Analytical Methods
·
2013
·Vol. 5
·期 19
·5227-5233
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IF 1.855
Sha Peng,Jing Cheng,Miao Zhang,Mi Chen,Hongbin Zhou,Min Cheng
A very simple and effective method for the extraction and determination of oleanolic acid (OA) and ursolic acid (UA) in Radix Actinidiae chinensis was developed using ultrasound-assisted dispersive liquid–liquid microextraction (UA-DLLME) and high performance liquid chromatography–mass spectrometry (HPLC–MS). Ethanol was used as the solvent to extract OA and UA from Radix Actinidiae chinensis, assisted by ultrasonic waves. When the extraction process was finished, the two target analytes in the extraction solvent were rapidly transferred from the ethanol extract to another extraction solvent (chloroform) with the help of a dispersive solvent (tetrahydrofuran) by using DLLME. A series of extraction parameters were investigated and optimized. Under the most favorable conditions, the limits of detection (LOD, S/N = 3) and enrichment factors were 2.0 ng g−1, 89.4 and 6.0 ng g−1, 84.5 for OA and UA, respectively. The recoveries of the spiked sample solutions at three different concentration levels of 200, 500 and 1000 ng g−1 ranged between 88.2 and 96.6%. The proposed method was the first successfully applied for the extraction and determination of OA and UA in Radix Actinidiae chinensis.
研究领域:
药学
·
分析化学
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高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2019
·Vol. 28
·期 6
·892-899
·
IF 1.72
Sun Li,Chu Xiang-Wu,Liu Chun-mei,Sheng Li-Xin,Chen Zhuan-Xin,Cheng Ke-Guang
As pharmacophore hybridization has been used frequently in the discovery of new drugs, ursolic acid/glycyrrhetinic acid-uracil/thymine hybrids have been synthesized and evaluated their antiproliferative activity by the MTT assay. The results displayed that, the hybrids of glycyrrhetinic acid ( 7a – 7b to 10a – 10b ) exhibited slightly better antiproliferative activity than that of ursolic acid hybrids ( 3a – 3b to 6a – 6b ). Two single glycyrrhetinic acid-thymine hybrids ( 8a and 10a ) possessed good antiproliferative activity against tested A549 cell line (IC 50 = 10.7 and 18.3 µM, respectively). And three hybrids ( 3a , 5a , and 10b ) exhibited about 80% inhibitory ratio against tested Hela cell line.
研究领域:
药物化学
·
肿瘤学
·
分子生物学
·
药理学
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Pharmaceutics
·
2025
·Vol. 17
·期 10
·1297
·
IF 5.5
Guang Li,Wenyu Yuan,Yu Ying,Yang Zhang
Background/Objectives: Pharmaceutical preparation technologies can enhance the bioavailability of poorly water-soluble drugs. Ursolic acid (UA) has been found to possess anti-cancer and hepatoprotective properties, demonstrating its potential as a therapeutic agent; however, its hydrophobicity and low solubility present challenges in the development of drug formulations. This study investigates the preparation of a nano-UA suspension by wet grinding, researches the influence of process parameters on particle size, and explores the rules of particle breakage and agglomeration by combining model fitting.Methods: Wet grinding experiments were conducted using a laboratory-scale grinding machine. The particle size distributions (PSDs) of UA suspensions under different grinding conditions were measured using a laser particle size analyzer. A single-factor experimental design was employed to optimize operational conditions. Model parameters for a population balance model considering both breakage and agglomeration were determined by an evolutionary algorithm optimization method. By measuring the degree to which UA inhibits the colorimetric reaction between salicylic acid and hydroxyl radicals, its antioxidant capacity in scavenging hydroxyl radicals was indirectly evaluated.Results: Wet grinding process conditions for nano-UA particles were established, yielding a UA suspension with a D50 particle size of 122 nm. The scavenging rate of the final grinding product was improved to three times higher than that of the UA raw material (D50 = 14.2 μm).Conclusions: Preparing nano-UA suspensions via wet grinding technology can significantly enhance their antioxidant properties. Model regression analysis of PSD data reveals that increasing the grinding mill’s stirring speed leads to more uniform particle size distribution, indicating that grinding speed (power) is a critical factor in producing nanosuspensions.
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PubMed
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Food & Function
·
2020
·Vol. 11
·期 7
·6091-6103
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IF 4.171
Wangjun Hao,Erika Kwek,Zouyan He,Hanyue Zhu,Jianhui Liu,Yimin Zhao,Ka Ying Ma,Wen-Sen He,Zhen-Yu Chen
Ursolic acid (UA) is a triterpenoid acid widely abundant in fruits and vegetables such as apple, blueberry and cranberry. The present study was carried out to investigate the effect of UA supplementation in diet on blood cholesterol, intestinal cholesterol absorption and gut microbiota in hypercholesterolemic hamsters. A total of thirty-two hamsters were randomly assigned to four groups and given a non-cholesterol diet (NCD), a high-cholesterol diet containing 0.1% cholesterol (HCD), an HCD diet containing 0.2% UA (UAL), or an HCD diet containing 0.4% UA (UAH) for 6 weeks. Results showed that UA supplementation reduced plasma cholesterol by 15–16% and inhibited intestinal cholesterol absorption by 2.6–9.2%. The in vitro micellar cholesterol solubility experiment clearly demonstrated that UA could displace 40% cholesterol from micelles. In addition, UA decreased the ratio of Firmicutes to Bacteroidetes, whereas it enhanced the growth of short chain fatty acid (SCFA)-producing bacteria in the intestine. In conclusion, UA possessed a cholesterol-lowering activity and could favorably modulate the gut microbiota.
研究领域:
营养学
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药理学
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微生物学
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代谢学
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DOI
PubMed
高影响因子
VIRUS RESEARCH
·
2022
·
IF 6.286
Bo-Yang Li,Jia-Cheng Qin,Yu-Feng Shen,Fei Yang,Tao Wang,Fei Ling,Gao-Xue Wang
Micropterus salmoides rhabdovirus (MSRV) has a high mortality rate and causes huge economic losses to the aquaculture industry. In this study, we identified that ursolic acid (UA) had antiviral efficacy against MSRV in vitro and in vivo . The results showed that UA inhibited MSRV replication in grass carp ovary (GCO) cells with a half-maximal inhibitory concentration (IC 50 ) of 5.55 μM, reduced viral titers and decreased cytopathic effects (CPE). Mechanistically, UA does not directly damage viral particles. On the other hand, UA inhibits MSRV replication by altering viral binding and release. Furthermore, pre- and post-treatment assays revealed that UA had preventive and therapeutic effects. For in vivo studies, UA could enhance the survival rate of MSRV-infected largemouth bass. Similarly, UA reduced the viral load of MSRV in the heart, spleen and brain at 3, 5 and 7 d post-infection. In conclusion, UA is an effective inhibitor of rhabdovirus in aquaculture.
研究领域:
水产养殖学
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病毒学
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药理学
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PubMed
高影响因子
DRUG DELIVERY
·
2019
·
IF 3.829
Weijie Li,Ruicong Yan,Yong Liu,Chuanchuan He,Xiaojuan Zhang,Yao Lu,Muhammad Waseem Khan,Chuanrui Xu,Tan Yang,Guangya Xiang
Overexpression of Bmi1 gene is an important feature of cancer stem cell in various human tumors. Therefore, Bmi1 gene can be a potential target for small interfering RNA (siRNA) mediated cancer therapy. Ursolic acid (UA) as a natural product plays a pivotal role in anti-tumor field, although its performance is limited by low bioavailability and poor hydrophilicity. A folate receptor-targeted cationic liposome system was designed for the purpose of investigating the relationship between Bmil siRNA and UA. The folate receptor-targeted cationic liposomes co-delivering UA and Bmi1 siRNA (FA-UA/siRNA-L) were fabricated by electrostatic interaction between folate UA liposome (FA-UA-L) and Bmi1 siRNA. Tumor growth is inhibited by FA-UA/siRNA-L in vitro and in vivo and this inhibition is contributed by a synergistic anti-tumor effect of UA and Bmi1 siRNA. The western blot measurement of apoptosis-protein and cancer stem cell (CSC) marked-protein demonstrated that UA led to activation-induced tumor cell death and Bmi1 siRNA resulted in inhibition of cancer stem cells. Overall, these results indicate that Bmi1 as a regulating gene for cancer stem cell is an effective target for cancer treatment using siRNA and co-delivery of UA and Bmi1 siRNA using folate-targeted liposomes is a promising strategy for improved anti-tumor effect.
研究领域:
肿瘤学
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药学
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分子生物学
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PubMed
高影响因子
PeerJ
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2024
·
IF 2.3
Jin Dong,Taowen Ye,Yanli Dong,Jie Hui,Xiaorong Wang
Background Oligospermia is one of the most common reasons for male infertility which is troubling numerous couples of child-bearing age. This investigation scrutinizes the implications and mechanistic underpinnings of ursolic acid’s effect on busulfan-induced oligospermia in mouse models. Methods A singular intraperitoneal injection of busulfan at a dosage of 30 mg/kg induced oligospermia. Two weeks subsequent to this induction, mice were subjected to various dosages of ursolic acid (10, 30, and 50 mg/kg body weight, respectively) on a daily basis for four consecutive weeks. Following this treatment period, a meticulous analysis of epididymal sperm parameters, encompassing concentration and motility, was conducted using a computer-assisted sperm analysis system. The histopathology of the mice testes was performed utilizing hematoxylin and eosin staining, and the cytoskeleton regeneration of the testicular tissues was analyzed via immunofluorescent staining. Serum hormone levels, including testosterone, luteinizing hormone, and follicle-stimulating hormone, as well as reactive oxygen species levels (inclusive of reactive oxygen species and malondialdehyde), were gauged employing specific enzyme-linked immunosorbent assay kits. Differentially expressed genes of testicular mRNA between the oligospermia-induced group and the various ursolic acid treatment groups were identified through RNA sequencing analysis. Results The results revealed that a dosage of 50 mg/kg ursolic acid treatment could increase the concentration of epididymal sperm in oligospermia mice, promote the recovery of testicular morphology, regulate hormone levels and ameliorate oxidative damage. The mechanism research results indicated that ursolic acid increased the expression level of genes related to motor proteins in oligospermia mice.
研究领域:
生殖生物学
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药理学
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分子生物学
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组织病理学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2025
·
IF 6.2
Yuan Zhu,Xiaoguang Yan,Weiguo Li,Jianjun Qiao,Guang-Rong Zhao
Ursolic acid, a plant-derived pentacyclic triterpenoid with anti-inflammatory, antioxidant, and other bioactive properties, holds significant potential for use in nutritional supplements and drug development. However, its extraction from medicinal plants is inefficient due to low yield and dependence on seasonality and geography. Herein, we use modular metabolic engineering to enhance ursolic acid production in Saccharomyces cerevisiae by dividing the biosynthetic pathway into five modules. First, the heterologous ursolic acid biosynthesis module was established using Catharanthus roseus α-amyrin synthase (CrMAS) and a fused α-amyrin oxidase (CrOAS) with cytochrome P450 reductase (CPR). Next, the full hybrid mevalonate pathway was overexpressed, and the copy number of CrMAS was optimized. The sterol pathway was further optimized by introducing N-degron tags to relieve the competition pathway and deleting the SSM4 gene to enhance the ERG1 stability. Acetyl-CoA supply was improved via phosphoketolase and acetyl-CoA synthase pathways, combined with fine-tuning of mitochondrial and cytosolic carbon flux. The final engineered strain produced 1083.62 mg/L of ursolic acid in shake-flask cultures and 8.59 g/L in a 5 L bioreactor via fed-batch fermentation, achieving the highest microbial ursolic acid titer reported to date. This study not only demonstrates the potential for efficient biosynthesis of triterpenoid compounds but also provides ideas that can be extended to other microbial hosts for the concentrated use of intracellular carbon sources in the synthesis of complex natural products.
研究领域:
代谢工程
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生物技术
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生物化学
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微生物生物技术
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PubMed
高影响因子
KOREAN JOURNAL OF CHEMICAL ENGINEERING
·
2026
·
IF 3.2
Kim Jung-Min,Ko Cheon-Kwang,Lee Bong-Seop
To enable the efficient extraction of ursolic acid, a non-polar bioactive compound, the applicability of alcohol-based deep eutectic solvents (DESs) was investigated. A series of DESs were prepared by combining a fixed hydrogen bond acceptor, choline chloride (ChCl), with various hydrogen bond donors (HBDs) such as glycerol, ethylene glycol, 1,3-propanediol, 1,2-propylene glycol, and 1,4-butanediol at different molar ratios. To evaluate their potential as green solvents, the cytotoxicity of the alcohol-based DESs was assessed, and the 1,2-propylene glycol-based DESs exhibited the lowest cytotoxicity. Due to the high viscosity of DESs, direct solubility measurements of ursolic acid were limited; thus, the COSMO-SAC model was employed to predict solubility and guide the screening of suitable DESs. Computational results suggested that DESs containing 1,2-propylene glycol and 1,4-butanediol provided superior solubility for ursolic acid. Based on both cytotoxicity and predicted solubility, the DES composed of ChCl and 1,2-propylene glycol at a 1:4 molar ratio was identified as the most biocompatible solvent system. Using this DES, ursolic acid was successfully extracted from rosemary and apple peel. Experimental validation confirmed that PG-based DES (ChCl:1,2-propylene glycol = 1:4) exhibited a solubility 70% lower for ursolic acid than pure ethanol. This study supports a strategic shift toward sustainable extraction technologies using DESs and provides a foundation for future research on their industrial applicability.
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高影响因子
TOXICOLOGY AND APPLIED PHARMACOLOGY
·
2020
·
IF 3.347
Haoyi Zheng,Haitao Feng,Wenzhong Zhang,Yantao Han,Wenwen Zhao
With the growth of the aging population, osteoporosis is becoming a global health problem. Ursolic acid (UA) is an active ingredient existed in a variety of foods and nature plants and owns plenty of pharmacological effects especially in treating metabolic disease . Our predication from network pharmacology hinted that UA has potential for ameliorating osteoporosis. Firstly through in vivo experiment, we confirmed that UA administration obviously protected against ovariectomy (OVX)-induced osteoporosis in rats by improving microarchitectural deterioration of trabecular bone ( P < 0.001), decreasing numbers of TRAP positive osteoclast in vertebra ( P < 0.001), as well as decreasing serum osteoclast-specific cytokines release ( P < 0.001). Besides, UA ameliorated kidney damage secondary to OVX-induced osteoporosis by ameliorating glomerular atrophy, decreasing BUN and creatinine levels in OVX rats. In vitro , UA noticeably decreased osteoclastic-special marker proteins c-Fos and NFATc1 expressions ( P < 0.001) in response to RANKL stimulation in macrophagy. Importantly, autophagy pathway was activated in the process of osteoclast differentiation and blocked by UA pretreatment . Furthermore, autophagy inhibitors suppressed osteoclast differentiation ( P < 0.001). Collectively, UA may ameliorate osteoporosis by suppressing osteoclast differentiation mediated by autophagy. Our research provides scientific support for UA treating osteoporosis and offers an optimal dose for daily intake of UA safely to prevent bone diseases.
研究领域:
药理学
·
老年医学
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骨骼生物学
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DOI
PubMed
高影响因子
MedChemComm
·
2019
·Vol. 10
·期 8
·1370-1378
·
IF 2.394
Chun-Mei Liu,Jia-Yan Huang,Li-Xin Sheng,Xiao-An Wen,Ke-Guang Cheng
Due to the obvious adverse effects of 5-fluorouracil that limit its clinical usefulness and considering the diverse biological activities of pentacyclic triterpenes, twelve pentacyclic triterpene-5-fluorouracil conjugates were synthesized and their antitumor activities were evaluated. The results indicated that all the single substitution targeted hybrids (7a–12a) possessed much better antiproliferative activities than the double substitution targeted hybrids (7b–12b). Hybrid 12a exhibited good antiproliferative activities against all the tested MDR cell lines. Furthermore, it was revealed that 12a could induce intracellular calcium influx, the generation of ROS, arrest the cell proliferation at the G1 phase, and activate the apoptotic signaling caspase-8, which eventually activates the apoptotic effector caspase-3 and causes the later nuclear apoptosis.
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高影响因子
Plants-Basel
·
2026
·Vol. 15
·期 16
·2443
·
IF 4.7
Yuhang Jiang,Zehong Qiu,Biaoshen Lin,Zhongping Yang,Yanping Hong
This study investigated the formation of a co-amorphous complex between ursolic acid and quercetin as a chemically defined model system for improving the formulation performance of a poorly soluble triterpenoid acid. Co-amorphous systems were prepared by solvent evaporation and physical grinding at different mass ratios. The optimal formulations were identified and evaluated by water-solubility measurement, powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), and in vivo expectorant–antitussive assays. The solvent-derived system showed higher water solubility than the ground system. PXRD and FTIR results suggested that the solvent method more effectively promoted loss of crystallinity and probable intermolecular interactions, whereas the grinding method largely retained the crystalline features of ursolic acid. Both ursolic acid–quercetin formulations exhibited enhanced expectorant and antitussive activities compared with pure ursolic acid. Although quercetin may contribute intrinsic pharmacological activity, the overall improvements were broadly consistent with the altered physicochemical properties of the co-amorphous systems, which may facilitate ursolic acid delivery. As a secondary exploratory comparison, plant-derived triterpenoid-acid-rich and flavonoid-rich fractions fromEriobotrya japonicaleaves were also co-processed; however, because these fractions were not compositionally characterized, their results were interpreted cautiously and were not used as the primary basis for mechanistic conclusions. Overall, the present study demonstrates that co-amorphous complexation of ursolic acid and quercetin is a promising strategy for improving the solubility-related properties and in vivo activity of a poorly soluble triterpenoid acid.
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