Kumar Shashank, Prajapati Kumari Sunita, Shuaib Mohd, Kushwaha Prem Prakash, Tuli Hardeep Singh, Singh Atul Kumar
Molecular Signaling & Drug Discovery Laboratory, Department of Biochemistry, Central University of Punjab, Bathinda, India.
Department of Biotechnology, Maharishi Markandeshwar (Deemed to be University), Ambala, India.
Front Pharmacol. 2021 Sep 27;12:737137. doi: 10.3389/fphar.2021.737137. eCollection 2021.
In the present article we present an update on the role of chemoprevention and other pharmacological activities reported on kurarinone, a natural flavanone (from 1970 to 2021). To the best of our knowledge this is the first and exhaustive review of kurarinone. The literature was obtained from different search engine platforms including PubMed. Kurarinone possesses anticancer potential against cervical, lung (non-small and small), hepatic, esophageal, breast, gastric, cervical, and prostate cancer cells. anticancer potential of kurarinone has been extensively studied in lungs (non-small and small) using experimental xenograft models. In anticancer studies, kurarinone showed IC in the range of 2-62 µM while efficacy was studied in the range of 20-500 mg/kg body weight of the experimental organism. The phytochemical showed higher selectivity toward cancer cells in comparison to respective normal cells. kurarinone inhibits cell cycle progression in G2/M and Sub-G1 phase in a cancer-specific context. It induces apoptosis in cancer cells by modulating molecular players involved in apoptosis/anti-apoptotic processes such as NF-κB, caspase 3/8/9/12, Bcl2, Bcl-XL, etc. The phytochemical inhibits metastasis in cancer cells by modulating the protein expression of Vimentin, N-cadherin, E-cadherin, MMP2, MMP3, and MMP9. It produces a cytostatic effect by modulating p21, p27, Cyclin D1, and Cyclin A proteins in cancer cells. Kurarinone possesses stress-mediated anticancer activity and modulates STAT3 and Akt pathways. Besides, the literature showed that kurarinone possesses anti-inflammatory, anti-drug resistance, anti-microbial (fungal, yeast, bacteria, and Coronavirus), channel and transporter modulation, neuroprotection, and estrogenic activities as well as tyrosinase/diacylglycerol acyltransferase/glucosidase/aldose reductase/human carboxylesterases 2 inhibitory potential. Kurarinone also showed therapeutic potential in the clinical study. Further, we also discussed the isolation, bioavailability, metabolism, and toxicity of Kurarinone in experimental models.
在本文中，我们介绍了kurarinone（一种天然黄烷酮，1970年至2021年）化学预防作用及其他药理活性的最新情况。据我们所知，这是对kurarinone的首次全面综述。文献来源于包括PubMed在内的不同搜索引擎平台。Kurarinone对宫颈、肺（非小细胞和小细胞）、肝、食管、乳腺、胃、宫颈和前列腺癌细胞具有抗癌潜力。Kurarinone的抗癌潜力已在肺（非小细胞和小细胞）中使用实验性异种移植模型进行了广泛研究。在抗癌研究中，kurarinone的IC值在2 - 62 μM范围内，而在实验生物体体重20 - 500 mg/kg范围内研究了其疗效。与相应的正常细胞相比，这种植物化学物质对癌细胞表现出更高的选择性。Kurarinone在癌症特异性背景下抑制G2/M期和亚G1期的细胞周期进程。它通过调节参与凋亡/抗凋亡过程的分子因子（如NF-κB、半胱天冬酶3/8/9/12、Bcl2、Bcl-XL等）诱导癌细胞凋亡。这种植物化学物质通过调节波形蛋白、N-钙黏蛋白、E-钙黏蛋白、基质金属蛋白酶2、基质金属蛋白酶3和基质金属蛋白酶9的蛋白表达来抑制癌细胞转移。它通过调节癌细胞中的p21、p27、细胞周期蛋白D1和细胞周期蛋白A蛋白产生细胞生长抑制作用。Kurarinone具有应激介导的抗癌活性，并调节STAT3和Akt信号通路。此外，文献表明Kurarinone还具有抗炎、抗耐药、抗微生物（真菌、酵母、细菌和冠状病毒）、通道和转运体调节、神经保护和雌激素活性以及酪氨酸酶/二酰基甘油酰基转移酶/葡萄糖苷酶/醛糖还原酶/人羧酸酯酶2抑制潜力。Kurarinone在临床研究中也显示出治疗潜力。此外，我们还讨论了Kurarinone在实验模型中的分离、生物利用度、代谢和毒性。
