Molander Marianne, Nielsen Line, Søgaard Søren, Staerk Dan, Rønsted Nina, Diallo Drissa, Chifundera Kusamba Zacharie, van Staden Johannes, Jäger Anna K
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Natural History Museum of Denmark, University of Copenhagen, DK-1307 Copenhagen, Denmark.
J Ethnopharmacol. 2014 Nov 18;157:171-80. doi: 10.1016/j.jep.2014.09.027. Epub 2014 Sep 23.
Snakebite envenomation, every year, causes estimated 5-10,000 mortalities and results in more than 5-15,000 amputations in sub-Saharan Africa alone. Antiserum is not easily accessible in these regions or doctors are simply not available, thus more than 80% of all patients seek traditional practitioners as first-choice. Therefore it is important to investigate whether the plants used in traditional medicine systems contain compounds against the necrosis-inducing enzymes of snake venom.
Extracts from traditionally used plants from DR Congo, Mali and South Africa were tested in hyaluronidase, phospholipase A2 and protease enzyme bioassays using Bitis arietans and Naja nigricollis as enzyme source.
A total of 226 extracts from 94 different plant species from the three countries, Mali, Democratic Republic of Congo and South Africa were tested in phospholipase A2, proteases and hyaluronidase enzyme assays. Forty plant species showed more than 90% inhibition in one or more assay. Fabaceae, Anacardiaceae and Malvaceae were the families with the highest number of active species, and the active compounds were distributed in different plant parts depending on plant species. Polyphenols were removed in the search for specific enzyme inhibitors against hyaluronidase, phospholipase A2 or proteases from extracts with IC50 values below 100µg/ml. Water extracts of Pupalia lappacea, Combretum molle, Strychnos innocua and Grewia mollis and ethanol extract of Lannea acida and Bauhinia thonningii still showed IC50 values below 100µg/ml in either the hyaluronidase or protease bioassay after removal of polyphenols.
As four of the active plants are widely distributed in the areas where the snake species Bitis arietans and Naja nigricollis occur a potential inhibitor of the necrotic enzymes is accessible for many people in sub-Saharan Africa.
仅在撒哈拉以南非洲地区，每年蛇咬伤中毒估计就导致5000至10000人死亡，并造成超过5000至15000例截肢。在这些地区，抗蛇毒血清不易获得，或者根本没有医生，因此超过80%的患者首先会寻求传统医生的帮助。因此，研究传统医学系统中使用的植物是否含有对抗蛇毒中诱导坏死酶的化合物非常重要。
以鼓腹咝蝰和黑颈眼镜蛇为酶源，对来自刚果民主共和国、马里和南非的传统使用植物提取物进行透明质酸酶、磷脂酶A2和蛋白酶生物测定。
对来自马里、刚果民主共和国和南非这三个国家的94种不同植物的226种提取物进行了磷脂酶A2、蛋白酶和透明质酸酶测定。40种植物在一种或多种测定中显示出超过90%的抑制率。豆科、漆树科和锦葵科是活性物种数量最多的科，活性化合物根据植物种类分布在不同的植物部位。在从IC50值低于100μg/ml的提取物中寻找针对透明质酸酶、磷脂酶A2或蛋白酶的特定酶抑制剂时，去除了多酚类物质。去除多酚类物质后，糙叶山麻杆、多花风车子、无毒马钱子和软叶扁担杆的水提取物以及酸叶石楠和托宁紫荆的乙醇提取物在透明质酸酶或蛋白酶生物测定中仍显示IC50值低于100μg/ml。
由于四种活性植物在鼓腹咝蝰和黑颈眼镜蛇这两种蛇类出现的地区广泛分布，撒哈拉以南非洲的许多人都有可能获得坏死酶的潜在抑制剂。
