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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

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

Combined Antitumor Effect of ursolic acid And 5-Fluorouracil on Human Esophageal Carcinoma Cell Eca-109 In Vitro

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Chinese Journal of Cancer Research 2010年第1期22卷 62-67页

作者： Guo-qing Chen Zhen-wei Yao Wei-ping Zheng Li Chen Hong Duan Yi Shen Research Center of Tissue Engineering and Stem cell Department of Pathophysiology Chongqing Medical University Chongqing 400016 China Department of Obsttrics and Gynecology the First Affiliated Hospital Chongqing Medical University Chongqing 400016 China

Objective： To study the combined antitumor effect and possible mechanisms of ursolic acid with 5-fluorouracil （5-FU） on human esophageal carcinoma cell Eca-109 in vitro. Methods： Eca-109 cells were treated with ursolic acid （10-50 μmol/L） and/or 5-fluorouracil （48.0-768.8 μmol/L） for 48 h in vitro. And then cell proliferation was determined by MTT assay. Cell cycle and apoptosis rate were analyzed by flow cytometry （FCM）. The morphological changes of apoptosis were observed by fluorescent microscopy. At last the expression of P27kipl, bcl-2 and bax were detected by western blot. Results： Results： In comparison with single agent treatment, the combination of ursolic acid and 5-fluorouracil produced greater efficacy in growth inhibition, cell cycle arrest at G0/G1 phase, and apoptosis induction （P〈0.05）. Western blot analysis showed that the combination use of ursolic acid and 5-fluorouracil suppressed the expression of bcl-2 and increased the expressions of bax and P27kip1. Conclusion： ursolic acid combined with 5-fluorouracil showed adjuvant antiproliferative effects on human esophageal carcinoma cell Eca-109 in vitro, which mainly due to the induction of cell cycle arrest as well as apoptosis.

关键词： ursolic acid 5-fluorouracil Eca-109 cells Apoptosis Cell cycle P27kip1

Anti-tumor Effect and Its Mechanisms of ursolic acid on Human Esophageal Carcinoma Cell Eca-109 in Vivo

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Chinese Journal of Cancer Research 2008年第3期20卷 205-210页

作者：陈国庆沈宜段红 Department of Pathophysiology Chongqing University of Medical Sciences Chongqing 400016 China

Objective： To investigate the anti-tumor effect and possible mechanisms of ursolic acid on human esophageal carcinoma in vivo. Methods： Atransplanted tumor model by injecting Eca-109 cells into subcutaneous tissue of BALB/c nude mice was established. 40 nude mice bearing tumors were randomly divided into 4 groups and 0.2 ml saline or 0.2 ml ursolic acid （25-100 mg·kg^-1·d^-1） was injected into abdominal cavity respectively once everyday and lasted for fourteen days. The changes of tumor volume were measured continuously and tumor inhibition rate was calculated. The morphological changes of apoptosis were observed by electron microscope. The expressions of COX-2, bcl-2 and Bax protein in transplanted tumors were detected by immunohistochemistry. At last the PGE2 level of transplanted tumors was detected byradioimmunoassay. Results： Treatment of nude mice with 25, 50, or 100 mg·kg^-1·d^-1 of ursolic acid significantly inhibited the growth of the human esophageal carcinoma tumor in nude mice and induced Eca-109 cells apoptosis as demonstrated by electron microscopy analyses. The expressions of COX-2 and bcl-2 in the transplanted tumors were decreased in ursolic acid groups, while the Bax increased. The PGE2 level of transplanted tumors was decreased in ursolic acid groups with adose-relatedmanner. Conclusion： ursolic acid has anti-tumor effects against human esophageal carcinoma cells in vivo, which are likely mediated via induction of tumor cell apoptosis and inhibition of COX-2 and PGE2.

关键词： ursolic acid Esophageal carcinoma Apoptosis COX-2 PGE2

Synthesis and Anti-tumor Activity of Novel Amide Derivatives of ursolic acid

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Chemical Research in Chinese Universities 2008年第1期24卷 42-46页

作者： LIU Dan MENG Yan-qiu ZHAO Juan CHEN Li-gong College of Pharmaceuticals ＆ Biotechnology Tianjin University Tianjin 300072 P. R. China Faculty of Pharmaceutical Engineering Shenyang Institute of Chemical Technology Shenyang 110142 P. R. China

ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, ^1H NMR and MS. Cell growth inhibitory effects of the derivatives against Hela cell were evaluated by MTT assay. All these derivatives were found to have stronger cell growth inhibitory than their parent compound, ursolic acid. The derivatives with a substituted acetyl group at C3 hydroxyl group show better activities than those with an unsubstituted hydroxyl group.

关键词： ursolic acid Amide derivatives Anti-tumor activity

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

ursolic acid ameliorates azoxymethane/dextran sulfate sodium-caused colorectal cancer by inhibition of Wnt signaling cascade

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中国药理学与毒理学杂志 2021年第10期35卷 780-781页

作者： ZHAO Hui SUN Qiang ZENG Sha CHEN Li LIU Mao-lun REN Shan YANG Han MING Tian-qi TAO Qiu LU Jin-jian XU Hai-bo State Key Laboratory of Southwestern Chinese Medicine Resources Department of PharmacologyChengdu University of Traditional Chinese MedicineChengdu 611137China Institute of Chinese Medical Sciences University of MacaoMacaoChina

OBJECTIVE To investigate the pharmacological effect of ursolic acid(UA)on colitis-associated colorectal cancer(CAC)and its underlying mechanism based on the Wnt signaling pathway.METHODS The CAC model in mice was established by azoxymethane(AOM)combined and dextran sulfate sodium salt(DSS),accompanied by treatment with various dosages of UA and concomitant appraisal of body weight,stool and physical state of the mice.After the sacrifice of the mice,the tumor and length of the colorectum were measured,followed by retrieval of the liver,spleen,thymus and tumor tissue for downstream assays.The levels of inflammatory factors interleukin-6(IL-6),IL^(-1)βand C-reactive protein(CRP)in the tumor and serum were examined by enzyme-linked immunosorbent assay(ELISA).The pathological changes of colorectal tissues were observed by HE staining.The levels in tumors of Wnt/β-catenin signaling pathway-related proteins Wnt4,GSK-3β,β-catenin,TCF4,LEF1,c-Myc,cyclin D1 and apoptosis-related protein Bcl-2 were assayed by immunohistochemistry(IHC).The mRNA expressions of Wnt4,GSK-3β,β-catenin,TCF4,LEF1,c-Myc,cyclin D1,Bcl-2,Bax,caspase-9 and caspase-3 in tumors were detected by real-time quantitative RT-PCR(RT-qPCR).The protein levels of Wnt4,GSK-3β,β-catenin,TCF4,LEF1,c-Myc,cyclin D1,phospho-β-catenin,phospho-GSK-3β,Bcl-2 and Bax in tumors were probed by analyzed by Western blotting(WB).Also,RNA-seq was employed to assess the gut microbiota in the mice.RESULTS UA significantly ameliorated the symptoms of AOM/DSS-induced mouse CAC,evidenced by improved physical state,body weight,survival rate,colorectal length,the mass of liver,thymus,spleen,and decreased CAC load and colorectal mass.UA attenuated the levels of IL-6,IL^(-1)βand CRP in the mouse serum and colorectal tumor in a dose-dependent manner.HE staining showed that UA lessened carcinogenesis in the colorectum,with lower infiltration of lymphocytes,versus the control.IHC indicated that UA mitigated the expression of Wnt4,β-catenin,TCF4,LEF1,c-Myc,cyclin D1,Bcl-2,and promoted the GS

关键词： ursolic acid colitis associated cancer Wnt/β-catenin signaling pathway

Pharmacological research progress of ursolic acid for the treatment of liver diseases

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Traditional Medicine Research 2021年第4期6卷 125-135页

作者： Yu Liang Qian-Qian Niu Yuan-Hong Zhao First Teaching Hospital of Tianjin University of Traditional Chinese Medicine Tianjin 300381China National Clinical Research for Chinese Medicine Acupuncture and Moxibustion Tianjin 300381China

ursolic acid is a natural pentacyclic triterpenoid with various pharmacological activities such as anti-inflammatory,hepatoprotective,antitumor,and hypoglycemic activity.This natural product is widely present in many common Chinese herbal medicines such as Hedyotis diffusa and Prunella vulgaris.The present review highlights the pharmacological research progress of ursolic acid in liver disease,with a focus on providing directions for future research and clinical practice of ursolic acid.Modern studies have demonstrated that ursolic acid can adjust the activities of enzymes such as superoxide dismutase and NADPH oxidase to balance oxidative stress,reduce inflammation,as well as to repair damaged liver.Research also showed that ursolic acid targeted lipid metabolic genes,activating autophagy and reducing lipid deposition in hepatocytes,further preventing the progress of fatty liver.Besides,the combination of ursolic acid with caspase-3 was able to prevent apoptosis and relieve liver injury.Furthermore,ursolic acid was showed to target the intestine by alleviating mucosal injury and restoring the balance of the intestinal microecology and protect liver through the enterohepatic axis.In terms of antitumor activity,ursolic acid targeted several tumor suppressor genes including gene of phosphate and tension homology deleted on chromsome ten and p53,and affected the expression of cyclin and apoptosis-related proteins involving Bax,Bcl-2,and Bcl-x,which acted on signal transduction pathways including phosphatidylinositol-3-kinase/protein kinase B,extracellular regulated protein kinases and proteina fosforilata 21 wide-type actiated factorlp 1.The same compound interacted with caspases,resulting in inhibition of cell proliferation and induction of apoptosis.In addition,ursolic acid also exerted anticancer activity through inhibiting angiogenesis,tumor invasion and metastasis,and improving immunity.Other studies have noted the importance of nano-preparations of ursolic acid for its clinical applications.This review provide

关键词： Liver cancer Liver fibrosis Liver injury Liver protection Pharmacological mechanism ursolic acid

Phytochemicals in diets for breast cancer prevention:The importance of resveratrol and ursolic acid

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Food Science and Human Wellness 2012年第1期1卷 1-13,I0002页

作者： Rahul Venugopal Rui Hai Liu Department of Food Science Cornell UniversityIthacaNY 14853-7201USA Institute of Comparative and Environmental Toxicology Stocking HallCornell UniversityIthacaNY 14853USA

Breast cancer is the second leading cause of death from cancer in women in the United States.A growing emphasis is being placed on alternative medicine and dietary approaches toward prevention of potential diseases.Phytochemicals are bioactive compounds that are naturally present in foods that,when acting in synergy,bestow potential anti-cancer properties.Resveratrol,a phytoalexin,and ursolic acid,a pentacyclic triterpenoid,are two bioactive compounds that are at the forefront in scientific research.Previous animal studies have documented the anti-cancer properties of resveratrol on breast cancer cells and research groups have recently been able to identify the anti-cancer,anti-inflammatory and induction of apoptosis properties of resveratrol along with the signal transduction pathways that the compound affects.ursolic acid has been cast into the limelight with the recent discovery documenting its anti-inflammation and anti-cancer activities by targeting signal pathways,especially in the prevention of breast cancer.©2012 Production and hosting by Elsevier B.V.on behalf of Beijing Academy of Food Sciences.

关键词： Phytochemicals Cancer Resveratrol ursolic acid Diet and cancer