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Zhao H.,PLA Fourth Military Medical University | Zhao H.,Cultivation Project of Collaborative Innovation Center for Chinese Medicine in QinBa Mountains | Yuan J.,PLA Fourth Military Medical University | Yuan J.,Cultivation Project of Collaborative Innovation Center for Chinese Medicine in QinBa Mountains | And 8 more authors.
Journal of Agricultural and Food Chemistry | Year: 2015

The purpose of our research is to find a new lipid emulsion to deliver a low water-soluble compound, cinnamaldehyde (CA). Its characteristics, pharmacokinetics, antitumor efficacy, and toxicity were evaluated. The mean particle size, zeta potential, and encapsulation efficiency of the submicromemter emulsion of CA (SME-CA) were 130 ± 5.92 nm, -25.7 ± 6.00 mV, and 99.5 ± 0.25%, respectively. The area under the curve from 0 h to termination time (AUC0-t) of SME-CA showed a significantly higher value than that of CA (589 ± 59.2 vs 375 ± 83.5 ng h/L, P < 0.01). Tissue distribution study showed various changes; among them, a 27% higher concentration was found in brain tissue when using SME-CA at 15 min after administration. For the efficacy evaluation, SME-CA exhibited 8- and 11-fold antitumor activity in the depression of HeLa and A549 cell lines with the IC50 decreasing to 0.003 and 0.001 mmol/L, respectively. The LD50 values of CA and SME-CA in mice were 74.8 and 125 mg/kg, suggesting increased safety from the new formulation. The new formulation exhibited lower toxicity, higher antitumor activity, and a more satisfactory pharmacokinetic property, which displayed great potential for future pharmacological application. © 2015 American Chemical Society. Source

Chen Y.,PLA Fourth Military Medical University | Chen Y.,Cultivation Project of Collaborative Innovation Center for Chinese Medicine in QinBa Mountains | Cao Y.,PLA Fourth Military Medical University | Cao Y.,Cultivation Project of Collaborative Innovation Center for Chinese Medicine in QinBa Mountains | And 16 more authors.
Phytomedicine | Year: 2013

Aim To examine the efficacy of YuanHu painkillers (YHP) as a treatment for primary dysmenorrhea and to reveal YHP's principle formula. Methods A Wistar rat uterine contraction model was utilized in this study. Rats were given 0.698 g/kg YHP, 0.07 g/kg tetrahydropalmatine (THP; YHP's main component), 0.02 g/kg imperatorin (IMP), or THP + IMP (0.07 + 0.02 g/kg) as polypharmacy (PG) by gavage. H&E staining and histopathological examination of the uteri tissue samples were performed. We then detected superoxide dismutase (SOD) and malondialdehyde (MDA), nitric oxide (NO), as well as inducible nitric oxide synthase (iNOS), i-κB, nuclear factor-κB (NF-κB), and cyclooxygenase-2 (COX-2) indices. Results PG significantly inhibited the uterine contraction of the primary dysmenorrhea rat model (p < 0.05), and was significantly different than single-agent therapy (p < 0.05). Histopathological examination showed inflammation in the uteri of the control group which YHP and its main constitutes alleviated. THP significantly inhibited the contraction of isolated uteri caused by Ach, PGF2α and oxytocin in a concentration-dependent fashion. THP and IMP both significantly affected the levels of NO, activation of NF-κB, up-regulated the expression of i-κB and down-regulated the expression of both iNOS and COX-2. IMP obviously decreased the level of MDA and increased the activation of SOD (p < 0.05). PG obviously improved all the parameters mentioned above (p < 0.05). Conclusions YHP exerted protective effects on primary dysmenorrhea in rats and remarkably alleviated the severity of experimental primary dysmenorrhea. The combined strategy proved to be more effective than either THP or IMP alone and may have synergistic effects in combination in primary dysmenorrhea. Mechanisms that might account for the beneficial effects include abating oxidative stress, inhibiting over-inflammatory reaction, and alleviating the contraction of isolated rat uteri by inhibiting the influx of extracellular Ca2+. Broad potential for future clinical practice is foreseeable. © 2013 Elsevier GmbH. Source

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