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1.
Drug Evaluation Research ; (6): 1510-1519, 2017.
Artigo em Chinês | WPRIM | ID: wpr-664648

RESUMO

Ursolic and oleanolic acids antagonize ox-LDL-,C-reactive protein-,non-enzymatic glycation end products-,hyper-glucose-,H2O2-,lipopolysaccharide-induced endothelial cell injury,and their vascular pharmacologic effects are in many ways.Ursolic and oleanolic acids can inhibit the proliferation of vascular smooth muscle cells,and antagonize serum-,ox-LDL-,hyper-glucose-,leptin-induced vascular smooth muscle cell proliferation,thus produce vascular protection and improve vascular function;Ursolic and oleanolic acids can relieve diabetic vascular complication in diabetic mellitus rats,and vascular stenosis induced by carotid balloon catheter injury,and suppress the proliferation of vascular adventitial fibroblasts and prevent vascular stenosis induced by various experimental atherosclerosis models;they can also inhibit the proliferation of vascular endothelial cells,and have a dual action to antagonize inhibiting or promoting proliferation induced by various injurious factions.Thus they have a dual role of regulation in angiogenesis,and suppress angiogenesis of cornea,diabetic retina,and tumor tissues,have effects of vascular relaxation and resistance decrease,and have hypotensive effects in normal and various hypertensive animals.

2.
Drug Evaluation Research ; (6): 1664-1670, 2017.
Artigo em Chinês | WPRIM | ID: wpr-664607

RESUMO

Oleanolic acid has a widespread pharmacologic effect,including anti-inflammation,antitumor,anfidiabetes,anti-atherosclerosis,hepatoprotection,anti-osteoporosis,etc.Bioavailability of oleanolic acid by oral administration is low,and is absorbed by intestine through passive transport.Oleanolic acid dispersion preparation can increase its solubility and bioavailability,and concentrate on liver to help treat for hepatic disease.The pharmacokinetic parameters,process in body of oleanolic acid,and the pharmacokinetic feature of oleanolic acid dispersion and its prodrug are reviewed,and its research advance on pharmacokinetics is summarized,which provides a reference for rational utilization of oleanolic acid.

3.
Drug Evaluation Research ; (6): 1019-1028, 2017.
Artigo em Chinês | WPRIM | ID: wpr-662849

RESUMO

Some animal model experiments have found that salidroside has protective effect for injuries in various neurons and brain tissue induced by various causes,so it is expected to be used in the prevention and treatment of peripheral nerve injury,and cerebral ischemic and neurodegenerative diseases,such as cerebral infarction,Alzheimer's disease,Parkinson's disease,epilepsy,depression,Tourette syndrome,amyotrophic lateral sclerosis,and diabetic encephalopathy.Its mechanisms of neuroprotection are multiple:(1) Salidroside protects neurons and stem cells from apoptotic injury by antioxidation,blocking NOX2/ROS/MAPKs and REDD 1/mTOR/p70S6K signaling pathways,and promoting AMPK/SIRT1,RhoA-MAPK and PI3K/Akt signaling pathways against various injurious factors-induced oxidative stress,inhibiting expression of inflammatory cytokines,preventing intracellular Ca2+ overload and caspase-3 activation;(2) Salidroside obstructs endogenous amyloid-β production by inhibition of expression of β-site amyloid precursor protein cleaving enzyme 1 and β-secretase activity.(3) Salidroside accelerates repair,regeneration and functional recovery of nerve by block Notch signaling pathway,and promoting BMP signaling pathway,super-regulating expression of neurotrophic factors,inducing neural stem cells and mesenchymal stem cells to differentiate into neural cells,and improving proliferation and function of Schwann cells.

4.
Drug Evaluation Research ; (6): 1019-1028, 2017.
Artigo em Chinês | WPRIM | ID: wpr-660870

RESUMO

Some animal model experiments have found that salidroside has protective effect for injuries in various neurons and brain tissue induced by various causes,so it is expected to be used in the prevention and treatment of peripheral nerve injury,and cerebral ischemic and neurodegenerative diseases,such as cerebral infarction,Alzheimer's disease,Parkinson's disease,epilepsy,depression,Tourette syndrome,amyotrophic lateral sclerosis,and diabetic encephalopathy.Its mechanisms of neuroprotection are multiple:(1) Salidroside protects neurons and stem cells from apoptotic injury by antioxidation,blocking NOX2/ROS/MAPKs and REDD 1/mTOR/p70S6K signaling pathways,and promoting AMPK/SIRT1,RhoA-MAPK and PI3K/Akt signaling pathways against various injurious factors-induced oxidative stress,inhibiting expression of inflammatory cytokines,preventing intracellular Ca2+ overload and caspase-3 activation;(2) Salidroside obstructs endogenous amyloid-β production by inhibition of expression of β-site amyloid precursor protein cleaving enzyme 1 and β-secretase activity.(3) Salidroside accelerates repair,regeneration and functional recovery of nerve by block Notch signaling pathway,and promoting BMP signaling pathway,super-regulating expression of neurotrophic factors,inducing neural stem cells and mesenchymal stem cells to differentiate into neural cells,and improving proliferation and function of Schwann cells.

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