Kwanashie H O, Ejiofor J I, Abdu-Aguye I, Nkweteyim J N, Olanipekun M R
Department of Pharmacology and Clinical Pharmacy, Ahmadu Bello University, PMB 1045, Zaria 810271, Kaduna State, Nigeria.
Phytother Res. 2009 Feb;23(2):236-40. doi: 10.1002/ptr.2598.
Earlier pharmacological screening showed that siculine syrup (a traditional herbal remedy purported to be useful in the prevention and treatment of sickle cell pain - crises, due to sickle cell anaemia - SCA) had antisickling and analgesic activities as well as antimicrobial and diuretic effects. SCA is an important haemoglobinopathy in Africa and many other communities/countries worldwide, with relatively high morbidity and mortality. The present study was to determine the effects of the extract on various isolated muscle preparations - smooth, skeletal and cardiovascular. Siculine (4-20 microg/mL), like acetylcholine (40-400 microg/mL), contracted the isolated rat uterus concentration dependently. Similar effects were observed with the guinea-pig ileum and rabbit jejunum (2-20 microg/mL). In contrast to these effects, the direct (muscle) and indirect (nerve) stimulations of rat phrenic nerve-diaphragm were relaxed by siculine (4 and 8 microg/mL) and d-tubocurarine (0.8 microg/mL). Siculine also concentration-dependently decreased both the rate and force of contraction of guinea-pig atria and rabbit heart and also resulted in a fall in cat blood pressure in a manner similar to those of acetylcholine. The possible therapeutic and/or toxicological consequences of these effects including the hypotensive activity is noteworthy since siculine syrup is used by the local population for the prevention and treatment of sickle cell pain crises.
早期的药理学筛选表明,西库林糖浆(一种传统草药制剂,据称对预防和治疗镰状细胞贫血所致的镰状细胞疼痛危象有用)具有抗镰状化和镇痛活性,以及抗菌和利尿作用。镰状细胞贫血在非洲以及世界其他许多社区/国家都是一种重要的血红蛋白病,发病率和死亡率相对较高。本研究旨在确定该提取物对各种离体肌肉制剂——平滑肌、骨骼肌和心血管肌的作用。西库林(4 - 20微克/毫升)与乙酰胆碱(40 - 400微克/毫升)一样,能使离体大鼠子宫产生浓度依赖性收缩。在豚鼠回肠和兔空肠(2 - 20微克/毫升)中也观察到类似的作用。与这些作用相反,西库林(4和8微克/毫升)和d - 筒箭毒碱(0.8微克/毫升)可使大鼠膈神经 - 膈肌的直接(肌肉)和间接(神经)刺激松弛。西库林还能使豚鼠心房和兔心脏的收缩速率和力量呈浓度依赖性降低,并且导致猫血压下降,其方式与乙酰胆碱相似。鉴于当地人群使用西库林糖浆预防和治疗镰状细胞疼痛危象,这些作用(包括降压活性)可能产生的治疗和/或毒理学后果值得关注。