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FOOD CHEMISTRY · 2022 · IF 9.231

Rapid screening of antioxidant from natural products by AAPH-Incubating HPLC-DAD-HR MS/MS method: A case study of Gardenia jasminoides fruit

Guo-Dong Zhuang,Wen-Ting Gu,Shu-Hong Xu,Dong-Min Cao,Si-Min Deng,Yong-Sheng Chen,Shu-Mei Wang,Dan Tang

A new AAPH-Incubating HPLC-DAD-HR MS/MS method was developed for the rapid and high-throughput screening of antioxidants directly in natural products and applied to Gardenia jasminoides fruit. This method was assumed that the peak areas of compounds with potential antioxidant activity in HPLC chromatograms would be significantly reduced or disappeared after incubating with the AAPH which can release ROO at physiological conditions (37 °C, pH 7.4). Additionally, the activity of antioxidants can be evaluated by comparing the peak reduction rates and the screened components can be further identified by HRMS/MS. Then, 17 potential natural antioxidants from the crude extract of GJF was screened. Among them, three major components including crocin I, crocin II and crocetin showed excellent ROO scavenging activity, which were further validated by the ORAC assay. In conclusion, our study provided a simple and effective strategy to rapidly screen antioxidants in natural products.

CAS / MDL: 2997-92-4
研究领域: 分析化学 · 植物化学 · 天然产物研究
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FOOD CHEMISTRY · 2022 · IF 9.231

Comprehensive characterization of ingredients in Crocus sativus L. from different origins based on the combination of targeted and nontargeted strategies

Wei Si,Lele Xiong,Han Zhou,Huimin Wu,Zhe Liu,Guoqiang Liu,Yanfang Liu,Aijin Shen,Xinmiao Liang

As a valuable medicinal and edible plant, C rocus sativus L. has had wide applications since ancient times. Herein, a comprehensive approach for characterization of constituents in saffron was established based on the combination of targeted and non-targeted strategies. A targeted UPLC-ESI/MS n strategy was applied for in-depth identification of crocins, and a non-targeted UPLC-ESI/MS 2 approach characterized other components. This integration strategy was used to analyze ingredients in 21 batches of saffrons from 6 origins. Forty-seven crocins belonging to 8 types were identified including 32 new crocins. Among them, 6 new compounds with specific structures were reported for the first time, i.e. trans -6(G, 2G), trans -4(GT, g), trans -3(GT), cis -3(GT), methyl ester- trans -2(G) and methyl ester- cis -2(G). Besides, 91 non-crocin components were identified including 43 new compounds. Based on systematic investigation of crocins and non-crocins, we found that crocins were the critical components to distinguish saffrons from different origins, especially between domestic and foreign samples.

研究领域: 药用植物学 · 分析化学 · 植物科学
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NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY · 2024 ·Vol. 397 ·期 8 ·6037-6050 · IF 3.1

Comparative pharmacokinetic investigation on crocetin in hyperlipidemia and normal rats after oral administration

She Cheng-Ye,Deng Yuan-Xiong,Wu Qin-Yu,Li Jing

Crocetin as one of the main components of saffron possesses a lot of pharmacological effects, especially the beneficial effects in the treatment of hyperlipidemia. However, the pharmacokinetics of crocetin in the pathological state of hyperlipidemia has not been reported. In present study, the pharmacokinetics of crocetin in hyperlipidemia rats after oral administration of crocetin was investigated and the possible mechanisms for the pharmacokinetics were explored. High-fat diet was used to induce hyperlipidemia in rats. The pharmacokinetics of crocetin was investigated in hyperlipidemia and normal rats after oral and intravenous administration of crocetin, and the possible mechanisms of the pharmacokinetic changes were investigated in terms of metabolism and absorption using in vitro incubation with liver microsomes and the everted gut sac method, respectively. Results indicated that the AUCs of crocetin in hyperlipidemia rats after oral administration of crocetin were remarkably decreased when compared with those in normal rats. Moreover, crocetin was also metabolized more rapidly in the liver microsomes of hyperlipidemia rats and intestinal absorption of crocetin was significantly reduced in hyperlipidemia rats. It suggested that the remarkably decreased AUCs of crocetin in hyperlipidemia rats might partly result from the result of faster metabolic elimination and reduced absorption of crocetin in the hyperlipidemia pathological state. And the present investigations conducted on rats demonstrate that further investigations into the kinetics of crocetin in humans with hyperlipidemia are necessary in order to ensure an adequate dosage in this indication.

研究领域: 药理学 · 生物化学
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FOOD CHEMISTRY · 2021 · IF 7.514

Greener extraction process and enhanced in vivo bioavailability of bioactive components from Carthamus tinctorius L. by natural deep eutectic solvents

Xin Tong,Jiehong Yang,Yu Zhao,Haofang Wan,Yu He,Ling Zhang,Haitong Wan,Chang Li

Natural deep eutectic solvents (NaDESs) are promising green alternatives to conventional solvents widely applied in the extraction of natural products due to their physical and chemical superiorities. In present study, 22 NaDESs consisted from food grade ingredients were screened in ultrasonic assisted extraction (UAE) of bioactive compounds from safflower. The oral bioavailabilities of hydroxysafflor yellow A (HSYA) and anhydrosafflor yellow B (ASYB) in the extracts were then investigated in SD rats with the help of HPLC-MS technique. The results revealed that l -proline-acetamide ( l -Pro-Am) was an effective solvent with the yields of HSYA and ASYB at 32.83 and 8.80 mg/g. Pharmacokinetic studies revealed that the blood level of HSYA and ASYB were significantly higher after oral administration of l -Pro-Am extract than that of aqueous extract. Especially, the relative bioavailabilities (to aqueous extract) of HSYA and ASYB were calculated 183.5% and 429.8%.

研究领域: 药理学 · 化学工程 · 分析化学
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Coatings · 2023 ·Vol. 13 ·期 4 ·714 · IF 3.4

Development of Antimicrobial Microcapsules of Saffron Petal Essential Oil by Condensation Method and Its Excellent Binding on Cotton Fibers

Su Liu,Liuxin Shi,Mengyun Liu,Wei Chen,Qiang Cheng,Xiuli Song

In recent years, textiles with antimicrobial properties have attracted more and more attention. As natural antimicrobial agents, essential oils’ potential application value lies in their ability to provide textiles with antimicrobial functions. In this paper, organic solvent extraction (n-hexane, petroleum ether, ethanol) and steam distillation were used to extract saffron petal essential oil (SPEO). It was found that organic solvent extraction (ethanol) had the highest extraction rate and the most apparent bacteriostatic effect. SPEO-Ms were prepared using the composite condensation method with gelatin and chitosan. The microstructure, encapsulation efficiency, slow-release performance, infrared spectrum, and thermal stability of the SPEO-Ms were evaluated. The results showed that the microencapsulated essential oil had good bacteriostatic properties. Antimicrobial cotton fabric was prepared by impregnating microcapsules onto cotton fibers. The effects of the microcapsules’ concentration on the whiteness, air permeability, moisture permeability, and bacteriological inhibition of the fabric were investigated. The results revealed that SPEO-Ms have the potential to be used as a new antimicrobial agent in textiles.Keywords:saffron flower petal essential oil;microcapsule;antimicrobial cotton fabric;cotton fabric

CAS / MDL: 111-30-8
研究领域: 纺织科学 · 微生物学 · 植物化学
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FOOD CHEMISTRY · 2024 · IF 8.5

Dissecting the binding effect of Crocetin glucosyltransferase 2 in crocetin biotransformation in saffron (Crocus sativus L.) from different origins

Jiying Zhu,Wei Jia,Jian Peng

Crocus sativus L. is a both medicinal and food bulbous flower whose qualities are geographically characterized. However, identification involving different places of origin of such substances is currently limited to single-omics mediated content analysis. Integrated metabolomics and proteomics, 840 saffron samples from six countries (Spain, Greece, Iran, China, Japan, and India) were analyzed using the QuEChERS extraction method. A total of 77 differential metabolites and 14 differential proteins were identified. The limits of detection of the method were 1.33 to 8.33 μg kg −1 , and the recoveries were 85.56% to 105.18%. Using homology modeling and molecular docking, the Gln84, Lys195, Val182 and Pro184 sites of Crocetin glucosyltransferase 2 were found to be the targets of crocetin binding. By multivariate statistical analysis (PCA and PLS-DA), different saffron samples were clearly distinguished. The results provided the basis for the selection and identification of high quality saffron from different producing areas.

研究领域: 植物化学 · 分子生物学 · 食品科学
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JOURNAL OF FOOD COMPOSITION AND ANALYSIS · 2023 · IF 4.3

Quality evaluation and origin traceability of the imported and domestic saffron spice (Crocus sativus L.) products in China market using chemical composition and stable isotope analysis

Liu Zhi,Gao Xianmei,Yang Jian,Zhao Duoyong,Li Bin,Zhang Zihong,Chen Piao,Wang Dongguang

Saffron spice, as a high value-added but not high-tech processed agricultural product, is easily faked and mislabeled its quality grade and origin for higher market profits and competitiveness. In this work, an analytical strategy combining chemical composition analysis and stable isotope ratio analysis of saffron spices was explored for verifying their quality and origin authenticity in China market. The crocins contents and stable isotope ratios of 70 saffron spice samples collected from five provinces of China and 95 imported products from Iran and Spain were determined together. The contents of crocins may be effective as the indexes of their quality evaluation but not for origin traceability. Relatively, regional difference of stable isotope ratios is significant (p < 0.05) between different origins. Partial least-squares discriminant analysis (PLS-DA) based on chemical compositions and stable isotope ratios of 165 saffron spice samples can identify imported products from Iran and Spain with the accuracies of 98.5 % and 100 %, but still may mis-discriminate samples from Henan and Xinjiang province of China as Iran products, which was further solved by PLS-DA of products from these origins. This strategy is promising as an effective tool for combating commercial frauds and ensuring the authenticity of saffron spice in China market.

CAS / MDL: 64-18-6 67-56-1
研究领域: 食品科学 · 分析化学 · 植物学
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FOOD CHEMISTRY · 2023 · IF 8.8

A novel 3D-fluorescence sensing strategy based on HN-chitosan polymer probe for rapid identification and quantification of potential adulteration in saffron

Wanjun Long,Gaoqiong Deng,Yanmei Zhu,Qingyang Han,Hengye Chen,Yuanbin She,Haiyan Fu

Saffron is a candidate for various kinds of fraud to make huge profits. The present study proposed an efficient three-dimensional (3D) fluorescence sensing strategy based on hydrophilic hydrazine-naphthalimide functionalized chitosan (HN-chitosan) polymer probe for rapid identification and quantification of potential adulteration in saffron. The amino functional group in the HN-chitosan probe reacted specifically with the Oxygen-containing group of active ingredients in saffron, amplifying the signal difference between saffron and the adulterants, which was comprehensively characterized by 3D fluorescence. Four advanced chemometrics methods were applied for the classification of saffron and adulterated saffron, and good performance were obtained in both training and prediction sets. Furthermore, the PLS regression model was applied to the prediction of adulteration level in saffron and showed satisfactory accuracy. This strategy provides a new solution for rapid identification and quantification of potential adulteration in saffron, which contributes to the healthy development of its industry.

研究领域: 食品科学 · 分析化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Chitosan/γ-polyglutamic acid-based Pickering emulsion gel: A promising transdermal carrier for crocetin

Yicheng Yang,Qinan Huang,Lipei Miao,Qihong Zhang,Chongyang Wu,Weike Su,Jingbo Yu

Crocetin (CT), a natural carotenoid dicarboxylic acid known for its high medicinal value, faces challenges such as poor water solubility, low bioavailability and instability, limiting its therapeutic applications. To overcome these challenges, this study introduces a novel Pickering emulsion gel stabilized by naturally sourced chitosan (CS) and γ -polyglutamic acid ( γ -PGA) nanoparticles (CS/ γ -PGA NPs) as a potential transdermal carrier for CT. The CS/ γ -PGA NPs were synthesized using an electrostatic crosslinking method pretreated by mechanical ball-milling, producing uniform and stable nanoparticles. These NPs stabilized a CT-loaded Pickering emulsion gel (CT-PE) with cornmint oil as the oil phase, achieving up to 98.53 % encapsulation efficiency. The CT-PE exhibited enhanced rheological properties, storage stability, sustained and targeted in vitro transdermal release, potent antioxidant activity, and effective antimicrobial effects with no cytotoxicity. Microstructural analysis revealed a dense network of aggregated particles forming a moderately strong gel structure, wherein encapsulated CT enhances emulsion stability through interaction with the gel network. The synergy between CS and γ -PGA facilitated a biocompatible and efficient carrier system, markedly boosting CT's therapeutic effectiveness. These results highlight CT-PE's potential as an effective transdermal carrier for CT, promising for future dermatological treatments and drug delivery systems.

研究领域: 药剂学 · 材料科学 · 生物医学工程
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Foods · 2023 ·Vol. 12 ·期 8 ·1668 · IF 5.2

Effective Therapeutic Verification of Crocin I, Geniposide, and Gardenia (Gardenia jasminoides Ellis) on Type 2 Diabetes Mellitus In Vivo and In Vitro

Haibo Zhou,Sen Zhang,Lianghua Chen,Yimei Liu,Luhong Shen,Jiuliang Zhang

For many centuries, Gardenia (Gardenia jasminoidesEllis) was highly valued as a food homologous Chinese herbal medicine with various bioactive compounds, including crocin I and geniposide. However, the functional mechanism underlying the hypoglycemic effect of gardenia is absent in the literature. To evaluate the effect of gardenia and its different extracts on type 2 diabetes mellitus (T2DM) in in vivo and in vitro experiments, the dried gardenia powder was extracted using 60% ethanol and eluted at different ethanol concentrations to obtain the corresponding purified fragments. After that, the active chemical compositions of the different purified gardenia fragments were analyzed using HPLC. Then, the hypoglycemic effects of the different purified gardenia fragments were compared using in vitro and in vivo experiments. Finally, the different extracts were characterized using UPLC-ESI-QTOF-MS/MS and the mass spectrometric fragmentation pathway of the two main compounds, geniposide and crocin I, were identified. The experimental results indicated that the inhibitory effect of the 40% EGJ (crocin I) on the α-glucosidase was better than the 20% EGJ (geniposide) in vitro. However, the inhibitory effect of geniposide on T2DM was better than crocin I in the animal experiments. The different results in vivo and in vitro presumed potentially different mechanisms between crocin I and geniposide on T2DM. This research demonstrated that the mechanism of hypoglycemia in vivo from geniposide is not only one target of the α-glucosidase but provides the experimental background for crocin I and the geniposide deep processing and utilization.Keywords:gardenia;α-glucosidase;crocin I;geniposide;type 2 diabetes mellitus

CAS / MDL: 64-19-7
研究领域: 药理学 · 药物化学 · 糖尿病研究
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ACS Omega · 2025 · IF 4.3

Biodegradable Microneedle Patch Confers Crocin with Outstanding Effects in the Treatment of Myocardial Infarction

Qian Liu,Rui Zhao,Danni Zhang,Zhaohuan Lou,Jiangyue Wu,Shiying Hou,Bin Yang,Yunyun Lu,Mengyao Yuan,Shudong Lin,Tianlei Wang,Liang Jin,Ling Zhang

Crocin (CRO), the main active component of Crocus sativus (saffron), exhibits significant therapeutic potential for the treatment of myocardial infarction (MI). However, its clinical application is hindered by poor oral administration due to the intestinal barrier. To overcome this limitation, a CRO-incorporated biodegradable microneedle (CRO–DMN) patch was developed to transdermally deliver CRO into the bloodstream, enhancing its therapeutic effect against MI. The microneedle patch, fabricated from sodium hyaluronate (HA), demonstrated excellent mechanical strength, effectively penetrating the stratum corneum and facilitating CRO infiltration to a depth exceeding 300 μm successfully. Studies revealed that CRO was fully released within 30 min postapplication, and the skin self-healed within 90 min after patch removal. Importantly, administration of CRO–DMNs to MI mice resulted in significant improvements in cardiac function and reductions in infarct size compared with CRO treatment alone. Additionally, CRO–DMNs also provided superior protective effects on the myocardium and mitochondria and significantly increased angiogenesis in the infarction border area. In conclusion, CRO–DMNs represent a promising transdermal drug delivery system that effectively improves the therapeutic efficacy of CRO in the treatment of MI.

研究领域: 药理学 · 生物医学工程 · 心血管病学
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JOURNAL OF SEPARATION SCIENCE · 2022 ·Vol. 45 ·期 13 ·2394-2405 · IF 3.614

Ligand fishing based on tubular microchannel modified with monoamine oxidase B for screening of the enzyme's inhibitors from Crocus sativus and Edgeworthia gardneri

Xu-Wei Qi,Yi-Ming Liu,Yi-Kao Hu,Hao Yuan,Emmanuel Ayodeji Ayeni,Xun Liao

A novel strategy of performing ligand fishing with enzyme-modified open tubular microchannel was proposed for screening bioactive components present in medicinal plants. Monoamine oxidase B was immobilized onto the surface of the microchannel for the first time to specifically extract its ligands when the plant's extracts solution flows through the channel. The thermal and the storage stability of immobilized monoamine oxidase B were significantly enhanced after immobilization. Crocin I and Ⅱ were extracted from Crocus sativus , and tiliroside was extracted from Edgeworthia gardneri . All the three compounds were inhibitors of the enzyme with the half-maximal inhibitory concentration values of 26.70 ± 0.91, 19.88 ± 2.78, and 15.65 ± 0.85 μM, respectively. The enzyme inhibition kinetics and molecular docking were investigated. This is the first report on the inhibitory effects of tiliroside and crocin Ⅱ. The novel ligand fishing method proposed in this work possesses advantages of rapidness, high efficiency, and tiny sample consumption compared to routine ligand fishing, with promising potential for screening active natural products in complex mixtures.

研究领域: 生物化学 · 药理学 · 植物化学
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