The State Key Laboratories of Pharmacodynamics and Pharmacokinetics

Tianjin, China

The State Key Laboratories of Pharmacodynamics and Pharmacokinetics

Tianjin, China
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Liu Z.,Tianjin University | Gao W.,Tianjin University | Man S.,Tianjin University of Science and Technology | Zhang Y.,Tianjin University | And 4 more authors.
Environmental Toxicology and Pharmacology | Year: 2014

Rhizoma Paridis saponins (RPS) with a good antitumor effect in clinical use showed low bioavailability and toxicity. Combination of Rhizoma Curcuma longa with RPS, which called LouHuang preparation (LH), not only overcame the RPS limitations but also improved its anticancer effect. The median lethal dose (LD50) of LH in mice was 3410.9mg/kg by oral acute toxicity test. LH relieved the inhibition of RPS on the gastric emptying (70.13±4.80% vs. 49.12±8.06%). As for the antitumor effect, the tumor weight/volume inhibition rate, tumor volume growth rate, and water/food efficiency ratio were calculated. LH had the highest inhibition ratio of 57.07±2.97% for H22 model, 43.22±0.72% for S180 model, and 46.8±0.97% for EAC model, which were higher than RPS. Compared to ZiLongJin (ZLJ), a marked antitumor drug in China, LH also had the higher inhibition rate for tumor weight and tumor volume growth, which weaker than CTX. The water/food efficiency ratio reflected the difference of the quality life of the mice bearing tumor cells or not. CTX attenuated body weight gain and increased food efficiency ratio compared to control group. LH did not affect the body weight or water/food intake. The active part of LH was RPS and turmeric polysaccharides with the inhibition of 58% and 47% on H22 and S180 tumor models. The research provided theoretical and practical basis for LH application. © 2014 Elsevier B.V.


PubMed | College of Logistics, Tianjin University and The State Key Laboratories of Pharmacodynamics and Pharmacokinetics
Type: Journal Article | Journal: Journal of ethnopharmacology | Year: 2014

Cerebralcare Granule (CG), one of the famous classical recipes in traditional Chinese medicine, is developed from the Decoction of Four Drugs. It has been used for treatment of cerebrovascular related diseases, such as hypertension. It is well known that vasodilatation plays a very important role in hypertensive. Despite the popular medicinal use of CG, little data was available to its activity and mechanism involved in vasodilatation. Therefore, we aimed to investigate the vasorelaxant effects of CG on isolated rat thoracic aorta so as to assess some of the possible mechanisms. The present study was performed to examine the vasodilative activity of CG and its mechanisms in isolated rat thoracic aorta.CG was studied on isolated rat thoracic aorta in vitro, including endothelium-intact and endothelium-denuded aortic rings. In present study, specific inhibitors including NO synthase inhibitor NG-nitro-L-arginine methyl ester (L-NAME), cyclooxygenase (COX) inhibitor indomethacin (INDO), non-selective K+ channel inhibitor tetraethylammonium chloride (TEA), Kir channel inhibitor BaCl2, KATP channel inhibitor Glibenclamide (Gli) and cholinergic receptor antagonist atropine were used, they were added 20 min before NE contraction and then added CG-induced vasodilation.Removal of endothelium or pretreatment of aortic rings (intact endothelium) with L-NAME (0.1 mM) or INDO (0.01 mM) significantly blocked the CG induced relaxation. Pretreatment with the non-selective K+ channel inhibitor TEA (1 mM), or the Kir channel inhibitor BaCl2 (0.1 mM), neither of them had no influence on the CG-induced response (p>0.05). However, pretreatment with the KATP channel inhibitor Gli (0.01 mM) produced significant inhibition on the CG-induced response (p<0.01). Besides, CG also inhibited the contraction triggered by NE in endothelium-denuded rings in Ca2+-free medium. CG (0.4, 0.8 and 3.2 mg/mL) produced rightward parallel displacement of CaCl2 curves and reduced the maximum contraction induced by 30 mM CaCl2 to 31.19.3%, 18.86.9% and 9.44.5%, respectively. The relaxation, induced by CG on endothelium-intact rat aortic rings pre-contracted with NE, was significantly attenuated in the presence of atropine (EC50=3.7 mg/mL, p<0.01).Our results suggest that CG induces relaxation in rat aortic rings through an endothelium-dependent pathway mediated by NO/cGMP pathway and an endothelium-independent pathway involving blockade of Ca2+ channels, inhibition of Ca2+ mobilization from intracellular stores, opening of KATP channel. In addition, the muscarinic receptor stimulation is also one of the vasorelaxant mechanisms.


PubMed | The State Key Laboratories of Pharmacodynamics and Pharmacokinetics, Tianjin University and College of Logistics
Type: Journal Article | Journal: Iranian journal of pharmaceutical research : IJPR | Year: 2014

High performance liquid chromatography (HPLC) with diode array detection (DAD) and electrospray ionization tandem mass spectrometry (ESI/MS/MS) was used to analyze the main components in the methanol extract of Fructus Aurantii (FA) and the metabolites in rat biological samples after oral administration of the methanol extract of FA. There were 31 constituents identified in the extract of FA including 2 alkaloids, 1 coumarin, 10 flavonoid glycosides and 18 ploymethoxylated flavones. According to the UV spectrum and MS fragment character of main components in the methanol extract of FA, 18 parent constituents and 11 metabolites were tentatively identified in rat biological samples. Three groups of components in biological samples detected included flavonoid glycosides, their glucuronides and ploymethoxylated flavones. It was interested that flavonoid glycosides, their glucuronides and ploymethoxylated flavones can be investigated in rat plasma and urine, while in rat feces samples only flavonoid glycosides were detected. Triglycosyl, naringenin, neoeriocitrin, neoeriocitrin narirutin and hesperidin were the main components in rat feces which were found either in the plasma or in urine samples. However, naringin and neohesperidin were the main flavonoid glycosides which absorbed after oral administration. Except flavonoid glycosides and their glucuronides, ploymethoxylated flavones also the constituents absorbed because it was investigated mainly in rat plasma and urine but not in feces samples. The identification and elucidation of parent and metabolism components analyzed in biological samples provided the data for further pharmacological and clinical research on FA.


PubMed | College of Logistics, Tianjin University and The State Key Laboratories of Pharmacodynamics and Pharmacokinetics
Type: Journal Article | Journal: Journal of ethnopharmacology | Year: 2014

Wei-Chang-An pill (WCA pill), a traditional Chinese medicine, has been used for treating various gastrointestinal diseases for several decades. Despite the popular medicinal use of WCA pill, less data was available to its activity and mechanism in gastrointestinal disorders. To examine the effects of the methanol extract of WCA pill (ME) on gastrointestinal tract so as to assess some of the possible mechanisms involved in the clinical treatment.ME was studied on gastrointestinal transit in vivo including gastric emptying and small intestinal motility in normal and neostigmine-induced mice, as well as on the isolated tissue preparations of rat jejunum in vitro.In vivo, the gastric emptying decreased and intestinal transit increased after administration of ME in normal mice. However, administration of ME accelerated the intestinal transit ranging from 0.01 to 0.8 mg/mL and reduced it at the concentration of 1.6 and 3.2 mg/mL, while the gastric emptying was inhibited throughout the concentrations in neostigmine-induced mice. in vitro, ME caused inhibitory effect on the spontaneous contraction of rat-isolated jejunum in dose-dependent manner ranging from 0.01 to 6 mg/mL and also relaxed the acetylcholine chloride (Ach, 10(-6) M)-induced and K+ (60 mM)-induced contractions. ME shifted the Ca2+ concentration-response curves to right, similar to that caused by verapamil (0.025 mM).These results indicated that ME might play a bidirectional role in gastrointestinal transit modulation and the effects on isolated tissue are probably mediated through calcium influx and muscarinic receptors, which provides pharmacological basis for the clinical use of WCA pill in gastrointestinal tract disorders.


Jiang Q.,Tianjin University | Gao W.,Tianjin University | Li X.,Tianjin University | Xia Y.,Tianjin University | And 5 more authors.
Food Hydrocolloids | Year: 2012

The physicochemical, morphological and crystal structure characterization of the starches separated from rhizomes of Dioscorea opposita Thunb. Dioscorea alata Linn., Dioscorea nipponica Makino, Dioscorea bulbifera Linn. and Dioscorea septemloba Thunb. were studied and compared. Amylose content varied between 13.58% and 20.05%. Water-binding capacity, swelling power, solubility and total starch content of starches differed significantly. Scanning electron micrographs revealed that the surface was smooth or rough, the granules were oval to spherical and the size was obviously different. D. nipponica displayed A-type pattern. D. opposita D. alata, D. septemloba and D. bulbifera starches all exhibited C-type crystal. While the crystallinity degree of the starches separated from the five species were about 33.90%, 37.63%, 43.11%, 32.06% and 53.35%, respectively. The gelatinization transition temperatures (T o, T p and T c) and enthalpy of gelatinization (ΔH gel) and peak height index (PHI) were determined. D. OT, D. AL and D. BL starches showed the higher enthalpy of gelatinization. Pasting viscosity of D. OT and D. BL starches were much higher than others. The five plants could be separated into two groups: D. OT, D. AL and D. BL; D. ST and D. NM. © 2012 Elsevier Ltd.


Jiang Q.,Tianjin University | Gao W.,Tianjin University | Li X.,Tianjin University | Man S.,Tianjin University of Science and Technology | And 4 more authors.
Food Hydrocolloids | Year: 2014

The effect of alkali-treatment for 0, 15, and 30 days at 35°C on amylose content, morphological properties, crystalline properties, swelling power, solubility, absorbance spectra and invitro digestibility of starches from Dioscorea zingiberensis, Dioscorea persimilis and Dioscorea opposita were investigated. The amylose content of all the three starches decreased after 15 days of alkaline treatment and then increased after 30 days of alkaline treatment. There were similar changes in relative crystallinity for D.zingiberensis and D.persimilis starches. It was observed that the three starches displayed a reduction trend in swelling power with a significant increase in solubility. Adhesion among some of the starch granules was observed after alkali-treatment for 30 days in D.zingiberensis and D.opposita starches, while D.persimilis starch showed some hollows on the granule surface. The rise in the absorbance ratio of 1047/1035 and 1047/1022cm-1 from FT-IR was observed during alkali-treatment for D.persimilis and D.opposita starches. Alkali-treatment elevated the invitro digestibility with resistant starch values climbing up from 50.16% to 64.95% and from 66.14% to 70.74% for D.zingiberensis and D.persimilis starches, respectively, but there was no significant change in resistant starch value for D. opposita starch. © 2014 Elsevier Ltd.


Man S.,Tianjin University | Gao W.,Tianjin University | Zhang Y.,Tianjin University of Traditional Chinese Medicine | Huang L.,Chinese Institute of Materia Medica | Liu C.,The State Key Laboratories of Pharmacodynamics and Pharmacokinetics
Biomedical Chromatography | Year: 2011

On-line ultra-performance liquid chromatography (UPLC) coupled with diode-array detection (UPLC/DAD) and electrospray ionization quadrupole time-of-flight mass spectrometry (ESI-Q-TOF-MS) were used for separation, identification and structural analyses of saponins in Rhizoma Paridis saponins (RPS) and rat plasma after oral administration of RPS. Thirty steroidal saponins in RPS were identified by comparing their retention time, accurate mass measurement and positive and negative mass spectrometry data with that of reference compounds. The UPLC/Q-TOF-MS method was proved to be rapid and efficient in that 30 steroidal saponins, including three kinds of saponins (prototype, pennogenyl and diosgenyl saponins) were tentatively characterized within 6min. After oral administration of RPS, 21 original saponins were absorbed in RPS-treated rat plasma. Our results indicated that UPLC/Q-TOF-MS is a rapid and effective tool for identification of a series of saponins at trace level. © 2010 John Wiley & Sons, Ltd.


Man S.,Tianjin University | Gao W.,Tianjin University | Zhang Y.,Tianjin University of Traditional Chinese Medicine | Wang J.,Tianjin University | And 3 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2010

High-performance liquid chromatographic (HPLC) with evaporative light scattering detection (ELSD) and HPLC with electrospray ionization multistage tandem mass spectrometry (HPLC-ESI-MS n) were used to identify and quantify steroid saponins in Paris and Trillium plants. The content of the known saponins such as Paris I, II, III, V, VI, VII, H, gracillin and protodioscin in Paris and Trillium plants was determined simultaneously using the developed HPLC-ELSD method. Furthermore, other 12 steroid saponins were identified by HPLC-ESI(+/-)-MS n detection. In the end, a developed analytical procedure was proved to be a reliable and rapid method for the quality control of Paris and Trillium plants. In addition, the alternative resources for Paris yunnanensis used as a traditional Chinese medicine were discovered according to the hierarchical clustering analysis of the saponin fraction of these plants. © 2010 Elsevier B.V.


PubMed | The State Key Laboratories of Pharmacodynamics and Pharmacokinetics and Tianjin University
Type: Journal Article | Journal: Neurochemical research | Year: 2016

Cerebralcare granule() (CG) is a preparation of Traditional Chinese Medicine that widely used in China. It was approved by the China State Food and Drug Administration for treatment of headache and dizziness associated with cerebrovascular diseases. In the present study, we aimed to investigate whether CG had protective effect against D-galactose (gal)-induced memory impairment and to explore the mechanism of its action. D-gal was administered (100mg/kg, subcutaneously) once daily for 8weeks to induced memory deficit and neurotoxicity in the brain of aging mouse and CG (7.5, 15, and 30g/kg) were simultaneously administered orally. The present study demonstrates that CG can alleviate aging in the mouse brain induced by D-gal through improving behavioral performance and reducing brain cell damage in the hippocampus. CG prevents aging mainly via suppression of oxidative stress response, such as decreasing NO and MDA levels, renewing activities of SOD, CAT, and GPx, as well as decreasing AChE activity in the brain of D-gal-treated mice. In addition, CG prevents aging through inhibiting NF-B-mediated inflammatory response and caspase-3-medicated neurodegeneration in the brain of D-gal treated mice. Taken together, these data clearly demonstrates that subcutaneous injection of D-gal produced memory deficit, meanwhile CG can protect neuron from D-gal insults and improve memory ability.


PubMed | The State Key Laboratories of Pharmacodynamics and Pharmacokinetics and Tianjin University
Type: | Journal: Journal of agricultural and food chemistry | Year: 2016

Prunella vulgaris L. is as a major plant in the Chinese traditional functional beverage Guangdong herbal tea for the treatment of fevers, diarrhea, and sore mouth. In this study, ethyl acetate parts of aqueous extracts from P.vulgaris L. (EtOAc-APV) were found to demonstrate potent acetylcholinesterase (AChE) inhibition in vitro. Therefore, this study was designed to further investigate the effects of EtOAc-APV on scopolamine (SCOP)-induced aging rats. Male Wistar rats were randomly divided into four groups (n = 12) and given orally by gavage EtOAc-APV (100 mg/kg) for 3 weeks. SCOP (1 mg/kg, ip) was administered to rats 30 min before starting behavioral tests consecutively for 3 days. EtOAc-APV could attenuate SCOP-induced brain senescence in rats by improving behavioral performance and decreasing brain cell damage, which was associated with a notable reduction in AChE activity and MDA level, as well as an increase in SOD and GPx activities. Additionally, EtOAc-APV administration could reduce the expression of NF-B and GFAP, which showed an anti-neuroinflammatory effect on the SCOP-treated rat. Overall, the current study highlights P.vulgaris L. as an antidementia dietary supplement.

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