关键词: Apis mellifera syriaca HeLa cell lines PLA2 anticoagulant effect bee venom melittin proteolytic activity

Mesh : Humans HeLa Cells Melitten / pharmacology chemistry Bee Venoms / pharmacology chemistry Anticoagulants / pharmacology chemistry Phospholipases A2 / metabolism Animals Bees Proteolysis / drug effects Antineoplastic Agents / pharmacology chemistry Cell Survival / drug effects Blood Coagulation / drug effects

来  源:   DOI:10.3390/molecules27051653   PDF(Pubmed)

Abstract:
Bee venom (BV) is one of the most remarkable natural products that has been a subject of studies since ancient times. Recent studies have shown that Apis mellifera syriaca venom possesses antibacterial as well as cytotoxic effects on cancer cell lines. The venom contains a variety of bioactive molecules-mainly melittin (MEL) and phospholipase A2 (PLA2), as well as other compounds that are not well characterized. In this work, we continue the biological characterization of A. mellifera syriaca venom by testing its anticoagulant effect on human plasma using the prothrombin time (PT) test, as well as assessing its proteolytic activity. In addition, the cytotoxicity of the crude venom-and of its two main components, MEL and PLA2-was tested on HeLa cancer cell lines for the first time. The results obtained showed the capacity of A. mellifera syriaca venom to increase clotting time, thereby proving its anticoagulant effect. Moreover, the venom did not demonstrate a significant proteolytic activity unless administrated at concentrations ≥ 5 mg/mL. Finally, we showed that crude A. mellifera syriaca venom, along with MEL, exhibit a strong in vitro cytotoxic effect on HeLa cancer cell lines, even at low concentrations. In summary, our findings could serve as a basis for the development of new natural-based drug candidates in the therapeutic field.
摘要:
蜂毒(BV)是自古以来一直是研究主题的最著名的天然产物之一。最近的研究表明,蜜蜂蛇毒对癌细胞具有抗菌和细胞毒性作用。毒液中含有多种生物活性分子-主要是蜂毒素(MEL)和磷脂酶A2(PLA2),以及其他没有很好表征的化合物。在这项工作中,我们通过使用凝血酶原时间(PT)测试来测试其对人血浆的抗凝血作用,继续进行A.melliferasyriaca毒的生物学表征,以及评估其蛋白水解活性。此外,粗毒液及其两种主要成分的细胞毒性,MEL和PLA2-首次在HeLa癌细胞系上测试。获得的结果表明,A.melliferasyriaca毒增加凝血时间的能力,从而证明其抗凝作用。此外,除非以≥5mg/mL的浓度给药,否则毒液没有显示出明显的蛋白水解活性。最后,我们展示了粗A.melliferasyriaca毒液,和MEL一起,对HeLa癌细胞系表现出强烈的体外细胞毒性作用,即使在低浓度。总之,我们的发现可以作为治疗领域开发新的天然药物候选物的基础.
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