Abstract:
:1. This study was undertaken to determine the effects of OSW-1 (3 beta, 16 beta, 17 alpha-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-beta-D-xylopyranosyl)- (1-->3)-(2-O-acetyl-alpha-L-arabinopyranoside)) on the pituitary-ovarian system and the functions of aortic smooth muscle. 2. A single s.c. injection of OSW-1 (9 micrograms kg-1) on the morning of pro-oestrus inhibited the occurrence of the expected next pro-oestrus, whereas administration of OSW-1 at a dose of 4.5 micrograms kg-1 did not affect the oestrous cycle. OSW-1 treatment on the day of dioestrus-1 did not affect the oestrous cycle. 3. At doses of 4.5 and 9 micrograms kg-1 OSW-1, the serum oestradiol (E2) levels at the expected next pro-oestrus were significantly lower than in control (pro-oestrus). The serum luteinizing hormone (LH) levels 4 days after 9 micrograms kg-1 OSW-1 treatment were also markedly lower than those of control. OSW-1 (4.5 micrograms kg-1) did not affect the levels of inhibin, progesterone and gonadotrophins on the same day. 4. OSW-1 did not inhibit the preovulatory LH surge which occurs on the afternoon of pro-oestrus day. 5. The expression of mRNA coding for the cholesterol side chain cleavage cytochrome P-450 (p450scc), an ovarian steroidal limiting enzyme, was suppressed at 24 and 96 h after OSW-1 treatment. 6. Administration of OSW-1 (9 micrograms kg-1) tended to reduce the relaxation of isolated thoracic aorta ring preparations induced by acetylcholine, while there was no difference in the relaxation induced by sodium nitroprusside. 7. Our results show that OSW-1 inhibits ovarian E2 secretion and that the decrease in E2 secretion may contribute to its effects on the oestrous cycle and the sensitivity of the thoracic aorta to relaxation. The decrease in the levels of ovarian steroids induced by OSW-1 may be due to its direct inhibitory action on the gene expression of the steroidal enzyme and on the proliferation of granulosa cells in the ovary.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Tamura K,Honda H,Mimaki Y,Sashida Y,Kogo Hdoi
10.1038/sj.bjp.0701309subject
Has Abstractpub_date
1997-08-01 00:00:00pages
1796-802issue
8eissn
0007-1188issn
1476-5381journal_volume
121pub_type
杂志文章abstract::1. Neurotensin was infused intravenously, in the presence or absence of intravenous atropine or intraarterial tetrodotoxin, into dogs anaesthetized with sodium pentobarbitone. Net and unidirectional fluxes of sodium and blood flows in the ileum were measured. Arterial and mesenteric venous blood pressures, haematocrit...
journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1988.tb11506.x
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abstract:BACKGROUND AND PURPOSE:Venoms are a rich source of ligands for ion channels, but very little is known about their capacity to modulate G-protein coupled receptor (GPCR) activity. We developed a strategy to identify novel toxins targeting GPCRs. EXPERIMENTAL APPROACH:We studied the interactions of mamba venom fractions...
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更新日期:2010-01-01 00:00:00
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doi:10.1111/j.1476-5381.1970.tb10347.x
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doi:10.1038/sj.bjp.0707533
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