ABSTRACT
Objective To identify the chemical constituents of volatile oil from the Chinese traditional medicine coastal glehnia root and to compare the differences between coastal glehnia root of different locations. Methods A total of 16 batches of the coastal glehnia root were collected from several major production areas from September 2012 to March 2013, and then they were ground into powder. The volatile oil was extracted from the powder samples using the methods described in Chinese Pharmacopoeia Appendix. Gas chromatography-mass spectometry (GC-MS) was used to get the spectra of volatile oil of each sample and NIST 11. 0 database was used to identify the chemical constituents of coastal glehnia root. Results and Conclusion From 16 batches of 48 coastal glehnia root volatile oil samples, we identified 12 common components. The 12 common chemical constituents can serve as the characteristic composition of volatile oil of the coastal glehnia root, and falcarinol is the major main chemical constituent. The three batches collected from Hebei province had fewer chemical components and lower contents. We also found that the coastal glehnia root samples with root bark had more volatile oil components and higher contents than the samples without bark; moreover, eicosapentaenoic acid was only found in the samples with root bark. Peeling the bark may reduce the contents of some volatile oils such as eicosapentaenoic acid, which may affect the medicinal activity of the coastal glehnia root.
ABSTRACT
O plasma da serpente Bothrops jararaca é rico em inibidores de proteases, alguns dos quais com atividade inibitória sobre toxinas presentes no veneno de serpentes da mesma espécie. Um desses inibidores apresenta massa molecular de 110 kDa, é um potente inibidor de cisteíno-peptidase e libera um peptídeo que induz contração de musculatura lisa homóloga. Por estas características, essa proteína, denominada BjHK (Bothrops jararaca High Molecular Weight Kininogen), foi correlacionada ao cininogênio de alta massa molecular de mamíferos. Além dessas propriedades, verificou-se que essa proteína inibe metaloproteases presentes no veneno de B. jararaca. Esse efeito também foi observado no cininogênio de alta massa molecular humano e correlacionado a porções do domínio 5 dessa proteína. O objetivo do presente projeto é procurar possíveis homologias entre a BjHK e o cininogênio humano, além de possíveis atividades inibitórias sobre agregação plaquetária e adesão celular, atividades estas também descritas no cininogênio de alta massa molecular humano...
The Bothrops jararaca snake plasma is rich in protease inhibitors, some of which have inhibitory activity on toxins from its own venom. One of these, which has a molecular mass of 110 kDa, is a potent inhibitor of cysteine-peptidase and releases a peptide that induces contraction of homologous smooth musculature. For these characteristics this protein, named BjHK (Bothrops jararaca High Molecular Weight Kininogen) was correlated to mammalian high molecular weight kininogens. Moreover, it was found that this protein inhibits metalloproteases present in the B. jararaca venom. This effect was also observed in human high molecular weight kininogen and correlated to portions of the domain 5 of this protein. The aim of this project is to search for homologies between BjHK and the human kininogen, as well as a possible inhibitory activity of this protein on platelet aggregation and cells adhesion. These activities were also described in human high molecular weight kininogen...
Subject(s)
Animals , Bothrops , Snakes , Snake Venoms/immunology , Snake Venoms/toxicity , Enzymes , Mammals/immunologyABSTRACT
Objective: To establish a liquid chromatography-mass spectometry (LC-MS) method fordetermination of paclitaxel in human plasma, and to study the pharmacokinetics of paclitaxel liposomefor injection (L-PTX) and conventional paclitaxel injection (C-PTX) in patients with cancer. Methods: Anopen, randomized and controlled study was designed. Sixteen patients with cancer were divided into twogroups receiving a single dose of 175 mg/m2 L-PTX and C-PTX, respectively. The blood samples werecollected at 1.5 and 3 h during intravenous infusion and at 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36, 48 and 72 hafter the end of infusion. The drug concentration in the blood was determined by LC-MS method, andthe pharmacokinetic parameters were calculated by DAS2.0 software and compared. Results: The mainpharmacokinetic parameters of L-PTX and C-PTX after a single intravenous infusion of 175 mg/m2 wereas follows: peak plasma concentrations (Cmax) were 6 455 ± 2 247 μg/L and 7 400 ± 1 542 μg/L; theareas under the plasma concentration-time curve (AUC0-∞) were 14 812 ± 2 846 μg·h· L-1 and 21 693 ± 2 657 mu;g·h·L-1 the plasma elimination half-life ( t1/2z) were 30.5 ± 7.3 h and 13.7 ± 3.2 h; the apparentvolumes of distribution (Vz) were 526.8 ± 112.1 L/m2 and 162.9 ± 49.1 L/m2; the plasma clearancerates (CLz) were 12.3 ± 2.7 L·h-1·m-2 and 8.2 ± 1.0 L·h-1·m-2, respectively. The statistical analysisshowed that there was a significant difference in major pharmacokinetic parameters between L-PTX and C-PTX ( P<0.05). Conclusion: The pharmacokinetic properties of paclitaxel in vivo are changed when itis encapsulated by liposome. Compared with C-PTX, the L-PTX is uniquely different in distribution andelimination aspects in patients with cancer, and it demonstrates improved tissue affinity and effect ofdelayed release. Copyright© 2011 by TUMOR.