The content of the asarone submicro emulsion injection was determind by HPLC method, and thereby a quality evaluation method was established based on indexes of pH value, particle size, peroxide value, methoxy aniline values, free fatty acid, lysophosphatidylcholine, visible foreign substances, insoluble particle, sterility, bacterial endotoxin and impurities, etc. The results showed that the injection exhibited uniform physical appearance and all the products were in milkwhite liquid. The content of the three batches products were respectively 102.9%, 100.8%, 97.70% of the labeled amount, with mean particle size of 210-250 nm, and other indexes all met with the standards. The reserved samples showed no obvious change in terms of detection indexes and indicated good stability after the accelerated stability test and long-term stability for 12 months. The quality evaluation method established in this study could be applied to quality control and stability investigation of asarone submicron emulsion injection, which laid a basis for further clinical research and application.
Anisoles ; chemistry ; Chromatography, High Pressure Liquid ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Emulsions ; chemistry ; Particle Size ; Quality Control

OBJECTIVETo investigate the effects of Tangzhiping Granule (TZPG) on blood lipids and free fatty acids (FFA) in rats with insulin resistant diabetes (IRD).

METHODSA blank control group consisted of randomly selected normal rats was set up. The remaining rats were established to IRD model by high-fat high-sugar diet feeding and streptozotocin injection. Then the 32 successfully modeled rats were randomized into the model group (treated by saline), the Tangmaikang group (treated with Tangmaikang Granule 1.35 g/kg), and the two TZPG groups treated with high dose (2.70 g/kg) and low dose TZPG (1.35 g/kg) respectively through intragastric infusion for 4 weeks. The body weight (BW), fasting blood glucose (FBG), insulin (INS), blood lipids including triglyceride (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), and FFA were detected, and the insulin sensitivity index (ISI) calculated.

RESULTSCompared with the blank control group, BW, FBG and INS increased while ISI decreased in the model group (P < 0.05 or P < 0.01). All the above-mentioned abnormal indices were improved in the three treated groups (Tangmaikang, high and low dose TZPG group), but the improvements in the high dose TZPG group were more significant than those in the other two groups (P < 0.05 or P < 0.01). Similar outcomes were also seen in blood lipids detection, in which TG, TC, LDL-C and FFA were higher and HDL-C were lower in model rats than those in blank controls, they were improved in the three treated groups (P < 0.05), and the best improvements were seen in the high dose TZPG group (P < 0.05).

CONCLUSIONTZPG could reduce levels of BW, FBG, INS, TC, TG, LDL-C and FFA, and increase levels of ISI and HDL-C in rat model of insulin resistant type 2 diabetes, so as to improve the insulin resistance in them.

Animals ; Diabetes Mellitus, Experimental ; drug therapy ; Diabetes Mellitus, Type 2 ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Fatty Acids, Nonesterified ; blood ; Female ; Insulin Resistance ; Lipids ; blood ; Male ; Phytotherapy ; Random Allocation ; Rats ; Rats, Wistar

OBJECTIVETo prepare and evaluate an intravenous emulsion of tanshinone II(A).

METHODSoybean phospholipid mixing with poloxamer 188 was used as emulsifier. Oleic acid and glycerol were used as co-emulsifier and isoosmotic adjusting agent, respectively. The coarse emulsion was first prepared and following homogenization was carried out for the coarse emulsion by using a high pressure homogenizer.

RESULTThe average diameter of the prepared tanshinone II (A) emulsion was 211 nm with a zeta potential of -32. 1 mV. There had no changes of diameter, zeta potential, pH value, content and physical appearance for the tanshinone II (A) emulsion stored at 25 degrees C away from light during one year.

CONCLUSIONThe physicochemical properties of the prepared tanshinone II (A) emulsion was stable, which could meet the requirements of intravenous administration.

Centrifugation ; Diterpenes, Abietane ; Drug Stability ; Drug Storage ; Emulsions ; Hydrogen-Ion Concentration ; Injections, Intravenous ; Particle Size ; Phenanthrenes ; administration & dosage ; chemistry ; Quality Control ; Temperature

OBJECTIVETo observe effect and mechanism of n-Butanol lysate of alcohol extracts from Actinidia rufa root (monomer of R6,R8).

METHODTunel, Wright's stain with Giemsa's stain dyeing, and Hoechst 33258-PI double dyeing assay were used to detect the apoptosis of SGC7901 tumor cells treated with R6, R8. The SGC7901 tumor cells were randomly divided into control group and two treatment groups administered 0.05 g x L(-1) R6, R8, respectively, for 72 h). FCM assay was used to detect the apoptosis. Agarose electrophoresis assay was used to detect DNA strand break of tumor cells and reveal anti-tumor action mechanism.

RESULTThe apoptosis percentage of the tumor cell in 24 h, 48 h, 72 h was (17.08 +/- 2.78)% , (29.68 +/- 2.96)%, (52.46 +/- 3.81)%; (14.75 +/- 2.14)%, (27.35 +/- 3.79)%, (45.64 +/- 5.24)%, respectively, for the treatment group, significantly higher than that in the control group (1.94 +/- 1.55)%, (2.78 +/- 1.84)%, (11.8 +/- 2.79)% (P < 0.01) by tunnel assay. Wright's stain with Giemsa's stain dyeing assay, Hoechst 33258-PI and FCM double dyeing assay showed same action. R6 and R8 had the effect of inducing the DNA histogram of tumor cells (P < 0.01).

CONCLUSIONThe anti-tumor mechanisms may be associated with inducing the injury of DNA and stimulating apoptosis.

Actinidia ; chemistry ; Apoptosis ; drug effects ; Cell Line, Tumor ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Flow Cytometry ; Humans ; Immunohistochemistry ; Plant Roots ; chemistry

OBJECTIVETo evaluate the efficacy and safety of subcutaneous injection of recombinant human interleukin-2 (Proleukin) in the treatment of metastatic renal cell carcinoma (RCC).

METHODSForty-one patients with pathologically confirmed metastatic RCC after radical nephrectomy were enrolled into this study. Two or four consecutive cycles of subcutaneous injection of rhLL-2 were given, with each cycle duration of five weeks consisting of 4 weeks of treatment and one week of rest. The rhLL-2 was injected twice daily subcutaneously at a dose of 9 MIU on D1-D5 during week one, then 9 MIU twice daily on D1-D2 and followed by 9 MIU daily on D3-D5 during week 2-4. Patients were evaluated after the second cycle of treatment. If an objective response or stable disease was observed, the patient would receive another two cycles of treeatment.

RESULTSOf the 41 patients, the overall objective response rate was 17.1% (95% confidence interval, 5.6% to 28.6%) with a complete response (CR) rate of 0.0% and partial response rate (PR) of 17.1%. However, nineteen patients (46.3%) still had a stable disease (SD), and 15 (36.6%) had progressed disease (PD). The disease control rate was 63.4% and the median time to progression (mTTP) was 6 months. The 1-year survival rate was 71.2% with a median overall survival (mOS) rate of 22.5 months. Among 36 PP population, the overall objective response rate was 19.4% (95% confidence interval, 6.5% to 32.3%) with CR rate of 0.0% and PR rate of 19.4%. Sixteen patients(44.4%) had stable disease, and 13 (36.1%) progressed disease. The disease control rate was 63.9%. The 1-year survival rate was 66.7% with a median time to progression of 6 months. The median overall survival (mOS) had not reached yet. The follow-up data showed that the long term survival of the patient who responsed to the IL-2 therapy can be prolonged. Severe toxicity (> or = grade III) was rarely observed. Grade I or II toxicities such as fatigue (100.0%) and fever (82.9%) were frequently observed but reversible.

CONCLUSIONSubcutaneous injection of recombinant human interleukin-2 may prolong the survival of patients with a metastatic renal cell carcinoma. This regimen is tolerable with rare severe toxicities.

Adult ; Aged ; Antineoplastic Agents ; administration & dosage ; adverse effects ; therapeutic use ; Carcinoma, Renal Cell ; drug therapy ; secondary ; surgery ; Disease Progression ; Fatigue ; chemically induced ; Female ; Fever ; chemically induced ; Follow-Up Studies ; Humans ; Injections, Subcutaneous ; Interleukin-2 ; administration & dosage ; adverse effects ; analogs & derivatives ; therapeutic use ; Kidney Neoplasms ; drug therapy ; pathology ; surgery ; Lung Neoplasms ; secondary ; Male ; Middle Aged ; Nephrectomy ; Proportional Hazards Models ; Recombinant Proteins ; administration & dosage ; adverse effects ; therapeutic use ; Remission Induction ; Survival Rate

OBJECTIVE To investigate the neuroprotective effect and possible mechanisms of lute-olin-7-O-β-D-glucuronide (LGU) against focalcerebral ischemic injury. METHODS The focal cerebral ischemic injury model was established by middle cerebral artery occlusion (MCAO). Male Sprague Dawley rats were randomly divided into sham group,model group(MCAO),LGU group(0.24,0.72 and 2.16 mg·kg-1)and positive control group(Edaravone at 5 mg·kg-1).LGU was injected intravenously 30 min after MCAO.Neurological severity score,infarct volume and brain water content were detected 24 h after MCAO and the levels of Na+-K+ATPase,Ca2+ATPase,TNF-α and IL-1β were detected to explore the possible mechanisms.For the therapeutic time window test,LGU(0.72 mg·kg-1)was injected intrave-nously 0.5, 2, 4, 6, 8, 10 and 12 h respectively after MCAO. To evaluate motion behavior, LGU were injected intravenously 30 min after MCAO and once per day during detection period. The changes of motor coordination were detected by rotating rod method and grip strength analysis, and the changes of gaits were detected using DigiGait Imaging System. RESULTS LGU improved the neurological severity score, infarct volume ratio and brain water content. The therapeutic time window of LGU for cerebral infarction and brain edema was at least 6 h and for neurological dysfunction was 12 h.LGU also prolonged the latency on rotarod, increased the forelimb tension and improved 8 gait parameters, including stance duration,stride length,stance width,paw area,paw area variability,gait symmetry,ataxia coefficient and tau propulsion.Furthermore,LGU increased Na+-K+-ATPase and Ca2+-ATPase levels in the cortex and hippocampus in the ischemic side,reduced the levels of TNF-α and IL-1β in the serum. CONCLUSION LGU has a significant neuroprotective effect against cerebral ischemic injury via improving energy metabolism and reducing inflammation.

OBJECTIVETo study the effect of qingxin kaiqiao formula and saponin on the learning and memory ability and the expression of the apoptosis signal transducers Abeta and betaAPP in AD rat brain.

METHODThe comparative observation method was adopted for the animal test. Forty male SD rats were randomly divided into five groups, namely the normal group, the model group, the aricept group, the qingxin kaiqiao formula group and the saponin group, with eight rats in each group. Abeta(25-35) (10 g x L(-1)) was injected into their bilateral amygdala to establish the AD rat model. Since the next day, they were intragastrically administered with Aricept (1.67 mg x kg(-1)), Qingxin Kaiqiao decoction (12.67 mL x kg(-1)), saponin (6.30 mg x kg(-1)) and double distilled water filling for 2 weeks to observe their spatial memory ability in a Morris water maze and study the expression of Caspase-3, Abeta and betaAPP in brain tissues by immunohistochemistry.

RESULTEach traditional Chinese medicine groups showed significant improvement in the learning and memory ability of AD rats and notable differences (P < 0.05, P < 0.01) compared with the control group. The qingxin kaiqiao formula group and the saponin group showed a decrease in the expressions of Caspase-3, Abeta and betaAPP in cerebral cortex and hippocampus area, displaying notable differences (P < 0.01, P < 0.05) compared with the control group.

CONCLUSIONqingxin kaiqiao formula and saponin can obviously improve the learning and memory ability of AD rats with by decreasing the expression of Caspase-3, Abeta and betaAPP in cortex and hippocampus.

Alzheimer Disease ; drug therapy ; genetics ; Amyloid beta-Peptides ; genetics ; Animals ; Apoptosis ; drug effects ; Caspase 3 ; metabolism ; Cerebral Cortex ; drug effects ; metabolism ; Disease Models, Animal ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; Hippocampus ; drug effects ; metabolism ; Learning ; drug effects ; Male ; Maze Learning ; drug effects ; Memory ; drug effects ; Rats ; Rats, Sprague-Dawley ; Saponins ; administration & dosage ; pharmacology ; Time Factors

The study was purposed to investigate the growth inhibitory effect of tanshinones on K562 cell line and the relationship between their structures and cytotoxicity. The modified MTT assay was adopted to measure the inhibitory effect of tanshinones at different concentrations and chemical structures on K562 cells, and the changes of cell morphology were observed by inverted phase contrast microscopy. The results indicated that the tanshinones could inhibit the proliferation of K562 cells effectively, and their cytotoxicities on K562 cells showed concentration- and time-dependent manners. The IC(50) of dihydrotanshinone I, tanshinone I, tanshinone IIA and cryptotanshinone at 24 hours were 0.91, 4.04, 5.95, 13.85 µg/ml at 48 hours were 0.37, 1.35, 1.71, 6.71 µg/ml; at 72 hours were 0.33, 0.46, 0.82, 6.02 µg/ml, respectively. It is concluded that all of the four tanshinones have proliferation inhibitory effect on K562 cell line, among them the dihydrotanshinone I is the most active one, followed by tanshinone I, tanshinone IIA and cryptotanshinone subsequently, indicating that the chemical structure of aromatic ring A of tanshinones can enhance their cytotoxicity and the structure of furan ring C may influence the cytotoxicity, but their mechanism is still remained to be further investigated.
Cell Proliferation ; drug effects ; Diterpenes, Abietane ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Humans ; K562 Cells ; Structure-Activity Relationship

OBJECTIVETo summarize the sonographic features of the lymphoma in the abdominal lymph nodes.

METHODThe clinical data and sonographic findings of 41 lymphoma patients with original appearance of abdominal mass or lymphadenectasis were retrospectively analyzed.

RESULTSAmong these 41 cases, the retroperitoneal and mesenteric lymph nodes were most commonly involved.These patients were divided into two types according to sonographic appearances:solitary mass(n=14) and multiple nodules(n=27) .Solitary hypoechoic mass in abdomen was found in the former type, mostly with irregular or lobular shape, and the inner echo was often heterogenous.The typical appearances of the latter type were multiple enlarged lymph nodes, mostly round or oval, with homogeneous inner echo and clear margins.Some other sonographic characteristics were also helpful for the diagnosis of lymphoma, such as cobblestone sign, intranodular reticulation, vessels-embedded sign, and hilar vascularity.

CONCLUSIONUltrasonography can provide useful information in the diagnosis of the lymphoma in the abdominal lymph nodes.

Abdominal Neoplasms ; diagnostic imaging ; Adult ; Aged ; Female ; Humans ; Lymph Nodes ; diagnostic imaging ; Lymphoma ; diagnostic imaging ; Male ; Middle Aged ; Retrospective Studies ; Ultrasonography ; Young Adult

OBJECTIVETo explore the sonographic characteristics of intraveous leiomyomatosis (IVL) with intracardiac extension and improve its diagnosis.

METHODSThe clinical and sonographic data of 13 female patients with pathologically confirmed IVL with intracardiac extension who were treated in our hospital between 2002 and 2012 were retrospectively analyzed. These patients aged 44 years old (range: 38-49 years), and 10 of them were first-episode patients and the remaining 3 were recurrent patients. Eight patients had a history of hysterectomy for leiomyoma.

RESULTSThe first-episode symptoms included exertional chest tightness and shortness of breath (n=5), abdominal distention and edema of low extermity (n=4), exertional palpitation of cardiac origin (n=3), and menorrhagia (n=1). Ultrasonography showed that all patients had isoechoic or hypoechoic tumors extended through the inferior vena cava into right heart chambers (62% in right atrium alone and 38% in right ventricle and atrium). Nine masses in right heart chamber (69.2%) were oval and 4 (30.8%) were serpentine, which were all with well-demarcated borders and most (80%) with heteroechogenic texture. Ten patients had hypoechoic or mixed echoic tumors in pelvic cavity or uterus, and 6 of them had abundant blood flow.

CONCLUSIONSIVL with intracardiac extension has certain sonographic characteristics. Ultrasonography is a valuable tool in the diagnosis of IVL with intracardiac extension.

Adult ; Female ; Humans ; Leiomyomatosis ; diagnostic imaging ; pathology ; Middle Aged ; Myocardium ; pathology ; Retrospective Studies ; Ultrasonography ; Vascular Neoplasms ; diagnostic imaging ; pathology