Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, 226015, Uttar Pradesh, India; Jawaharlal Nehru University, New Delhi, 110067, India.
Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, 226015, Uttar Pradesh, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, Uttar Pradesh, India.
Pharmacol Res. 2020 Nov;161:105202. doi: 10.1016/j.phrs.2020.105202. Epub 2020 Sep 15.
To date, cancer is the second leading cause of death worldwide after cardiac arrest. A large number of synthetic drugs are available for the treatment of different types of cancer; however, a major problem associated with these drugs is its toxicity towards the normal cells. To overcome these problems, researchers explore plants derived phytochemicals because of their pleiotropic action and least toxicity towards the normal cells. Tangeretin is a polymethoxylated flavone found extensively in citrus fruits and has shown potent anti-cancer activity in different types of cancer cells. Hence, this review examines the anti-cancer activity of tangeretin via different molecular targets/pathways. Tangeretin induces apoptosis via intrinsic as well as extrinsic pathways and arrest the cell cycle. It also suppresses cell proliferation by modulating PI3K/AKT/mTOR, Notch, and MAPK signalling pathways. Besides, it induces autophagic cell death, suppresses migration, invasion, and angiogenesis. Further, the role of tangeretin in multi-drug resistance and combination therapy, different biological sources of tangeretin, its derivatives, and pharmacokinetics profile and toxicity studies are also discussed. Towards the end, the challenges associated with tangeretin usage as potential anti-cancer phytochemicals have also been discussed. Tangeretin, like a pandora's box, needs to be explored further, and more research is warranted to improve its usefulness for better human health.
迄今为止，癌症是全球仅次于心脏骤停的第二大死亡原因。有大量的合成药物可用于治疗不同类型的癌症；然而，这些药物的一个主要问题是它们对正常细胞的毒性。为了克服这些问题，研究人员探索了植物来源的植物化学物质，因为它们具有多效性作用，对正常细胞的毒性最小。橘红素是一种广泛存在于柑橘类水果中的多甲氧基黄酮，已显示出对不同类型癌细胞的强大抗癌活性。因此，本综述通过不同的分子靶点/途径检查了橘红素的抗癌活性。橘红素通过内在和外在途径诱导细胞凋亡，并阻止细胞周期。它还通过调节 PI3K/AKT/mTOR、Notch 和 MAPK 信号通路来抑制细胞增殖。此外，它诱导自噬性细胞死亡、抑制迁移、侵袭和血管生成。此外，还讨论了橘红素在多药耐药和联合治疗中的作用、橘红素的不同生物来源、其衍生物以及药代动力学特征和毒性研究。最后，还讨论了将橘红素用作潜在抗癌植物化学物质的相关挑战。橘红素就像潘多拉的盒子一样，需要进一步探索，需要更多的研究来提高其对人类健康的有益性。
