Redox-Neutral Coupling of Allyl Alcohols with Trifluoromethyl Ketones via Synergistic Ni-Ti Bimetallic Catalysis.

A redox-neutral coupling of allyl alcohols with trifluoromethyl ketones has been developed via Ni-Ti bimetallic catalysis. This innovative method allows for the efficient synthesis of various β-tertiary trifluoromethyl alcohol-substituted ketones with yields of up to 98%. The reaction is scalable and compatible with a wide range of substrates, including complex bioactive molecules.

Iodine-catalyzed regioselective direct sulfenylation of uracil with sulfonyl hydrazide as sulfur source under solvent free conditions.

A facile method was developed for the selective thioetherification of uracils using sulfonyl hydrazide as the thioetherification reagent. This method offers advantages such as avoiding the use of additives and expensive metal catalysts, and providing good to excellent yields of various uracil thioethers. Experimental studies have demonstrated that the reaction follows a free radical pathway.

Two new alkaloids from Dendrobium nobile Lindl. exhibited neuroprotective activity, and dendrobine alleviated Aβ -induced apoptosis by inhibiting CDK5 activation in PC12 cells.

Dendrobium nobile Lindl. is registered in the Chinese Pharmacopoeia as a traditional medicine. Phytochemical investigation of the ethanol extract of D.

Cp*Co-catalyzed formal [4 + 2] cycloaddition of 2-phenyl-1-imidazoles to afford imidazo[1,2-]quinazoline derivatives.

A synthetic protocol based on Cp*Co-catalyzed C-H amidation/annulation of 2-aryl-1-imidazoles with 1,4,2-dioxazol-5-ones was developed to give imidazo[1,2-]quinazoline derivatives with broad substrate scope in moderate to good yields. The method has good prospects of application in the synthesis of imidazo[1,2-]quinazoline drugs.

Dihydrophenanthrenes and phenanthrenes from .

Two previously undescribed dihydrophenanthrene derivatives ( and ) were isolated along with twelve known analogues from the whole plant of . The structures of the new compounds were elucidated on the basis of detailed spectroscopic analysis. The NMR data of known phenanthrene derivatives ( and ) were revised by 2D NMR.

Seven new prenylated flavanones from the roots of Sophora flavescens and their anti-proliferative activities.

Aiming to discover potent anti-proliferative agents from the roots of Sophora flavescens, seven new prenylated flavanones were isolated, along with 16 known compounds. Their structures were elucidated by interpretation of their spectroscopic data (1D and 2D NMR, UV, IR, CD, and HRESIMS) and comparison to literature data. In the in vitro assay, 21 showed anti-proliferative activity against human hepatoma cells (HepG2).

New benzoic acid glycosides from .

Two new benzoic acid derivatives, sophophenoside A () and sophophenoside B (), were isolated from . Their structures were elucidated by detailed spectroscopic analysis and chemical methods. Compounds and were assayed for their hepatoprotective activity on the cytotoxic effect of D-galactosamine on HL-7702 cells, and compound exhibited a moderate hepatoprotective activity at a concentration of 10 M.

Immunomodulatory effect of polysaccharides from the extraction of (Blume) Hook. f. et Thomson (Campanulaceae) roots in female rats.

In this study, the crude polysaccharides of (CJP) was obtained from (Blume) Hook. f. et Thomson using hot water extraction method, which was separated and purified by DEAE-cellulose column and Sepharose CL-6B column.

Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.

Here we reported novel apigenin-rivastigmine hybrids were rationally designed and synthesized by the multi-target-directed ligands (MTDLs) strategy, their activity in vitro results revealed that compound 3d showed significant antioxidant potency (ORAC = 1.3 eq), and it was a reversible huAChE (IC = 6.8 μM) and huBChE (IC = 16.

Licochalcone A suppresses the proliferation of sarcoma HT-1080 cells, as a selective R132C mutant IDH1 inhibitor.

IDH1 mutations are closely related to the development and progression of various human cancers, such as glioblastoma, sarcoma, and acute myeloid leukemia. By screening dozens of reported natural compounds using both wild-type and mutant IDH1 enzymatic assays, we discovered Licochalcone A is a selective inhibitor to the R132C-mutant IDH1 with an IC value of 5.176 μM, and inhibits the proliferation of sarcoma HT-1080 cells with an IC value of 10.

Cobalt(ii)-catalyzed benzylic oxidations with potassium persulfate in TFA/TFAA.

A cobalt-catalyzed C(sp)-H oxygenation reaction to furnish aldehyde was herein reported. This transformation demonstrated high chemo-selectivity, and tolerated various methylarenes bearing electron-withdrawing substituents. This reaction provided rapid access to diverse aldehydes form methylarenes.

[Absorptive characteristic of Bletilla striata extract in Caco-2 cell monolayer].

To investigate the active fraction from Bletilla striata in Caco-2 cell monolayer,so as to explore its absorption mechanism of oral administration preliminarily.Active fraction from B.striata in Caco-2 cell monolayer was analyzed by UPLC-Q-TOF and detected by UPLC-MS/MS,and the effects of different concentrations,pH and P-glycoprotein inhibitors on Caco-2 cells Monolayer were investigated.

[Effects of Lidocaine on the Rho/ROCK Signal Transduction of the Posterior Basilar Artery in Rabbit SAH].

Objective: To observe the expression of Rho/Rho-associated kinase (ROCK) signaling pathway in the basilar artery and the effect of lidocaine on this signaling pathway after subarachnoid hemorrhage (SAH) in rabbits.

Methods: 24 New Zealand white rabbits were randomly divided into sham operation (sham) group, SAH group, and occipital cisterna lidocaine (CD) group. There were 8 rabbits in each group.

[Left ventricle segmentation in echocardiography based on adaptive mean shift].

The use of echocardiography ventricle segmentation can obtain ventricular volume parameters, and it is helpful to evaluate cardiac function. However, the ultrasound images have the characteristics of high noise and difficulty in segmentation, bringing huge workload to segment the object region manually. Meanwhile, the automatic segmentation technology cannot guarantee the segmentation accuracy.

[Neuroprotection Mechanism of Lidocaine in Rabbits with Early Brain Injury Resulted from Subarachnoid Hemorrhage].

Objectives: To determine the neuroprotection mechanism of lidocaine on early brain injury resulted from subarachnoid hemorrhage.

Methods: Eighteen New Zealand white rabbits were randomly divided into three groups: Sham group, subarachnoid hemorrhage (SAH) group and lidocaine treatment (LD) group. Operations were performed on all animals under anesthesia.

Cationic liposomes induce cell necrosis through lysosomal dysfunction and late-stage autophagic flux inhibition.

Aim: The application of cationic liposomes (CLs) as nonviral vectors is hampered by their cellular toxicity. Thus we aim to investigate the mechanisms underlying the cellular toxicity of CLs.

Materials & Methods: The effect of CLs on the autophagic flux, autophagosome-lysosome fusion, lysosome membrane permeabilization and cell necrosis of liver cells was investigated.

miRNA: A Novel Link Between Rice Ragged Stunt Virus and Oryza sativa.

Rice ragged stunt disease caused leads to severe loss of rice yield. Recently, rice ragged stunt virus (RRSV) were found to be increasingly common in rice-growing regions of China and Vietnam. RRSV may cause problem by interacting with microRNAs (miRNAs) of host cells and the mechanism is not clear yet.

Intermittent administration of human parathyroid hormone (1-34) increases fixation of strontium-doped hydroxyapatite coating titanium implants via electrochemical deposition in ovariectomized rat femur.

Previous studies have demonstrated the effect of human parathyroid hormone (1-34) (PTH) or strontium-doped hydroxyapatite coating (Sr-HA) on osteoporotic bone implantation. However, reports about effects of PTH plus Sr-HA on bone osseointegration of titanium implants in a state of osteoporosis were limited. This study was designed to investigate the effects of intermittent administration of human parathyroid hormone (1-34) on strontium-doped hydroxyapatite coating (Sr-HA) implant fixation in ovariectomized (OVX) rats.

The effects of combined human parathyroid hormone (1-34) and simvastatin treatment on osseous integration of hydroxyapatite-coated titanium implants in the femur of ovariectomized rats.

The effect of human parathyroid hormone 1-34 (PTH) and simvastatin (SIM) alone could promote bone healing in osteoporotic osseous integration of the implant, but there are no reports about the combined use of PTH and SIM for promotion of bone healing around implant in osteoporotic settings still limited. This study aims to investigate effects of PTH+SIM on osseous integration of the implant in OVX rats. Female Sprague-Dawley rats were used for this study.

Effect exerted by Teriparatide upon Repair Function of β-tricalcium phosphate to ovariectomised rat's femoral metaphysis defect caused by osteoporosis.

In this study, we tested the effect of Teriparatide (PTH) in combination with β-tricalcium phosphate (β-TCP) as a bone void filler in an ovariectomised rat distal femoral metaphysis model.β-TCP is a completely resorbable synthetic calcium phosphate and the Teriparatide is a drug that can promote bone formation in the condition of osteoporosis. A critical size defect of 3mm in diameter, a through-hole bone defect, was drilled into each distal femur of the ovariectomised rats.