[Pharmacokinetic Effect of Acteoside in Blood Deficiency Rats].

Objective: To study the different pharmacokinetics effect of acteoside extracted from Rehmanniae Radix Preparata in normal and blood deficiency rats. Methods: Injected acetyl phenylhydrazine and cyclophosphamide to make blood deficiency rats models subcutaneously,and gave mice the ethand extracts of Rehmanniae Radix preparata by oral administration,the concentration of acteoside in rats at different time points were detected by HPLC method, pharmacokinetic parameters were calculated by 3p87 software. Results: The determination of acteoside in the linear range were 0. 2 ~ 80 µg / m L, the limit of detection and quantification was 0. 03 and 0. 12µg/m L,respectively. Compared with the normal group,the content of AUC0-tand AUC0-∞of corresponding dose in model group rats increased significantly, and the average dwell time and the elimination half-life prolong significantly. Conclusion: This method has high specificity,high sensitivity and simple operation, which can be used for the determination to pharmacokinetic process of acteoside in blood deficiency model.

[Study on Anti-Inflammatory and Analgesic Effects of Different Processing Products of Strychnos nux-vomica Seeds].

Objective: To study the differences of anti-inflammatory and analgesic effects between oil,sand and vinegar processing Strychnos nux-vomica seeds. Methods: Mouse auricular swelling and writhing test and mice hot water tail flick latency effect method were used to study and compare the anti-inflammatory and analgesic effects of different processing products of Strychnos nux-vomica seeds. Results: The anti-inflammatory and analgesic effects of vinegar processing Strychnos nux-vomica seeds was better than that of oil and sand processing products. Conclusion: This study can provide theoretical basis for the optimization of processing technology of reducing toxicity and enhancing effects of processed Strychnos nux-vomica seeds.

[Pharmacokinetic Study on Brucine in Different Administration Methods of Liposome in Rats].

OBJECTIVE: To compare the pharmacokinetic differences of brucine in rats after different administration methods of brucine liposome. METHODS: To determine brucine in rat plasma at different points in time by HPLC after oral administration, intramuscular injection, subcutaneous injection and intravenous injection of brucine liposome, respectively. The pharmacokinetic parameters were calculated and analyzed by DAS 3.0. RESULTS: Compared with other groups, AUC(0 --> t) of subcutaneous injection were higher, C(max) were lower and MRT(0 --> 1), were significantly improved. The pharmacokinetics parameters and absolute bioavailability of brucine show that bioavailability in rats after different administration methods of brucine liposome is subcutaneous injection > intramuscular injection > oral administration.

[Effect and Mechanism of Litchi Semen Effective Constituents on Insulin Resistance in Rats with Type 2 Diabetes Mellitus].

OBJECTIVE: To observe the effect of Litchi Semen Effective Constituents (LSEC) on insulin resistance (IR) in rats with Type 2 Diabetes Mellitus(T2DM), and to explore its mechanism. METHOD: T2DM models in rats with IR were induced by high-fat feeding combined with streptozocin, then the rats were randomly divided into four groups: model group, LSEC high-dose group (1. 87 g/kg), LSEC low-dose group(0. 47 g/kg) and rosiglitazone group(3. 87 x 10(-3) g/kg), blank group was established as control. After medication for four weeks, effects of LSEC on glucose or lipid metabolism and insulin resistance were investigated, histopathology and ultrastructure changes of pancreatic tissues were observed,Stem-loop Real-time fluorescence quantitative RT-PCR was used for evaluation of GRP78 mRNA and CHOP mRNA levels in pancreatic tissue of rats. RESULT: LSEC of high-dose group obviously improved fasting blood glucose, serum TG level and glucose tolerance in T2DM rats (P <0. 05 or P <0. 01). ISI was increased, HOMA-IR index was decreased, histopathology change of pancreatic tissue were alleviated, damaged organelle, such as endoplasmic reticulum and mitochondria were repaired in both groups of LSEC. Expression levels of GRP78 mRNA of both groups of LSEC and CHOP mRNA of high-dose group in pancreatic tissue were obviously lower than those of model group (P <0. 01). CONCLUSION: LSEC can improve glycolipid metabolism and IR, increase insulin sensitivity to cure T2DM, its effects may be attributed, at least in part, to inhibit the expression of GRP78 mRNA and CHOP mRNA.

[In vivo Pharmacokinetics of Notoginsenoside R1 in Ischemia Rats After Acute Myocardial Infarction].

OBJECTIVE: To establish an HPLC-UV method for determining pharmacokinetic difference of notoginsenoside R1 between normal rats and ischemic rats. METHODS: 48 male SD rats were randomly divided into normal group and acute myocardial ischemia( AMI) model group induced by pituitrin and each group was classified into high,middle and low-dose of groups with notoginsenoside R1 (200, 100 and 50 mg/kg) respectively. Blood samples were collected at different points in time after they were administered once by gavage and separated by Waters symmetry C18 column (250 mm x 4.6 mm, 5 µm) under the detective wavelength 203 nm, the mobile phase was acetonitrile-water with icariin as the internal standard and the pharmacokinetic parameters were calculated by DAS 2. 0. RESULTS: Notoginsenoside R1 had good linearity in the ranges of 0.2~125 µg/mL (R2 = 0.9997) with SNR 1:3 and the lowest detection limit was 0.053 µg/mL, the extraction rate, RSDs of within-day and between-day, specificity, accuracy and precision accorded with the require-ment of bio-sample pretreatment. Compared to the normal group, AUC0-t, and AUC0-∞ was significantly increased (P < 0.01) and the terminal half-life was prolonged markedly (P < 0.01) in AMI group. CONCLUSIONS: The method is simple, accurate and had high specificity and sensitivity, that could be applied in quantitative determination of notoginsenoside R1 and research of pharmacokinetics; the relative bioavailability of notoginsenoside R1 is increased significantly in AMI group,which indicates that notoginsenoside R1 has better effect in model rat.

[Analysis of volatile composition of different specification of Panax notoginseng].

OBJECTIVE: To analyse the volatile compositions of different specification of Panax notoginseng. METHODS: Volatile compositions from different specification of Panax notoginseng were detected by Headspace Solid-Phase Micro-Extraction with GC/MS. RESULTS: Terpenoids were the main compositions in different specification of Panax Notoginseng, and a-guaiene was the fundamental ingredient. The type, content and quantity of the compounds were different in different type of Panax notoginseng. CONCLUSION: Terpenoids were the main pharmacodynamics of the volatile compositions of Panax notoginseng and worthy of further study.

Scurvy in a young man: a rare case report.

Scurvy, resulting from vitamin C deficiency, has nonspecific constitutional symptoms, including weakness, malaise, and fatigue. It is frequently misdiagnosed due to the lack of specific clinical manifestations. Although there are sporadic cases of scurvy currently reported in children, scurvy in young people is seldom encountered. Here, we report on a 25-year-old male patient without any underlying conditions who presented with severe pain and ecchymoses of both lower extremities. He was diagnosed with scurvy due to a long history of staying indoors and inadequate intake of fruits or vegetables.

Clinical Significance of Different Profiles of anti-Ro Antibodies in Connective Tissue Diseases.

Objective: Anti-Ro60 and anti-Ro52 antibodies are associated with different connective tissue diseases (CTDs). However, the clinical significance of anti-Ro antibodies is not always consistent among different global regions. The aim of this study was to investigate the clinical characteristics of patients with anti-Ro antibodies. Methods: A total of 1596 inpatients with anti-Ro antibodies were included in the study. Demographic, clinical, and serological data were compared between individuals with different profiles of anti-Ro antibodies: patients with anti-Ro52 antibodies alone, patients with anti-Ro60 antibodies alone, and patients with combined anti-Ro52 and anti-Ro60 antibodies. Results: Of the 1596 patients, 1362 (85.3%) were female, the mean age was 45.5 years, and systemic lupus erythematosus (SLE) (46.0%) and Sjogren's syndrome (SS) (19.0%) were the most common CTD diagnoses. Among the patients with anti-Ro52 antibodies alone, idiopathic inflammatory myopathy (18.8%) and SLE (17.6%) were the most common CTD diagnoses. The coexistent autoantibodies of this group were significantly lower compared with those of the other two groups, while the presence of anti-Jo1 antibodies were significantly higher compared with those of the other two groups (3.7% vs. 0.6% vs. 1.9%, p = 0.029). In addition, the patients with isolated anti-Ro52 antibodies were more likely to suffer from interstitial lung disease (35.5% vs. 11.3% vs. 13.7%, p < 10-4) and pulmonary arterial hypertension (10.1% vs. 5.3% vs. 3.6%, p = 0.001) compared with the other two groups of patients. Compared with patients with isolated anti-Ro52 or anti-Ro60 antibodies, the patients with combined anti-Ro52 and anti-Ro60 antibodies were more likely to suffer from xerophthalmia and xerostomia. Furthermore, hypocomplementemia, hyperglobulinemia, and proteinuria were particularly prevalent in patients with anti-Ro60 antibodies. Conclusion: Different profiles of anti-Ro antibodies were significantly associated with clinical phenotypic features in CTDs, indicating the potential diagnostic and prognostic value of these antibodies in clinical practice.

[Study on the chemical constituets in ethyl acetante extraction from semen litchi].

OBJECTIVE: To study the chemical constituents in ethyl acetate extraction of Semen Litchi. METHODS: The compounds were isolated and purified by column chromatography on silica gel and Sephadex LH-20 coupled with preparative silica gel TLC, their structures were identified by physicochemical properties and spectrum analysis. RESULTS: Five compounds were isolated and identified as stigmasterol (1), P-hydroxy-benzaldehyde (2), protocatechuic acid (3), daucosterol (4) and kaempferol-3-O-beta-D-glucopyranoside (5). CONCLUSION: Compounds 2 and 5 are obtained from this plant for the first time.

[Effects of Erigeron breviscapus injection on TNF-alpha, PAI-1 and tPA in rats with acute myocardial infarction].

OBJECTIVE: To research the effects of Erigeron breviscapus injection (EBI) on TNF-alpha, PAI-1 and tPA in rats with acute myocardial infarction. METHODS: Models of acute myocardial infarction (AMI)were produced by ligation of left anterior descending coronary artery, then rats were randomly divided into control and experimental groups, then respectively gavaged NS, and the low, middle and high dosage of EBI for one week. The cardiac function index and the expression of TNF-alpha, tPA and PAI-1 were measured. RESULTS: Compared with the NS group, the cardiac function LVEDP, MAP, LVPmax, +/- dp/dt of AMI rat was improved by EBI in all dosage range, and the expression of TNF-alpha and PAI-1, LVEDP were decreased (P < 0.05), the expression of tPA, MAP, LVPmax and +/- dp/dt were increased obviously (P < 0.05) and had a dose-effect relationship. CONCLUSION: EBI can inhibit the expression of TNF-alpha and PAI-1, increase the expression of tPA,which can prevent the ongoing thrombopoiesis after AMI and improve the cardiac function. This maybe attributes to the inhibition of the overexpression of TNF-alpha.

[Effects of Panax notoginseng saponins on ACE2 and TNF-alpha in rats with post-myocardial infarction-ventricular remodeling].

OBJECTIVE: To research the effects of Panax notoginseng saponins (PNS) on angiotensin-converting enzymes 2 ( ACE2) and tumor necrosis factor-alpha (TNF-alpha) in rats with post-myocardial infarction ventricular remodeling. METHODS: Models of acute myocardial infarction (AMI) were produced by ligation of left anterior descending coronary artery, 24 hours after operation the rats were randomly divided into control and experiment groups, then respectively administrated with NS, fosinopril and low, middle and high dosage of PNS for four consecutive weeks. To observe effects of PNS on malondialdehyde (MDA), nitric oxide (NO), glutathione peroxidase (GSH-Px), ACE2 and TNF-alpha in rats with post-myocardial infarction ventricular remodeling. RESULTS: Compared with NS group, MDA significantly decreased, the activity of GSH-Px significantly increased (P < 0.05 or P < 0.01), NO of the high-dose PNS group decreased (P < 0.05), Compared with the NS group, ACE2 increased and TNF-a significantly decreased in low-dose PNS group, middle and high-dose groups (P < 0.05). CONCLUSION: PNS can stimulate ACE2 to inhibit the expression of TNF-alpha and enhance the antioxidance. PNS can reduce pathological injury of cardiac myocytes in myocardial ischemia and cardiac muscle, which can improve ventricular remodeling.

How Do Structurally Distinct Compounds Exert Functionally Identical Effects in Combating Obesity?

Although the concept of inflammatory obesity remains to be widely accepted, a plethora of antibiotics, anti-inflammatory agents, mitochondrial uncouplers, and other structurally distinct compounds with unknown mechanisms have been demonstrated to exert functionally identical effects on weight reduction. Here we summarize a universal mechanism in which weight loss is modulated by mitochondrial biogenesis, which is correlated with conversion from the mitochondria-insufficient white adipose tissue to the mitochondria-abundant brown adipose tissue. This mechanistic description of inflammatory obesity may prove useful in the future for guiding pathology-based drug discovery for weight reduction.

Antitumor and apoptotic activities of the chemical constituents from the ethyl acetate extract of Artemisia indica.

Cancer is one of the most eminent diseases of modern times and numerous natural products derived from medicinal plants have been identified as potential sources of antitumor drugs. A successful anticancer drug must target or inhibit tumor cells whilst causing minimal damage to healthy cells. The present study aimed to investigate the antitumor efficacy of ethyl acetate extract, and other isolated compounds from Artemisia indica, on MCF­7, BHY, Miapaca­2, Colo­205 and A­549 cell lines. The apoptotic activity of the compounds was studied using flow cytometry. The different cancer cell lines were treated with the ethyl acetate extract and varying concentrations of compounds (denoted a­g) isolated from the A. indica. The cytotoxicity was evaluated by MTT assay and the apoptotic properties of the compounds and the extract were assessed using flow cytometry. In MCF­7 cells, the effect on mitochondrial membrane potential loss (ΛΨm) induced by compounds b and d was also studied. Bioassay­guided fractionation of the ethyl acetate extract from the shoot and root parts of A. indica led to the identification of the compounds a­g as: 5­hydroxy­3,7,4'­trimethoxyflavone; ludartin; maackiain; lupeol; cis­matricaria ester; trans­matricaria ester; and 6­methoxy­7,8­methylenedioxy coumarin, respectively. All the compounds exhibited mild to potent inhibition of cell proliferation in all the cell lines, with the half maximal inhibitory concentration values ranging from 25.18­88.12 µM. Ludartin and lupeol were observed to have the most potent inhibitory effects. Based on the initially identified antiproliferative effects, these two compounds were evaluated for their effects on cell cycle phase distribution, DNA damage and their effects on mitochondrial membrane potential loss (ΛΨm). The two compounds induced DNA damage and mitochondrial membrane potential loss in MCF­7 cells. The results of the current study suggest that lupeol and ludartin, isolated from A. indica, produce anticancer effects by inducing DNA damage and a reduction of mitochondrial membrane potential, and may be used as potent anticancer agents, subsequent to further study.

[Effects of Panax notoginsenoside on TNF-alpha and MMP-2 expressions in rats with post-myocardial infarction ventricular remodeling and the mechanism].

OBJECTIVE: To observe the effects of Panax notoginsenoside (PNS) on tumor necrosis factor-alpha (TNF-alpha) and matrix metalloproteinases-2 (MMP-2) expressions in rats with post-myocardial infarction ventricular remodeling and explore the mechanism. METHODS: Rat models of acute infarction ventricular (AMI) were established by ligation of the left anterior descending coronary artery. Twenty-four hours after the operation, the rats were randomized into control and experimental groups for intragastric administration of normal saline (control), fosinopril and PNS at the low, medium and high doses for 4 consecutive weeks. The effects of PNS on the cardiac function index including the left ventricular end-diastolic dimension (LVIDd), left ventricular end-systolic diameter (LVIDs), ejection fraction (EF), percentage of left ventricular systole (FS), mitral early diastolic flow velocity mouth (MV), and heart rate (HR) were observed, and the changes in TNF-alpha and MMP-2 expression were detected after post-myocardial infarction ventricular remodeling. RESULTS: Compared with the control group, PNS at the medium and high doses produced significant improvements in the EF, FS and MV of the rats (P<0.01 or 0.05). TNF-alpha and MMP-2 expressions were significantly decreased by PNS treatment at low, medium and high doses (P<0.01). CONCLUSION: PNS can inhibit or reduce the expression of TNF-alpha and MMP-2, thereby enhancing left ventricular systolic and diastolic functions, decreasing peripheral resistance, and improving the cardiac function of rats with post-myocardial infarction left ventricular remodeling.

[Effects of Chansu injection on transplanting-tumor models S180 in mice and human colon cancer HT-29 in nude mice].

OBJECTIVE: To study the antitumor effects of Chansu injection on transplanting- tumor of S(180 ) in mice and human colon cancer HT-29 in nude mice. METHODS: Using transplanting- tumor models of S(180 ) in mice and human colon cancer HT-29 in nude mice,the tumor inhibitive ratio(IR) of Chansu injection was determined and apoptosis was microscopically observed. RESULTS: Compared with tumor-negative control groups, IR at different dosage of Chansu in models of S(180) and HT-29 was 19.1% - 38.2% and 9.5% - 15.8% respectively,there was a dose-dependent relationship in models of S ( 180) (P< 0.05) and HT- 29 (P> 0.05). The tumor growth was markedly inhibited by cyclophosphamide (CTX) in model of S( 180) with IR of 70.7% and in model of HT-29 with IR of 67.1%, compared with control groups, both P< 0.01; apoptosis induced by CTX was markedly observed by in microscope examination. No significant side effects were shown in the study group. CONCLUSIONS: Chansu injection can significantly inhibit tumor growth in model of S(180), but not in model of HT- 29. Different type of tumor has different drug-sensitivity.