Pharmacognosy & Phytochemistry Division, Department of Pharmaceutical Sciences, University of Kashmir, Hazratbal, Srinagar 190006, India.
Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences, University of Kashmir, Hazratbal, Srinagar 190006, India.
Molecules. 2022 Apr 12;27(8):2471. doi: 10.3390/molecules27082471.
Cancer is a major health problem across the globe, and is expeditiously growing at a faster rate worldwide. The endoplasmic reticulum (ER) is a membranous cell organelle having inextricable links in cellular homeostasis. Altering ER homeostasis initiates various signaling events known as the unfolded protein response (UPR). The basic purpose of the UPR is to reinstate the homeostasis; however, a continuous UPR can stimulate pathways of cell death, such as apoptosis. As a result, there is great perturbation to target particular signaling pathways of ER stress. Flavonoids have gained significant interest as a potential anticancer agent because of their considerable role in causing cytotoxicity of the cancerous cells. Luteolin, a flavonoid isolated from natural products, is a promising phytochemical used in the treatment of cancer. The current study is designed to review the different endoplasmic reticulum stress pathways involved in the cancer, mechanistic insights of luteolin as an anticancer agent in modulating ER stress, and the available luteolin patent formulations were also highlighted. The patents were selected on the basis of pre-clinical and/or clinical trials, and established antitumor effects using patent databases of FPO IP and Espacenet. The patented formulation of luteolin studied so far has shown promising anticancer potential against different cancer cell lines. However, further research is still required to determine the molecular targets of such bioactive molecules so that they can be used as anticancer drugs.
癌症是全球范围内的一个主要健康问题，在全球范围内迅速以更快的速度增长。内质网（ER）是一种膜细胞器，在细胞内稳态中具有不可分割的联系。改变 ER 内稳态会引发各种信号事件，称为未折叠蛋白反应（UPR）。UPR 的基本目的是恢复内稳态；然而，持续的 UPR 会刺激细胞死亡途径，如细胞凋亡。因此，针对 ER 应激的特定信号通路存在很大的干扰。由于其在引起癌细胞细胞毒性方面的重要作用，类黄酮作为一种潜在的抗癌剂引起了极大的关注。木犀草素是一种从天然产物中分离出来的类黄酮，是一种有前途的用于治疗癌症的植物化学物质。本研究旨在综述参与癌症的不同内质网应激途径、木犀草素作为一种抗癌剂在调节 ER 应激中的作用的机制见解，以及已有的木犀草素专利配方也得到了强调。专利是根据临床前和/或临床试验选择的，并利用 FPO IP 和 Espacenet 的专利数据库建立了抗肿瘤作用。迄今为止，研究的木犀草素专利配方已显示出对不同癌细胞系具有有希望的抗癌潜力。然而，仍需要进一步研究以确定此类生物活性分子的分子靶标，以便将它们用作抗癌药物。
