Four new lignans from Schisandra sphenanthera

Three new 7,8-secolignans, schisandlignans A–C (1, 2, and 4), one new dibenzocyclooctadiene lignan, schisandlignan D (5), together with nine known lignans 3′,4′-dimethoxybenzoic acid (3″,4″-dimethoxyphenyl)-2-methyl-3-oxobutyl ester (3), gomisin J (6), rubrisandrin A(1b) (7), interiotherin B (8), schisantherin D (9), ( ? )-machilusin (10), ganschisandrine (11), henricine A (12), and (+)-1-hydroxy pinoresinol (13), were isolated from the rattan of Schisandra sphenanthera. Their structures were determined by analysis of 1D and 2D NMR spectroscopic data.     

A new highly oxygenated nortriterpenoid from Schisandra chinensis

A new highly oxygenated nortriterpenoid, 2β-hydroxy-micrandilactone C (1), and three related known triterpenoids (2–4) have been isolated from the leaves and stems of Schisandra chinensis. The structure of the new compound was elucidated by means of NMR and MS spectroscopic analyses.     

当归与五味子挥发油的超临界CO2萃取工艺

目的探讨当归与五味子及由二者组成的复方的超临界萃取工艺.方法应用超临界装置,用CO 2 萃取当归与五味子及其复方,以萃取油为考察目标,摸索不同工艺条件的影响规律.结果在萃取物粒径一定、CO 2 流量控制在5.0L·min -1 的条件下,提取率与萃取压力、温度和萃取物的组成密切相关.单味当归与五味子及复方的提取率随萃取压力升高而增大;随着萃取温度的增高,单味当归的提取率下降,而单味五味子的提取率增大.在相同的工艺条件下,其复方的提取率高于数学加权值.结论在超临界CO 2 萃取过程中,复方的提取率并不简单地等于单味提取率的数学加权值,组成也是影响提取率的重要因素.     

南五味子木脂素提取物清洁验证分析方法研究

目的 对南五味子木脂素提取物生产所用设备进行清洁验证分析方法研究.方法 采用HPLC法对南五味子木脂素提取物中主成分五味子酯甲和五味子甲素进行分析方法和取样方法研究.结果 五味子酯甲的检测限（LOD）为0.12 mg·L^-1,定量限（LOQ）为0.41 μg · L^-1,线性范围为203.5～ 5.09 mg·L^-1,取样回收率为77.8％;五味子甲素的检测限（LOD）为0.24 mg·L^-1,定量限（LOQ）为0.82 mg·L^-1,线性范围为209.66～ 5.24 mg·L^-1,取样回收率为80.9％.结论 五味子酯甲和五味子甲素的分析方法和取样方法有效可行.     

Effects of Schisandra sphenanthera extract on the pharmacokinetics of midazolam in healthy volunteers

AIMS

To assess the effect of Schisandra sphenanthera extract (SchE) on the pharmacokinetics of midazolam, a probe drug of CYP3A, and its metabolite 1′-hydroxy midazolam in healthy volunteers.

METHODS

Twelve healthy male volunteers were orally treated with SchE, three capsules twice daily for 7 days. Pharmacokinetic investigations of oral midazolam administration at 15 mg were performed both before and at the end of the SchE treatment period. The plasma midazolam and 1′-hydroxy midazolam concentrations were determined by high-performance liquid chromatography–tandem mass spectrometry. Estimated pharmacokinetic parameters before and with SchE were calculated with noncompartmental techniques.

RESULTS

Following administration of SchE, the average increases (%) of individual increases in AUC, AUMC and C_max of midazolam were 119.4% [95% confidence interval (CI) 83.9, 155.0], 183.4% (95% CI 120.5, 246.2) and 85.6% (95% CI 14.4, 156.9), respectively (P < 0.01 or 0.05). On average, there was a 133.3% (95% CI 8.9, 257.7) increase in midazolam t_max (P < 0.01). The average decrease (%) in CL/F was 52.1% (95% CI 44.9, 59.4) (P < 0.01). No significant changes were seen in midazolam half-life. After co-administration of SchE, the average increase (%) in t_max of 1′-hydroxy midazolam was 150.0% (95% CI 22.2, 277.8) (P < 0.05). No significant differences were observed in the other pharmacokinetic parameters of 1′-hydroxy midazolam.

CONCLUSIONS

SchE can markedly increase the oral bioavailability of midazolam in healthy volunteers. SchE is an inhibitor of CYP3A and has a high susceptibility to alter the disposition of drugs metabolized by CYP3A.     

华中五味子化学成分的研究

目的对传统中药华中五味子中的化学成分进行初步研究。方法运用多种色谱方法分离纯化,通过现代波谱解析技术(如NMR和MS等)和理化数据的文献对照,鉴定结构。结果与结论从华中五味子中分离得到了10个化合物,分别鉴定为五味子酚(schisanhenol,1)、五味子酯乙(schisantherin B,2)、chicanine(3)、pregomisin(4)和甘五酸(schizandronic acid,5)、去氧五味子素(6)、前戈米辛(7)、内消旋二氢愈创木脂素(8)、五味子酯甲(9)、戈米辛P顺芷酸酯(10)。首次从该植物中分离得到化合物前戈米辛(7)。     

Effects of Schisandra sphenanthera extract on the pharmacokinetics of tacrolimus in healthy volunteers

AIM: To assess the effect of Schisandra sphenanthera extract (SchE) on the pharmacokinetics of tacrolimus in healthy volunteers. METHODS: Twelve healthy male volunteers were orally treated with SchE, three capsules twice daily for 13 days. Pharmacokinetic investigations of oral tacrolimus administration at 2 mg were performed both before and at the end of the SchE treatment period. Whole blood tacrolimus concentrations were determined by enzyme-linked immunosorbent assay. Estimated pharmacokinetic parameters before and with SchE were calculated with noncompartmental techniques. RESULTS: Following administration of SchE, the average percentage increases of individual increases in AUC, AUMC and C(max) of tacrolimus were 164.2% [95% confidence interval (CI) 70.1, 258.4], 133.1% (95% CI 49.5, 261.3) and 227.1% (95% CI 155.8, 298.4), respectively (P < 0.01 or 0.05). On average, there was a 36.8% (95% CI 13.4, 60.2) increase in tacrolimus t(max) (P < 0.01). The average percentage decreases in CL/F and V/F were 49.0% (95% CI 31.1, 66.9) and 53.7% (95% CI 40.1, 67.4), respectively (P < 0.01). CONCLUSIONS: SchE can increase the oral bioavailability of tacrolimus. The results of this study will add important information to the interaction area between drugs and herbal products.     

南五味子对2型糖尿病大鼠肝脏保护作用的研究

目的研究南五味子对2型糖尿病大鼠肝脏保护作用。方法雄性SD大鼠40只,随机分10只大鼠为空白对照组,其余采用高脂高糖饲料加STZ联合诱导2型糖尿病大鼠模型,将成模大鼠按体重、血糖随机分为模型组,南五味子高(A1)、低剂量(A2)组(给药剂量分别为8 g·kg-1、5 g·kg-1)。给药30 d后检测2型糖尿病大鼠空腹血糖(FBG)、口服糖耐量(OGTT)、谷丙转氨酶(ALT)、谷草转氨酶(AST)、肝脏总抗氧化能力(T-AOC),并计算脏器指数。结果与模型组比较,给药组可以有效降低2型糖尿病大鼠FBG、OGTT、ALT、AST水平,提高T-AOC。结论南五味子能够改善2型糖尿病大鼠肝脏功能,对2型糖尿病造成的肝脏损害具有一定的保护作用。     

Chemical constituents from Schisandra plena

The chemical constituents of the leaves and stems of Schisandra plena are described for the first time. This investigation has resulted in the isolation of a new sesquiterpenoid, plenoxide (1). In addition, eleven known compounds, including sesquiterpenoids, coumarins, flavanones, triterpenoids and steroids have also been isolated. The structure and stereochemistry of 1 has been determined on the basis of spectroscopic analysis. Detailed analysis of 2D NMR data led to the conclusion that the chemical shifts of earlier compounds similar to bullatantriol need revision.     

Chemical constituents from Schisandra plena

The chemical constituents of the leaves and stems of Schisandra plena are described for the first time. This investigation has resulted in the isolation of a new sesquiterpenoid, plenoxide (1). In addition, eleven known compounds, including sesquiterpenoids, coumarins, flavanones, triterpenoids and steroids have also been isolated. The structure and stereochemistry of 1 has been determined on the basis of spectroscopic analysis. Detailed analysis of 2D NMR data led to the conclusion that the chemical shifts of earlier compounds similar to bullatantriol need revision.     

南、北五味子药材的HPLC指纹图谱建立及化学模式识别分析

目的:建立南、北五味子药材的高效液相色谱(HPLC)指纹图谱,并进行化学模式识别分析。方法:采用HPLC法,以五味子甲素为参照,绘制南、北五味子各10批样品(编号分别为N1～N10、S1～S10)的HPLC指纹图谱;采用《中药色谱指纹图谱相似度评价系统(2012版)》进行相似度评价,确定共有峰;采用SPSS 20.0和SIMCA 14.1软件进行聚类分析(HCA)、无监督模式主成分分析(PCA)、有监督模式正交偏最小二乘法-判别分析(OPLS-DA);以变量重要性投影值(VIP)大于1为标准,筛选影响南、北五味子质量的差异标志物。结果:南、北五味子分别指认出32、33个共有峰;10批南五味子和10批北五味子的相似度均大于0.9,南、北五味子的相似度为0.50;南、北五味子共有19个共有特征峰,共指认出其中的5个,即五味子醇甲、五味子醇乙、五味子酯甲、五味子甲素、五味子乙素。HCA结果显示,N1～N10聚为一类,S1～S10聚为一类,其中N1、N3、N8、N9聚为一类,其余聚为一类;S1、S3、S6、S9聚为一类,其余聚为一类。无监督模式PCA结果显示,前2个主成分因子的累积方差贡献率为...     

超高效液相色谱法同时测定南、北五味子中的7种木脂素含量

目的：建立UPLC测定五味子中7种木脂素的方法,并测定不同地区的南、北五味子中木脂素成分含量。方法：色谱柱ZORBAX Eclipse Plus C₁₈ column （1.8 μm,100 mm×2.1 mm）;流动相乙腈-水,梯度洗脱;流速0.3 mL·min^-1;柱温40℃;检测波长220 nm;进样体积1 μL。结果：各成分即五味子醇甲、五味子醇乙、五味子酯甲、五味子酯乙、五味子甲素、五味子乙素、五味子丙素之间基本达到基线分离,且线性关系良好,线性范围分别为0.984~246.000,0.636~159.000,0.552~138.000,0.472~1.180,0.952~2.380,1.120~2.810,0.436~1.090 μg·mL^-1（r>0.999 6）。平均加样回收率在98.29%~102.5%之间,RSD在1.4%~1.9%之间。结论：所建立的测定方法快速、稳定、可靠,适用于不同产地南、北五味子中木脂素含量的测定。     

不同产地南五味子红外指纹图谱鉴别

目的:建立南五味子药材红外指纹图谱的鉴定分析新方法。方法:对不同产地南五味子药材进行红外光谱指纹图谱鉴别,并进行相似度计算与分析。结果:获得了6种不同产地南五味子药材的红外指纹图谱。结论:粉末的红外指纹图谱鉴定法可用于不同产地南五味子药材的鉴定和识别,相似度的计算结果进一步证明了方法的可行性。     

南五味子软胶囊对大鼠长期毒性的实验研究

目的观察南五味子软胶囊连续灌胃给药13周对大鼠产生的毒性反应。方法南五味子软胶囊分别以1.2、0.438、0.16g.kg-1.d-1灌胃给药,每周给药6 d,试验周期为13周,各试验组剩余的1/2动物观察4周恢复期变化。按中药新药长期毒性试验要求观察动物的一般状况、体重变化、血液细胞学及生化学指征、解剖及组织病理学检查。结果各剂量药组与对照组大鼠比较,白天自发活动减少,高剂量组减少最为明显,但夜间活动无明显差异。血液及生化指标与对照组相比无明显差异,脏器未出现给药相关的病变。结论南五味子软胶囊长期灌胃服用未见毒性反应,长期服用安全。     

Highly oxygenated triterpenoids from the roots of Schisandra chinensis and their anti-inflammatory activities

A new highly oxygenated triterpenoid, schinchinenlactone D (1), and three known compounds (2–4) were isolated from the roots of Schisandra chinensis. Their structures were determined by combining the spectroscopic analysis with the theoretical computations. The anti-inflammatory activities of compounds 1–4 were evaluated, and compound 3 exhibits the most significant activity in the inhibition of NO production with an IC₅₀ value of 10.6 μM.     

Heteroclitin H,a new lignan from Kadsura heteroclita

A new dibenzocyclooctadiene lignan, heteroclitin H (1), was isolated together with seven known compounds, heteroclitin D (2), interiorin B (3), interiorin (4), neokasuranin (5), interiotherin C (6), gomisin J (7) and (+)-anwulignan (8), from the stems of Kadsura heteroclita. Their structures were elucidated by spectroscopic methods. This is the first report of the isolation of compounds 3, 5, 6, 7 and 8 from K. heteroclita.     

Heteroclitin H, a new lignan from Kadsura heteroclita

A new dibenzocyclooctadiene lignan, heteroclitin H (1), was isolated together with seven known compounds, heteroclitin D (2), interiorin B (3), interiorin (4), neokasuranin (5), interiotherin C (6), gomisin J (7) and (+)-anwulignan (8), from the stems of Kadsura heteroclita. Their structures were elucidated by spectroscopic methods. This is the first report of the isolation of compounds 3, 5, 6, 7 and 8 from K. heteroclita.     

南北五味子及其制剂与其他药物相互作用的研究进展

五味子为木兰科植物五味子（北五味子）及华中五味子（南五味子）的干燥成熟果实,其制剂已被广泛应用于临床。本文综合了近些年国内外相关文献,对南北五味子作用机制进行归纳总结,对南北五味子与其他药物的相互作用以及其相关制剂的联合用药进行了概述,从而为临床安全用药提供参考。     

Dibenzocyclooctadiene lignans from Schisandra neglecta and their anti-HIV-1 activities

Two new dibenzocyclooctadiene lignans, schinegllignans A and B (1 and 2), together with 11 known (3–13) were isolated from the fruit of Schisandra neglecta. Their structures and stereochemistries were elucidated by spectroscopic methods, including 1D, 2D NMR, and HR-ESI-MS techniques. Compounds 1 and 2 were evaluated for their anti-HIV activities, and they showed moderate anti-HIV-1 activities with therapeutic index values of 18.5 and 24.6.     

Schisandrone, a New 4-Aryltetralone Lignan from Schisandra sphenanthera.

A new 4-aryltetralone lignan, named schisandrone was isolated from the dried fruits of SCHISANDRA SPHENANTHERA, collected in Gansu province. The chemical structure and absolute configuration was elucidated on the basis of chemical and spectral analysis.