This study aimed to characterize the chemical composition of a new sulfated polysaccharide from the red alga Gracilaria chouae and evaluate its activation effects on RAW264.7 macrophages. It showed that the obtained G. chouae polysaccharide (GCP-3A) was a sulfated acidic polysaccharide with a molecular weight of 11.87 kDa. GCP-3A was composed of xylose, galactose, glucose, and mannose with a molar ratio of 3.00:29.28:0.63:0.45, and it contained α,β‍-glycosidic linkages. Scanning electron microscopy (SEM) and a Congo red test showed that it was a heterogeneous polysaccharide with irregular interwoven sheets and rods, and did not have a triple-helix conform‍ation. Furthermore, GCP-3A significantly promoted the proliferation of RAW264.7 macrophages and the secretion of nitric oxide (NO) in tests of 3-‍(4,‍5-dimethylthiahiazo-2-yl)‍-2,‍5-diphenytetrazoliumromide(MTT) and NO.
Gracilaria/chemistry* ; Macrophages ; Molecular Weight ; Polysaccharides/pharmacology* ; Sulfates/pharmacology*

OBJECTIVEHerein, the synthesis, component, microstructure and pharmacological and toxicology researches of the Synthetic Mercury Sulfide (S-HgS) a kind of common drug in Chinese, Mongolia, Tibetan medicine, and Indian medicine system were summarized. The similar cognition about mercury toxicity & pharmacological action from some Asian regions was analyzed, and it can supply some useful direction for the traditional Asian medicine system.

METHODRecent literatures both domestic and abroad were summarized and analyzed.

RESULTS-HgS is the basis of Vermilion, Mongolia-Vermilion, Zuotai, and Ras-sindoor. Athough the processes of synthesis are very different, but the microstructure and pharmacological & toxicology of S-HgS is similar.

CONCLUSIONS-HgS has a far-ranging application,and unique curative effect. New technology such as nanotechnology can be used for improving the advancement of traditional Asian medicine.

Humans ; Medicine, Traditional ; Mercury Compounds ; adverse effects ; chemistry ; pharmacology ; Sulfates ; adverse effects ; chemistry ; pharmacology

To elucidate the adsorption mechanism of CS-A to the surface of titanium, 5 ml solutions of the CS-A were reacted with 2 g of native and 2 g of calcium-treated titanium powder for 48 h at 37 degrees C. Residual CS-A was detected by the carbazole elaborate method. The results showed that no CS-A attached to native titanium. Comparatively, titanium treated with calcium produced a significant adsorption of CS-A. At concentration of 60 micrograms/ml, the adsorption of CA-A to calcium-treated titanium powder attained the maximum, 83 micrograms/g. Only EDTA can liberate the bound CS-A from titanium surface. These findings suggest that calcium ion is necessary for the adsorption of CS-A to titanium.
Adsorption ; Calcium ; Chondroitin Sulfates ; pharmacology ; Static Electricity ; Surface Properties ; Titanium ; chemistry

新冠病毒感染疫情严重威胁着世界各国人民的生命健康。目前，对病毒感染的防治研究主要集中在抑制病毒与分子受体的结合上。AXL作为新发现的严重急性呼吸综合征冠状病毒2型（SARS-CoV-2）受体，在协助病毒感染人体呼吸系统中发挥着重要作用，是未来临床干预的潜在靶点。本研究对已发表的单细胞测序数据进行整理和分析，发现AXL在年轻人肺细胞中的表达水平明显高于老年人。人胚肺二倍体成纤维细胞（2BS）是衰老研究的公认细胞株。本文采用2BS细胞构建复制性细胞衰老模型，发现年轻细胞中AXL的蛋白水平明显高于衰老细胞，据此推测年轻人感染的风险可能更高，需要注意防护。我们发现一种羊栖菜褐藻多糖硫酸酯组分（SFW-3）可显著下调年轻2BS细胞中AXL的表达水平，表明SFW-3具有一定的抗SARS-CoV-2感染的研究价值，同时表明2BS细胞株也可作为潜在的SARS-CoV-2体外感染模型。
Humans ; SARS-CoV-2 ; Sargassum/metabolism* ; Diploidy ; Sulfates/metabolism* ; COVID-19 ; Polysaccharides/pharmacology* ; Lung

OBJECTIVETo observe the ability of triple helix-forming oligonucleotides (TFOs) modified with manganese porphyrin to combine with and cleave HBV DNA fractions.

METHODSTFO were modified with manganese porphyrin and acridines, and then reacted with the (32)P labeled HBV DNA fragments at 37 degrees C in vitro (pH 7.4). Electrophoretic mobility shift assays and DNase I footprinting tests were used to show the affinity and specificity of TFO to bind to target sequences. The ability of TFO to cleave HBV DNA fragments was tested by cleavage experiments.

RESULTSTFO modified with manganese porphyrin and acridine could bind to the target sequence in a sequence-dependent manner, with a Kd value of 3.5 x 10(-7) mol/L and a relative affinity of 0.008. In the presence of potassium monopersulfate (KHSO(5)), TFO modified with manganese porphyrin and acridine could cleave the target sequence where the triplex DNA was formed.

CONCLUSIONIn the presence of KHSO(5), TFO modified with manganese porphyrin and acridine could bind and cleave the target HBV-DNA in a sequence-dependent manner.

DNA ; drug effects ; pharmacology ; DNA, Viral ; chemistry ; drug effects ; Hepatitis B virus ; genetics ; Manganese ; pharmacology ; Metalloporphyrins ; pharmacology ; Potassium Compounds ; pharmacology ; Sulfates ; pharmacology

SATB1 plays a crucial role in the invasion and metastasis of breast cancer,and inhibition of SATB1 expression can effectively control breast cancer metastasis. In this study,homogeneous polysaccharides were isolated from Poria cocos and their sulfated derivatives were prepared to screen out the polysaccharide compositions with inhibitory effects on SATB1 expression. Smal-molecule components were removed from P. cocos by ethanol extraction,and P. cocos crude polysaccharide PPS was obtained by water extraction and ethanol precipitation. Then PPS was successively separated by DEAE Sepharose fast flow anion-exchange and Superdex-75 gel permeation chromatographic steps to give PPSW-1. The structure of PPSW-1 was identified and its sulfated derivatives were prepared. Then their inhibitory effects on human breast cancer MDA-MB-231 cells were investigated. A kind of polysaccharide,PPSW-1 with inhibitory effect on human breast cancer MDA-MB-231 cells,was obtained from P. cocos,with a relative molecular weight of 3. 06×104,and structure of 1,6-branched 1,3-α-D-galactan. PPSW-1 and its sulfated derivative Sul-W-1 showed good inhibitory effect on cells migration,and the water solubility of Sul-W-1 was better than that of PPSW-1. In addition,it was found that polysaccharide of P. cocos and its sulfated derivative can inhibit expression of SATB1. In this study,a kind of homogeneous polysaccharide with inhibitory effect on human breast cancer MDA-MB-231 cells was isolated from P. cocos,and its sulfated derivative with similar efficacy but better solubility was prepared,laying the foundation for the substance basis study of P. cocos.
Breast Neoplasms ; pathology ; Cell Line, Tumor ; Cell Movement ; Humans ; Matrix Attachment Region Binding Proteins ; metabolism ; Phytochemicals ; isolation & purification ; pharmacology ; Polysaccharides ; isolation & purification ; pharmacology ; Sulfates ; Wolfiporia ; chemistry

OBJECTIVETo observe the effect of nano-Se-chondroitin sulfate on the growth and apoptosis of chondrocytes from patients with Kashin-Beck disease (KBD) exposed to T-2 toxin in vitro.

METHODSSamples of the articular cartilage were obtained from 6 patients with grade II/III KBD diagnosed in line with the National Clinical Diagnostic Criteria of KBD (WS/T 207-2010) for chondrocyte separation and culture in vitro. The separated chondrocytes were treated with synthesized nano-Se-chondroitin sulfate particles and T-2 toxin, alone or in combination, and the cell growth and apoptosis were observed using MTT assay, HE staining and flow cytometry.

RESULTSThe synthesized nano-Se-chondroitin sulfate, with a selenium entrapment ratio of 10.1%, spontaneously formed nanoparticles in distilled water with sizes ranging from 30 to 200 nm. Fourier-transform infrared spectroscopy suggested a possible covalent bond that bound Nano-Se and chondroitin sulfate. Within the concentration range of 50-200 ng/ml, nano-Se-chondroitin sulfate significantly inhibited T-2 toxin-induced apoptosis of the cultured chondrocytes and reduced the early apoptosis rate to (8.64∓1.57)% (P<0.05).

CONCLUSIONNano-Se-chondroitin sulfate can inhibit T-2 toxin-induced apoptosis of cultured chondrocytes from KBD patients in vitro, and serves as a promising candidate therapeutic agent for KBD.

Apoptosis ; drug effects ; Cells, Cultured ; Chondrocytes ; drug effects ; pathology ; Chondroitin Sulfates ; administration & dosage ; pharmacology ; Humans ; Kashin-Beck Disease ; pathology ; Middle Aged ; Nanostructures ; T-2 Toxin ; toxicity

AIMTo investigate more efficient synthetic method of the nitrogen analogue 4 of salacinol (1) for searching new antidiabetic agents.

METHODSThe synthesis of the key intermediate 2, 4-O-isopropylidene-L-erythritol 1,3-cyclic sulfate (2a) was accomplished by modification of reports from D-glucose via seven steps in much more less expensive. Using this method, an efficient synthesis of 4 was carried out. The glycosidase inhibitory activity of 4 was tested for the intestinal alpha-glucosidase in vitro and compared with that of salacinol.

RESULTSA nitrogen analogue 4 of salacinol (1) was synthesized by the coupling reaction between the cyclic sulfate 2a and an azasugar 3b.

CONCLUSIONSubstitution of the sulfur atom in 1 with a nitrogen reduced the activity considerably.

Animals ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Glycoside Hydrolase Inhibitors ; Intestinal Mucosa ; drug effects ; enzymology ; Molecular Structure ; Nitrogen Compounds ; chemical synthesis ; pharmacology ; Rats ; Structure-Activity Relationship ; Sugar Alcohols ; chemical synthesis ; chemistry ; pharmacology ; Sulfates ; chemical synthesis ; chemistry ; pharmacology ; alpha-Glucosidases ; metabolism

To study the possibility of using hydroxypropyl chitosan-based blend membranes as carriers of corneal cells in tissue engineering, we prepared three kinds of blend membranes labeled hydroxypropyl chitosan/chondroitin sulfate, hydroxypropyl chitosan/gelatin/chondroitin sulfate and hydroxypropyl chitosan/oxidized hyaluronic acid/chondroitin sulfate. The transparency, water content and ability of protein adsorption of the blend membranes were measured. To evaluate the cytocompatibility of the blend membranes with corneal epithelial cells, rabbit corneal epithelial cells were cultured on the surface of the carrier membranes. The morphological characteristics, cell adhesion, cell proliferation and the activity of lactate dehydrogenase (LDH) in the media were investigated. Three kinds of blend membranes had good optical transmittance, suitable water content and ability of protein adsorption. The results showed that the less injury was made to corneal epithelial cells by the hydroxypropyl chitosan/gelatin/chondroitin sulfate blend membrane than the others. This kind of membrane was favor of the growth and adhesion of corneal epithelial cells. The hydroxypropyl chitosan/gelatin/chondroitin sulfate blend membrane is a promising carrier of corneal cells and can be used in reconstruction of tissue engineered cornea.
Animals ; Biocompatible Materials ; chemistry ; pharmacology ; Cell Culture Techniques ; methods ; Cell Proliferation ; drug effects ; Cells, Cultured ; Chitosan ; chemistry ; Chondroitin Sulfates ; chemistry ; Epithelium, Corneal ; cytology ; Gelatin ; chemistry ; Membranes, Artificial ; Rabbits ; Tissue Engineering ; methods

OBJECTIVETo construct artificial bone with collagen-hydroxyapatite (HA) or collagen-HA-chondroitin sulfate (CS) as the scaffolds, and observe their biological properties.

METHODSThe artificial bones were constructed by attaching recombinant human bone morphogenetic protein 2 (rhBMP-2) on those scaffolds. And then they were embedded into muscles of rats. Every weekend those newly formed bones were taken from muscles for comparing the difference in osteogenetic capability of two kinds of artificial bone in vivo.

RESULTSBoth kinds of artificial bones could induce bone regeneration in muscle. The collagen-HA-CS artificial bone was superior to the collagen-HA artificial in bone-guided degree.

CONCLUSIONSThe CS could promote the form action of new bone and accelerate the bone healing.

Animals ; Biocompatible Materials ; Bone Morphogenetic Protein 2 ; Bone Morphogenetic Proteins ; pharmacology ; Bone Regeneration ; Bone Substitutes ; Chondroitin Sulfates ; Collagen ; Hydroxyapatites ; Implants, Experimental ; Osteoblasts ; cytology ; Osteogenesis ; drug effects ; Rats ; Transforming Growth Factor beta