Lycobetaine ( AT-1840 ) is an effective antitumor substance. In the present work it was demonstrated that in a dose of 40 pig/kg AT-1840 could decrease the percentage of G, cells, meanwhile it increased G2 + M cells remarkably by means of flow fluocytometry method, AT-1840 could also inhibit the progression of cells from G2 to G1 phase. 8 to 72 h after, the injection the mitotic index was decreased significantly and recovered gradually in 6 d. It could inhibit the prophase and metaphase greatly, but had no marked influence on anaphase & telophase.

Objective To study the hypoglycemic effect of total flavonoids from stems and leaves of scatellaria baicalensis (SSTF)on diabetic mice and to explore the therapeutic mechanism.Methods Diabetic mice models were established by intraperitoneal injection of alloxan(200 mg/kg),and the changes of mice blood glucose ,superoxide dismutase activity and malondialdelyde content were observed after preventive or curative treatment with SSTF.Results Preventive treat- ment with SSTF can obviously inhibit the increase of mice blood glucose induced by alloxan ,and the therapeutic treat- ment with SSTF can lower the blood glucose levels of diabetic mice.Both preventive and therapeutic treatment groups can increase serum superoxide dismutase activity and decrease malondialdelyde content.Conclusion SSTF have significant preventive and therapeutic effects on diabetic mice,and the mechanism is related to the anti-oxidation activity.

AIM: To investigate the effects of fenofibrate on angiotensin Ⅱ ( AngⅡ)-induced cardiomyocyte hypertrophy .METHODS:Primary neonatal cardiomyocytes were pretreated with fenofibrate (10μmol/L) for 1 h followed by stimulation with AngⅡ(100 nmol/L).The mRNA levels of ANF, BNP andβ-MHC were measured by real-time PCR. Western blotting was employed to determine the nuclear translocations of NFATc 4 and p65-NFκB.Co-immunoprecipitation was used to investigate the interaction of NFATc 4 with p65-NFκB in the nucleus of cardiomyocytes .In addition, the DNA binding activity of NFATc4 on the BNP promoter was determined by EMSA .RESULTS:Fenofibrate significantly inhibited AngⅡ-induced cardiomyocyte hypertrophy .Fenofibrate treatment inhibited the nuclear translocations of NFATc 4 and p65-NFκB, as well as the interactions of NFATc 4 with p65-NFκB in the nucleus of cardiomyocytes induced by AngⅡ.Fenofi-brate inhibited the binding activity of NFATc 4 with the BNP promoter , which was strengthened by AngⅡ.CONCLU-SION:Fenofibrate enhances the interaction of NFATc 4 with PPARα, decreases the interaction of NFATc 4 with p65-NFκB in the nucleus of cardiomyocytes , and inhibits the DNA binding activity of NFATc 4 induced by AngⅡ, which may be the important mechanisms of fenofibrate on inhibiting cardiac hypertrophy .

Objective To investigate the effect of Scutellaria baicalensis stem-leaf total flavonoids(SSTF) on blood glucose,blood lipid levels and insulin resistance in type 2 diabetic rats with hyperlipidemia,and to explore the possible therapeutic mechanism. Methods Experimental rat model was established by feeding high-fat diet and intraperitoneal injection of small-dose streptozotocin. The effects of SSTF on blood glucose,blood lipid,insulin sensitive index(ISI) and antioxidative capacity of experimental rat model were investigated. Results SSTF significantly reduced the serum fasting blood glucose(FBG),total cholesterol(TC),and low-density lipoprotein cholesterol(LDL-C) levels,increased high-density lipoprotein cholesterol(HDL-C) level and ISI,and reduced triglyceride(TG) level to some extent. SSTF also had an effect on decreasing malondialdehyde(MDA) content in both serum and liver tissue,increasing serum superoxide dismutase(SOD) activity significantly and glutathione(GSH) content to some extent. Conclusion SSTF have significant effect on decreasing blood glucose and blood lipid and improving insulin resistance in type 2 diabetic rats with hyperlipidemia. Its therapeutic mechanism may be related to the antioxidation function.

Objective To investigate the effect of Scutellaria baicalensis stem-leaf total flavonoids(SSTF)on lipid metabolism in hyperlipidemia rats.Methods On the basis of establishing hyperlipidemia rat model,blood and liver lipids,lipid metabolic enzyme,and the amount of fecal bile acids were investigated after feeding of fatty emulsion for 30 days.Results Compared to the model group,SSTF significantly reduced the serum levels of total cholesterol(TC),triglyceride(TG),low density lipoprotein cholesterol(LDL-C),and increased high density lipoprotein cholesterol(HDL-C),increased the activity of lecithin cholesterol acyltransferase(LCAT).SSTF also showed the effect on decreasing liver TC,TG and increasing the amount of fecal bile acids.Conclusion SSTF have an effect on decreasing lipid metabolism in hyperlipidemia rats,and the possible mechanism is associated to the increase of LCAT activity and fecal bile acids excretion.

AIM: To study the effects of prearuptorin C (Pra-C) on myocardial sarcolemma Na~+, K~+-ATPase activity, myocardial mitochondria Na~+, K~+-ATPase, Ca~ 2+ -ATPase, Mg~ 2+ -ATPase activities and apperent Km and Vmax in spontaneously hypertensive (SHR) and renovascular hypertensive rats (RHR). METHODS: ATPase activity was measured with colourmetric method. Apparent Km and Vmax of both Na~+, K~+-ATPase in myocardial sarcolemma and Ca~ 2+ -ATPase in myocardial mitochondria were calculated according to Lineweaven-Burk double-reciprocal plot method with liner regression. RESULTS: The Vmax of both Na~+, K~+-ATPase in myocardial sarcolemma and Ca~ 2+ -ATPase in myocardial mitochondria were lower in SHR untreated group than that in SD control rats, while Km was higher than that in SD control rats. In RHRs untreated group, only Vmax was decreased, while the Km had no statistically change. Pra-C prevented the reduction of ATPase in amount, but not affected their intrinsic characteristics. CONCLUSIONS: The results suggest that both amounts and affinities to ATP of Na~+, K~+-ATPase and Ca~ 2+ -ATPase were decreased in SHRs, but in RHRs, only amounts of ATPase was decreased, while their affinities to ATP were unchanged. Treatment with Pra-C prevents the decrease in amount of ATPase.

OBJECTIVETo determine the effects and related mechanism of Scutellaria baicalensis stem-leaf total flavonoid (SSTF) on vascular smooth muscle cells (VSMCs) proliferation induced by high triglyceride blood serum (HTG).

METHODVSMCs isolated from rat aorta were cultured in vitro and proliferation was stimulated by HTG, SSTF was added to influence the proliferation of VSMCs. The proliferation and cell cycle of VSMCs were determined by MTT assay and flow cytometry, respectively. CO released into the culture media was quantitated by measuring carbon monoxide hemoglobin (COHb). The protein expressions of HO-1 and extracellular signal-regulated kinase (ERK/p-ERK) were detected by Western blot analysis.

RESULT500 mg x L(-1) SSTF could obviously suppress the cell multiplication by HTG's induction, remarkably increase the production of COHb in VSMCs, obviously suppresse the mitotic cycle progress of VSMCs (P < 0.05, P < 0.01), in the time and dosage dependence. Furthermore, 500 mg x L(-1) SSTF remarkably declined the ERK/p-ERK protein expression (P < 0.01), but did not have the influence on the HO-1 protein's expression.

CONCLUSIONSSTF inhibited the proliferation of VSMCs directly by blocking cell cycle progression, and the ERK signal transduction way possibly participated in the cytoprotection of SSTF.

Animals ; Cell Proliferation ; drug effects ; Cricetinae ; Drugs, Chinese Herbal ; pharmacology ; Flavonoids ; pharmacology ; Gene Expression ; drug effects ; Male ; Mitogen-Activated Protein Kinases ; genetics ; metabolism ; Myocytes, Smooth Muscle ; cytology ; drug effects ; metabolism ; Plant Leaves ; chemistry ; Plant Stems ; chemistry ; Rats ; Rats, Sprague-Dawley ; Scutellaria baicalensis ; chemistry ; Triglycerides ; blood ; pharmacology

[ABSTRACT]AIM:ToinvestigatethedifferenteffectsofERK1/2/PPARα/SCAD(short-chainacyl-CoAdehy-drogenase) signal pathways on the cardiac hypertrophy induced by insulin-like growth factors 1 ( IGF-1) or phenylephrine ( PE) .METHODS:The neonatal rat cardiomyocytes induced by IGF-1 were used as the model of physiological cardiac hypertrophy , and those induced by PE were used as the model of pathological cardiac hypertrophy .The surface area of the cardiomyocytes, the expression of p-ERK1/2, PPARαand SCAD, the activity of SCAD and the content of free fatty acid in the cardiomyocytes were measured .RESULTS:Compared with the control cells , the surface area of the cardiomyocytes in-duced by IGF-1 and PE were both increased .Compared with the controls , the expression of SCAD and PPARα, and the activity of SCAD in the cardiomyocytes induced by IGF-1 were increased , while the expression of p-ERK1/2 was de-creased.However, the cardiomyocytes treated with PE showed decreased expression of SCAD and PPARα, decreased activ-ity of SCAD and increased expression of p-ERK1/2.Meanwhile, the decrease in free fatty acid in IGF-1-induced cardio-myocytes and the increase in PE-induced cardiomyocytes indicated that the fatty acid utilization was increased in the cardio -myocytes induced by IGF-1, but decreased in the cardiomyocytes induced by PE .CONCLUSION: The changes of p-ERK1/2, PPARαand SCAD in the cardiac hypertrophy induced by IGF-1 or PE indicate that the effects of ERK 1/2/PPARα/SCAD signal pathways are different between physiological cardiac hypertrophy and pathological cardiac hypertro -phy , and that SCAD may be a molecular marker of these 2 different cardiac hypertrophies and a potential therapeutic target for pathological cardiac hypertrophy .

A cold saponification method for determination of 5 lutein stereoisomers in dairy products by high performance liquid chromatography ( HPLC ) was developed. Samples were cold-saponified at room temperature and extracted by n-hexane/petroleum/dichloromethane ( 2: 2: 1 , V/V/V ) . Then 5 lutein stereoisomers were separated on a YMC C30 column with gradient elution using methanol/methyl tert-butyl ether as the mobile phase, and data were acquired by a photodiode array detector at wavelength of 445 nm. The calibration curve was linear in the range of 0 . 127-5 . 082 mg/L with correlation coefficient of 0 . 9999 , and the recoveries were from 96 . 7% to 102 . 2% with the RSDs in the range of 4 . 1%-5 . 4% ( n=6 ) . The limit of detection was 0 . 010 μg/g ( S/N=3 ) , and the limit of quantification was 0 . 030 μg/g ( S/N=10 ) . By presenting results of good accuracy, precision and sensitivity, this method validates its suitability for routine analysis of 5 lutein stereoisomers in dairy products.

AIM:To investigate the change of short-chain acyl-CoA dehydrogenase (SCAD) expression during cardiomyocyte apoptosis and to explore the relationship between SCAD and cardiomyocyte apoptosis .METHODS: The neonatal rat cardiomyocytes treated by tert-butyl hydroperoxide (tBHP) were used as the model of cardiomyocyte apoptosis . The cell viability , the expression of SCAD at mRNA and protein levels , the activity of SCAD and the content of free fatty acids were determined .RESULTS:The mRNA and protein expression of SCAD decreased in the cardiomyocyte apoptosis model.Compared with negative control group , SCAD expression and activity were both significantly decreased in siRNA-1186 group, but the content of free fatty acids were obviously increased in the cardiomyocytes .Meanwhile, SCAD siRNA treatment triggered the same apoptosis as cardiomyocytes treated with tBHP .CONCLUSION: Down-regulation of SCAD may play an important role in primary cardiomyocyte apoptosis .Increase in the expression of SCAD may become an impor-tant part in intervening cardiomyocyte apoptosis .