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水飞蓟宾、水飞蓟宁和 2,3-脱水水飞蓟宾对缺氧和有氧体外条件下幼虫(绦虫)的差异影响。

Differential Effects of the Flavonolignans Silybin, Silychristin and 2,3-Dehydrosilybin on Larvae (Cestoda) under Hypoxic and Aerobic In Vitro Conditions.

机构信息

Department of Experimental Pharmacology, Institute of Parasitology, Slovak Academy of Sciences, Hlinkova 3, SK 040 01 Košice, Slovakia.

Laboratory of Molecular Structure Characterization, Institute of Microbiology of the Czech Academy of Sciences, Vídeňská 1083, CZ 142 20 Prague, Czech Republic.

出版信息

Molecules. 2018 Nov 16;23(11):2999. doi: 10.3390/molecules23112999.

Abstract

larvae represent a suitable model for evaluating the larvicidal potential of various compounds. In this study we investigated the in vitro effects of three natural flavonolignans-silybin (SB), 2,3-dehydrosilybin (DHSB) and silychristin (SCH)-on larvae at concentrations of 5 and 50 μM under aerobic and hypoxic conditions for 72 h. With both kinds of treatment, the viability and motility of larvae remained unchanged, metabolic activity, neutral red uptake and concentrations of neutral lipids were reduced, in contrast with a significantly elevated glucose content. Incubation conditions modified the effects of individual FLs depending on their concentration. Under both sets of conditions, SB and SCH suppressed metabolic activity, the concentration of glucose, lipids and partially motility more at 50 μM, but neutral red uptake was elevated. DHSB exerted larvicidal activity and affected motility and neutral lipid concentrations differently depending on the cultivation conditions, whereas it decreased glucose concentration. DHSB at the 50 μM concentration caused irreversible morphological alterations along with damage to the microvillus surface of larvae, which was accompanied by unregulated neutral red uptake. In conclusion, SB and SCH suppressed mitochondrial functions and energy stores, inducing a physiological misbalance, whereas DHSB exhibited a direct larvicidal effect due to damage to the tegument and complete disruption of larval physiology and metabolism.

摘要

幼虫是评估各种化合物的杀幼虫潜力的合适模型。在这项研究中,我们在有氧和缺氧条件下,以 5 和 50 μM 的浓度,研究了三种天然类黄酮木脂素 - 水飞蓟宾(SB)、2,3-脱水水飞蓟宾(DHSB)和水飞蓟宾(SCH)对幼虫的体外影响,持续 72 小时。在这两种处理方式下,幼虫的活力和运动能力保持不变,代谢活性、中性红摄取和中性脂质浓度降低,而葡萄糖含量显著升高。孵育条件根据浓度的不同,改变了各个 FL 的作用。在这两种条件下,SB 和 SCH 在 50 μM 时更能抑制代谢活性、葡萄糖、脂质浓度和部分运动能力,但中性红摄取增加。DHSB 根据培养条件表现出杀幼虫活性,并以不同的方式影响运动能力和中性脂质浓度,同时降低葡萄糖浓度。DHSB 在 50 μM 浓度下会导致幼虫不可逆的形态改变,以及微绒毛表面受损,伴随着不受调节的中性红摄取。总之,SB 和 SCH 抑制了线粒体功能和能量储备,导致生理失衡,而 DHSB 由于对表皮的损害以及对幼虫生理和新陈代谢的完全破坏,表现出直接的杀幼虫作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c394/6278466/11cdcaaa7622/molecules-23-02999-g001.jpg

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