当前位置：
X-MOL 学术
›
Chem. Bio. Drug Des.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Anticancer activity of VmCT1 analogs against MCF‐7 cells
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-11-29 , DOI: 10.1111/cbdd.13123 Cibele Nicolaski Pedron 1 , Gislaine Patricia Andrade 1 , Roseli Hiromi Sato 1 , Marcelo Der Torossian Torres 1 , Giselle Cerchiaro 1 , Anderson Orzari Ribeiro 1 , Vani Xavier Oliveira 1
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-11-29 , DOI: 10.1111/cbdd.13123 Cibele Nicolaski Pedron 1 , Gislaine Patricia Andrade 1 , Roseli Hiromi Sato 1 , Marcelo Der Torossian Torres 1 , Giselle Cerchiaro 1 , Anderson Orzari Ribeiro 1 , Vani Xavier Oliveira 1
Affiliation
|
Antimicrobial peptides are considered promising drug candidates due to their broad range of activity. VmCT1 (Phe–Leu–Gly–Ala–Leu–Trp–Asn–Val–Ala–Lys–Ser–Val–Phe–NH2) is an α‐helical antimicrobial peptide that was obtained from the Vaejovis mexicanus smithi scorpion venom. Some of its analogs showed to be as antimicrobial as the wild type, and they were designed for understanding the influence of physiochemical parameters on antimicrobial and hemolytic activity. Some cationic antimicrobial peptides exhibit anticancer activity so VmCT1 analogs were tested to verify the anticancer activity of this family of peptides. The analogs were synthesized, purified, characterized, and the conformational studies were performed. The anticancer activity was assessed against MCF‐7 mammary cancer cells. The results indicated that [Glu]7‐VmCT1‐NH2, [Lys]3‐VmCT1‐NH2, and [Lys]7‐VmCT1‐NH2 analogs presented moderated helical tendency (0.23–0.61) and tendency of anticancer activity at 25 μmol/L in 24 hr of experiment; and [Trp]9‐VmCT1‐NH2 analog that presented low helical tendency and moderated anticancer activity at 50 μmol/L. These results demonstrated that single substitutions on VmCT1 led to different physicochemical features and could assist on the understanding of anticancer activity of this peptide family.
中文翻译：
VmCT1类似物对MCF-7细胞的抗癌活性
由于抗菌肽的广泛活性，被认为是有前途的候选药物。VmCT1（Phe–Leu–Gly–Ala–Leu–Trp–Asn–Val–Ala–Lys–Ser–Val–Phe–NH 2）是一种α-螺旋抗菌肽，得自史密斯拟杆菌蝎毒。它的某些类似物显示出与野生型一样的抗菌性，它们的设计目的是了解理化参数对抗菌和溶血活性的影响。一些阳离子抗微生物肽表现出抗癌活性，因此对VmCT1类似物进行了测试，以验证该肽家族的抗癌活性。合成，纯化，表征类似物，并进行构象研究。评估了对MCF-7乳腺癌细胞的抗癌活性。结果表明，[Glu] 7 -VmCT1-NH 2，[Lys] 3 -VmCT1-NH 2和[Lys] 7 -VmCT1-NH 2类似物在24 h实验中表现出缓和的螺旋趋势（0.23-0.61）和25μmol/ L的抗癌活性趋势；[Trp] 9 -VmCT1-NH 2类似物在50μmol/ L时具有低螺旋趋势和适度的抗癌活性。这些结果表明，VmCT1上的单取代导致不同的理化特性，并且可以帮助理解该肽家族的抗癌活性。
更新日期：2017-11-29
中文翻译：
VmCT1类似物对MCF-7细胞的抗癌活性
由于抗菌肽的广泛活性，被认为是有前途的候选药物。VmCT1（Phe–Leu–Gly–Ala–Leu–Trp–Asn–Val–Ala–Lys–Ser–Val–Phe–NH 2）是一种α-螺旋抗菌肽，得自史密斯拟杆菌蝎毒。它的某些类似物显示出与野生型一样的抗菌性，它们的设计目的是了解理化参数对抗菌和溶血活性的影响。一些阳离子抗微生物肽表现出抗癌活性，因此对VmCT1类似物进行了测试，以验证该肽家族的抗癌活性。合成，纯化，表征类似物，并进行构象研究。评估了对MCF-7乳腺癌细胞的抗癌活性。结果表明，[Glu] 7 -VmCT1-NH 2，[Lys] 3 -VmCT1-NH 2和[Lys] 7 -VmCT1-NH 2类似物在24 h实验中表现出缓和的螺旋趋势（0.23-0.61）和25μmol/ L的抗癌活性趋势；[Trp] 9 -VmCT1-NH 2类似物在50μmol/ L时具有低螺旋趋势和适度的抗癌活性。这些结果表明，VmCT1上的单取代导致不同的理化特性，并且可以帮助理解该肽家族的抗癌活性。
京公网安备 11010802027423号