The protective effects of cordycepin on MPTP-induced dopaminergic neuron damage in mice and its mechanism / 中国药理学通报

Aim To observe the protective effects of cordycepin ( Cor) on dopaminergic neurons in 1-meth-yl-4-phenyl-1 , 2 , 3 , 6-tetrahydropyridine ( MPTP )-in-duced mouse model of Parkinson's disease ( PD) and to explore its mechanism. Methods C57BL/6 mice were administered with MPTP to establish the PD mod-el. Mice in Cor groups were pretreated with Cor (2.5,5.0 and 10.0 mg·kg-1 ) by intragastric administra-tion, respectively. The motor functions of the mice were observed in the open-field test, rotarod test and pole test. The content of DA, the numbers of TH-im-munoreactive cells and apoptotic cells were measured respectively by HPLC-ECD, immunohistochemistry staining and TUNEL staining. The expression of apop-tosis related proteins and MAPK signaling pathway-re-lated proteins ( p38 , p-p38 , ERK1/2 , p-ERK1/2 JNK1/2 and p-JNK1/2 ) were determined by Western blot. Results Cor could significantly improve the mo-tor dysfunction in PD mice. The contents of DA, DOPAC and HVA in the striatum remarkably increased after administration of Cor in MPTP-induced mice. Mo-reover, Cor could obviously reduce both the loss of TH-immunoreactive neurons and the numbers of TUNEL-positive cells in substantia nigra pars compacta ( SNpc) of PD mice. The protein expressions of Bax and cleaved caspase-3 were markedly down-regulated,whereas those of Bcl-2 and the ration of Bcl-2/Bax were significantly up-regulated by Cor pre-treatment followed by MPTP treatment. Furthermore, the protein expressions of p-p38 , p-ERK1/2 and p-JNK1/2 signif-icantly decreased in substantia nigra in Cor groups. Conclusions The results suggest that Cor can protect DA neurons against MPTP-induced injury by inhibiting apoptosis, which may be closely relevant to the inhibi-tion of MAPK signaling pathways.

Pharmacological effects on the central nervous system and toxicity of cordycepin:research advances / 国际药学研究杂志

Cordycepin(3′-deoxyadenosine),a derivative of the nucleoside adenosine,is a major functional component of Cordyceps militaris. It has been found that cordycepin possesses a variety of pharmacological activities,such as antibacterial,antivial, antiinflammatory,antitumor,immunoregulation,hypolipidemic,and hypoglycemic activities. In recent years,the effects of cordyce-pin on the central nervous system(CNS)have attracted great attention,and it has been found that cordycepin could not only affect the function of the CNS but also protect nerves from injuries. This paper reviews the effects of cordycepin on sedation and hypnosis ,the im-provement of learning and memory,and the protection of nerve injuries caused by cerebral ischemia/hemorrhage ,nerve toxin(gluta-mate,β-amyloid,rotenone and 6-hydroxydopamine,etc.),lipopolysaccharide and trauma,along with the in vitro toxicity as well as acute and subacute in vivo toxicity,so as to offer valuable references for future study and application of cordycepin.

Effects of human recombinant interleukin-1 receptor antagonist on isolated trachea smooth muscle of the guinea pig / 药学学报

<p><b>AIM</b>To study the effects of human recombinant interleukin-1 receptor antagonist (IL-1ra) on isolated trachea smooth muscle (TSM) of the guinea pig.</p><p><b>METHODS</b>Changes of the tension of isolated trachea were measured by force-displacement transducer and MedLab recording system in vitro.</p><p><b>RESULTS</b>IL-1ra showed direct relaxed effect on TSM in normal and ovalbumin sensitized guinea pig. The EC50 values were 8.06 x 10(-8) and 5.88 x 10(-7) mol.L-1 respectively. IL-1ra (1 x 10(-7)-1 x 10(-5) mol.L-1) concentration-dependently inhibited the contraction of TSM induced by 1 x 10(-3) mol.L-1 histamine (His), 1 x 10(-3) mol.L-1 acetylcholine (ACh) and 1 x 10(-6) mol.L-1 5-hydroxytryptamine (5-HT) (P < 0.05 or 0.01). When IL-1ra was given in advance, the contractile actions of His, ACh and 5-HT were antagonized by IL-1ra (1 x 10(-7)-1 x 10(-5) mol.L-1), the pD'2 value for His was 6.6 +/- 0.3. However, the contractile action of ACh was enhanced by IL-1ra at low concentration of 1 x 10(-9)-1 x 10(-8) mol.L-1. IL-1ra significantly prevented and inhibited the contraction of sensitized TSM induced by antigen ovalbumin, the IC50 value was 4.48 x 10(-7) mol.L-1.</p><p><b>CONCLUSION</b>The results indicate that IL-1ra, within certain concentration, can relax the normal, contracted and sensitized ISM of the guinea pig in vitro.</p>

Effect of bambuterol on experimental asthma and its mechanism in guinea pigs / 中国临床药理学与治疗学

Aim To probe the effect of bambuterol on experimental asthma and its pharmacodynamic and pharmacokinetic chracteristics,as well as its mechanism. Methods Experimental asthma model on guinea pigs was induced by histamine and ovalbumin in vivo and their trachea flake and pulmonary bar were emptied to the research in vitro respectively. Results Bambuterol inhibited asthma induced by histamine and ovalbumin in guinea pigs in a dose-dependent manner. Bambuterol gave no relaxation to all trachea flake,but the intragastric gavage(ig) of plasma of the bambuterol-treated guinea pigs relaxed trachea flake and pulmonary bar,and the effect on pulmonary bar was stronger than that on trachea flake. The peak value appeared about 4 h after administration,and the action continued for more than 24 h. Conclusion Bambuterol as pro-drug of terbutaline metabolized in body has a mild and permanent effect on the model of experimental asthma in guinea pigs.