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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 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
✓ 已验证 产品关联 DOI PubMed 高影响因子
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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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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
✓ 已验证 产品关联 DOI PubMed 高影响因子
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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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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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FOOD RESEARCH INTERNATIONAL · 2025 · IF 8

A comparative study on the bioactivities and chemical compositions of Dancong summer tea and Anhua dark tea: Excavation of glycolipid-lowering functional factors

Shiqiang Peng,Lianzhu Lin,Mouming Zhao

Drinking tea is beneficial to reduce the incidence of obesity. Unlike Fuzhuan brick tea (DT, a typical dark tea) widely reported to have good glycolipid-lowering activity (GLA), there is little information on GLA of Dancong summer tea (OT, a typical oolong tea). A comparative study on GLA and chemical compositions of OT and DT was systematically conducted. The results showed that OT had advantages in high content of polyphenols, leading to its better GLA including glycolipid digestion enzyme inhibitory activity and cholesterol micellar solubility inhibition activity than DT’s. A total of 21 compounds mainly including catechins, flavonoids, phenolic acids and phenylpropanoids were screened as the key differentially active micromolecules (KDAM) by UPLC-QTOF-MS/MS-based untargeted metabolomic analysis combined with multivariate analysis, which resulted in the difference of GLA between OT and DT. Moreover, the high affinity capacity and interaction mode between KDAM with α -glucosidase/ α -amylase/pancreatic lipase/cholesterol esterase were validated by molecular docking. Although the accumulation of polyphenols makes OT has a poor flavor as a beverage, our research demonstrated that OT with high content of polyphenols could be used in functional foods to facilitate the prevention of obesity.

CAS / MDL: 64-18-6
研究领域: 食品科学 · 营养学 · 植物化学
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BIOORGANIC CHEMISTRY · 2022 · IF 5.307

Discovery and structural optimization of 9-O-phenylsulfonyl-berberines as new lipid-lowering agents

Yuan Kong,Yong-Jia Yi,Xiao-Qing Liu,Pan Yu,Lin-Guo Zhao,Dong-Dong Li

Berberine is a quaternary isoquinoline alkaloid that exhibits potent hypoglycemic and hypolipidemic activity. Many medicinal chemists are currently working on structural modifications around the parent scaffold of berberine, expecting to further enhance its hypolipidemic activity and reducing its cytotoxicity. In this study, a focused berberine-like compound library containing 12,600 molecules was built via the introduction of various “drug-like” fragments at the C8 and C9 positions of berberine. Sixteen comopounds were hit by using the in-house QSAR models previously reported by our group. Considering synthesis feasibility and the cost of building-blocks, only four berberine analogs (library ID: 2028 , 3847 , 6033 , and 12456 ) were selected and synthesized for investigating their lipid-lowering activities. Preliminary lipid-lowering study showed that compound 12456 with the phenylsulfonyl group at the C9 position had potent cholesterol inhibitory activity in HepG2 cells, superior to that of the parent compound berberine. Subsequently, a total of twenty-five 9- O -phenylsulfonyl-berberines ( 1a - 1y ) and twenty-four 9- O -phenylsulfonyl-tetrahydroberberine ( 2a - 2x ) were designed, synthesized, and evaluated by lipid-lowering experiments. The results displayed that most compounds exhibited more lipid-lowering activities than berberine. Among them, compound 1m inhibited cholesterol production close to 50% in both cell models when compared with the blank control; the inhibition of triglycerides exceeded 70%. Moreover, 1m also had significant pharmacological effects on the inhibition of LDLC and promotion of HDLC production, especially in the HepG2 cell model, in which the inhibitory rate against LDLC was close to 70% and the increase rate of HDLC was more than 75%. The hypolipidemic experiment of SD rats demonstrated that after 40 days of administration ( 1m , 15 mg/kg/d), blood cholesterol was reduced by 19.6%, triglycerides reduced by 34.52%, and LDLC reduced by 41.49%, when compared with the high-fat diet model (HFD). In addition, after 80 days of administration, the three indexes of 1m were still better than that of berberine. Oil Red O staining and H&E staining results showed that 1m exhibited potent lipid scavenging activity. All in all, 1m was discovered and identified as a potent lipid-lowering agent and a new berberine-like candidate, being evaluated by subsequent studies.

研究领域: 药理学 · 药物化学
✓ 已验证 DOI PubMed 高影响因子
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PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY · 2020 · IF 1.415

Process optimization in ginseng fermentation by Monascus ruber and study on bile acid-binding ability of fermentation products in vitro

Chongyan Zhao,Fang Yang,Feng Lin,Qingsong Qu,Zhixun Li,Xing Liu,Lu Han,Xinyuan Shi

Ginseng (Panax ginseng C. A. Meyer) is a famous Traditional Chinese Medicine, which is widely used to treat cardiovascular disease. Monascus ruber (M. ruber) is a fungus used in food and medicine fermentation, and lovastatin, its metabolite, is used extensively in the treatment of dyslipidemia. In this study, ginseng has been fermented by M. ruber, and the response surface methodology (RSM) was applied to optimize fermentation parameters to obtain optimal fermentation system, with further exploring to lipid-lowering activity of P. ginseng C. A. Meyer–M. ruber fermentation products (PM). The concentration of ginseng, temperature, and rotating speed were set as variables and the lovastatin yield was optimized by a Box–Behnken design (BBD) analyzed by RSM. The binding capacity of PM for sodium taurocholate and sodium cholate was assayed by UV spectrophotometry. The highest content of lovastatin production (85.53 μg g−1) was obtained at a ginseng concentration of 1.96%, temperature of 30.11 °C, and a rotating speed of 160.47 rpm. PM exhibited bile acid binding capacity, which was stronger than unfermented ginseng. The RSM can be used to optimize the fermentation system to obtain the best fermentation process. In addition, the fermentation of ginseng by M. ruber can enhance the lipid-lowering effect.

CAS / MDL: 145-42-6
研究领域: 药理学 · 生物技术 · 中药学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Enzymatic hydrolysates of κ-carrageenan by κ-carrageenase-CLEA immobilized on amine-modified ZIF-8 confer hypolipidemic activity in HepG2 cells

Chunhua Zhu,Mingjing Mou,Leilei Yang,Zedong Jiang,Mingjing Zheng,Zhipeng Li,Tao Hong,Hui Ni,Qingbiao Li,Yuanfan Yang,Yanbing Zhu

κ-Carrageenase can degrade κ-carrageenan to produce bioactive κ-carrageenan oligosaccharides (KCOs) that have potential applications in pharmaceutical, food, agricultural, and cosmetics industries. Immobilized enzymes gain their popularity due to their good reusability, enhanced stability, and tunability. In this study, the previously characterized catalytic domain of Pseudoalteromonas purpurea κ-carrageenase was covalently immobilized on the synthesized amine-modified zeolitic imidazolate framework-8 nanoparticles with the formation of cross-linked enzyme aggregates, and the immobilized κ-carrageenase was further characterized. The immobilized κ-carrageenase demonstrated excellent pH stability and good reusability, and exhibited higher optimal reaction temperature, better thermostability, and extended storage stability compared with the free enzyme. The KCOs produced by the immobilized κ-carrageenase could significantly decrease the TC, TG, and LDL-C levels in HepG2 cells, increase the HDL-C level in HepG2 cells, and reduce the free fatty acids level in Caco-2 cells. Biochemical assays showed that the KCOs could activate AMPK activity, increase the ratios of p-AMPK/AMPK and p-ACC/ACC, and downregulate the expression of the lipid metabolism related proteins including SREBP1 and HMGCR in the hyperlipidemic HepG2 cells. This study provides a novel and effective method for immobilization of κ-carrageenase, and the KCOs produced by the immobilized enzyme could be a potential therapeutic agent to prevent hyperlipidemia.

研究领域: 生物化学 · 药学 · 生物技术 · 细胞生物学
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PLANTA MEDICA · 2022 ·Vol. 88 ·期 13 ·1190-1198 · IF 3.007

Phloridzin Highly Accumulated in Malus rockii Rehder and Its Structure Revision and Hypolipidemic Activity

Li-Juan Lang,Min Wang,Chang Lei,Yi Shen,Qi-Jie Zhu,Hong-Mei Diao,Hao Chen,Lei Shen,Xiang Dong,Bei Jiang,Chao-Jiang Xiao

Phloridzin is a lead compound of the prestigious antidiabetic gliflozins. The present study found that phloridzin highly accumulated in Malus rockii Rehder. The content of phloridzin in M. rockii was the highest among wild plants, with the percentage of 15.54% in the dry leaves. The structure of phloridzin was revised by proton exchange experiments and extensive 2D NMR spectra. Phloridzin exhibited significant hypolipidemic activity in golden Syrian hamsters maybe by increasing the expression of CYP7A1, at the doses of 50 mg/kg and 200 mg/kg. The total performance of anti-hyperlipidemic effect of phloridzin may be superior to that of lovastatin, though lovastatin was more active than phloridzin. In addition, phloridzin exhibited moderate antimalarial activity with inhibition ratio of 31.3 ± 10.9% at a dose of 25 mg/kg/day, and showed moderate analgesic activity with 28.0% inhibition at a dose of 50 mg/kg.

CAS / MDL: 53-86-1
研究领域: 药理学 · 植物学 · 生物化学 · 药物化学
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JOURNAL OF FOOD PROCESSING AND PRESERVATION · 2022 ·Vol. 46 ·期 7 ·e16603 · IF 2.609

Effects of ultrasonic-microwave assisted extraction with green solvent on the chemical constituents, antioxidant, and hypolipidemic activities of Manchurian walnut oil

Chang Liu,Hai-Yan Ni,Yuan-Hang Chang,Ze-Lin Wang,Ning Wan,Liu Cao,Zhi-Guo Liu,Yu-Jie Fu

A fast and efficient extraction method, ultrasonic-microwave-assisted extraction (UMAE) with a new green solvent Dimethyl carbonate (DMC), was developed for the extraction of Manchurian walnut kernel oil (MWKO). Through Box–Behnken design and analysis, the optimum extraction conditions were obtained: extraction time 28 min, liquid–solid ratio 7 ml/g, irradiation power 400 w, and the maximum extraction yield was 59.30%, which was 1.85-fold and 1.24-fold to that of ultrasonic-assisted extraction and Soxhlet extraction. Gas chromatography–mass spectrometry analysis showed that the unsaturated fatty acid content of the MWKO extracted with all three solvents was higher than 90%. The MWKO possessed stronger antioxidant activity with the tests of DPPH free radical scavenging, ABTS free scavenging, and ferric ion reducing ability. The lipid-lowering activity of MWKO was tested, and it was found that MWKO extracted by UMAE-DMC significantly inhibited lipid accumulation in HepG2 cells. In conclusion, UMAE-DMC is a perfect extraction method for selective extracting seed oil from plants. Practical applications In the present study, compared with the traditional method SE and UAE, UMAE-DMC has the advantages of shorter extraction time, higher extraction efficiency, and lower energy consumption. UMAE-DMC is a green and alternative extraction method for selective extracting of seed oil from plants. In addition, the MWKO possesses higher nutritional value and should be used as special edible oil for human health.

研究领域: 食品科学 · 植物化学
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