Objective To explore the effects of phentolamine on the function of the islets isolated from normal rats.Methods The SD rats islets were isolated by digestive method with collagenase and DNase.Millipore Multiscreen Assay System was used to observe the effects of phentolamine on the function of isolated islets. Insulin and glucagon were measured by RIA. Results ⑴Insulin secretion of the isolated islets incubated in culture medium was glucose concentration-dependent manner. Phentolamine had stimulate insulin secretion significantly. Nifedipine (Ca 2+ channel blocker) and diazoxide (K + channel opener) had inhibit the insulin release, but their effects were abolished by phentolamine. ⑵Glucagon secretion of the isolated islets in culture medium incubated was inhibited by glucose. Phentolamine inhibited glucagon secretion significantly, and the inhibiting effect was also concentration-dependent manner,both the nifedipine and diazoxide had the effect too. Conclusion Phentolamine could stimulate insulin secretion, and inhibit glucagon secretion in the isolated islets.It maybe has some hypoglycemic effects on diabetes.

Objective To explore the effects of the clonidine-displacing substance(CDS)on the function of isolated islets from normal rats. Methods The SD rat islets were isolated by digestive method with collagenase and DNase, and incubated in RPMI 1640 culture medium overnight. Multiscreen Assay System was used to observe the effects of CDS on the function of the isolated islets. Insulin and glucagon were measured by RIA. Results Glucagon secretion of the isolated islets in incubation medium was inhibited by glucose. CDS could significantly inhibit glucagon secretion in concentration-dependent manner. Insulin secretion of the isolated islets was dependent on the glucose concentration of incubation medium. CDS could stimulate insulin secretion significantly. Nifedipine (Ca 2+ channel blocker) and diazoxide (K + channel opener) could inhibit the insulin release of the isolated islets, the effect of which could be abolished by CDS. Conclusion As an endogenous ligand of imidazoline receptors, CDS could stimulate insulin secretion, and inhibit glucagon release in the isolated islets.

Inflammation is one of the key pathological process of atherosclerosis (AS),and multiple risk factors of AS have consanguineous relationships with the regulation of inflammatory signal pathway.So it could be effective approach to control inflammation,even the pathological process of AS if we do the deep research on AS inflammatory signal pathway and make out the potential medicine.

Atherosclerosis(AS),the major cause of ischemic cerebrovascular disorder(CVD)destroying human health,the damage-reaction theory and inflammation theory proposed by professor Ross were popular because those theories were explainning the beginning and developing of AS well.The key point is anti-inflammatory.Through the intervention of some key factors in inflammatory response network,the theory provide a great significance and value on the treatment of AS.We considered that AS pathogenesis of "Endogenous Heat Toxin,Phlegm and Blood Stasis" in Chinese medicine has substantial relationship with current mainstream theory of AS-"injury-response theory,inflammatory reaction theory",which is a good integrating point for AS pathogenesis in both theoretical systems of Chinese and Western Medicine.With the entry point of intervention of "Endogenous Heat Toxin" or "inflammatory response",on the basis of activating blood circulation to dissipate blood stasis and heat-clearing and detoxicating,it is a beneficial attempt with theoretical and practical significance to discuss the role of Chinese medicine on prevention and treatment of AS.With the mainline of AS anti-inflammatory theory,this article analyzed and discussed the research ideas of Chinese Herbs intervene AS inflammatory reaction combined with our work of the research group.

Neurodegenerative diseases are threating our health seriously.Inflammation plays an important role in the initiation and development of neurodegenerative diseases, and its primary characteristics are the activation of microglia and the increasing level of inflammation cytokines.This review describes the relationship between neuroinflammation and several neurodegenerative diseases, and the models in vivo and in vitro.In addition, combining with traditional Chinese medicines knowledge of encephalopathy, we summarizes pharmacological effects and mechanisms of multiple herb extracts and monomer compounds in preventing the activation of microglia and inhibiting neuroinflammation, thus, to provide the basis for gradually revealing the related rules and characteristics of treating encephalopathy by traditional Chinese medicine, and improving the accuracy of the clinical drugs, as well as developing new drugs for the prevention and control of encephalopathy.

The fruit of Ziziphus jujuba was known as fine quality in the Shennong's Herbal. It is sweet in taste and mild in property with the effect of regulating the middle, invigorating the spleen, assisting twelve meridians, harmonizing stomach-qi, unclogging nine orifices, and moderating hundreds of herbs. In recent years, the efficacies of Ziziphus jujuba have been widely studied with considerable meaningful achievements. In this article, main research progresses in recent ten years were reviewed, which included resources, chemical components and pharmacological effects of Ziziphus jujuba. The research and development of medication, health care product and food with Ziziphus jujuba as its main ingredient were summarized for further references in related studies.

OBJECTIVETo study the absorption characteristics of alkaloids in Coptis chinensis in rat intestinal.

METHODIn situ single-pass perfused rat intestinal model was used and the concentrations of berberine and palmatine were determined by HPLC, the drug absorption rate constant (K(a)) and apparent absorption coefficient (P(app)) were tested to evaluate their absorption characteristics.

RESULTThe absorption of berberine and palmatine in different regions of rat intestinals was significantly different. From bigness to smallness, the P(app) value of berberine at 50 mg x L(-1) were ileum, duodenum, jejunum and colon, of palmatine at 50 mg x L(-1) were ileum, colon, jejunum and duodenum. The concentration of berberine and palmatine had distinctive effect on the K(a) value of berberine and palmatine were ordered from larger to little as in Wujiwan compatibility, Coptis chinensis extractive and single compound.

CONCLUSIONThe berberine and palmatine were absroped at all regions of rat intestinal. The absorption characteristics of 2 alkaloids were not passive diffusion. The other ingredients in Wujiwan compatibility and Coptis chinensis extractive could promote the absorption of alkaloids.

Alkaloids ; pharmacokinetics ; Animals ; Berberine ; pharmacokinetics ; Berberine Alkaloids ; pharmacokinetics ; Coptis ; Intestinal Absorption ; Male ; Perfusion ; Rats ; Rats, Wistar

OBJECTIVEDevelop an LC-MS method to determine evodiamine and rutaecarpine in rats plasma simultaneously. The method was employed to investigate pharmacokinetics of evodiamine and rutaecarpine.

METHODBlood samples were collected in different time after oral administrated with the extracts of Euodiae Fructus, the plasma concentration of evodiamine and rutaecarpine was determined by LC-MS, pharmacokinetic parameters were calculated by WinNonlin 5.1 software.

RESULTThe linear ranges of evodiamine and rutaecarpine were 0.5-100 microg x L(-1) (r = 0.995 9), 1-200 microg x L(-1) (r = 0.999 3) respectively. The average recovery were exceeded 76% (n = 5), the precision of inner-day and inter-day were less than 15%. The pharmacokinetics parameters AUC, t1/2, CL _F of evodiamine were: (2 215.24 +/- 414.49), (4 230.62 +/- 753.77), (13 219.21 +/- 3 740.95) min x ng(-1) x mL(-1); (146.57 +/- 38.38), (114.38 +/- 14.65), (163.37 +/- 8.83) min; (184 607.29 +/- 32 502.21), (192 878.22 +/- 31 897.37), (19 3224.63 +/- 62 278.74) mL x min(-1). The pharmacokinetics parameters AUC, t1/2, CL_F of rutaecarpine were (2 283.53 +/- 298.51), (4 424.84 +/- 276.95), (14 239.93 +/- 3648.27) min x ng(-1) x mL(-1); (167.10 +/- 15.82), (131.58 +/- 20.07), (144.41 +/- 13.65) min; (1 177 340.54 +/- 2 4942.21), (181 262.92 +/- 11 162.22), (177 508.10 +/- 52 611.80) mL x min(-1).

CONCLUSIONThe method described in this report has high sensitivity and selectivity, and was suitable for pharmacokinetic studies of evodiamine and rutaecarpine. The kinetic process of evodiamine and rutaecarpine in rats in vivo were all yielded to be one-compartment model.

Administration, Oral ; Animals ; Evodia ; Indole Alkaloids ; pharmacokinetics ; Male ; Plant Extracts ; pharmacokinetics ; Quinazolines ; pharmacokinetics ; Rats ; Rats, Wistar

Cathepisn D plays a key role in early process of apoptosis before mitochondrion damage and caspases activations, and also involves in Alzheimer's disease (AD). Glycosaminoglycans (GAGs) have been suggested to inhibit the progress of apoptosis. Fucoidan, a nature GAGs mimetic, is shown as a potential candidate for neuroregressive disease. Here we reported PC12 cells response to oxidative stress with clear cathepsin D release, followed by caspase-3 activation. We found that fucoidan treatment can alleviate cathepsin D and caspase-3 activation, and improve cell survival. Furthermore, for the first time, fucoidan was shown to directly inhibit human liver cathepsin D by a dose-dependent way. These results support that cathepsin D involves in early apoptosis, suggest that fucoidan can decrease apoptosis at lysosome-cathepsin D level, which opens a new therapeutic approach to AD.
Alzheimer Disease ; drug therapy ; metabolism ; Animals ; Apoptosis ; drug effects ; Caspase 3 ; metabolism ; Caspase Inhibitors ; Cathepsin D ; antagonists & inhibitors ; metabolism ; Cell Line, Tumor ; Cell Survival ; drug effects ; Humans ; Hydrogen Peroxide ; metabolism ; Oxidative Stress ; drug effects ; PC12 Cells ; Polysaccharides ; pharmacology ; Rats

OBJECTIVETo investigate whether extracts of Danshen and Chuanxinlian (SL) could promote the function recovery in pre-monocytic cell line THP-1 induced by TNF-alpha.

METHODSL extracts (0.125-2 g x L(-1)) were used to incubate THP-1 for 24 h before stimulation with TNF-alpha (20 microg x L(-1)), the adhesion, migration, lipid uptake and secretion of THP-1 were observed.

RESULTSL (0.5-2 g x L(-1)) had obvious effect on decreasing the THP-1 adhesion. The number of passed membrane was much fewer than that of control cells in SL (0.125-2 g x L(-1)). SL (0.125-2 g x L(-1)) reduced the total cholesterol content significantly. The levels of IL-6 in SL (2 g x L(-1)) were significantly decreased,and IL-10 was increased than that before the treatment.

CONCLUSIONSL extracts could promote the function recovery such as adhesion, migration, lipid uptake and secretion of THP-1 induced by TNF-alpha, which probably is one of the mechanisms of inhibit the inflammatory reaction in initiation and development of AS.

Animals ; Cell Adhesion ; drug effects ; Cell Line ; Cell Movement ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Lipid Metabolism ; drug effects ; Male ; Monocytes ; cytology ; drug effects ; metabolism ; secretion ; Rabbits ; Salvia miltiorrhiza ; chemistry ; Tumor Necrosis Factor-alpha ; pharmacology