Chen Jun, Liu Ji-Hong, Wang Tao, Xiao Heng-Jun, Yin Chun-Ping, Yang Jun
Department of Urology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Asian J Androl. 2008 Mar;10(2):307-12. doi: 10.1111/j.1745-7262.2008.00342.x. Epub 2007 Dec 20.
To further investigate the relaxation mechanism of neferine (Nef), a bis-benzylisoquinoline alkaloid extracted (isolated) from the green seed embryo of Nelumbo nucifera Gaertn in China, on rabbit corpus cavernosum tissue in vitro.
The effects of Nef on the concentrations of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in isolated and incubated rabbit corpus cavernosum tissue were recorded using 125I radioimmunoassay.
The basal concentration of cAMP in corpus cavernosum tissue was 5.67 +/- 0.97 pmol/mg. Nef increased the cAMP concentration in a dose-dependent manner (P < 0.05), but this effect was not inhibited by an adenylate cyclase inhibitor (cis-N-[2-phenylcyclopentyl]azacyclotridec-1-en-2-amine, MDL-12, 330A) (P > 0.05). The accumulation of cAMP induced by prostaglandin E1 (PGE1, a stimulator of cAMP production) was also augmented by Nef in a dose-dependent manner (P < 0.05). The basal concentration of cGMP in corpus cavernosum tissue is 0.44 +/- 0.09 pmol/mg. Nef did not affect this concentration of cGMP, either in the presence or in the absence of a guanyl cyclase inhibitor (1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, ODQ) (P > 0.05). Also, sodium nitroprusside (SNP, a stimulator of cGMP production)-induced cGMP production was not enhanced by Nef (P > 0.05).
Nef, with its relaxation mechanism, can enhance the concentration of cAMP in rabbit corpus cavernosum tissue, probably by inhibiting phosphodiesterase activity.
进一步研究从中国莲(Nelumbo nucifera Gaertn)绿色种子胚中提取(分离)的双苄基异喹啉生物碱甲基莲心碱(Nef)对兔海绵体组织的体外舒张机制。
采用125I放射免疫分析法记录Nef对离体培养的兔海绵体组织中环磷酸腺苷(cAMP)和环磷酸鸟苷(cGMP)浓度的影响。
海绵体组织中cAMP的基础浓度为5.67±0.97 pmol/mg。Nef以剂量依赖性方式增加cAMP浓度(P<0.05),但这种作用不受腺苷酸环化酶抑制剂(顺式-N-[2-苯基环戊基]氮杂环十三碳-1-烯-2-胺,MDL-12,330A)的抑制(P>0.05)。前列腺素E1(PGE1,一种cAMP产生的刺激剂)诱导的cAMP积累也被Nef以剂量依赖性方式增强(P<0.05)。海绵体组织中cGMP的基础浓度为0.44±0.09 pmol/mg。无论有无鸟苷酸环化酶抑制剂(1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮,ODQ),Nef均不影响该cGMP浓度(P>0.05)。此外,硝普钠(SNP,一种cGMP产生的刺激剂)诱导的cGMP产生也未被Nef增强(P>0.05)。
Nef通过其舒张机制,可能通过抑制磷酸二酯酶活性来提高兔海绵体组织中cAMP的浓度。