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Zhang Z.-W.,Hebei University of Science and Technology | Zhang X.-F.,Hebei University of Science and Technology | Feng J.,Hebei University of Science and Technology | Yang Y.-H.,Hebei University of Science and Technology | And 3 more authors.
Journal of Organic Chemistry

A formal synthesis of cephalotaxine, the parent member of the Cephalotaxus alkaloids, was achieved. It features a practical four-step assembly of the benzazepine-bearing pentacyclic ring system through two alkylation reactions, acidic hydrolysis, and aldolization. © 2012 American Chemical Society. Source

Wang L.,Tianjin University of Science and Technology | Yang S.,Tianjin University of Science and Technology | Cao J.,Tianjin University of Science and Technology | Zhao S.,Shijiazhuang Yiling Pharmaceutical Co. | Wang W.,Tianjin University of Science and Technology
Chemical and Pharmaceutical Bulletin

The coacervation between gelatin and sodium alginate for ginger volatile oil (GVO) microencapsulation as functions of mass ratio, pH and concentration of wall material and core material load was evaluated. The microencapsulation was characterized by scanning electron microscopy (SEM), Fourier transform infrared (FT-IR), and thermal gravimetric analysis (TGA). SEM and FT-IR studies indicated the formation of polyelectrolyte complexation between gelatin and sodium alginate and successful encapsulation of GVO into the microcapsules. Thermal property study showed that the crosslinked microparticles exhibited higher thermal stability than the neat GVO, gelatin, and sodium alginate. The stability of microencapsulation of GVO in a simulated gastric and an intestinal situation in vitro was also studied. The stability results indicated that the release of GVO from microcapsules was much higher in simulated intestinal fluid, compared with that in simulated-gastric fluid. © 2016 The Pharmaceutical Society of Japan. Source

Liu M.Y.,Shijiazhuang Yiling Pharmaceutical Co.
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials

To establish an HPLC method for simultaneous determination of six organic acids in Lonicerae japonicae Flos and Lonicerae Flos in different habitats. The chromatographic separation was carried out on a Waters C18 column (4. 6 mm x 250 mm, 5 microm) with gradient elution of acetonitrile and 0.1% phosphoric acid at a flow rate of 1 mL/min. The detection wave-length was 326 nm. The contents of neochlorogenic acid and cryptochlorogenic acid in Lonicerae japonicae Flos in different habitats were very low. The contents of chlorogenic acid in Lonicerae japonicae Flos in Pingyi, Fei County, Fengqiu and Jvlu were significantly higher than that in Shangluo, but the contents of other organic acids were similar. The contents of six kinds of organic acids in Lonicerae Flos in different origins were obviously higher than those in Lonicerae japonicae Flos. A simple, accurate and credible method is developed and validated for quality control of six organic acids from Lonicerae japonicae Flos and Lonicerae Flos. Source

Wang D.,Huazhong University of Science and Technology | Tian M.,Huazhong University of Science and Technology | Qi Y.,Huazhong University of Science and Technology | Chen G.,Huazhong University of Science and Technology | And 6 more authors.
Journal of Ethnopharmacology

Ethnopharmacological relevance Jinlida granule (JLDG), composed of seventeen Chinese medical herbs, is a widely used Chinese herbal prescription for treating diabetes mellitus. However, the mechanism underlying this effect remains unclear. To determine the main components in JLDG and to explore the effect of JLDG on autophagy and lipid accumulation in NIT-1 pancreatic β cells exposed to politic acid (PA) through AMP activated protein kinase (AMPK) signaling pathway. Materials and methods JLDG was prepared and the main components contained in the granules were identified by ultra performance liquid chromatography (UPLC) fingerprint. Intracellular lipid accumulation in NIT-1 cells was induced by culturing with medium containing PA. Intracellular lipid droplets were observed by Oil Red O staining and triglyceride (TG) content was measured by colorimetric assay. The formation of autophagosomes was observed under transmission electron microscope. The expression of AMPK and phospho-AMPK (pAMPK) proteins as well as its downstream fatty acid metabolism-related proteins (fatty acid synthase, FAS; acetyl-coA carboxylase, ACC; carnitine acyltransferase 1, CPT-1) and autophagy-related genes (mammal target of rapamycin, mTOR; tuberous sclerosis complex 1, TSC1; microtubule-associated protein 1 light chain 3, LC3-II) were determined by Western blot. The expression of sterol regulating element binding protein 1c (SREBP-1c) mRNA was examined by real time PCR (RT-PCR). Results Our data showed that JLDG could significantly reduce PA-induced intracellular lipid accumulation in NIT-1 pancreatic β cells. This effect was associated with increased protein expression of pAMPK and AMPK in NIT-1 cells. Treatment with JLDG also decreased the expression of AMPK downstream lipogenic genes (SREBP-1c mRNA, FAS and ACC proteins) whereas increased the expression of fatty acid oxidation gene (CPT-1 protein). Additionally, JLDG-treated cells displayed a markedly increase in the number of autophagosomes which was accompanied by the down-regulation of mTOR and the up-regulation of TSC1 and LC3-II proteins expression. However, when AMPK phosphorylation was inhibited by Compound C, JLDG supplementation did not exhibit any effect on the expression of these AMPK downstream molecules in NIT-1 cells. Conclusions The results suggest that JLDG could reduce intracellular lipid accumulation and enhance the autophagy in NIT-1 pancreatic β cells cultured with PA. The mechanism is possibly mediated by AMPK activation. © 2014 The Authors. Source

Shijiazhuang Yiling Pharmaceutical Co. | Date: 2012-09-26

()-(S)-3-(3-hydroxy)-butylphthalide (a compound shown by Formula I) and an ester formed of the same and an acid are proved by experiments to be applicable to treatment and prevention of cerebral ischemic diseases and have a sleep-improving function. The acid refers to a pharmaceutically acceptable inorganic or organic acid. The inorganic acid refers to nitric acid, sulfuric acid, or phosphoric acid. In addition to an acid radical, the organic acid at least comprises at least one of an amino group, a hydroxyl group, and a carboxyl group. None of the compound shown by Formula I and the ester thereof is water-soluble. An ester generated from the compound and the acid further react with an acid or a base to generate a salt which is water-soluble and is used to prepare injection preparation. The experiment proves that the salt does not stimulate vessels.

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