Pharmacokinetics and Pharmacodynamics of the Triterpenoid Ursolic Acid in Regulating the Antioxidant, Anti-inflammatory, and Epigenetic Gene Responses in Rat Leukocytes

Zhang, Chengyue; Wang, Chao; Li, Wenji; Wu, Renyi; Guo, Yue; Cheng, David; Yang, Yuqing; Androulakis, Ioannis P.; Kong, Ah‐Ng Tony

doi:10.1021/acs.molpharmaceut.7b00469

Cited by 48 publications

(36 citation statements)

References 38 publications

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“…Ursolic acid (UA) is a pentacyclic triterpenoid found in many herbs and spices like rosemary and thyme, especially in valuable Chinese medicinal herbs such as Fructus Ligustrum lucidum [ 18 ] and Forsythiae fructus [ 19 ]. It shows potentially beneficial activities in treating cardiovascular disease due to its anti-oxidative [ 14 ], anti-inflammatory effects [ 20 ], and other biological activities [ 21 , 22 ]. However, it also demonstrates potential adverse effects.…”

Section: Introductionmentioning

confidence: 99%

Ursolic Acid Attenuates Atherosclerosis in ApoE−/− Mice: Role of LOX-1 Mediated by ROS/NF-κB Pathway

et al. 2018

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Atherosclerosis, a chronic inflammatory disease, is a major contributor to cardiovascular diseases. Ursolic acid (UA) is a phytonutrient with widely biological effects including anti-oxidative, anti-inflammatory, and so on. At present, the effect of UA on atherosclerosis and the mechanism of action are still obscure. This study focused on investigating the effects of UA on atherosclerosis both in vivo and in vitro. We first selected LOX-1 as our target, which was reckoned as a new promising receptor for treating atherosclerosis. The evaluation in vitro suggested that UA significantly decreased endothelial LOX-1 expression induced by LPS both in mRNA and protein levels. Pre-treatment of UA also inhibited TLR4/MyD88 signaling activated by LPS. Moreover, UA reduced ROS production and suppressed the activation of NF-κB stimulated by LPS. Particularly, the evaluation in vivo further verified the conclusion obtained in vitro. In ApoE−/− mice fed with an atherogenic diet, both UA (100 mg/kg/day) and simvastatin significantly attenuated atherosclerotic plaque formation and shrunk necrotic core areas. The enhanced expression of LOX-1 in atherosclerotic aorta was also dramatically decreased by administration of UA. Taken together, these results suggested that UA, with anti-atherosclerotic activity through inhibition of LOX-1 mediated by ROS/NF-κB signaling pathways, may become a valuable vascular protective candidate for the treatment of atherosclerosis.

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Section: Introductionmentioning

confidence: 99%

Ursolic Acid Attenuates Atherosclerosis in ApoE−/− Mice: Role of LOX-1 Mediated by ROS/NF-κB Pathway

et al. 2018

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“…The hydrophobic PUA and amphiphilic DSPE‐PEG2000 can spontaneously self‐assemble in water. The formed nanoparticles had a stable and small particle size (≈122 nm), which was beneficial for subsequent application in vivo . The presence of stabilizer containing hydrophilic PEG chains allows the PUA solution dissolved in DMSO to rapidly nucleate and self‐assemble after contact with the aqueous phase, ensuring the stability and monodispersity in size of the nanoparticles.…”

Section: Resultsmentioning

confidence: 99%

Nanodrug Carrier Based on Poly(Ursolic Acid) with Self‐Anticancer Activity against Colorectal Cancer

Guan

et al. 2019

Adv Funct Materials

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As the second most common cause of cancer‐related death worldwide, colorectal cancer (CRC) requires novel therapy strategies. Biodegradable polymers are used as drug carriers for treating CRC and other cancers. However, one of the limitations for the polymeric drug carriers is that they do not directly involve the treating procedure. Herein, to develop a polymeric drug delivery system with additional therapeutic effect from that of the polymer itself, poly(ursolic acid) (PUA) is, for the first time, simply synthesized via polycondensation of ursolic acid (UA), a bioactive ingredient widely distributed in herbal medicine. PUA can self‐assemble into nanoparticles (PUA‐NPs) with a diameter of ≈122 nm and an effective load of ≈10.1%, and deliver drugs, such as paclitaxel (PUA‐NPs@PTX). In vitro studies show that PUA‐NPs@PTX have strong cytotoxicity against colorectal cancer CT26 cells, while in vivo results indicate that these NPs have a prolonged blood circulation time, enhanced tumor accumulation, and significantly improved antitumor efficacy in CT26 tumor‐bearing mice. Furthermore, both in vitro and in vivo results confirm that the PUA‐NPs themselves have therapeutic effects on CT26 cells, without causing obvious toxicity to main organs, such as bledding or necrosis. In summary, such a therapeutic polymer platform provides a new therapeutic strategy for treating cancer.

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“…However, the contents of other compounds (salidroside, wedelolactone, oleanolic acid, and ursolic acid) in these samples were higher than in EZWP. These compounds cannot be ignored in the quality evaluation of EZW due to their good antioxidant activity [ 9 , 25 , 26 , 27 ]. The above results indicated that the quality control of a single index could not reflect the overall quality of the TCM herbal formula.…”

Section: Resultsmentioning

confidence: 99%

“…According to ChP 2015, it is composed of FLL (steamed) powder and aqueous extracts of HE, possessing the functions of tonifying the liver and kidney yin, strengthening tendon and bone, and arresting hemorrhage [ 4 ]. The main compounds from EZW, including phenylethanoid glycosides, iridoid glycosides, coumarins, triterpenes, and others, have antioxidant abilities [ 5 , 6 , 7 , 8 , 9 ], and EZW also plays many critical roles in protecting the liver and kidney [ 10 , 11 ]. However, the quality control of EZW still depends on the quantitation of the single-index specnuezhenide in the ChP 2015.…”

Section: Introductionmentioning

confidence: 99%

A Comprehensive Quality Evaluation Method Based on C30-HPLC and an Analytic Hierarchy Process for the Chinese Herbal Formula, Erzhiwan

Nie

Yao

2018

Molecules

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The quantitative analysis of multiple indexes remains an important quality evaluation method of traditional Chinese medicine (TCM) herbal formulas. The Chinese Pharmacopoeia 2015 only stipulates the content of a single component, specnuezhenide, in Erzhiwan composed of the Fructus Ligustri Lucidi (FLL) powder and aqueous extracts of Herba Ecliptae (HE). To generalize the intrinsic quality of Erzhiwan, a novel C30-HPLC method with good precision, accuracy, and reproducibility was developed for the simultaneous determination of six compounds, including two isomers, and then an analytic hierarchy process was further applied to integrate and discriminate the quality of four samples prepared via different methods. The results of the analysis were in agreement with the antioxidant tests in vitro. This comprehensive strategy could provide a reference and suggestions for the improvement of the quality evaluation method of TCM herbal formulas.

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Pharmacokinetics and Pharmacodynamics of the Triterpenoid Ursolic Acid in Regulating the Antioxidant, Anti-inflammatory, and Epigenetic Gene Responses in Rat Leukocytes

Cited by 48 publications

References 38 publications

Ursolic Acid Attenuates Atherosclerosis in ApoE−/− Mice: Role of LOX-1 Mediated by ROS/NF-κB Pathway

Ursolic Acid Attenuates Atherosclerosis in ApoE−/− Mice: Role of LOX-1 Mediated by ROS/NF-κB Pathway

Nanodrug Carrier Based on Poly(Ursolic Acid) with Self‐Anticancer Activity against Colorectal Cancer

A Comprehensive Quality Evaluation Method Based on C30-HPLC and an Analytic Hierarchy Process for the Chinese Herbal Formula, Erzhiwan

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