ObjectivePolyamidoamine(PAMAM) dendrimers enhance the solubility of nicotinic acid. MethodsPAMAM dendrimers of generation 1 to 6 were prepared and the effect of pH and concentration of the dendrimers on the solubility enhancement of nicotinic acid was investigated. ResultsThe pH and concentration of the dendrimers influence the solubility enhancement of nicotinic acid. Conclusions Electrostatic interaction between the carboxyl group of the nicotinic acid and the amine groups of the dendrimers is involved.

Fibrosis ; Hematoma, Subdural ; Humans ; Osteogenesis ; Subdural Space ; Tomography, X-Ray Computed

Adenocarcinoma ; metabolism ; pathology ; surgery ; Adenoma ; metabolism ; pathology ; surgery ; Adult ; Aged ; Colorectal Neoplasms ; metabolism ; pathology ; surgery ; Female ; Humans ; Intestinal Mucosa ; metabolism ; pathology ; Lymphatic Metastasis ; Male ; Middle Aged ; Neoplasm Staging ; Receptors, CXCR ; metabolism ; Young Adult

Acute-on-chronic kidney disease (ACKD) increases the risk of progression of chronic kidney disease (CKD). This study aimed to evaluate the ability of a novel criteria of reference change value of the serum creatinine optimized criteria for acute kidney injury in CKD (cROCK) to detect ACKD patients. Methods: This was a retrospective observational study with a 3-year follow-up. All included patients with CKD stage 3 were evaluated using cROCK, Kidney Disease Improving Global Outcomes (KDIGO), and their combined criteria. The renal composite endpoints, major adverse cardiovascular events (MACEs), and all-cause mortality were recorded as clinical outcomes. Results: A total of 812 patients was enrolled. The cROCK criteria detected more ACKD events than did the KDIGO (68.0% vs. 59.5%, p < 0.001). Compared to KDIGO (−) & cROCK (−) group, ACKD patients diagnosed by cROCK had significantly higher hazard ratio [HR] for renal composite endpoints (HR, 3.591; p < 0.001), MACEs (HR, 1.748; p < 0.001), and all-cause mortality (HR, 2.985; p < 0.001). The patients in KDIGO (+) & cROCK (+) group had the lowest survival probability when considering renal composite endpoints, MACEs, and all-cause mortality (all p < 0.001). Furthermore, cROCK resulted in the largest area under the receiver operating characteristic curve (AUC) for predicting renal composite endpoints, and the combined criteria led to the largest AUC for predicting MACEs and allcause mortality. Conclusion: Compared to the KDIGO, the cROCK detected more ACKD events. Combining both cROCK and KDIGO criteria might improve the predictive ability for long-term outcomes in ACKD patients.

Objective To investigate allopurinol ( a xanthine oxidase in-hibitor) improves insulin resistance of rats fed with high -fructose diet. Methods Male Wistar rats were randomly divided into 3 groups and each group was fed one of the following diets for 4 weeks:standard chow diet(normal group), high -fructose diet(model group), and high -fructose diet plus allopurinol(allopurinol 25μg? g-1, test group).Insu-lin sensitivity index was assessed from the oral glucose tolerance test ( OGTT) and the euglycemic clamp studies .Results Serum uric acid and plasma insulin concentrations were significantly decreased with allo-purinol treatment.That the serum uric acid of the model group with (1.82 ±0.10 ) mg? dL-1 was significantly increased than normal group with ( 1.33 ±0.12 ) mg? dL-1 , and improved by test group with (0.90 ±0.27) mg? dL-1.There was no difference in the levels of glu-cose with OGTT among the 3 groups.The model group produced a marked decrease in insulin sensitivity index ( GIR) compared with normal group (P<0.05).Allopurinol treated high -fructose fed rats showed a signifi-cant increase in GIR , reaching a similar level as that of the normal group (P<0.05).Conclusion Allopurinol may improve of insulin resistance in high-fructose induced insulin resistant .

OBJECTIVETo observe the effect of Kanglaite injection(KLT) on the proliferation and telomerase activity of mesangial cells in rats.

METHODMTT, telomere repeat amplification protocal (TRAP), ELISA, PAGE and silver-stain were applied to detect the growth rate and telomerase activity of MC after stimulation of KLT and IL-1.

RESULTThe growth rate of MC was enhanced by IL-1 stimulation, which was accompanied with a redection of the activity of telomerase. Adversely, the growth rate of MC was reduced by KLT, which was accompanied with an enhancement of activity of telomerase. Moreover, the growth rate of MC and the activity of telomerase were both inhibited by the combinative use of IL-1 and KLT without any influence from the sequence of their administration.

CONCLUSIONKLT could inhibit proliferation and telomerase activity of MC with or without pre-stimulation with IL-1. KLT might be useful to prevent and treat glomerular nephritis related to MC proliferation.

Animals ; Cell Proliferation ; drug effects ; Cells, Cultured ; Coix ; chemistry ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacology ; Glomerular Mesangium ; cytology ; enzymology ; Injections ; Plant Oils ; administration & dosage ; isolation & purification ; pharmacology ; Plants, Medicinal ; chemistry ; Rats ; Seeds ; chemistry ; Telomerase ; metabolism

OBJECTIVETo study the interaction of fluorine (F), calcium (Ca) and iodine (I) on body weight of rats.

METHODSOne-month-old Wistar rats were randomly divided into 8 groups: moderate concentrations of F, Ca, I (group 1); moderate concentrations of F, I and high concentration of Ca (group 2); moderate concentrations of Ca, I and high concentration of F (group 3); moderate concentration of I and high concentrations of F, Ca (group 4); moderate concentrations of F, Ca and low concentration of I (group 5); moderate concentration of F,high concentration of Ca and low concentration of I (group 6); moderate concentration of Ca, high concentration of F and low concentration of I (group 7); high concentrations of F, Ca and low concentration of I (group 8) based on 2 x 2 x 2 factorial design. The moderate concentration of F was 90 microg/d and the high concentration of F was 2700 microg/d. The moderate Ca concentration was 13 mg/d and the high Ca concentration was 260 mg/d. The moderate concentration of I was 3.5 microg/d and the low concentration of I was 0.23 microg/d. After twenty weeks, body weight was measured.

RESULTSAccording to the results of factorial ANOVA, significant interaction effects of F with Ca were found (F = 5.933, P = 0.017). The empty body weight was measured at the end of the fifth month. When both iodine and fluorine were at the optimal level, the weight of group 2 [(262.5 +/- 47.1) g] and group 1 [(307.9 +/- 55.0) g] showed significant difference (t = 4.24, P < 0.05). When both iodine and fluorine were at low level, the weight of group 6 [(248.8 +/- 30.0) g] and group 5 [(293.3 +/- 19.7) g] showed significant difference (t = 4.16, P < 0.05). Animals with optimal iodine and calcium [(269.3 +/- 27.3) g] showed significant difference compared to the weight of low level iodine and optimal fluorine [(307.9 +/- 55.0) g]. When the low level iodine and optimal calcium were applied, weight of group 7 [(261.9 +/- 31.3) g] and group 5 [(293.3 +/- 19.7) g] showed significant difference. (t = 2.94, P < 0.05).

CONCLUSIONInteraction effects of F with Ca were found on body weight in rats.

Animals ; Body Weight ; drug effects ; Calcium, Dietary ; pharmacology ; Drug Interactions ; Female ; Fluorides ; Fluorine ; pharmacology ; Iodine ; pharmacology ; Male ; Rats ; Rats, Wistar

This article is report the study of the pharmacokinetics and metabolic disposition of exogenous phosphocreatine (PCr) in rats by means of an ion-pair HPLC-UV assay. PCr and its metabolite creatine (Cr) and related-ATP in rat plasma and red blood cell (RBC) were simultaneously determined. A blank plasma and RBC were initially run for baseline subtraction. Plasma and RBC samples were deproteinized with 6% PCA prior to HPLC. Following i.v. administration of PCr 500 mg x kg(-1) and 1 000 mg x kg(-1) the C-T curve could be described by the two-compartment model with t1/2beta 22.5-23.3 min, V(d) 0.956 4-0.978 6 L x kg(-1), CL 0.029 L. kg(-1) x min(-1). The Cr as PCr degraded product appeared as early as 2 min post i.v. dosing with t(max) 20 min, t1/2kappa (m) 40.6-42.7 min and f(m) 60%-76%. After po administration of PCr, the parent drug in plasma was undetectable, but the metabolite Cr was detected with t(max) 65-95 min, t1/2kappa (m) 56.0-57.7 min, metabolite-based bioavailability F(m) 55.02%-62.31%. PCr i.v. administration resulted in significant elevation of ATP level in RBC but not in plasma, the related-ATP in RBC was characterized by t(max) 68-83 min, t1/2kappa 49-52 min. In RBC no exogenous PCr was found but Cr was detected following i.v. administration of PCr, with the t(max) 120 min and t1/2k (m) 70 min for Cr. The above results indicate that PCr eliminates and bio-transforms in body very rapidly; K > K(m) confers ERL, instead of FRL, type upon the metabolic disposition of Cr. Following po administration of PCr, the degraded product Cr is absorbed but not the parent drug PCr. The formed Cr can be accounted for by most of i.v. and po PCr. Intravenous dosing leads apparently increased and sustained Cr and related-ATP concentration in RBC.
Adenosine Triphosphate ; blood ; pharmacokinetics ; Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Biotransformation ; Cardiotonic Agents ; administration & dosage ; blood ; pharmacokinetics ; Creatine ; administration & dosage ; metabolism ; pharmacokinetics ; Erythrocytes ; metabolism ; Injections, Intravenous ; Male ; Phosphocreatine ; administration & dosage ; blood ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo study the chemical constituents of the leaf of Isatis indigotica.

METHODChromatography and spectral analysis were respectively used to isolate and identify the constituents.

RESULTThree compounds were isolated from the ethanol extracts of theleaf of I. indigotica, and identified as indirubin, tryptanthrin and L-pyroglutamic acid.

CONCLUSIONL-pyroglutamic acid was isolated from the genus for the first time, and tryptanthrin was isolated from the leaf of this plant for the first time.

Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Indoles ; chemistry ; isolation & purification ; Isatis ; chemistry ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Pyrrolidonecarboxylic Acid ; chemistry ; isolation & purification ; Quinazolines ; chemistry ; isolation & purification