Xu X.,Ningxia Medical University |
Xu X.,Key Laboratory of Hui Ethnic Medicine Modernization |
Zhang Z.,Ningxia Medical University |
Zhang Z.,Key Laboratory of Hui Ethnic Medicine Modernization |
And 6 more authors.
Molecules | Year: 2017
Cistanoside A (Cis A), an active phenylethanoid glycoside isolated from Cistanche deserticola Y. C. Ma, has received our attention because of its possible role in the treatment of osteoporosis. In the present study, we evaluated the effects of Cis A on an ovariectomized (OVX) mice model and investigated its underlying molecular mechanisms of action. After 12 weeks of orally-administrated intervention, Cis A (20, 40 and 80 mg/kg body weight/day) exhibited significant antiosteoporotic effects on OVX mice, evidenced by enhanced bone strength, bone mineral density and improved trabecular bone microarchitecture. Meanwhile, the activities of bone resorption markers, including tartrate-resistant acid phosphatase (TRAP), deoxypyridinoline (DPD) and cathepsin K, were decreased, and the bioactivity of bone formation marker alkaline phosphatase (ALP) was increased. Mechanistically, Cis A inhibited the expression of TNF-receptor associated factor 6 (TRAF6), an upstream molecule that is shared by both nuclear factor kappa-light chain enhancer of activated B cells (NF-κB) and phosphatidylinositol 3-kinase (PI3K)/Akt pathways and subsequently suppressed the levels of receptor activators of nuclear factor kappaB ligand (RANKL), downregulated the expression of NF-κB and upregulated osteoprotegerin (OPG), PI3K and Akt, which means Cis A possessed antiosteoporotic activity in ovariectomized mice via TRAF6-mediated NF-kappaB inactivation and PI3K/Akt activation. Put together, we present novel findings that Cis A, by downregulating TRAF6, coordinates the inhibition of NF-κB and stimulation of PI3K/Akt pathways to promote bone formation and prevent bone resorption. These data demonstrated the potential of Cis A as a promising agent for the treatment of osteoporosis disease. © 2017 by the authors; licensee MDPI, Basel, Switzerland.
Huang Y.,Key Laboratory of Hui Ethnic Medicine Modernization |
Song Y.,Key Laboratory of Hui Ethnic Medicine Modernization |
Huang M.,Ningxia Medical University |
Fan Y.-R.,Key Laboratory of Hui Ethnic Medicine Modernization |
And 4 more authors.
Research on Chemical Intermediates | Year: 2016
A series of novel bis-naphalenyl compounds with different diamine linkers were synthesized and characterized by 1H NMR, 13C NMR, and HR-MS. The DNA binding abilities of the compounds were studied by using flourescence titration, DNA thermal denaturation experiments, viscosity titration, and NMR studies. The DNA binding abilities of all the bis-naphalenyl compounds were on the same order of magnitude. Compared with the groove binding mode of the monomer, the bis-naphalenyl compounds exhibited partial intercalating binding mode. The cytotoxicity activities of the compounds were evaluated by MTT assay in vitro. According to the results of MTT assay, bis-naphalenyl compound 3c with hexamethylenediamine linker, and 3d with p-xylylenediamine linker were found to be more toxic against BGC823 cells. The IC50 values of the two compounds were similar to that of the control drug (5-Fluorouracil) on BGC823 cells. Compared with the results on BGC823 cells, better results were found on SW480 cells. Compounds 3c and 3d exhibited smaller IC50 values than that of control drug (5-Fluorouracil). The IC50 values of 3c, 3d, and 5-Fluorouracil were 52.01, 66.09, and 230.11 μM, respectively. © 2016 Springer Science+Business Media Dordrecht
Wang H.,Ningxia Medical University |
Ma Y.-H.,Qinghai University for Nationalities |
Wang W.-P.,Ningxia Medical University |
Wang W.-P.,Key Laboratory of Hui Ethnic Medicine Modernization |
Wang W.-P.,Ningxia Engineering & Technology Research Center For Modernization of Hui Medicine
Chinese Journal of New Drugs | Year: 2016
Objective: To study the influences of particle size and different solvents on glycyrrhetinic acid (GA)-loaded microparticles during the hydrogel template process. Methods: GA-PLGA microparticles were fabricated using different PVA templates and organic solvents by a novel hydrogel template method. Then the morphology was oberved by SEM, and the drug loading, encapsulation efficiency, and in vitro release profiles were analyzed. Results: The obtained microparticles showed desirable morphology as microdiscs with homogeneous size and predefined shape and high drug loading capacity, and the release profiles could be adjusted by changing particle size and solvent systems. Conclusion: The hydrogel template technique can be applied to precisely define the size and shape of microparticles, and is suitable for different solvents, which is beneficial for adjusting of the release profiles of microparticles. © 2016, Chinese Journal of New Drugs Co. Ltd. All right reserved.
Luo S.X.,Ningxia Medical University |
Zhang R.X.,Ningxia Medical University |
Huang Q.,Ningxia Medical University |
Huang Q.,Key Laboratory of Hui Ethnic Medicine Modernization |
And 3 more authors.
Journal of Inclusion Phenomena and Macrocyclic Chemistry | Year: 2016
The chemical and enzymatic hydrolysis of the secondary 5-fluorouracil-1-acetic acid/β-cyclodextrin conjugate were evaluated for potential application as a colon-targeted prodrug. In aqueous buffer solutions at a pH of 1–10, the pH-rate profile for hydrolysis of the conjugate was interpreted in terms of spontaneous or water-catalyzed, and specific base-catalyzed reactions. In the solutions of α-amylase, the conjugate was degraded to 5-fluorouracil-1-acetic acid/small saccharide conjugates. In the solutions of carboxyl esterase, the conjugate was gradually hydrolyzed to 5-fluorouracil-1-acetic acid at the similar rate as that in the absence of the carboxyl esterase. 5-Fluorouracil-1-acetic acid was rapidly released when the conjugate was hydrolyzed firstly by α-amylase and secondly by carboxyl esterase. On the other hand, the rate of hydrolysis of the conjugate was accelerated significantly by the colonic fluids of rats. It is important to note that the secondary conjugate released the parent drugs more slowly than the primary one. © 2016, Springer Science+Business Media Dordrecht.
Chen Z.,Ningxia Medical University |
Lei Y.-Y.,Ningxia Medical University |
Hei J.,Ningxia Medical University |
Hu J.,Ningxia Medical University |
And 6 more authors.
Chinese Traditional and Herbal Drugs | Year: 2015
Objective: To investigate the inhibitory effect of polysaccharide (PS) extract from Trigonellae Semen (TS, the seeds of Trigonella foenum-graecum) and its enzymatically digested low molecular weight oligosaccharide (OS) on dyslipidemia, and to preliminarily elucidate the mechanism. Methods: The combinative activity of PS and OS on cholesterol micelles was determined in vitro. SD rats were made by high fat diet and used as the hyperlipidemia models, which were given the high fat diet mixed with the complex of PS or OS with the concentration of 2.5% for 8 weeks and then collected the feces of rats in each group for 1 week. The rats were sacrificed after treated for 9 weeks to get the serum and liver. The indexes of blood lipid and antioxidant activity in serum and the indexes of liver function were determined. Histopathology assay of liver tissues was observed by HE staining. The excretion of cholesterol and bile acid in feces were also determined. Results: Each drug-dealing group exhibited lowered TC, TG, and LDL-C levels, and elevated HDL-C level in serum. Besides, restored liver tissue could be observed. Moreover, PS and OS exhibited the excellent activity of combining to cholesterol micelles, suppressing superoxide dismutase (SOD) level, and accelerating the excretion of bile acid. Conclusion: Both PS and OS of TS, especially the later, show the considerable effects on dyslipidemia. ©, 2015, Editorial Office of Chinese Traditional and. All right reserved.
Wang W.,Ningxia Medical University |
Wang W.,Ningxia Engineering and Technology Research Center for Modernization of Hui Medicine |
Wang W.,Key Laboratory of Hui Ethnic Medicine Modernization |
Lei Y.,Ningxia Medical University |
And 7 more authors.
Artificial Cells, Nanomedicine and Biotechnology | Year: 2016
The aim of the present study was to prepare and evaluate microparticle formulation encapsulated with glycyrrhetinic acid (GA) based on bovine serum albumin (BSA). The drug-loaded nanoparticles were firstly formed by a simple desolvation method, and were further assembled into microparticles using zinc chloride and glutaraldehyde as crosslinkers. The obtained microparticles contained approximately 30% (w/w) drug and showed as spherical particles with a size of about 2 μm. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) analysis indicated that GA lost its crystallinity during the nano/microencapsulation process. In vitro dissolution study demonstrated a typical sustained-release pattern for 24 h with a burst of 28.1% at the first 30 min, which fitted well by Higuchi model. After intravenous administration into mice, the microparticle formulation remained a higher drug level than the solution formulation in blood and liver for more than 18 h. These results suggested the potential benefit of using the prepared albumin microparticles as a promising vector for enhanced liver delivery of poorly water-soluble drug. © 2016 Informa UK Limited, trading as Taylor & Francis Group