Komiyama K, Tronquet C, Hirokawa Y, Funayama S, Satoh O, Umezawa I, Oishi S
Jpn J Antibiot. 1986 Mar;39(3):746-50.
In the course of a search for novel antibiotics, an antiplatelet substance was isolated from the fermentation broth of Streptomyces sp. No. 82-85. Thereafter, the active substance was identified as pyrrole-2-carboxylic acid (P2C) by structural studies. The effects of P2C on adenosine diphosphate (ADP)-, arachidonic acid-, collagen- or tumor cell-induced platelet aggregation were examined in vitro and ex vivo. In in vitro studies, P2C (25-100 micrograms/ml) suppressed the aggregation of platelets of normal Wistar rats. The intraperitoneal administration of P2C (200 mg/kg) to rats and rabbits suppressed platelet aggregation induced by ADP, arachidonic acid and collagen when examined for 0.5-3 hours after administration. The agent also suppressed platelet aggregation induced by both mouse syngenic tumors, Meth-A fibrosarcoma and IMC carcinoma in vitro.
在寻找新型抗生素的过程中,从链霉菌属82 - 85号菌株的发酵液中分离出一种抗血小板物质。此后,通过结构研究确定该活性物质为吡咯 - 2 - 羧酸(P2C)。体外和体内研究了P2C对二磷酸腺苷(ADP)、花生四烯酸、胶原或肿瘤细胞诱导的血小板聚集的影响。在体外研究中,P2C(25 - 100微克/毫升)抑制正常Wistar大鼠血小板的聚集。给大鼠和兔子腹腔注射P2C(200毫克/千克)后,在给药后0.5 - 3小时检测发现,其可抑制ADP、花生四烯酸和胶原诱导的血小板聚集。该药物还在体外抑制小鼠同基因肿瘤Meth - A纤维肉瘤和IMC癌诱导的血小板聚集。