Sugiura M, Shoyama Y, Saito H, Abe K
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
J Pharmacol Exp Ther. 1994 Nov;271(2):703-7.
The effects of crocin (crocetin di-gentiobiose ester) and its analogs on long-term potentiation (LTP) of evoked potential in the dentate gyrus were investigated by using anesthetized rats. Intracerebroventricular injection of crocin (51.2 nmol) alone did not affect the synaptic potential evoked by single stimulation of the medial perforant path, and neither inhibited nor facilitated the LTP induced by strong (30 pulses at 60 Hz) or weak (20 pulses at 60 Hz) tetanus. Administration of ethanol (30 v/v%, 2 ml/kg i.v.) blocked the LTP induced by application of tetanus (30 pulses at 60 Hz), but the LTP-blocking effect of ethanol was prevented by preadministration of crocin (51.2 nmol i.c.v.). Crocetin gentiobiose glucose ester also antagonized the LTP-blocking effect of ethanol, but it required a higher dose (102.5 nmol i.c.v.) to exhibit a more significant effect than crocin. Crocetin di-glucose ester at a dose up to 102.5 nmol (i.c.v.) did not significantly affect the LTP-blocking effect of ethanol. Neither gentiobiose alone (102.5 nmol i.c.v.) nor glucose alone (204.9 nmol i.c.v.) mimicked the activity of crocin. These results suggest that crocin can prevent the ethanol-induced impairment of hippocampal synaptic plasticity in vivo and that gentiobioses attached to the fatty acid chain are important for crocin to exert the biological activity.
采用麻醉大鼠，研究了藏红花素（藏红花酸二龙胆二糖酯）及其类似物对齿状回诱发电位长时程增强（LTP）的影响。单独脑室内注射藏红花素（51.2 nmol）不影响内侧穿通路径单次刺激诱发的突触电位，对强（60 Hz，30个脉冲）或弱（60 Hz，20个脉冲）强直刺激诱导的LTP既无抑制作用也无促进作用。静脉注射乙醇（30 v/v%，2 ml/kg）可阻断强直刺激（60 Hz，30个脉冲）诱导的LTP，但预先脑室内注射藏红花素（51.2 nmol）可防止乙醇的LTP阻断作用。藏红花酸龙胆二糖葡萄糖酯也可拮抗乙醇的LTP阻断作用，但与藏红花素相比，其需要更高剂量（102.5 nmol脑室内注射）才能表现出更显著的作用。剂量高达102.5 nmol（脑室内注射）的藏红花酸二葡萄糖酯对乙醇的LTP阻断作用无显著影响。单独的龙胆二糖（102.5 nmol脑室内注射）或葡萄糖（204.9 nmol脑室内注射）均不能模拟藏红花素的活性。这些结果表明，藏红花素可预防体内乙醇诱导的海马突触可塑性损伤，且脂肪酸链连接的龙胆二糖对藏红花素发挥生物活性很重要。
