Progress of the development of anti-COVID-19 drugs / 药学学报

Since the outbreak of the novel coronavirus (SARS-CoV-2) disease COVID-19 (also known as 2019-nCoV) caused by SARS-CoV-2 in the end of 2019, it has spread rapidly in worldwide. Besides developing effective vaccines, it is urgent to develop safe and effective anti-SARS-CoV-2 drugs to fight this disease. Paxlovid, molnupiravir, sotrovimab and bebtelovimab are urgently authorized by FDA have been proved to be effective against Omicron. This manuscript mainly reviews the recent progress of effective inhibitors against the virus in the world, including receptor inhibitors, antibodies, natural product inhibitors, synthetic inhibitors and broad-spectrum antiviral drugs that are effective against other RNA viruses.

Progresses and analysis in fibrinolytic drugs induced hemorrhage / 药学学报

At present, most clinical thrombolytic drugs are plasminogen activators, which are highly dependent on the plasminogen level of the patient. Therefore, the efficacy of those drugs is restricted. Unlike the conventional thrombolytic plasminogen activator drugs, fibrinolytic drugs have direct fibrinolytic activity. Thus, fibrinolytic drugs can directly dissolve the thrombus, and its thromlysis efficacy is not restricted by the patients' plasminogen. This is a new type of thrombolytic drug with higher thrombolytic efficiency and safety, and has become one of the research hotspots at present. Although more and more agents that can be used as fibrinolytic drugs have been discovered, only a few of them can successfully be applied in clinical practice. The mainly underlying reason is the risk of bleeding. In this paper, based on the latest research progress of fibrinolytic drugs, the bleeding mechanisms and coping strategies of fibrinolytic drugs were systematically reviewed, five types of bleeding mechanisms of fibrinolytic drugs were summarized, and three types of coping strategies were proposed. We hope our work can provide theoretical basis for the development of safer and more efficient fibrinolytic drugs.

18F-FDG hybrid PET/MR radiomics based on different segmentation methods for distinguishing Parkinson′s disease from multiple system atrophy / 中华核医学与分子影像杂志

Objective:To explore the impact of different segmentation methods on differential diagnostic efficiency of 18F-FDG PET/MR radiomics to distinguish Parkinson′s disease (PD) from multiple system atrophy (MSA). Methods:From December 2017 to June 2019, 90 patients (60 with PD and 30 with MSA; 37 males, 53 females; age (55.8±9.5) years) who underwent 18F-FDG PET/MR in Union Hospital, Tongji Medical College, Huazhong University of Science and Technology were retrospectively collected. Patients were randomized to training set and validation set in a ratio of 7∶3. The bilateral putamina and caudate nuclei, as the ROIs, were segmented by automatic segmentation of brain regions based on anatomical automatic labeling (AAL) template and manual segmentation using ITK-SNAP software. A total of 1 172 radiomics features were extracted from T 1 weighted imaging (WI) and 18F-FDG PET images. The minimal redundancy maximal relevance (mRMR) and least absolute shrinkage and selection operator (LASSO) algorithm were used for features selection and radiomics signatures (Radscore) construction, with 10-fold cross-validation for preventing overfitting. The diagnostic performance of the models was assessed by ROC curve analysis, and the differences between models were calculated by Delong test. Results:There were 63 cases in training set (42 PD, 21 MSA) and 27 cases in validation set (18 PD, 9 MSA). The Radscore values were significantly different between the PD group and the MSA group in all training set and validation set of radiomics models ( 18F-FDG_Radscore and T 1WI_Radscore) based on automatic or manual segmentation methods ( z values: from -5.15 to -2.83, all P<0.05). ROC curve analysis showed that AUCs of 18F-FDG_Radscore and T 1WI_Radscore based on automatic segmentation in training and validation sets were 0.848, 0.840 and 0.892, 0.877, while AUCs were 0.900, 0.883 and 0.895, 0.870 based on manual segmentation. There were no significant differences in training and validation sets between Radiomics models based on different segmentation methods ( z values: 0.04-0.77, all P>0.05). Conclusions:The 18F-FDG PET/MR radiomics models based on different segmentation methods achieve promising diagnostic efficacy for distinguishing PD from MSA. The radiomics analysis based on automatic segmentation shows greater potential and practical value in the differential diagnosis of PD and MSA in view of the advantages including time-saving, labor-saving, and high repeatability.

Effects of transurethral resection of the prostate versus plasmakinetic resection of the prostate on erectile function in patients with giant benign prostatic hyperplasia / 中国基层医药

Objective:To investigate the efficacy of transurethral resection of the prostate (TURP) versus plasmakinetic resection of the prostate (PKRP) in the treatment of patients with giant benign prostatic hyperplasia and their effects on erectile function. Methods:A total of 100 patients with GBPH who received treatment in the General Hospital of Taiyuan Iron and Steel (Group) Co., Ltd., from February 2017 to January 2020 were included in this study. They were randomly assigned to undergo either PKRP (PKRP group, n = 50) or TURP (TURP group, n = 50). Perioperative indicators were recorded. Urodynamic indicators and serum indicators pre- and post-operation were compared between the two groups. Erectile function and quality of life were compared between the two groups. The incidences of postoperative complications such as erectile dysfunction, urinary incontinence and urethral stricture were calculated. Results:Operative time, hospital stay, catheter indwelling time, and intraoperative blood loss in the PKRP group were significantly shorter and less than those in the TURP group ( t = 14.35, 8.74, 6.20, 8.34, all P < 0.001). There were no significant differences in residual urine volume and maximum urine flow rate measured before surgery between the two groups ( t = 0.59, 0.73, both P > 0.05). After surgery, residual urine volume decreased and maximum urine flow rate increased in each group. Residual urine volume was significantly lower and maximum urine flow rate was significantly higher in the PKRP group compared with the TURP group ( t = 19.85, 11.67, both P < 0.001). Before surgery, there were no significant differences in serum prostate-specific antigen and free prostate-specific antigen between the two groups ( t = 0.43, 0.33, both P > 0.05). After surgery, both serum prostate-specific antigen and free prostate-specific antigen decreased in each group, and both serum prostate-specific antigen and free prostate-specific antigen were significantly lower in the PKRP group than those in the TURP group ( t = 16.01, 5.09, both P < 0.001). Before surgery, there were no significant differences in quality of life (QOL) score and International Index of Erectile Function (IIEF) score between the two groups ( t = 0.62, 0.63, both P > 0.05). After surgery, IIEF score was increased and QOL score was decreased in each group. After surgery, IIEF score in the PKRP group was significantly higher than that in the TURP group [(25.06 ± 3.61) points vs. (21.52 ± 3.05) points, t = 5.29, P < 0.001], and QOL score in the PKRP group was significantly lower than that in the TURP group [(1.05 ± 0.18) points vs. (1.58 ± 0.29) points, t = 5.29, 10.98, both P < 0.001]. The incidence of complications in the PKRP group was significantly lower than that in the TURP group ( χ2 = 5.98, P < 0.05). Conclusion:This study investigated the effects of TURP versus PKRP on giant benign prostatic hyperplasia from the aspects including erectile function, QOL, and perioperative indicators. This study is of certain innovation. Findings from this study confirm that both PKRP and TURP can improve erectile function, serum indicators, and urodynamic indicators in patients with giant benign prostatic hyperplasia. PKRP is preferred because it is less invasive, results in better improvements in erectile function, serum indicators, and urodynamic indicators, and has fewer complications than TURP.

Clinical application of 99Tc m-sulfur colloid lymphoscintigraphy in the diagnosis of lower limb lymphedema after gynecological tumor surgery / 肿瘤研究与临床

Objective:To explore the significance of 99Tc m-sulfur colloid lymphoscintigraphy in the diagnosis of lower limb lymphedema after gynecological tumor surgery. Methods:The clinical data of patients with lower limb lymphedema after gynecological tumor surgery in Union Hospital Affiliated to Tongji Medical College of Huazhong University of Science and Technology from May 2015 to October 2019 were retrospectively analyzed. 99Tc m-sulfur colloid lymphoscintigraphy was performed in all patients. The results of lymphatic vessel imaging, lymph node imaging and their combination in the diagnosis of lower limb lymphedema were analyzed. The diagnostic efficacy of lymphatic vessel imaging alone, lymph node imaging alone and their combination was evaluated by the receiver operating characteristic (ROC) curve and the area under the curve (AUC), and the Youden index, sensitivity and specificity were calculated. Results:Among the 100 lower limbs of 50 patients, 56 limbs had lymphedema and 44 limbs had no obvious edema. When diagnosis was based on abnormal lymphatic vessel imaging alone, among 56 lower limbs with lymphedema, lower limbs lymphatic vessel imaging was positive in 38 (67.9%) and negative in 18 (32.1%); among 44 lower limbs without obvious edema, lower limbs lymphatic vessel imaging was positive in 6 (13.6%) and negative in 38 (86.4%); the sensitivity was 67.9%, the specificity was 86.4%, and the Youden index was 0.543. When diagnosis was based on abnormal lymph node imaging alone, among 56 lower limbs with lymphedema, lower limbs lymph node imaging was positive in 42 (75.0%) and negative in 14 (25.0%); among 44 lower limbs without obvious edema, lower limbs lymph node imaging was positive in 13 (29.5%) and negative in 31 (70.5%); the sensitivity was 75.0%, the specificity was 70.5%, and the Youden index was 0.455. When diagnosis was based on the combination of lymphatic vessel imaging and lymph node imaging, among 56 lower limbs with lymphedema, lymphatic vessel imaging and lymph node imaging were positive in 48 (85.7%) and negative in 8 (14.3%); among 44 lower limbs without obvious edema, lymphatic vessel imaging and lymph node imaging were positive in 14 (31.8%) and negative in 30 (68.2%); the sensitivity was 85.7%, the specificity was 68.2%, and the Youden index was 0.539. The AUC for the combined diagnosis of lymphatic vessel imaging and lymph node imaging was 0.781, the AUC for the diagnosis of abnormal lymphatic vessel imaging was 0.771, and the AUC for the diagnosis of abnormal lymph node imaging was 0.739 (all P < 0.01). Conclusions:99Tc m-sulfur colloid lymphoscintigraphy is of great help in the diagnosis of lower limb lymphedema after operation of gynecological tumors. The combination of lymph node imaging and lymphatic vessel imaging is more effective in the diagnosis of lower limb lymphedema.

Gegen Qinliantang and Its Combinations Inhibit Oxidative Stress Injury in Ulcerative Colitis Rats by Regulating Nrf2/NQO1 Signaling Pathway / 中国实验方剂学杂志

ObjectiveTo explore the underlying mechanism of Gegen Qinliantang （GGQL） in the treatment of ulcerative colitis （UC） in rats and discuss the effects of modification of GGQL on its efficacy. MethodThe UC model was induced in rats by free access to 5% dextran sulfate sodium in saline solution. Male SD rats were randomly divided into a normal group， a model group， a positive control group （sulfasalazine enteric-coated tablets， 350 mg·kg-1）， a GGQL group （17 g·kg-1）， a Glycyrrhizae Radix et Rhizoma （GR）-absent GGQL group （17 g·kg-1）， a Puerariae Lobatae Radix （PLR）-absent GGQL group （17 g·kg-1）， a GR-PLR group （17 g·kg-1）， and a Scutellariae Radix （SR）-Coptidis Rhizoma （CR） group （17 g·kg-1）. The in vitro antioxidant activities of GGQL and its combinations were evaluated by 2，2-diphenyl-1-picrylhydrazyl （DPPH）， 2，2′-azino-bis（3-ethylbenzothiazoline-6-sulfonic acid） （ABTS）， and fluorescence recovery after photobleaching （FRAP） methods. The degree of colonic tissue injury in each group was evaluated based on the weight changes of rats， the length of the colon， the colon sections， and hematoxylin-eosin （HE）-stained histopathologic sections. The serum levels of myeloperoxidase （MPO）， lipid peroxide （LPO）， malondialdehyde （MDA）， total superoxide dismutase （T-SOD）， catalase （CAT）， and reduced glutathione （GSH） were measured by colorimetry. The mRNA and protein expression of nuclear factor-erythroid 2 related factor （Nrf2）， quinone oxidoreductase 1 （NQO1）， and heme oxygenase-1 （HO-1） in colon tissues was detected by real-time fluorescence-based quantitative polymerase chain reaction （Real-time PCR） and Western blot， respectively. ResultCompared with the normal group， the model group showed colonic mucosal necrosis， inflammatory infiltration， increased serum levels of MPO， LPO， and MDA （P<0.01）， blunted activities of T-SOD， CAT， and GSH （P<0.01）， decreasing trend of mRNA expression of Nrf2， NQO1， and HO-1， reduced expression of Nrf2 protein （P<0.01）， and decreasing trend of expression of NQO1 and HO-1 proteins. Compared with the model group， the GGQL and its combination groups showed improved pathological injury and morphological structure of colon tissues in UC rats， reduced serum levels of MPO， LPO， and MDA （P<0.05）， potentiated T-SOD activity （the PLR-absent GGQL group）， CAT activity （the GR-absent GGQL group and the SR-CR group）， and GSH activity （P<0.01）， and increased mRNA and protein expression of Nrf2， NQO1， and HO-1 in colon tissues. The difference in the GGQL group was significant （P<0.05）. ConclusionGGQL has a restorative effect on the pathological injury of UC rats， and its mechanism may be related to the activation of the Nrf2 signaling pathway and inhibition of oxidative stress response. The absence of PLR or only presence of SR and CR has a great impact on the treatment of UC. The results can provide references for the clinical rational medication of Chinese medicine and the research on the mechanism of compound combinations.

Mechanism of Banxia Xiexintang on Rats with Chronic Gastritis Based on Quantitative Proteomics / 中国实验方剂学杂志

Objective:To study the biological basis of Banxia Xiexintang against chronic gastritis by using quantitative proteomics. Method:The experimental rats were divided into normal group，chronic gastritis model group，and Banxia Xiexintang group. The chronic gastritis model was established four weeks later by gavage with 56% ethanol. After treatment，the stomach tissues were stained with hematoxylin and eosin （HE） to observe the histopathological damage and improvement of gastric tissue in each group. The protein in gastric tissue was extracted. The differential proteins among different groups were studied by quantitative proteomics using tandem mass spectrometry tag（TMT），and the key differentially expressed proteins（DEPs） were verified by Western blot. Result:A total of 4 452 proteins were identified from rat stomach tissues，of which 318 proteins were different between the model and the normal group. After the intervention of Banxia Xiexintang，compared with the model group，there were a total of 258 differential proteins， which were mainly enriched in cell killing，nucleoid and hijacked molecular function. Kyoto encyclopedia of genes and genomes（KEGG） pathway enrichment included tricarboxylic acid（TCA） cycle，steroid hormone biosyntheis，and Retrograde endocannabinoid signaling，as well as phosphatidylinositol 3-kinase（PI3K）/protein kinase B（Akt），nuclear transcription factor-<italic>κ</italic>B（NF-<italic>κ</italic>B） signal pathways. Western blot verification found that 14-3-3 theta，Tenascin-C，ntercellular adhesion molecule-1（ICAM-1），stem cell factor（SCF），Caspase-3，GTPase of the Immunity-associated protein 4（GIMAP4） and mitochondrial pyruvate carrier 1（Mpc1） might be the crucial proteins for the treatment of chronic gastritis. Conclusion:The mechanism of Banxia Xiexintang in the treatment of chronic gastritis involves energy metabolism，hormone regulation，inflammation and immune processes. The target proteins found by differential proteomics and the signaling pathways may be the biological basis of Banxia Xiexintang in the treatment of chronic gastritis.

Revealing the synergistic mechanism of Shenfu Decoction for anti-heart failure through network pharmacology strategy / 中国天然药物

The present study was designed to investigate the targets and synergistic mechanism of Shenfu Decoction (SFD) in the treatment of heart failure. A heart failure animal models was established to evaluate the pharmacological effects of SFD for anti-heart failure, then constructed ingredient-target interaction network by developing ingredient and target databases, the Discovery sdudio software was used for molecular docking. In addition, we validated the predicted protein targets of active ingredients in SFD by using surface plasmon resonance (SPR) technology. Our results demonstrated that SFD could enhance ejection fraction, alleviate myocardial histopathological characteristics, and reduce the level of angiotensin converting enzyme (ACE), aldosterone (ALD), atrial natriuretic polypeptide (ANP) and Renin (REN) in heart failure rat model. In addition, the ingredient database including 349 constituents and target database including 236 proteins were established, and 75 proteins were screened and identified by molecular docking strategy. 22 core target proteins were identified through network pharmacology, and the component-core target network was constructed. Finally, the affinity between the compounds and targets were verified by the SPR analysis method. The present study suggested that SFD may act on ACE 2, REN, ACE, ICAM-1, EGF, HTR2B, PARP1, NPPB and other proteins through AC, BAC, ACN, Re, Rg1, Rb1 to exert synergistic effects against heart failure.

Protection management and procedures of nuclear medicine imaging during novel coronavirus (2019-nCov) infection epidemic period / 中华核医学与分子影像杂志

At the end of December 2019, acute respiratory infectious diseases caused by a new type of coronavirus were prevalent in Wuhan and other cities of China. Different from radiology examinations, the protocols of nuclear medical imaging examinations are complicated, in which more workplaces and staff are needed, resulting more complex management of patients and higher protection requirements. Combined with the characteristics of SPECT and PET imaging procedures, this paper puts forward some suggestions on the protective process of imaging examinations for patients with confirmed or suspected noval coronavirus infec- tion. The main purpose is to protect medical staff from virus infection, effectively reduce the risk of virus transmission during the examination process, and ensure the medical quality and safety.

Protection management and procedures of nuclear medicine imaging during novel coronavirus (2019-nCov) infection epidemic period / 中华核医学与分子影像杂志

At the end of December 2019, acute respiratory infectious diseases caused by a new type of coronavirus were prevalent in Wuhan and other cities of China. Different from radiology examinations, the protocols of nuclear medical imaging examinations are complicated, in which more workplaces and staff are needed, resulting more complex management of patients and higher protection requirements. Combined with the characteristics of SPECT and PET imaging procedures, this paper puts forward some suggestions on the protective process of imaging examinations for patients with confirmed or suspected novel coronavirus infection. The main purpose is to protect medical staff from virus infection, effectively reduce the risk of virus transmission during the examination process, and ensure the medical quality and safety.

Protection management and procedures of nuclear medicine imaging during novel coronavirus (2019-nCov) infection epidemic period / 中华核医学与分子影像杂志

At the end of December 2019,acute respiratory infectious diseases caused by a new type of coronavirus were prevalent in Wuhan and other cities of China.Different from radiology examinations,the protocols of nuclear medical imaging examinations are complicated,in which more workplaces and staff are needed,resulting more complex management of patients and higher protection requirements.Combined with the characteristics of SPECT and PET imaging procedures,this paper puts forward some suggestions on the protective process of imaging examinations for patients with confirmed or suspected novel coronavirus infection.The main purpose is to protect medical staff from virus infection,effectively reduce the risk of virus transmission during the examination process,and ensure the medical quality and safety.

The effect of perioperative fluid therapy on early postoperative pulmonary complications after orthotopic liver transplantation / 中华外科杂志

Objective@#To investigate the effect of perioperative fluid therapy on early postoperative pulmonary complication (PPC) after orthotopic liver transplantation (OLT).@*Methods@#The clinical data of 132 patients who underwent OLT in the First Affiliated Hospital of Xi′an Jiaotong University from April 2016 to December 2017 were analyzed retrospectively. These patients included 96 males and 36 females, aged (47.3±9.6) years (range: 24-69 years). Based on the clinical manifestations, laboratory and imaging findings of patients in ICU and PPC occurrence within 7 days after OLT surgery, the patients were divided into 2 groups: non-PPC group and PPC group. Univariate and multivariate logistic regression analyses were used to evaluate the association between perioperative variables and PPC. The Kaplan-Meier method was used to estimate cumulative survival of recipients with or without PPC within 2-years.@*Results@#During the follow-up, 11 patients (8.3%) died and 72 patients (54.5%) developed PPC after operation. There were 34 cases, 6 cases, 3 cases, 4 cases, 15 cases, 6 cases and 4 cases of only pleural effusion, only pulmonary edema, only pneumonia, pleural effusion with pneumonia, pleural effusion with pulmonary edema, pleural effusion with atelectasis, and pleural effusion with pneumonia and pneumonia in PPC, respectively. Univariate analysis showed that the preoperative factors (model for end-stage liver disease score), the intra-operative factors (duration of surgery, total infusion volume, total blood products) and the postoperative cumulative fluid balance within the first 24 h, 48 h, and 72 h were the prognosis factors of PPC (P<0.05). At least two out of the first three postoperative days with a fluid balance of ≤-500 ml was a protective factor. Using multivariate analysis by Logistic regression, only the red blood units >10 U (OR=3.55, 95% CI: 1.35-9.26, P=0.010) and the cumulative fluid intake >12 L (OR=2.98, 95% CI: 1.14-7.80, P=0.026) within the first 72 h after operation were independent prognosis factors of PPC after OLT. Kaplan-Meier analysis showed that the cumulative survival rate was lower in PPC group than that in non-PPC group (χ2=6.590, P=0.01).@*Conclusion@#Massive red blood cell transfusion and the cumulative fluid volume >12 L during perioperative 72 hours are independent prognosis factors of PPC after OLT.

Simultaneous determination of six constituents in different kinds of Atractylodes rhizome by GC / 中成药

AIM To establish a GC method for the simultaneous determination of β-eudesmol,atractylon,atractylodin,atractylolide Ⅰ,atractylaxanthin Ⅱ and (4E,6E,12E)-tetradecene-8,10-diyne-1,3-diacetate in Atractylodes rhizome,and cluster analysis of A.rhizome according to the content level.METHODS The analysis of A.rhizome solution was performed on an HP-5 capillary column (30 m × 0.32 mm,0.25 μm) with FID as the detector,the initial temperature 100 ℃,with 10 ℃/min to 135 ℃;with 1 ℃/min to 150 ℃;with 50 ℃/min to 200 ℃ (keeping 6 minutes),and with 50 ℃/min to 250 ℃ (keeping 8 minutes).The FID detector temperature was 300 ℃ and the injector temperature was 250 ℃,with the flow rate carrier gas 1.4 L/min;The tail gas was N2 (99.999％),with the ratio of carrier gas Air ∶ H2 ∶ N2 =400 ∶ 30 ∶ 25;The sample volume was 1 μL,and the split ratio was 20 ∶ 1.The results were analyzed by cluster analysis with SPSS 21.0 statistical software.RESULTS Six constituents showed good linear relationships within their own ranges (r ＞ 0.999 6),whose average recoveries were 99.46％-100.95％ with the RSDs of 0.09-0.41.A.rhizome was divided into three categories.CONCLUSION This accurate,stable and reproducible method can be used for the quality control of A.rhizome.

Simultaneous determination of eleven constituents in Huxin Oral Liquid by LC-MS/MS / 中成药

AIM To establish a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the simultaneous content determination of matrine,oxymatrine,salvia acid B,tanshinol,protocatechualdehyde,liquiritin,astragaloside,cinnamaldehyde,tanshinone Ⅱ A,ophiopogonin D and ruscogenin in Huxin Oral Liquid (Glycyrrhizae Radix et Rhizoma,Astragali Radix,Ophiopogonis Radix,etc.).METHODS The analysis of methanol extract of this drug was performed on a 25 ℃ thermostatic Ultimate XB-C18 column (4.6 mm × 100 mm,3 μm),with the mobile phase comprising of water-methanol (containing 0.05％ formic acid) flowing at 0.4 mL/min in a gradient elution manner.RESULTS Eleven constituents showed good linear relationships with-in their own ranges (r ＞0.999 0),whose average recoveries were 96.66％-103.2％ with the RSDs of 1.4％-3.4％.CONCLUSION This sensitive,reliable and accurate method can be used for the quality control of Huxin Oral Liquid.

Application progress of 18F-FDG PET/CT in the diagnosis and treatment of gastrointestinal stromal tumors / 中华核医学与分子影像杂志

Gastrointestinal stromal tumor (GIST) is the most common mesenchymal tumor of the gastrointestinal tract.It can be classified as benign,malignant potential undetermined and malignant according to their biological behaviors.Early diagnosis,accurate staging and therapeutic response evaluation have an effect on the clinical decision-making and prognosis.Those factors used to be assessed by traditional imaging techniques,such as CT,EUS and MRI.While 18F-fluorodeoxyglucose (FDG) PET/CT,combining the advantages of both anatomic information from CT and functional information from PET,plays a considerable role in the diagnosis,staging,clinical decision-making,response evaluation,prognosis and recurrence detection of GIST.Consequently,18F-FDG PET/CT will be helpful to guide the personalized treatment of GIST.This review introduces the application progress of 18F-FDG PET/CT in GIST.

Radioimmunotherapy in solid tumors / 中华核医学与分子影像杂志

Radioimmunotherapy (RIT) is often used as an adjuvant therapy or consolidation therapy for cancer due to its relative high specificity and minimized radiation damage to non-targeted organs.The progress of RIT in solid tumors was slow,however,it has been developed quickly recently especially in elimination of residual micro-tumor lesions due to the application of α radionuclide,the progress in antibody preparation,and the implementation of new therapeutic strategies.

Preparation of 99Tcm-SHNH-AC133 and imaging on colon cancer bearing mice / 中华核医学与分子影像杂志

Objective To prepare 99Tcm-succinimidyl-6-hydrazinonicotinate hydrochloride (SHNH)-AC133 and evaluate its targeting ability on CD133 positive colon cancer by Gamma imaging,and to explore its feasibility as a molecular probe for cancer stem cells (CSCs).Methods CD133 expression was detected by immunofluorescence assay and flow cytometry on Lovo cell lines and tumor xenografts.CD133 specific monoclonal antibody (AC133) was conjugated with SHNH,and then labeled with 99Tcm to prepare 99Tcm-SHNH-AC133.The radiolabeled yield and radiochemical purity were investigated.Colon cancer xenografts were developed and Gamma imaging were performed.Region of interest (ROI) was drawn and the tumor/non-tumor (T/NT) ratio was calculated.For the blocking experiment,animals were pre-injected with excess unlabeled AC133.Two-sample t test was used to analyze the data.Results CD133 was expressed on the surface of Lovo cells.And the percentage of CD133 positive cells in Lovo tumor tissues was (29.5±3.4)％.The radiolabeled yield of 99Tcm-SHNH-AC133 was more than 85％ and radiochemistry purity was (97.7±2.4)％.Gamma imaging demonstrated that 99Tcm-SHNH-AC133 could specifically target to Lovo tumors which could be gradually visible after 12 h.The tumor uptake was obvious at 24 h and T/NT ratio was 8.16±0.45.In blocking study,the tumor uptake was significantly reduced by pre-injection of excess unlabeled AC133 (3.52±0.13;t=19.8,P＜0.05).Conclusions 99Tcm-SHNH-AC133 has high labeling yield and radiochemistry purity.The excellent targeting properties of 99Tcm-SHNH-AC133 on CD133 positive colon cancer demonstrate that it is a promising imaging agent for CSCs tracking in vivo.

Research advances on hypolipidemic effect of polysaccharides / 中国中药杂志

Hyperlipidemia is a systemic chronic metabolic disease caused by dyslipidemia in the body. It is an important risk factor of accelerating atherosclerosis, which will cause coronary heart disease, thrombus and other cardiovascular diseases, so it is a "invisible killer" for human health. Controlling and lowering blood lipids can reduce the risk of cardiovascular and cerebrovascular diseases. The current therapies for hyperlipidemia mainly include chemical synthetic medicines. However, long-term use of hypolipidemic drugs would cause various side effects, and the demand of effective and nontoxic drugs for hyperlipidemia patients is eager. Polysaccharide has attracted worldwide concerns due to its characteristics of good biocompatibility and less side effects. Polysaccharide is a kind of biological macromolecule which is widely found in plant cell walls, animal cell membranes and microorganism cell walls. A number of studies have shown that polysaccharides from natural materials have broad biological activities, such as anti-tumor, immunomodulatory, antioxidant, hypoglycemic, and hypolipidemic effects, with broad application prospect. This paper has reviewed and summarized the polysaccharides with hypolipidemic effect and their mechanisms which have been reported at home and abroad, hoping to provide certain reference for their development and application in lowering blood lipids.

Tissue distribution of TPGS modified artesunate liposome and its metabolites in rats / 中国中药杂志

Artesunate, which is a widely used anti-malaria medicine, can be made into liposome to overcome its poor bioactivity. Its tissue distribution in rats may change with different dosage forms, which therefore shall be studied after ARS-TPGS-Lipo was injected. Based on this experiment, ARS-TPGS-Lipo and ARS-Lipo were prepared by thin-film hydration method. LC-MS/MS method was used to simultaneously determine ARS and DHA in rat tissues at different time points. The results showed that this method was suitable for the content analysis of ARS and DHA in biological samples. The distribution of ARS and DHA in ARS-TPGS-Lipo, ARS-Lipo and ARS groups were quite different. The content of ARS-TPGS-Lipo in liver was the highest, with significant differences.ARS and DHA contents in ARS group eliminated rapidly. ARS and DHA contents in ARS-Lipo group were higher in liver and spleen, while those in ARS-TPGS-Lipo group significantly increased only in liver (<0.05).

Feasibility study of QAMS for quantitative analysis of multiple structural types of ingredients in Atractylodis Rhizome by GC / 中国中药杂志

In this study， quantitative analysis of multi-components with single marker(QAMS) was established and validated to simultaneously determine four sesquiterpenoids(β-eudesmol， atractylon， atractylolideⅠ， atractylolide Ⅱ) in Atractylodis Rhizome based on the gas chromatographic method(GC). Using β-eudesmol as the contrast， the relative correctionfactors(RCF) of the other three sesquiterpenoids were determined by GC. Within the line arranges，the values of RCF of β-eudesmol to atractylon， atractylolideⅠand atractylolide Ⅱ were 0.823， 0.690 and 0.766， respectively. The RCF had a good reproducibility in various instruments， chromatographic columns. According to their RCF， we simultaneously determined four sesquiterpenoids in Atractylodis Rhizome only using one marker. The results of QAMS method were validated by comparing with that of internal standard method， and no obvious significant difference was found.