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Huo M.,China Pharmaceutical University | Zou A.,China Pharmaceutical University | Yao C.,China Pharmaceutical University | Zhang Y.,Jiangsu Chia Tai Tianqing Pharmacy Co. | And 5 more authors.
Biomaterials | Year: 2012

In this study, a ligand-PEG-lipid conjugate, octreotide-polyethene glycol-deoxycholic acid (OCT(Phe)-PEG-DOCA, or OPD) was successfully synthesized and used as a targeting molecule for N-deoxycholic acid-O, N-hydroxyethylation chitosan (DAHC) micelles for efficient cancer therapy. DAHC micelles exhibited good loading capacities for doxorubicin (DOX), a model anti-cancer drug, and the modification of OPD showed no significant effect on drug load while slightly increasing the particle size and partly shielding the positive charges on the surface of micelles. Accelerated release rate of DOX from micelles were also observed after OPD modification and the release profile exhibited pH-sensitive properties. Compared with DAHC-DOX micelles, OPD-DAHC-DOX micelles exhibited significantly stronger cytotoxicity to MCF-7 cells (SSTRs overexpression) but with hardly any difference from WI-38 cells (no SSTRs expression). The results of flow cytometry and confocal laser scanning microscopy further revealed that OPD-DAHC-DOX micelles could be selectively taken into tumor cells by SSTRs-mediated endocytosis. In vivo investigation of micelles on nude mice bearing MCF-7 cancer xenografts confirmed that OPD-DAHC micelles possessed much higher tumor-targeting capacity than the DAHC control and exhibited enhanced anti-tumor efficacy and decreased systemic toxicity. These results suggest that OPD-DAHC micelles might be a promising anti-cancer drug delivery carrier for targeted cancer therapy. © 2012 Elsevier Ltd. Source

Li J.,China Pharmaceutical University | Huo M.,China Pharmaceutical University | Wang J.,China Pharmaceutical University | Zhou J.,China Pharmaceutical University | And 6 more authors.
Biomaterials | Year: 2012

A targeted intracellular delivery system of paclitaxel (PTX) was successfully developed based on redox-sensitive hyaluronic acid-deoxycholic acid (HA-ss-DOCA) conjugates. The conjugates self-assembled into nano-size micelles in aqueous media and exhibited excellent drug-loading capacities (34.1%) and entrapment efficiency (93.2%) for PTX. HA-ss-DOCA micelles were sufficiently stable at simulated normal physiologic condition but fast disassembled in the presence of 20m. m reducing agent, glutathione. Invitro drug release studies showed that the PTX-loaded HA-ss-DOCA micelles accomplished rapid drug release under reducing condition. Intracellular release of fluorescent probe nile red indicated that HA-ss-DOCA micelles provide an effective approach for rapid transport of cargo into the cytoplasm. Enhanced cytotoxicity of PTX-loaded HA-ss-DOCA micelles further confirmed that the sensitive micelles are more potent for intracellular drug delivery as compared to the insensitive control. Based on flow cytometry and confocal microscopic analyses, observations revealed that HA-ss-DOCA micelles were taken up to human breast adenocarcinoma cells (MDA-MB-231) via HA-receptor mediated endocytosis. Invivo investigation of micelles in tumor-bearing mice confirmed that HA-ss-DOCA micelles possessed much higher tumor targeting capacity than the insensitive control. These results suggest that redox-sensitive HA-ss-DOCA micelles hold great potential as targeted intracellular delivery carriers of lipophilic anticancer drugs. © 2011. Source

Qin J.-H.,Anhui Agricultural University | Li N.,State Key Laboratory of Natural and Biomimetic Drugs | Tu P.-F.,State Key Laboratory of Natural and Biomimetic Drugs | Ma Z.-Z.,Peking University | Zhang L.,Anhui Agricultural University
Journal of Agricultural and Food Chemistry | Year: 2012

The aim of this study was to evaluate tea polyphenol and purine alkaloid contents of pu-erh tea (Camellia assamica) in a fermentation solid system with Aspergillus niger and Aspergillus fumigatu. In addition, the objective was to find the major intermediate product during fermentation by HPLC-MS n analysis. The results showed the change of catechin, ester-catechins and gallic acid by quantitative analysis. In the early stages, the contents of ester-catechins were lightly increased. Then, ester-catechins were gradually degraded to produce catechins and gallic acid. Furthermore, a major metabolic intermediate compound of catechins was observed and elucidated by HPLC-DAD-MS n analysis. This study provided a reliable dynamic data description and metabolic pathway of tea polyphenols for postfermented pu-erh tea. © 2012 American Chemical Society. Source

Ma L.-Y.,State Key Laboratory of Natural and Biomimetic Drugs | Yang X.-W.,State Key Laboratory of Natural and Biomimetic Drugs
Chinese Traditional and Herbal Drugs | Year: 2016

Objective: To study the chemical constituents of alkaline hydrolysates of total saponins from the stems and leaves of Panax ginseng. Methods: The chemical constituents were isolated and purified by various chromatographic methods, and the chemical structures were identified by NMR and MS spectra analyses. Results: A total of 30 compounds were isolated and identified. Among them, 28 were determined as 20(S)-protopanaxadiol (1), 20(R)-protopanaxadiol (2), dammar-20(21),24-diene-3β,6α,12β-triol (3), dammar-20(22)E,24-diene-3β,6α,12β-triol (4), 20(S)-protopanaxatriol (5), 20(R)-protopanaxatriol (6), 20(S)-ginsenoside Rh2 (7), 20(R)-ginsenoside Rh2 (8), ginsenoside Rh16 (9), isoginsenoside Rh3 (10), 20(S)-dammar-3β,6α,12β,20,25-pentol (11), 20(R)-dammar-3β,6α,12β,20,25-pentol (12), ginsenoside Rk3 (13), 20(S)-ginsenoside Rh1 (14), 20(R)-ginsenoside Rh1 (15), ginsenoside F1 (16), ginsenoside Rh19 (17), 20(R)-ginsenoside Rh19 (18), dammar-20(22)E-ene-3β,6α,12β,25-tetrol (19), notoginsenoside T2 (20), ginsenoside Rg6 (21), 20(22)E-ginsenoside F4 (22), ginsenoside Rk1 (23), 20(S)-ginsenoside Rg3 (24), 20(R)-ginsenoside Rg3 (25), 20(S)-ginsenoside Rg2 (26), 20(R)-ginsenoside Rg2 (27), and 3β,6α,12β,25-tetrahydroxy-dammar-20(22)E-ene-6-O-α-L-rhamno- pyranosyl-(1→2)-β-D-glucopyranoside (28). Conclusion: Compound 18 is a new saponin. Compounds 3, 4, 11, 12, and 19 are rare dammarane-type triterpenes, and 7-10, 13-18, and 20-28 are rare ginsenosides. © 2016, Editorial Office of Chinese Traditional and Herbal Drugs. All right reserved. Source

Yang X.-B.,Chinese Academy of Sciences | Yang X.-B.,Beijing University of Chinese Medicine | Yang X.-B.,State Key Laboratory of Natural and Biomimetic Drugs | Yang X.-W.,State Key Laboratory of Natural and Biomimetic Drugs | And 2 more authors.
Zhongguo Zhongyao Zazhi | Year: 2014

Corydalis Rhizoma, the dried tuber of Corydalis yanhusuo (Papaveraceae) distributed traditionally mainly in southeastern and now cultivated in northwestern and other district in China, is one of the commonly used and well-known traditional Chinese medicine. It has been widely used to treat spastic pain, abdominal pain, pain due to injury, and promote blood circulation. Its main chemical constituents were alkaloids, which were divided into the two types of protoberberines and aporphines. Among them, some alkaloids were found to elicit profound effects on the dopaminergic system in the central nervous system, which plays an important role in regulating nociception. In this article, the chemical composition and structure-types, new methods of qualitative and quantitative analysis as well as characteristics of biotransformation, absorption, distribution, metabolism, excretion, pharmacokinetic, and drug-drug interaction for the alkaloids were revealed. These results would greatly contribute to the establishment of bioactive material base of Corydalis Rhizoma. Source

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