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Frontiers of Chemical Science and Engineering 2023年第12期17卷 2101-2113页

作者： Yihong Yang Siyue Ma Ting Li Jingjing He Shitao Liu Hongwu Liu Jiaojiao Zhang Xiang Zhou Liwei Liu Song Yang National Key Laboratory of Green Pesticide Key Laboratory of Green Pesticide and Agricultural Bioengineering(Ministry of Education)Center for R&D of Fine Chemicals of Guizhou UniversityGuiyang 550025China

In response to the reduction of food production and economic losses caused by plant bacterial diseases, it is necessary to develop new, efficient, and green pesticides. Natural products are rich and sustainable source for the development of new pesticides due to their low toxicity, easy degradation, and eco-friendliness. In this study, we prepared three series of Ursolic acid derivatives and assessed their antibacterial ability. Most target compounds exhibited outstanding antibacterial activities. Among them, the relative optimal EC50 values of Xanthomonas oryzae pv. oryzae and Xanthomonas axonopodis pv. citri were 2.23 (A17) and 1.39 (A16) μg·mL^(-1), respectively. The antimicrobial mechanism showed that compound A17 induced an excessive accumulation and production of reactive oxygen species in bacteria and damaged the cell membrane integrity to kill bacteria. More interestingly, the addition of low concentrations of exogenous hydrogen peroxide enhanced the antibacterial efficacy of compound A17 against Xanthomonas oryzae pv. oryzae. These entertaining results suggested that compound A17 induced an apparent apoptotic behavior in the tested bacteria. Overall, we developed the promising antimicrobial agents that destroyed the redox system of phytopathogenic bacteria, further demonstrating the unprecedented potential of Ursolic acid for agricultural applications.

关键词： Ursolic acid antibacterial activities reactive oxygen species apoptosis

Design,synthesis and biological evaluation of fluorescent derivatives of Ursolic acid in living cells

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Chinese Chemical Letters 2024年第5期35卷 287-289页

作者： Wenyi Mei Lijuan Xie Xiaodong Zhang Cunjian Shi Fengzhi Wang Qiqi Fu Zhenjiang Zhao Honglin Li Yufang Xu Zhuo Chen Shanghai Key Laboratory of New Drug Design State Key Laboratory of Bioreactor EngineeringSchool of PharmacyEast China University of Science and TechnologyShanghai 200237China Innovation Center for AI and Drug Discovery East China Normal UniversityShanghai 200062China Lingang Laboratory Shanghai 200031China

Ursolic acid(UA)is a naturally occurring ursane triterpenoid,which exhibits a wide range of unique biological activities.To clarify its mechanism of action(MOA),a series of fluorescent derivatives of UA(5a-c)were designed and synthesized by conjugation with 7-nitrobenzo-2-oxa-1,3-diazole(NBD)fluorophore.Among them,5c exhibited similar anti-proliferative activity with UA against HCT116 cells(half maximal inhibitory concentration(IC_(50))=9.21±0.50μmol/L).Cell imaging experiment indicated that 5c was rapidly taken up in HCT116 cells in a dose and time-dependent manner.Then,5c was found to localize in endoplasmic reticulum(ER),lysosomes,and mitochondria,but not in nucleus of HCT116 cells by confocal microscopy studies.Preliminary MOA proved that UA induced autophagy with a unique intracellular distribution mechanism involving ER and lysosome.In all,our work provides new clues for revealing the molecular mechanism of UA as an antitumor agent.

关键词： Pentacyclic triterpenoid Ursolic acid Fluorescent derivatives Autophagy Apoptosis

Evolution from small molecule to nano-drug delivery systems:An emerging approach for cancer therapy of Ursolic acid

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Asian Journal of Pharmaceutical Sciences 2020年第6期15卷 685-700页

作者： Jingwei Shao Yifan Fang Ruirui Zhao Fangmin Chen Mingyue Yang Jiali Jiang Zixuan Chen Xiaotian Yuan Lee Jia Cancer Metastasis Alert and Prevention Center and Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and ChemotherapyCollege of ChemistryFuzhou UniversityFuzhou 350116China Marine Drug R&D Center Institute of OceanographyMinjiang UniversityFuzhou 350108China

Ursolic acid(UA),a natural pentacyclic triterpenoid,possesses widespread biological and pharmacological activities.However,drawbacks such as low bioavailability,poor targeting and rapid metabolism greatly hinder its further clinical application.Recently,with the development of nanotechnology,various UA nanosystems have emerged as promising strategies for effective cancer therapy.This article reviews various types of UA-based nanodelivery systems,primarily with emphasis placed on novel UA-based carrier-free nanodrugs,which are considered to be innovative methods for cancer therapy.Moreover,this review presents carrier-free nano-drugs that co-assembled of UA and photosensitizers that displayed synergistic antitumor performance.Finally,the article also describes the development and challenges of UA nanosystems for future research in this field.Overall,the information presented in this review will provide new insight into the rational utilization of nano-drugs in cancer therapy.

关键词： Ursolic acid Nanosytems Carrier-free Photosensitizer Anticancer

Synthesis,Crystal Structures and Cytotoxic Activities of Two New Pyrimidine Derivatives of Ursolic acid

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Chinese Journal of Structural Chemistry 2021年第2期40卷 239-245,148页

作者：王文燕李阿良刘青松孙月谷文 Jiangsu Provincial Key Lab for the Chemistry and Utilization of Agro-forest Biomass Jiangsu Key Lab of Biomass-based Green Fuels and ChemicalsCo-innovation Center for Efficient Processing and Utilization of Forest ProductsCollege of Chemical EngineeringNanjing Forestry UniversityNanjing 210037China

The title compounds(5a and 5b)were synthesized from Ursolic acid and their structures were characterized by spectroscopic methods including ESI-MS,^(1)H-NMR,^(13)C-NMR and elemental analysis.The crystal structures of compounds 5a and 5b were determined by single-crystal X-ray diffraction analysis.Compound 5a crystallizes in monoclinic system,P21 space group with a=12.258(3),b=10.396(2),c=15.570(3)Å,b=107.21(3)°,Z=2,V=1895.3(7)Å^(3),Mr=659.90,Dc=1.156 Mg/m^(3),S=1.003,µ=0.076 mm^(−1),F(000)=716,the final R=0.0686 and wR=0.1430 for 1859 observed reflections(I>2σ(I)).Compound 5b crystallizes in monoclinic system,P21 space group with a=12.371(3),b=10.647(2),c=15.722(3)Å,b=109.44(3)°,Z=2,V=1952.8(8)Å^(3),M_(r)=655.93,D_(c)=1.116 Mg/m^(3),S=1.002,µ=0.069 mm^(−1),F(000)=716,the final R=0.0686 and wR=0.1882 for 2574 observed reflections(I>2σ(I)).The preliminary cytotoxic assay indicated that compound 5b exhibited notable cytotoxic activity against MCF-7 and HeLa cells with the IC_(50)values of 10.71±0.23 and 12.63±0.31μM,respectively.

关键词： Ursolic acid pyrimidine crystal structure cytotoxic activity

Host-guest interaction of β-cyclodextrin with isomeric Ursolic acid and oleanolic acid:physicochemical characterization and molecular modeling study

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The Journal of Biomedical Research 2017年第5期31卷 395-407页

作者： Yuan Huang Peng Quan Yongwei Wang Dongsheng Zhang Mingwan Zhang Rui Li Nan Jiang Department of Pharmacy Affiliated Wuxi Peoples HospitalNanjing Medical University Department of Pharmaceutical Sciences Shenyang Pharmaceutical University School of Pharmacy Nanjing Medical University Department of Colorectal Surgery The First Affiliated Hospital of Nanjing Medical University

Ursolic acid(UA) and oleanolic acid(OA) are insoluble drugs. The objective of this study was to encapsulate them into β-cyclodextrin(β-CD) and compare the solubility and intermolecular force of β-CD with the two isomeric triterpenic acids. The host-guest interaction was explored in liquid and solid state by ultraviolet-visible absorption,1H NMR, phase solubility analysis, and differential scanning calorimetry, X-ray powder diffractometry, and molecular modeling studies. Both experimental and theoretical studies revealed that β-CD formed 1: 1 water soluble inclusion complexes and the complexation process was naturally favorable. In addition, the overall results suggested that ring E with a carboxyl group of the drug was encapsulated into the hydrophobic CD nanocavity. Therefore, a clear different inclusion behavior was observed, and UA exhibited better affinity to β-CD compared with OA in various media due to little steric interference, which was beneficial to form stable inclusion complex with β-CD and increase its water solubility effectively.

关键词： β-cyclodextrin oleanolic acid Ursolic acid host-guest interaction molecular modeling

Ursolic acid synergistically enhances the therapeutic effects of oxaliplatin in colorectal cancer

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Protein & Cell 2016年第8期7卷 571-585页

作者： Jianzhen Shan Yanyan Xuan QiZhang Chunpeng Zhu Zhen Liu Suzhan Zhang Department of Medical Oncology The Second Affiliated Hospital Zhejiang University School of Medicine Hangzhou 310009 China Cancer Institute of Zhejiang University School of Medicine Hangzhou 310009 China Department of Hepatobiliary and Pancreatic Surgery The Second Affiliated Hospital Zhejiang University School of Medicine Hangzhou 310009 China Department of Gastroenterology The Second Affiliated Hospital Zhejiang University School of Medicine Hangzhou 310009 China

Oxaliplatin is a key drug in chemotherapy of colorectal cancer （CRC）. However, its efficacy is unsatisfied due to drug resistance of cancer ceils. In this study, we tested whether a natural agent, Ursolic acid, was able to enhance the efficacy of oxaliplatin for CRC. Four CRC cell lines including SW480, SW620, LoVo, and RKO were used as in vitro models, and a SW620 xenograft mouse model was used in further in vivo study. We found that Ursolic acid inhibited proliferation and induced apoptosis of all four cells and enhanced the cytotoxicity of oxaliplatin. This effect was associated with down-regulation of Bcl-xL, Bcl-2, survivin, activation of caspase-3, 8, 9, and inhibition of KRAS expression and BRAF, MEKll2, ERK1/2, p-38, JNK, AKT, IKKa, IKBa, and p65 phosphorylation of the MAPK, PI3K/AKT, and NF-KB signaling pathways. The two agents also showed synergistic effects against tumor growth in vivo. In addition, Ursolic acid restored liver function and body weight of the mice treated with oxaliplatin. Thus, we concluded that Ursolic acid could enhance the therapeutic effects of oxaliplatin against CRC both in vitro and in vivo, which offers an effective strategy to minimize the burden of oxaliplatin-induced adverse events and provides the groundwork for a new clinical strategy to treat CRC.

关键词： Ursolic acid colorectal cancer oxaliplatin,signaling pathways

Ursolic acid induces neural regeneration after sciatic nerve injury

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Neural Regeneration Research 2013年第27期8卷 2510-2519页

作者： Biao Liu Yan Liu Guang Yang Zemin Xu Jiajun Chen Department of Hand Surgery China-Japan Union Hospital of Jilin University Department of Neurology China-Japan Union Hospital of Jilin University

In this study, we aimed to explore the role of Ursolic acid in the neural regeneration of the injured sciatic nerve. BALB/c mice were used to establish models of sciatic nerve injury through unilateral sciatic nerve complete transection and microscopic anastomosis at 0.5 cm below the ischial tuber-osity. The successful y generated model mice were treated with 10, 5, or 2.5 mg/kg Ursolic acid via intraperitoneal injection. Enzyme-linked immunosorbent assay results showed that serum S100 protein expression level gradual y increased at 1-4 weeks after sciatic nerve injury, and significantly decreased at 8 weeks. As such, Ursolic acid has the capacity to significantly increase S100 protein expression levels. Real-time quantitative PCR showed that S100 mRNA expression in the L 4-6 segments on the injury side was increased after Ursolic acid treatment. In addition, the muscular mass index in the soleus muscle was also increased in mice treated with Ursolic acid. Toluidine blue staining revealed that the quantity and average diameter of myelinated nerve fibers in the injured sciatic nerve were significantly increased after treatment with Ursolic acid. 10 and 5 mg/kg of Ursolic acid produced stronger effects than 2.5 mg/kg of Ursolic acid. Our findings indicate that Ursolic acid can dose-dependently increase S100 expression and promote neural regeneration in BALB/c mice fol owing sciatic nerve injury.

关键词： neural regeneration traditional Chinese medicine Ursolic acid triterpenoid sciatic nerve peripheralnerve injury S100 muscular atrophy nerve myelin sheath grants-supported paper neuroregeneration

Research Progress of Ursolic acid's Anti-Tumor Actions

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Chinese Journal of Integrative Medicine 2014年第1期20卷 72-79页

作者：臧丽丽吴宝宁林原王军傅雷唐泽耀 Pharmacology Department Dalian Medical University Medicine Department Dalian Third People's Hospital

Ursolic acid（UA）is a sort of pentacyclic triterpenoid carboxylic acid purified from natural plant.UA has a series of biological effects such as sedative,anti-inflammatory,anti-bacterial,anti-diabetic,antiulcer,etc.It is discovered that UA has a broad-spectrum anti-tumor effect in recent years,which has attracted more and more scholars’attention.This review explained anti-tumor actions of UA,including（1）the protection of cells’DNA from different damages;（2）the anti-tumor cell proliferation by the inhibition of epidermal growth factor receptor/mitogen-activated protein kinase signal or of FoxM1 transcription factors,respectively;（3）antiangiogenesis,（4）the immunological surveillance to tumors;（5）the inhibition of tumor cell migration and invasion;（6）the effect of UA on caspase,cytochromes C,nuclear factor kappa B,cyclooxygenase,tumor necrosis factor-related apoptosis-inducing ligand（TRAIL）or mammalian target of rapamycin signal to induce tumor cell apoptosis respectively,and etc.Moreover,UA has selective toxicity to tumor cells,basically no effect on normal cells.With further studies,UA would be one of the potential anti-tumor agents.

关键词： Ursolic acid anti-tumor research progress

Transcriptome sequencing analysis of Ursolic acid-mediated proliferation suppression on cutaneous T-cell lymphoma cells

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Traditional Medicine Research 2023年第2期8卷 36-44页

作者： Cheng Wang Peng-Cheng Ma Bao-Le Cai Hong-Yang Li Ling-Jun Li Pharmacal Research Laboratory Jiangsu Key Laboratory of Molecular Biology for Skin Diseases and STIsInstitute of DermatologyChinese Academy of Medical SciencesPeking Union Medical CollegeNanjing 210042China Department of Dermatology Zhongda Hospital Southeast UniverstiyNanjing 210009China

Background:Ursolic acid is a triterpenoid compound found in natural plants that exhibits antiproliferative effects in various cancer cells.Our study is the first to demonstrate the strong inhibitory effects of Ursolic acid on the proliferation of cutaneous T-cell lymphoma(CTCL)cells.We aimed to further investigate the underlying mechanism of the proliferation inhibition induced by Ursolic acid in CTCL cells using transcriptome sequencing.Methods:Cell counting kit-8 assays were used to observe the effects of six traditional medicine monomers on the proliferation of CTCL cells.Transcriptome sequencing was used to identify differentially expressed genes after Ursolic acid treatment.Bioinformatics analysis was performed to determine the potential mechanism.Real-time quantitative PCR and western blotting analyses were performed to confirm the sequencing results and verify the possible mechanisms of Ursolic acid-mediated proliferation inhibition in CTCL cells.Results:Ursolic acid exhibited the strongest inhibitory effect on the proliferation of CTCL cells among the six traditional medicine monomers.Transcriptome sequencing analysis showed that 2,466 genes were significantly altered.Combined with Kyoto Encyclopedia of Genes and Genomes functional enrichment analysis and protein-protein interaction network analysis,the interaction of various pathways and signaling molecules,such as tumor necrosis factor-α,NLR family pyrin domain containing 1,c-Jun N-terminal kinase,and melanoma differentiation-associated gene 5,accounted for the anti-tumor effects of Ursolic acid in CTCL cells.Conclusion:Ursolic acid significantly inhibited the proliferation of CTCL cells,and our study laid a theoretical foundation for the future treatment of CTCL using Ursolic acid.

关键词： Ursolic acid cutaneous T-cell lymphoma transcriptome sequencing proliferation apoptosis

Ursolic acid Inhibits T-Cell Activation through Modulating Nuclear Factor-κB Signaling

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Chinese Journal of Integrative Medicine 2012年第1期18卷 34-39页

作者：曾光陈疆梁清华游万辉吴汉军熊新贵 Institute of Integrative Medicine Xiangya HospitalCentral South University Telemedicine Centre Xiangya HospitalCentral South University

Objective： To investigate the effects of Ursolic acid （UA） on T-cell proliferation and activation, as well as to examine its effect on nuclear factor- κ B （NF- κ B） signaling pathway in T cells. Methods： T-cells isolated from BALB/c mice were incubated with UA at concentrations ranging from 5-30μmol/L in the presence of phorbol 12-myristate 13-acetate （PMA） or PMA plus ionomycin. The proliferation of T cells was measured by the MIF assay. The expressions of CD69, CD25, and CD71 on T-cell surface were analyzed using flow cytometry. The level of interleukin-2 （IL-2） in the culture supernatant of activated T cells was quantified by enzyme-linked immunosorbent assay （ELISA）. The level of phosphorylated I κ B-α （p-I κ B-α ） in total protein and p65, a subunit of NF- κ B, nuclear translocation were measured by Western blot analysis. Results： UA in a dose-dependent manner significantly decreased the proliferation and inhibited the surface expressions of CD69, CD25, and CD71 in murine T lymphocytes upon in vitro activation （P〈0.01）. Significant reduction of IL-2 production was found in activated T cells treated with UA （P〈0.01）. The PMA-induced increase in p-I κ B-α protein was inhibited, and nuclear translocation of p65 from the cytoplasm was blocked by UA. Conclusion： UA is a potent inhibitor for T cell activation and proliferation; these effects are associated with the inhibition of NF- κ B signaling pathway.

关键词： Ursolic acid T-cell activation CD69 CD25 CD71 nuclear factor- κ B