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This study aimed to analyze the effect of Bletilla striata polysaccharide(BSP) on endogenous metabolites in serum of tumor-bearing mice treated with 5-fluorouracil(5-FU) by untargeted metabolomics techniques and explore the mechanism of BSP in alleviating the toxic and side effects induced by 5-FU. Male BALB/C mice were randomly divided into a normal group, a model group, a 5-FU group, and a 5-FU + BSP group, with eight mice in each group. Mouse colon cancer cells(CT26) were transplanted into the mice except for those in the normal group to construct the tumor-bearing mouse model by subcutaneous injection, and 5-FU chemotherapy and BSP treatment were carried out from the second day of modeling. The changes in body weight, diarrhea, and white blood cell count in the peripheral blood were recorded. The mice were sacrificed and sampled when the tumor weight of mice in the model group reached approximately 1 g. TUNEL staining was used to detect the cell apoptosis in the small intestine of each group. The proportions of hematopoietic stem cells and myeloid progenitor cells in bone marrow were measured by flow cytometry. Five serum samples were selected randomly from each group for untargeted metabolomics analysis. The results showed that BSP was not effective in inhibiting colon cancer in mice, but diarrhea, leukopenia, and weight loss caused by 5-FU chemotherapy were significantly improved after BSP intervention. In addition, apoptotic cells decreased in the small intestinal tissues and the percentages of hematopoietic stem cells and myeloid progenitor cells in bone marrow were significantly higher after BSP treatment. Metabolomics results showed that the toxic and side effects of 5-FU resulted in significant decrease in 29 metabolites and significant increase in 22 metabolites in mouse serum. Among them, 19 disordered metabolites showed a return to normal levels in the 5-FU+BSP group. The results of pathway enrichment indicated that metabolic pathways mainly involved pyrimidine metabolism, arachidonic acid metabolism, and steroid hormone biosynthesis. Therefore, BSP may ameliorate the toxic and side effects of 5-FU in the intestinal tract and bone marrow presumably by regulating nucleotide synthesis, inflammatory damage, and hormone production.
Subject(s)
Animals , Male , Mice , Colonic Neoplasms/drug therapy , Diarrhea , Fluorouracil/adverse effects , Hormones , Metabolomics , Mice, Inbred BALB C , Polysaccharides/pharmacologyABSTRACT
As the main active ingredient of the orchidaceous herb Bletilla striata, B. striata polysaccharide(BSP) has pharmacological activities such as promoting coagulation, anti-inflammation, anti-oxidation, promoting wound healing, anti-tumor, and immunomodulation, and is biodegradable and non-toxic. Additionally, it has the material properties of suspension thickening, film-forming adhesion, coating and solubilizing, targeting and slow releasing, effect-enhancing and toxicity-reducing, etc., playing the role of unification of medicines and excipients. Therefore, BSP has a wide application prospect in the fields of drug delivery system and trauma repair. This paper reviews the research progress of BSP application in new drug delivery systems and biomaterials based on the related li-terature in recent years, with the aim of providing reference for the further research and application of BSP.
Subject(s)
Biocompatible Materials , Drug Delivery Systems , Orchidaceae , Polysaccharides , Wound HealingABSTRACT
Objective: To prepare carboxymethyl Bletilla striata polysaccharide-chitosan@curcumin (CM-BSP) polyelectrolyte complex films, optimize their preparation technology, and evaluate its quality. Methods: CM-BSP was synthesized, then CM-BSP and CS formed water-insoluble complex by electrostatic bonding, the Cur-loaded polyelectrolyte complex films were prepared by a volatilization of solvent method. The formulation and preparation technology were optimized using an orthogonal design method and the morphology and structure were observed by scanning electron microscopy and fourier transform microscopic infrared spectroscopy. Results: The optimal prescription was of CM-BSP 117 mg, CS 233 mg, glycerol 25%, Cur 20 mg. The mean thickness of Cur-loaded polyelectrolyte complex films was (74.0 ± 2.0) μm, drug loading capacities was 95.41%, and in vitro release rate was 93.78%. Conclusion: The obtained polyelectrolyte complex films displayed an smooth exterior inspection, uniform distribution, good drug loading capacities and in vitro release rate.
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Objective: To optimize Bletilla striata polysaccharide (BSP)/polyvinylalcohol (PVA) wet spinning process by Box- Behnken response surface method and prepare the composite fiber and performe their structural characterization and performance evaluation. Methods: Taking the OD value of three types of mechanical property data (breaking force, breaking strength and elongation at break) of the fiber as the evaluation index, five factors (BSP mass fraction, PVA mass fraction, volumetric mix ratio of BSP/PVA, coagulation time and spinning speed) were investigated by single factor experiments. On the basis of the results of single factor experiments, three factors (BSP mass fraction, volumetric mix ratio of BSP/PVA, coagulation time) were investigated by response surface method to optimize BSP/PVA composite fiber wet spinning process. The morphology, structure, thermal property, and absorption property of the fibers were characterized and analyzed by SEM, IR, DSC, and water absorption test. Berberine hydrochloride (BH) was used as model drug to evaluate the drug loading property of the composite fiber and antibacterial activity of the drug loading fiber. Results: The optimal spinning process of composite fiber were as follows: BSP mass fraction was 7.5%, volume mixing ratio of BSP/PVA was 1:1 and coagulation time was 3 min. The composite fiber had a dense surface and formed a three-dimensional network structure inside, generated intermolecular forces, which enhanced the thermal and mechanical properties, and exhibited excellent water absorption capacity. The encapsulation efficiency of the composite fiber reached 70.2%. And the drug loading fiber formed obvious inhibition zone in the bacteriostatic zone test, which presented excellent antibacterial effect against E. coli and S. aureus. Conclusion: The optimized spinning process is feasible and low cost. The prepared composite fiber has better physical property and certain coating ability, and its application in the field of biomedical textiles is worth further study.
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Objective: Because of the adhesion of Bletilla striata polysaccharide (BSP), it was mixed with sodium alginate (SA) as a composite carrier to prepare mucoadhesive PNS-BSP composite microspheres. Panax notoginseng saponins (PNS) dispersion with sustained release property was used as an encapsulating drug. Methods: The composite microsphere was prepared by ion cross-linking method. The formulation process was investigated and optimized by single factor test and orthogonal design. The microspheres were evaluated by scanning electron microscope (SEM), particle size distribution, DSC, swelling properties, in vitro mucoadhesive properties, and in vitro release characteristics. Results: PNS-BSP composite microspheres had good roundness, rough surface and wrinkles. The microspheres showed a narrow size distribution. PNS was uniformly dispersed in microspheres in an amorphous state. The microspheres prepared by the best prescription process were stable in process and reproducible. Compared with the microspheres prepared by directly adding PNS, the drug loading, encapsulation efficiency and yield of PNS dispersion microspheres were increased significantly, which were 10.34%, 51.25%, and 82.21%, respectively. The drug loading, encapsulation efficiency, and yield were 4.04%, 12.16%, and 61.35% of PNS microspheres. The addition of BSP increased the swelling properties of the SA microspheres, and significantly increased the retention rate in the stomach of rats. The release of ginsenoside Rg1 in PNS-BSP microspheres was released slower compared to PNS. Conclusion: The bioadhesion of microspheres was increased by the addition of BSP. The drug loading, encapsulation efficiency, and yield of the microspheres were increased by the preparation of PNS as a dispersion, and the microspheres also had a certain sustained-release effect.
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Objective To prepare palmatine-loaded flexible nano-liposomes (PFL) films with Bletilla striata polysaccharide (BSP) as membrane material, and evaluate its pharmacy related performance in order to lay the foundation for further application. Methods The PFL was prepared by injection method and the films of PFL based on Bletilla striata polysaccharide (PFL-BPF) was prepared by homogenate coating method. The PFL-BPF was characterized and evaluated by electron microscopy, differential scanning calorimeter (DSC), and in vitro transmucosal membrane experiment. Results The PFL and BSP had good compatibility and easy to film with BSP as membrane material. The appearance of PFL-BPF obtained was smooth, non-bubble, flexible, and suitable stiffness; PFL-BPF had good biological adhesion. The time of scouring the film agent from mucous membrane with normal saline was (130 ± 7) min. At 0.5 h, the dose of PFL-BPF promoting palmatine (PA) infiltration to mucosa was 32.41 μg/g. It was 3.17 times higher than those of PA solution based on BSP (PL-BPF) and 1.9 times for PA common liposomes based on BSP (BLP + PA-BPF) (t-test, P < 0.05); At 2.5 h, it was 2.67 times and 1.89 times higher than those of PL-BPF and BLP + PA-BPF, respectively. It showed that PFL-BPF could significantly promote the water-soluble drug PA through mucosa membrane and release it slowly. The results of DSC showed that the possible mechanism for promoting the absorption of PA through mucosa membrane was that the flexible liposomes disturbed the mucosal epithelial cells and carried the drug into the mucosal tissue. Conclusion The PFL-BPF had the advantages of good film-forming property, lasting adhesive attraction, strong scour resistance, simple and feasible preparation process, and could promote drug permeation into mucosa obviously. Therefore, the flexible nano-liposomes film is a good drug carrier for the transmucosal drug delivery applications and has a wide application prospect.
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Objective To prepare reactive oxygen species (ROS)-responsive Bletilla striata polysaccharide (Oxi-BSP) micelles, optimize their preparation technnology, and evaluate its in vitro characterizations. Methods Oxi-BSP was synthesized, then curcumin (Cur)-loaded micelles were prepared by a dialysis method. The formulation and preparation technology was optimized using an orthogonal design method. The morphology was observed by transmission electron microscope, while the particle size, particle distribution, and zeta potential were determined by laser particle size analyzer. Hydrogen peroxide was used to simulate the ROS environment and then the change of micellar morphology was observed. Results The Cur-loaded micelles were spherical with homogeneous distribution, the mean size was (225.33 ± 2.97) nm, the zeta potential was (-16.80 ± 0.37) mV, the encapsulation efficiencies was (85.75 ± 0.87)%, and drug loading capacities was (20.21 ± 0.44)%. And the micelles were responsive to ROS stimuli. Conclusion The obtained micelles display an uniform particle size distribution with moderate drug encapsulation efficiencies and drug loading capacities.
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Microspheres (MS) are an excellent transarterial chemoembolization carrier for cancer treatment. Then the Bletilla striata polysaccharide (BSP) that was isolated from the rattan of Bletilla striata was used as skeleton material, and the matrine (ME) loaded Bletilla striata polysaccharide microspheres (ME-BSPMS) were prepared by emulsify-chemical crosslinking method. ME-BSPMS was characterized for appearance shape, particle size, drug loading, swelling ratio, suspension property, drug entrapment condition and in vitro release characteristics. The results showed that the ME-BSPMS appeared as round spherical and smooth shape by SEM, with an average size of (85 ±7) μm. ME-BSPMS with a good suspension in physiological saline and the swelling ratio could reach upwards of (53 ±4.2)% in 20 minutes, also with a large amount of drug loading of (30.12 ±3.25)%. The results of DSC scanning indicate that good compatibility exists between the ME and BSP, and the ME could be embedded fully in the matrix of the ME-BSPMS. The accumulation drug release from ME-BSPMS was (25.38 ±1.57)% at 12 h, this suggests that the ME-BSPMS has a good sustained release effect. These results indicate that the ME-BSPMS may be a promising transarterial chemoembolization carrier for cancer treatment.
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Objective To investigate the effect of the bletilla striata polysaccharide on the expression of ovarian vascular endothelial growth factor(VEGF) and serum malondialdehyde(MDA)and endometrial morphology in rat during perimenopause period.Methods The animal model of perimenopause rats was established by unforced aging.A total of 40 female SD rats(12~14 months old)were randomly divid-ed into four groups:Chinese medicine low(0.5 g/kg),medium(1 g/kg),high(2 g/kg) dosage group and the elder model group.The rats were given with corresponding drugs for 8 weeks.The content changes of ovarian VEGF protein was detected by western blot;serum MDA con-tent was detected by thiobarbituric acid;the morphology of endometrium in rats was observed by HE staining.Results Eight weeks later, compared with the elder model group,the VEGF protein expression in Chinese medicine low,medium,high dosage group increased,the serum MDA content in Chinese medicine low,medium,high,dosage group reduced,the differences were statistically significant( P<0.01),with dose dependence.Endometrial thickening and glandular increasing with the increase of dose.Conclusion Bletilla striata polysaccharide can upregulate the expression of VEGF protein,and down regulate the level of serum MDA,which improves the uterine function so as to delay the process of perimenopause in rats.
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Objective To explore the feasibility of bletilla striata polysaccharide as a drug delivery material .Method With hydrophobic cholesterol succinyl bletilla striata polysaccharide (CHSB) as the carrier ,the model drug paclitaxel (PTX) loaded nanoparticles were prepared via dialysis method .The morphology of nanoparticles was observed by Transmission Elec-tron Microscope (TEM) .The particle size ,distribution and zeta potential were characterized by Dynamic Light Scattering in-strument (DLS) .The entrapment efficiency ,drug loading and in vitro release were determined by high performance liquid chromatography (HPLC) .Differential Scanning Calorimetry (DSC) was used to confirm the drug form in the drug loaded nan-oparticles .The in vitro antitumor activity of nanoparticles was assayed by MTT .The uptake of nanoparticles by QGY-7703 liver cancer cells was observed by fluorescence labeling method .Results The prepared nanoparticles had spherical shape with uniform particle size distribution .The drug was loaded in the interior of the nanoparticles .Drug loading and encapsulation effi-ciency were affected by the CHSB in certain range .The cytotoxicity of drug loaded nanoparticles on liver cancer cells was stron-ger than the free drug .The fluorescence of Rhodamine B labeled drug nanoparticles were observed in the cells .Conclusion Cholesterol succinyl bletilla striata polysaccharide (CHSB) is highly feasible as an insoluble drug carrier .It can be used as a po-tential Nano carrier material .
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Objective: To optimize the decolorization technology of activated carbon for the plant pigment in Bletilla striata polysaccharide.Methods: Using L 9 (3 4) orthogonal test with activated carbon as the decolorizer, the amount of activated carbon, decolorization temperature, decolorization liquid pH and decolorization time were investigated.The decolorization rate and polysaccharide retention rate were investigated.The decolorization rate and polysaccharide retention rate were taken as the indices.Results: The optimum decolorization technology was as follows: the amount of activated carbon was 1.0%, the decolorization temperature was 40 ℃, the pH value was 5 and the decolorization time was 30 min.Under those conditions, the decolorization rate of Bletilla striata polysaccharide was 91.3% and the retention rate of polysaccharide was 80.6%.Conclusion: The selected decolorization technology of activated carbon can make Bletilla striata polysaccharide get the best decolorizing effect.
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Objective: To deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alopecuroides (TASA) was prepared. Methods: The pellet was prepared by extrasion-spheronizing and subsequently coated with three layers of two polymers. Results: The pellet core consisted of 40% TASA, 1:2 in ratio of Bletilla striata polysaccharide (BSP), an enzyme-degradable material, to microcrystalline cellulose (MCC), filler, and 1% CMC-Na solution as binder by optimization. Concerning of the three coated layers, the outer layer was coated with Eudragit RS30D for controlling drug release in colon, the intermediate layer and the inner layer were coated with same polymer, Eudragit S100, for preventing drug release in upper gastrointestinal tract, which required 23.2%, 21.7%, and 9.3% weigh gain, respectively. The coated pellets released 1.20% of sophoridine and 1.98% of matrine in media mimicking the stomach condition for 2 h, and 23.88% of sophoridine and 22.91% of matrine in media mimicking the intestine for 3 h and finally 90.25% of sophoridine and 89.94% of matrine in colonic conditions within 24 h. And the similarity factor f of sophoridine and matrine of release curve for investigated formulation was internal in (50-100) and > 80, demonstrating that sophoridine and matrine in formulation achieved a synchronous release. Conclusion: The coated pellets achieve a certain colon-specific release and synchronous release.
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Objective To investigate the inhibitory effect of Bletilla striata extracts (BSE) on bleomycin-induced pulmonary fibrosis (PF) in rats and study the chemical characteristics of the active component. Methods B. striata was extracted with 95% ethylalcohol to obtain the ethanol extract. The residue was extracted with water and precipitated with ethanol to obtain the B. striata polysaccharide (BSP). Sprague Dawley male rats were intratracheally administered of bleomycin (BLM, 5 mg/kg) to induce PF. PF Rats were administered with ethanol BSE (300 mg/kg body mass) and BSP (300 mg/kg body mass) once daily for 28 d by gavage. On 14 d and 28 d, the lungs were harvested to observe the pathological and collagen deposition changes. The lung coefficient and the content of hydroxyproline (HYP) were also determined. The phenol-sulfuric acid method was used to detect the total sugar content, the relative molecular mass was detected by high performance gel permeation chromatography (HPGPC) and the monosaccharide components were analyzed by high performance liquid chromatography (HPLC). Results Compared with PF model group, the histopathological changes in lung tissue treated with BSP group were obviously improved, the level of HYP in lung tissues and the lung coefficient were significantly decreased (P<0.05, P<0.01). But the group treated with ethanol BSE had no significant improvement. The content of BSP was 81.41%, and the number average molecular weight (Mn) of BSP was about 2.23×105. The BSP was mainly composed of glucose and mannose. Conclusion HYP could significantly decrease lung HYB and collagen deposition of PF rats, and has the potiential for inhibition of PF.
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Objective To evaluate the protective effect of Bletilla striata polysaccharide ( BSPS) on immunological and chemical liver injury in mice. Methods Thirty Kunming male mice were randomly divided into five groups, including the normal control group,model control group,and low-,middle-,and high-dose BSPS groups (n=6 each).Tail vein injection of ConA was carried out to establish the ConA-induced liver injury model.After different treatments,all the animals were sacrificed,and the plasma levels of ALT and AST were tested.Additionally,sixty Kunming male mice were randomly divided into six groups,including the normal control group,model control group,silymarin group,and low-,middle-,and high-dose BSPS groups (n=10 each).Tail vein injection of CCl4 was performed to establish the CCl4-induced acute liver injury model.After different treatments,the plasma levels of ALT and GSH were tested.The effects of BSPS on the weights of the liver and spleen were examined. Results The levels of ALT and AST were reduced in BSPS-treated mice when compared with those experiencing only ConA-induced liver injury ( model control group) ,and significant difference was found between the middle-and high-dose BSPS groups and the model control group (P<0.01,P<0.05).The weights of the liver and spleen and the level of ALT were reduced in BSPS-treated mice as compared with those with only CCl4-induced acute liver injury (model control group),while the level of GSH was significantly increased in middle-and high-dose BSPS groups (P<0.05). Conclusion BSPS at low,middle,and high doses can prevent against the ConA-induced immunological liver injury and CCl4-induced acute liver injury in mice.
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Objective To investigate the inhibitory effect of Bletilla striata extracts(BSE)on bleomycin-induced pulmonary fibrosis(PF)in rats and study the chemical characteristics of the active component. Methods B. striata was extracted with 95%ethyl?alcohol to obtain the ethanol extract. The residue was extracted with water and precipitated with ethanol to obtain the B. striata polysac?charide(BSP). Sprague Dawley male rats were intratracheally administered of bleomycin(BLM,5 mg/kg)to induce PF. PF Rats were administered with ethanol BSE(300 mg/kg body mass)and BSP(300 mg/kg body mass)once daily for 28 d by gavage. On 14 d and 28 d, the lungs were harvested to observe the pathological and collagen deposition changes. The lung coefficient and the content of hydroxy?proline(HYP)were also determined. The phenol-sulfuric acid method was used to detect the total sugar content,the relative molecular mass was detected by high performance gel permeation chromatography(HPGPC)and the monosaccharide components were analyzed by high performance liquid chromatography(HPLC). Results Compared with PF model group,the histopathological changes in lung tissue treated with BSP group were obviously improved ,the level of HYP in lung tissues and the lung coefficient were significantly decreased (P<0.05,P<0.01). But the group treated with ethanol BSE had no significant improvement. The content of BSP was 81.41%,and the number average molecular weight(Mn)of BSP was about 2.23 × 105. The BSP was mainly composed of glucose and mannose. Conclusion HYP could significantly decrease lung HYB and collagen deposition of PF rats,and has the potiential for inhi?bition of PF.
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Objective To prepare proanthocyanidins/bletilla striata polysaccharide/chitosan microspheres ( PC/BSP/CTS ) and the physic-chemical characterizations were investigated.Methods The PC/BSP/CTS microspheres were prepared by spray drying method.The morphology of PC/BSP/CTS microspheres was observed by Scanning Electron Microscopy(SEM), and its physic-chemical characteristics such as diameters, release in vitro, moisture content, swelling ratio, solid density were studied.ResuIts The PC/BSP/CTS microspheres were successfully prepared by spray drying method, SEM showed that PC/BSP/CTS microspheres had the spherical shape with smooth surfaces.The diameters of microsphere A, B and C were 10~20, 2~15, 10~25μm.The in-vitro release showed that the cumulative release of three kinds of microspheres A, B, C was 25.07 %, 38.83 %and 60.00 % in 24 h, which had no burst release, while with time prolonged to 48 h, the cumulative release was 28.89%, 43.17% and 72.86%, respectively.The results of moisture content, swelling ratio, solid density were 15.35% ~23.51%, 46.50% ~105.80%, 0.375 ~0.496. ConcIusion The PC/BSP/CTS microspheres are successfully prepared by spray drying method which possess good characteristics and sustained-release effect, which would be as a good pulmonary drug delivery system.