Decrease of Coronal Optic Nerve Sheath Diameter is Associated With Postoperative Cognitive Decline in Patients Undergoing Carotid Endarterectomy.

Objective: Patients undergoing carotid endarterectomy (CEA) have a significant possibility of developing postoperative cognitive decline (POCD). POCD after surgery could be result from cerebral hypotension induced by cross-clamping or postoperative hyperperfusion. Optic nerve sheath diameter (ONSD) exhibits an excellent correlation with invasive intracranial pressure monitoring, Here, the authors explored the risk factors of POCD in patients undergoing CEA, paying close attention to ONSD to test the hypothesis that decrease of coronal ONSD was related to the incidence of POCD.

Decreased LF/HF ratio is associated with worse outcomes in patients who received mechanical thrombectomy under general anesthesia for emergent large vessel occlusion: a retrospective study.

Background And Purpose: We aimed to determine whether heart rate variability (HRV) was correlated to long-term outcome in patients who received mechanical thrombectomy (MT) under general anesthesia for emergent large vessel occlusion (ELVO).

Methods: Data from 106 patients receiving MT under general anesthesia to treat ELVO between January 1, 2017 and December 31, 2019 were collected in a multicenter chart review. Univariate analysis, Chi-square test, and bivariate logistic regression were performed to assess the correlations between preoperative risk factors such as HRV and long-term outcome (as indicated by the modified Rankin score [mRS] at 90 days after MT).

[Determination of 2,4-dihydroxybenzophenone in mouse brain by high performance liquid chromatography].

Objective: To optimize and establish the experimental methods for the determination of 2,4-dihydroxybenzophenone (BP-1) in mouse brain.

Methods: BP-1 was determined by high performance liquid chromatography (HPLC) and separated by Waters Symmetry C18 (4.6 mm×250 mm, 5 μm) using isocratic elution, and the sample preparation conditions were optimized by orthogonal experiment design.

[Protective effect of 2,4-dihydroxybenzophenone on cocaine-induced hepatotoxicity and neurotoxicity in mice].

Objective: To investigate the protective effect of 2,4-dihydroxybenzophenone(BP-1) on acute hepatotoxicity and neurotoxicity induced by cocaine in mice, and its possible mechanism.

Methods: Male ICR mice were pretreated with BP-1(100,200,400 mg/kg, ig, 4 d), cocaine(75 mg/kg) was injected 30 minutes after BP-1 administration on day 4.Twenty-four hours after the injection of cocaine, the serum activities of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and lactate dehydrogenase (LDH) were assayed by HITACHI-7170A automatic analyzer.

Protective effects of 5-methoxypsoralen against acetaminophen-induced hepatotoxicity in mice.

Aim: To investigate the hepatic protective effects of 5-methoxypsoralen (5-MOP) and to learn if 5-MOP causes hepatotoxicity at protective doses.

Methods: C57BL/6J mice were administrated orally with 5-MOP at doses of 12.5, 25 and 50 mg/kg body weight respectively every morning for 4 d before given acetaminophen (APAP) subcutaneously at a dose of 500 mg/kg.

Protective effects of 2,4-dihydroxybenzophenone against acetaminophen-induced hepatotoxicity in mice.

Aim: To examine the effects of 2,4-dihydroxybenzophenone (BP-1), a benzophenone derivative used as an ultraviolet light absorbent, on acetaminophen (APAP)-induced hepatotoxicity in C57BL/6J mice.

Methods: Mice were administered orally with BP-1 at doses of 200, 400 and 800 mg/kg body weight respectively every morning for 4 d before a hepatotoxic dose of APAP (350 mg/kg body weight) was given subcutaneously. Twenty four hours after APAP intoxication, the serum enzyme including serum alaine aminotransferase (ALT), aspartate aminotransferase (AST), lactate dehydrogenase (LDH) were measured and liver histopathologic changes were examined.

Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.

To aid in the pursuit of selective kinase inhibitors, we have developed a unique ATP site binder tool for the detection of binders outside the ATP site by nuclear magnetic resonance (NMR). We report here the novel synthesis that led to this paramagnetic spin-labeled pyrazolopyrimidine probe (1), which exhibits nanomolar inhibitory activity against multiple kinases. We demonstrate the application of this probe by performing NMR binding experiments with Lck and Src kinases and utilize it to detect the binding of two compounds proximal to the ATP site.

[The hepatoprotective effect of aqueous extracts from Ficus hirta on N, N-dimethylformamide induced acute liver injury in mice].

Objective: To investigate the effect of aqueous extract from Ficus hirta on N, N-Dimethylformamide (DMF) induced liver injury in mice.

Methods: C57BL/6 mice and ICR mice were randomly divided into 5 groups: negative control group, positive control group and three treated groups respectively. Treated groups were administered orally with 100, 200, 300 g/kg Ficus hirta aqueous extract per day respectively for 5 days.

[Effect of roots of Ficus hirta on cocaine-induced hepatotoxicity and active components].

Objective: To investigate the protective effect of the roots of F. hirta against the cocaine-induced hepatotoxicity and it's active components.

Method: Cocaine hydrochloride was subcutaneously injected to make male ICR mice liver wounded.

Identification of potent and selective MMP-13 inhibitors.

A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 microM) inhibitor that did not bear a zinc chelator. Structure-based drug design strategies were employed to append a Zn-chelating group to one end of the molecule and functionality to enhance selectivity to the other.

[Study on the use of haemoglobin denaturation test as an alternative to Draize eye irritation test].

Objective: To use haemoglobin denaturation test (HD test) as an alternative to Draize eye irritation test (Draize test).

Methods: Fourteen cosmetic ingredients were tested by HD test. The results were compared with two kinds of scores in Draize test, i.

Catalytic domain crystal structure of protein kinase C-theta (PKCtheta).

A member of the novel protein kinase C (PKC) subfamily, PKC, is an essential component of the T cell synapse and is required for optimal T cell activation and interleukin-2 production. Selective involvement of PKC in TCR signaling makes this enzyme an attractive therapeutic target in T cell-mediated disease processes. In this report we describe the crystal structure of the catalytic domain of PKC at 2.

Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.

The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue degradation. In our preceding paper, we have reported on a series of novel and orally active N-hydroxy-alpha-phenylsulfonylacetamide derivatives. However, these compounds had two drawbacks (moderate selectivity and chirality issues).