Inhibition of the lethal and myotoxic activities of Crotalus durissus terrificus venom by Tabernaemontana catharinensis:: Identification of one of the active components
Inhibition of the lethal and myotoxic activities of Crotalus durissus terrificus venom by Tabernaemontana catharinensis:: Identification of one of the active components
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DOI：
10.1055/s-2000-8577
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发表时间：
2000-06-01
期刊：
影响因子：
2.7
通讯作者：
Sampaio, SV
中科院分区：
文献类型：
--
作者：
Batina, MD;Cintra, ACO;Sampaio, SV
在巴西民间医学中，被有毒动物咬伤的受害者通常会用从不同国家植物中提取的植物提取物进行治疗。大部分提取物的化学和药理性质尚未调查。在Assis-SP的农村社区，Toberneemontana cusarinensis(“leiteiro”，“牛奶”)的根皮被涂在蛇咬伤的部位，据信可以中和毒液的效果。本文报道了从华支睾吸虫乙醇提取物中提取的冻干水提物(AE)和一种纯化合物对南美响尾蛇(C.D.derficus)蛇毒的致死和肌毒活性的抑制能力。AE10 mg/100g剂量(肌肉注射，大鼠)20 S后注射(I.M.)毒液和2.5mgAE/100g的毒液，在25℃下与毒液孵育1h后注射(I.M.)能中和2LD(50)的致死活性。这些数据表明，华支睾吸虫可以作为一种模型分子的来源，能够中和可怕钩端螺旋体毒液诱导的致死性和肌肉毒性。它的乙醇提取物在硅胶60色谱柱上进行分级，得到组分A到F。组分A主要由非极性化合物、萜烯和甾醇组成。组分D显示出明显的抗蛇毒活性，这与该组分中存在的季胺类生物碱12-甲氧基-4-甲基瓦查罗汀有关。该生物碱在2LD50为1.7 mg/100g时，经20 S注射后，对小鼠的致死率为100%。
In Brazilian folk medicine, victims of bites by poisonous animals are usually treated with plant extracts derived from the diverse national flora. The chemical and pharmacological properties of most extracts were yet not investigated. In the rural community of Assis-SP, the root bark of Tobernaemontana catharinensis ("leiteiro", "cow milk") is applied to the site of the snake bite and believed to neutralize the effect of the venom. We report here the ability of the lyophilized aqueous extract (AE) and of a pure compound obtained from the ethanolic extract of T. catharinensis to inhibit the lethal and myotoxic activities of C. d. terrificus (South American rattlesnake) venom. Doses of 10 mg AE/100 g, injected (i.m., rat) 20 s after injecting (i.m.) the venom and that of 2.5 mg AE/100 g, incubated for 1 h at 25 degrees C with the venom before injection (i.m.) were able to neutralize the lethal activity of 2LD(50). These data indicate that T. catharinensis could be used as a source of a model molecule able to neutralize the lethality and myotoxicity induced by C. d. terrificus venom. Its ethanolic extract was then fractionated on a silica gel 60 chromatography column affording fractions A to F. Fraction A consisted basically of non-polar compounds, terpenes and sterols. Fraction D showed a pronounced antiophidian activity which was later correlated with the presence of the quaternary alkaloid 12-methoxy-4-methylvoachalotine in this fraction. This alkaloid was isolated and inhibited 100% lethality when injected 20 s after 2 LD50 at 1.7 mg/100 g.