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Bone metastases are common in malignant tumors and the effect of conventional treatment is limited. How to effectively inhibit tumor bone metastasis and deliver the drug to the bone has become an urgent issue to be solved. While bone targeting drug delivery systems have obvious advantages in the treatment of bone tumors. The research on bone-targeted anti-tumor therapy has made significant progress in recent years. We introduced the related tumor pathways of bone metastases. The tumor microenvironment plays an important role in metastatic bone tumors. We introduce a drug-loading systems based on different environment-responsive nanocomposites for anti-tumor and anti-metastatic research. According to the process of bone metastases and the structure of bone tissue, we summarized the information on bone-targeting molecules. Bisphosphate has become the first choice of bone-targeted drug delivery carrier because of its affinity with hydroxyapatite in bone. Therefore, we sought to summarize the bone-targeting molecule of bisphosphate to identify the modification effect on bone-targeting. And this paper discusses the relationship between bisphosphate bone targeting molecular structure and drug delivery carriers, to provide some new ideas for the research and development of bone-targeting drug delivery carriers. Targeted therapy will make a more outstanding contribution to the treatment of tumors.

Organogels are excellent drug carrier for controlled release. Organogels based on amino acid derivatives has been widely used in the area of drug delivery. In this study, a series of the organogel system based on amino acid derivatives gelators was designed and prepared to investigate the structure-property correlation in organogels. To investigate the factors that influence the property of drug release, we varied the formulation in the organogels: gelator structure, gelator concentration, volume of antigelation solvent, and drug loading. Through the Box–Behnken tests, the optimum organogel formulation in vitro was obtained. The self-healing properties of the organogel have been utilised for injection of a model lipophilic risperidone in situ, and sustained release of the drug has been studied over about one week in vivo. In conclusion, the gelation ability of gelators could be adjusted by the gelator structure. Gel property is related with the whole composition of the formulation. As drug carrier, the drug release property of organogels is affected by multiple factors. Our investigation of the gel release property will play a theoretical guiding role in the application in the in situ drug delivery system.

This study investigated the structural elucidation, anti-radical and immunomodulatory activities of polysaccharides from the roots of Glehnia littoralis. A crude polysaccharide was extracted from the roots of G. littoralis through the ultrasonic-assisted extraction and further purified by DEAE-52 cellulose and Sephadex G-100 gel column, a major polysaccharide fraction named GLP80-1 was obtained. The chemical properties and structure of GLP and GLP80-1 were characterized by acid hydrolysis, methylation analysis, along with high performance gel permeation chromatography, Fourier transform infrared, nuclear magnetic resonance, scanning electron microscope, thermogravimetric analysis and X-ray diffraction. The molecular weight distributions of GLP were determined as 1.89 × 106 and 1.26 × 104 Da. The monosaccharide composition of GLP was glucose, glucuronic acid, galactose and arabinose with molar ratios of 0.91:0.04:0.03:0.02, respectively. The average molecular weight of GLP80-1 was determined as 1.63 × 104 Da. The structure of GLP80-1 was deduced to be a homogenous glucan, comprised a main chain of (1→4)-linked-α-D-Glcp with a single α-D-Glcp branch substituted at C-6. The results of biological activities in vitro showed that GLP and GLP80-1 exhibited free radical scavenging effects, and displayed promotion for the proliferation of mouse spleen lymphocytes and RAW264.7 cells. The data indicated that GLP and GLP80-1 had the potential to be explored as novel natural antioxidant and immunomodulator for application in functional food.

Polysaccharide was one of the considered major active ingredient in

The preparation conditions of Glehniae Radix polysaccharide-iron complex (GLP80-Fe) were optimized and the physicochemical properties were characterized by Ultraviolet-visible spectroscopy (UV-Vis), Fourier Transform Infrared Spectroscopy (FT-IR), X-ray diffraction (XRD), Transmission electron microscope (TEM), Thermogravimetric analyzer, and Differential scanning calorimetry (TGA-DSC), respectively. The stability and reducibility of GLP80 and GLP80-Fe were analyzed, and the monosaccharide composition was determined by gas chromatograph (GC). In vitro antioxidant activity of GLP80 and GLP80-Fe were evaluated by determining the radical (DPPH and hydroxyl radical) scavenging abilities. The results showed that the highest iron content of GLP80-Fe (15.61%±0.04) was obtained at the optimum conditions: reaction temperature was 38.0°C, reaction time was 3.0 h, FeCl3 addition was 2.9 mL and pH was 9. GLP80-Fe was a complex with β-FeOOH as the core and polysaccharides on its surface, and it was stable at pH 3 ~ 14. GC showed that the major monosaccharides were mannose (Man) and galactose (Gal) with a ratio of 1:5.15. In vitro free-radical scavenging activity of GLP80-Fe was significantly better than GLP80. The IC50 of GLP80-Fe against DPPH and hydroxyl radical were 3.785 mg/mL and 1.460 mg/mL, respectively.

This study investigated the structural elucidation, anti-radical and immunomodulatory activities of polysaccharides from the roots of

Background Jujube (Ziziphus jujuba Mill.) fruit is one of the largest productions in China and its increasing production has drawn considerable attention from researchers. Polysaccharide is one of the most abundant components of jujube, and it represents a major group of biolotegically active constituents. This study intended to investigate the special structure of a homogeneous acidic polysaccharide (PZMP4) produced from Ziziphus Jujuba cv. Muzao fruit using novel methods, including DEAE-Sepharose Fast Flow and Sephacryl S-300 column chromatography. Results The structure of PZMP4 was determined via high-performance gel permeation chromatography (HPGPC), gas chromatography (GC), Fourier transform infrared spectroscopy (FT-IR), methylation analysis, nuclear magnetic resonance spectroscopy (NMR), scanning electron microscopy (SEM), and atomic force microscopy (AFM). The results reveal that PZMP4 with a molecular weight of 27.90 kDa was composed of rhamnose, arabinose, mannose, glucose, galactose, and galacturonic acid at a ratio of 2.32:2.21:0.22:0.88:2.08:8.83. Advanced structural analysis revealed a netted structure with molecular aggregates of PZMP4. Structural features demonstrated that the basic backbone of PZMP4 appeared to mainly consist of (1→4)-linked GalpA with three branches bonded to O-3 of (1→3)-linked Araf, (1→2)-linked Rhap, and terminated with GalpA. Conclusions PZMP4’s unique structure could imply distinct bioactivities and have considerable utilization in functional food. Graphic abstract

The quality of polysaccharides from different regions was studied by using multiple fingerprint analysis and chemometric analysis. Polysaccharides from 10 batches of Glehnia littoralis were compared based on Fourier-transform infrared spectroscopy (FT-IR), high-performance liquid chromatography (HPLC), gel permeation chromatography (GPC), and proton nuclear magnetic resonance (1H-NMR). According to the results, the 10 batches of polysaccharides from G littoralis had high similarity by analyzing HPLC, FT-IR, 1H-NMR, and GPC fingerprints. Through cluster analysis, samples and adulterants in different regions could be classified. Three monosaccharides (galactose, glucose, and galacturonic acid), molecular weights (4.33 × 105-4.91 × 105, 4.04 × 104-4.71 × 104, and 5.02 × 103-5.83 × 103), and H-1 (4.99, 5.39, and 5.42 ppm) of α-glucose could be used as markers for quality control of medicinal materials of the roots of G littoralis.

(R)-3-aminopiperidine ((R)-APD), a key intermediate for alogliptin, trelagliptin, and linagliptin, was successfully resolved from racemic 3-aminopiperidine with an enantiomerically pure resolving agent, namely, (R)-4-(2-chlohydroxy-1.3.2-dioxaphosphorinane 2-oxide ((R)-CPA), via diastereomeric salt formation. By this resolution approach, (R)-3-aminopiperidine was obtained in 99.5% yield with 99.6%e.e.

A novel polysaccharide (GLP) with a molecular weight of 1.37 × 105 Da was purified from the roots of G. littoralis. Using monosaccharide composition, methylation analysis, GC-MS, 1D and 2D NMR, the structure of GLP was determined to be a 1 → 4)-α-D-Glcp glycoside linkage, while the terminal group of 1→)-α-D-Glcp was bonded to the main chain via O-6. Then, GLP-NPs were prepared by nano-precipitation method, the particle size of GLP-NPs was 288.4 nm and PDI was 0.340. GLP-NPs-AgNPs were prepared using GLP-NPs as reducing agent. GLP-NPs-AgNPs were characterized by ultraviolet-visible spectrophotometer (UV-Vis), Fourier transform infrared spectroscopy (FT-IR), transmission electron microscope (TEM) and X-ray diffraction (XRD). The yield of GLP-NPs-AgNPs was 38.77%, the particle size was 12.5 nm and the chelation rate of silver nanoparticles with polysaccharides was 67.5%. GLP-NPs-AgNPs had better antioxidant and antibacterial activities than GLP and GLP-NPs. In the present work, a simple and eco-friendly approach for the synthesis of silver nanoparticles (AgNPs) using G. littoralis polysaccharides nanoparticles (GLP-NPs) as reducing agent.

In this study, the crude polysaccharides of

In this study, the crude polysaccharides of C. javanica (CJP) was obtained from Codonopsis javanica (Blume) Hook. f. et Thomson using hot water extraction method, which was separated and purified by DEAE-cellulose column and Sepharose CL-6B column. The structure of the purified component was preliminary characterized by gas chromatography-mass spectrometer (GC-MS), high performance gel permeation chromatography (HPGPC) and infrared spectroscopy (IR). By examining the degree of delayed-type hypersensitivity (DTH) in mice and carbon particle clearance index, the immunomodulatory activity was clarified. The results showed that the extraction rate of CJP was 24.9 ± 0.5%. After purification, the refined polysaccharides component (CJP-2) was obtained. The structural characterization results indicated that CJP-2 was mainly composed of mannose, glucose, and galactose, and its molecular weight was 790 Da. Immunomodulation results showed that the low and medium levels of CJP significantly enhanced the degree of DTH in mice (P < 0.05). CJP can improve the clearance index of mice and enhance their charcoal removal function. The study indicates that C. javanica is a good source of polysaccharides, and CJP may be a new type of immunomodulator.

In this study, response surface methodology (RSM) was used to optimize the ultrasonic-assisted extraction parameters of Sojae Semen Praeparatum polysaccharides (SSPP-80), the optimum conditions were determined as follows: ultrasonic frequency of 100 W, ultrasonic power of 80 Hz, ultrasonic temperature of 52℃, ultrasonic time of 23 minutes, and liquid to raw material ratio of 40 mL/g. Based on these conditions, polysaccharides extraction rate was 7.72% ± 0.26%. Then, 2 novel polysaccharides (SSPP-80‐1, SSPP-80‐2) were isolated from SSPP by DEAE-cellulose 52 chromatography. The chemical compositions, physicochemical properties, and structure of SSPPs were investigated by simultaneous thermal analyzer (TGA), scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FI-IR), and high-performance liquid chromatography (HPLC). The results showed that SSPP-80 and 2 fractions were mainly composed of mannose (Man), glucose (Glc), galactose (Gal), xylose (Xyl), and arabinose (Ara). In addition, the antioxidant activities were evaluated against the DPPH and hydroxyl radical in vitro, the IC50 of SSPP-80, SSPP-80‐1 and SSPP-80‐2 against DPPH free radical were 4.407, 8.267, and 5.204 mg/mL, respectively, whereas the IC50values for removing hydroxyl groups were 5.318, 3.516, and 4.016 mg/mL, respectively. It demonstrated that SSPP-80 and 2 fractions had certain antioxidant activity. Theoretical basis for use of Sojae Semen Praeparatum polysaccharides was provided by this study.

A novel water-soluble polysaccharide named PEPW80-1, with a molecular mass of 4.7 kDa, was isolated from the pulp tissues of Phyllanthus emblica, and purified by sephadex G-100 column and sephacryl S-300 HR chromatography. The structural features of PEPW80-1 were investigated by a combination of acid hydrolysis, periodate oxidation-Smith degradation, methylation analysis, gas chromatography-mass spectrometry, scanning electron microscope, Fourier transform infrared spectroscopy, and nuclear magnetic resonance spectroscopy. The results showed that PEPW80-1 had a specific optical rotation of [α]25/D = +113° (c = 0.5 mg/mL) and its backbone composed of (1,3)-linked-β-L-rhamnose and (1,3,6)-linkage-β-D-galactose, with two branch chains of (1,4)-linked-α-D-galactose and (1,6)-linked-β-D-galactose and terminated with 1-α-L-arabinose. The antioxidant assays showed that PEPW80-1 possess 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activity and hydroxyl radical-scavenging activity, enhancing reductive power. The results of immunomodulatory assays in vitro showed that PEPW80-1 could promote the proliferation of mouse splenocytes. Those proposed that PEPW80-1 might be developed as a potential value-added product with the activities of immunomodulator and free-radical inhibitors.

Protein extracted from Douchi was hydrolyzed by alcalase based on a single-factor experiment and response surface methodology was employed to optimize hydrolysis conditions. The optimum conditions were determined to be: 63℃ extraction temperature, 1.4% quantities of enzyme and substrate, and 1.7 h extraction time. The optimal protein hydrolysate was subsequently subjected to ultrafiltration, and the fraction of molecular weight 10–50 kDa was identified as the most potent contributor to antioxidant activity. Amino acid analysis indicated that acidic amino acids were the most abundant in all fractions of the protein hydrolysate. Infrared spectroscopy showed there were no significant differences in secondary structure between fractions.

A new polysaccharide (CMPB90-1) was isolated from cultured Cordyceps militaris by alkaline extraction. The chemical structure of CMPB90-1 was determined by analysis of physicochemical and spectral data. The backbone of CMPB90-1 is composed of (1→6)-linked α-D-glucopyranosyl and (1→3)-linked α-D-glucopyranosyl residues, with branching at O-6, which consists of (1→4)-linked β-D-mannopyranosyl and (1→6)-linked α-D-glucopyranosyl residues, respectively. β-D-Galactopyranosyl residues is the terminal unit. In vitro immunomodulatory assay revealed that CMPB90-1 promoted proliferation of splenic lymphocytes, enhanced cytotoxicity of NK cells and promoted lymphocyte secretion of the cytokine interleukin-2. Besides, CMPB90-1 upregulated T-cell subpopulation, strengthened phagocytosis function of macrophages and induced their M1 polarization. The mechanism of the effects might be due to the activation of TLR2, MAPK and NF-κB pathways. The results proposed that CMPB90-1 can be researched and developed as a new functional food.

A novel polysaccharide (CMPA90-1; compound 1) was isolated from the cultured fruiting bodies of Cordyceps militaris. The chemical structure of compound 1 was elucidated by acid hydrolysis, periodate oxidation, Smith degradation, and methylation analysis, along with Fourier transform infrared spectroscopy, high-performance anion-exchange chromatography coupled with pulsed amperometric detection, gas chromatography-mass spectrometry, and one-dimensional [(1)H and (13)C nuclear magnetic resonance (NMR)] and two-dimensional NMR (heteronuclear single-quantum coherence and heteronuclear multiple-bond correlation). Sulfation of compound 1 by the chlorosulfonic acid-pyridine (CSA-Pyr) method led to synthesis of its sulfated analogue (CMPA90-M1; compound 2). The ultrastructures of both compounds 1 and 2 were further characterized by scanning electron microscopy and atomic force microscopy. The results of antioxidant assays showed that compounds 1 and 2 exhibited free-radical-scavenging effects, ferrous-ion-chelating ability, and reducing power. Also, in the cytotoxicity assay, compounds 1 and 2 showed inhibitory activity against A549 cells, with IC50 values of 39.08 and 17.33 μg/mL, respectively.

A novel polysaccharide (LCPA50-S1) with immunomodulatory activity was extracted with simulated gastric medium from Litchi chinensis, and purified by DEAE-52 cellulose column, Sephadex G-50 column and Sephacryl S-300 HR chromatography. The structural characteristics of LCPA50-S1 were expounded through complete acid hydrolysis, partial acid hydrolysis, methylation and instrumental analysis. The results demonstrated that LCPA50-S1 is a heteropolysaccharide with a molecular weight of 1.58 × 10(5) Da. The backbone was composed of (1→4)-linked β-D-glucopyranosyl residues, (1→6)-linked β-D-galactopyranosyl, (1→3,6)-linked β-D-galactopyranosyl residues, (1→4,6)-linked α-D-glucopyranosyl residues and branched at O-6. The branches were consisted of (1→2)-linked α-L-rhamnopyranosyl residues, (1→4)-linked β-D-glucopyranosyl residues, and (1→6)-linked β-D-galactopyranosyl, terminated with (1→)-linked α-L-arabinopyranosyl residues and (1→)-linked β-D-galactopyranosyl residues, respectively. The immunoregulatory activity of LCPA50-S1 was evaluated through determination the effect of LCPA50-S1 on nitric oxide (NO) production of RAW264.7 macrophages and spleen lymphocyte proliferation as well as its cytokines secretion level. The results demonstrated that LCPA50-S1 increased NO and TNF-α production in RAW264.7 macrophages significantly, enhanced the proliferation as well as the interleukin-2 (IL-2) production of splenocytes. The data indicated that LCPA50-S1 had the potential to be explored as a novel natural immunomodulator for application in functional foods and medicine.

Two polysaccharides, LCP70S-1 and LCP70W, were isolated from the pulp tissues of Litchi chinensis by anion-exchange chromatography and gel-filtration chromatography, while the structure of LCP70S-1 was elucidated and its physico-chemical properties was analyzed. The results demonstrated that LCP70S-1 is composed of L-rhamnose, L-arabinose and D-galactose in the ratio of 1.06:6.39:4.21, and the main chain of the heteropolysaccharide possess (1→3,6)-linked galactopyranosyl branches at O-6. The three branches consist of (1→3)-linked rhamnopyranosyl residues, (1→3,6)-linked galactopyranosyl and (1→5)-linked arabinopyranosyl residues, and terminated with (1→)-linked arabinopyranosyl residues, respectively. The two polysaccharides were further evaluated with 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities and their reducing power in vitro. The results showed that LCP70W and LCP70S-1 possessed significant antioxidant activities, especially for LCP70S-1. As such, LCP70S-1 could potentially serve as an antioxidant and would value further study for human healthcare.

A novel polysaccharide (LCP50W) with a molecular weight of 4.72 × 10(4) Da was isolated from the pulp tissues of Litchi chinensis . The chemical structure of LCP50W was characterized using physicochemical and instrumental analyses. The results indicated that the main chain of LCP50W consisted of (1→3)-linked β-L-rhamnopyranosyl, (1→6)-linked α-D-glucopyranosyl, and (1→2,6)-linked α-D-glucopyranosyl residues, which branched at O-6. The three branches consisted of (1→2)-linked α-L-rhamnopyranosyl, (1→3)-linked α-D-galactopyranosyl, and (1→3)-linked α-L-mannopyranosyl residues, terminated with (1→)-linked α-L-arabinopyranosyl residues, respectively. The in vitro immunomodulatory assay revealed that LCP50W promoted the proliferation of mouse splenocytes and enhanced the cytotoxicity of NK cells. LCP50W boosted the secretion of Th1 cytokine IFN-γ while it inhibited the secretion of Th2 cytokine IL-4; it also enhanced the expression of T-bet while it inhibited the expression of GATA-3. Additionally, LCP50W promoted the development of cell cycle toward the S phase.

Two polysaccharides, LCP70S-1 and LCP70W, were isolated from the pulp tissues of Litchi chinensis by anion-exchange chromatography and gel-filtration chromatography, while the structure of LCP70S-1 was elucidated and its physico-chemical properties was analyzed. The results demonstrated that LCP70S-1 is composed of L-rhamnose, L-arabinose and D-galactose in the ratio of 1.06:6.39:4.21, and the main chain of the heteropolysaccharide possess (1→3,6)-linked galactopyranosyl branches at O-6. The three branches consist of (1→3)-linked rhamnopyranosyl residues, (1→3,6)-linked galactopyranosyl and (1→5)-linked arabinopyranosyl residues, and terminated with (1→)-linked arabinopyranosyl residues, respectively. The two polysaccharides were further evaluated with 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities and their reducing power in vitro. The results showed that LCP70W and LCP70S-1 possessed significant antioxidant activities, especially for LCP70S-1. As such, LCP70S-1 could potentially serve as an antioxidant and would value further study for human healthcare.

A novel polysaccharide (LCPA50-S1) with immunomodulatory activity was extracted with simulated gastric medium from Litchi chinensis, and purified by DEAE-52 cellulose column, Sephadex G-50 column and Sephacryl S-300 HR chromatography. The structural characteristics of LCPA50-S1 were expounded through complete acid hydrolysis, partial acid hydrolysis, methylation and instrumental analysis. The results demonstrated that LCPA50-S1 is a heteropolysaccharide with a molecular weight of 1.58 × 10(5) Da. The backbone was composed of (1→4)-linked β-D-glucopyranosyl residues, (1→6)-linked β-D-galactopyranosyl, (1→3,6)-linked β-D-galactopyranosyl residues, (1→4,6)-linked α-D-glucopyranosyl residues and branched at O-6. The branches were consisted of (1→2)-linked α-L-rhamnopyranosyl residues, (1→4)-linked β-D-glucopyranosyl residues, and (1→6)-linked β-D-galactopyranosyl, terminated with (1→)-linked α-L-arabinopyranosyl residues and (1→)-linked β-D-galactopyranosyl residues, respectively. The immunoregulatory activity of LCPA50-S1 was evaluated through determination the effect of LCPA50-S1 on nitric oxide (NO) production of RAW264.7 macrophages and spleen lymphocyte proliferation as well as its cytokines secretion level. The results demonstrated that LCPA50-S1 increased NO and TNF-α production in RAW264.7 macrophages significantly, enhanced the proliferation as well as the interleukin-2 (IL-2) production of splenocytes. The data indicated that LCPA50-S1 had the potential to be explored as a novel natural immunomodulator for application in functional foods and medicine.

A novel low-molecular-weight polysaccharide (CMP-1) with antioxidant, immunostimulatory and antitumor activities was isolated from the cultured Cordyceps militaris. The structure of CMP-1 was elucidated by a combination of physicochemical and instrumental analyses, and its average molecular weight was 4.3 kDa. The backbone of CMP-1 was composed of (1 → 4)-linked α-D-glucopyranosyl, (1 → 6)-linked β-D-glucopyranosyl and (1 → 4)-linked β-D-glucopyranosyl residues which branched at O-6. The branches consisted of (1 → 3)-linked α-L-rhamnopyranosyl terminated with (1 → )-linked α-D-glucopyranosyl residues. The ultrastructure of CMP-1 was further investigated by scanning electron microscope (SEM). The antioxidant assays showed that CMP-1 exhibited free radical-scavenging effects, ferrous ions-chelating ability and reducing power. In vitro test revealed that CMP-1 could significantly stimulate the mouse splenocyte proliferation. The cytotoxicity assay showed that CMP-1 inhibited the proliferation of HT-29, HeLa, HepG2 and K562 cells, with the IC50 values of 137.66, 162.59, 176.29 and 364.01 μg/mL, respectively.

OBJECTIVE To study the rubrofusarin glucosides from whole plants of Berchemia polyphylla var. leioclada, and their scavenging activities for 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. METHOD The chemical constituents were isolated and purified via repeated silica gel and Sephadex LH-20 column chromatography. Their structures were elucidated by spectral analysis and the compounds were tested for their scavenging activities on DPPH radical. RESULT Three rubrofusarin glucosides compounds were isolated and identified as rubrofusarin-6-O-beta-D-glucopyranoside (1), rubrofusarin-6-O-beta-D-(6'-O-acetyl) glucopyranoside (2), rubrofusarin-6-O-alpha-L-rhamnosyl-(1-6) -O-beta-D-glucopyranside (3). Three isolated compounds showed strong scavenging activities on DPPH radical, the concentration of half elimination ratio( micromol x L(-1)) of VitC and Compounds 1-3 were 18.2, 40.5, 23.3 and 13.6, respectively. CONCLUSION Compounds 1-3 were isolated from this plant for the first time and compound 2 was a new compound. They showed significant antioxidant activity, and the scavenging activity of compound 3 was a little stronger than that of VitC.