Objective To introduce the treatment efficacy of using allograft muscle ligament anatomical to rebuild anterior cruciate ligament (ACL) of knee joint under the arthroscopy.Methods Sixty-two cases patients with ACL rupture in anterior cruciate ligament reconstruction under arthroscopy.Allograft ligaments were used as graft,a bone tunnel was established in the proximal tibia and distal femur,and the graft was fixed by the extrusion screw.After the operation,the knee joint was fixed for 12 weeks,and the subjective evaluation was carried out according to the Lysholm and Larson knee score standards;in order to assess the stability of the ligament and the functional recovery of the knee joint,objective evaluation was carried out according to Lachman test in patients.Results The preoperative average Lysholm scale was (43.1±2.1) points,the final average score of 2 years after the reconstruction of the ligament was (91.0+2.3) points,there was significant difference (t=3.460,P=0.001).The preoperative average Larson scale was (41.0±2.9) points,the final average score of 2 years after the reconstruction of the ligament was (90.1±3.5) points,there was significant difference (t=3.232,P=0.001).Lachman test results were negative in 62 patients at the end of the review.No serious postoperative complications occurred,no knee infection,deep vein thrombosis and stiffness.All the patients can be completely straight 1 year after operation,knees up to 120 degrees.All patients were satisfied with the function at the end of the follow-up,no joint instability,no re-rupture occurred during the follow-up period.Conclusion Using the allogeneic single beam anatomy of anterior cruciate ligament reconstruction under arthroscopy can obtain satisfactory clinical efficacy.

A series of phthalimide-donepezil (PTA-DPZ) hybrids (5a-e, 6a-l) were designed, synthesized and evaluated as selective inhibitors of acetylcholinesterase (AChE). The results showed that some hybrids had strong AChE inhibitory activity with half maximal inhibitory concentration (IC₅₀) at nanomolar range, which was better than the control drugs galanthamine and tacrine, and equivalent to DPZ. Compound 6k exhibited the strongest inhibition to AChE with an IC₅₀ value of 0.13 μmol·L^-1. Kinetic and molecular modeling studies showed that 6k targeted both catalytic active site and peripheral anionic site of AChE. Moreover, some compounds could inhibit AChE-induced β-amyloid (Aβ) aggregation. In addition, absorption, distribution, metabolism and excretion prediction results showed 6k conforms to the Lipinski's rule of five and had high partition coefficient P value. These compounds, especially 6k, may be considered as a dual-functional lead compound for in-depth research.

Objective To assess the clinical threatment results of pilon fractures managed with arthroscopyassisted minimally invasive percutaneous plate osteosynthesis (MIPPO).Methods 33 patients with pilon fractures were classified into 3 groups according to the Ruedi-Allgower classification:type Ⅰ in 26 cases,type Ⅱ in 5 cases,type Ⅲ in 2 cases,including 29 males and 4 females,aged 22 to 51 years,mean 31.5 years of age.All patients were treated with arthroscopy-assisted MIPPO with the postoperative follow-up time of 12 to 84 months.Results The clinical surgery efficacy according to Mazur's criterion was evaluated as excellent in 22 cases,good in 8 cases,fair in 3 cases.The excellent and good rate was 90.9％.Conclusion Arthroscopy-assisted MIPPO surgical treatment is an effective method for Pilon fractures with the advantages of good healing,minimal trauma and less complications,it is worthy of clinical application.

Objective To assess the efficiency of total laminectomy and transpedicular screw placement techniques and a thoroughly decompression with a three column fixation device on the early cervical spine cord injury.Methods 27 patients were operated successfully with total cervical laminectomy through transpedicular screw techniques.Precise measurements of all cervical spines were made by postoperative CT scan of pedicle dimensions,angulation,and offset relative to the lateral mass boundaries.And meanwhile,cortical integrity and neurovascular injury were then assessed by obtaining postoperative computed tomography scans of each patient.Results Using manual techniques,220 pedicles were instrumented and all the cases were followed up between three to twenty-four months.The postoperative gradations were obviously better than the preoperative evaluation.Regardless of the technique used,the vertebral artery was the structure most likely to be injured.Conclusion Insufficient correlation between different surgeons' assessments of surface landmarks attests to the inadequacy of screw insertion techniques in the cervical spine based on such specific topographic.At the early stage of cervical spinal cord injury,using total laminonectomy decompression through cervical screws techniques to reconstruct spinal alignment could improve the prognosis of patients.

A series of tacrine-phenol-bifendate hybrids (7a-7e, 8a-8e) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs) with low hepatotoxicity. All the compounds had potent ChEs inhibitory activity with half-inhibitory concentration (IC₅₀) values at the nanomolar range. Compound 8d exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC₅₀ value of 156.39 nmol·L^-1 and compound 7b showed the most potent inhibition for butyrylcholinesterase with IC₅₀ value of 16.33 nmol·L^-1. Kinetic and molecular modeling studies showed that 8d targeted both the catalytic active site and the peripheral anionic site of AChE. In addition, these compounds showed low toxicity to hepatocytes, and compound 8d did not increase the level of reactive oxygen species in HepG2 cells.

Objective To evaluate the effect of mild hypothermia on the renal ischemia-reperfusion injury (IRI), and the expression profile of RNA-binding motif protein 3(RBM3) and its downstream effector molecules during this process. Methods Eighteen healthy SD male rats were randomly divided into the normal control (NC) group, IRI group and mild hypothermia pretreat (MHP) group, with 6 rats in each group. Serum creatinine level was measured to evaluate the renal function. Hematoxylin-eosin (HE) staining was performed to assess the renal tissue injury. Western blot was used to determine the relative expression levels of RBM3, Yes-associated protein 1(YAP1), nuclear factor E2-related factor 2(Nrf2), B cell-lymphoma-2(Bcl-2) and Bcl-2-associated X protein (Bax) in the kidney tissues. Immunohistochemical staining was employed to further detect the expression levels of RBM3 and YAP1 proteins. Terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) assay was adopted to detect the cell apoptosis of kidney tissues. Malondialdehyde (MDA) content and superoxide dismutase (SOD) activity were evaluated to determine the oxidative stress level of kidney tissues. Results Compared with the NC group, the serum creatinine level, the pathological injury score of kidney tissues and the expression levels of RBM3, YAP1 and Nrf2 proteins were significantly up-regulated, the Bcl-2/Bax ratio was considerably lower, the apoptosis rate was remarkably elevated, the MDA content was significantly increased and the SOD activity was dramatically reduced in the IRI and MHP groups (all P < 0.05). Compared with the IRI group, the serum creatinine level and the pathological injury score of kidney tissues were significantly decreased, the expression levels of RBM3, YAP1 and Nrf2 proteins were significantly up-regulated, the Bcl-2/Bax ratio was considerably higher, the apoptosis rate was significantly decreased, the MDA content was significantly decreased and the SOD activity was considerably elevated in the MHP group (all P < 0.05). Conclusions Mild hypothermia may exert protective effect upon renal IRI and it could alleviate cell apoptosis and oxidative stress injury induced by IRI, probably by up-regulating the expression level of RBM3 and its downstream effector molecules of YAP1 and Nrf2.

A novel series of bis-nicotine derivatives (3a-3i) were designed, synthesized and evaluated as bivalent anti-Alzheimer's disease agents. The pharmacological results indicated that compounds 3e-3i inhibited both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in the micromolar range (IC50, 2.28-117.86 micromol x L(-1) for AChE and 1.67-125 micromol x L(-1) for BChE), which was at the same potency as rivastigmine. A Lineweaver-Burk plot and molecular modeling study showed that these derivatives targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, these compounds could significantly inhibit the self-induced Abeta aggregation with inhibition activity (11.85%-62.14%) at the concentration of 20 micromol x L(-1).
Acetylcholinesterase ; metabolism ; Amyloid beta-Peptides ; antagonists & inhibitors ; metabolism ; Binding Sites ; Butyrylcholinesterase ; metabolism ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Nicotine ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology

A series of genistein-polyamine conjugates (4a-4h) were designed, synthesized and evaluated as multi-functional anti-Alzheimer agents. The results showed that these compounds had significant cholinesterases (ChEs) inhibitory activity. Compound 4b exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC50 value of 2.75 μmol/L, which was better than that of rivastigmine (5.60 μmol/L). Lineweaver-Burk plot and molecular modeling study showed that compound 4b targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, compound 4b showed potent metal-chelating ability. In addition, it was found that 4a-4h did not affect HepG-2 cell viability at the concentration of 10 μmol/L.

To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard, the intermediate 4-[N,N-bis(2-chloroethyl) amino] benzoic acid 4 was prepared in four steps utilizing p-amino benzoic acid as the starting material. Target compounds were synthesized by the catalytic esterification of DCC/DMAP and the structures of the six new esters were characterized by elemental analysis, 1H NMR, 13C NMR and MS. Antitumor activities were evaluated in vitro using MTT assay. The result showed that some derivatives were more potent than the intermediate 4, and compound 5c modified with dodecanol exhibited similar activity to the commercial drug melphalan.
Aminobenzoates ; chemical synthesis ; pharmacology ; Animals ; Antineoplastic Agents, Alkylating ; chemical synthesis ; pharmacology ; CHO Cells ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Cricetinae ; Cricetulus ; Humans ; Inhibitory Concentration 50 ; K562 Cells ; Melanoma, Experimental ; pathology ; Melphalan ; pharmacology ; Nitrogen Mustard Compounds ; chemical synthesis ; pharmacology

A series of tacrine-methoxybenzene hybrids (5a-5i) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). All the compounds had better ChEs inhibitory activities than tacrine with IC50 values at the nanomolar range. Compound 5h exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 6.74 nmol x L(-1) and compound 5f showed the most potent inhibition on butyrylcholinesterase with IC50 value of 3.83 nmol x L(-1). Kinetic and molecular modeling studies showed that these hybrids targeted both the catalytic active site and the peripheral anionic site of AChE.
Acetylcholinesterase ; metabolism ; Anisoles ; chemical synthesis ; chemistry ; pharmacology ; Binding Sites ; Butyrylcholinesterase ; metabolism ; Catalytic Domain ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Inhibitory Concentration 50 ; Tacrine ; chemical synthesis ; chemistry ; pharmacology