Transient receptor potential vanilloid 1 involved in the analgesic effects of total flavonoids extracted from Longxuejie ().

OBJECTIVE: To evaluate the analgesic effects of total flavonoids of Longxuejie (Resina Dracaenae Cochinchinensis) (TFDB) and explore the possible analgesic mechanism associated with transient receptor potential vanilloid 1 (TRPV1). METHODS: Whole-cell patch clamp technique was used to observe the effects of TFDB on capsaicin-induced TRPV1 currents. Rat experiments in vivo were used to observe the analgesic effects of TFDB. Western blot and immunofluorescence experiments were used to test the change of TRPV1 expression in DRG neurons induced by TFDB. RESULTS: Results showed that TFDB inhibited capsaicin-induced TRPV1 receptor currents in acutely isolated dorsal root ganglion (DRG) neurons of rats and the half inhibitory concentration was (16.7 ± 1.6) mg/L. TFDB (2-20 mg/kg) showed analgesic activity in the phase Ⅱ of formalin test and (0.02-2 mg per paw) reduced capsaicin-induced licking times of rats. TFDB (20 mg/kg) was fully efficacious on complete Freund's adjuvant (CFA)-induced inflammatory thermal hyperalgesia and capsaicin could weaken the analgesic effects. The level of TRPV1 expressions of DRG neurons was also decreased in TFDB-treated CFA-inflammatory pain rats. CONCLUSION: All these results indicated that the analgesic effect of TFDB may contribute to their modulations on both function and expression of TRPV1 channels in DRG neurons.

Efficacy and safety of Chinese herbal medicine as adjunctive therapy in sepsis patients with bloodstream infection: a propensity-matched analysis.

OBJECTIVE: To investigate the efficacy and safety of Chinese herbal medicine in treating sepsis patients with bloodstream infection. METHODS: A 6-year retrospective study was carried out at a university hospital in China. Adult sepsis patients with bloodstream infection were included. The primary outcome was 28-day mortality after admission. Propensity score method was used to adjust for possible confounding. 28-day mortality was estimated by Kaplan-Meier analysis and compared using the log-rank test. Cox regression analysis was carried out to identify factors impacting in-hospital mortality outcomes. RESULTS: Following the application of the propensity score method, a total of 176 patients were included. The all-cause 28-day mortality in the control group and Chinese herbal medicine group was 21.6% and 14.8%, respectively. Kaplan-Meier survival analysis showed that Chinese herbal medicine was associated with a lower hazard ratio (HR) in all-cause 28-day death compared with the control group [HR = 0.44, 95% CI(0.22, 0.90), P < 0.05]. The complications were similar between the two groups (P >0.05). Blood-activating and stasis-eliminating herb administration was associated with reduced in-hospital mortality among sepsis patients with bloodstream infection [HR = 0.54, 95% CI(0.34, 0.94), P < 0.05]. CONCLUSIONS: Chinese herbal medicine, especially the blood-activating and stasis-eliminating herb, might have certain efficacy and safety in treating sepsis patients with bloodstream infection. Clinicians should prescribe blood-activating and stasis-eliminating herb in treating these two coalescent critical diseases as long as no contraindications exist. However, further studies are needed to validate our results.

[Absorption mechanism of dragon's blood phenolic extracts in Caco-2 cells].

The purpose of this study was to study the absorption characteristics of eight main components from dragon's blood phenolic extracts in Caco-2 cells based on the humancolon cancer cell Caco-2 model, and to clarify the oral absorption mechanism of such phenolic extracts. UPLC-MS/MS was used in this study to determine the content of 8 active ingredients including thevetiaflavone, 7,4'-dihydroxyflavone, 7,4'-dihydroxy-5-methoxyhomoisoflavanone, 7,4'-dihydroxyhomoisoflavanone, loureirin C, loureirin A, loureirin B and pterostilbene from dragon's blood phenolic extracts, and Caco-2 cells were used to investigate the effects of incubation time, concentration, temperature, P-gp inhibitor, MRP inhibitor, OCTN1 inhibitor and OCTN2 inhibitor on the absorption of each component. In addition, the transport experiment was conducted to measure the apparent permeability coefficient P_(app) and transport rate of the eight main components to predict the oral absorption mechanism of dragon's blood phenolic extracts. The experimental results showed that the cell uptake of the eight main components in dragon's blood phenolic extracts was time-dependent and concentration dependent, and the uptake of each component did not need to consume energy, which was consistent with the passive diffusion process. P-gp inhibitor, MRP inhibitor and OCTN1 inhibitor had no effect on the cell uptake of each component, only the addition of OCTN2 inhibitor significantly reduced the uptake of pterostilbene(P<0.05). In the transport results, the ER values of the outflow rates of the eight components were all less than 1.5. The above results show that the absorption mechanism of the eight components in Draconis resina phenolic extract may be passive diffusion, and pterostilbene may be the substrate of OCTN2.

[Chemical profiling of Artemisia rupestris using HPLC-IT-TOF-MS].

Artemisia rupestris is widely used as a folk medicine of Uygur and Kazak with blood and detoxification, deaccumulation stagnation, clearing heat digestion and other effects. Currently, the chemical profile of A. rupestris has not been disclosed, resulting in a great obstacle for the systematic clarification of the efficacy materials and the quality evaluations. In this paper, HPLC-IT-TOF-MS was deployed to characterize the chemical constituents in A. rupestris. As a result, a total of 124 compounds were detected in 75% ethanol extract of A. rupestris. By comparing with the reference compounds, seven chlorogenic acids, and four flavonoids as well as one sesquiterpenoid were definitely identified. Moreover, twenty sesquiterpenes, sixty-five flavonoids and twenty-three chlorogenic acids were preliminarily identified by matching MS/MS spectral information with literature data and applying those empirical mass spectrometric cracking rules. In current study, the chemical composition of A. rupestris was profiled in depth, and the findings are envisioned to provide a theoretical basis for the further studies of this well-known herbal medicine, such as efficacy material characterization and quality assessment.

[Pharmacokinetics of praziquantel injection in healthy buffaloes].

Objective To investigate the pharmacokinetics and relative bioavailability of praziquantel injection in buffaloes in contrast to praziquantel tablet. Methods A single oral administration of praziquantel tablet at a dose of 20 mg/kg or intramuscular administration of praziquantel injection at a dose of 10 mg/kg was performed in six healthy adult buffalos according to a twoperiod crossover design. The praziquantel concentration in plasma was determined by a high performance liquid chromatography (HPLC) method. The pharmacokinetic parameters were calculated by non-compartmental analysis. Results The main pharmacokinetic parameters of praziquantel tablet were as follows: Tmax = (0.60±0.29)h, Cmax = (0.57±0.37)µg/ml, T1/2ß = (0.70±0.42)h, AUC = (0.80±0.70) (µg/ml)·h. The main pharmacokinetic parameters of praziquantel injection were as follows: Tmax = (0.65± 0.49)h, Cmax = (3.82±1.17)µg/ml, T1/2ß = (1.00±0.73)h, AUC = (1.61±0.89) (µg/ml)·h. The relative bioavailability of praziquantel injection was 402.5% in contrast to praziquantel tablet. Conclusion The praziquantel injection has pharmacokinetic characteristics of rapid absorption, high bioavailability and extensive distribution, and the clinical recommended dosage of praziquantel injection is 10 mg/kg.

A prospective randomized controlled trial to compare Pringle maneuver, hemihepatic vascular inflow occlusion, and main portal vein inflow occlusion in partial hepatectomy.

BACKGROUND: blood loss during liver resection and the need for perioperative blood transfusions have negative impact on perioperative morbidity, mortality, and long-term outcomes. METHODS: a randomized controlled trial was performed on patients undergoing liver resection comparing hemihepatic vascular inflow occlusion, main portal vein inflow occlusion, and Pringle maneuver. The primary endpoints were intraoperative blood loss and postoperative liver injury. The secondary outcomes were operating time, morbidity, and mortality. RESULTS: a total of 180 patients were randomized into 3 groups according to the technique used for inflow occlusion during hepatectomy: the hemihepatic vascular inflow occlusion group (n = 60), the main portal vein inflow occlusion group (n = 60), and the Pringle maneuver group (n = 60). Only 1 patient in the hemihepatic vascular occlusion group required conversion to the Pringle maneuver because of technical difficulty. The Pringle maneuver group showed a significantly shorter operating time. There were no significant differences between the 3 groups in intraoperative blood loss and perioperative mortality. The degree of postoperative liver injury and complication rates were significantly higher in the Pringle maneuver group, resulting in a significantly longer hospital stay. CONCLUSIONS: all 3 vascular inflow occlusion techniques were safe and efficacious in reducing blood loss. Patients subjected to hemihepatic vascular inflow occlusion, or main portal vein inflow occlusion responded better than those with Pringle maneuver in terms of earlier recovery of postoperative liver function. As hemihepatic vascular inflow occlusion was technically easier than main portal vein inflow occlusion, it is recommended.