Tan Yan, Tang Qiang, Hu Ben-Rong, Xiang Ji-Zhou
Department of Pharmacology, School of Basic Medical Sciences, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei 430030, China.
Zhonghua Nan Ke Xue. 2005 Jun;11(6):406-8.
To further investigate the action mechanisms of berberine (Ber), and assess the effects of Ber on the in vitro formation of cGMP and cAMP in the isolated rabbit corpus cavernosum.
Isolated segments of the rabbit corpus cavernosum were exposed to different concentrations of Ber, and, the dosage-dependent accumulations of cGMP and cAMP were determined in the tissue samples by means of 125I radioimmunoassay. Responses of the isolated tissue preparations to Ber were compared with those obtained with the reference compound sildenafil (Sil).
Ber increased cGMP concentrations directly (P < 0.05). In the presence of sodium nitroprusside (SNP), a stimulatory agent of cGMP, both Ber and Sil increased cGMP with increasing dosage (P < 0.01), the EC, values being 1.32 and 0.67 micromol/L respectively. With the same concentration, neither Ber nor Sil influenced the cAMP level significantly (P > 0.05). In the presence of PGE1, a stimulator of cAMP, Ber and Sil also raised the cAMP level concentration (P < 0.01 ), the EC, values being 4.90 (Ber) and 6.53 (Sil) micromol/L respectively.
Ber can increase cGMP and cAMP concentrations in the corpus cavernosum smooth muscles, which may contribute to its action of relaxing corpus cavernosum smooth muscles.
进一步研究黄连素(Ber)的作用机制,评估Ber对离体兔海绵体中cGMP和cAMP体外生成的影响。
将离体兔海绵体节段暴露于不同浓度的Ber中,通过125I放射免疫分析法测定组织样本中cGMP和cAMP的剂量依赖性积累。将离体组织制剂对Ber的反应与参考化合物西地那非(Sil)的反应进行比较。
Ber直接增加cGMP浓度(P<0.05)。在cGMP刺激剂硝普钠(SNP)存在的情况下,Ber和Sil均随剂量增加而增加cGMP(P<0.01),其EC50值分别为1.32和0.67μmol/L。在相同浓度下,Ber和Sil均未显著影响cAMP水平(P>0.05)。在cAMP刺激剂前列腺素E1(PGE1)存在的情况下,Ber和Sil也提高了cAMP水平(P<0.01),其EC50值分别为4.90(Ber)和6.53(Sil)μmol/L。
Ber可增加海绵体平滑肌中的cGMP和cAMP浓度,这可能有助于其舒张海绵体平滑肌的作用。