New advances in baicalein's antitumor effects and mechanisms / 药学实践杂志

Baicalein (BE) is an active ingredient derived from the root of Scutellaria baicalensis Georgi. It is a polyhydroxyflavonoid in structure and has many biological activities. Among them, the antitumor effects of baicalein have received widespread attention. It exerts anti-tumor effects by inducing tumor cell apoptosis and invasion, inhibiting tumor angiogenesis, and eliminating free radicals. This article reviews the most recent research works of baicalein in its anti-tumor effects and mechanisms. It is aimed to provide a theoretical basis for the search and development of potential new anti-tumor drugs.

Study on synthesis and antifungal activities of galloyl piperazine derivatives / 药学实践杂志

Objective To design, synthesize and measure antifungal activities of galloyl piperazine derivatives. Methods Trimethoxyl gallic acid was used as starting material, reacted with piperazine in the presence of PyBOP/DIEA to afford the intermediates. The target compounds were obtained through the reaction with corresponding acids after deprotection gave. The antifungal activities of the target compounds were evaluated by FLC-resistant Candida albican isolated according to the CLSI recommended method. Results 11 target compounds were synthesized and six of them showed more potent antifungal activities than gallic acid. Conclusion Galloyl piperazine derivatives could enhance antifungal activities. Galloyl moiety was an important pharmacophore, which could improve antifungal activities with the introduction of cinnamic acid and 2,3-dichlorobenzoic acid.

Research progress in sinomenine structural modification / 药学实践杂志

Sinomenine is an alkaloid found in the climbing plant Sinomenium acutum.Structurally,it belongs to the iso-quinoline derivatives,which have various bioactivities.Clinically,it is used in the treatment for rheumatism,rheumatoid arthri-tis and arrhythmia,etc.Nevertheless,due to the need of large dose,photo and thermal instability,quick metabolism in vivo and highly allergic for some patients,scientists have committed to modify its structure to develop the highly effective and low toxic derivatives.In this paper,the recent advances in structural modification of sinomenine are reviewed.