for screening potential active components and clarifying the active fraction of Yuanhu–Baizhi pair. APTES was modified on the surface of silica, which can provide an amino group to covalently link cell membrane fragments with the help of glutaraldehyde in order to improve the stability and column life span of the MCF7 CMC column. The comprehensive 2D MCF7-CMC system showed good separation and identification abilities. Our screen results showed that the retention components are mainly from the alkaloids in Yuanhu (12 compounds) and the coumarins (10 compounds) in Baizhi, revealing the active fractions of Yuanhu–Baizhi herbal medicine pair. Oxoglaucine, protopine, berberine, osthole, isopimpinellin and palmitic acid were selected as typical components to test the effects on cell proliferation and their IC₅₀ were calculated as 38.17 μM, 29.45 μM, 45.42 μM, 132.7 μM, 156.8 μM and 90.5 μM respectively. Cell apoptosis assay showed that the drug efficacy was obtained mainly through inducing cell apoptosis. Furthermore, a synergistic assay results demonstrated that oxoglaucine (representative of alkaloids from Yuanhu) and isopimpinellin (representative of coumarins from Baizhi) showed significant synergistic efficacy with GFT, indicating that these components may act on other membrane receptors. The proposed 2D CMC system could also be equipped with other cells for further applications. Besides, the follow-up in-vitro experimental strategy using cell proliferation assay, cell apoptosis assay and synergistic assay proved to be a practical way to confirm the active fractions of herbal medicine.     

HPLC同时测定麦冬中5个皂苷成分的含量

建立测定麦冬药材中麦冬皂苷D,麦冬皂苷D', ophiopojaponin C,去乙酰基ophiopojaponin A, 3-O-α-L-鼠李糖-(1→2)-β-葡萄糖麦冬苷元5种成分的HPLC方法。采用HPLC-ELSD方法,色谱柱为Kromasil 100-5C₁₈柱(4.6 mm×250 mm,5μm);流动相为乙腈(A)-水(B)溶液,梯度洗脱0~45 min,35%~55%A,体积流量1.0 mL·min^-1;柱温35℃,漂移管温度100℃,气体流速3.0 L·min^-1;进样量15μL。结果表明5种成分均达到基线分离,各成分均有较宽的线性范围和良好的线性关系(r>0.999);回收率在95.75%~103.1%。建立的麦冬皂苷含量测定方法准确灵敏、重复性好,可应用于麦冬药材质量评价中。     

不同品种及采收期党参药材中5种有效成分含量的比较研究

目的:建立同时测定党参药材中党参炔苷、丁香苷、苍术内酯Ⅰ、苍术内酯Ⅱ和苍术内酯Ⅲ含量的方法,并比较不同品种及采收期党参药材中上述5种成分的含量。方法:采用高效液相色谱法(HPLC)。色谱柱为Inertsil ODS-3,流动相为乙腈-水(梯度洗脱),检测波长为210 nm(党参炔苷)、220 nm(苍术内酯Ⅱ、苍术内酯Ⅲ、丁香苷)、276 nm(苍术内酯Ⅰ),流速为0.8 mL/min,柱温为30℃,进样量为20μL。结果:党参炔苷、丁香苷、苍术内酯Ⅰ、苍术内酯Ⅱ和苍术内酯Ⅲ检测质量浓度的线性范围为44.30～886.00μg/m L(r=0.999 7)、6.50～130.03μg/mL(r=0.999 6)、4.47～89.46μg/mL(r=0.999 5)、2.53～50.50μg/mL(r=0.999 4)、5.64～112.80μg/mL(r=0.999 5);定量限分别为2.446 0、0.168 0、0.248 1、0.065 7、0.099 8μg/mL,检测限分别为1.352 0、0.067 2、0.005 4、0.006 3、0.007 3μg/mL;精密度、稳定...     

Effect of microwave vacuum drying on the drying characteristics,color, microstructure,and antioxidant activity of green coffee beans

通过开展前胡切片微波真空干燥特性分析与模拟研究 ,探索前胡切片在微波真空干燥过程的水分及其成分变化规律,以期有效提高前胡切片的干燥效率和饮片品质。

进行不同干燥条件(微波功率密度、真空度和切片厚度)的前胡切片微波真空干燥实验,研究干燥过程的水分比和干燥速率变化情况,运用HPLC测定干燥后的前胡切片3个香豆素类成分(白花前胡甲素、白花前胡乙素和白花前胡素E)含量,并采用Weibull函数对干燥过程的水分比曲线进行模拟与分析。

前胡切片微波真空干燥过程存在加速、恒速和减速3个阶段。与真空度和切片厚度相比,通过提高微波功率密度可以更有效地缩短干燥时间、提高干燥效率。在实验参数范围内,较优干燥条件组合为微波功率密度3.0 W·g^–1,真空度800 Pa,切片厚度2 mm。所有干燥条件的变化对干燥后的前胡切片香豆素类成分含量影响均不显著。Weibull函数模拟与分析结果表明：不同干燥条件下的尺度参数为17.43~45.38,其值越小干燥时间越短,形状参数为1.41~1.77,均>1,表明干燥过程由内外部水分扩散共同控制。

研究工作既为前胡切片微波真空干燥的工艺改进和质量控制提供了重要的理论依据和技术支持,还将为前胡切片干燥的规范化和品质特征的形成提供重要参考。

     

Type-2 diabetes mellitus and cardiovascular disease

基于系统药理学、生物信息学、分子对接及体内外实验探讨草乌影响2型糖尿病(diabetes mellitus type 2,T2DM)的潜力及对T2DM相关症状的潜在机制。

利用数据库检索草乌相关化学成分、预测潜在作用靶点以及干预相关疾病;GEO数据库检索T2DM相对健康人的差异基因,与草乌作用靶点映射后置于DAVID数据库进行生物功能富集,利用单因素方差分析、二元Logistic回归分析及ROC曲线分析目标基因对于T2DM的敏感性。借助分子对接技术分析草乌化学成分与靶蛋白的结合位置及相互作用力。通过体内外T2DM模型验证草乌及其化学成分对目标蛋白表达的影响。

通过数据库检索与分析得到草乌干预靶点相关疾病304种(P<0.05,FDR<0.05),选取度值最高的T2DM(Degree=59)进行分析。T2DM相对健康人差异基因与草乌潜在作用靶点取交集得到43个目标基因,进行单因素方差分析得到有显著性差异的基因共9个,二元Logistic回归分析得到5个有意义基因,ROC曲线下面积AUC>0.5的基因共3个。分子对接得到草乌化学成分异波尔定碱[(+)-Isoboldine]与蛋白APEX1、CASP1、CBFB,欧乌头碱(Napelline)与蛋白CBX1、EHMT2结合,通过氢键相互作用、疏水相互作用、可电离性和静电相互作用等不同作用力结合,从而增加配体靶向作用蛋白的能力。T2DM大鼠经草乌水提物治疗2周后,草乌可能通过改善周围神经病变进而缓解T2DM症状。并且草乌可以影响大鼠肝组织中APEX1、CASP1、CBFB、CBX1、EHMT2的蛋白表达。草乌中(+)-Isoboldine和Napelline化学成分对体外模型的目标蛋白的影响与体内实验一致。

本研究初步揭示草乌可作为改善T2DM周围神经病变的潜在治疗药物,为中蒙药研发以及挖掘治疗T2DM新靶标药物奠定理论基础。