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PHYTOMEDICINE · 2023 · IF 7.9

Exploring the boost of steaming with wine on Ligustri Lucidi Fructus in treating postmenopausal osteoporosis based on superior “multi-component structure” and iron/bone metabolism coregulation

Jun Jiang,Baixiu Zhao,Jianpeng Xiao,Liang Shi,Wei Shang,Ye Shu,Zhiming Zhao,Junyi Shen,Jingjuan Xu,Hui Cai

Background Clinical studies indicated that postmenopausal osteoporosis (PMOP) often accompanied by iron overload risk factor, which exacerbated bone metabolism disorders and accelerated PMOP. Previous research found that multicomponent in Ligustri Lucidi Fructus (FLL) or wine-steamed FLL (WFLL) acted on the common targets of iron overload and PMOP simultaneously, which indicated that FLL and WFLL probably regulated iron/bone metabolism dually. Additionally, WFLL had more superior effect according to the theory of Chinese medicine for thousands of years. Purpose To reveal the “superior multi-component structure (SMCS)” and its molecular mechanisms in parallelly down-regulating iron overload and rescuing bone metabolism by WFLL. Designs and methods HPLC fingerprinting was established to compare the chemical profiles of FLL and WFLL; Then, the chemical compositions and quality markers of FLL and WFLL were analyzed by UPLC-Orbitrap-MS/MS coupled with OPLS-DA; The dynamic contents of quality markers and the multi-component structure at different wine steaming times (WST) were simultaneously determined by HPLC-DAD; Meanwhile, the dynamic efficacy of FLL at different WST were hunt by systematic zebrafish model. Subsequently, potential mechanism of WFLL in treating PMOP accompanied with iron overload was obtained from network pharmacology (NP) and molecular docking (MD). Finally, zebrafish and ovariectomy rat model were carried out to validate this potential mechanism. Results HPLC fingerprints similarity of 15 batches in FLL and WFLL were among 0.9-1.0. 126 compositions were identified, including 58 iridoids, 25 terpenes, 30 phenylethanoids, 7 flavonoids and 6 others. 20 quality markers associated with WFLL was revealed, and the ratio of Phenylethanols: Iridoids: Triterpenes (P/I/T) was converted from 1: 15: 4.5 to 1: 0.8: 0.9 during steaming (0 - 24 h) calculated by the quantification of 11 quality markers; The bone mineralization and motor performance of zebrafish larvae indicated that the optimum efficacy of WFLL at 12 h ( P < 0.05) in which the SMCS of P/I/T was converted to 1: 4: 1.8. NP discovered that BMP-Smad pathway is one of the potential mechanisms of FLL in anti PMOP and then regulated bone formation and iron overload simultaneously. MD revealed that 17 active ingredients and 10 core targets genes could spontaneously bind with appropriate affinity. Rats model verified that FLL and WFLL significantly reversed PMOP, based on the improvement in bone formation indexes (ALP, OPG, OGN), iron metabolism indicators (hepcidin, ferritin), bone microstructure (BMD, BV/TV, Tb. Th, Tb. N); Moreover, WFLL significant enhanced reversal effect in anti-PMOP compared to FLL ( P < 0.05). FLL and WFLL increased genes and proteins expression (Hep, BMP-6, p-Smad1/5, Smad4) related to BMP-Smad pathway compared with model group, and WFLL was more superior than FLL ( P < 0.05). Conclusion The SMCS of FLL was optimized by wine-steam, WFLL represented a dual effect in downregulating iron overload and promoting bone formation, and the BMP-Smad pathway is one of the potential molecular mechanisms.

CAS / MDL: 72-48-0
研究领域: 药理学 · 中药学 · 骨代谢 · 铁代谢 · 网络药理学 · 分子生物学
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Chemistry Central Journal · 2017 ·Vol. 11 ·期 1 ·1-10 · IF 2.442

Isolation, purification, structural analysis and coagulatory activity of water-soluble polysaccharides from Ligustrum lucidum Ait flowers

Yin Zhenhua,Zhang Wei,Zhang Juanjuan,Kang Wenyi

In this study, Ligustrum lucidum flowers as raw material, the extraction, isolation and coagulatory activity of polysaccharides were carried out for the first time. The crude polysaccharide was obtained by hot water extraction and ethanol precipitation, and preliminarily purified by Sevage method and D101 macroporous resin. Then the polysaccharide was further purified by DEAE-52 cellulose and Sephadex G-100 column chromatography, respectively. The structural characteristics were detected by LC, GC, FT-IR and NMR. Furthermore, the coagulatory activity of the polysaccharides were investigated by APTT, TT, PT and FIB assays in vitro. The results demonstrated that four polysaccharides were isolated from flowers of L. lucidum, named as LLP-1a, LLP-1b, LLP-2 and LLP-3, and the yields were 0.039, 0.0054, 0.0055 and 0.017%, respectively based on the weight of the dried flowers. The four polysaccharides components were free of nucleic acids and proteins, and their average molecular weights were 25,912, 64,919, 3,940,246 and 2,975,091 g/mol, respectively. The monosaccharide compositions of LLp-1a were l-rhamnose, l-arabinose, d-xylose, d-glucose and d-galactose (molar ratio of 3.16: 2.46: 1.00: 7.27: 4.22). Only d-galactose was detected from LLp-1b. LLp-2 was composed of l-arabinose, d-glucose and d-galactose (molar ratio of 1.28:1.32:1.00). LLp-3 was composed of l-rhamnose, l-arabinose, d-xylose, d-glucose and d-galactose (molar ratio of 5.85: 2.21: 2.23: 1.00: 2.25). Coagulation assays indicated that LLp-1a and LLp-3 had good anticoagulant effect in vitro, while LLp-1b showed procoagulant activity.

CAS / MDL: 76-05-1
研究领域: 植物化学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2023 ·Vol. 28 ·期 14 ·5309 · IF 4.6

A New HPLC-UV Method Using Hydrolyzation with Sodium Hydroxide for Quantitation of Trans-p-Hydroxycinnamic Acid and Total Trans-p-Hydroxycinnamic Acid Esters in the Leaves of Ligustrum robustum

Shi-Hui Lu,Xiao-Na Liang,Xiao-Jin Nong,Ran Chen,Xiu-Xia Li

Trans-p-hydroxycinnamic acid and its esters in the leaves ofLigustrum robustummight be a new resource to prevent diabetes and its complications. In the present study, a new HPLC-UV method using hydrolyzation with sodium hydroxide for quantitation oftrans-p-hydroxycinnamic acid and totaltrans-p-hydroxycinnamic acid esters in the leaves ofL. robustumwas developed, since it was difficult and troublesome to analyze no less than 34trans-p-hydroxycinnamic acid esters by usual HPLC. The extract ofL. robustumwas hydrolyzed with sodium hydroxide at 80 °C for 2 h, and then, hydrochloride was added. HPLC analysis was performed in reverse phase mode using a C-18 column, eluting with methanol-0.1% acetic acid aqueous solution (40:60,v/v) in isocratic mode at a flow rate of 1.0 mL·min−1and detecting at 310 nm. The linear range fortrans-p-hydroxycinnamic acid was 11.0–352.0 μg·mL−1(r2= 1.000). The limit of detection and limit of quantification were 2.00 and 6.07 μg·mL−1, respectively. The relative standard deviations of intra-day and inter-day variabilities fortrans-p-hydroxycinnamic acid were less than 2%. The percentage recovery oftrans-p-hydroxycinnamic acid was 103.3% ± 1.1%. It is the first HPLC method using hydrolyzation for quantification of many carboxylic esters. Finally, the method was used successfully to determinetrans-p-hydroxycinnamic acid and totaltrans-p-hydroxycinnamic acid esters in various extracts of the leaves ofL. robustum. The 60–70% ethanol extracts ofL. robustumshowed the highest contents of freetrans-p-hydroxycinnamic acid (3.96–3.99 mg·g−1), and the 50–80% ethanol extracts ofL. robustumdisplayed the highest contents of totaltrans-p-hydroxycinnamic acid esters (202.6–210.6 mg·g−1). The method can be applied also to the quality control of the products ofL. robustum.Keywords:trans-p-hydroxycinnamic acid;esters;Ligustrum robustum;HPLC-UV;hydrolyzation;sodium hydroxide;quantification

研究领域: 植物化学 · 分析化学 · 药用植物研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Foods · 2022 ·Vol. 11 ·期 20 ·3187 · IF 5.561

Wheat Starch Modified with Ligustrum robustum (Rxob.) Blume Extract and Its Action Mechanism

Nan Chen,Hao-Xiang Gao,Qiang He,Wei-Cai Zeng

We investigated the modification of wheat starch withLigustrum robustum(Rxob.) Blume extract (LRE) and determined the action mechanism. Based on differential scanning calorimetry, LRE decreased the gelatinization enthalpy of wheat starch from 19.14 to 7.15 J/g and changed gelatinization temperatures (including the variation in gelatinization onset temperature, peak temperature and conclusion temperature in different degrees). Moreover, LRE affected the pasting viscosity curve of wheat starch, and changed its rheological parameters (including the decrease in storage modulus and loss modulus, as well as the increase in loss tangent). Based on the analysis of scanning electron microscopy and wide-angle X-ray diffraction, LRE increased the hole size and the roughness of the gel microstructure, and decreased the crystallinity of wheat starch. Meanwhile, the evaluation results of the texture analyzer and the colorimeter showed that LRE could change the quality properties (including decrease hardness, fracturability andL*values, as well as increasea*andb*values) of wheat starch biscuits after hot air baking (170 °C). Furthermore, with molecular dynamics simulation analysis, phenolic compounds of LRE combined with starch molecules via H-bonds and affected the formation of molecular bonds (including intra- and intermolecular hydrogen bonds), so as to change the spatial conformation and properties of wheat starch during gelatinization and retrogradation. The present results suggest that LRE can modify the physicochemical properties of wheat starch and further improve its processing properties, indicating its potential in the design and development of starch foods (such as steamed buns, bread, biscuits, etc.).

研究领域: 食品科学 · 植物化学 · 生物物理学
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JOURNAL OF FOOD SCIENCE · 2022 ·Vol. 87 ·期 2 ·651-663 · IF 3.693

Potential of phenolic compounds in Ligustrum robustum (Rxob.) Blume as antioxidant and lipase inhibitors: Multi-spectroscopic methods and molecular docking

Hao-Xiang Gao,Heng-Yu Liang,Nan Chen,Bi Shi,Wei-Cai Zeng

Ligustrum robustum (Rxob.) Blume is traditionally served as a functional tea in China. In this work, the antioxidant activities of L. robustum (Rxob.) Blume extract (LRE) were evaluated and its inhibitory effect and mechanism on pancreatic lipase were further investigated. With the high contents of phenols (139.70 ± 1.41 mg gallic acid equivalent/g extract) and flavonoids (326.46 ± 7.36 mg rutin equivalent/g extract), LRE showed significant antioxidant activities ( p < 0.05) for scavenging free radicals and hydrogen peroxide, inhibiting lipid peroxidation and providing strong reducing power. Meanwhile, LRE displayed remarkable inhibitory activity on pancreatic lipase with a low half-effective inhibitory concentration (IC 50 ) of 2.469 ± 0.005 mg/ml which was further determined as non-competitive inhibition. The spectroscopic results showed that LRE inhibited the activity of pancreatic lipase by modifying the tertiary and secondary structures of lipase. Moreover, four phenolic compounds (acteoside, lipedoside A, oleuropein and ligurobustoside C) were identified from LRE by the high performance liquid chromatography-quadrupole- time of flight-mass spectrometry. In addition, according to molecular docking analysis, the four phenols could interact with pancreatic lipase by hydrogen bonds, so as to change the spatial structure of pancreatic lipase and inhibit its catalytic activity. The present results suggest that LRE not only exhibits strong antioxidant capacity but possesses effectively inhibitory activity on pancreatic lipase, which might have the potential to be developed as functional food and nutraceuticals for the prevention of metabolic diseases. Practical Application Ligustrum robustum (Rxob.) Blume extract has been confirmed to possess antioxidant activity and lipase inhibitory activity, which indicates that the L. robustum extract has the potential to prevent oxidative stress and regulate fat metabolism. This work suggests that L. robustum extract can be served as a novel resource to prepare nutraceuticals and functional food in food industries.

研究领域: 食品科学 · 药理学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH · 2024 ·Vol. 31 ·期 7 ·11214-11227 · IF 0

Synergistic effects of arbuscular mycorrhizal fungi and biochar are highly beneficial to Ligustrum lucidum seedlings in Cd-contaminated soil

Li Tiantian,Yang Huan,Zhang Naili,Dong Lijia,Wu Aiping,Wu Qiqian,Zhao Mingshui,Liu Hua,Li Yan,Wang Yanhong

Cadmium (Cd) contamination is a widespread environmental issue. There is a lack of knowledge about the impacts of applying arbuscular mycorrhizal fungi (AMF) and biochar, either alone or in their combination, on alleviating Cd phytotoxicity in Ligustrum lucidum . Therefore, a pot experiment was conducted in a greenhouse, where L. lucidum seedlings were randomly subjected to four regimes of AMF treatments (inoculation with sterilized AMF, with Rhizophagus irregularis , Diversispora versiformis , alone or a mixture of these two fungi), and two regimes of biochar treatments (with or without rice-husk biochar), as well as three regimes of Cd treatments (0, 15, and 150 mg kg −1 ), to examine the responses of growth, photosynthetic capabilities, soil enzymatic activities, nutritional concentrations, and Cd absorption of L. lucidum plants to the interactive effects of AMF, biochar, and Cd. The results demonstrated that under Cd contaminations, AMF alone significantly increased plant total dry weight, soil pH, and plant nitrogen (N) concentration by 84%, 3.2%, and 13.2%, respectively, and inhibited soil Cd transferring to plant shoot by 42.2%; biochar alone significantly enhanced net photosynthetic rate, soil pH, and soil catalase of non-mycorrhizal plants by 16.4%, 9%, and 11.9%, respectively, and reduced the soil Cd transferring to plant shoot by 44.7%; the additive effect between AMF and biochar greatly enhanced plant total dry weight by 101.9%, and reduced the soil Cd transferring to plant shoot by 51.6%. Furthermore, dual inoculation with D. versiformis and R. irregularis conferred more benefits on plants than the single fungal species did. Accordingly, amending Cd-contaminated soil with the combination of mixed-fungi inoculation and biochar application performed the best than either AMF or biochar alone. These responses may have been attributed to higher mycorrhizal colonization, soil pH, biomass accumulation, and biomass allocation to the roots, as well as photosynthetic capabilities. In conclusion, the combined use of mixed-fungi involving D. versiformis and R. irregularis and biochar addition had significant synergistic effects on enhancing plant performance and reducing Cd uptake of L. lucidum plants in Cd-contaminated soil. Graphical abstract

研究领域: 环境科学 · 植物科学 · 土壤生物学 · 微生物学 · 生态毒理学
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JOURNAL OF ETHNOPHARMACOLOGY · 2021 · IF 4.36

The network pharmacology integrated with pharmacokinetics to clarify the pharmacological mechanism of absorbed components from Viticis fructus extract

Xuanhao Chen,Xiaoyan Wang,Lin Ma,Shiming Fang,Jin Li,Evans Owusu Boadi,Jun He,Xiu-mei Gao,Yu Wang,Yan-xu Chang

Ethnopharmacological relevance Viticis fructus ( VF ) has been widely used in alleviating the swelling and pain, owning to its pharmacologically active components including agnuside, 10- O -vanilloylaucubin, luteolin and casticin. Aim of the study The pharmacokinetic profiles of the absorbed components from aqueous and ethanolic extracts of VF in rat plasma were performed, and explored the molecular mechanisms of absorbed components via network pharmacology . Materials and methods Ultra-performance liquid chromatography-tandem mass spectroscopy (UHPLC-MS/MS) was employed to identify the absorbed components from rat plasma. Liquid-liquid extraction with ethyl acetate was used to purify the plasma samples. Plasma pharmacokinetics parameters of the components absorbed were analyzed after oral administration of both extracts. Network pharmacology was used to predict the biological functions and potential signaling pathways of VF . The anti-cancer effects of VF extract and absorbed components have been confirmed by in vitro experiments. Results The method was very sensitive with lower limit of quantification (LLOQ) of 1.0, 2.5, 0.2 and 0.5 ng/mL for agnuside, 10- O -vanilloylaucubin, luteolin and casticin, respectively. With the exception of 10- O- vanilloylaucubin which was not detected in the ethanolic extract of VF , all other components were detected in both extracts in plasma. The pharmacokinetic parameters of the four components from rat plasma were significantly different between the two extracts. According to the results of network pharmacology, the absorption components of VF are enriched in 32 key pathways, and 15 pathways are related to cancer. Ultimately, the anti-cancer effects, as well as the signaling pathways of VF ethanolic extract and absorbed components were verified by in vitro experiments. Conclusion The optimized, sensitive and validated UHPLC-MS/MS method was successfully applied for the plasma pharmacokinetics comparison analysis of the two VF extracts. The combination of network pharmacology and pharmacokinetics provides a useful method to elucidate the biological effects and molecular mechanism of the absorbed components of VF .

CAS / MDL: 1634-04-4
研究领域: 药理学 · 药代动力学 · 网络药理学 · 中药 · 癌症研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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COMPOSITES PART B-ENGINEERING · 2025 · IF 14.2

Multifunctional hydrogel microspheres regulate the balance of osteoblastic-osteoclastogenesis to treat osteoporotic bone defects by the NFATc1/RANKL/MAPK signaling

Dongping Wang,Jiamin Yang,Chang Liu,Wei Lin,Shenglin Lei,Yuxian Chen,Pinying Cheng,Yilin Huang,Shuling Gu,Haishan Li,Yuewei Lin,Huizhi Guo,Guoye Mo,Bing Mai,Zheng Zhang,Qingtao Li,Yongxian Li,Xiaodong Cao,Shuncong Zhang

Osteoporosis (OP) is characterized by diminished bone mass and increased skeletal fragility, representing a metabolic disorder. Osteoporotic bone defects (OBD) pose significant treatment challenges due to the active generation of osteoclasts (OCs) and the suppression of osteogenic differentiation. These complications impose a substantial burden on patients and the healthcare system. To address this issue, alendronate sodium (AS) was incorporated into Gelatin methacryloyl (GelMA), and then loaded with ligustrum officinale polysaccharide (LOP) to form GelMA-AS-LOP microspheres. These multifunctional hydrogel microspheres, characterized by their abundant void structures, offered continuous drug release. GelMA-AS-LOP suppressed OCs’ activity and formation, enhanced osteogenic differentiation and mineralization, and exhibited low visceral toxicity. Consequently, they ameliorated the pathological microenvironment associated with OP and facilitate OBD regeneration. The hydrogel microspheres achieved this by promoting osteogenesis and modulating the NFATc1, RANKL (via LOP), and MAPK (via AS) signaling pathways, resulting in a dual synergistic effect.

CAS / MDL: 111-30-8
研究领域: 生物材料 · 组织工程 · 骨再生 · 药理学 · 细胞信号传导
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