Design, synthesis, and neuroprotective and anti-platelet aggregation research of 3-n-butylphthalide derivatives / 药学学报

Butylphthalide and ferulic acid exhibit excellent therapeutic effects in ischemic stroke. In this research, twelve 3-n-butylphthalide derivatives were designed by molecular hybridization strategy. The target compounds were obtained by nucleophilic substitution, reduction reaction, esterification reaction and elimination reaction, and the structure was confirmed by 1H NMR, 13C NMR and ESI-MS. All compounds were evaluated for neuroprotective activity against OGD/R-induced neurotoxicity in rat cortical neurons by MTT assay. The compounds with the best neuroprotective activity were biologically evaluated for their ability to inhibit platelet aggregation induced by arachidonic acid (AA) and adenosine diphosphate (ADP) via the Bron method．The results indicate that 7b exhibited potent neurocyte protective activity as well as prominent anti-platelet aggregation activity. Compound 7b has potential to be developed as a drug for ischemic stroke.

Design, synthesis, and biological evaluation of phenylpropenamides compounds as anti-platelet aggregation / 药学学报

Twenty phenylpropenamide analogs with structural novelty were designed and synthesized upon pharmacophore-combination strategy. The structures of target compounds were elucidated by IR, 1H NMR, 13C NMR and MS, and all the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by adenosine diphoshate (ADP) and (AA) arachidonic acid via Bron method. As a result, compounds 6b, 9b, 9d and 9h demonstrated potent inhibitory activity against platelet aggregation induced by AA. Meanwhile, compounds 6b, 6d, 6j, 9b and 9g exhibited significant suppression of platelet aggregation induced by ADP.

Design, synthesis and biological evaluation of the novel ligustrazine derivatives / 药学学报

Using ligustrazine as the leading compound, we designed and synthesized ten novel ligustrazine derivatives, whose structures were determined by 1H NMR, 13C NMR and MS. Inhibitory effects of the new compounds on the proliferation of A549, A549/DDP and HBE cells were detected by MTT assay. The inhibi-tory activity of the synthesized compounds on migration and invasion of A549 cells were evaluated through scratch assay and transwell assay. Mechanism of the inhibition on migration and invasion was investigated by Western blotting. In addition, the cell cycle was analyzed with flow cytometry. The results showed that, both compounds Z8 and Z10 have an anti-proliferative activity, and the potencies of inhibition of tumor-cell migration and invasion were attributed to the down-regulation of MMP-2 and MMP-9. The compounds Z8 and Z10 could also enhance G2/M arrest in A549 cell as revealed by cell cycle analysis.

Host contributions to Ebola virus replication, transcription and translation:research advances / 军事医学

Ebola virus(EBOV) disease,the fatality rate of which is as high as 25％-90％,can be transmitted by contac t between human and non-human primates.Early studies of the virus focused on the functions of viral proteins.Recently,the focus of research of EBOV has been switched to the host interaction factors during the process of virus reproduction.In this review,advances in studies on host contributions to EBOV replication,transcription and translation are summarized in order to enhance our understanding of contributions of the host to the virus reproduction process and provide reference for research strategies and new antiviral drugs.

Synthesis and biological evaluation of novel chalcone aromatic oxygen alkyl acids compounds / 药学学报

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.

Design, synthesis and anti-platelet aggregation activities of ligustrazine-tetrahydroisoquinoline derivatives / 药学学报

Abstract: 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.

Design, synthesis and antitumor activity of valproic acid salicylanilide esters / 药学学报

A series of valproic acid salicylanilide esters were designed and synthesized based on the principle of prodrug. The structures of the target compounds were confirmed by MS, 1H NMR and 13C NMR. Anti-tumor activities of these compounds against K562, A549, A431 cells in vitro were investigated by MTT assay and SRB assay. The results indicated that the compounds 6h-6j were found to have stronger cell growth inhibitory action than gefitinib, and comparable to niclosamide, which are worth to be intensively studied further.

Facial nerve preservation following microsurgical removal of large and huge acoustic neuroma / 中华外科杂志

<p><b>OBJECTIVES</b>To evaluate the long-term facial nerve function of patients following microsurgical removal of large and huge acoustic neuroma, and to identify the factors that influence these outcomes.</p><p><b>METHODS</b>A retrospective review was performed which included 176 consecutive patients with a large acoustic neuroma (≥ 30 mm) underwent a retrosigmoid craniotomy for tumor resection between January 2002 to November 2009. House-Brackmann (HB) Scale was used preoperatively and in a long-term follow-up after surgery. Test for linear trend was applied for statistic analysis.</p><p><b>RESULTS</b>Complete resection was achieved in 168 (95.5%) of these 176 patients with a mortality of 1.7%. Anatomic preservation of the facial nerve was attained in 96.0% of the patients. In the series of 96 patients who had at least 1-year follow-up (mean 3.0 years) the facial nerve function preservation (HB grade 1 - 2) was totally attained in 79 patients (82.3%), and 40 of 55 patients (72.7%) who presented huge tumors (diameter > 40 mm) among the 96 patients had facial nerve function preserved. Analysis showed that facial nerve function correlated linearly with tumor sizes (χ(2) = 14.114, ν = 1, P < 0.05).</p><p><b>CONCLUSIONS</b>Complete removal of large and giant acoustic neuroma may be obtained via retrosigmoid approach with facial nerve preservation. Excellent long-term facial function can be expected in the majority of patients who undergo microsurgical removal of vestibular schwannoma via the suboccipital retrosigmoid approach. Tumor size is a significant prognostic parameter for facial nerve function following vestibular schwannoma surgery.</p>

Synthesis of ferulic acid derivatives and their inhibitory effect on platelet aggregation / 药学学报

Ferulic acid, an useful compound of Chinese traditional medicine, was used as leading compound. Six ferulic acid derivatives were designed and synthesized based on bioisosterism. Their structures were characterized by IR, 1H NMR, 13C NMR and mass spectra. In vivo experiment showed that ferulic acid derivatives had good inhibitory effects on adenosine diphosphate (ADP) induced platelet aggregation, which were significantly higher than that of Ozagrel.

Design, synthesis and Na+/H+ exchanger isoform-1 inhibitory activity of feruloylagmatine analogues / 药学学报

In order to search for novel inhibitors of Na+/H+ exchanger isoform-1 (NHE-1), nine feruloylagmatine analogues were designed and synthesized from ferulic acid and agmatine. The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR and mass spectra, among which compounds 5f-5i were novel compounds. The results of preliminary pharmacological test showed that some of the compounds possessed strong NHE-1 inhibitory activity, among which compounds 5a, 5b and 6c were more potent than cariporide in NHE-1 inhibition.