Search

The purpose of this study was to explore the effect of polydatin on ventricular remodeling after myocardial infarction in coronary artery ligation rats and to elucidate the underlying mechanisms. A rat model of ventricular remodeling after myocardial infarction was established by left coronary artery ligation. Rats with coronary artery ligation were randomly divided into five groups: control, plus 40 mg/kg captopril, plus 25 mg/kg polydatin, plus 50 mg/kg polydatin, and plus 100 mg/kg polydatin. The sham-operated group was used as a negative control. Rats were administered intragastrically with the corresponding drugs or drinking water for seven weeks. At the end of the treatment, the left ventricular weight index and heart weight index were assessed. The cross-sectional size of cardiomyocytes was measured by staining myocardium tissue with hematoxylin and eosin. Collagen content was counted by Sirius red in aqueous saturated picric acid. The concentrations of angiotensin I, angiotensin II, aldosterone, and endothelin 1 in myocardium or serum were determined by radioimmunoassay. Hydroxyproline and nitric oxide concentrations and glutathione peroxidase and catalase activities in serum were measured by ultraviolet spectrophotometry. Our results showed that seven weeks of polydatin treatment resulted in a significantly reduced left ventricular weight index, heart weight index, serum concentrations of hydroxyproline and aldosterone, an increased concentration of nitric oxide as well as enhanced activities of glutathione peroxidase and catalase. Myocardial angiotensin I, angiotensin II, and endothelin 1 levels were also reduced. The cardiomyocyte cross-sectional area and collagen deposition diminished. This study suggests that polydatin may attenuate ventricular remodeling after myocardial infarction in coronary artery ligation rats through restricting the excessive activation of the renin-angiotensin-aldosterone system and inhibiting peroxidation. [ABSTRACT FROM AUTHOR]

In this study, we investigated the inhibition of spontaneous canine benign prostatic hyperplasia by a crude polysaccharide fraction extracted from Urtica fissa roots and stems. After oral administration of U. fissa polysaccharide fraction for 3 months, the dog prostatic volume reduced significantly when compared to that before treatment using CT examination. The high-dosage U. fissa polysaccharide fraction (120 mg/kg body weight/ day) and finasteride (0.5 mg/kg body weight/day) treatments showed both almost 30% reduction of the initial prostatic volume. At the end of the administration of U. fissa polysaccharide fraction, the prostates were excised, and the volumes were measured by water displacement. The prostatic volume showed significant decrease by 11%, 15%, and 21% for the 30, 60, and 120 mg/kg/day U. fissa polysaccharide fraction treatment groups, respectively, compared to the control group. Histological observation found that U. fissa polysaccharide fraction inhibited the dog prostatic epithelial cells proliferation and enlarged glandular lumen diameter. The crude polysaccharide fraction of U. fissa is a possible new candidate for the treatment of benign prostatic hyperplasia. [ABSTRACT FROM AUTHOR]

Four new hydroxycinnamic acid amides, scotanamines A-D (1-4), and seven known alkaloids, including N¹, N10-di-dihydrocaffeoylspermidine (5), scopolamine (6), anisodamine (7), hyoscyamine (8), anisodine (9), caffeoylputrescine (10), and N¹-caffeoyl-N³-dihydrocaffeoylspermidine (11), were obtained from the roots of Scopolia tangutica. The present study represents the first recognition of hydroxycinnamic acid amides containing putrescine or spermidine in S. tangutica. Compound 1, in particular, contains a moiety resulting from the condensation of nortropinone and putrescine. Compound 2 exhibited moderate agonist activity at the µ-opioid receptor (EC50 = 7.3 µM). Compound 2 was tested in vivo and induced analgesia analgesia in mice. The analgesic effect was recorded using the tail-flick assay and was reversed by naloxone. [ABSTRACT FROM AUTHOR]

This work describes an immunochemical approach for the quality control of Panax ginseng and a pharmacological study of ginsenoside Re, a major bioactive constituent in P. ginseng, using an enzyme-linked immunosorbent assay. A hybridoma secreting monoclonal antibody against ginsenoside Re was produced by fusing splenocytes immunized with a ginsenoside Re-bovine serum albumin conjugate with the hypoxanthine-aminopterinthymidine-sensitive mouse myeloma SP2/0 cell line. The method, at an effective measuring range of 7.8-500 ng ⋅ mL-1 of ginsenoside Re, successfully detected ginsenoside Re in Chinese traditional herb prescriptions. The results demonstrate that we generated a novel and reliable assay system for measuring ginsenoside Re in Chinese medicines more efficiently. Futhermore, we determined the ginsenoside Re concentrations in the saliva of six healthy adults after the oral administration of a ginseng capsule to study the pharmacokinetics of ginsenoside Re in human saliva. [ABSTRACT FROM AUTHOR]

Total steroid saponins isolated from Dioscorea zingiberensis have shown a variety of beneficial bioactivities. However, there are no reports about their neuroprotective effects, until now. Therefore, in the present study, we explored the neuroprotective effects of the total steroid saponins from D. zingiberensis on rats against transient focal cerebral ischemia-reperfusion and their underlying mechanisms. Healthy adult Sprague- Dawley rats were randomly assigned to six groups. After pretreatment with D. zingiberensis total steroid saponins intragastrically for six days, the rats were subjected to an ischemia injury by surgery on the middle cerebral artery occlusion for 90min. Compared to the ischemia-reperfusion group, the D. zingiberensis total steroid saponin group of rats, especially those given a 30-mg/ kg dose, showed not only a marked reduction in neurological deficit scores, cerebral infarct volume, and brain edema, but also an increase in neuron survival (Nissl bodies) in the hippocampal cornuammons 1 and cortex hemisphere of the ipsilateral ischemia. At the same time, the inflammatory cytokines in serum induced by themiddle cerebral artery occlusion were significantly decreased by the preadministration of D. zingiberensis total steroid saponins. Furthermore, the increase of caspase-3 was evidently reduced in the hippocampal cornuammons 1 and cortex of the hemisphere injured brain. Finally, the downregulating antiapoptotic Bcl-2 and upregulating proapoptotic Bax proteins were obviously suppressed. Taken together, the current findings suggest that D. zingiberensis total steroid saponins played a potential neuroprotective role against a severe injury induced by transient focal cerebral ischemic reperfusion in a rat experimental model, and this role may be mediated by its anti-inflammatory and antiapoptotic actions. [ABSTRACT FROM AUTHOR]

Quercetin is one of the most common flavonoids in the human daily diet. Its affects the coronary artery, especially L-type voltage-gated Ca2+ channels and voltage-gated K+ channels in the arterial smooth muscle cells, which are poorly understood. The present experiments were designed to study the myogenic effect of quercetin and its possible underlying mechanisms in the rat coronary artery. A wire myograph was used to observe themyogenic effects. Arterial smooth muscle cells were freshly isolated from the rat coronary artery and the intracellular free Ca2+ concentration was measured with molecular probe fluo-4-AM. The effects of quercetin on L-type voltage-gated Ca2+ channels and voltage-gated K+ channels were studied using a whole-cell patch clamp. Quercetin (3-30 µM) produced a depression and relaxation on the contraction induced by KCl or the thromboxane A2 analog 9,11-Dideoxy-9α,11α-methanoepoxy prostaglandin F2a. The vasorelaxation was attenuated by 4-aminopyridine, a specific voltage-gated K+ channel inhibitor, but was not affected by the NG-nitro-L-arginine methylester ester (a nitric oxide synthesis inhibitor), glibenclamide (a ATP-activated K+ channel inhibitor), iberiotoxin (a Ca2+-activated K channel inhibitor), BaCl2 (an inward rectifier K channel inhibitor), or by endothelium denudation. At the same concentrations, quercetin reduced the KCl-induced elevation of the intracellular free Ca2+ concentration, inhibited the inward Ca2+ currents through L-type voltage-gated Ca2+ channels, and increased the outward K+ currents through voltage-gated K+ channels in the rat coronary artery smooth muscle cells. Collectively, our results demonstrate that quercetin possesses vasospasmolytic effects in RCA and suggest that depression of the Ca2+ influx through L-type voltage-gated Ca2+ channels and augmentation of voltage-gated K+ channel activity in the myocytes may underlie coronary relaxation. [ABSTRACT FROM AUTHOR]

The pharmacokinetics and anti-inflammatory effects of Sanhuang Xiexin Tang, composed of Rhei Radix et Rhizoma, Scutellariae Radix, and Coptidis Rhizoma, prepared by decoction and maceration, were investigated and compared. Rats were orally administered with the decoction and maceration of Sanhuang Xiexin Tang at 30 g/kg. The concentrations of 10 active constituents (berberine, palmatine, jatrorrhizine, coptisine, wogonin, baicalin, wogonoside, emodin, aloe-emodin, and rhein) in plasma were determined by UPLC-MS/ MS. Mice were orally administered decoctions and macerations of Sanhuang Xiexin Tang continuously for 7 days at three doses and stimulated with lipopolysaccharide. The plasma concentrations of IL-10 and TNF-α were determined by ELISA. Different preparation methods resulted in significant differences in the pharmacokinetic characteristics of the SXT constituents, especially the protoberberine alkaloids. Maceration decreased the absorption of flavones while promoting the absorption of anthraquinones. Bioavailability of both flavones and anthraquinones increased after administration of macerated Sanhuang Xiexin Tang, especially those of baicalin and rhein, which increased by 3.27 and 7.10 times. Results of ELISA indicated that both the decoction and maceration of Sanhuang Xiexin Tang could significantly increase IL-10 production (p < 0.01) as well as decrease TNF-α production (p < 0.01). Macerated Sanhuang Xiexin Tang has a slightly higher antiinflammatory effect than the Sanhuang Xiexin Tang decoction. Different preparation methods affected the pharmacokinetic characteristics and anti-inflammatory effects of Sanhuang Xiexin Tang's active constituents. [ABSTRACT FROM AUTHOR]

Baicalin is a major bioactive component of Scutellaria baicalensis and a substrate of multiple drug resistance-associated protein 2. Expression of multiple drug resistance-associated protein 2 is regulated by NF-E2-related factor 2. The aim of this study was to explore whether ursodeoxycholic acid, an NF-E2-related factor 2 activator, could influence the oral bioavailability of baicalin. A single dose of baicalin (200 mg/kg) was given orally to rats pretreated with ursodeoxycholic acid (75mg/kg and 150 mg/kg, per day, intragastrically) or normal saline (per day, intragastrically) for six consecutive days. The plasma concentration of baicalin was measured with the HPLC method. The result indicated that the oral bioavailability of baicalin was significantly and dosedependently reduced in rats pretreated with ursodeoxycholic acid. Compared with control rats, the mean area under concentration-time curve of baicalin was reduced from 13.25±0.24mg/L h to 7.62±0.15mg/L h and 4.97±0.21mg/L h, and the Cmax value was decreased from 1.31±0.03 mg/L to 0.62±0.05mg/L and 0.36±0.04 mg/L in rats pretreated with ursodeoxycholic acid at doses of 75 mg/kg and 150 mg/kg, respectively, for six consecutive days. Hence, ursodeoxycholic acid treatment reduced the oral bioavailability of baicalin in rats, probably due to the enhanced efflux of baicalin from the intestine and liver by multiple drug resistance-associated protein 2. [ABSTRACT FROM AUTHOR]