Ali N, Shah Swa, Shah I
Institute of Basic Medical Sciences, Khyber Medical University, Peshawar, Khyber Pakhtunkhwa; Department of Pharmacy, University of Malakand, Chakdara, Dir. Khyber Pakhtunkhwa, Pakistan.
J Young Pharm. 2011 Apr;3(2):125-8. doi: 10.4103/0975-1483.80300.
The current work describes the antispasmodic action of Artemisia macrocephala, which is achieved via blocking of the calcium channels. This explains its traditional use as an antispasmodic.The crude methanolic extract of A. macrocephala was studied for possible relaxant effect(s) on spontaneous rabbits' jejunum preparations. Analytical-grade chemicals were used in the experimental protocols. A. macrocephala gave positive tests for flavonoids, saponins, glycosides, alkaloids, and terpenes. A. macrocephala caused relaxation of spontaneous rabbits' jejunum preparations (n=6) at a dose of 10.0 mg/mL (EC(50) = 6.95 ± 0.20 mg/mL; 95% CI: 6.2 to 7.5). Contractions induced by 80 mM potassium chloride (KCl) were also relaxed by the A. macrocephala at dose of 10.0 mg/mL. Attempting to find an explanation for the possible mode of action, we found that, A. macrocephala at concentration of 1.0 mg/mL produced rightward shift in the calcium chloride curves, with EC(50) value of -1.65 ± 0.02 log [Ca(++)] M vs control with EC(50) value of -2.44 ± 0.043 for calcium chloride curves. At a concentration of 1.0 mg/mL it could produce 52.4% of the control response at log [Ca(++)] M = -1.6. Similarly, verapamil at a concentration of 0.1 μM produced a rightward shift, with EC(50) value of -1.74 ± 0.026 log [Ca(++)] M (95% CI: -1.66 to -1.82; n=6) vs control with EC(50) value of -2.45 ± 0.05 log [Ca(++)] M (95% CI: - 2.23 to -2.91; n=6). The right shift of the EC(50) values is justification for the folkloric use of A. macrocephala as an antispasmodic, suggesting that the possible mode of action is through calcium channel blockade.
当前的研究描述了大头蒿的解痉作用,其通过阻断钙通道来实现。这解释了其作为解痉剂的传统用途。对大头蒿的粗甲醇提取物进行了研究,以探究其对兔空肠自发收缩标本可能的松弛作用。实验方案中使用了分析纯化学品。大头蒿对黄酮类、皂苷类、糖苷类、生物碱类和萜类呈阳性检测反应。大头蒿在剂量为10.0 mg/mL时可使兔空肠自发收缩标本(n = 6)松弛(半数有效浓度(EC(50))= 6.95 ± 0.20 mg/mL;95%置信区间:6.2至7.5)。大头蒿在剂量为10.0 mg/mL时也可使由80 mM氯化钾(KCl)诱导的收缩松弛。为了探寻可能的作用方式,我们发现,浓度为1.0 mg/mL的大头蒿使氯化钙曲线向右移位,氯化钙曲线的半数有效浓度(EC(50))值为 -1.65 ± 0.02 log [Ca(++)] M,而对照组氯化钙曲线的半数有效浓度(EC(50))值为 -2.44 ± 0.043。在log [Ca(++)] M = -1.6时,浓度为1.0 mg/mL的大头蒿可产生对照组反应的52.4%。同样,浓度为0.1 μM的维拉帕米使曲线向右移位,半数有效浓度(EC(50))值为 -1.74 ± 0.026 log [Ca(++)] M(95%置信区间:-1.66至 -1.82;n = 6),而对照组半数有效浓度(EC(50))值为 -2.45 ± 0.05 log [Ca(++)] M(95%置信区间:-2.23至 -2.91;n = 6)。半数有效浓度(EC(50))值的右移证明了大头蒿作为解痉剂的民间用途,表明其可能的作用方式是通过钙通道阻滞。