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Amphiphiles capsaicin and triton X-100 regulate the chemotherapy drug colchicine’s membrane adsorption and ion pore formation potency
Saudi Journal of Biological Sciences Pub Date : 2021-02-21 , DOI: 10.1016/j.sjbs.2021.02.054
Md Ashrafuzzaman 1
Affiliation  

Chemotherapy drugs (CDs), e.g. colchicine derivative thiocolchicoside (TCC) and taxol, have been found to physically bind with lipid bilayer membrane and induce ion pores. Amphiphiles capsaicin (Cpsn) and triton X-100 (TX100) are known to regulate lipid bilayer physical properties by altering bilayer elasticity and lipid monolayer curvature. Both CDs and amphiphiles are predicted to physically accommodate alongside lipids in membrane to exert their membrane effects. The effects of their binary accommodation in the lipid membrane are yet to be known. Firstly, we have performed experimental studies to inspect whether membrane adsorption of CDs (colchicine or TCC) gets regulated due to any membrane effects of Cpsn or TX100. We find that the aqueous phase presence of these amphiphiles, known to reduce the membrane stiffness, works towards enhancing the membrane adsorption of CDs. Our recently patented technology ‘direct detection method’ helps address the membrane adsorption mechanisms. Secondly, in electrophysiology records, we measured the amphiphile effects on the potency of ion channel induction due to CDs. We find that amphiphiles increase the CD induced channel induction potency. Specifically, the membrane conductance, apparently due to the ion channel induction by the TCC, increases substantially due to the Cpsn or TX100 induced alterations of the bilayer physical properties. Thus we may conclude that the binary presence of CDs and amphiphiles in lipid membrane may influence considerably in CD’s membrane adsorption, as well as the membrane effects, such as ion pore formation.



中文翻译:


两亲辣椒素和 Triton X-100 调节化疗药物秋水仙碱的膜吸附和离子孔形成效力



化疗药物(CD),例如秋水仙碱衍生物硫代秋水仙苷(TCC)和紫杉醇,已被发现与脂质双层膜物理结合并诱导离子孔。已知两亲辣椒素 (Cpsn) 和 Triton X-100 (TX100) 通过改变双层弹性和脂质单层曲率来调节脂质双层物理特性。预计环糊精和两亲物都会与膜中的脂质一起物理适应,以发挥其膜效应。它们在脂膜中二元调节的影响尚不清楚。首先,我们进行了实验研究,以检查 CD(秋水仙碱或 TCC)的膜吸附是否因 Cpsn 或 TX100 的膜效应而受到调节。我们发现,水相中存在的这些两亲物可以降低膜的刚度,有助于增强 CD 的膜吸附。我们最近的专利技术“直接检测方法”有助于解决膜吸附机制。其次,在电生理学记录中,我们测量了两亲物对 CD 引起的离子通道诱导效力的影响。我们发现两亲物增加了 CD 诱导的通道诱导效力。具体来说,膜电导显然是由于 TCC 的离子通道诱导,但由于 Cpsn 或 TX100 诱导的双层物理性质的改变而显着增加。因此,我们可以得出结论,脂膜中环糊精和两亲物的二元存在可能对环糊精的膜吸附以及离子孔形成等膜效应产生相当大的影响。

更新日期:2021-04-30
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