CN101073570A - 血根碱作为杀灭钉螺药物的应用 - Google Patents
血根碱作为杀灭钉螺药物的应用 Download PDFInfo
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Abstract
血根碱作为杀灭钉螺药物的应用。将钉螺用血根碱配制成浓度0.18－50.0mg/L的水溶液浸泡96h，对钉螺的杀灭率可达40－100％；当浓度为0.390mg/L时，杀灭率≥88％；当浓度为0.8mg/L时，杀灭率≥92％；当浓度为3.0mg/L时，杀灭率≥98％；当浓度为12.5mg/L时，杀灭率即可达100％。当血根碱浓度＝50mg/L时，钉螺浸泡72h，杀灭率即达100％。本发明有益效果：血根碱来源广泛，价格较低，在低浓度下就有明显杀灭钉螺的作用，而对人畜和水生植物及其它水生动物毒性低，对环境污染少。
Description
技术领域
本发明涉及一种杀灭钉螺的药物，尤其是涉及一种生物碱——血根碱作为杀灭血吸虫中间宿主-钉螺的药物的应用。
背景技术
血吸虫病是流行于世界74个国家的人畜共患寄生虫病，据WHO估计，全世界有6亿人处于感染血吸虫的危险环境中，其中约2亿人感染。我国的长江流域及其以南的12个省、直辖市、自治区均有流行，全国有434个流行县，受感染威胁的人口6600余万，慢性病人84万，推算年新感染或再感染人数约达20万，有血吸虫中间宿主-钉螺面积达384599.97hm2。消灭血吸虫中间宿主-钉螺，控制和阻断血吸虫病的传播是防治血吸虫病的重要对策。
钉螺的防治方法有改变环境灭螺、物理灭螺、生物灭螺及药物灭螺等。
药物灭螺效果比较持久，可因地域确定使用范围，是灭螺中使用较多的方法。目前，国内外常用的药物灭螺方法为化学药物灭螺。以往曾推广使用的五氯酚钠，杀螺效果好，价格低，但对人畜和水生动植物有严重危害，环境污染严重，已被WHO禁止使用。氯硝柳胺是目前仍在使用的化学杀螺剂，药效好，但钉螺接触药物后明显离水上爬，降低了杀螺效果，且价格昂贵，对非靶生物毒性大，影响该药的推广和应用。WHO及我国始终致力于灭螺药物的研究，期望研制出杀螺效果好、毒性低、少污染、价低廉的杀螺剂。
植物杀螺剂因其来源广、资源丰富、毒性低、易降解、污染小而备受关注。
研究表明，某些植物含有杀螺的化学成分。自1933年Archibald R.G首次报道Balanitaceae科的Balanites ageyptiace果实用以控制血吸虫病以来，植物杀螺剂的研究受到高度重视。迄今为止，全世界已对1000多种植物的杀螺作用进行了测试，筛选出近百种对螺类有杀灭和抑制作用的植物，并进行了有效化学成分的分析。我国通过对500余种植物资源的研究，已发现数十种植物对钉螺有毒杀作用，诸如油茶(Camellia)、赤桉(Euealyptus camldultensis)、异叶心桉(E.cordataf)、商陆(Phytolacce candra)、黄果茄(Solanumxanthocarpum)、重楼(Rhigome paridis)、盾叶薯蓣(Dioscoreagingiberensis)、竹节香附(Anemone raddeana)、禾叶山麦冬(Liriopegraminisolia)、槟榔(Areca catechu L.)等。已阐明了植物杀螺药主要有效成分为皂甙、鞣质、萘醌、烯基酚、黄酮、一萜、倍半萜、生物碱及呋喃香豆素等类化合物。含生物碱类植物具有杀螺作用已引起关注。文献已报道的具有杀螺作用的生物碱，有从黄果茄中提取的甾体生物碱、喹嗪生物碱，从豆科植物calparnia aurea中提取的灌豆碱，从槟榔种子中提取的槟榔碱，从乌头中提取的二萜生物碱，从麻风树种子中提取的麻风树碱。
虽然植物杀螺剂资源丰富，具有可就地取材，易生物降解的优点，使植物杀螺剂的研究备受关注，成为国内外杀螺剂研究的重点之一，但到目前为止，尚未研究出一种较好的能推广应用的植物性灭螺药物，植物杀螺剂的研究一直是国内外学者探索的课题。
从1993年开始，本发明者对血水草的杀灭钉螺及日本血吸虫尾蚴的作用进行了研究。血水草(Eomecon chionantha Hance)为罂粟科(Papaveraceae)白屈菜族(Chelidonium)血水草属(Eomecon)植物，别名水黄莲、广扁线、捆仙绳、牛黄等，系多年生草本植物，是我国独属、独种的特有物种，资源十分丰富，广泛分布于我国长江流域、华南、华东、西南地区，西北秦岭也有分布，特别是在长江中下游血吸虫疫区分布广泛，生长在山野、路旁、溪边、林边等较潮湿的泥土内，取材容易。具有多种药理作用，民间用于治疗毒蛇咬伤、疮疖、无名肿毒、急性结膜炎等。从血水草及其根茎中提取的生物碱，称血水草生物碱(Eomecon chiorantha Alkaloids，简称ECA)。研究发现，ECA具有杀灭钉螺及日本血吸虫尾蚴的作用，能抑制钉螺上爬，对鱼类毒性较低。血水草生物碱(ECA)为多种苯骈菲啶(Benzophenanthrdine)型生物碱的混合物，主要成分包括白屈菜红碱(Chelerythrine)、血根碱(Sanguinarine)、原阿片碱(Protopine)、α-别隐品碱(α-allocyptopine)。。
从血水草生物碱中分离出的血根碱也存在于其它罂粟科植物中。
有文献报道，纯品血根碱对治疗哮喘、支气管炎、痢疾、某些肿瘤等疾病有较好效果，但尚未发现它有其它用途的文献报道。
发明内容
本发明的目的在于提供一种来源广泛，价格较低，对人畜和水生动植物毒性低，对环境污染少，杀螺效果好的杀灭钉螺的药物。
本发明的目的是通过以下技术方案实现的：
(一)ECA的提取
秋季采新鲜血水草及根茎洗净晾干，完全干燥后碾成粗末，采用乙醇渗漉，减压浓缩，盐析法提取血水草生物碱。
(二)血根碱的分离
血水草生物碱包含以下化学成分：白屈菜红碱、血根碱、原阿片碱、α-别隐品碱、氧化血根碱(oxysanguinarine)，白屈菜红默碱(Chelerythridimerine)和羽扇豆醇乙酯(Lupenylacetate)。其中前四种生物碱为主要成分。通过氯仿萃取、反复柱色谱分离及用薄层层析法及高效液相色谱(HPLC)分离出血根碱，并进行含量测定。
所述血根碱的结构式为：
分子式为C20H14NO4。
试验用血根碱样品含血根碱98％。
其它罂粟科植物，例如博落回，也含有血根碱，因而血根碱也可从血水草之外的其它罂粟科植物中提取。
(三)血根碱杀灭钉螺方法
以50mg/L为最高浓度，然后按倍比稀释配置成9种不同浓度的血根碱水溶液，按照WHO“杀螺剂实验室终筛方法”规定的浸泡法，对血根碱进行实验室杀灭钉螺试验，设去氯水作空白对照。
本发明者发现，将钉螺用血根碱配制成浓度0.20-50.0mg/L的水溶液浸泡96h，对钉螺的杀灭率可达42-100％；当浓度为0.40mg/L时，杀螺率≥88％；当浓度为0.80mg/L时，杀灭率≥92％；当浓度为1.5mg/L时，杀灭率≥98％，当浓度为3.0mg/L时，杀灭率≥98％；当浓度＝12.5mg/L时，杀灭率即可达100％。当血根碱浓度为50mg/L时，钉螺浸泡72h，杀灭率即达100％。
本发明有益效果：血根碱来源广泛，价格较低，在低浓度下就有明显杀灭钉螺的作用，而对人畜和水生植物及其它水生动物毒性低，对环境污染少。
具体实施方式
以下结合实施例对本发明作进一步说明。这些实施例不得用于解释对本发明保护范围的限制。
(1)将血根碱配制成浓度为50、25、12.5、6.25、3.125、1.5625、0.78125、0.390625、0.1953125mg/L的水溶液9组，去氯水空白对照1组。每组2000ml。
(2)前1日从血吸虫病流行疫区采回钉螺，试验当日选用活钉螺，按50只为一组装入专用尼龙袋中。
(3)每500ml溶液中投入钉螺1袋(即1只钉螺/10ml药液)，每组浓度样品溶液放入钉螺4袋，置25℃恒温下进行试验，浸泡24h、48h、72h、96h；每组各取出1袋螺，用去氯水清洗2次，置室温下72h后测钉螺死活。
(4)用水测法及敲击法鉴定每只钉螺的死活，并记录，计算每组钉螺的死亡率。
灭螺试验结果如下表所示：
血根碱浸杀钉螺试验结果统计表
| 药物 | 浓度(mg/L) | 钉螺死亡数及死亡率(％) | |||||||
| 24h | 48h | 72h | 96h | ||||||
| 血根碱去氯水 | 50.025.012.56.253.1251.56250.781250.3906250.1953125 | 262221121131000 | 524442242262000 | 484538383426221750 | 9690767668524434100 | 5049484541403834110 | 10098969082807668220 | 5050504949464644210 | 1001001009898929288420 |
注：1、每组钉螺数均为50只；2、“钉螺死亡数及死亡率”栏中，每一小栏的左侧数字为钉螺死亡绝对数，右侧数字为死亡百分数。
应用BL-New Century(USB版本)数据处理系统，使用Bliss法计算得出：
钉螺浸泡48h，LC50为1.419393mg/L，
95％可信限为1.045692-1.926643mg/L；
钉螺浸泡72h，LC50为0.330738mg/L，
95％可信限为0.219364-0.498657mg/L；
钉螺浸泡96h，LC50为0.158233mg/L，
95％可信限为0.100593-0.248898mg/L。
试验结果表明，血根碱在低浓度下有明显杀灭钉螺的作用。当浓度达到12.5mg/L时，钉螺浸泡96h，杀灭率即可达100％。
血根碱存在于多种罂粟科植物中，资源丰富，其杀灭钉螺用途的发现，有利于血水草及其他罂粟科植物的开发应用。
Claims (8)
1.血根碱作为杀灭钉螺药物的应用。
2.根据权利要求1所述的血根碱作为杀灭钉螺药物的应用，其特征在于，所述血根碱杀灭钉螺的水溶液浓度≥0.4mg/L。
3.根据权利要求2所述的血根碱作为杀灭钉螺药物的应用，其特征在于，所述血根碱杀灭钉螺的水溶液浓度≥0.8mg/L。
4.根据权利要求3所述的血根碱作为杀灭钉螺药物的应用，其特征在于，所述血根碱杀灭钉螺的水溶液浓度≥1.5mg/L。
5.根据权利要求4所述的血根碱作为杀灭钉螺药物的应用，其特征在于，所述血根碱杀灭钉螺的水溶液浓度≥6.25mg/L。
6.根据权利要求5所述的血根碱作为杀灭钉螺药物的应用，其特征在于，所述血根碱杀灭钉螺的水溶液浓度≥12.5mg/L。
7.根据权利要求6所述的血根碱作为杀灭钉螺药物的应用，其特征在于，所述血根碱杀灭钉螺的水溶液浓度≥25mg/L。
8.根据权利要求7所述的血根碱作为杀灭钉螺药物的应用，其特征在于，所述血根碱杀灭钉螺的水溶液浓度≥50mg/L。
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| CN102246826A (zh) * | 2011-05-11 | 2011-11-23 | 王乃利 | 一种含有天然植物毒素的生物农药及其制备方法 |
| CN110590463A (zh) * | 2019-10-25 | 2019-12-20 | 湖北大学 | 一种施肥杀螺双效有机肥杀螺剂、制备方法及其应用 |
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| CN102246826A (zh) * | 2011-05-11 | 2011-11-23 | 王乃利 | 一种含有天然植物毒素的生物农药及其制备方法 |
| CN110590463A (zh) * | 2019-10-25 | 2019-12-20 | 湖北大学 | 一种施肥杀螺双效有机肥杀螺剂、制备方法及其应用 |
| CN110590463B (zh) * | 2019-10-25 | 2021-10-15 | 湖北大学 | 一种施肥杀螺双效有机肥杀螺剂、制备方法及其应用 |
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