Al-Sayed Eman, Hamid Hoda Abdel, Abu El Einin Hanaa M
Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University , Cairo , Egypt and.
Pharm Biol. 2014 Jun;52(6):698-705. doi: 10.3109/13880209.2013.865240. Epub 2014 Feb 7.
Schistosomiasis is a parasitic disease that results in severe organ damage. Snail control is the best measure to control schistosomiasis. Plant-derived molluscicides have gained increasing attention for the control of schistosomiasis because they have low toxicity towards non-target organisms. Tannins are particularly suitable for snail control because they are less toxic than saponins to non-target organisms.
To identify the most toxic components of two plants belonging to the family Myrtaceae, namely Eucalyptus globulus Labill. and Melaleuca styphelioides Sm against the different developmental stages of Schistosoma mansoni and its snail host.
The 80% MeOH leaf extracts of the tested plants and their isolated compounds were screened for their molluscicidal activity (expressed as LC50 and LC90 after 24 h exposure) against the snail Biomphalaria alexandrina. The anti-schistosomal activity of the tested samples was determined at 20 ppm (after 1 or 2 h exposure) against the different developmental stages of S. mansoni, including the miracidia, cercariae and worms. Biochemical parameters were measured to determine the toxicity mechanisms of the treated snails. The structures of the isolated compounds were elucidated based on NMR, UV and HRESI-MS/MS data.
Potent molluscicidal activity was observed for the ellagitannin dimer eucalbanin B (12), with an LC50 value of 55 ppm. Treatment of the snails with the LC25 of eucalbanin B (30.8 ppm) resulted in a significant decrease in the protein level by 22.7% and 25.8% in the snail tissues and hemolymph, respectively. The decreased protein content was attributed to destruction of the snail tissue and impairment in protein synthesis under stress conditions of intoxication with eucalbanin B. Alterations in the activities of the transaminases and phosphatases in the treated snails indicated destruction and intoxication of the snail tissues. A significant increase in the levels of the transaminases alanine aminotransferase (ALT) (57.8%) and aspartate aminotransferase (AST) (113.2%) in the snail hemolymph and a significant decrease in their tissue levels to 7.4 and 48.6%, respectively, were attributed to their release from the damaged tissue into the hemolymph. Alkaline phosphatase (ALP) was significantly increased by 38.5 and 181.4% in the hemolymph and tissues, respectively. Acid phosphatase (ACP) was also significantly increased by 48.4 and 21.2% in the hemolymph and tissues, respectively. The 80% MeOH extract of E. globulus together with mallophenol B (3), 2,2,8-trimethyl-6-formyl-chrom-3-ene-7-O-β-d-glucopyranoside (5) and benzyl alcohol 7-O-(3',4',6'-tri-O-galloyl)-β-d-glucopyranoside (10) exhibited miracidicidal activity with almost 100% toxicity at 20 ppm for the three compounds and 80% toxicity for the extract. Moreover, E. globulus extract showed cercaricidal and schistosomicidal activity with 100 and 40% mortality, respectively.
E. globulus is a potential source for biocidal compounds against S. mansoni and its snail host. This is the first study to test the biocidal activity of the isolated compounds.
血吸虫病是一种会导致严重器官损伤的寄生虫病。控制钉螺是控制血吸虫病的最佳措施。植物源杀螺剂因其对非靶标生物毒性低而在血吸虫病防治中受到越来越多的关注。单宁特别适合用于控制钉螺,因为它们对非靶标生物的毒性比皂苷小。
鉴定桃金娘科的两种植物,即蓝桉(Eucalyptus globulus Labill.)和白千层(Melaleuca styphelioides Sm)对曼氏血吸虫及其钉螺宿主不同发育阶段毒性最强的成分。
筛选受试植物的80%甲醇叶提取物及其分离得到的化合物对埃及钉螺的杀螺活性(暴露24小时后以LC50和LC90表示)。在20 ppm浓度下(暴露1或2小时后)测定受试样品对曼氏血吸虫不同发育阶段,包括毛蚴、尾蚴和成虫的抗血吸虫活性。测量生化参数以确定处理后钉螺的毒性机制。根据核磁共振、紫外和高分辨电喷雾电离串联质谱数据阐明分离得到的化合物的结构。
观察到鞣花单宁二聚体桉白菌素B(12)具有很强的杀螺活性,LC50值为55 ppm。用桉白菌素B的LC25(30.8 ppm)处理钉螺后,钉螺组织和血淋巴中的蛋白质水平分别显著降低了22.7%和25.8%。蛋白质含量的降低归因于钉螺组织的破坏以及在桉白菌素B中毒应激条件下蛋白质合成受损。处理后钉螺中转氨酶和磷酸酶活性的变化表明钉螺组织受到破坏和中毒。钉螺血淋巴中谷丙转氨酶(ALT)(57.8%)和谷草转氨酶(AST)(113.2%)水平显著升高,而它们在组织中的水平分别显著降低至7.4%和48.6%,这归因于它们从受损组织释放到血淋巴中。碱性磷酸酶(ALP)在血淋巴和组织中分别显著升高了38.5%和181.4%。酸性磷酸酶(ACP)在血淋巴和组织中也分别显著升高了48.4%和21.2%。蓝桉的80%甲醇提取物与马洛酚B(3)、2,2,8 - 三甲基 - 6 - 甲酰基 - 色烯 - 7 - O - β - D - 吡喃葡萄糖苷(5)和苄醇7 - O -(3',4',6' - 三 - O - 没食子酰基) - β - D - 吡喃葡萄糖苷(10)对毛蚴具有杀蚴活性,这三种化合物在20 ppm时毒性几乎达100%,提取物毒性为80%。此外,蓝桉提取物显示出杀尾蚴和杀血吸虫活性,死亡率分别为100%和40%。
蓝桉是针对曼氏血吸虫及其钉螺宿主的生物活性化合物的潜在来源。这是首次测试分离得到的化合物的生物活性的研究。