萝卜硫素的成药性及其在肿瘤和神经退行性疾病中的作用
The Pharmaceutical Properties of Sulforaphane and Its Role in Tumor and Neurodegenerative Diseases
吴见乐 1刘锡建 2刘儒华 3江峰 4缪丹5
作者信息
- 1. 赣南医学院,江西省医用组织工程材料与生物制造重点实验室,赣州 341000;赣南医学院康复学院,赣州 341000
- 2. 上海工程技术大学化学化工学院,上海 201620;赣州华汉生物科技有限公司,赣州 341100
- 3. 赣州华汉生物科技有限公司,赣州 341100
- 4. 赣南医学院,江西省医用组织工程材料与生物制造重点实验室,赣州 341000;赣州华汉生物科技有限公司,赣州 341100
- 5. 赣南医学院,江西省医用组织工程材料与生物制造重点实验室,赣州 341000
- 折叠
摘要
萝卜硫素是一种来源于十字花科类蔬菜的天然活性物质,具有强大的抗氧化和抗癌能力.研究表明,萝卜硫素可通过调节Nrf2、NF-κB、HSF1-HSP信号通路和调控表观遗传,从而作用于Ⅱ相解毒酶、HDAC和DNMT,影响癌症、神经退行性疾病等疾病的发生、发展.此外,由于萝卜硫素具有易吸收易代谢等特点,用纳米材料包裹萝卜硫素可提高其生物利用度和稳定性,更好发挥其疗效.近年来已有多项Ⅰ/Ⅱ期临床实验显示,萝卜硫素具有良好的成药性,这表明萝卜硫素在治疗癌症和神经退行性疾病方面有极高的药用潜力.本文主要针对萝卜硫素的药代动力学、作用靶点、安全性及其在肿瘤和神经退行性疾病中的研究进展进行综述,为萝卜硫素未来应用于肿瘤和神经退行性疾病的治疗提供参考.
Abstract
Sulforaphane is a naturally occurring active substance derived from cruciferous vegetables with potent antioxidant and anticancer properties.Researches have shown that sulforaphane has good bioavailability and can be absorbed by the small intestine through passive transport,followed by excretion in the form of urine via the hydrophobic acid pathway.In addition,since sulforaphane is easy to be absorbed and metabolized,wrapping sulforaphane with nanomaterials can improve its bioavailability and stability,prolong its action time in human body,and better utilize its therapeutic effect.In terms of mechanism of action,sulforaphane can activate Nrf2 and HSF1 signaling pathways,induce the expression of phase Ⅱ detoxification enzymes HO-1,NADPH,GST and HSP,thus regulating the concentration of oxidative stress ROS in vivo;inhibit NF-κB signaling pathway,thus suppressing the expression of inflammatory factors TNF-α,IL-1 and IL-6;regulate epigenetic modifications,thus inhibiting HDAC and DNMT,and increasing the concentration of histone H3 and H4.By regulating the expression levels of the above factors,sulforaphane can affect the occurrence and development of cancer,neurodegenerative diseases and other diseases.In recent years,several phase Ⅰ/Ⅱ clinical trials have shown that sulforaphane has good drug-generating properties.For example,researchers have found that patients with skin cancer have not shown any health problems and their corresponding functional problems have improved greatly after long-term use of sulforaphane.This suggests that in the future sulforaphane has a very high medicinal potential for the treatment of cancer and neurodegenerative diseases.In this paper,we review the pharmacokinetics,target of action and safety of sulforaphane and its research progress in tumor and neurodegenerative diseases to provide a reference for the future application of sulforaphane in the treatment of tumor and neurodegenerative diseases.
关键词
萝卜硫素/药代动力学/信号通路/肿瘤/神经退行性疾病Key words
sulforaphane/pharmacokinetic/signal pathway/tumor/neurodegenerative disease引用本文复制引用
基金项目
国家自然科学基金(21961003)
江西省自然科学基金(20212ACB206001)
江西省"千人计划"(jxsq2018106059)
赣州市自然科学基金()
中央引导地方科技发展专项基金(20231ZDF03071)
江西省教育厅科学研究项目(GJJ2201443)
出版年
2024
NETL
NSTL
维普
万方数据