Food & Function
·
2019
·Vol. 11
·期 1
·1165-1175
·
IF 3.241
Xiaoxia Chen,Tianyu Li,Degang Qing,Jun Chen,Qian Zhang,Chunyan Yan
Humulus lupulus is a perennial climbing plant of the subfamily Cannabioideae native to the Northern Hemisphere. The primary use of H. lupulus is in the brewing industry, where it is an essential ingredient for imparting a unique flavor (bitterness and aroma) to beer. The female flowers of H. lupulus are also used in traditional Chinese medicine, but the biologically active ingredients underlying its benefits remain unclear. China is the largest producer and consumer of H. lupulus in Asia. Using the waste from the beer-brewing process of H. lupulus as raw materials, the biologically active polysaccharides can be screened. This is useful for the full utilization of H. lupulus, potentially leading to disease prevention and treatment. In this study, we isolated a homogeneous polysaccharide (HLP50-1) with a molecular weight of 49.13 kDa from female flowers of H. lupulus via a DEAE-Cellulose 52 anion exchange column and a Sephadex G-75 gel filtration column. Methylation, GC-MS, and NMR analyses revealed that the HLP50-1 comprised →4)-α-D-Glcp-(1→, →6)-α-D-Manp-(1→, →3)-α-L-Rhap-(1→, β-D-Glcp-(1→, α-L-Araf-(1→, →4,6)-2-OAc-β-D-Galp-(1→, β-D-Galp-(1→, →3,6)-β-D-Glcp-(1→, →2,3,4)-α-D-Xylp-(1→, →6)-α-D-Glcp-(1→, →3)-α-D-Galp-(1→, →4)-α-D-Galp-(1→. Advanced structural analysis showed that the HLP50-1 contained irregular fragments of different sizes and shapes with a smooth surface. The aggregates appeared be composed of accumulated crystals. Furthermore, the osteogenic activities of the HLP50-1 were evaluated via MC3T3-E1 cells in vitro. The results showed that 0.13 μM HLP50-1 led to outstanding proliferation, differentiation, and mineralization of the MC3T3-E1 cells. Therefore, HLP50-1 has osteogenic effects, and it may be a candidate for the treatment of osteoporosis. It has broad application prospects in functional foods, health-care products, and pharmaceuticals.
研究领域:
药理学
·
分子生物学
·
生物技术
✓ 已验证
DOI
PubMed
高影响因子
Food & Function
·
2019
·Vol. 10
·期 2
·824-835
·
IF 3.241
Xiaoxia Chen,Xin Hou,Degang Qing,Qian Zhang,Chunyan Yan
Humulus lupulus is distributed mainly in Asia, Europe, and North America, and the flowers and infructescences are used worldwide in beer brewing as an essential flavoring ingredient. In China, the main producing areas are the Xinjiang Uygur Autonomous Region and Gansu provinces. The annual production of H. lupulus in China accounts for about 13% of worldwide production, ranking third after the United States and Germany. The female flower of H. lupulus also is used in traditional Chinese medicine, but the bioactive components responsible for its benefits remain unclear. In this study, we isolated a homogeneous polysaccharide (HLP50-2) from female flowers of H. lupulus via DEAE-52 cellulose and Sephadex G-75 gel filtration chromatography. The molecular weight was 73.25 kDa. Chemical methods, gas chromatography-mass spectrometry, and nuclear magnetic resonance analyses showed that HLP50-2 consisted of →4)-β-D-GlcAp-(1→, →4)-α-L-Rhap-(1→, →5)-α-L-Araf-(1→, α-L-Araf-(1→, →3,6)-β-D-Galp-(1→, α-D-Galp-(1→, →3,4,6)-β-D-Galp-(1→, β-D-Xylp-(1→, →6)-α-D-Galp-(1→, and →4)-β-D-Galp-(1→. Advanced structural analysis indicated that HLP50-2 has a sheet-like structure with uneven distribution and the surface was smooth. In addition, we used MC3T3-E1 cells to evaluate the osteogenic activity of HLP50-2. The results show that HLP50-2 significantly promoted the proliferation, differentiation, and mineralization of MC3T3-E1 cells at concentrations of 12.5 μg mL−1 and 25 μg mL−1. In particular, at 25 μg mL−1, the promoting mineralization effect of HLP50-2 was better than that of the positive control, 17β-estradiol, and the alkaline phosphatase activity after 10 d of treatment was comparable to that of the positive control. The extraction, isolation, purification, structural identification, and osteogenic activity of H. lupulus polysaccharides suggest that homogeneous polysaccharide HLP50-2 has pronounced anti-osteoporosis activity. Therefore, it has broad application prospects in pharmaceutical industries and health-care products.
研究领域:
植物化学
·
药理学
·
生物医学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF FOOD AND DRUG ANALYSIS
·
2024
·Vol. 32
·期 4
·506
·
IF 2.6
Tian-Shuang Xia,Sheng-Yan Xu,Li-Yong Lai,Yi-Ping Jiang,Na-Ni Wang,Hai-Liang Xin
Bitter acids (BA) are main component of Humulus lupulus L. (hops). They are known for beer brewing and have various biological and pharmacological properties, especially the bone-protective effect confirmed by our previous in vivo study. Here we aimed to elucidate the anti-senior osteoporosis (SOP) effect of BA on osteoblasts and explore its underlying mechanism. In vitro SOP model was established by D-galactose (D-gal) injured osteoblasts, and the bone formation markers and apoptosis level were measured. mCherry-EGFP-LC3 adenovirus infection and autophagic markers including beclin1 and LC3 proteins were detected to investigate the autophagy level in osteoblasts. To further verify whether BA play the bone-protective role through regulating autophagy, the autophagy inhibitor 3-MA was used, and the cell proliferation, ALP activity, bone mineralization, apoptosis rate and SA-β-gal staining areas were measured. Finally, the protein expressions of AKT/mTOR signaling pathway were detected by Western blotting, and AKT agonist SC79 and mTOR agonist MHY1485 were used to further study the mechanism of BA on AKT/mTOR-mediated autophagy. The results showed that BA stimulated osteoblastic differentiation and inhibited apoptosis proteins Bcl-2/Bax in D-gal-treated osteoblasts. BA also increased the expression of autophagic markers beclin1 and LC3-II/LC3-I in D-gal-treated osteoblasts. mCherry-EGFP-LC3 autophagic double fluorescent adenovirus showed BA promoted the generation of autolysosomes and autophagosomes in D-gal-injured osteoblasts, indicating that BA might prevent osteoblastic bone loss through activating autophagy. Autophagy inhibitor 3-MA was used to further verify whether BA played the bone-protective role via regulating autophagy. The results revealed the promotion effects of BA on proliferation, ALP activity, and mineralized nodule formation in D-gal-injured osteoblasts were eliminated after autophagy blocking with 3-MA, and the inhibitory effects of BA on apoptosis rate and SA-β-gal staining areas were also eliminated. Moreover, BA reduced the phosphorylation levels of AKT, mTOR, p70S6K, and 4EBP in AKT/mTOR pathway, and the promotion of BA on the autophagic markers was blocked after the activation of AKT and mTOR by SC79 and MHY1485. In conclusion, it was the first time to demonstrate that BA improved cell activities and bone formation in aging osteoblasts, and revealed the mechanism of BA against SOP in osteoblasts was activating AKT/mTOR-mediated autophagy.
研究领域:
药理学
·
细胞生物学
·
分子生物学
·
老年医学
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产品关联
DOI
PubMed
高影响因子
FOOD CONTROL
·
2021
·
IF 5.548
Kai Hong,Zhenzhen Xu,Limin Wang,Agbaka Johnpaul,Yongqiang Cheng,Chenyan Lv,Changwei Ma
Humulus lupulus (hop) cone is a key ingredient in beer, which determines its taste and aroma. The impact of ripening on the bitter acids, aroma compounds, and polyphenols of hops has been reported separately, there is no systematic study on all three components. Here, three hop varieties (‘TP1’, ‘TP2’, and ‘QTF’) in China were sampled to investigate the correlation between the harvest maturity and these three components, which indicated that polyphenols synthesized earlier than hop bitter acids, followed by the aroma compounds. Variety differences of the hop cultivars prompted the obvious separation in the partial least-squares discriminant analysis (PLS-DA). Among three hop cultivars. ‘TP1’ with the highest contents of aroma compounds contributed to flower aroma, and with higher contents of bitter acids which contributed to bitter taste. In contrast, ‘TP2’ has been reported to be rich in caffeic acid, salicylic acid, syringaldehyde, (+)-catechin, and (−)-epicatechin. To analyze the hop aroma characteristics, two matrices of hop tea and late-hopped beer were prepared and used for sensory evaluation. Compared to ‘TP2’ and ‘QTF’, the hop tea with ‘TP1’ scored best for ‘strong’ (P < 0.01), ‘herbal’ (P < 0.05) and ‘citrus’ (P < 0.01). While the ‘strong’ and ‘herbal’ characteristics from terpene compounds receded in the late-hopped beer, the ‘citrus’ and ‘fruity’ notes from terpenol compounds remained noticeable.
研究领域:
植物科学
·
农学
·
食品科学
·
化学
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产品关联
DOI
高影响因子
ELECTROPHORESIS
·
2026
·
IF 2.6
Zhixu Chen,Biao Sun,Hanlin Zeng,Xinyang Li,Erwin Adams,Xiaoqi Zhang,Zhengjin Jiang,Jincai Wang
Neuraminidase inhibitors (NAIs) are a crucial therapy for combatting the influenza virus. This study employed an at-line nanofractionation technique to precisely localized potential NAIs in the extract of Humulus lupulus L. Twelve potential compounds, mainly phloroglucinol derivatives, were screened and identified. Seven of these compounds were subsequently isolated, purified, and structurally elucidated by NMR. Among them, Compound 5 showed remarkable inhibitory activity against both neuraminidase (NA, IC 50 = 0.8 µM) and the H3N2 influenza virus (EC 50 = 3.8 µM), confirming its potential as a lead compound for anti-influenza development. Compounds 4 and 8 , identified as hitherto uncharacterized phloroglucinol derivatives, also demonstrated significant inhibition against NA and the H3N2 influenza virus. Molecular docking revealed that Compounds 4 and 5 exhibited superior binding affinities compared to oseltamivir, with 4 forming critical hydrogen bonds with acidic residues (Glu119, Glu227, and Asp151) in the “150-cavity,” which significantly enhances its inhibitory potency against NAs.
✓ 已验证
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2021
·
IF 7.514
Limin Wang,Yunsen Zhang,I. Agbaka Johnpaul,Kai Hong,Yumei Song,Xiao Yang,Chenyan Lv,Changwei Ma
Hops are abundant in natural bioactive compounds. In this work, nine prenylated bitter compounds from hop were evaluated for their inhibitory activity against α-glucosidase. As a result, four flavonoids and one phloroglucinol (lupulone, LP) outperformed acarbose in inhibiting α-glucosidase. Isoxanthohumol (IX) and LP with two types of structures were selected for inhibition mechanism studies by spectroscopic methods and molecular dynamics simulation (MD). Results showed that IX acted as noncompetitive inhibitor and bound to α-glucosidase in allosteric sites via hydrogen bonds, hydrophobic, van der Waals (vdW), and electrostatic force, whereas LP was uncompetitive inhibitor and bound to catalytic sites via hydrophobic and vdW interactions. Notably, the conformation around binding site of α-glucosidase formed stable α-helix and tightened after binding IX and LP, respectively, which helped to elucidate noncompetitive and uncompetitive inhibitory mechanisms. This work demonstrated that two types of prenylated bitter compounds are discrepant in their mechanisms of interaction with α-glucosidase.
研究领域:
植物化学
·
生物化学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）