RESUMO
Cancer treatment faces numerous challenges, such as inadequate drug targeting, steep price tags, grave toxic side effects, and limited therapeutic efficacy. Therefore, there is an urgent need for a safe and effective new drug to combat cancer. Microbial polysaccharides, complex and diverse biological macromolecules, exhibit significant microbial variability and uniqueness. Studies have shown that terrestrial microbial polysaccharides possess a wide range of biological activities, including immune enhancement, antioxidant properties, antiviral effects, anti-tumour potential, and hypoglycemic functions. To delve deeper into the structure-activity relationship of these land-based microbial polysaccharides against cancer, we conducted a comprehensive review and analysis of anti-cancer literature published between 2020 and 2024. The anticancer efficacy of terrestrial microbial polysaccharides is influenced by multiple factors, including the microbial species, existing form, chemical structure, and polysaccharide purity. According to the literature, an optimal molecular weight and good water solubility are essential for demonstrating anticancer activity. Furthermore, the addition of mannose and galactose has been found to significantly enhance the anticancer properties of these polysaccharides. These insights will serve as a valuable reference for future research and progress in the field of cancer drug therapy, particularly with regards to terrestrial microbial polysaccharides.
Assuntos
Antineoplásicos , Neoplasias , Humanos , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Neoplasias/tratamento farmacológico , Polissacarídeos/química , Polissacarídeos/uso terapêutico , Polissacarídeos/farmacologia , Polissacarídeos Bacterianos/química , Polissacarídeos Bacterianos/farmacologia , Polissacarídeos Bacterianos/uso terapêutico , Relação Estrutura-Atividade , Animais , Polissacarídeos Fúngicos/química , Polissacarídeos Fúngicos/farmacologia , Polissacarídeos Fúngicos/uso terapêuticoRESUMO
To comprehensively study the ginsenosides distribution in the various tissues of American ginseng, the qualitative and quantitative-targeted and nontargeted mass spectroscopic methods were established using the high-performance liquid chromatography coupled with Qtrap triple quadrupole mass spectrometry (HPLC-QtrapQQQ-MS). The total ginsenosides of the root, stem, and leaf of American ginseng were determined by a colorimetric method, and the contents showed the order from high to low root, stem, and leaf. Eighty-two kinds of ginsenosides were detected in the different parts of American ginseng by enhanced mass scan-information-dependent data acquisition (IDA)-enhanced product ion (EPI) scan mode, including 69 from the root, 62 from the stem, and 48 from the leaf. An HPLC-multiple reaction monitoring (MRM) method was established, and 28 representative ginsenosides were further quantified in the three parts. Nearly all ginsenosides had the highest contents in the root and the lowest content in the leaf. Three types of ginsenosides (protopanaxadiol [PPD]-, protopanaxatiol [PPT]-, and oleanolic acid [OA]-types) were analyzed by precursor ion-IDA-EPI and MRM-IDA-EPI scan modes. Root had the most abundant ginsenosides in PPD- and PPT-type ginsenosides. Meanwhile, the OA-type ginsenosides are significantly enriched in the stem and leaf of American ginseng. The results provided a supplement to the quality assessment of American ginseng. PRACTICAL APPLICATION: The distribution profile of ginsenosides in the parts of American ginseng is different. Except for the root, the stem, and leaf of American ginseng have the most abundant ginsenosides in oleanolic acid type. The results reported herein can help the manufacturers choose appropriate materials to extract the ginsenosides.
Assuntos
Ginsenosídeos , Ácido Oleanólico , Panax , Espectrometria de Massas em Tandem/métodos , Panax/química , Cromatografia Líquida de Alta Pressão/métodosRESUMO
Co-assembled foxtail millet (FP)-sodium casein (NaCas) nanocomplex and NaCas coated FP nanoparticles (NPs) were produced by using pH-cycle and anti-solvent methods, respectively. Subsequently, the effects of chitosan hydrochloride (CHC) coating on the particle size, surface charge and physicochemical stability of the two different FP/NaCas nanoparticles (NPs) were evaluated. With the addition of CHC, the particle size of NaCas coated FP NPs and co-assembled FP-NaCas nanocomplex significantly increased from 128.3 nm and 69.5 nm to 183.5 nm and 113.8 nm, respectively. The stability of the two kinds of CHC coated FP-based NPs to different pH values and varying ionic strengths was different due to their different NP structures. Using different fabrication formulations, co-assembled FP-NaCas NPs entrapped curcumin in relatively hydrophilic microenvironment and showed higher curcumin retention rate in comparison with NaCas coated FP NPs in terms of long-term storage stability. The results revealed that the produced CHC coated FP/NaCas nanocomplexes could be very beneficial in entrapping and delivering bioactive substances.
Assuntos
Quitosana , Curcumina , Nanopartículas , Setaria (Planta) , Curcumina/química , Caseínas/química , Quitosana/química , Prolaminas , Nanopartículas/química , Tamanho da Partícula , Concentração de Íons de Hidrogênio , Portadores de Fármacos/químicaRESUMO
In addition to its high nutritious value, sea cucumber has been recognized by folk medicine for a long time. This study investigated the structure and hyperglycemic activity of a neutral polysaccharide (NPsj) from sea cucumber Stichopus japonicus, whose molecular weight was determined as 301.75 kDa by HPGPC method. Monosaccharide composition analysis indicated that NPsj is a glucan. The structure of NPsj was obtained by combining the analysis of methylation analysis, FTIR, NMR, periodate oxidation, Smith degradation and ESI-MS, which is mainly composed of (1 â 4)-α-d-glucoses with ß-d-glucose(1â) branches substituted at O-6 every 7-9 of 1,4 linked glucoses. An in vitro insulin resistance Hep G2 cells model and a 3 T3-L1 cells model were established, and the NPsj has significant effect to increase glucose consumption with no toxicity at 10-100 µg/mL. Furthermore, NPsj upregulates the phosphorylation of Akt1 and down-regulated GSK3ß, and then reduces the phosphorylation of GS, indicating its mechanism of ameliorating insulin resistance via Akt/GSK3ß/GS signaling pathway.
Assuntos
Resistência à Insulina , Pepinos-do-Mar , Stichopus , Animais , Glicogênio Sintase Quinase 3 beta/metabolismo , Hipoglicemiantes/metabolismo , Hipoglicemiantes/farmacologia , Polissacarídeos/metabolismo , Polissacarídeos/farmacologia , Pepinos-do-Mar/química , Stichopus/metabolismoRESUMO
Fucosylated chondroitin sulfate was obtained from the sea cucumber Holothuria fuscogilva (FCShf). The structure was elucidated by NMR and HILIC-FTMS analysis. FCShf contained a chondroitin core chain [â3)-ß-D-GalNAc-(1 â 4)-ß-D-GlcA-(1â]n, where the sulfation positions were the O-4 or O-6 of the GalNAc residues. The ratio of sulfated and non-sulfated GalNAc at O-6 was 1:2, while the ratio of GalNAc at O-4 was 1:1. 2,4-disulfated-fucose (Fuc2,4S), 4-sulfated-fucose (Fuc4S) and 3,4-disulfated-fucose (Fuc3,4S) were attached to the O-3 of GlcA with a molar ratio of 1.00: 0.62: 1.32. The FCShf could significantly promote the proliferative rate, NO production and neutral red uptake of RAW 264.7 cells within the concentration range of 10-300 µg/mL. Compared with the fucosylation and deacetylation degrees, the molecular weight of FCShf had markedly influence on the activation of RAW 264.7 cells. A decrease in molecular weight dramatically improved the immunoregulatory activities. Furthermore, FCShf activated RAW 264.7 cells through TLR-2/4-NF-κB pathway.
Assuntos
Holothuria , Pepinos-do-Mar , Animais , Sulfatos de Condroitina/química , Fucose/química , Holothuria/metabolismo , Camundongos , Células RAW 264.7 , Pepinos-do-Mar/química , Sulfatos/metabolismoRESUMO
In this study, curcumin (Cur)-loaded chondroitin sulfate (CS)-sodium caseinate (NaCas)-stabilized foxtail millet prolamin (FP) composite nanoparticles (NPs) were fabricated via a one-pot process. FP is capable of self-assembly via liquid antisolvent precipitation under neutral and alkaline conditions (pH 7.0-11.0). Under this condition, the microstructures of hydrophobic FP cores, amphiphilic NaCas and hydrophilic CS shells were fabricated readily by a one-pot method. With an optimal FP/NaCas/CS weight ratio of 3 : 2 : 4, FP-NaCas-CS NPs shared globular microstructures at about 145 nm, and hydrophobic interactions, electrostatic forces, and hydrogen bonds were the main driving forces for the formation and maintenance of stable FP-NaCas-CS NPs. CS coating enhanced the pH stability but reduced the ionic strength stability. The formed NPs were stable over a wide pH range from 2.0 to 8.0 and elevated salt concentrations from 0 to 3 mol L-1 NaCl. FP-NaCas-CS NPs exhibited a higher Cur encapsulation efficiency of 93.4% and re-dispersion capability after lyophilization. Moreover, CS coating promoted selective accumulation in CD44-overexpressing HepG2 cells, resulting in higher inhibition of tumor growth compared to free Cur and FP-NaCas NP-encapsulated Cur. As for comparison, encapsulated Cur exhibited reduced cytotoxicity on normal liver cells L-O2. This preclinical study suggests that FP-NaCas-CS NPs could be very beneficial in terms of encapsulating hydrophobic drugs, improving the effectiveness of cancer therapies and reducing side effects on normal tissues.
Assuntos
Curcumina , Nanopartículas , Neoplasias , Setaria (Planta) , Caseínas/química , Sulfatos de Condroitina/química , Curcumina/química , Humanos , Nanopartículas/química , Tamanho da Partícula , ProlaminasRESUMO
Foxtail millet nanoparticles with smaller mean size at â¼130 nm and narrower polydispersity index at â¼0.05 were prepared in citric acid-potassium phosphate buffer (pH 8.0). Through lecithin (Lec)/sodium alginate (Alg) coating, a hydrophobic FP core, a Lec monolayer, and a hydrophilic Alg shell were formed spontaneously. Dissociation experiment revealed that electrostatic interaction and hydrogen bonding were main driving forces for the formation and maintenance of stable FP-Lec/Alg NPs. In addition, Lec/Alg coated NPs exerted an important role in sustaining the controlled release of the encapsulated quercetin under simulated gastrointestinal tract conditions. Cellular uptake test exhibited that FP-Lec-Alg NPs cold enter epithelial cells in a time-dependent manner, showing the maximum uptake efficiency were 22% and 24%, respectively, after 2 h of incubation. About 220 nm NPs can be recovered by adding 10% (w/v) sucrose. FP-Lec-Alg NPs were found to be promising delivery materials to deliver quercetin and improve its bioavailability.
Assuntos
Nanopartículas , Setaria (Planta) , Alginatos/química , Ácido Cítrico , Lecitinas , Nanopartículas/química , Fosfatos , Compostos de Potássio , Prolaminas , Quercetina , SódioRESUMO
The development of food proteins as effective delivery systems is of great significance for the encapsulation of active compounds. Foxtail millet prolamin (FP) has a high level of hydrophobic amino acids and proline, meets the basic characteristics of delivery system, and was described here for the first time as an effective delivery system for the encapsulation of curcumin. The interaction between FP and curcumin was confirmed by fluorescence spectroscopy, showing the joint driving of hydrophobic forces and hydrogen bonds. Curcumin-loaded caseinate-stabilized FP nanodispersions were prepared by anti-solvent/evaporation method. The mean particle size was about 220-235 nm, sharing features of a spherical shape, uniform particle size, and smooth surfaces. High level of curcumin was encapsulated in the FP-based nanoparticles, exhibiting high particle yield (>88.4%) and encouraging encapsulation efficiency (>71.3%). X-ray diffraction and Fourier transform infrared spectroscopy demonstrated that the encapsulated curcumin was amorphous state and interacted with proteins via non-covalent bonds. The nano-sized particles can effectively prevent the degradation of curcumin during heat treatment, and significantly enhance the antioxidant and anti-tumor properties. This study provides a new encapsulant for effective protection and targeted delivery of hydrophobic active biomolecules.
Assuntos
Curcumina , Nanopartículas , Setaria (Planta) , Portadores de Fármacos , Tamanho da Partícula , ProlaminasRESUMO
A fucosylated chondroitin sulfate was isolated from the body wall of sea cucumber Stichopus japonicus (FCSsj), whose structure was characterized by NMR spectroscopy and HILIC-FTMS. At the ratio of 1.00:0.26:0.65, three fucosyl residues were found: 2,4-disulfated-fucose (Fuc2,4S), 4-sulfated-fucose (Fuc4S) and 3,4-disulfated-fucose (Fuc3,4S), which were only linked to the O-3 of glucuronic acid residues (GlcA). Besides mono-fucosyl moieties, di-fucosyl branches, namely Fuc2,4Sα(1â3)Fuc4S, were also found to be attached to the O-3 of GlcA. The antidiabetic activity of FCSsj was evaluated using glucosamine induced insulin resistant (IR) Hep G2 cells in vitro. It was found that FCSsj significantly promoted the glucose uptake and glucose consumption of IR-Hep G2 cells in a dose-dependent manner, and could alleviate the cell damage. Furthermore, FCSsj could promote the glycogen synthesis in the glucosamine-induced IR-Hep G2 cells. These results provided a supplement for studying the antidiabetic activity of FCSsj.
Assuntos
Sulfatos de Condroitina/química , Sulfatos de Condroitina/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Stichopus/química , Animais , Fucose/química , Glucose/metabolismo , Ácido Glucurônico/química , Glicogênio/metabolismo , Células Hep G2 , Humanos , Resistência à Insulina , Espectroscopia de Ressonância Magnética/métodos , Pepinos-do-Mar/químicaRESUMO
Sea cucumber (Stichopus japonicus) is a high-protein food with the potential to release certain peptides through enzymolysis. This work is to explore the characteristics of peptides released from Stichopus japonicus protein in the process of digestion. Hydrolysates were obtained by gastrointestinal digestion and fractioned to <3, 3-10, 10-30 and >30â¯kDa fractions. Fifty-eight peptides from <3â¯kDa fraction were characterized using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Hydrolysates could improve glucose uptake of 3â¯T3-L1 cells and high insulin-induced insulin-resistant Hep G2 cells. Molecular docking showed that the released peptides had similar binding mode with anagliptin, a dipeptidyl peptidase IV (DPP-IV) inhibitor. The <3â¯kDa fraction in gastro and intestinal digestion showed the greatest DPP-IV inhibitory potency (IC50 0.51 and 0.52â¯mg/mL, respectively). The results indicated that sea cucumber could be used as a functional food to release antidiabetic peptides through gastrointestinal digestion.
Assuntos
Hipoglicemiantes/farmacologia , Peptídeos/análise , Peptídeos/farmacologia , Stichopus/química , Células 3T3-L1 , Animais , Cromatografia Líquida , Digestão , Dipeptidil Peptidase 4/química , Dipeptidil Peptidase 4/metabolismo , Inibidores da Dipeptidil Peptidase IV/química , Inibidores da Dipeptidil Peptidase IV/farmacologia , Células Hep G2 , Humanos , Hidrólise , Hipoglicemiantes/metabolismo , Camundongos , Simulação de Acoplamento Molecular , Peptídeos/química , Stichopus/metabolismo , Espectrometria de Massas em TandemRESUMO
Inulavosin, a natural melanogenesis inhibitor, has been synthesized smoothly from readily available and inexpensive starting materials by using a Ga(OTf)3-catalyzed room temperature hetero Diels-Alder dimerization of salicyl alcohol derivative and a regioselective phenol monobromination as the key steps.