气相-质谱联用分析冠心苏合丸中的挥发性组分

 采用气相 质谱联用对冠心苏合丸及药材中的挥发性成分进行了分析。采用选择离子监测法 ,以水杨酸甲酯为内标 ,对冠心苏合丸中的两个指标成分冰片和苯甲酸苄酯进行了定量测定。冰片和苯甲酸苄酯的平均加标回收率分别为 91 7%和 89 7% ,RSD分别为 5 6 %和 2 3%。     

In vivo microdialysis with ultra performance liquid chromatography–mass spectrometry for analysis of tetramethylpyrazine and its interaction with borneol in rat brain and blood

Tetramethylpyrazine (TMP) has been widely used in the treatment of ischemic cerebrovascular disease. However, the mechanism of TMP and how to increase its bioavailability need to be further explored. In our study, an in vivo microdialysis sampling technique coupled with ultra‐performance liquid chromatography–mass spectrometry method was developed to investigate the pharmacokinetic properties of TMP and its interaction with different doses of borneol (BO) in rats. Linearity of TMP in brain and blood dialysates exhibited good linear relationships over the concentration range of 0.991–555.14 ng/mL. The specificity, linearity, accuracy, precision, matrix effect and stability were within acceptable ranges. The results demonstrated that BO had a marked impact on the pharmacokinetic properties of TMP. After co‐administration, the areas under the concentration–time curve (AUC) of TMP in brain and blood were significantly increased. Meanwhile, the peak concentration of TMP in brain was also enhanced. The AUC_Brain/AUC_Blood of TMP, increased from 44% to 56 and 60.8% after co‐administration with BO (15 and 30 mg/kg). The pharmacodynamic results showed that TMP co‐administration with BO enhanced the cerebral blood flow during the period of ischemia and reduced the infarct volume. Overall, it might be an effective way to treat stroke to use TMP co‐administered with BO.     

The effectiveness of borneol on pharmacokinetics changes of four ginsenosides in Shexiang Baoxin Pill in vivo

Shexiang Baoxin Pill (SBP) is a traditional Chinese medicine, widely used for cardiovascular diseases in the clinic. Ginsenosides are important effective components in SBP, but their pharmacokinetic characteristics are still not known. In this paper, we studied the pharmacokinetics of ginsenoside Rb1, Rc, Re and Rg1 in SBP and investigated the effect of borneol on the pharmacokinetic characteristic of ginsenosides based on an Agilent G6410A triple quadrupole LC/MS system. Results showed that the pharmacokinetic parameters of ginsenoside Rb1, Rc, Re and Rg1 in rat plasma after oral administration of SBP are significantly different with oral administration of SBP without Borneolum Syntheticum. Plasma pharmacokinetic profiles after oral administration of ginsenoside Rb1, Rc, Re, Rg1 and co‐administration with borneol at three different ratios (10:1, 1:1 and 1:10 ginsenoside vs borneol, w/w) were also determined. It was demonstrated that borneol can elevate the plasma concentration of ginsenosides after co‐admininstration. Copyright © 2013 John Wiley & Sons, Ltd.     

3,5-二硝基苯甲酸冰片酯的合成及结构表征

冰片在中药中被广泛应用。利用前药原理,对冰片母体进行修饰,以冰片和3,5-二硝基苯甲酸为原料,以对甲苯磺酸为催化剂,合成了3,5-二硝基苯甲酸冰片酯,目标化合物的结构经FT-IR、13C NMR、1H NMR和元素分析加以确证。该化合物具有一定的研究开发价值。     

Oxidation of secondary terpene alcohols by chlorine dioxide

Secondary terpene alcohols cis- and trans-verbenol, neo-iso-verbanol, borneol, iso-borneol, and menthol were oxidized by chlorine dioxide into the corresponding ketones. It was shown that the nature of the solvent and catalyst and the structure of the starting compound, including the stereochemistry of the hydroxyl, influenced the oxidation process. Translated from Khimiya Prirodnykh Soedinenii, No. 6, pp. 585–587, November–December, 2008.     

Comparative essential oil composition of aerial parts of Tanacetum dumosum Boiss. from Southern Zagros,Iran.

The essential oils of leaves and flowers of Tanacetum dumosum Boiss., an endemic medicinal shrub, were extracted by using hydrodistillation method and analysed using GC and GC–MS. A total of 43 and 44 compounds were identified in the essential oils from the leaves and flowers of T. dumosum, respectively. The major chemical constituents of leaves oil were borneol (27.9%), bornyl acetate (18.4%), 1,8-cineol (17.5%), α-terpineol (5.3%), cis-chrysanthenyl acetate (3.3%), camphene (2.7%) and terpinene-4-ol (1.9%), while the main components of the flower oil were isobornyl-2-methyl butanoate (41.1%), trans-linalyl oxide acetate (11.9%), 1,8-cineole (7.7%), thymol (4.2%), linalool (3.9%), camphor (2.9%), isobornyl propanoate (2.9%), α-terpineol (2.1%) and caryophyllene oxide (2.0%). Major qualitative and quantitative variations for some main chemical compounds among different aerial parts of T. dumosum were identified. High contents of borneol, bornyl acetate, 1,8-cineol and linalool in the leaves and flowers of T. dumosum show its potential for use in the food and perfumery industry.     

Synthesis and crystal structure of a novel chiral compound prepared from (-)-borneol as a natural chiral auxiliary

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硼酸酯化法分离龙脑、异龙脑与樟脑

用硼酸与异龙脑的异构化产物—龙脑、异龙脑和樟脑的混合物进行反应，得到硼酸莰酯和樟脑。莰酯与樟脑分离后，经水解得到龙脑和异龙脑。     

GC–MS/MS method for the determination and pharmacokinetic analysis of borneol and muscone in rat after the intravenous administration of Xingnaojing injection

A simple and sensitive gas chromatography with tandem mass spectrometry method was developed and validated for the simultaneous determination of borneol and muscone in rat plasma. The analytes and internal standard, naphthalene, were extracted using a convenient one‐step liquid–liquid extraction method with ethyl acetate. The chromatographic separation was realized on a HP‐5MS capillary column and detected in multiple reaction monitoring mode. Excellent linearity (R ² ≥ 0.996) was shown over 10.0–5000 ng/mL for borneol and 2.5–250 ng/mL for muscone. The lower limit of quantitation was 10 and 2.5 ng/mL for borneol and muscone, respectively. The intra‐ and interday precisions were less than 7.52%, and the accuracy values were between  −8.03 and 14.52%. The extraction recovery, matrix effect, and stability were sufficient to meet the Food and Drug Administration criteria. Meanwhile, the assay was successfully applied to the preclinical pharmacokinetic study of borneol and muscone following intravenous administration of Xingnaojing injection, a modern Chinese herbal medicine preparation.