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Objective: To investigate the osteoblastogenic activity of the ethyl acetate (EtOAc) extract of Smilax glabra Roxb roots and its major active compound astilbin. Methods: Astilbin was isolated from EtOAc extract using silica gel chromatography combined with fraction crystallization. Chemical structure of astilbin was determined by analysis of the spectroscopic data in comparison with the literature. MTT method was used to detect the toxicity. Alkaline phosphatase (ALP) activity was determined by the spectrophotometric method at 405 nm using p-nitrophenyl phosphate as a substrate. Calcium deposition was stained with alizarin red-S, distained with cetylpyridium chloride, and quantified at 562 nm. In silico model for astilbin-ALP interaction was analyzed using AutoDock 4.2.6. The changes in expression of osteoblast differentiation related genes were determined using quantitative real-time PCR. Results: Both the EtOAc extract and astilbin had no toxicity toward osteoblast MC3T3-E1 cells at 5.0, 10, 25, and 50 μg/mL. At 25 μg/ mL, they enhanced ALP activity and mineralization of osteoblasts up to 30% and 55% for the EtOAc extract and 22% and 41% for astilbin, respectively. Molecular docking analysis of astilbin-ALP interaction revealed Arg167, Asp320, His324, and His437 were key residues participating in hydrophobic interaction; meanwhile, His434 and Thr436 residues were involved in hydrogen bond formation in the active site of human tissue-nonspecific ALP. Moreover, the expression level of genes opn, col1, osx, and runx2 were up-regulated in astilbin treated samples with the fold changes as 2.2; 3.7; 4.1; 2.3, respectively at 10 μg/mL (P<0.05). Conclusions: The EtOAc extract and its major compound astilbin exhibit osteoblastogenic activity by up-regulating important markers for bone cell differentiation. It could be a new and promising osteogenic agent with dual actions for therapeutic applications.
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Objective: To predict the targets and pathways for the main active components of Smilax glabra in the treatment of gout based on network pharmacology. Methods The active components and targets of the S. glabra were obtained by TCMSP database and Drugbank database. Furthemore, the interaction network among the targets was established by Cytoscape software. Meanwhile, crosslink analysis was performed to screen out the active components and potential targets. Finally, the information was obtained from the MAS 3.0 biomolecular function system, and then the target pathway network model was established. Results In this study, a total of 11 effective components and 39 effective targets were predicted, which related to adipocytokine signaling pathway, ERbB signaling pathway, and Toll like receptor signaling pathway. Among these pathways, MAPK1, RELA, PTGS2 genes may play a crucial role. Conclusion This study investigated the characteristics on multi-component, multi-target and multi-pathway of S. glabra, which provided a new idea and method for further study on anti-gout mechanism of S. glabra.
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Objective: To establish a method of quantitative analysis of multi-components by single-marker (QAMS) for simultaneously determination of neoastilbin, astilbin, neoisoastilbin, isoastilbin, and engeletin in Smilax glabra, and research the tendency of content changes in different growth years by QAMS. Methods: An HPLC method was established to determine the relative correction factors of four other flavonoids by using astilbin as the internal reference standard. Then the method was used to determine the various content of five flavonoids in different growth years and validate the feasibility and accuracy by comparing the content results determined by the external standard method with QAMS. The dynamic change regularity of flavonoids in S. glabra was investigated. Results: A total of 23 samples from five batches in different growth years were simultaneously determined by external standard method and QAMS, the results deviation were all less than 1.0%. The content of five flavonoids in different growth years was different, astilbin decreased with the increase of growth years, neoastilbin, neoisoastilbin and isoastilbin had the reverse trend. Conclusion: The established QAMS method is feasible and accurate for the simultaneous determination of five flavonoids in S. glabra. Growth years have a certain impact on the content of each component.
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Objective To investigate the protective effect of Smilax Glabra Roxb on the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by IL-1 in human vascular endothelial cells (HUVECs). Methods Take human umbilical vascular endothelial cells as study subject, use immunofluorescence staining, serum pharmacology of the traditional Chinese medicine and flow cytometer. The level of VCAM-1 is represented by the mean fluorescence intensity. Results IL-1 increases the expression of VCAM-1, the expression of VCAM-1 in group of serum containing drugs is lower than control group. Conclusion Smilax Glabra Roxb can inhibit the effect of IL-1 induced increase of VCAM-1 expression in HUVECs.
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The ethanol extract of smilax glabra roxb (SG) (100mg/kg of body weight) reduced the blood level of glucose and plasma insulin levels of GK rat 4h after intraperitoneal administration (p< 0.01). While in the normal rat, it reduced only the glycemia. On isolated pancreas islets, SG concentration of 2mg – 4 mg/ml/h has no effect on insuline recretion. The finding suggests that hypoglycemic effect of SG is caused by the increase of the sensibility of target tissue to insuline.
Subject(s)
Rats , Blood Glucose , Diabetes Mellitus , Plant Proteins , Animal ExperimentationABSTRACT
Cryophylisat powder of ethanolic fluid extract of Smilax glabra (SG) was administered orally on mouse with a single dose of 1g/kg of body mass. Hypoglycemic effect exerted with 10.58% approximatively. Continous use of 7 days of this dose increased the hypoglycemic action. Oral SG effects manifested lately with less level than injectable SG. Apart from the increase of synthetization capacity of glycogene, SG promote the sensitivity of the tissues to insuline.
Subject(s)
Mice , Glucose Tolerance Test , Hypoglycemic AgentsABSTRACT
Cryophylisat powder of ethanolic fluid extract of Smilax glabra with the oral dose of 1.25g and 2.5g/kg of body mass (5-10 times of active dose on hypoglycemic effect was administered in rabbit in 15-30 days continously. These doses did not influenced on the body mass, the hematologies indices as well as the functional indices of lever and kidney. However, in microscopic image, there are some degenerative mainfestations of low levels of liver cells among two groups using the studied preparation.