To study the central pharmacological effect of the water and chloroform-extract compounds from C. chinese in mice.The independent activity test and the hypnotic synergism test by sub-threshold hypnotic dosage of pentobarbital were employed to evaluate the central pharmacological effect of the extract-compounds, and the minimal neurotoxicity was evaluated by the rotorod test.the extract-compounds exhibited significant dose-related inhibition effect of the spontaneous motor activity in mice after intraperitoneal administration. And the two extract-compounds promoted the hypnotic effect by sub-threshold hypnotic dosage administration of pentobarbital, and produced ED50 value of 2.36 g kg (-1) and 0.75 g kg(-1), respectively. Also, both extract-compounds showed no neurotoxicity in the experiment.The extract compounds from C. chinese showed inhibitional effect on CNS.
Twenty-one phenylpropanoids, including 1 new (1) and 20 known phenylpropanoids (2-21), were isolated and identified from the fruits of Nicandra physaloides. The structures of these compounds were established by 1D and 2D NMR spectra referring to the literatures, together with mass spectrometry. It was found that the isolated compounds, except for 7, 18 and 19, showed the different levels of inhibitions on NO production by LPS-induced RAW 264.7 cells at IC50 values from 27.0 to 97.3 μM.
Abstract Objectives This single-centre, retrospective propensity score matching (PSM) study designed to study the impact of cardiopulmonary bypass (CPB) on postoperative acute kidney injury (AKI) and the relationship between AKI and long-term outcomes in elderly patients undergoing coronary artery bypass grafting (CABG). Methods After PSM, 466 pairs of patients (A group, on-pump; B group, off-pump) who were aged≥70 years undergoing first isolated CABG surgery from January 2012 to December 2016 entered the study. AKI was defined and classified according to the Acute Kidney Injury Network (AKIN) criteria. The incidence and severity of in-hospital AKI was compared. The impacts of AKI on the long-term outcomes including new onset of dialysis and mortality were analyzed. Results The two PSM groups had similar baseline and procedure except whether the CPB was used or not. In hospital and 30-day mortality was of no difference(χ2=0.051, p=0.821). AKI of any severity occurred in 40.3% of all patients, with stage 1 accounting for most cases. No difference regarding the incidence and severity of AKI could be found: AKIN stage 1: 139 (29.8%) vs 131 (28.1%); AKIN stage 2: 40 (8.6%) vs 35 (7.5%); AKIN stage 3: 18 (3.9%) vs 13 (2.8%), (u=0.543, p=0.532). No difference was observed in the in-hospital new onset of dialysis (χ2=0.312, P=0.576). The use of CPB was not found to influence long-term new onset of dialysis (χ2=0.14, p=0.708) and mortality (χ2=0.099, p=0.753). Comparing with non-AKI patients, AKI patients were associated with an increased rates of new onset of dialysis (χ2=8.153, p=0.004) and mortality (χ2=6.277, p=0.012) during the follow-up. Comparing with non-AKI patients, the HR for long-term new onset of dialysis and mortality in AKI patients was 1.83 and 1.31 respectively (95%CI 1.12-2.86, p=0.007; 95%CI 1.17-2.58, p=0.015). Conclusions For elderly CABG patients, AKI was common, but deterioration of dialysis was a seldom incidence. Comparing with on-pump, off-pump did not decrease the rates or severity of AKI, long-term new onset of dialysis or mortality. AKI was associated with an increased long-term new onset of dialysis and decreased long-term survival.
Early nutrition after acute ischemic stroke is crucial. We explored early enteral nutrition for stroke patients and evaluated changes in blood indicators as a predictor of stroke prognosis.
A sugar active targeting system for the platinum(IV) prodrug [oxaliplatin(IV)–COOH or in short form OxaPt(IV)] of clinically relevant oxaliplatin (OxaPt(II)) has been reported here for the first time. To achieve this, a series of hydrophilic biocompatible polyurethanes containing free pair-wised pendant amino groups (PU) were synthesized and then lactobionic acid (LA) was grafted to the polyurethane as a targeting moiety, in order to prepare PU–LA conjugates. Thereafter, the prodrug, OxaPt(IV) was introduced into the PU–LA conjugates resulting in the formation of polyurethane platinum(IV) conjugates (PU–LA/Pt) with targeting LA groups. Similarly, PU–Pt conjugates without the LA targeting groups were also prepared. These conjugates were self-assembled into micelles [non-targeting micelles: M(PU–Pt) and targeting micelles: M(PU–LA/Pt)] in water. An in vitro study demonstrated that, compared with M(PU–Pt), M(PU–LA/Pt) demonstrated a lower IC50 (79 μM vs. 126 μM) at 72 h and greater cellular uptake of drugs in HepG2 cells. An in vivo study revealed that M(PU–Pt) and M(PU–LA/Pt) displayed much higher blood drug concentrations and bioavailabilities than the free drug, OxaPt(IV). Moreover, M(PU–LA/Pt) showed enriched distribution in the liver and xenograft H22 tumors as well as better antitumor efficacy. M(PU–LA/Pt) may be a promising polymeric prodrug of the widely used OxaPt(II) for the clinical treatment of various liver cancers.
Naringenin (NRG) is a natural flavonoid compound abundantly present in citrus fruits and has the potential to treat respiratory disorders. However, the clinical therapeutic effect of NRG is limited by its low bioavailability due to poor solubility. To enhance the solubility, naringenin nanosuspensions (NRG-NSps) were prepared by applying tocopherol polyethylene glycol succinate (TPGS) as the nanocarrier via the media-milling method. The particle size, morphology, and drug-loading content of NRG-NSps were examined, and the stability was evaluated by detecting particle size changes in different physiological media. NRG-NSps exhibited a flaky appearance with a mean diameter of 216.9 nm, and the drug-loading content was 66.7%. NRG-NSps exhibited good storage stability and media stability. NRG-NSps presented a sustainable release profile, and the cumulative drug-release rate approached approximately 95% within 7 d. NRG-NSps improved the antitussive effect significantly compared with the original NRG, the cough frequency was decreased from 22 to 15 times, and the cough incubation period was prolonged from 85.3 to 121.6 s. Besides, NRG-NSps also enhanced expectorant effects significantly, and phenol red secretion was increased from 1.02 to 1.45 μg/mL. These results indicate that NRG-NSps could enhance the bioavailability of NRG significantly and possess a potential clinical application.
Abstract Objectives: This single-centre, retrospective propensity score matching (PSM) study designed to study the impact of cardiopulmonary bypass (CPB) on postoperative acute kidney injury (AKI) and the relationship between AKI and long-term outcomes in elderly patients undergoing coronary artery bypass grafting (CABG). Methods: After PSM, 466 pairs of patients (A group, on-pump; B group, off-pump) who were aged≥70 years undergoing first isolated CABG surgery from January 2012 to December 2016 entered the study. AKI was defined and classified according to the Acute Kidney Injury Network (AKIN) criteria. The incidence and severity of in-hospital AKI was compared. The impacts of AKI on the long-term outcomes including new onset of dialysis and mortality were analyzed. Results: The two PSM groups had similar baseline and procedure except whether the CPB was used or not. In hospital and 30-day mortality was of no difference(χ2=0.051, p=0.821). AKI of any severity occurred in 40.3% of all patients, with stage 1 accounting for most cases. No difference regarding the incidence and severity of AKI could be found: AKIN stage 1: 139 (29.8%) vs 131 (28.1%); AKIN stage 2: 40 (8.6%) vs 35 (7.5%); AKIN stage 3: 18 (3.9%) vs 13 (2.8%), (u=0.543, p=0.532). No difference was observed in the in-hospital new onset of dialysis (χ2=0.312, P=0.576). The use of CPB was not found to influence long-term new onset of dialysis (χ2=0.14, p=0.708) and mortality (χ2=0.099, p=0.753). Comparing with non-AKI patients, AKI patients were associated with an increased rates of new onset of dialysis (χ2=8.153, p=0.004) and mortality (χ2=6.277, p=0.012) during the follow-up. Multivariable logistic regression manifested that the HR for long-term new onset of dialysis and mortality in AKI patients vs. non-AKI patients was 1.83 and 1.31 respectively (95%CI 1.12-2.86, p=0.007; 95%CI 1.17-2.58, p=0.015). The HR for long-term new onset of dialysis and mortality in on-pump group vs. off-pump group was 1.07 and 1.11 respectively (95%CI 1.03-1.23, p=0.661; 95%CI 1.09-1.64, p=0.702). Conclusions: For elderly CABG patients, AKI was common, but deterioration of dialysis was a seldom incidence. Comparing with on-pump, off-pump did not decrease the rates or severity of AKI, long-term new onset of dialysis or mortality. AKI was associated with an increased long-term new onset of dialysis and decreased long-term survival.
L. is effective in the treatment of breast cancer (BRCA); however, the underlying mechanism is still unclear. The aim of this study was to elucidate the mechanism of treatment of BRCA by
Secondary osteoporosis is frequently due to the use of high-dose glucocorticoids (GCs). The existing strategy for managing glucocorticoid-induced osteoporosis (GIOP) is considered insufficient and remains in a state of ongoing evolution. Therefore, it is crucial to develop more precise and effective agents for the treatment of GIOP. The constituents of
A novel mononuclear trigonal prism indium( iii ) complex, namely, In(H 2 nha) 3 (1) (H 3 nha = 3-hydroxy-2-napthanoic hydroxamic acid), displaying efficient detection of Al 3+ and B 4 O 7 2− by fluorescence enhancement effect.
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