Exploring Tryptophan-based Short Peptides: Promising Candidate for Anticancer and Antimicrobial Therapies.

IF 2.6 4区医学 Q3 CHEMISTRY, MEDICINAL

Anti-cancer agents in medicinal chemistry Pub Date : 2024-09-18 DOI:10.2174/0118715206260662240613054521

Neha Rai, Richa Tripathy Tiwari, Adarsh Sahu, Ekta Verma, Swati Rathore, Shailendra Patil, Asmita Gajbhiye Patil

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Abstract

Background: Ultra-short peptides are essential therapeutic agents due to their heightened selectivity and reduced toxicity. Scientific literature documents the utilization of dipeptides, tripeptides, and tetrapeptides as promising agents for combating cancer. We have created a range of tryptophan-based peptides derived from literature sources in order to assess their potential as anticancer drugs.

Methods: We present the results of our study on the antibacterial and anticancer effectiveness of 10 ultra-short peptides that were produced utilizing microwave-assisted solid phase peptide synthesis. The synthesized peptides underwent screening for in vitro antibacterial activity using the agar dilution method.

Results: HPLC, LC-MS, 1H NMR, and 13C NMR spectroscopy were used to analyze the synthesized peptides. In tests using the HeLa and MCF-7 cell lines, the synthesized peptides' anticancer efficacy was assessed. The study found that two peptides showed potential median inhibitory concentration (IC50) values of 3.9±0.13 μM and 1.8±0.09 μM, respectively, and showed more activity than the reference medication doxorubicin.

Conclusion: The antibacterial activity of synthesized peptides 3b and 4b was found to be better than the other synthetic peptides. MIC value of roughly 5-50 μg/mL for peptides 3a, 4c, and 4d showed strong antifungal activity against Candida albicans. The synthesized peptides were also evaluated for their anticancer activity against HeLa and MCF-7 cell lines, and found that peptides 3e and 4e were more potent than other peptides against doxorubicin.

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探索基于色氨酸的短肽：有望成为抗癌和抗菌疗法的候选药物。

背景：超短肽具有选择性强和毒性低的特点，是一种重要的治疗药物。科学文献记载了二肽、三肽和四肽作为抗癌药物的应用前景。我们从文献中提取了一系列基于色氨酸的肽，以评估它们作为抗癌药物的潜力：我们展示了利用微波辅助固相肽合成技术生产的 10 种超短肽的抗菌和抗癌效果的研究结果。我们采用琼脂稀释法对合成的多肽进行了体外抗菌活性筛选：结果：使用 HPLC、LC-MS、1H NMR 和 13C NMR 光谱分析了合成的多肽。在使用 HeLa 和 MCF-7 细胞系进行的测试中，评估了合成肽的抗癌功效。研究发现，两种肽的潜在中位抑制浓度（IC50）值分别为 3.9±0.13 μM 和 1.8±0.09 μM，其活性高于参考药物多柔比星：结论：合成肽 3b 和 4b 的抗菌活性优于其他合成肽。肽 3a、4c 和 4d 的 MIC 值约为 5-50 μg/mL，对白色念珠菌具有很强的抗真菌活性。此外，还评估了合成肽对 HeLa 和 MCF-7 细胞系的抗癌活性，结果发现肽 3e 和 4e 比其他肽对多柔比星更有效。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Anti-cancer agents in medicinal chemistry ONCOLOGY-CHEMISTRY, MEDICINAL

CiteScore

5.10

自引率

3.60%

发文量

323

审稿时长

4-8 weeks

期刊介绍： Formerly: Current Medicinal Chemistry - Anti-Cancer Agents. Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents. Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication. Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.