Design, synthesis, and biological evaluation of ligustrazine/resveratrol hybrids as potential anti-ischemic stroke agents / 中国天然药物

To search for potent anti-ischemic stroke agents, a series of tetramethylpyrazine (TMP)/resveratrol (RES) hybrids 6a-t were designed and synthesized. These hybrids inhibited adenosine diphosphate (ADP)- or arachidonic acid (AA)-induced platelet aggregation, among them, 6d, 6g-i, 6o and 6q were more active than TMP. The most active compound 6h exhibited more potent anti-platelet aggregation activity than TMP, RES, as well as positive control ticlopidine (Ticlid) and aspirin (ASP). Furthermore, 6h exerted strong antioxidative activity in a dose-dependent manner in rat pheochromocytoma PC12 cells which were treated with hydrogen peroxide (HO) or hydroxyl radical (·OH). Importantly, 6h significantly protected primary neuronal cells suffered from oxygen-glucose deprivation/reoxygenation (OGD/R) injury, comparable to an anti-ischemic drug edaravone (Eda). Together, our findings suggest that 6h may be a promising candidate warranting further investigation for the intervention of ischemic stroke.

In vitro Antiviral activity of a berberine derivant HB-13 against herpes simplex virus / 中华皮肤科杂志

Objective To evaluate the in vitro antiviral activity of HB-13,a compound derivant from berberine and its prodrug berberine,against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2). Methods Vero cells were cultured in vitro and infected with HSV.Then,various concentrations of HB-13, berberine,and aciclovir were used to treat these infected cells.The cytopathic effect was observed to deter- mine the antiviral effects and cytotoxicity of HB-13 and berberine.Results For HB-13,berberine and acy- clovir,the half toxicity concentration (TC_(50)) to Vero cells was 31.99,380 and more than 800?g/mL, respectively;the average half inhibitory concentration (IC_(50)) against HSV-1 was 1.328,more than 100,and 0.443?g/mL,respectively,the treatment index (TI) against HSV-1 was 24.09,less than 3.80,and more than 1805.87,respectively;the IC_(50) against HSV-2 was 1.344,more than 100,and 0.679?g/mL,respectively,the TI against HSV-2 was 23.80,less than 3.80 and more than 1178.20,respectively.Conclusion HB-13 possesses marked antiviral activity against HSV-1 and HSV-2 in vitro,while berberine does not.