Activity-guided fractionation strategy was used to investigate chemical constituents from the roots of Podocarpus macrophyllus. Successfully, two new norditerpenes, 2β-hydroxymakilactone A (1) and 3β-hydroxymakilactone A (2), along with ten known analogues (3 - 12) were isolated. The structures of 1 and 2 were elucidated by spectroscopic analysis including 1D-, 2D-NMR, and HR-ESI-MS data. The previously reported structure of 2,3-dihydro-2α-hydroxypodolide was revised as 2,3-dihydro-2β-hydroxypodolide (3) by spectroscopic analysis, and was further confirmed by X-ray crystallographic analysis. Cytotoxic activities of all isolated compounds against five human solid tumour cell lines (AGS, HeLa, MDA-MB-231, HepG-2, and PANC-1) were evaluated. All of them exhibited anti-proliferative activities (IC = 0.3 - 27 μm), except for 10. Compounds 1, 4, 5, 6, and 8 exhibited potent inhibitory activities with IC < 1 μm against HeLa and AGS cells.
A practical synthesis of (±)-cermizine B was achieved. The nine-step synthesis mainly comprised two uninterrupted Michael additions including a highly diastereoselective 1,4-addition of 2-picoline to methyl 4-methyl-6-oxocyclohex-1-ene-1-carboxylate, Krapcho decarboxylation, a double reductive amination that resulted in ring closure and dearomatization of pyridine in 24% overall yield.
Incremental vertical ground movements due to coal mining can increase landslide susceptibility greatly in a short time and have thus triggered a large number of geological disasters, especially in the Karst Region, where a lot of steep slopes are on fractured rocks. Therefore, the landslide susceptibility maps (LSM) in Karst Region should be updated regularly. This paper presents an efficient methodology to update and refine LSM by using Persistent Scatterer Interferometry (PSI) data directly. First, an original LSM was produced by using a support vector machine (SVM) algorithm, and the distribution of coal mining was considered a crucial factor to generate the LSM. Then, the Permanent Scatterer Interferometric Synthetic Aperture Radar (PSInSAR) technique was implemented to retrieve displacement time-series. Finally, the landslide displacement map, produced by the PSInSAR analysis, was projected to the direction of the steepest slope and resampled to the same cell in the LSM, to update the original LSM. This methodology is illustrated with the case study of Bijie in the Karst Region of Southwest China, wherein the ascending RADARSAT-2 and descending Sentinel-1 datasets are processed for the period of 2017–2019. The results show that the susceptibility degree increased in 56.41 km2 of the study area, and 80 percent of the increased susceptibility degree was caused by coal mining. The comparison between original and refined LSM in two specific areas revealed that the proposed method can produce more-reliable landslide susceptibility maps in areas of intense mining activities in the Karst Region.
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