Design, synthesis of novel N, N'-bis-(halogenophenyl)-4- methoxybenzene-1, 3-disulfonamides and evaluation of their anti-platelet aggregation activity / 药学学报

Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.

Feasibility of in vivo isotope labeled autologous mononuclear bone marrow cells monitoring post cardiac transplantation in a swine model of myocardial infarction / 中华心血管病杂志

<p><b>OBJECTIVE</b>To observe in vivo stem cell distribution and viability after transplantation by noninvasive imaging of 18F-fluorodeoxyglucose (18F-FDG) labeled autologous mononuclear bone marrow cells.</p><p><b>METHODS</b>Myocardial infarction was established in 8 swine by ligating left anterior descending coronary artery after anesthesia. Bone marrow (20 ml) was drawn through ileum. After isolation, mononuclear bone marrow cells were labeled by radionuclide 18F-FDG and intramyocardially injected into infarction region. Whole body planar scan and myocardial tomography scan were performed immediately, 1 h, 2 h, and 3 h post stem cell injection. Viability and stability of radionuclide labeled stem cells were determined at 3 h post labeling in vitro.</p><p><b>RESULTS</b>The labeling efficiency was (67 +/- 14)%. Mean dose of radioactive in marrow cells was (32 +/- 7) MBq. Trypan blue staining showed in vitro viability was (95 +/- 3)% at 3 h post labeling. After intramyocardial injection, labeled mononuclear bone marrow cell retention rate in infarction region was (83 +/- 6)%, (49 +/- 8)%, (32 +/- 6)% and (24 +/- 5)% immediately, 1 h, 2 h, and 3 h post injection, respectively.</p><p><b>CONCLUSIONS</b>Distribution and viability of stem cell after cardiac transplantation could be effective monitored by 18F-FDG labeled autologous mononuclear bone marrow cell technique in acute stage in this model.</p>

Impact of viable myocardium assessed by 99Tcm-MIBI SPECT and 18F-FDG PET imaging on clinical outcome of patients with left ventricular aneurysm underwent revascularization / 中华心血管病杂志

<p><b>OBJECTIVE</b>To evaluate the impact of viable myocardium assessed by (99)Tc()m-MIBI SPECT and (18)F-fluorodeoxyglucose (FDG) PET imaging in patients with left ventricular aneurysm (LVA) underwent revascularization (RVS).</p><p><b>METHODS</b>Forty-six consecutive patients with LVA (mean LVEF 36% +/- 7%), underwent (99)Tc(m)-sestamibi SPECT and (18)F-FDG PET examinations and received RVS therapy, were followed-up for a mean period of 80 +/- 27 months. Viable myocardium in aneurysm was defined as perfusion-metabolism mismatch score (MMS) >/= 2.0. Patients were divided into four groups by aneurysm viability and aneurysmectomy. Group A1 (n = 8): viability-; Group A2 (n = 15): viability-, aneurysmectomy; Group B1 (n = 10): viability +; and Group B2 (n = 13): viability +, aneurysmectomy.</p><p><b>RESULTS</b>The cardiac event rates during follow up were similar among groups [A1 (25%, 2/8), B1 (40%, 6/15), A2 (20%, 2/10) and B2 (31%, 4/13; P > 0.05)]. After revascularization, LVEF was improved (> 10%) in groups A2, B1 and B2 (P < 0.05). Multivariate logistic regression analysis showed that LV-MMS (OR = 2.34, 95% CI 1.08 - 5.06, P < 0.05), distal vessel disease (OR = 0.008, 95% CI 0.001 - 0.560, P < 0.05) and nonaneurysm perfusion score (OR = 0.24, 95% CI 0.07 - 0.85, P < 0.05) were significantly associated with the improvement of LVEF after revascularization.</p><p><b>CONCLUSIONS</b>Long term cardiac events rate post revascularization was not affected by viable myocardium or aneurysmectomy in LVA patients. Viable myocardium in LVA patients was associated with better LVEF improvement after revascularization.</p>