Bioassay-guided fractionation of a methanol extract of the seeds of Caesalpinia sappan led to the isolation of 12 new cassane-type diterpenes, caesalsappanins A-L (1-12). Their structures were elucidated on the basis of NMR and HRESIMS analysis, and the absolute configuration of compound 1 was determined by single-crystal X-ray crystallography. All isolated compounds were tested against a chloroquine-resistant Plasmodium falciparum strain for antiplasmodial activities and against a small panel of human cancer cell lines for antiproliferative activities. Compounds 7 and 8 displayed antimalarial activity against the chloroquine-resistant K1 strain of P. falciparum with IC50 values of 0.78 and 0.52 μM and selectivity indices of 17.6 and 16.4, respectively. Compound 10 showed antiproliferative activity against the KB cancer cell line with an IC50 value of 7.4 μM.

Abstract. The regional transport of air pollutants, controlled by emission sources and meteorological factors, results in a complex source–receptor relationship of air pollution change. Wuhan, a metropolis in the Yangtze River middle basin (YRMB) of central China, experienced heavy air pollution characterized by hourly PM2.5 concentrations reaching 471.1 µg m−3 in January 2016. To investigate the regional transport of PM2.5 over central eastern China (CEC) and the meteorological impact on wintertime air pollution in the YRMB area, observed meteorological and other relevant environmental data from January 2016 were analyzed. Our analysis presented noteworthy cases of heavy PM2.5 pollution in the YRMB area with unique “non-stagnant” meteorological conditions of strong northerly winds, no temperature inversion, and additional unstable structures in the atmospheric boundary layer. This unique set of conditions differed from the stagnant meteorological conditions characterized by near-surface weak winds, air temperature inversion, and stable structure in the boundary layer that are typically observed in heavy air pollution over most regions in China. The regional transport of PM2.5 over CEC aggravated PM2.5 levels, thus creating heavy air pollution in the YRMB area. This demonstrates a source–receptor relationship between the originating air pollution regions in CEC and the receiving YRMB region. Furthermore, a backward trajectory simulation using a Flexible Particle dispersion (FLEXPART) Weather Research and Forecasting (WRF) model to integrate the air pollutant emission inventory over China was used to explore the patterns of regional transport of PM2.5 governed by the strong northerly winds in the cold air activity of the East Asian winter monsoon season. It was estimated that the regional transport of PM2.5 from non-local air pollutant emissions contributes more than 65 % of the PM2.5 concentrations to the heavy air pollution in the YRMB region during the study period, revealing the importance of the regional transport of air pollutants over China as a causative factor of heavy air pollution over the YRMB area.

Eight new cassane-type diterpenes, caesalpins A-H (1-8), were isolated from the ethyl acetate extract of Caesalpinia minax. Compound 1 displayed significant antiproliferative activity against HepG-2 (IC50 4.7 μM) and MCF-7 (IC50 2.1 μM) cells, and compounds 2 and 4 exhibited selective cytotoxic activities against MCF-7 (IC50 7.9 μM) and AGS (IC50 6.5 μM) cells.

Natural daphnane diterpenoids, mainly distributed in plants of the Thymelaeaceae and Euphorbiaceae families, usually include a 5/7/6-tricyclic ring system with poly-hydroxyl groups located at C-3, C-4, C-5, C-9, C-13, C-14, or C-20, while some special types have a characteristic orthoester motif triaxially connectedat C-9, C-13, and C-14. The daphnane-type diterpenoids can be classified into five types: 6-epoxy daphnane diterpenoids, resiniferonoids, genkwanines, 1-alkyldaphnanes and rediocides, based on the oxygen-containing functions at rings B and C, as well as the substitution pattern of ring A. Up to now, nearly 200 daphnane-type diterpenoids have been isolated and elucidated from the Thymelaeaceae and Euphorbiaceae families. In-vitro and in-vivo experiments of these compounds have shown that they possess a wide range of biological activities, including anti-HIV, anti-cancer, anti-leukemic, neurotrophic, pesticidal and cytotoxic effects. A comprehensive account of the structural diversity is given in this review, along with the cytotoxic activities of daphnane-type diterpenoids, up to April 2019.