Li Yonghong, Pham Victor, Bui Michelle, Song Liankun, Wu Chunli, Walia Arman, Uchio Edward, Smith-Liu Feng, Zi Xiaolin
Department of Urology, University of California, Irvine, CA, USA.
Department of Pharmaceutical Sciences, University of California, Irvine, CA, USA.
Curr Pharmacol Rep. 2017 Dec;3(6):384-395. doi: 10.1007/s40495-017-0106-1. Epub 2017 Sep 14.
extracts have been used as a dietary supplement in healthy populations, including athletes, to non-specifically enhance the natural resistance of the body to both physical and behavior stresses for fighting fatigue and depression. We summarize the information with respect to the new pharmacological activities of extracts and its underlying molecular mechanisms in this review article.
In addition to its multiplex stress-protective activity, extracts have recently demonstrated its anti-aging, anti-inflammation, immunostimulating, DNA repair and anti-cancer effects in different model systems. Molecular mechanisms of extracts's action have been studied mainly along with one of its bioactive compounds, salidroside. Both extracts and salidroside have contrast molecular mechanisms on cancer and normal physiological functions. For cancer, extracts and salidroside inhibit the mTOR pathway and reduce angiogenesis through down-regulation of the expression of HIF-1α/HIF-2α. For normal physiological functions, extracts and salidroside activate the mTOR pathway, stimulate paracrine function and promote neovascularization by inhibiting PHD3 and stabilizing HIF-1α proteins in skeletal muscles. In contrast to many natural compounds, salidroside is water-soluble and highly bioavailable via oral administration and concentrated in urine by kidney excretion.
extracts and salidroside can impose cellular and systemic benefits similar to the effect of positive lifestyle interventions to normal physiological functions and for anti-cancer. The unique pharmacological properties of extracts or salidroside deserve further investigation for cancer chemoprevention, in particular for human urinary bladder cancer.
提取物已被用作健康人群(包括运动员)的膳食补充剂,以非特异性地增强身体对身体和行为压力的天然抵抗力,从而对抗疲劳和抑郁。在这篇综述文章中,我们总结了关于提取物的新药理活性及其潜在分子机制的信息。
除了其多重应激保护活性外,提取物最近在不同模型系统中还表现出抗衰老、抗炎、免疫刺激、DNA修复和抗癌作用。提取物作用的分子机制主要是与其一种生物活性化合物红景天苷一起研究的。提取物和红景天苷在癌症和正常生理功能方面具有相反的分子机制。对于癌症,提取物和红景天苷通过下调HIF-1α/HIF-2α的表达来抑制mTOR途径并减少血管生成。对于正常生理功能,提取物和红景天苷通过抑制PHD3并稳定骨骼肌中的HIF-1α蛋白来激活mTOR途径,刺激旁分泌功能并促进新血管形成。与许多天然化合物不同,红景天苷是水溶性的,口服后生物利用度高,并通过肾脏排泄集中在尿液中。
提取物和红景天苷对正常生理功能和抗癌可产生类似于积极生活方式干预效果的细胞和全身益处。提取物或红景天苷独特的药理特性值得进一步研究用于癌症化学预防,特别是对人类膀胱癌。