前西班牙酮，一种来自益母草的新型血小板活化因子受体拮抗剂。
Prehispanolone, a novel platelet activating factor receptor antagonist from Leonurus heterophyllus.
作者信息
Lee C M, Jiang L M, Shang H S, Hon P M, He Y, Wong H N
机构信息
Department of Biochemistry, Chinese Medicinal Material Research Centre, Shatin, N.T., Hong Kong.
出版信息
Br J Pharmacol. 1991 Jul;103(3):1719-24. doi: 10.1111/j.1476-5381.1991.tb09853.x.
Abstract
- Using an in vitro radioligand binding assay for the platelet activating factor (PAF) receptor, we have identified a novel, specific PAF antagonist, prehispanolone, from a Chinese medicinal herb Leonurus heterophyllus. 2. The presence of sodium ions inhibited specific [3H]-PAF binding to rabbit platelet membrane with an IC50 of 5.2 mM, decreased the inhibitory potency of PAF but increased the inhibitory potency of prehispanolone. 3. Prehispanolone and several of its derivatives inhibited the binding of [3H]-PAF to rabbit platelets with potencies closely resembling that of inhibition of PAF-induced aggregation. 4. The integrity of the tetrahydrofuran ring of prehispanolone is critical for its interaction with the PAF receptor. 5. By hydrogenating the dihydrofuran ring and replacing the keto group of prehispanolone with a hydroxyl group, we obtained a compound, LC5507, that is more stable and more active than prehispanolone as a PAF receptor antagonist.
摘要
- 我们使用血小板活化因子（PAF）受体的体外放射性配体结合试验，从一种中草药益母草中鉴定出一种新型的特异性PAF拮抗剂——前西班牙酮。2. 钠离子的存在会抑制特异性[3H]-PAF与兔血小板膜的结合，IC50为5.2 mM，降低了PAF的抑制效力，但提高了前西班牙酮的抑制效力。3. 前西班牙酮及其几种衍生物抑制[3H]-PAF与兔血小板的结合，其效力与抑制PAF诱导的聚集密切相似。4. 前西班牙酮的四氢呋喃环的完整性对其与PAF受体的相互作用至关重要。5. 通过氢化二氢呋喃环并将前西班牙酮的酮基替换为羟基，我们得到了一种化合物LC5507，它作为PAF受体拮抗剂比前西班牙酮更稳定且活性更高。
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