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Chen Y.-L.,Anhui University | Chen Y.-L.,China Pharmaceutical University | Gui S.-Y.,Anhui University | Gui S.-Y.,Anhui Academy of Chinese Medicine | And 3 more authors.
Yaoxue Xuebao | Year: 2016

Phytantriol (PT), ethanol (ET) and water were used to prepare in situ cubic liquid crystal (ISV2). The pseudo-ternary phase diagram of PT-ET-water was constructed and isotropic solution formulations were chosen for further optimization. The physicochemical properties of isotropic solution formulations were evaluated to optimize the composition of ISV2. In situ hexagonal liquid crystals (ISH2) were prepared based on the composition of ISV2 with the addition of Vitamin E acetate (VitEA) and the amount of VitEA was optimized by in vitro release behavior. The phase structures of liquid crystalline gels formed by ISV2 and ISH2 in excess water were confirmed by crossed polarized light microscopy and small angle X-ray scattering, respectively. Rheological properties of ISV2 and ISH2 were studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using a dialysis membrane diffusion method. Pharmacokinetics was investigated by determination of sinomenine hydrochloride (SMH) concentration in synovial membrane after intra-articular injection of SMH-loaded ISH2 in adjuvant-induced arthritis rats. The optimal ISV2 (PT/ET/water, 64:16:20, w/w/w) loaded with 6 mg·g-1 of SMH showed a suitable pH, injectable and formed a cubic liquid crystalline gel in situ with minimum water absorption in the shortest time. The optimal ISV2 was able to sustain the drug release for 144 h. The optimal ISH2 system was prepared by addition of 5% VitEA into PT in the optimal ISV2 system. This ISH2 (PT/VitEA/ET/water, 60.8:3.2:16:20, w/w/w/w) was an injectable isotropic solution with suitable pH. The new ISH2 was able to sustain the drug release for more than 240 h. Local pharmacokinetics study indicated that the retention time and AUC0-∞ of ISH2 group were increased significantly compared with that of SMH solution group and the AUC0-∞ of ISH2 group was 6.01 times higher than that of SMH solution group. The developed ISH2 was suitable for intra-articular injection that may apply to patients in the treatment of rheumatoid arthritis. Source


Xie D.,Anhui University | Xie D.,Anhui Academy of Chinese Medicine | Zhang E.-L.,Anhui University | Zhang E.-L.,Anhui Academy of Chinese Medicine | And 5 more authors.
Yaoxue Xuebao | Year: 2015

Fifteen novel ligustrazine-tetrahydroisoquinoline derivatives were designed and synthesized according to the association principle of pharmaceutical chemistry. The structures were identified by IR, NMR and ESI-MS. The inhibitory activities of platelet aggregation induced by ADP and AA have been measured by Bron method. Preliminary pharmacological results showed that compounds 7g, 7h and 7n had potent inhibitory activity against platelet aggregation induced by AA, and the compound 7O showed significant inhibitory activity against platelet aggregation induced by ADP. Source


Wu D.-Q.,Anhui University | Wu D.-Q.,Anhui Academy of Chinese Medicine | Huang W.-F.,Anhui University | Huang W.-F.,Anhui Academy of Chinese Medicine | And 6 more authors.
Zhongguo Zhongyao Zazhi | Year: 2015

Sodium houttuyfonate (SH) is a derivative of effective component of a Chinese material medica, Houttuynia cordata, which is applied in anti-infection of microorganism But, the antimicrobial mechanisms of SH still remain unclear. Here, we firstly discovered that SH effectively inhibits the three types of virulence related motility of Pseudomonas aeruginosa, i.e., swimming, twitching and swarming. The plate assay results showed that the inhibitory action of SH against swimming and twitching in 24 h and swarming in 48 h is dose-dependent; and bacteria nearly lost all of the motile activities under the concentration of 1 × minimum inhibitory concentration (MIC) (512 mg · L-1) same as azithromycin positive group (1 × MIC, 16 mg · L-1). Furthermore, we found that the expression of structural gene flgB and pilG is down-regulated by SH, which implies that inhibitory mechanism of SH against motility of P. aeruginosa may be due to the inhibition of flagella and pili bioformation of P. aeruginosa by SH. Therefore, our presented results firstly demonstrate that SH effectively inhibits the motility activities of P. aeruginosa, and suggest that SH could be a promising antipseudomonas agents in clinic. Source


Wang T.-M.,Anhui University | Wang T.-M.,Anhui Academy of Chinese Medicine | Yan Y.-Y.,Anhui University | Yan Y.-Y.,Anhui Academy of Chinese Medicine | And 8 more authors.
Chinese Traditional and Herbal Drugs | Year: 2014

Objective: To observe the effects of ethyl acetate extract from Huanglian Jiedu Decoction (EAHJD) on the virulence factors of Candida albicans. Methods: Egg-yolk medium, milk-plate medium, and olive oil emulsification were used respectively to test the activities of phospholipase (PL), aspartic protease (Sap), and lipase (Lip) of C. albicans. The water-hydrocarbon two-phase assay was applied to measure the cell surface hydrophobicity (CSH) of C. albicans. qRT-PCR was adopted to observe the expression of virulence factors related genes. Results: EAHJD had no effect on the activity of PL. EAHJD (1 250 μg/mL) could significantly inhibit the activity of PL and Lip better than that by 312 μg/mL EAHJD. EAHJD could reduce CSH of C. albicans in a dose-independent manner and CSH1 was down-regulated by 7.69, 3.57, and 2.95 folds by 1 250, 312, and 78 μg/mL EAHJD, respectively. The expression of secretory enzyme related genes displayed different changing folds: PLC1, Sap2, Sap3, Sap9, Lip3, Lip4, and Lip6 were down-regulated; PLB1, PLC2, Sap1, Sap10, and Lip5 had no distinct change treated by EAHJD. Conclusion: EAHJD could inhibit the activities of virulence factors of C. albicans. ©, 2014, Editorial Office of Chinese Traditional and Herbal Drugs. All right reserved. Source


Huang W.-J.,Anhui University | Huang W.-J.,Anhui Academy of Chinese Medicine | Xie D.,Anhui University | Xie D.,Anhui Academy of Chinese Medicine | And 8 more authors.
Yaoxue Xuebao | Year: 2016

Six novel ligustrazine chalcone aromatic oxygen alkyl acids compounds and two pyridine chalcone aromatic oxygen alkyl acids ester compounds were synthesized according to the traditional Chinese medicine theory removing blood stasis. The structures of target compounds were identified by IR, NMR and ESI-MS. The inhibitory activities of platelet aggregation induced by adenosine diphosphate (ADP) and arachidonic acid (AA) were measured by the liver microsomal incubation method in vitro. Hypolipidemic activities of compounds were tested in vivo for better inhibitory activities of platelet aggregation. Preliminary pharmacological results showed that compounds 7c, 8a and 11a had potent inhibitory activity against platelet aggregation induced by AA, compounds 7c, 7d, 8a and 11b showed significant inhibitory activity against platelet aggregation induced by ADP. Compounds 7c and 8a exhibited good hypolipidemic activities in high-fat-diet (HFD) induced hyperlipidemia C57/BL6 mice and worthy for further investigation. Source

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