Anti-Inflammatory ent-Kaurane Diterpenoids from Isodon serra

Ten new ent-kaurane diterpenoids, including two pairs of epimers 1/2 and 4/5 and a 6,7-seco-ent-kauranoid 10, were obtained from the aerial parts of Isodon serra. The structures of the new compounds were confirmed by extensive spectroscopic methods and electronic circular dichroism (ECD) data analysis. An anti-inflammatory assay was applied to evaluate their nitric oxide (NO) inhibitory activities by using LPS-stimulated BV-2 cells. Compounds 1 and 9 exhibited notable NO production inhibition with IC50 values of 15.6 and 7.3 μM, respectively. Moreover, the interactions of some bioactive diterpenoids with inducible nitric oxide synthase (iNOS) were explored by employing molecular docking studies.https://pubs.acs.org/journal/jnprdf2021-09-29hj2021Plant Production and Soil Scienc

Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities

A phytochemical investigation to obtain bioactive substances as lead compounds or agents for cancer led to the obtainment of six new and two known clerodane diterpenoids from the leaves of Casearia kurzii. Their structures were elucidated using NMR techniques and electronic circular dichroism (ECD) calculations. The subsequent biological cytotoxicity evaluation of these isolates toward human lung cancer A549, human cervical cancer HeLa, human chronic myeloid leukemia K562, and human hepatocellular carcinoma HepG2 was carried out. The most active compound 4 with an IC50 value of 9.7 μM against HepG2 cells was selected to examine the cytotoxic mechanism, which induced the apoptosis and arrested the HepG2 cell cycle at S stage. The in vivo zebrafish experiments revealed that compound 4 had the property of inhibiting tumor proliferation and migration.The National Key Research and Development Program of China, the National Natural Science Foundation of China, Hundred Young Academic Leaders Program of Nankai University, the Natural Science Foundation of Tianjin, State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources and the open project of Key Laboratory of Xinjiang Uygur Autonomous Region.http://www.elsevier.com/ locate/bmclhj2021Plant Production and Soil Scienc

Caseahomopene A, a ring-expanded homotriterpenoid from Casearia kurzii showing anti-inflammatory activities in vitro and in vivo

Caseahomopene A (1), a rare natural product with a ring-expanded homotriterpenoid skeleton, was isolated from the leaves of Casearia kurzii. The structure including the absolute configuration was determined by spectroscopic data and X-ray crystallography analysis. Compound 1 showed anti-inflammatory effects in vitro and in vivo using LPS-stimulated cell and zebrafish model. As a potential anti-inflammatory agent, the anti-inflammatory mechanism of 1 was also investigated.The National Key Research and Development Program of China, the National Natural Science Foundation of China, the Natural Science Foundation of Tianjin, China, Hundred Young Academic Leaders Program of Nankai University, and State Key Laboratory of Bioactive Substance and Function of Natural Medicines (Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College).http://www.elsevier.com/ locate/bmcl2021-05-01hj2021Plant Production and Soil Scienc