AIMTo evaluate the in vitro/in vivo correlation for three kinds of self-designed sustained-release nitrendipine formulations using deconvolution method.

METHODSThe characteristics of in vivo release were calculated by deconvolution method using the data of plasma concentration of three kinds of self-designed sustained-release nitrendipine formulations in healthy dogs, in which the in vivo results of nitrendipine solution after oral administrated to dogs were used as weight function. It was the compared with characteristics of in vitro release to assess the in vitro/in vivo correlations.

RESULTSThe good correlations of in vitro/in vivo were shown in three kinds of self-designed sustained-release nitrendipine formulations using deconvolution method.

CONCLUSIONThe deconvolution method exhibited advantage in evaluation of in vitro/in vivo correlation for self-designed sustained-release nitrendipine formulations.

Administration, Oral ; Animals ; Delayed-Action Preparations ; Dogs ; Methylcellulose ; analogs & derivatives ; Microspheres ; Nitrendipine ; administration & dosage ; blood ; pharmacokinetics ; Powders ; Silicone Gels ; Technology, Pharmaceutical ; methods

AlM: To measure the retinal electrical activities in patients with diabetic retinopathy ( DR ) by applying multifocal electroretinogram ( mf-ERG) and evaluate the degree of visual damage at different stages of DR
METHODS:Thirty cases ( 30 eyes ) aged 50 ~70 years old, excluding other diseases, were as normal group, and 99 cases ( 99 eyes ) diagnosed with type 2 diabetes were as experiment group. The cases received mf-ERG examination in the standard state, respectively. The results were statistically analyzed
RESULTS: For DR patients with early and background stage, the reaction density of mf - ERG P1 wave decreased as the disease worsened, significantly reduced in non - proliferating stage and decreased more significantly in the background of the stage Ⅲ. This showed that in the macula, electrical activity had weakened before the retina without visual or morphological changes, and with the development of the disease, the electrical activity decreased more obviously.
CONCLUSlON:mf-ERG can evaluate the severity of DR, especially suit in the early and background period of DR.

Objeetive:To study the expression and clinical significance of NF-κ Bp65 protein and selective autophagy adaptor protein SQSTM1/p62 1(p62) in gastric carcinoma and its clinical significance.Methods:NF-κ Bp65 protein and p62 protein were determined in 72 cases of gastric carcinoma by immunohistochemistry PV-9000,and the relationship between them in the occurrence and development of gastric cancer was analyzed.Results:The positive expression of in gastric cancer tissues of NF-κ Bp65 (65.3％) was significantly higher than that of paracancerous gastric tissues (27.8％,P＜0.05);the positive expression rate of p62 (66.7％)was significantly higher than that in paracancerous gastric tissues (30.6％,P＜0.05);The expression of NF-κ Bp65,p62 was significantly correlated with the cancerous tissue differentiation degree,infiltrative depth,and lymph node metastasis (P＜0.05);NF-κ Bp65,p65 expression in the gastric cancer was positively correlated (P＜0.05).Conclusions:p62 and NF-κ Bp65 may be involved in apoptosis and cell proliferation of gastric carcinoma,and play anessential role in carcinogenesis.Detection of the two indexes would be used to assess and predict the prognosis of gastric cancer patients.

OBJECTIVETo study the distribution of genomovars and microevolution of Yersinia pestis in the Qinghai-Tibet Plateau.

METHODSPrimer pairs targeting the twenty-two different regions(DFRs) were designed for detecting the presence or deletion of each DFR in 297 strains isolated from the Qinghai-Tibet Plateau.

RESULTS9 genomovars, i. e. Genomovar 1, 5, 6, 7, 8, 10, 11, new type and Ype-ancestor were identified in the Marmota himalayana plague focus of the Qinghai-Tibet Plateau. Among these genomovars, genomovar 5,8 and 10 were dominant types. The total rate of the three genomovars was 80.6% (204/253) and the genomovars in different regions were different. All of 44 strains of Y. pestis in the Microtus fuscus plague focus of the Qinghai-Tibet Plateau belonged to genomovar 14.

CONCLUSIONThe distribution of genomovars of Y. pestis in the Qinghai-Tibet plateau had remarkable characteristics geographically. Based on the distribution of genomovars of Y. pestis, the routes of transmission and microevolution of Y. pestis were proposed.

Biological Evolution ; China ; Geography ; Humans ; Plague ; transmission ; Yersinia pestis ; genetics

OBJECTIVETo study the influence of Yanyankang powder on Th1/Th2 in rats with experimental autoimmune uveitis (EAU).

METHODSThe EAU models were induced in Lewis rats by immunization with interphotoreceptor retinoid binding protein (IRBP) 1177-1191 in complete Freund's adjuvant. The rats were randomly divided into 3 groups: a model control group, a Yanyankang group, and a prednisone group, 9 rats in each group. The model control group was intervened with saline solution by gavage. The Yanyankang group was intervened with Yanyankang powder 4 g/(kg day) by gavage. The prednisone group were intervened with prednisone acetate tablets 5 mg/(kg d) by gavage. All groups were intervened after immunization once every 2 days for 18 days and monitored by slit-lamp biomicroscopy daily until day 18. The levels of gamma interferon (INF-γ) and interleukin-10 (IL-10) in the supernatants of T cells were determined by enzyme-linked immunosorbent assay. Polymerase chain reaction (PCR) technology was used for measuring Th1 and Th2 related cytokine mRNA expressions.

RESULTSSlighter intraocular inflammation was found in the Yanyankang group and the prednisone group than the control group. The levels of the IFN-γ and IL-10 in the supernatants of the spleen lymph node cells were 382.33±6.30, 155.87±4.46 μg/L in the Yanyankang group and 270.93±7.76, 265.32±11.88 μg/L in the prednisone group. Both had significant differences compared with the control group (941.53±8.59, 20.67±4.65 μg/L; =0.01). The PCR results showed the same tendency.

CONCLUSIONYanyankang powder showed favorable effects in the rats with EAU by influencing the function of Th1 and Th2 cells.

Animals ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Eye ; pathology ; Female ; Immunization ; Inflammation ; pathology ; Interferon-gamma ; genetics ; metabolism ; Interleukin-10 ; genetics ; metabolism ; Lymph Nodes ; drug effects ; metabolism ; Powders ; RNA, Messenger ; genetics ; metabolism ; Rats, Inbred Lew ; Spleen ; metabolism ; Th1 Cells ; drug effects ; immunology ; Th2 Cells ; drug effects ; immunology ; Uveitis ; drug therapy ; genetics ; immunology

ObjectiveTo explore the application value of real-time contrast-enhanced ultrasound (RTCEU) in improving the detection rate of transrectal ultrasound-guided prostate biopsy.

METHODSThis prospective study included 91 male patients with abnormally high PSA (4－20 μg/L) or abnormalities in DRE or MRI, who underwent 12+X prostate biopsy following conventional transrectal ultrasonography (TRUS) and RTCEU examination. We compared the numbers of suspected prostatic nodules before and after RTCEU as well as the detection rates of prostate cancer between conventional TRUS-guided 12PBx and 12PBx plus lesion-targeted biopsy procedures.

RESULTSTotally, 57 of the 86 suspected lesions on TRUS (66.3%), and 108 of the 118 abnormal nodules on RTCEU (91.5%) were confirmed to be prostate cancer. RTCEU achieved a significantly higher detection rate than TRUS (P<0.01). A total of 39 cases of prostate cancer (42.8%) were detected by RTCEU, while only 28 (30.7%) by TRUS, with statistically significant difference in the detection rate between the two procedures (P=0.033).

CONCLUSIONSReal-time contrast-enhanced ultrasound can significantly improve the detection rate of prostate cancer and provide a valuable guide to targeted prostate biopsy.

Contrast Media ; Endoscopic Ultrasound-Guided Fine Needle Aspiration ; Humans ; Magnetic Resonance Imaging ; Male ; Prospective Studies ; Prostate ; diagnostic imaging ; pathology ; Prostate-Specific Antigen ; blood ; Prostatic Neoplasms ; blood ; diagnostic imaging ; pathology ; Ultrasonography, Interventional

Aim To determine the antiviral and anti-inflammatory effects of the recommended prescription for COVID-2019-lung-spleen qi deficiency(4-1)against in vitro infection of SARS-CoV-2 and common coronaviruses.Methods The main chemical substances of 4-1 were analyzed by LC-MS.The toxicity and antiviral effects of of 4-1 were detected by MTT and by CPE assay, respectively.The viral loads in cell supernatant and the expression of inflammatory factors induced by viral infection were determined by qRT-PCR.Results The recommended prescription 4-1 contained 94 chemical compounds, including flavonoids, steroids, sesquiterpenoids, and so on.The range of selection indexes for SARS-CoV-2 and common coronaviruses was 8.44±0.4952.26±2.3.This prescription could inhibit the proliferation of SARS-CoV-2, the expression of ACE2 and S mRNA, and down regulate IL-1α and CCL-5/RANTES at 10, 5, and 2.5 g•L-1 doses.Further, at doses of 20, 10 and 5 g•L-1, it could inhibit the proliferation of three common coronaviruses and suppress the overexpression of IL-6, CXCL-8/IL-8, CXCL-10/IP-10, TNF-α, IFN-α, CCL-2/MCP-1, MIG and CCL-5/RANTES induced by OC43/229E infection.The inhibitory effects were dose-dependent.Conclusions The prescription 4-1 has antiviral and anti-inflammation effects against multiple coronaviruses.This study provides the research basis for the treatment of common respiratory viral infections and emerging infectious diseases such as COVID-19 by using traditional Chinese medicine.