Search Results (5)

New Caledonia is a biodiversity hotspot with flora closely related to that of Australia and has received considerable attention. Endiandra (Cryptocaryeae; Lauraceae) is distributed from tropical Asia to Oceania, including New Caledonia, with northeastern Australia and New Guinea as diversity centers, but the genus in New Caledonia remains understudied. Here, four species of Endiandra native to New Caledonia were sequenced, and their complete plastome sequences were analyzed. A plastome-based phylogenomic tree of Cryptocaryeae was reconstructed, and divergence times were estimated. The phylogenomic tree supports the monophyly of Endiandra. Interestingly, the species of Endiandra from New Caledonia were grouped into two separate subclades, with one subclade including three species and the other subclade containing only one species. The stem and crown ages of the first subclade were 33.18 Ma and 14.5 Ma, respectively, and the second subclade diverged by approximately 10.36 Ma. The structural characteristics of the newly sequenced plastomes were compared with those of Beilschmiedia species from different continents. The results indicate that the plastome sequences of the four species of Endiandra are longer than those of Beilschmiedia. Additionally, Endiandra has more simple sequence repeats (SSRs) than Beilschmiedia, though the difference is slight. The Guanine-Cytosine (GC) content of Endiandra was lower than that of Beilschmiedia. Five highly variable regions were identified, including matK-rps16, ycf1, petA-psbJ, petN-psbM, and ndhF. The Endiandra species in New Caledonia originated through long-distance dispersal followed by local divergence, rather than vicariance. Additionally, we identified at least two instances of floristic exchange between New Caledonia and Australia. Our study provides further evidence for understanding the biogeographic history between these two regions. Full article

Idiopathic pulmonary fibrosis (IPF) is the most common and lethal form of the interstitial pneumonias. The cause of the disease is unknown, and new therapies that stop or reverse disease progression are desperately needed. Recent advances in next-generation sequencing have led to an abundance of freely available, clinically relevant, organ-and-disease-specific, single-cell transcriptomic data, including studies from patients with IPF. We mined data from published IPF data sets and identified gene signatures delineating pro-fibrotic or antifibrotic macrophages and then used the Enrichr platform to identify compounds with the potential to drive the macrophages toward the antifibrotic transcriptotype. We then began testing these compounds in a novel in vitro phenotypic drug screening assay utilising human lung macrophages recovered from whole-lung lavage of patients with silicosis. As predicted by the Enrichr tool, glitazones potently modulated macrophage gene expression towards the antifibrotic phenotype. Next, we assayed a subset of the NatureBank pure compound library and identified the cyclobutane lignan, endiandrin A, which was isolated from the roots of the endemic Australian rainforest plant, Endiandra anthropophagorum, with a similar antifibrotic potential to the glitazones. These methods open new avenues of exploration to find treatments for lung fibrosis. Full article

Plants of the Lauraceae family are widely used in traditional medicine and are sources of various classes of secondary metabolites. Two genera of this family, Beilschmiedia and Endiandra, have been the subject of numerous investigations over the past decades because of their application in traditional medicine. They are the only source of bioactive endiandric acid derivatives. Noteworthy is that their biosynthesis contains two consecutive non-enzymatic electrocyclic reactions. Several interesting biological activities for this specific class of secondary metabolites and other constituents of the two genera have been reported, including antimicrobial, enzymes inhibitory and cytotoxic properties. This review compiles information on the structures of the compounds described between January 1960 and March 2015, their biological activities and information on endiandric acid biosynthesis, with 104 references being cited. Full article

A total of 115 different plant extracts from our collection, representing 96 plant species, have been evaluated for in vitro antileishmanial activity against L. amazonensis promastigotes. In addition, the extracts were screened for cytotoxic activity against BALB/c mouse macrophages in order to assess a selectivity index. Crude extracts that showed a selectivity index (CC₅₀ for macrophage / IC₅₀ for promastigotes) ³ 5 or with IC₅₀ < 12.5 μg/mL against promastigotes, a total of 28 extracts, were further screened for anti-amastigote activity. A total of 25 extracts showed promising activity against L. amazonensis promastigotes with low cytotoxic activity. Ten of these extracts showed selectivity indices, (CC₅₀ for macrophages / IC₅₀ for amastigotes) greater than 10 and are considered “hits”, worthy candidates for further phytochemical exploration: Conostegia xalapensis methanol bark extract, Endiandra palmerstonii bark extract, Eugenia monteverdensis acetone bark extract, Eugenia sp. “fine leaf” acetone bark extract, Exothea paniculata chloroform bark extract, Mallotus paniculatus ethanol bark extract, Matelea pseudobarbata ethanol extract, Quercus insignis ethanol bark extract, Sassafras albidum dichloromethane bark extract, and Stemmadenia donnell-smithii acetone bark extract. Full article

A phytochemical investigation of the methanolic extract of the bark of Endiandra kingiana led to the isolation of seven new tetracyclic endiandric acid analogues, kingianic acids A–G (1–7), together with endiandric acid M (8), tsangibeilin B (9) and endiandric acid (10). Their structures were determined by 1D- and 2D-NMR analysis in combination with HRMS experiments. The structure of compounds 9 and 10 were confirmed by single-crystal X-ray diffraction analysis. These compounds were screened for Bcl-xL and Mcl-1 binding affinities and cytotoxic activity on various cancer cell lines. Compound 5 showed moderate cytotoxic activity against human colorectal adeno-carcinoma (HT-29) and lung adenocarcinoma epithelial (A549) cell lines, with IC₅₀ values in the range 15–17 µM, and compounds 3, 6 and 9 exhibited weak binding affinity for the anti-apoptotic protein Mcl-1. Full article