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.

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.

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.

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.

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.

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 study the scientific theory on detoxification (attenuation) of Stellera chamaejasme (ScL) by processing and the impact on drug effect of ScL before and after being processed with vinegar.

METHODThe difference in ingredients of ScL before and after being processed vinegar was compared by using PHLC-MS technique. A subcutaneously transplanted tumor model of H22 hepatoma was established to compare the lethal effect and weight change between tumor-loaded mice and normal mice. After consecutive oral administration in tumor-loaded mice, the impacts on tumors and immune organs were compared before and after being processed with vinegar. Luciferase Report Gene was employed to investigate the target genes TGF-beta, AP1 and NF-kappaB.

RESULTThe LD50 (median fatal dose) of extract Zp1102 exhibited higher than that of the processed one Zp1103, that is 9. 89 g x kg(-1) vs. 16.85 g x kg(-1). According to the test, Zp1102 showed more effective anti-tumor activities in vivo than that of Zp1103 in a same dosage, with the tumor inhibitory rate 36.24% (P < 0.01) at the dosage of2 g x kg(-1) and 34.40% (P < 0.05) at the dosage of 1 g x kg(-1). At the dosage of 1 g x kg(-1), Zp1102 showed a tumor inhibitory rate of 34.52% (P < 0.05), much higher from 21.55% in Zp1103. Both Zp1102 and Zp1103 had basically no impact on the report gene NF-kappaB, besides that Zp1102 up-regulated the report gene after increase in NF-kappaB concentration and down-regulated TGF-beta, but Zp1103 can only up-regulate NF-kappaB expression without any impact on TGF-beta.

CONCLUSIONProcessed ScL extracts show less toxic than unprocessed extracts and slight reduction in anti-tumor activity, which may be related to the regulation of transforming growth factor TGF-beta.

Acetic Acid ; chemistry ; Animals ; Chromatography, High Pressure Liquid ; Lethal Dose 50 ; Male ; Mice ; NF-kappa B ; physiology ; Neoplasms, Experimental ; drug therapy ; Phytotherapy ; Thymelaeaceae ; chemistry ; toxicity ; Transforming Growth Factor beta ; physiology

OBJECTIVETo in vitro compare the induction of extracts of Stellera chamaejasme ESC, ESC-1 and ESC-2 on NCI-H157 cell apoptotic.

METHODThe apoptosis rate was inspected by flow cytometry; caspase-3, 8, 9 activities was measured by spectrophotometry. Fas, Fas-L, TNF-alpha, Trail-R, Cyto-C, Smac/diablo protein expressions of apoptosis pathway was observed by Elisa method.

RESULTCompared with the control group, ESC, ESC-1, ESC-2 can significantly improve the apoptosis rate of NCI-H157 cell. ESC significantly improved cells caspase-3, 8 activity, ESC-2 can significantly improve the activity of caspase-3, 8, 9. ESC, ESC-1, ESC-2 significantly increased Fas expression and ESC significantly increased Fas/Fas-L ratio. ESC, ESC-1, ESC-2 significantly increased TNF-alpha protein expression. ESC-1 significantly lowered TRAIL-R expression. ESC, ESC-1, ESC-2 had no significant effect on Cyto-C. ESC-1, ESC-2 significantly reduced Smac protein expression.

CONCLUSIONThe apoptotic effect induced by ESCs may be related to the regulation of death receptor pathway proteins. Induction mechanisms of ESCs were so complicated that it may have a two-way regulatory effect. Its induction in apoptosis is a result from comprehensive regulation and control.

Apoptosis ; drug effects ; Caspases ; metabolism ; Cell Line, Tumor ; Humans ; Neoplasms ; chemistry ; drug therapy ; pathology ; Plant Extracts ; pharmacology ; Receptors, TNF-Related Apoptosis-Inducing Ligand ; analysis ; Thymelaeaceae ; chemistry ; Tumor Necrosis Factor-alpha ; analysis ; fas Receptor ; analysis

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