Volatile components in Yinchenzhufu decoction and their pharmacokinetics after oral administration in rats.

In China, Yinchenzhufu decoction (YCZFD) has been used to treat cholestatic liver disease in clinical practice for hundreds of years. Nonvolatile components in YCZFD, their composition, components absorbed in blood, and pharmacokinetic characteristics have been clarified. However, information about its volatile components is limited. The aim of the present study was to identify the components of the volatile oil (VO) of YCZFD, quantify the major volatile components in YCZFD, and reveal their pharmacokinetic characteristics. In YCZFD, 85 components representing 95.36% of the total oil composition were identified by gas chromatography-mass spectrometry. Next, 11 highly abundant components were quantified in YCZFD and YCZFD VO. Finally, a sensitive headspace solid-phase dynamic extraction-chromatography-quadruple mass spectrometry method for determining 8 volatile components in rat plasma was established and applied to compare the pharmacokinetics of YCZFD and YCZFD VO after oral administration in rats. These volatile components were rapidly absorbed and eliminated, and they presented highly different exposure levels. The area under the concentration-time curves of some volatile components in YCZFD was higher than that in YCZFD VO. The results showed that the water extract of YCZFD increased the exposure of volatile components. Our study provides valuable information for understanding the potential effective components of YCZFD.

Effect of limb rotation on radiographic alignment measurement in mal-aligned knees.

PURPOSE: Long-leg-radiography (LLR) is commonly used for the measurement of lower limb alignment. However, limb rotations during radiography may interfere with the alignment measurement. This study examines the effect of limb rotation on the accuracy of measurements based on the mechanical and anatomical axes of the femur and tibia, with variations in knee flexion and coronal deformity. METHODS: Forty-five lower limbs of 30 patients were scanned with CT. Virtual LLRs simulating five rotational positions (neutral, ± 10[Formula: see text], and ± 20[Formula: see text] internal rotation) were generated from the CT images. Changes in the hip-knee-ankle angle (HKA) and the femorotibial angle (FTA) were measured on each image with respect to neutral values. These changes were related to knee flexion and coronal deformity under both weight- and non-weight-bearing conditions. RESULTS: The measurement errors of the HKA and FTA derived from limb rotation were up to 4.84 ± 0.66[Formula: see text] and 7.35 ± 0.88[Formula: see text], respectively, and were correlated with knee flexion (p < 0.001) and severe coronal deformity (p < 0.001). Compared with the non-weight-bearing position, the coronal deformity measured in the weight-bearing condition was 2.62[Formula: see text] greater, the correlation coefficients between the coronal deformity and the deviation ranges of HKA and FTA were also greater. CONCLUSIONS: Flexion and severe coronal deformity have a significant influence on the measurement error of lower limb alignment. Errors can be amplified in the weight-bearing condition compared with the non-weight-bearing condition. When using HKA and FTA to represent the mechanical axis and the anatomical axis on LLR, limb rotation impacts the anatomic axis more than the mechanical axis in patients with severe deformities. Considering LLR as the gold standard image modality, attention should be paid to the measurement of knee alignment. Especially for the possible errors derived from weight-bearing long-leg radiographs of patients with severe knee deformities.

Anti-convulsant effects of cultures bear bile powder in febrile seizure via regulation of neurotransmission and inhibition of neuroinflammation.

ETHNOPHARMACOLOGICAL RELEVANCE: Natural bear bile powder (NBBP) has been used to treat seizures for thousands of years, but its application is greatly restricted due to ethical reasons. Cultured bear bile powder (CBBP), which is produced by biotransformation, may be an appropriate substitute for NBBP. However, the anti-convulsant effects of CBBP and its mechanisms remain unclear. AIM OF THE STUDY: This study aimed to investigate the anti-convulsant effects and possible mechanisms of CBBP in a febrile seizure (FS) rat model. MATERIALS AND METHODS: FS was induced by placing the rats in a warm water bath (45.5 °C). The incidence rate and latency of FS, and hematoxylin-eosin staining (HE) were conducted for neurological damage. The levels of 4 bile acids and 8 main neurotransmitters in vivo were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The expression of bile acid related transports, neurotransmitter receptors, inflammatory factors, neurotrophic factors and glial fibrillary acidic protein (GFAP) in hippocampal tissues were detected by real-time PCR, western blotting, and immunohistochemistry. RESULTS: Pre-treatments with CBBP and similarly, NBBP, significantly reduced the incidence rate and prolonged the latency of FS. Additionally, CBBP alleviated the histological injury induced by FS in the rat hippocampus tissue. LC-MS/MS analyses revealed that CBBP markedly increased the levels of tauroursodeoxycholic acid (TUDCA), taurochenodeoxycholic acid (TCDCA), ursodeoxycholic acid (UDCA), and chenodeoxycholic acid (CDCA) in FS rats. Furthermore, the content of gamma-aminobutyric acid (GABA) was up-regulated in rats pre-treated with CBBP whereas GFAP was down-regulated. CBBP also significantly suppressed the expression of interleukin -1ß (IL-1ß), tumor necrosis factor α (TNF-α), nuclear factor kappa B (NF-κB), and brain-derived neurotrophic factor (BDNF) and its TrkB receptors, and improved the expression of GABA type A receptors (GABAAR) and farnesoid X receptors (FXR). CONCLUSIONS: The present study demonstrated that CBBP had anti-convulsant effects in a FS rat model. CBBP may protect rats against FS, probably by up-regulating FXR, which was activated by increasing brain bile acids, up-regulating GABAergic transmission by inhibiting BDNF-TrkB signaling, and suppressing neuroinflammation by inhibiting the NF-κB pathway.

A validated surrogate analyte UPLC-MS/MS assay for quantitation of TUDCA, TCDCA, UDCA and CDCA in rat plasma: Application in a pharmacokinetic study of cultured bear bile powder.

Bear bile is a valuable medicinal material used in traditional Chinese medicine for over 2000 years. However, developing a substitute has become necessary because of protection measures for this endangered species. The ingredients of in vitro cultured bear bile powder (CBBP) include tauroursodeoxycholic acid (TUDCA), taurochenodeoxycholic acid (TCDCA), ursodeoxycholic acid (UDCA) and chenodeoxycholic acid (CDCA, and it has pharmacological properties that are similar to those of natural bear bile powder (NBBP). In this study, the pharmacokinetic parameters of both CBBP and NBBP were measured in rats with a new surrogate analyte LC-MS method using stable isotopes as surrogate analytes (D4-TUDCA, D4-TCDCA, D4-UDCA and D4-CDCA) with response factors validated in authentic matrix (plasma) for simultaneously monitoring the authentic analytes (TUDCA, TCDCA, UDCA and CDCA). The method validation was satisfactory for the linear regression (r, 0.9975-0.9994), precision (RSD intra-day, 0.72-9.35%; inter-day, 3.82-9.02%), accuracy (RE, -12.42-5.67%) and matrix effect (95.53-99.80%), along with analyte recovery (95.90-98.82%) and stability (89.48-101.81%) of surrogate analytes, and precision (RSD intra-day, 1.06- 11.51%; inter-day, 2.23- 11.38%), accuracy (RE, -7.40-10.76%) and stability (87.37-111.70%) of authentic analytes. We successfully applied this method to evaluate the pharmacokinetics of CBBP and NBBP in rats, which revealed the critical in vivo properties of both bear bile preparations.

Simultaneous determination of multiple compounds of Da-Huang-Xiao-Shi decoction in rat plasma by LC-MS/MS and its application in a pharmacokinetic study.

Da-Huang-Xiao-Shi decoction (DHXSD), a traditional Chinese medicinal formula, has been used mainly to treat jaundice for more than 1700 years in China. In this study, we developed a rapid, sensitive, and accurate LC-MS/MS method to simultaneously determine multiple, potentially bioactive compounds of DHXSD, including five alkaloids (berberine, phellodendrine, palmatine, jatrorrhizine, and magnoflorine), five anthraquinones (rhein, aloe-emodin, emodin, chrysophanol, and physcion), two iridoid glycosides (geniposide and genipin 1-gentiobioside), and one iridoid aglycone (genipin) in rat plasma. Plasma samples collected from rats were treated immediately with 5% acetic acid to avoid the degradation of genipin. After protein precipitation with acetonitrile containing 5% acetic acid, the compounds were reconstituted in acetonitrile-water (50:50, v/v) solution containing 6.5% formic acid and separated on the ACQUITY™ UPLC BEH C18 column (2.1 × 100 mm; 1.7 µm) using a mobile phase composed of 2 mM ammonium formate in water (solvent A) and acetonitrile (solvent B) at a flow rate of 0.3 mL/min. Quantitation was performed on a Triple Quand 5500 tandem mass spectrometer coupled with an electrospray ionization (ESI) source. Multiple reaction monitoring (MRM) was used to quantify compounds in positive and negative ion modes. The method validation results showed that the specificity, linearity, precision and accuracy, recovery, matrix effect, and stability of the 13 compounds met the requirements for their quantitation in biological samples. This newly established method was successfully used in a pharmacokinetic study on rats orally treated with DHXSD. Besides, glucuronide and sulfate metabolites were also determined in rat plasma after hydrolysis. This is the first method developed for the simultaneous quantification of multiple compounds of DHXSD in vivo. Our study provides relevant information on the pharmacokinetics of DHXSD and the relationship between the compounds of DHXSD and their therapeutic effects.

A systematic review and meta-analysis of the prevalence, trends, and geographical distribution of HIV among Chinese female sex workers (2000-2011): implications for preventing sexually transmitted HIV.

OBJECTIVE: The aim of this meta-analysis was to investigate temporal and geographical trends in the HIV epidemic among female sex workers (FSWs) recruited from various venues in China. METHODS: Chinese and English peer-reviewed articles published between January 2000 and February 2013 were systematically searched. Standard meta-analysis methods were used to calculate the pooled HIV prevalence, in accordance with the PRISMA guidelines. RESULTS: The national HIV prevalence among FSWs declined from 0.74% (95% confidence interval (CI) 0.37-1.49%) in 2000-2002 to 0.40% (95% CI 0.31-0.53%) in 2009-2011. All Chinese regions demonstrated significant declines in HIV prevalence, apart from the East and South Central regions, in which the epidemics stabilized at low/moderate levels. Despite a significant decline from 1.92% (95% CI 0.86-4.24%) to 0.87% (95% CI 0.65-1.18%) during 2000-2011, Southwest China still bore the greatest HIV disease burden. Nationwide, FSWs recruited from detention centres had the highest HIV prevalence (0.92%, 95% CI 0.46-1.88%), followed by voluntary counselling and testing sites (0.80%, 95% CI 0.46-1.67%) and entertainment venues (0.61%, 95% CI 0.47-0.79%). The prevalences among FSWs in high-, middle-, and low-tier entertainment venues were 0.59% (95% CI 0.32-1.45%), 0.92% (95% CI 0.50-1.77%), and 1.10% (95% CI 0.71-2.16%), respectively. High- and middle-tier FSWs had a significantly lower risk of HIV infection than lower-tier FSWs (high/low: odds ratio (OR) 0.48, 95% CI 0.40-0.59; middle/low: OR 0.49, 95% CI 0.37-0.66). CONCLUSIONS: The HIV epidemic has shown a gradual declining or stabilizing trend among Chinese FSWs. Intervention efforts should be diverted to high-risk subgroups of FSWs, such as drug-using and low-tier FSWs.

Risk behaviours among female sex workers in China: a systematic review and data synthesis.

BACKGROUND: Commercial sex is one of the major modes of HIV transmission in China. Understanding HIV risk behaviours in female sex workers (FSW) is of great importance for prevention. This study aims to assess the magnitude and temporal changes of risk behaviours in Chinese FSW. METHOD: Five electronic databases were searched to identify peer-reviewed English and Chinese language articles published between January 2000 and December 2012 that reported risk behaviours among FSW in China, including condom use, HIV testing, and drug use. Linear regression and Spearman's rank correlation were used to examine temporal trends in these risk factors. The study followed PRISMA guidelines for meta-analyses and was registered in the PROSPERO database for systematic reviews. RESULTS: A total of 583 articles (44 English, 539 Chinese) investigating 594,583 Chinese FSW were included in this review. At last sex, condom use was highest with commercial partners (clients), increasing from 53.7% in 2000 to 84.9% in 2011. During this same time period, condom use increased with regular partners from 15.2% to 40.4% and with unspecified partners from 38.6% to 82.5%. Increasing trends were also found in the proportion of sampled FSW who reported testing for HIV in the past 12 months (from 3.2% in 2000 to 48.0% in 2011), while drug use behaviours decreased significantly from 10.9% to 2.6%. CONCLUSION: During the first decade of 2000, Chinese FSWs' self-reported risk behaviours have decreased significantly while HIV testing has increased. Further outreach and intervention efforts are needed to encourage condom use with regular partners, continue promotion of HIV testing, and provide resources for the most vulnerable FSW, particularly low tier FSW, who may have limited access to sexual health and prevention programs.

Prevalence of HIV and syphilis infections among long-distance truck drivers in China: a data synthesis and meta-analysis.

By 2009, 46 national sentinel surveillance sites had been established for long-distance truck drivers (LDTDs) in China, but the overall disease burden of HIV and syphilis among LDTDs has remained unclear. This study aimed to summarize the prevalence levels of these infections from available published peer-reviewed studies through a comprehensive systematic review and meta-analysis. Forty-six eligible articles were selected in this review. The pooled prevalence estimates of HIV and syphilis among Chinese LDTDs during 1995-2010 were 0.19% (95% confidence interval (CI) 0.15-0.24%) and 0.86% (95% CI 0.70-1.06%), respectively, corresponding to a 3.33 (95% CI 2.40-4.62) and 1.65 (95% CI 1.35-2.03) times higher risk of infection among LDTDs than the general Chinese population. However, these infection risks were much lower than those of LDTDs in other developing country settings and at-risk groups in China. Current surveillance resources have been disproportionately focused on LDTDs and should be diverted to other at-risk groups.