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PROCESS BIOCHEMISTRY · 2024 · IF 3.7

Polygonati rhizoma fermentation by Monascus ruber and evaluation of fermentation products in vitro

Zijun Tao,Jian Zhang,Fuge Niu,Huien Zhang,Zhongfa Chen,Shanfu Wang,Yuli Zhang,Jie Li,Peng Liu

This study investigated the conditions for polygonati rhizoma (PR) fermentation by Monascus ruber and the lipid-lowering activity of the resulting product. Monascus ruber was used for the solid-state fermentation of PR, and the response surface method was used to optimize the fermentation culture medium parameters. The optimal fermentation system yielded a maximum monacolin K concentration of 21.82 ± 0.34 mg/g. The fermentation conditions were as follows: 12.5 mmol/kg of L-glutamic acid, 0.64 mmol/kg of cyclic adenosine monophosphate , 3.0 wt% of yeast extract powder, a fermentation period of 15 days, and a fermentation temperature of 30 ℃. The binding capacities of unfermented PR, “Nine-Steam-Nine-Bask” processed Polygonati rhizoma (NPR), and Monascus ruber solid-state fermented polygonati rhizoma (MPR) to sodium cholate, sodium taurocholate , and sodium glycolate were determined. MPR showed a stronger bile acid-binding capacity than unfermented PR. In addition, MPR exhibited the highest cholesterol inhibitory capacity of 51.43±1.41 %. Thus, MPR can be used as a potential antilipemic agent with potent hypolipidemic effects.

研究领域: 中药学 · 微生物学 · 生物化学
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2023 ·Vol. 24 ·期 2 ·1593 · IF 5.6

Esculetin Alleviates Nonalcoholic Fatty Liver Disease on High-Cholesterol-Diet-Induced Larval Zebrafish and FFA-Induced BRL-3A Hepatocyte

Ji Ma,Yang Deng,Tingting Yang,Maoru Li,Jing Shang

Non-alcoholic fatty liver disease (NAFLD), defined in recent years as metabolic-associated fatty liver disease (MAFLD), is one of the most common liver diseases in the world, with no drugs on market. Esculetin (ESC) is an active compound discovered in a variety of natural products that modulates a wide range of metabolic diseases and is a potential drug for the treatment of NAFLD. In this study, we used an HCD-induced NAFLD larval zebrafish model in vivo and an FFA-induced BRL-3A hepatocyte model in vitro to evaluate the anti-NAFLD effect of ESC. Lipid lowering, anti-oxidation and anti-inflammation effects were revealed on ESC and related gene changes were observed. This study provides a reference for further study and development of ESC as a potential anti-NAFLD/MAFLD drug.Keywords:esculetin;non-alcoholic fatty liver disease;lipid-lowering;antioxidant

研究领域: 药理学 · 肝病学 · 分子生物学
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Foods · 2025 ·Vol. 14 ·期 11 ·1894 · IF 5.1

Flavor Quality and Lipid-Lowering Function of Mixed Fermented Pu-erh Tea with Various Monascus Species

Xiaomin Chen,Yao Hu,Zhen Zeng,Xu Zhang,Yahui Huang

As a potential raw material with a variety of bioactive compounds, Pu-erh raw tea can produce rich flavor and health benefits through natural fermentation or microbial fermentation in traditional processing. However, the traditional fermentation process has some problems such as a long fermentation period and unstable quality. Monascus, a kind of fungus used in both medicine and food, has been proved to have many beneficial effects such as lowering cholesterol and regulating blood lipids. Therefore, in this study we investigated whether the fermentation of mixed monascus could significantly improve the flavor quality and lipid-lowering activity of Pu-erh raw tea. We added four kinds of monascus to unfermented Pu-erh raw tea (UT) to obtain a fermented Pu-erh raw tea (FT). The quality of the two tea samples was determined and an in vitro lipid-lowering experiment was conducted. The results show that the contents of water extractives, flavone, trans-catechins (GCG and CG), theabrownins, and caffeine in FT are significantly higher than those in UT, increasing by 19.41%, 14.47%, 18.76%, 29.82%, and 10.67%, respectively. In terms of aroma, linalool was the characteristic compound of UT, presenting a floral note. D-Limonene was the key characteristic substance of FT, manifested as lemon, toast, and wood. In terms of taste, FT has a high content of bitter amino acids and caffeine, a low content of catechins, and is rich in carbohydrate substances, forming a characteristic mild and mellow slightly bitter taste with reduced astringency. In addition, the relative contents of active substances with lipid-lowering effects such as quercetin, quercitrin, ascorbic acid, and sorbitol in FT were higher than those in UT, increasing by 83.09%, 81.73%, 89.86%, and 92.76%, respectively. The effect of FT on regulating cellular lipid metabolism was superior to UT based on cell experiments. The research results provide a scientific basis for the deep processing and functional development of Pu-erh raw tea.

CAS / MDL: 67-56-1 67-63-0
研究领域: 食品科学 · 微生物学 · 生物化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Enhancing stability of liposomes using high molecular weight chitosan to promote antioxidative stress effects and lipid-lowering activity of encapsulated lutein in vivo and in vitro

Gaoshuai Zhang,Meijing Zhang,Yiqiao Pei,Kun Qian,Jiao Xie,Qun Huang,Suwen Liu,Na Xue,Yujiao Zu,Hao Wang

Lutein is an antioxidant with multiple beneficial functions. However, its therapeutic potential is hampered by its low water solubility and bioavailability. The goal of this study is to compare the stability of lutein-loaded liposomes (Lu-lip) and low (LC)/high molecular weight (HC) chitosan-coated Lu-lip, along with their antioxidant capacity using H 2 O 2 -induced HepG2 cells and their lipid-lowering activity using high-fat diet mice. Both LC and HC reduced the lutein degradation rate by 17.5 % and 26.72 % in a challenging environment at pH 6 and T  = 4 °C. Compared to LC, the HC coating improved the size- and zeta-potential-stability of Lu-lip at 5 < pH < 7, with the best performance at pH 6. The HC coating prolonged the lutein release profile, increased the cellular uptake of Lu-lip, and reduced the reactive oxygen species (ROS) levels and the H 2 O 2 -induced necrotic cell ratios by increasing the activities of catalase (CAT), superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px). Animal experiments have shown that oral administration of LC and HC coated Lu-lip can significantly reduce body weight levels, total triglycerides (TG), total cholesterol (TC), and non-high-density lipoprotein (n-HDL-C) in high-fat diet mice while significantly increasing the levels of CAT, SOD and GSH-Px in the liver of mice. LC and HC coated Lu-lip can reduce fat accumulation in the liver and epididymal adipose tissue.

研究领域: 药理学 · 生物化学
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Antioxidants · 2023 ·Vol. 12 ·期 7 ·1448 · IF 7

Bio-Assay-Guided Isolation of Fractions and Constituents with Antioxidant and Lipid-lowering Activity from Allium cepa

Kongming Fan,Yan Li,Qiaofeng Fu,Jinmin Wang,Yong Lin,Linyu Qiu,Li Ran,Junli Yang,Chunyan Yang

Active fractions and constituents with antioxidant and lipid-lowering activities were investigated using bio-assay-guided isolation and identification. The data showed that the antioxidant fraction ofA. cepawas AC50%, the main constituents of which were quercetin and isoquercitrin, by way of both ultra-high performance liquid chromatography–mass spectrometry (UPLC-MS) and bio-assay-guided purification and elucidation. Similarly, the lipid-lowering active fraction ofA. cepawas AC30% with the main constituents of 3,4-dihydroxybenzoic acid and quercetin 3,4′-O-diglucoside. Also, bio-assay-guided isolation led to the isolation and identification of five known compounds with a purity of more than 98%, and quercetin was both the best free radical scavenger and lipid-lowering constituent. Moreover, the mechanism of the lipid-lowering effect of AC30% might be its reduction in mRNA expression levels of sterol regulatory element binding protein 2 (SREBP2) and FAS gene in lipid synthesis. Otherwise, reducing the mRNA expression level of lipid synthesis genes, including SREBP1, SREBP2, fatty acid synthetase (FASN),β-Hydroxyβ-methylglutaryl-CoA (HMGCR), stearoyl CoA desaturase 1 (SCD1), and increasing the mRNA expression level of lipid decomposition gene, such as carnitine palmitoyl transferease-1 (CPT1), might be involved in the lipid-lowering activity of quercetin. This study suggested thatAllium cepamight be used to prevent and treat oxidative stress and dislipidemia-related disorders, including NAFLD.Keywords:Allium cepa;lipid lowering;antioxidant;effective fractions;active constituents

研究领域: 植物化学 · 药理学 · 分子生物学
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FOOD CHEMISTRY · 2023 · IF 8.8

Effects of ultra-high pressure assisted extraction on the structure, antioxidant and hypolipidemic activities of Porphyra haitanensis polysaccharides

Mingjing Zheng,Xin Tian,Zhipeng Li,Tao Hong,Yanbing Zhu,Yuanfan Yang,Qingbiao Li,Hui Ni,Zedong Jiang

Porphyra haitanensis polysaccharides (PHP) has potential antioxidant and hypolipidemic activities, but still needs improvement. Therefore, ultra-high pressure (UHP) assisted extraction was applied to modify the structure, antioxidant, and hypolipidemic activities of PHP. UHP assisted extraction increased the total sugar, uronic acid, and 3,6-anhydro-ʟ-galactose contents of PHP, which increased by 15.85%–16.12%, 18.95%–24.32%, 20.54%–23.66% with 500–600 MPa UHP, respectively. Meanwhile, UHP modified PHP became more rough and porous than native PHP. Besides, UHP assisted extracted PHP showed better in vitro antioxidant and hypolipidemic abilities. Especially, 500–600 MPa UHP increased 72.43%–86.42% 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacities, 12.32%–12.82% pancreatic lipase inhibitory ability, and 14.93%–15.23% glycocholate binding abilities of PHP ( p < 0.05). Moreover, UHP assisted extracted PHP greatly decreased the lipid droplet and triglyceride contents of 3T3-L1 adipocytes ( p < 0.05). Our findings can provide the theoretical basis for the high value utilization of Porphyra haitanensis and its polysaccharides with UHP modification.

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

Hypolipidaemic and antioxidant effects of various Chinese dark tea extracts obtained from the same raw material and their main chemical components

Wanjun Ma,Yali Shi,Gaozhong Yang,Jiang Shi,Junpeng Ji,Yue Zhang,Jiatong Wang,Qunhua Peng,Zhi Lin,Haipeng Lv

In order to investigate the hypolipidaemic and antioxidant effects of various dark teas produced from different post-fermentation using the same raw material, a hyperlipidaemia zebrafish model combined with binding bile salts assay and antioxidant assays were performed in this study. Results showed that the hypolipidaemic effect of dark tea extracts increased significantly ( p  < 0.05) while the antioxidant ability decreased sharply compared with raw material. Particularly, Liupao tea (50%) and Pu-erh tea (48%) showed promising hypolipidaemic potential; however, the antioxidant capacity of Pu-erh tea decreased (31–49%) most dramatically. Besides, the levels of total polyphenols and catechins decreased sharply, but theabrownin, gallic acid, and caffeine increased significantly after post-fermentation. Moreover, the potential mechanisms of regulating hyperlipidaemia by dark tea extracts were discussed. These results suggest that microbial fermentation significantly affects the bioactivity of dark teas, and provide theoretical basis for processing and improving of dark tea products for hyperlipidaemia therapy.

研究领域: 营养学 · 生物化学 · 食品科学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Extraction optimization, purification, characterization, and hypolipidemic activities of polysaccharide from pumpkin

Haizhao Song,Yanhui Zhang,Qianqian Huang,Fang Wang,Luanfeng Wang,Ling Xiong,Xinchun Shen

Polysaccharides derived from pumpkin have garnered increasing interest due to their diverse biological activities. In this study, pumpkin polysaccharides were extracted using an ultrasound-assisted extraction method, optimized via response surface methodology. The optimal extraction conditions were identified as follows: a solid-liquid ratio of 1:60 (g/mL), an extraction time of 1.9 h, an extraction temperature of 62 °C, and an ultrasonic power of 286 W. Under these conditions, the total carbohydrate content in pumpkin polysaccharides reached 71.14 ± 1.53 %, closely aligning with the predicted value. Post extraction, the polysaccharides were purified using DEAE Sepharose Fast Flow and Sephadex G-100 columns, resulting in a pure fraction termed PPS3. Structural analysis revealed that PPS3, with a molecular mass of 5.96 × 10 4  Da, consisted of mannose, glucosamine hydrochloride, rhamnose, glucuronic acid, galacturonic acid, glucose, galactose, and arabinose in a molar ratio of 0.005:0.004:0.041:0.013:0.545:0.004:0.241:0.147, respectively. The backbone primarily contained →4)-α-D-GalpA-6-OMe-(1→ residue with several branched chains. Functionally, PPS3 demonstrated potent in vitro hypolipidemic activities. These findings elucidated the structural characteristics of pumpkin polysaccharides and suggested their potential as natural hypolipidemic agents.

CAS / MDL: 50-99-7
研究领域: 食品科学 · 生物化学 · 药理学
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JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS · 2014 · IF 2.15

Rapid analysis of hypolipidemic drugs in a live zebrafish assay

Juan Zhou,Yi-Qiao Xu,Sheng-Ya Guo,Chun-Qi Li

Introduction Hyperlipidemia is the most common form of dyslipidemia , which is the key risk factor for cardiovascular disease and stroke. The development of effective and safe drug treatments for hyperlipidemia has been proven challenging. Methods In this study, taking advantage of the transparency of larval zebrafish, we developed a zebrafish hyperlipidemia model for drug screening and efficacy assessment. Zebrafish at 5 d.p.f (days post fertilization) were fed with 0.1% egg yolk for 48   h (hours), followed by drug treatment for 24   h or 48   h. Tested drugs were administered into the zebrafish by direct soaking. Drug effect was evaluated based on quantitative analysis of Oil Red O (ORO) in zebrafish vena caudalis. Results All 5 human hypolipidemic drugs (simvastatin, lovastatin , ezetimibe , bezafibrate and hyodesoxycholic acid) showed significant hypolipidemic effects ( p   <   0.01) in a dose-dependent manner in the zebrafish hyperlipidemia model. 'We also found a well-known Chinese tea Pu-erh tea significantly reduced lipids in this model ( p   <   0.001 and p   <   0.01). Discussion Our results demonstrate that the zebrafish hyperlipidemia model developed and validated in this study could be used for in vivo hyperlipidemia studies and drug screening and for assessing hypolipidemic drugs with different mechanisms.

CAS / MDL: 163222-33-1 83-49-8
研究领域: 药理学 · 心血管疾病研究 · 药物筛选
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FOOD SCIENCE AND TECHNOLOGY RESEARCH · 2014 · IF 0.355

The Feasibility of Novel Liposome Consisted of Sphingomyelin and β-sitosterol for Gypenosides Delivery

Fan Yu,Jingming Yang,Xinhui Tang,Yan Hu

The limited stability of liposome and high dose of cholesterol severely restricts the application of liposome as an effective formulation in food and drug fields. The feasibility of novel liposomes consisting of sphingomyelin and β-sitosterol, with high stability and lowering cholesterol function, was investigated. The result of molecular modeling indicated that liposome consisting of sphingomyelin and β-sitosterol was practicable. Gypenosides loaded liposome consisting of sphingomyelin and β-sitosterol (GSSL) was successfully prepared attaining a 91.3% entrapment efficiency, exhibiting an average particle size of 205 nm; −33.1 mV zeta potential with smooth continuous surface was observed by AFM. The results of stability experiments indicated that GSSL was more stable than that ordinary gypenosides loaded liposome composed of lecithin and cholesterol (GLCL). Furthermore, GSSL demonstrated much better lipid lowering effects than ordinary GLCL liposome. Therefore, replacing lecithin and cholesterol with sphingomyelin and β-sitosterol in preparation of liposomes is feasible and recommended.

研究领域: 药剂学 · 食品科学 · 分子生物学
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Scientific Reports · 2025 ·Vol. 15 ·期 1 ·1-13 · IF 3.9

Effect of magnetization on antibacterial, lipid-lowering and antioxidant activities of isoquinoline alkaloids

Feng Xueting,Li Weijie,Wang Xiaoling,Tang Jie,Yao Shun

The magnetization strategy of isoquinoline alkaloids has been successfully used in the extraction and isolation, but the effect of the magnetization on biological activities of those alkaloids still deserves further investigation. Therefore, the antibacterial, lipid-lowering and antioxidant activities of five isoquinoline alkaloids (berberine, tetrahydroberberine, palmatine, tetrahydropalmatine and tetrahydropapavine) before and after magnetization were compared in this study, and the results showed that the relevant activities were enhanced after magnetization. Additionally, among the five magnetic derivatives studied, berberine magnetic derivative ([Ber·H] + [FeCl 4 ] − ) had the best antibacterial effect on S. aureus and E. coli with MIC of 200 and 800 µM, respectively; palmatine magnetic derivative ([Pal·H] + [FeCl 4 ] − ) showed the strongest lipid-lowering activity with IC50 of 429 mM, and the inhibitory effect and type on lipase was reversible and mixed inhibition of competition and non-competition type; tetrahydroberberine magnetic derivative ([THBer·H] + [FeCl 4 ] − ) had the strongest antioxidant activity. This study provides new ideas and references for the further application of magnetization strategy.

CAS / MDL: 50-81-7
研究领域: 药理学 · 生物化学
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MOLECULAR PHARMACEUTICS · 2025 · IF 4.5

Bile Acid-based Microcapsule-Like Cocrystals of Phytosterols with Enhanced Solubility, Bioavailability, and Bioactivity

Lei Tang,Yinan Feng,Yifei Bian,Zhixiong Sun,Qiaoce Ding,Dongying Chen,Jian-Rong Wang,Xuefeng Mei

Phytosterols are a class of natural steroids found in various plants. Commercially available phytosterols (PS) are primarily extracted from the deodorized distillate of soybean oil and consist predominantly of β-sitosterol with smaller amounts of stigmasterol and campesterol. Numerous studies have consistently demonstrated the significant lipid-lowering activity of PS. However, the application of PS is limited due to their low oral bioavailability. To enhance the water solubility and in turn the absorption of PS at the molecular level, microcapsule-like cocrystals were designed using bile acids via hydrogen bonding. As expected, four microcapsule-like cocrystals were successfully prepared: β-sitosterol with cholic acid (CA) and chenodeoxycholic acid (CDCA), and PS with CA and CDCA. The cocrystal of PS with CA (PS–CA) was selected for further investigation, and the results demonstrated that PS–CA exhibited significantly enhanced solubility in vitro and markedly improved oral bioavailability in vivo. Specifically, the AUC1–24 h of PS–CA was 6 times that of PS, while the Cmax was 4 times. Moreover, as a result of the improved bioavailability of PS, PS–CA showed superior lipid-lowering activity.

CAS / MDL: 474-25-9 81-25-4 83-48-7
研究领域: 药剂学 · 药物化学 · 分子药理学 · 生物药剂学 · 药物代谢 · 纳米医学 · 天然产物化学
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