Synthesis of novel quinolinomatrine derivatives and their insecticidal/acaricidal activities.

In continuation of our program to discover natural product-based pesticidal agents, a series of new quinolinomatrine derivatives were prepared. Especially three-dimensional structures of five compounds were unambiguously determined by single-crystal X-ray diffraction. Among them, 21-chloroquinolinomatrine exhibited good insecticidal and acaricidal activities against two crop-threatening insect pests, Mythimna separata and Tetranychus cinnabarinus.

14-Formyl-15-aryloxy/methoxymatrine and 14-Aryloxymethylidenyl-matrine Derivatives as Anti-HIV-1 Agents.

Background: The human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS) has always been a global health threat and leading cause of deaths. However, due to the emergence of drug-resistant HIV, an inevitable consequence of increasing use of antiretroviral drugs posed a major threat to antiretroviral therapy success.

Objective: The discovery of anti-HIV-1 agents will be used for the effective treatment of HIV/AIDS.

Seven-Membered Lactam Derivatives of Podophyllotoxins as New Pesticidal Agents.

As a continuation of our efforts to discover and develop natural-product-based insecticidal agents, three novel and unusual 7-membered lactam derivatives of podophyllotoxin were prepared by thionyl chloride-mediated ring-expanded Beckmann rearrangement. The steric configurations of 3a-c were unambiguously identified by X-ray crystallography. It demonstrated that the configuration of the picropodophyllotoxin C4-oximes could also be confirmed by the corresponding C-ring expansion products via Beckmann rearrangement.

Synthesis of some ester derivatives of 4'-demethoxyepipodophyllotoxin/2'-chloro-4'-demethoxyepipodophyllotoxin as insecticidal agents against oriental armyworm, Mythimna separata Walker.

Podophyllotoxin is a naturally occurring non-alkaloid toxin isolated from the roots and rhizomes of Podophyllum peltatum and P. hexandrum. In continuation of our program aimed at the discovery and development of natural product-based insecticides, two series of ester derivatives of 4'-demethoxyepipodophyllotoxin/2'-chloro-4'-demethoxyepipodophyllotoxin were prepared.

Matrine: Bioactivities and Structural Modifications.

Matrine is a quinolizidine alkaloid isolated from the roots of Sophora flavescens (Kushen), Sophora tonkinensis, and Sophora alopecuroides (Kudouzi). Matrine and its derivatives have displayed a broad scope of biological properties such as anticancer activity, anti-inflammatory activity, antiviral activity, analgesic effect, anti-fibrotic activity, insecticidal activity, antimicrobial activity, etc. The present review has summarized the biological activities and structural modifications of matrine and its derivatives focused on their N-1 position and lactam ring from 2010 to 2015.