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ursolic acid
CHROMATOGRAPHIA · 2020 ·Vol. 83 ·期 9 ·1121-1131 · IF 1.596

Monolithic Column Prepared with UiO-66-2COOH MOF as Monomer for Enrichment and Purification of Ursolic Acid in Plants by Online Solid-Phase Extraction

Pang Xiaoya,Liu Haiyan,Yu Huan,Zhang Miaomiao,Bai Ligai,Yan Hongyuan

A method for preparing a metal–organic framework (MOF)–polymeric monolith was established by in situ radical polymerization with derivatized UiO-66-2COOH and N- isopropylacrylamide (NIPAAm) as co-monomers. It was worth noting that the obtained monolith possessed characteristics of relatively uniform porous structure and a high surface area (84.16 m 2 g −1 ). The adsorption capacity of the monolith increased from 22.87 to 44.92 mg −1 due to the addition of MOF. The monolith was used as adsorbent and coupled with HPLC for the online purification and extraction of ursolic acid (UA) in medicinal plant. The limit of detection (LOD, S / N  = 3) and the limit of quantification (LOQ, S / N  = 10) were 0.17 μg mL −1 and 0.57 μg mL −1 , respectively; the relative standard deviation (RSD) of intra-day and inter-day assays for five plant samples were 1.00–3.67% and 2.43–5.76%, respectively; a good accuracy was demonstrated by the recovery of 92.2–103.28%. The results indicated that the MOF–polymer monolith was feasible for the online enrichment and purification of UA in plant.

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Nanomedicine-Nanotechnology Biology and Medicine · 2017 · IF 5.72

A self-assembly nanodrug delivery system based on amphiphilic low generations of PAMAM dendrimers-ursolic acid conjugate modified by lactobionic acid for HCC targeting therapy

Zhichun Shen,Bowen Li,Yajun Liu,Guirong Zheng,Yan Guo,Ruirui Zhao,Kai Jiang,Lulu Fan,Jingwei Shao

Ursolic acid (UA), a natural triterpene acid, is a promising anti-cancer drug due to its inhibitory effect on tumor growth and metastasis. However, clinical translation of UA is limited by its poor water solubility and low bioavailability. To overcome these problems, herein an amphiphilic self-assembly nanodrug composed of UA, lactobionic acid (LA) and low-polyamidoamine (low-PAMAM) dendrimers is developed. This near-spherical nanodrug with a uniform size (~180 nm) demonstrated to have an enhanced cytotoxicity against liver cancer SMMC7721 cells, and could attenuate the migration and adhesion of SMMC7721 cells at non-toxic concentrations by suppressing metastasis-related protein MMP-9 expression. Furthermore, in vivo study indicates that the nanodrug exhibited prolonged circulation time in blood as well as increased AUC, MRT and C max , and could effectively inhibit the tumor growth in H22 mice model. Overall, the UA-based nanodrug delivery system reported in the present work represents a novel strategy for targeted tumor therapy.

CAS / MDL: 538-75-0 74124-79-1
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JOURNAL OF NANOBIOTECHNOLOGY · 2026 · IF 15

Synergistic anti-obesity therapy: ursolic acid-loaded mesoporous polydopamine nanoparticles (MPDA@UA) in an injectable OHA-CMCS hydrogel with a mild photothermal effect for adipocyte reprogramming

Li Tingting,Zhao Yueming,Lin Mian,Hu Jiajun,Duan Kairui,Zhu Hu,Zi Taotao,Lee Bae Hoon

Obesity and its metabolic complications urgently require safe, effective, and minimally invasive interventions. Here, we engineered an injectable, self-healing hydrogel system (OCMU hydrogel) based on oxidized hyaluronic acid (OHA) and carboxymethyl chitosan (CMCS) for the localized delivery of plant-based ursolic acid (UA) loaded in mesoporous polydopamine (MPDA) nanoparticles. This system synergistically induces white adipose browning through combined photothermal therapy (PTT) and pharmacological action, effectively counteracting obesity. The OCMU hydrogel exhibited excellent self-healing properties, high UA loading capacity (81.04%), efficient photothermal conversion, and favorable biocompatibility. Mechanistically, the system promotes lipolysis, mitochondrial biogenesis, and adipose browning via activation of the AMPK/SIRT1/PGC-1α pathway, with a 439% increase in UCP1 expression in vitro. In obese mice, OCMU combined with PTT reduced body weight by 10.94% and inguinal fat by 56.32%, while significantly improving metabolic profiles and alleviating inflammation. Notably, the combination of mild PTT and naturally derived UA achieved superior anti-obesity efficacy compared to monotherapies, highlighting a favorable safety and efficacy profile. This work establishes a promising platform in which UA and mild PTT act in concert to reprogram adipocyte metabolism, offering a safe and synergistic approach to combat obesity. Graphical

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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES · 2019 · IF 2.813

A metal organic framework polymer monolithic column as a novel adsorbent for on-line solid phase extraction and determination of ursolic acid in Chinese herbal medicine

Xiaoya Pang,Haiyan Liu,Huan Yu,Miaomiao Zhang,Ligai Bai,Hongyuan Yan

A metal organic framework (MOF)-polymer monolithic column was prepared by redox initiation using modified MOF and N -methylolacrylamide (NMA) as co-monomers. The obtained monolithic column was characterized by scanning electron microscopy (SEM) and nitrogen adsorption-desorption isotherm measurement. It was used as a solid phase extraction (SPE) absorbent for the online enrichment of ursolic acid (UA) by high performance liquid chromatography . The adsorption amount of UA on the monolith was compared with that of silica gel-C18 adsorbent and the monolith without MOF material. The MOF-polymer monolithic column showed high selectivity and good permeability. Under the optimum conditions for extraction and determination, the calibration equation was y = 79.854× + 0.1939; the linear range was 0.001–0.9 mg/mL; the linear regression coefficient was 0.9993; the limit of detection (LOD) and the limit of quantification (LOQ) were 0.17 μg/mL and 0.57 μg/mL, respectively; the inter-day and intra-day accuracies were <6.44%; the recovery was in the range of 86.52–105.26%. The MOF-polymer monolithic column was successfully used as SPE column for enrichment and determination of UA in Chinese herbal medicine.

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Analytical Methods · 2019 ·Vol. 12 ·期 5 ·638-645 · IF 2.378

A functionalized multi-walled carbon nanotube-based composite monolith as a solid-phase extraction adsorbent for on-line purification and enrichment of ursolic acid in medicinal plants

Huan Yu,Haiyan Liu,Chunliu Yang,Xiaoya Pang,Miaomiao Zhang,Hongyuan Yan,Ligai Bai,Dandan Han

A novel poly(f-MWCNTs-co-ST-co-EDMA) monolith was prepared using functionalized multi-walled carbon nanotubes (MWCNTs) and styrene (ST) as comonomers and ethylene glycol dimethacrylate (EDMA) as the crosslinker. The surface morphology and internal structure of the monolith were determined by scanning electron microscopy (SEM), nitrogen adsorption–desorption isotherm and mercury intrusion porosimetry. The monolith possessed a homogeneous and continuous structure and large surface area. The monolith was used as the sorbent for on-line enrichment and purification of ursolic acid. The linear range was 0.0002–3.5 mg mL−1; the limit of detection (LOD) and the limit of quantitation (LOQ) were 0.52 μg mL−1 and 1.72 μg mL−1, respectively. The intra-day and inter-day precisions, which were expressed as the relative standard deviation (RSD), were no more than 0.76% and 1.51%, respectively. The recoveries were between 94.05% and 109.68% in several medicinal plants. The composite monolith showed low back pressure and high adsorption capacity for the enrichment and purification of ursolic acid.

CAS / MDL: 121-69-7 77-52-1
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Journal of Materials Chemistry B · 2023 ·Vol. 11 ·期 15 ·3453-3472 · IF 7

Combined chemo-immuno-photothermal therapy based on ursolic acid/astragaloside IV-loaded hyaluronic acid-modified polydopamine nanomedicine inhibiting the growth and metastasis of non-small cell lung cancer

Fan Xu,Minghua Li,Zujun Que,Mingliang Su,Wang Yao,Yu Zhang,Bin Luo,Yan Li,Zhanxia Zhang,Jianhui Tian

Combining chemotherapy and immunotherapy is a promising strategy for the treatment of non-small cell lung cancer (NSCLC) metastasis. However, platinum-based chemotherapeutics and immune checkpoint blockade-based cancer immunotherapy have toxic side effects and limitations. Ursolic acid (UA) and astragaloside IV (AS-IV) are natural compounds with anticancer activity sourced from Traditional Chinese medicine (TCM). However, their poor water solubilities and targeted deletions limit their medicinal value. In this study, we fabricated hyaluronic acid (HA)-modified UA/(AS-IV)-loaded polydopamine (PDA) nanomedicine (UA/(AS-IV)@PDA-HA) with a high yield at a low cost via simple synthesis. This represents a novel multifunctional nanomedicine that combines chemotherapy, photothermal therapy (PTT), and immunotherapy with an active tumor-targeting ability. The as-prepared nanomedicine not only increased the aqueous solubilities of UA and AS-IV, but also improved their active targeting abilities. HA binds specifically to the overexpressed cluster of differentiation 44 (CD44) on the surface of most cancer cells, thereby improving drug targeting. While evaluating the anticancer effect of UA/(AS-IV)@PDA-HA in vitro and in vivo, the PDA nanodelivery system significantly improved UA-mediated cytotoxicity and anti-metastatic ability against NSCLC cells. In addition, the system also improved the AS-IV-mediated self-immune response of tumor-related antigens, which further inhibited the growth and distant metastasis of NSCLC. Further, PDA nanomaterial-mediated PTT inhibited tumor growth substantially. UA/(AS-IV)@PDA-HA not only significantly eradicated the primary tumor but also strongly inhibited the distant metastasis of NSCLC in vitro and in vivo. Thus, it has immense potential for development as an efficient anti-metastatic agent for NSCLC.

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BIOMATERIALS · 2017 · IF 8.402

Simultaneous inhibition of growth and metastasis of hepatocellular carcinoma by co-delivery of ursolic acid and sorafenib using lactobionic acid modified and pH-sensitive chitosan-conjugated mesoporous silica nanocomplex

Ruirui Zhao,Tao Li,Guirong Zheng,Kai Jiang,Lulu Fan,Jingwei Shao

Co-delivery multiple drugs using nanocarriers has been recognized as a promising strategy for cancer treatment to enhance therapeutic efficacy. In this study, a pH sensitive mesoporous silica nanoparticles (MSN) based controlled release nanoparticles for co-delivery of sorafenib (SO), a multi-tyrosine kinase inhibitor, and ursolic acid (UA), a sensitive agent for SO, was developed, which was decorated with pH sensitive chitosan (CS) and lactobionic acid (LA) targeting to asialoglycoprotein receptor (ASGPR) over-expressing hepatocellar carcinoma cells (denoted as USMNs-CL). The nanocomplex enhanced bioavailability of hydrophobic drugs, efficient tumor cell targeting and exhibited pH-responsive function and sustained release profile. USMNs-CL showed synergistic cytotoxicity and could attenuate the adhesion, migration of ASGPR over-expressing liver cancer SMMC-7721 cells at non-toxic concentrations. Moreover, the complex nanoparticles significantly increased the cellular apoptosis and down-regulated the expression of EGFR and VEGFR2 proteins related with cell proliferation and tumor angiogenesis . In vivo , compared with UA or SO alone, the nanocomplex significantly reduced the tumor burden in hepatocellular carcinoma (HCC) H22 tumor-bearing mice model and inhibited the lung metastasis in the H22 lung metastasis models. Overall, co-delivery of UA and SO by MSN-CS-LA nanocarriers could provide a promising strategy for HCC combinational therapy, especially for the HCC metastasis chemoprevention.

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Oncotarget · 2016 · IF 5.008

A novel co-drug of aspirin and ursolic acid interrupts adhesion, invasion and migration of cancer cells to vascular endothelium via regulating EMT and EGFR-mediated signaling pathways: multiple targets for cancer metastasis prevention and treatment

Qiao Tang,Yajun Liu,Tao Li,Xiang Yang,Guirong Zheng,Hongning Chen,Lee Jia,Jingwei Shao

Metastasis currently remains the predominant cause of breast carcinoma treatment failure. The effective targeting of metastasis-related-pathways in cancer holds promise for a new generation of therapeutics. In this study, we developed an novel Asp-UA conjugate, which was composed of classical “old drug” aspirin and low toxicity natural product ursolic acid for targeting breast cancer metastasis. Our results showed that Asp-UA could attenuate the adhesion, migration and invasion of breast cancer MCF-7 and MDA-MB-231 cells in a more safe and effective manner in vitro . Molecular and cellular study demonstrated that Asp-UA significantly down-regulated the expression of cell adhesion and invasion molecules including integrin α6β1, CD44, MMP-2, MMP-9, COX-2, EGFR and ERK proteins, and up-regulated the epithelial markers “E-cadherin” and “β-catenin”, and PTEN proteins. Furthermore, Asp-UA (80 mg/kg) reduced lung metastasis in a 4T1 murine breast cancer metastasis model more efficiently, which was associated with a decrease in the expression of CD44. More importantly, we did not detect side effects with Asp-UA in mice such as weight loss and main viscera tissues toxicity. Overall, our research suggested that co-drug Asp-UA possessed potential metastasis chemoprevention abilities via influencing EMT and EGFR-mediated pathways and could be a more promising drug candidate for the prevention and/or treatment of breast cancer metastasis.

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