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).

Objective To detect the levels of CD+4 CDHi25 CDLo127 regulatory T (Treg) cells and NKG2D-expressing NK cells in peripheral blood of lung cancer patients and investigate their relationship,and explore their roles in the immune escape of lung cancer and clinical significance.Methods The levels of CD+4 CDHi25 CDLo127 Treg cells,NK cells and NKG2D-expressing NK cells were measured in peripheral blood of 70 lung cancer patients and 50 healthy controls.Results Compared with control group,the levels of CD+4 CDHi25 CDLo127 Treg cells enormously increased [(8.4±4.1) ％,(6.7±1.7) ％] (t =3.09,P ＜ 0.05),while the value of NKG2D obviously decreased [(83.3±4.9) ％,(87.4±2.9) ％] (t =3.16,P ＜ 0.05); And the group of NK cells is not different [(15.6±8.3) ％,(17.2±4.2) ％] (t =-1.33,P ＞ 0.05); NKG2D-expressing NK cells had a perfect negative correlation with CD+4 CDLo25 CDLo127 Treg cells (r =-0.302,P ＜ 0.05).Conclusion Accumulation of Treg cells in serum may lead to the down-modulation of NKG2D-expressing NK which participates the tumor immune escape.They may be potential indicators evaluating immune functions and prognosis of lung cancers.

Objective To investigate early changes of angiopoietin-2(Ang-2)in multiple trauma patients and assess its clinical significance.Methods Forty-five multiple trauma patients aged 2060 years admitted to the hospital within one hour after injury were randomly divided into three groups according to injury severity score(ISS).Blood specimens were obtained immediately upon arrival in the emergency department and plasma samples were assayed for comparing changes of Ang-2,TNF-a and IL-6.Meanwhile,plasma level of Ang-2 was measured and analyzed under different oxygenation index,shock index and base deficit.Results Plasma level of Ang-2 was positively correlated with ISS(P ＜ 0.01)and was concordant with the plasma levels of TNF-a and IL-6(P＜0.01).Furthermore,plasma level of Ang-2 was elevated upon increase of shock index or decrease of oxygenation index(P ＜ 0.01).Plasma level of Ang-2 was elevated with the increase of base deficit(P ＜ 0.01).Conclusions High level of Ang-2 is a marker of endothelial activation and dysfunction early after trauma.Ang-2 is related tightly with the injury severity,inflammation factors,systemic oxygenation and tissue hypoperfusion and may have a tight relation with pathophysiological development and clinical outcome after trauma.

Objective The aim of this study is to investigate CD+8 natural killer T cell receptors NKG2D and NKG2A expression in peripheral blood of patients with lung cancer and discuss the relation between imbalance expression of NKG2A and NKG2D and tumor immune escape. Methods Flow cytometry was used to determine the percentage of NKG2D and NKG2A-expressing of CD+8 NKT cells in peripheral blood of 95 untreated lung cancer patients and 50 healthy controls. Results NKG2D was lower expressed on CD+8 NKT in lung cancer, the level of NKG2D in patients (77.07±5.77) % was significantly lower than that in the controls (84.13±4.49) % (t =8.14, P <0.05). In the TNM stage, the level of NKG2D in patients of Ⅰ-ⅢA, ⅢB, Ⅳ stage were (81.07±5.02) %, (76.95 ±4.70)%, (72.80±5.16) %, respectively, the level of NKG2D was significantly decreased in order (F =18.74, P <0.05). NKG2A was expressed higher on CD+8 NKT in lung cancer, the level of NKG2A in patients (33.58±8.82) % was significantly higher than that in the controls (25.31 ±8.38) % (t =-5.46, P<0.05). In the TNM stage, the level of NKG2A in patients of Ⅰ - Ⅲ A, ⅢB, Ⅳ stage were (25.10±6.93) %, (33.24±3.76) %, (43.64±6.10) %, respectively, the level of NKG2A was significantly increased in order (F =75.73,P <0.05). Conclusion Imbalance expression of NKG2A and NKG2D may restrain the function of CD+8 NKT cell of lung cancer patients in peripheral blood and that may be one of important factors in tumor immunological escape.

Objective To find the effective therapeutic arrangement through investigating the clinical characteristics of chronic cardiac insufficiency with anaemia. Methods A total of 46 cases of anemia from 315patients who had been admitted to department of cardiology, the First Affiliated Hospital, Harbin Medical University for chronic cardiac insufficiency with anaemia were selected. They were divided into two groups. There were 22 patients in the first group who only accepted treatment to improve cardiac function (normal cardiac, diuretic,vasodilator therapy, etc.), and 24 patients in the second group who accepted treatment to improve cardiac function while receiving anti-anemia therapy treatment, oral ferrous sulfate tablets(0.3 g/tablet), 1 tablet each time, 3 times a day and(or) 2 times per week subcutaneous erythropoietin 3000 U. The hemoglobin(Hb), red blood cell(RBC) ,hematocrit (HCT), left ventricular ejection fraction (LVEF), fractional shortening (FS), stroke volume (SV) , cardiac output(CO) and E peak and A peak ratio(E/A) were observed before and after treatment. By logistic regression, grade grade Ⅱ , Ⅲ , Ⅳ, the incidence of anaemia were 7.9% (10/126), 19.2% (23/120) and 24.6% (17/69),respectively. Grade Ⅱ compared with grades Ⅲ, Ⅳ, the difference was statistically significant (x2 = 4.08, 3.12, all (3.49 ± 0.17) × 1012/L, (0.36 ± 0.08)%, (48.9 ± 3.11)%, (15.6 ± 1.8)%, (38.9 ± 3.7)%, (4.4 ± 1.6)% and (130.7 ±5.75)g/L, (4.12 ± 0.25) × 1012/L, (0.43 ± 0.02)%, (58.5 ± 2.65)%, (18.0 ± 2.5)%, (49.1 ± 7.7)%, (5.1 ± 1.2)%in the first and second groups, respectively. The difference between the two groups was statistically significant(t =value of Hb, RBC, HCT, LVEF, FS,SV, CO were (102.7 ± 6.93)g/L, (3.41 ± 0.12) × 1012/L, (0.35 ± 0.07)%,(47.5 ± 2.86)%, (16.0 ± 2.4)%, (38.2 ± 7.9)%, (3.7 ± 1.4)%, respectively. Compared with those after treatment,the difference was statistically significant (t = 15.632, 13.325, 5.569, 17.182, 3.186, 2.999, 3.074, all P ＜ 0.05);Ⅳ-level relative risk were 1.62, 3.14(P ＜ 0.05 or ＜ 0.01) . Conclusions Based on the standard treatment with treatment of anemia, cardiac contractile function can be improved.

OBJECTIVETo observe the effect of Zhitiaokang capsule (ZTK) on serum insulin-like growth factor-2 (IGF-2) in patients with hyperlipidemia (HLP).

METHODSPatients with HLP were randomly divided into the treated group (n = 124) and the control group (n = 62), they were treated by ZTK and Zhibituo tablet respectively for 8 weeks as one therapeutic course. The changes of blood lipids and serum IGF-2 before and after treatment were observed.

RESULTSZTK could significantly reduce blood lipids and increase serum content of IGF-2.

CONCLUSIONZTK could improve the insulin resistant status and inhibit the development of hyperlipidemia in patients by means of raising serum content of IGF-2 and suppressing vascular endothelial cell apoptosis.

Adolescent ; Adult ; Aged ; Capsules ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Hyperlipidemias ; blood ; drug therapy ; Hypolipidemic Agents ; therapeutic use ; Insulin-Like Growth Factor II ; Male ; Middle Aged ; Phytotherapy ; Proteins ; metabolism

A 52-year-old female patient with Hashimoto encephalopathy was admitted to hospital for clinical treatment, and the findings on MR spectroscopy (MRS) and MR imaging (MRI) in the brain were reported. MRS revealed the decreases in N-acetylaspartate (NAA/Cr=1.19) and myo-inositol peaks, and the elevations in lipid, lactate, glutamate/glutamine multiplet and choline (Cho/Cr=1.21) peaks which supported a cerebral inflammatory change, in addition to multifocal hyperintensities on T2WI and fluid-attenuated inversion recovery (FLAIR) images, slight hyperintensities on diffusion weighted imaging (DWI), hypointensities on T1WI. The atrophy of the brain was revealed on follow-up MRI two years later.
Brain Diseases ; diagnosis ; Encephalitis ; Female ; Hashimoto Disease ; diagnosis ; Humans ; Magnetic Resonance Spectroscopy ; Middle Aged

Objective To evaluate the clinical diagnostic application and operative efficacy of the expression of NKG2D in peripheral blood CD+8 NKT cell and its ligand sMICA in patients with esophageal or cardiac carcinoma.Methods The peripheral blood NKG2D positive CD+8 NKT cell percentage was concomitantly determined by flow cytometry in 53 preoperative patients including 29 postoperative patients with esophageal or cardiac carcinoma and 30 healthy controls.The serum sMICA was determined by ELISA.Results The peripheral blood NKG2D positive CD+8 NKT cell percentage in patients was significantly lower than that in controls [(77.632±8.972) % vs (89.053±6.515) %] (t = -6.113,P ＜0.05); with stage Ⅱ,Ⅲ,Ⅳ,it decreased significantly in order (F = 99.251,P ＜0.01);with lymph node metastasis lower than that without lymph node metastasis (t = -10.384,P ＜0.01); squamous carcinoma was higher than adenocarcinoma (t =9.899,P ＜0.01); postoperative was significantly higher than preoperative (t =-4.319,P ＜0.01).The level of serum sMICA in patients was significantly higher than that in controls [(326.28±85.407) pg/ml vs (210.00±92.560) pg/ml](t =7.292,P ＜0.01); with stage Ⅱ,Ⅲ,Ⅳ,it increased significautly in order (F =63.355,P ＜0.01); with lymph node metastasis higher than that without lymph node metastasis (t =7.770,P ＜0.01); squamous carcinoma was lower than adenocarcinoma (t =-7.593,P＜0.01); postoperative was significantly lower than preoperative (t =7.027,P ＜0.01).Serum sMICA could inhibit peripheral blood CD+8 NKT cell activation receptor NKG2D (F =142.773,P ＜0.05),determination coefficient R2 = 0.7368.Conclusion The level of peripheral blood CD+8NKT cell activation receptor NKG2D and serum sMICA in patients could be an assistant indicator for

Acute Disease ; Animals ; Ginkgo biloba ; Glutathione ; analysis ; Lung ; drug effects ; metabolism ; pathology ; Malondialdehyde ; analysis ; Paraquat ; toxicity ; Phytotherapy ; Plant Extracts ; therapeutic use ; Poisoning ; drug therapy ; Rats ; Superoxide Dismutase ; analysis ; Treatment Outcome

Cycloartane triterpenoids, which exist widely in nature, are mainly distributed in Astragalus (Leguminosae) species, Trib. Cimicifuga (Ranunculaceae) and Thalictrium (Ranunculaceae) species and possess various bioactivities. Along with the development of isolation techniques of phytochemistry, more and more this kind of compounds are isolated and identified. However, bioactivity researches on the compounds are relatively lagged behind. Most researches are still in screening level, deficient in mechanism elucidation, short of action proven in vivo and SAR analysis. The author summarized the bioactivity of this kind of compounds from all aspects: anti-tumor, anti-virus, antibacterial, anti-inflammation, immune-regulatory, cardiovascular system, hepatic protection and so forth. This will be benefit for the further research and development of the compounds.
Animals ; Anti-Infective Agents ; isolation & purification ; pharmacology ; Anti-Inflammatory Agents ; isolation & purification ; pharmacology ; Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Astragalus Plant ; chemistry ; Cimicifuga ; chemistry ; Humans ; Plants, Medicinal ; chemistry ; Thalictrum ; chemistry ; Triterpenes ; isolation & purification ; pharmacology