Identification of metabolites of antitumor lead compound T-OA in rat urine by HPLC-HRMS / 中国中药杂志

<p><b>OBJECTIVE</b>To study the major metabolites of antitumor lead compound T-OA (oleanolic acyl-3, 5, 6-trimethyl pyrazine-2-methyl ester) in rat urine, in order to preliminarily infer its metabolic mode in rats.</p><p><b>METHOD</b>Rat urines of the blank group, the raw material group (ligustrazine TMP and oleanolic acid OA Moore equivalent) and the T-OA group were collected and freeze-dried; Solids were extracted by ethyl acetate; And then the extracts were re-dissolved with acetonitrile. HPLC-HRMS coupling technique was adopted to find the potential mass spectrum peak under ESI(+) (see symbol) ESI(-) modes. Metabolite-related information was obtained by comparing the three groups of spectra.</p><p><b>RESULT</b>One metabolite of OA and two metabolites of TMP were identified in the raw material group; none metabolite of T-OA but one phase II metabolite was detected in the T-OA group.</p><p><b>CONCLUSION</b>It is the first time to identify one phase II metabolite of T-OA and one phase II metabolite of OA were identified in rat urine. On that basis, the researchers preliminarily inferred that T-OA does not show the efficacy in the form of raw material. The HPLC-HRMS method established could be used to identify metabolites of related derivative structures. This paper could also provide certain reference for designing pro-drugs based on oleanolic acid.</p>

Synthesis and protective effect of ligustrazine intermediates against CoCl2-induced neurotoxicity in differentiated PC12 cell / 中国中药杂志

Ligustrazine, one of the major effective components of the Chinese traditional medicinal herb Ligusticum Chuanxiong Hort, has been reported plenty of biological activities, such as protect cardiovascular and cerebrovascular, neuroprotection and anti-tumor, et al. Because of its remarkable effects, studies on structural modification of ligustrazine have attracted much attention. Ligustrazine synthetic derivatives reported in recent decades are mainly derived from four primary intermediates (TMP-COOH, TMP-OH, TMP-NH2, HO-TMP-OH). To explore the neuroprotection activitiy of ligustrazine intermediates, six ligustrazine intermediates (2, 5, 8, 11, 12, 13) were synthesized and their protective effects against CoCl2-induced neurotoxicity in differentiated PC12 cells were studied. The target compounds were prepared via different chemical methods, including oxidation, substitution, esterification and amidation without changing the structure nucleus of ligustrazine. Compared with TMP (EC50 = 56.03 micromol x L(-1)), four compounds (2, 5, 12 and 13) exhibited higher activity (EC50 < 50 micromol x L(-1)) respectively, of which, compound 2 displayed the highest protective effect against the damaged PC12 cells (EC50 = 32.86 micromol x L(-1)), but target compounds 8 and 11 appeared lower activity (EC50 > 70 micromol x L(-1)). By structure-activity relationships analysis, the introduction of carboxyl, amino to the side chain of ligustrazine and appropriately increase the proportion of ligustrazine may contribute to enhance its neuroprotective activity, which provides a reference for the design, synthesis and activity screening of relevant series of ligustrazine derivatives in the future.

Computed tomographic demonstrations of HIV seropositive pulmonary tuberculosis and their relationship with CD4+ T-lymphocyte count / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Factors of cell-mediated immunity and allergy together play their roles in the pathogenesis of pulmonary tuberculosis (PTB) and its prognosis. The purpose of this study was to investigate the computed tomographic demonstrations of HIV seropositive PTB and the relationship between its pathogenesis and CD4(+) T-lymphocyte count.</p><p><b>METHODS</b>The documented CT images of a total of 44 patients with HIV seropositive PTB, definitely diagnosed by etiological or pathological examinations, their clinical data and their CD4(+) T-lymphocyte count were retrospectively reviewed.</p><p><b>RESULTS</b>There were 15 cases of miliary tuberculosis, accounting for 34.1% of the total cases; 15 cases of nodular tuberculosis, 34.1%; 6 cases of ground-glass opacity, 13.6%; 5 cases of cord-liked fiber shadows, 11.4%; 16 cases of flaky and flocculating shadows, 36.4%; 5 cases of cavitation, 11.4%; 5 cases of tumor shadows, 11.4%; 2 cases of pleural thickening, 4.5% and 11 cases of pleural effusion, 25.0%; 1 case of calcification, 2.3%; 16 cases of lymphadenectasis, 36.4%. The foci were located around the pulmonary hilum, anterior segment of superior lobe, basal segment of inferior lobe, medial lobe and lingual lobe. CD4(+) T-lymphocyte count was closely related to the imaging demonstrations of HIV seropositive PTB.</p><p><b>CONCLUSIONS</b>CT scanning can demonstrate various signs of PTB. CD4(+) T-lymphocyte level determines the variety of imaging demonstrations of HIV seropositive PTB and its prognosis.</p>

Diagnostic imaging, preautopsy imaging and autopsy findings of / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Aquired immune deficiency syndrome (AIDS) presents a challenge to medical researchers because of its unique pathological and clinical picture. The clinical data, particularly autopsy evidence, from China have failed to provide enough pathological and etiological evidence for AIDS diagnosis, which impairs the reliability of the diagnosis and our full understanding of the occurrence and development of AIDS complications. The purpose of this study was to investigate the imaging and pathologic characteristics of AIDS.</p><p><b>METHODS</b>Autopsy, imaging and pathological data from 8 cases of AIDS were retrospectively analyzed. Routine CT scanning of different body parts was performed during their periods of hospitalization. Transverse CT scanning was conducted from the skull to the pelvis immediately after the occurrence of death. After routine formalin fixing, 7 cardevers were cross sectioned for autopsy in freezing state and 1 for gross autopsy. Tissues were obtained from each section and organs for pathological examinations.</p><p><b>RESULTS</b>The autopsy data indicated the presence of parasitic infections, bacterial infections, fungal infections, and virus infections in AIDS patients. Pneumocystis pneumonia, pulmonary tuberculosis, coccobacteria pneumonia, Aspergillus pneumonia, cytomegalovirus pneumonia, toxoplasma encephalitis, lymphoma and cerebrovascular diseases were found in these patients.</p><p><b>CONCLUSIONS</b>During the course of AIDS progression, the concurrent multiple infections as well as tumor development may result in multiple organ pathological changes and clinically complex symptoms that further complicate the imaging and pathological manifestations, thus resulting in difficult differential diagnosis. A combination of imaging data and autopsy data can help to clarify the diagnosis.</p>

Design and preliminary clinical application of a new digitalized navigation template for fixation of the inferior tibiofibular joint / 南方医科大学学报

<p><b>OBJECTIVE</b>To design and prepare a new digitalized navigation template for fixation of inferior tibiofibular joint using three-dimensional reconstruction and reverse engineering techniques.</p><p><b>METHODS</b>Five patients with inferior tibiofibular joint rupture without fibula fracture underwent three-dimensional CT scanning of the lower limbs. The image data were transferred into Mimics software, and after reconstruction of the three-dimensional models of inferior tibiofibular joint rupture and saving in .stl format, the three-dimensional models were imported into Imageware10.0 software to determine the three-dimensional plane of reference. The location of the optimal pedicle channel was defined using reverse engineering and AO internal fixation principle. The template was designed according to the anatomic features of the fibular surface, and the optimal pedicle channel and the template were overlapped as the navigational template, which was manufactured by rapid prototyping. The inferior tibiofibular joint was reduced and the template was placed distally on the external fibula, and the location for screw insertion was defined by the navigation template.</p><p><b>RESULTS AND CONCLUSION</b>The digitalized model of the inferior tibiofibular joint was established. The navigation template manufactured offered good compatibility and was applied successfully for fixation of the inferior tibiofibular joint. This approach provides a new means for fixation of ruptured inferior tibiofibular joint using the reverse engineering and digitized 3-dimensional reconstruction techniques.</p>

Dynamic enhanced scanning of the pulmonary nodules with 16-slice spiral CT / 南方医科大学学报

<p><b>OBJECTIVE</b>To assess the value of dynamic enhanced CT scanning in diagnosis of pulmonary nodules.</p><p><b>METHODS</b>Sixty-nine patients with pulmonary nodules underwent examination with dynamic enhanced CT scanning. Of these patients, 53 with definite diagnoses confirmed by histological or clinical data were divided into three groups according to the nature of the nodules, namely the malignant group (n=34), benign group (n=13) and active inflammatory group (n=6). The time-density curve (T-DC) and the corresponding parameters of these patients were compared.</p><p><b>RESULTS</b>Significant differences in the net enhancement and S/A ratio were found among the 3 groups (P<0.001). The active inflammatory nodules showed the highest enhancement, followed by malignant nodules and then by benign nodules, with significant differences between any of the two groups (P<0.05). At the diagnostic threshold of net enhancement by 25 Hu or S/A ratio by 10% for malignant nodules, a higher negative predictive value and accuracy were obtained. The difference in the wash-out value among the 3 groups was statistically significant (P<0.05). When diagnostic criteria for malignancy was defined by a wash-in value of 25 Hu or higher and wash-out value of 0-35 Hu, the false-positive rate was decreased from 57.89% to 47.37%.</p><p><b>CONCLUSION</b>The application of 16-slice spiral CT and its CT perfusion software allows convenient dynamic enhancement study of pulmonary nodules and can be helpful in their differential diagnosis.</p>

Hemodynamic study of primary hepatocellular carcinoma evolved from viral-induced cirrhosis using CT perfusion imaging / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the hemodynamic changes of primary hepatocellular carcinoma (HCC) evolved from hepatic cirrhosis using CT perfusion imaging.</p><p><b>METHODS</b>Thirty-two patients with primary hepatocellular carcinoma evolved from virus-induced fibrosis or cirrhosis underwent dynamic CT scanning of the target slices for 60 min. The perfusion parameters of the hepatic parenchyma and HCC including the blood flow (BF), blood volume (BV), mean transit time (MTT), permeability-surface area product (PS), hepatic arterial fraction (HAF), IRF time of arrival (IRF TO) were obtained. Paired-sample t test was used to determine the differences in the perfusion parameters between the hepatic parenchyma and the primary HCC mass.</p><p><b>RESULTS</b>Compared with hepatic BF (117.13-/+31.05 ml/100 mg/min), BV (14.73-/+3.91 ml/100 mg), PS (31.93-/+5.91 ml/100 mg/min), HAF (25.02-/+8.19%), MTT (12.79-/+3.31 s), IRF TO (3.14-/+1.09 s), the primary HCC mass showed significant increments in the BF (239.69-/+96.07 ml/100 mg/min), BV (20.26-/+6.73 ml/100 mg), PS (37.50-/+9.50 ml/100 mg/min), HAF (68.97-/+15.22%) with decreased MTT (7.17-/+1.38 s) and IRF TO (2.42-/+0.94 s). Significant differences were found in all the perfusion parameters between the hepatic parenchyma and HCC (P<0.05).</p><p><b>CONCLUSION</b>Liver perfusion parameters can represent the hemodynamic changes in the HCC derived from hepatic cirrhosis.</p>

High-field MRI and pathological diagnosis of supratentorial primitive neuroectodermal tumors / 南方医科大学学报

<p><b>OBJECTIVE</b>To analyze the magnetic resonance imaging (MRI) features of supratentorial primitive neuroectodermal tumors (sPNET) and improve the diagnosis of this disease.</p><p><b>METHODS</b>MRI manifestations of 14 cases of PNET were retrospectively analyzed and compared with their pathological features.</p><p><b>RESULTS</b>The supratentorial lesions involved the occipital lobe in 4, frontal lobe in 3, fronto-occipital lobe in 2, temporo-occipital lobe in 3, lateral ventricle in 1 case and the saddle region in 1. All the lesions were large in volume and most of them presented heterogeneous signals in MRI. Of the 14 cases, 12 showed cystic degeneration and necrosis, 2 had hemorrhage and 6 showed signs of emptied small blood vessels. Twelve cases had heterogeneous enhancement and 2 had moderate enhancement. Pathologically, 10 cases of neuroblastomas were identified, along with 3 ganglioneuroblastomas and 1 atypical rhabdoid tumor.</p><p><b>CONCLUSION</b>MRI findings of PNET are rather characteristic to assist in the diagnosis and treatment of the disease, but a final definite diagnosis still relies on pathological examination.</p>

Imaging findings of craniopharyngioma in relation to its surgical management: a retrospective analysis / 南方医科大学学报

<p><b>OBJECTIVE</b>To analyze the CT and magnetic resonance imaging (MRI) findings of craniopharygioma and explore the correlation between the pathological findings and clinical features of the disease.</p><p><b>METHODS</b>The CT and MRI findings of 123 pathologically confirmed craniopharygioma cases were reviewed retrospectively in conjunction with the pathological findings and surgical data.</p><p><b>RESULTS</b>This patient cohort consisted of 70 male and 53 female patients with their age ranging from 1 to 72 years (mean 23.82 years). Of the 123 craniopharyngioma patients, 59 were found to have adamantinous craniopharyngiomas, 41 had papillary squamous craniopharyngiomas, and 23 had mixed tumors. Solid tumor was found in 18 cases, cystic tumor in 38 cases, and calcification in 78 cases; in 23 cases, the posterior of the tumor did not exhibit clear boundary from the wall of the three cerebral ventricles, and in 11 cases CT and MRI displayed hypophysial stalk, which was found intraoperatively in 53 cases.</p><p><b>CONCLUSIONS</b>MRI allows clear vision of the range of craniopharyngioma involvement and the anatomical structures surrounding the tumor. CT, on the other hand, shows better performance in displaying the calcification foci. Accurate identification of the site, dimension, calcification patterns and relation between the hypophysial stalk and hypothalamus by the imaging modalities significantly benefits the optimization of the surgical plan for the tumor.</p>

Preparation and characterization of superparamagnetic iron oxide nanoparticles / 南方医科大学学报

<p><b>OBJECTIVE</b>To determine the physical and magnetic properties of superparamagnetic iron oxide (SPIO) nanoparticle prepared in our laboratory and evaluate its possibility for use as contrast agents in magnetic resonance imaging (MRI).</p><p><b>METHODS</b>The SPIO nanoparticle was obtained by means of classical coprecipitation in dextran solution and its size determined by electron microscopy and photon-correlation spectroscopy. The iron content was determined by phenanthroline photometry, and T(2) values as well as relaxivity evaluated with a clinical MR system at 1.5T.</p><p><b>RESULTS</b>Dextran-coated magnetite particles with a hydrodynamic diameter of 85.9 nm were prepared. The iron core size was 15 nm and the formation of Fe(3)O(4) crystal in SPIO nanoparticles was confirmed by X-ray diffraction (XRD) analysis. These particles possessed some characteristics of superparamagnetic and show a smaller spin-spin relaxation, with relaxivity and saturation magnetization of 0.1567 mmol(-1)/ms(-1) and 80 emu/g Fe, respectively.</p><p><b>CONCLUSIONS</b>A stable SPIO nanoparticle with a dextran coating have been developed, and in vitro evaluation of its physical and magnetic properties suggests its potential for use as the contrast agent in MRI.</p>

Phase-contrast magnetic resonance angiography for assessment of intracranial venous sinus lesions / 南方医科大学学报

<p><b>OBJECTIVE</b>To review the presentations of intracranial venous sinus lesions in phase-contrast (PC) magnetic resonance angiography (MRA) and discuss the diagnostic value of this imaging modality for these lesions.</p><p><b>METHODS</b>This study involved 52 patients with intracranial venous sinus lesions, including 21 with dural venous sinus malformation, 7 dural arteriovenous fistula (6 caroticocaveneous fistula, CCF), 5 venous sinus thrombus and 19 meningioma invading the venous sinuses. All patients underwent PC and time-of-flight (TOF) MRA with a 1.5 Tesla MR scanner, with 28 of them undergoing subsequent digital subtraction angiography (DSA).</p><p><b>RESULTS</b>PC MRA showed extensive hyperintense signals that identified the lesions, feeding arteries, deferent veins and venous sinuses in 21 cases of dural arteriovenous fistula, but the lesion signals appeared homogeneous. In these cases, PC and TOF MRA had equally good performance in displaying the feeding arteries with success in 20 of the 21 cases (95.2%), whereas the former resulted in a greater rate of deferent vein display [90.5% (19/21)] than the latter [76.2% (16/21), P<0.05]. The 6 CCF cases showed ipsilateral cavernous sinus expansion and upper ophthalmic vein dilations. In the 5 cases of venous sinus thrombis, 4 had transverse sinus thrombus and 1 superior sagittal sinus thrombus. All the cases presented signal disappearance in the sinuses in PC MRA and hyperintense signals in MRI, and some cases had also cerebral superficial hemorrhage and edema. The 19 cases of meningioma invading the venous sinus displayed sinus shift, stenosis and occlusion in PC MRA.</p><p><b>CONCLUSION</b>PC MRA has great advantages in displaying the anatomical structure and lesions of the venous sinuses.</p>

Electrochemical behavior of dopamine at the poly (isonicotinic acid) modified glassy carbon electrode / 药学学报

<p><b>AIM</b>To study the determination of dopamine (DA) in the presence of ascorbic acid (AA) using poly (isonicotinic acid) film modified electrode.</p><p><b>METHODS</b>The cyclic voltammetry and differential pulse voltammetry were used to study the electrochemical behavior of DA at the poly (isonicotinic acid) film modified electrode.</p><p><b>RESULTS</b>The poly (isonicotinic acid) film modified electrode showed an electrocatalytic effect on DA, and shifted the oxidation of AA to negative potential. The difference between the oxidation potentials of DA and AA was 204 mV, thus, AA did not interfere with the determination of DA. The linear range between the anodic currents and DA concentration was: 1.0 x 10(-7)-2.0 x 10(-5) and 2.0 x 10(-5)-1.0 x 10(-4) mol.L-1. The detection limit was 8.0 x 10(-9) mol.L-1.</p><p><b>CONCLUSION</b>The useful life period of the modified electrode is three weeks at least. The modified electrode can be used to the determination of DA in the sample.</p>