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Neomenthol prevents the proliferation of skin cancer cells by restraining tubulin polymerization and hyaluronidase activity
Journal of Advanced Research ( IF 6.992 ) Pub Date : 2021-06-10 , DOI: 10.1016/j.jare.2021.06.003
Kaneez Fatima, Nusrat Masood, Zahoor Ahmad Wani, Abha Meena, Suaib Luqman

Introduction

Neomenthol, a cyclic monoterpenoid, is a stereoisomer of menthol present in the essential oil of Mentha spp. It is used in food as a flavoring agent, in cosmetics and medicines because of its cooling effects. However, neomenthol was not much explored for its anticancer potential. Targeting hyaluronidase, Cathepsin-D, and ODC by phytochemicals are amongst the efficient approaches for cancer prevention and treatment.

Objectives

To investigate the molecular and cell target-based antiproliferative potential of neomenthol on human cancer (A431, PC-3, K562, A549, FaDu, MDA-MB-231, COLO-205, MCF-7, and WRL-68) and normal (HEK-293) cell lines.

Methods

The potency of neomenthol was evaluated on human cancer and normal cell line using SRB, NRU and MTT assays. The molecular target based study of neomenthol was carried out in cell-free and cell-based test systems. Further, the potency of neomenthol was confirmed by quantitative real-time PCR analysis and molecular docking studies. The in vivo anticancer potential of neomenthol was performed on mice EAC model and the toxicity examination was accomplished through in silico, ex vivo and in vivo approaches.

Results

Neomenthol exhibits a promising activity (IC50 17.3±6.49 μM) against human epidermoid carcinoma (A431) cells by arresting the G2/M phase and increasing the number of sub-diploid cells. It significantly inhibits hyaluronidase activity (IC50 12.81±0.01 μM) and affects the tubulin polymerization. The expression analysis and molecular docking studies support the in vitro molecular and cell target based results. Neomenthol prevents EAC tumor formation by 58.84% and inhibits hyaluronidase activity up to 10% at 75 mg/kg bw, i.p. dose. The oral dose of 1000 mg/kg bw was found safe in acute oral toxicity studies.

Conclusion

Neomenthol delayed the growth of skin carcinoma cells by inhibiting the tubulin polymerization and hyaluronidase activity, which are responsible for tumor growth, metastasis, and angiogenesis.



中文翻译:

新薄荷醇通过抑制微管蛋白聚合和透明质酸酶活性来防止皮肤癌细胞的增殖

介绍

新薄荷醇是一种环状单萜,是薄荷属植物精油中薄荷醇的立体异构体由于其清凉作用,它在食品中用作调味剂、化妆品和药品。然而,新薄荷醇的抗癌潜力并未得到太多探索。通过植物化学物质靶向透明质酸酶、组织蛋白酶 D 和 ODC 是预防和治疗癌症的有效方法之一。

目标

研究新薄荷醇对人类癌症(A431、PC-3、K562、A549、FaDu、MDA-MB-231、COLO-205、MCF-7 和 WRL-68)和正常人的基于分子和细胞靶标的抗增殖潜力(HEK-293) 细胞系。

方法

使用 SRB、NRU 和 MTT 测定法评估了新薄荷醇对人类癌症和正常细胞系的效力。在无细胞和基于细胞的测试系统中进行了基于分子靶标的新薄荷醇研究。此外,通过实时定量 PCR 分析和分子对接研究证实了新薄荷醇的效力。该体内物对小鼠模型EAC进行新薄荷醇的抗癌潜力和毒性检查是通过实现在计算机芯片上离体体内方法。

结果

新薄荷醇通过阻止 G2/M 期和增加亚二倍体细胞的数量,对人表皮样癌 (A431) 细胞表现出有希望的活性 (IC 50 17.3±6.49 μM)。它显着抑制透明质酸酶活性 (IC 50 12.81±0.01 μM) 并影响微管蛋白聚合。表达分析和分子对接研究支持基于体外分子和细胞靶标的结果。新薄荷醇在 75 mg/kg bw,ip剂量下可防止 EAC 肿瘤形成 58.84%,并抑制透明质酸酶活性高达 10% 。在急性口服毒性研究中发现口服剂量为 1000 毫克/千克体重是安全的。

结论

新薄荷醇通过抑制导致肿瘤生长、转移和血管生成的微管蛋白聚合和透明质酸酶活性来延缓皮肤癌细胞的生长。

更新日期:2021-06-10
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