Honda H, Mimaki Y, Sashida Y, Kogo H
Department of Pharmacology, Tokyo University of Pharmacy and Life Science, Japan.
Biol Pharm Bull. 1997 Apr;20(4):428-30. doi: 10.1248/bpb.20.428.
The tension of isolated ring preparation of the aorta from rats was measured isometrically to study the influence of OSW-1 [3 beta,16 beta,17 alpha-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-beta-D-xylopyranosyl)-(1 right arrow 3)-(2-O-acetyl-alpha-L-arabinopyranoside)], a steroidal saponin, on the endothelium dependent and independent relaxation caused by acetylcholin (ACh) and sodium nitroprusside (SNP), respectively. OSW-1 (10(-7) M), which has more than 100 times higher concentration for anti-tumor activity, had no influence on either the endothelium dependent or independent relaxation. OSW-1 (10(-6) M, 0.9 microgram/ml) slightly reduced the endothelium dependent relaxation caused by ACh but did not affect the SNP-induced relaxation. In contrast to OSW-1, 1 mg/ml of saponin significantly suppressed the ACh-induced relaxation and shifted the dose-relaxation curve for SNP to the right. OSW-1 (10(-7) and 10(-6) M) did not affect the norepinephrine-induced contraction but 1 mg/ml of saponin significantly attenuated it. The results suggest that though the higher concentration of OSW-1 shows weaker influence on the endothelium function compared with saponin, OSW-1 at an anti-tumor dose has no influence on either endothelium or smooth muscle function.
通过等长测量法测定大鼠主动脉离体环制剂的张力，以研究甾体皂苷OSW-1[3β,16β,17α-三羟基胆甾-5-烯-22-酮16-O-(2-O-4-甲氧基苯甲酰基-β-D-吡喃木糖基)-(1→3)-(2-O-乙酰基-α-L-阿拉伯吡喃糖苷)]分别对乙酰胆碱（ACh）和硝普钠（SNP）引起的内皮依赖性和非内皮依赖性舒张的影响。OSW-1（10⁻⁷M）的浓度比其抗肿瘤活性所需浓度高100多倍，对内皮依赖性或非内皮依赖性舒张均无影响。OSW-1（10⁻⁶M，0.9微克/毫升）略微降低了ACh引起的内皮依赖性舒张，但不影响SNP诱导的舒张。与OSW-1相反，1毫克/毫升的皂苷显著抑制了ACh诱导的舒张，并使SNP的剂量-舒张曲线右移。OSW-1（10⁻⁷和10⁻⁶M）不影响去甲肾上腺素诱导的收缩，但1毫克/毫升的皂苷显著减弱了该收缩。结果表明，尽管与皂苷相比，较高浓度的OSW-1对内皮功能的影响较弱，但抗肿瘤剂量的OSW-1对内皮或平滑肌功能均无影响。
