ABSTRACT
OBJECTIVETo evaluate antithrombotic efficacy and preliminary pharmacokinetics of Bg115-2.METHODSProthrombin time (PT) and activated partial thromboplastin time (APTT) in vitro were determined using assay kits,respectively.The effect on venous thrombosis was evaluated with the model of inferior sinus venous thrombosis in mice.Bleeding reaction was measured by tail bleeding time test.Preliminary pharmacokinetic study was conducted using FXa activity assay.RESULTSBg115-2 (sc) 0.75 -3.0 mg·kg-1 prolonged PT (P＜0.05,P＜0.01) and APTT (P ＜ 0.01) dose-dependently. In the inferior sinus venous thrombosis model,Bg115-20.19 - 3.0 mg· kg-1 significantly reduced thrombus mass with ID50 of 0.19 mg· kg-1.Interestingly,Bg115-2 (ig) 1.5 -6.0 mg·kg-1 also significantly reduced venous thrombus mass (P ＜0.01 ).Bg115-2 was similar to nadroparin calcium in bleeding reaction,and ED2/ID50 reached up to 26.8.Furthermore,Bg115-2 3.0 mg· kg-1 displayed a pharmacokinetic character with a two-compartment model.t1/2,cmax and AUC were (6.18 + 1.45 ) h,(5.20 + 0.66) mg·L-1 and (43.75 +8.20)mg·L-1 ·h,respectively.CONCLUSIONBg115-2 is a potent and oral effective inhibitor of venous thrombosis in mice with slight bleeding side-effect.It has longer t1/2 and the distribution character of a twocompartment model.
ABSTRACT
<p><b>OBJECTIVE</b>To separate effective constituents from Millettia nitida var. hirsutissima.</p><p><b>METHOD</b>Compounds were isolated by chromatography methods, structures were identified by spectroscopic means.</p><p><b>RESULT</b>Eight flavonoids (1-8) and two triterpenes (9-10) were isolated from this plant. They were identified as calycosin (1), genistin (2), gliricidin (3), 8-O-methylretusin (4), afromosin-7-O-beta-D-glucopyranoside (5), lanceolarin (6), soliquiritigenin (7), symplocoside (8), lupeol (9), 3beta-friedelanol (10).</p><p><b>CONCLUSION</b>The compounds (1-10) were obtained from M. nitida var. hirsutissima for the first time. The 13C-NMR dada of 1 were correct assignment on the basis of 2D-NMR spectral analysis.</p>
Subject(s)
Drugs, Chinese Herbal , Chemistry , Flavonoids , Chemistry , Millettia , Chemistry , Triterpenes , ChemistryABSTRACT
AIM To investigate the effects of honokiol on ischemic neurological deficiency and on the scavenging ability of ischemia reperfusion (I-R) brain tissue for reactive oxygen species (ROS). METHODSCerebral ischemia was induced by middle cerebral artery occlusion (MCAO) in rats. I-R in mice were induced by blood stream pause in bilateral common carotid arteries for 30 min and reperfusion for 30 min. The activities of ROS scavenging enzymes were determined with colorimetric methods. RESULTS Intravenous honokiol in 5-50 μg·kg-1 significantly decreased the neurological deficiency score, and diminished cerebral infarction volume in rats. In I-R brain tissue of mice, intravenous honokiol in 7-70 μg·kg-1 evidently enhanced the activities of superoxide dismutase, catalase, glutathione peroxidase and peroxidase, and markedly lowered lipid peroxidative product malondialdehyde content. Moreover honokiol significantly increased Na+-K+-ATPase activity in I-R brain tissue. CONCLUSION Honokiol ameliorates the neurological deficiency behavior and diminishes infarction volume in MCAO rats; and enhances cerebral scavenging ability for ROS and Na+-K+-ATPase activity in cerebral I-R mice. It is indicated that honokiol is a protective agent for cerebral ischemia and I-R.
ABSTRACT
AIM: To investigate the effect of monascus purpureus fermented rice (MR) on alcohol fatty liver model in quails. METHODS: A fatty liver model was established in quails, then the lipid levels of the models were tested in both plasma and liver, and the examination in the pathological histology of liver was conducted. RESULTS: 1.6 g?kg -1 ?d -1 of MR given orally for 20 d significantly decreased TC, TG and LDL (P
ABSTRACT
AIM To investigate the effect of Icarrin on penile erection and cyclic GMP levels in rabbit corpus cavernosum(RCC). METHODS Effects of various concentration of Icariin on cGMP level in RCC were measured by 125 I radioimmunoassay procedure with Sildenafil and papaverine as the positive controls RESULTS In the presence of SNP, Icariin increased cGMP concentration in rabbit corpus cavernosum in a dose dependent manner ( P