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1.
Carbohydr Polym ; 329: 121781, 2024 Apr 01.
Article En | MEDLINE | ID: mdl-38286551

Arabinogalactan (AG), a biologically active substance found abundantly in plants, is of significant interest in plant physiology due to its unique physicochemical properties. Yariv reagent, widely utilized in AG-II related applications, forms insoluble precipitates when bound to AG-II. This paper provides a comprehensive overview of the synthesis methods, physicochemical properties, and various dissociation methods of the Yariv reagent to enhance its utility in AG-II studies. Furthermore, the review explores the binding mechanisms and applications of the Yariv reagent, highlighting the advancements in studying the Yariv-AG complex in plant physiology. The aim of this review is to inspire new research ideas and foster novel applications of the Yariv reagent from synthesis to implementation.


Glucosides , Phloroglucinol , Glucosides/chemistry , Glucosides/metabolism , Phloroglucinol/chemistry , Plant Physiological Phenomena , Polysaccharides , Plant Proteins/metabolism , Mucoproteins/metabolism
2.
Carbohydr Polym ; 327: 121659, 2024 Mar 01.
Article En | MEDLINE | ID: mdl-38171656

Ophiopogonis Radix is a well-known Traditional Chinese Medicine and functional food that is rich in polysaccharides and has fructan as a characteristic component. In this study, an inulin neoseries-type fructan designated as OJP-W2 was obtained and characterized from Ophiopogonis Radix, and its potential therapeutic effect on liver fibrosis in vivo were investigated. Structural studies revealed that OJP-W2 had a molecular weight of 5.76 kDa and was composed of glucose and fructose with a molar ratio of 1.00:30.87. Further analysis revealed OJP-W2 has a predominantly lineal (1-2)-linked ß-D-fructosyl units linked to the glucose moiety of the sucrose molecule with (2-6)-linked ß-D-fructosyl side chains. Pharmacological studies revealed that OJP-W2 exerted a marked hepatoprotective effect against liver fibrosis, the mechanism of action was involved in regulating collagen deposition (α-SMA, COL1A1 and liver Hyp contents) and TGF-ß/Smads signaling pathway, alleviating liver inflammation (IL-1ß, IL-6, CCL5 and F4/80) and MAPK signaling pathway, and inhibiting hepatic apoptosis (Bax, Bcl-2, ATF4 and Caspase 3). These data provide evidence for expanding Ophiopogonis Radix-acquired fructan types and advancing our understanding of the specific role of inulin neoseries-type fructan in liver fibrosis therapy.


Fructans , Inulin , Humans , Fructans/pharmacology , Fructans/therapeutic use , Fructans/chemistry , Inulin/pharmacology , Inulin/therapeutic use , Liver Cirrhosis/drug therapy , Polysaccharides , Glucose
3.
Carbohydr Polym ; 327: 121669, 2024 Mar 01.
Article En | MEDLINE | ID: mdl-38171660

Steamed Polygonatum cyrtonema has been commonly used clinically for its gaining effect, whose main active ingredient is a polysaccharide. A water-soluble polysaccharide named PSP-W-1 was isolated from steamed Polygonatum cyrtonema. PSP-W-1 was characterized as a galactan having a backbone consisting predominately of 1,4-ß-linked Galp branched at the C-6 position by T-ß-linked Galp with a molecular weight of 14.4 kDa. PSP-W-1 could inhibit the overproduction of inflammatory factors and inflammatory mediators (iNOS, IL-6, COX-2) in dextran sodium sulfate-induced colitis mice. Oral administration of PSP-W-1 dramatically alleviated colonic pathological damage, repaired the intestinal barrier (occludin and ZO-1) and regulated the intestinal microbiota by increasing the abundance of norank_f_Muribaculaceae, Lactobacillus and norank_f_norank_o_Clostridia UCG-014, while decreasing the abundance of Bacteroides and Escherichia-Shigella to alleviate colitis symptoms. Overall, our findings suggest that PSP-W-1 might be a therapeutic option for both the prevention and treatment of colitis.


Colitis , Gastrointestinal Microbiome , Polygonatum , Animals , Mice , Colitis/chemically induced , Colitis/drug therapy , Intestines , Steam , Polysaccharides/pharmacology , Polysaccharides/therapeutic use , Colon , Dextran Sulfate , Mice, Inbred C57BL , Disease Models, Animal
4.
Carbohydr Polym ; 326: 121637, 2024 Feb 15.
Article En | MEDLINE | ID: mdl-38142102

Studies have shown that terrestrial acidic polysaccharides containing carboxyl groups and seaweed sulfated polysaccharides have strong potential in anti-liver fibrosis. However, there is no investigation on the anti-liver fibrosis of fructan, a ubiquitous natural polysaccharide. The present study aimed to understand the effect of fructan in ameliorating carbon tetrachloride (CCl4)-induced liver fibrosis in mice. Here, an inulin-like fructan ABWW from Achyranthes bidentata Bl. was characterized by fructose enzymatic hydrolysis, methylation analysis, ESI-MS, and NMR. It was composed of →2)-ß-d-Fruf-(1→ and →2)-ß-d-Fruf-(1, 6→, terminated with →1)-α-d-Glcp and →2)-ß-d-Fruf residues. The biological studies showed that ABWW could improve liver damage and liver fibrosis induced by CCl4in vivo and inhibit hepatic stellate cell (HSC) activation and migration in vitro. We further demonstrated that ABWW inhibited LX2 activation via suppressing the FAK/PI3K/AKT signaling pathway. Hence, ABWW might be a potential novel active compound for anti-fibrosis new drug development.


Inulin , Proto-Oncogene Proteins c-akt , Mice , Animals , Proto-Oncogene Proteins c-akt/metabolism , Inulin/metabolism , Phosphatidylinositol 3-Kinases/metabolism , Hepatic Stellate Cells , Signal Transduction , Liver Cirrhosis/chemically induced , Liver Cirrhosis/drug therapy , Liver Cirrhosis/metabolism , Carbon Tetrachloride , Liver/metabolism
5.
Carbohydr Polym ; 299: 120216, 2023 Jan 01.
Article En | MEDLINE | ID: mdl-36876818

An arabinogalactan (PTPS-1-2) was isolated and characterized from Pollen Typhae, and its potential antitumor effects on activating macrophages to produce immunomodulatory factors and promoting apoptosis in colorectal cancer cells were investigated. Structural characterization showed that PTPS-1-2 had a molecular weight of 59 kDa and was composed of rhamnose, arabinose, glucuronic acid, galactose, and galacturonic acid with a molar ratio of 7.6: 17.1: 6.5: 61.4: 7.4. Its backbone was predominantly composed of T-ß-D-Galp, 1,3-ß-D-Galp, 1,6-ß-D-Galp, 1,3,6-ß-D-Galp, 1,4-α-D-GalpA, 1,2-α-L-Rhap, additionally, branches contained 1,5-α-L-Araf, T-α-L-Araf, T-ß-D-4-OMe-GlcpA, T-ß-D-GlcpA and T-α-L-Rhap. PTPS-1-2 activated RAW264.7 cell by triggering the NF-kB signaling pathway and M1 macrophage polarization. Furthermore, the conditioned medium (CM) of Mφ pretreated with PTPS-1-2 exerted marked antitumor effects by inhibiting RKO cell proliferation and suppressing cell colony formation. Collectively, our findings suggested that PTPS-1-2 might be a therapeutic option for the prevention and treatment of tumors.


Apoptosis , Galactans , Macrophages , Galactose , Animals , Mice , RAW 264.7 Cells
6.
Carbohydr Polym ; 306: 120605, 2023 Apr 15.
Article En | MEDLINE | ID: mdl-36746571

Pectin exists extensively in nature and has attracted much attention in biological applications for its unique chemical and physical characteristics. Functionalized pectin, especially pectic conjugates, has given many possibilities for pectin to improve its properties and bioactivity as well as to deliver active molecules. To better exploit this strategy of pectic functionalization, this review presents in detail the structural modifications of pectin, different synthetic methods, and design strategies of pectic conjugates involving both traditional chemical and "green" approaches. Here, the research ideas and applications of pectic prodrugs as well as the development of preparation based on pectic conjugates are reviewed, with emphasis on crosslinking systems of functionalized pectin and nanosystems based on self-assembly techniques. We hope this review will provide comprehensive and valuable information for the functionalization and systematization of the pectic conjugate from synthesis to application.


Pectins , Pectins/chemistry
7.
Carbohydr Polym ; 303: 120452, 2023 Mar 01.
Article En | MEDLINE | ID: mdl-36657842

The pollen of Typha angustifolia L. decoction was clinically used to treat hyperlipidemia in China. A pectin polysaccharide (PTPS-2-2) was obtained from T. angustifolia pollen through water extraction, ion-exchange chromatography, and gel chromatography. Structural characterization showed that PTPS-2-2 had a molecular weight of 54 kDa and was composed of rhamnose, arabinose, xylose, galactose, and galacturonic acid with a molar ratio of 11.5: 36.5: 4.1: 36.7: 11.2. PTPS-2-2 consisted of rhamnogalacturonan I (RG-I) and arabinogalactan II (AG-II) domains. Its backbone was predominantly composed of →4-α-D-GalpA-(1 â†’ 2)-α-L-Rhap-(1→, with branches of 1,3-Galp, 1,6-Galp, 1,3,6-Galp, T-Araf, 1.5-Araf and T-Xylp, connected to the 4-position of 1,2-Rhap and the 3-position of 1,4-GalpA. The inhibitory effect of PTPS-2-2 on lipid accumulation was studied in vitro, using L02 cells induced by oleic acid. This experiment shows that PTPS-2-2 treatment at 100-400 µg/mL dose-dependently reduce cellular triglycerides (TG), cholesterol (TC), aspartate aminotransferase (AST), alanine aminotransferase (ALT) and malondialdehyde (MDA) levels, while elevated superoxide dismutase (SOD) levels. This indicated that PTPS-2-2 potentially ameliorated oleic acid-induced hepatic steatosis by inhibiting lipid accumulation and oxidative stress.


Oleic Acid , Typhaceae , Pectins/pharmacology , Pectins/chemistry , Polysaccharides/pharmacology , Polysaccharides/chemistry , Galactose/chemistry
8.
Int J Biol Macromol ; 229: 909-930, 2023 Feb 28.
Article En | MEDLINE | ID: mdl-36608864

The genus Polygonatum is gaining increasing attention from nutrition experts as well as health-conscious consumers because of its excellent performance in providing nutrients. Among these plants, Polygonatum sibiricum and Polygonatum odoratum have been selected for inclusion in China's Medicinal Food Directory due to their high safety profile. Polysaccharides are considered the main functional component and one of the main active ingredients of the plant. In addition, polysaccharides from genus Polygonatum have a variety of nutritional, biological and health-promoting properties, such as immunomodulatory, anti-inflammatory, cardiovascular protective, neuroprotective, antitumor, antidiabetic, antiosteoporosis, and hepatoprotective properties. This paper reviews the origin, extraction, purification, structural characteristics, biological activity, safety, toxicological evaluation, and structure-activity relationship of polysaccharides from the genus Polygonatum. Ultimately, we hope that this work can provide a more useful reference for understanding the polysaccharide structure and developing of new functional foods from polysaccharides of the genus Polygonatum.


Polygonatum , Polygonatum/chemistry , Polysaccharides/pharmacology , Polysaccharides/chemistry , Antioxidants/chemistry , Immunomodulation , Hypoglycemic Agents
9.
Int J Biol Macromol ; 230: 123252, 2023 Mar 01.
Article En | MEDLINE | ID: mdl-36639082

Nonalcoholic steatohepatitis (NASH) is a chronic liver disease characterized by inflammation and hepatic steatosis that may coincide with fibrotic activity. To date, no pharmacological agents have been approved for NASH treatment. Here, a homogeneous (1,3),(1,6)-ß-D-glucan (PUP-W-1, Mw: 41.07 kDa) was successfully purified from Polyporus umbellatus (Pers.) Fries sclerotia and characterized. The analysis showed that the PUP-W-1 backbone consisted of a repeating chain of eight →3)-ß-D-Glcp-(1 â†’ units, with branched chains of four ß-D-Glcp residues, joined by repeating 1,6-linkage units at the O-6 position of the backbone. The pharmacological effects of PUP-W-1 treatment in the context of NASH pathogenesis were explored using a methionine choline-deficient (MCD) diet-induced murine steatohepatitis model. The MCD model mice exhibited pronounced steatohepatitis, inflammatory activity, steatosis, stellate cell activation, and mild fibrotic activity. Treatment of the mice for three weeks with PUP-W-1 prevented the development of NASH due to the suppression of inflammation, lipid accumulation, and fibrosis. As suggested by these findings, PUP-W-1 may hold promise as a natural drug candidate or precursor for the treatment of NASH.


Non-alcoholic Fatty Liver Disease , Polyporus , Mice , Animals , Non-alcoholic Fatty Liver Disease/pathology , Glucans/pharmacology , Polyporus/chemistry , Diet , Choline/analysis , Methionine/analysis , Inflammation/pathology , Mice, Inbred C57BL , Liver
10.
Molecules ; 27(23)2022 Nov 29.
Article En | MEDLINE | ID: mdl-36500431

A rapid, sensitive, and specific LC-MS/MS method was developed and fully validated for the detection of paeoniflorin only in rat plasma, and applied to pharmacokinetic studies, including intravenous, multi-dose oral and combined administrations with verapamil. In this study, tolbutamide was used as the internal standard, and the protein precipitation extraction method, using acetonitrile as the extraction agent, was used for the sample preparation. Subsequently, the supernatant samples were analyzed on a Phenomenex Gemini® NX-C18 column with a flow rate of 1.0 mL/min in a gradient elution procedure. In the extracted rat plasma, the method exhibited high sensitivity (LLOQ of 1.0 ng/mL) upon selecting ammonium adduct ions ([M+NH4]+) as the precursor ions and good linearity over the concentration range of 1.0−2000 ng/mL, with correlation coefficients >0.99. The intra- and inter-batch accuracy RE% values were within ±8.2%, and the precision RSD% values were ≤8.1% and ≤10.0%, respectively. The results show that the method can be successfully applied to quantitate paeoniflorin in biological samples. Additionally, paeoniflorin is subsequently confirmed to be the substrate of the P-gp transporter in vivo and in vitro for the first time, which would be necessary and beneficial to investigate the clinical safety and efficacy of PF with other drugs in the treatment of rheumatoid arthritis.


Tandem Mass Spectrometry , Verapamil , Rats , Animals , Chromatography, Liquid/methods , Tandem Mass Spectrometry/methods , Monoterpenes/pharmacokinetics , Reproducibility of Results , Chromatography, High Pressure Liquid/methods
11.
Carbohydr Polym ; 296: 119952, 2022 Nov 15.
Article En | MEDLINE | ID: mdl-36088031

The gut cell wall is considered an impenetrable barrier to orally administrated polysaccharides. We recently reported a selective lymphatic route for Radix Astragali polysaccharide RAP to enter Peyer's patches (PPs) to trigger immune responses. However, how RAP enters PPs is unclear. Herein, we screened the intestinal epithelial cells of mice and found that the follicle-associated epithelium cells were specifically bound with FITC-RAP. Further studies in vitro and in vivo revealed that RAP was efficiently transported by microfold (M) cells. We also confirmed that M cell-transported RAP directly contacted dendritic cells. More importantly, for the first time, we verified this interesting M cell-mediated transcytosis of RAP in the human distal ileum. Mechanistically, we identified M cells to be the transporter cells that independently deliver RAP into the lymphatic system to trigger immune responses. This interesting transcytosis mechanism might apply to many other immunomodulatory polysaccharides orally dosed to human body.


Astragalus Plant , Peyer's Patches , Epithelial Cells/metabolism , Epithelium , Humans , Polysaccharides/metabolism , Polysaccharides/pharmacology
12.
Carbohydr Polym ; 293: 119741, 2022 Oct 01.
Article En | MEDLINE | ID: mdl-35798434

A homogalacturonan (HG) FPLP obtained from Ficus pumila L. was reported to have anti-diabetic activity but how this is influenced by degree of methyl-esterification (DM) of HG is unknown. To comprehensively analyze the role of DM in hypoglycemic activity in insulin-resistant HepG2 cells, HG derivatives (0 < DM < 100) were prepared from FPLP (DM25) by alkali or methanol acidified with acetyl chloride. Interestingly, a quadratic curve relationship revealed that hypoglycemic effect increased and then decreased with DM, and which was the most pronounced with DM54. DM might regulate activity by altering the intracellular drug concentration through cellular uptake. Furthermore, HG-DMn (0 < n < 100) were dependent on macropinocytosis, while HG-DMn (30 < n < 100) were also dependent on caveolae-mediated endocytosis. For HG, higher lipophilicity, smaller particle size, and more endocytosis mechanisms involved were favorable for cellular uptake, thereby increasing the intracellular drug concentration and enhancing the hypoglycemic activity. This work provides ideas for future investigations on structure-activity relationships.


Esters , Hypoglycemic Agents , Esters/pharmacology , Hep G2 Cells , Humans , Hypoglycemic Agents/pharmacology , Pectins/pharmacology
13.
Front Nutr ; 9: 914380, 2022.
Article En | MEDLINE | ID: mdl-35757268

Dendrobium officinale Kimura et Migo has been used as a traditional Chinese medicine (TCM) and a functional food for thousands of years. Carbohydrate is one of the most important effective substances and indicative components in D. officinale. However, since the qualitative and quantitative analysis of polysaccharides in D. officinale remains a challenge and limitation, herein, an oligosaccharide-quality marker approach was newly developed for quality assessment of D. officinale by spectrum-effect relationships between high performance liquid chromatographic (HPLC) fingerprints and anti-inflammatory effects. The HPLC fingerprints of 48 batches of oligosaccharides from D. officinale (DOOS) were developed and analyzed with similarity analysis (SA) and hierarchical cluster analysis (HCA), and eight common peaks were identified. In vitro screening experiment indicated that DOOS potentially inhibited nitric oxide (NO) production and effectively reduced the release of inflammatory cytokines, such as TNF-α, IL-6, and IL-1ß in RAW 264.7 cells, thereby reducing the inflammatory response of cells. Finally, the HPLC fingerprint of different batches of DOOS was combined with in vitro anti-inflammatory activity to assess the spectrum-effect relationships of DOOS by gray correlation analysis (GCA), in addition, the purified oligosaccharide components were identified and validated for NO inhibitory activity. Our results showed four DOOS (maltotetraose, maltopentaose, maltohexaose, and mannohexaose) were relevant to anti-inflammatory effects and could be as quality markers for the quality control of D. officinale. It suggests that the "oligosaccharide-spectrum-effect" relationships approach is a simple and reliable method for the quality control of herb medicines or nutritious foods.

14.
Carbohydr Polym ; 292: 119653, 2022 Sep 15.
Article En | MEDLINE | ID: mdl-35725160

Gut barrier makes a huge research gap between in vivo and in vitro studies of orally bioactive polysaccharides: whether/how they contact the related cells in vivo. A hyperbranched heteroglycan RAP from Radix Astragali, exerting antitumor and immunomodulatory effects in vitro and in vivo, is right an example. Here, we determined first that RAP's antitumor activity is immune-dependent. Being undegraded and non-absorbing, RAP quickly entered Peyer's patches (PPs) in 1 h where it directly targeted follicle dendritic cells and initiated antitumor immune responses. RAP was further delivered to mesenteric lymph node, bone marrow, and tumor. By contrast, the control Dendrobium officinale polysaccharide did not enter PPs. These findings revealed a blood/microbiota-independent and selective lymphatic route for orally administrated RAP to directly contact immune cells and trigger antitumor immune responses. This route bridges the research gap between the in vitro and in vivo studies and might apply to many other bioactive polysaccharides.


Drugs, Chinese Herbal , Peyer's Patches , Astragalus propinquus , Immunity , Polysaccharides/metabolism , Polysaccharides/pharmacology
15.
Chin Med ; 17(1): 56, 2022 May 12.
Article En | MEDLINE | ID: mdl-35549741

BACKGROUND: The unripe fruits of Rubus chingii Hu. ("Fu-peng-zi" in Chinese) is a well-known herbal tonic in traditional Chinese medicine (TCM) for tonifying liver and kidney. However, little is known regarding its therapeutic efficacy against liver fibrosis and the underlying mechanism. METHODS: The current research aims to explore the potential of Rubus chingii Hu. unripe fruits extract (RF) in the treatment of liver fibrosis and explore the underlying mechanism. RF was administered (450 and 900 mg·kg- 1 of body weight per day) orally to male C57BL/6 mice with CCl4-induced liver fibrosis for 3 weeks. The histopathological changes and fibrosis stage in liver tissue were assessed using hematoxylin and eosin (H&E) and Sirius red staining. The distribution of α-SMA and Col1A1 in the liver was analyzed to determine the hepatic stellate cells (HSCs) activation using immunohistochemistry and immunofluorescent analysis. Various biochemical markers in serum (ALT, AST) and liver (Hyp, IL1-ß, IL6, TNF-α and MCP-1) were observed to assess the liver's injury, fibrosis, and inflammation. In liver tissue, fibrosis-associated proteins including α-SMA, TGF-ß1, Smad2/3, p-Smad2/3, and Smad4 were detected through a Western blot assay. Pyrosequencing-based analysis of bacterial 16 S ribosomal RNA from variable regions V3-V4 of fecal samples characterized the gut microbiota. Spearman's rank correlation analysis was performed for the association between altered bacterial genera by RF and pharmacodynamics parameters. RESULTS: Three weeks of RF treatment can significantly lower liver inflammatory levels, pathological abnormalities, and collagen fibrous deposition in mice with CCl4-induced liver fibrosis. The expressions of α-SMA and Col1A1 were lowered by RF, while the expression levels of TGF-ß/Smads signaling pathway-related proteins, including TGF-ß1, p-Smad2/3, and Smad4, were dramatically decreased by RF. The RF treatment significantly increased or reduced 18 different bacterial species, restoring the CCl4-induced gut microbiota imbalance to the normal group's levels. According to correlation analysis, the bacterial genera Bifidobacterium and Turicibacter were the most significant in restoring CCl4-induced liver fibrosis. CONCLUSIONS: RF can reduce liver damage and delay the onset of liver fibrosis through modulating TGF-ß/Smads signaling pathway. Furthermore, RF's anti-liver fibrosis effect was related to balancing the gut microbial community, partly attained by increasing Bifidobacterium and Turicibacter in liver fibrosis.

16.
Int J Biol Macromol ; 194: 163-171, 2022 Jan 01.
Article En | MEDLINE | ID: mdl-34861274

In the present study, a water-soluble neutral polysaccharide (CAPW-1) with an average molecular weight of 64 kDa was purified from the root of Cynanchum atratum Bunge (Apocynaceae). The monosaccharide residue analysis revealed that CAPW-1 was composed of arabinose and galactose with a relative molar ratio of 7: 3. The backbone of CAPW-1 was consisted of 1,3-Galp and 1,3,6-Galp, the branches were attached to the O-6 of 1,3-Galp, and the side chains contained 1,6-Galp, 1,3,6-Galp, 1,5-linked, 1,3-linked, 1,3,5-linked, and terminal-Araf, which was attached to the O-3 of side 1,6-Galp. The bioactivity study indicated CAPW-1 could stimulate the proliferation of RAW264.7 cells and promote the secretion of nitric oxide (NO), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) with no cytotoxicity. The results suggested a potential application of CAPW-1 as an immunostimulant for the treatment of diseases such as infection and tumor.


Adjuvants, Immunologic/chemistry , Adjuvants, Immunologic/pharmacology , Galactans/chemistry , Galactans/pharmacology , Vincetoxicum/chemistry , Animals , Biomarkers , Chemical Phenomena , Galactans/isolation & purification , Humans , Hydrolysis , Immunomodulation/drug effects , Macrophages/drug effects , Macrophages/immunology , Macrophages/metabolism , Mice , Molecular Structure , Molecular Weight , Monosaccharides/chemistry , RAW 264.7 Cells , Spectrum Analysis
17.
Food Funct ; 12(12): 5399-5406, 2021 Jun 21.
Article En | MEDLINE | ID: mdl-33988204

Inhibition of glucose uptake in the intestine through sodium-dependent glucose transporter 1 (SGLT1) or glucose transporter 2 (GLUT2) may be beneficial in controlling postprandial blood glucose levels. Gallic acid and ten of its derivatives were identified in the active fractions of Terminalia chebula Retz. fructus immaturus, a popular edible plant fruit which has previously been associated with the inhibition of glucose uptake. Gallic acid derivatives (methyl gallate, ethyl gallate, pentyl gallate, 3,4,6-tri-O-galloyl-ß-d-glucose, and corilagin) showed good glucose transport inhibition with inhibitory rates of 72.1 ± 1.6%, 71.5 ± 1.4%, 79.9 ± 1.2%, 44.7 ± 1.2%, and 75.0 ± 0.7% at 5 mM d-glucose and/or 56.3 ± 2.3, 52.1 ± 3.2%, 70.2 ± 1.7%, 15.6 ± 1.6%, and 37.1 ± 0.8% at 25 mM d-glucose. However, only 3,4,6-tri-O-galloyl-ß-d-glucose and corilagin were confirmed GLUT2-specific inhibitors. Whilst some tea flavonoids demonstrated minimal glucose transport inhibition, their gallic acid derivatives strongly inhibited transport effect with GLUT2 specificity. This suggests that gallic acid structures are crucial for glucose transport inhibition. Plants, such as T. chebula, which contain high levels of gallic acid and its derivatives, show promise as natural functional ingredients for inclusion in foods and drinks designed to control postprandial glucose levels.


Biological Transport/drug effects , Gallic Acid/chemistry , Gallic Acid/pharmacology , Glucose/metabolism , Plant Extracts/pharmacology , Postprandial Period/drug effects , Caco-2 Cells , Flavonoids , Fruit/chemistry , Gallic Acid/analogs & derivatives , Glucose Transporter Type 2 , Glucosides , Humans , Hydrolyzable Tannins , Intestines , Sodium-Glucose Transporter 1 , Terminalia/drug effects
18.
Biomed Pharmacother ; 137: 111338, 2021 May.
Article En | MEDLINE | ID: mdl-33578234

Polysaccharide is one of main components in Polygonatum sibiricum (PS), which is an herbal medicine widely used in East Asia. Polysaccharides from Polygonatum sibiricum has been shown to exhibit multiple biological activities, such as anti-diabetes, anti-inflammation, antioxidant, immunity modulation, and anticancer. Since hematopoietic system is one of determinant factors in cancer control, we here explored the effect of polysaccharide-rich extract from Polygonatum sibiricum (PREPS) on hematopoiesis in the mice bearing triple negative breast cancer (TNBC). We found that the 4T1 TNBC tumor significantly increased myeloid cells in peripheral blood, bone marrow and spleen, while decreasing bone marrow hematopoietic stem and progenitor cells (HSPCs), indicative of an inhibition of medullary hematopoiesis. When 4T1 TNBC tumor-bearing mice were treated with PREPS, the percentage of myeloid cells within tumor-infiltrating immune cells was reduced. In addition, PREPS also inhibited hematopoietic cell expansion in the spleen, which was induced by TNBC tumors. Importantly, PREPS markedly increased HSPCs and common lymphoid progenitors in the bone marrow that had been suppressed by TNBC tumors. These findings suggest that PREPS protect hematopoiesis inhibited by TNBC tumors in the bone marrow. Although PREPS alone did not achieve statistical significance in the suppression of TNBC tumor growth, it may have a long-lasting anti-tumor effect to assist TNBC therapies by sustaining hematopoiesis and lymphoid regeneration in bone marrow.


Bone Marrow/drug effects , Drugs, Chinese Herbal/pharmacology , Hematinics/pharmacology , Hematopoiesis/drug effects , Polygonatum/chemistry , Polysaccharides/pharmacology , Triple Negative Breast Neoplasms/metabolism , Animals , Cell Proliferation/drug effects , Disease Models, Animal , Drugs, Chinese Herbal/isolation & purification , Drugs, Chinese Herbal/therapeutic use , Female , Hematinics/isolation & purification , Hematinics/therapeutic use , Hematopoietic Stem Cells/drug effects , Hematopoietic Stem Cells/metabolism , Mice , Mice, Inbred BALB C , Plants, Medicinal/chemistry , Polysaccharides/isolation & purification , Polysaccharides/therapeutic use , Protective Agents/pharmacology , Spleen/drug effects , Tumor-Associated Macrophages/drug effects , Tumor-Associated Macrophages/metabolism
19.
Front Pharmacol ; 11: 558471, 2020.
Article En | MEDLINE | ID: mdl-33381024

Wei-Fu-Chun (WFC) tablet is a commercial medicinal product approved by China Food and Drug Administration, which is made of Panax ginseng C.A.Mey., Citrus aurantium L., and Isodon amethystoides (Benth.). WFC has been popularly used for the treatment of precancerous lesions of gastric cancer (PLGC) in clinical practice. In this study, a UHPLC-ESI-Q-TOF/MS method in both positive and negative ion mode was employed to rapidly survey the major constituents of WFC. 178 compounds including diterpenoids, triterpenes, sesquiterpenes, flavonoids, saponins, phenylpropanoids, lignans, coumarins, organic acids, fatty acids, quinones, and sterols, were identified by comparing their retention times, accurate mass within 5 ppm error, and MS fragmentation ions. In addition, 77 absorbed parent molecules and nine metabolites in rat serum were rapidly characterized by UHPLC-ESI-Q-TOF/MS. The network pharmacology method was used to predict the active components, corresponding therapeutic targets, and related pathways of WFC in the treatment of PLGC. Based on the main compounds in WFC and their metabolites in rat plasma and existing databases, 13 active components, 48 therapeutic targets, and 61 pathways were found to treat PLGC. The results of PLGC experiment in rats showed that WFC could improve the weight of PLGC rats and the histopathological changes of gastric mucosa partly by inhibiting Mitogen-activated protein kinase (MAPK) signaling pathway to increase pepsin secretion. This study offers an applicable approach to identify chemical components, absorbed compounds, and metabolic compounds in WFC, and provides a method to explore bioactive ingredients and action mechanisms of WFC.

20.
Carbohydr Polym ; 248: 116780, 2020 Nov 15.
Article En | MEDLINE | ID: mdl-32919569

In this study, the beneficial effects of a homogalacturonan(HG)-type pectic polysaccharide from Ficus pumila L. fruits (FPLP) in obese mice were investigated. The 17-week FPLP treatment effectively attenuated obesity, as mainly demonstrated by the reductions of body weight, serum total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) levels in high-fat diet (HFD)-induced obese mice. The decreased Firmicutes to Bacteroidetes abundance ratio, enriched Akkermansia, and reduced Blautia abundance suggested that FPLP ameliorated the HFD-induced gut dysbiosis. FPLP also influenced the levels of metabolites altered upon HFD feeding, including increases in myristoleic acid and pentadecanoic acid levels. The correlation studies indicated that FPLP ameliorated HFD-induced rise in TC and LDL-C levels through regulating gut microbial community and their associated metabolites. In conclusion, this study extends our understanding of the relationships among gut microbiota (Akkermansia and Blautia), metabolites (myristoleic acid and pentadecanoic acid), HG-type pectin and its TC- and LDL-C- lowering functions.


Gastrointestinal Microbiome/drug effects , Gastrointestinal Tract/drug effects , Obesity/prevention & control , Pectins/pharmacology , Polysaccharides/pharmacology , Akkermansia/drug effects , Animals , Bacteroidetes/drug effects , Body Weight/drug effects , Diet, High-Fat/adverse effects , Dysbiosis/etiology , Dysbiosis/prevention & control , Ficus/chemistry , Firmicutes/drug effects , Fruit/chemistry , Gastrointestinal Tract/metabolism , Gastrointestinal Tract/microbiology , Male , Mice, Inbred C57BL , Obesity/etiology , Pectins/administration & dosage , Polysaccharides/administration & dosage , Population Dynamics
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