A5036826480- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Traditional and Medicinal Uses of Annonaceae
- Bioactive Natural Diterpenoids Research
- Plant biochemistry and biosynthesis
- Natural product bioactivities and synthesis
- Mosquito-borne diseases and control
- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- interferon and immune responses
- Biological and pharmacological studies of plants
- Toxin Mechanisms and Immunotoxins
- Bioactive natural compounds
- Natural Antidiabetic Agents Studies
- Biochemical and Molecular Research
- Insect Pest Control Strategies
- Crystallography and molecular interactions
- Microbial Natural Products and Biosynthesis
- Phytochemistry and Biological Activities
- Bioactive Compounds and Antitumor Agents
- Medicinal Plants and Neuroprotection
- Piperaceae Chemical and Biological Studies
- Signaling Pathways in Disease
- Ginseng Biological Effects and Applications
- Sesquiterpenes and Asteraceae Studies
Institut de Chimie des Substances Naturelles
2016-2025
Centre National de la Recherche Scientifique
2014-2025
Université Paris-Saclay
2016-2024
University College Dublin
2015-2019
University of Puerto Rico at Carolina
2018
Natural products represent an inexhaustible source of novel therapeutic agents. Their complex and constrained three-dimensional structures endow these molecules with exceptional biological properties, thereby giving them a major role in drug discovery programs. However, the search for new bioactive metabolites is hampered by chemical complexity matrices which they are found. The purification single constituents from such requires significant amount work that it should be ideally performed...
From a set of 292 Euphorbiaceae extracts, the use molecular networking (MN)-based prioritization approach highlighted three clusters (MN1–3) depicting ions from bark extract Codiaeum peltatum. Based on their putative antiviral potential and structural novelty, MS-guided purification compounds present in MN1 MN2 afforded two new daphnane-type diterpenoid orthoesters (DDO), codiapeltines A (1) B (2), actephilols (3) C (4), four known 1,4-dioxane-fused phenanthrene dimers (5–8). The structures...
Four unprecedented chlorinated monoterpenyl quinolones have been isolated using a molecular networking based prioritisation strategy. The bio-inspired total synthesis of chloroaustralasine A involving chloroperoxydase-mediated hydroxychlorination is described.
Hijacking host cell lipid homeostatic pathways is a hallmark of infection by RNA-positive viruses. A key protein exploited these viruses to facilitate replication the exchanger Oxysterol-binding (OSBP), making it an attractive target for antiviral strategies. However, known OSBP ligands are poorly selective, and those natural origin, referred as ORPphilins, exhibit pronounced cytotoxicity. Here, we describe macarangin B, new racemic flavonoid isolated from Vietnamese bushy tree. This...
In an effort to find potent inhibitors of the protein kinases DYRK1A and CDK1/Cyclin B, a systematic in vitro evaluation 2,500 plant extracts from New Caledonia French Guyana was performed. Some were found strongly inhibit activity these kinases. Four aristolactams one lignan purified ethyl acetate Oxandra asbeckii Goniothalamus dumontetii, eleven aporphine alkaloids isolated alkaloid Siparuna pachyantha, S. decipiens, guianensis poeppigii. Among compounds, velutinam, aristolactam AIIIA...
In continuation of our efforts to find new antimalarial drugs, a systematic in vitro evaluation using chloroquine resistant strain Plasmodium falciparum (FcB1) was undertaken on extracts prepared from various parts Vietnamese plants. The ethyl acetate extract obtained the stem bark Artocarpus styracifolius (Moraceae) exhibited strong antiplasmodial activity (87 % at 10 µg/mL) whereas weak cytotoxicity observed human fibroblast cell line (MRC-5). Phytochemical investigation this led isolation...
A rapid screening by 1H and 1H–13C HSQC NMR spectroscopy of EtOAc extracts Endiandra Beilschmiedia species allowed the selection ferruginea leaves flowers extract for a chemical investigation, leading to isolation 11 new tetracyclic endiandric acid analogues, named ferrugineic acids A–K (1–11). Their structures were determined 1D 2D spectroscopic analysis in combination with HRMS data. These compounds assayed Bcl-xL Mcl-1 binding affinities. Ferrugineic B, C, J (2, 3, 10) exhibited...
In the search of new inhibitors for human coronavirus (HCoV), we screened extracts endemic Annonaceae plants on an assay using a cellular model Huh-7 cells infected with alphacoronavirus HCoV-229E. The EtOAc bark extract rare Southeast Asian plant
A unique collection of 292 extracts from 107 New Caledonian Euphorbiaceae species sensu lato was profiled by LC-MS2 and the metabolite content organized molecular networking. Based on assumption that taxon-specific molecules are more likely to be structurally novel, taxonomic data were mapped spectral networks detect genus-specific clusters. Using this approach, a group compounds genus Austrobuxus highlighted. The subsequent MS-guided purification fruit EtOAc extract carunculatus led...
The overexpression of antiapoptotic members (BCL-2, BCL-xL, MCL-1, etc.) the BCL-2 family contributes to tumor development and resistance chemotherapy or radiotherapy. Synthetic inhibitors targeting these proteins have been developed, some hematological malignancies are now widely treated with a inhibitor (venetoclax). However, acquired venetoclax drugs due an upregulation MCL-1 has observed, rendering attractive new target for treatment. Six (S64315, AZD-5991, AMG-176, AMG-397, ABBV-467...
Induced by the spread of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), COVID-19 pandemic underlined clear need for antivirals against coronaviruses. In an effort to identify new inhibitors SARS-CoV-2, a screening 824 extracts prepared from various parts 400 plant species belonging Rutaceae and Annonaceae families was conducted using cell-based HCoV-229E inhibition assay. Due its significant activity, ethyl acetate extract leaves Clausena harmandiana selected further chemical...
Abstract Drimane sesquiterpenoid dialdehydes are natural compounds with antiproliferative properties. Nevertheless, their mode of action has not yet been discovered. Herein, we demonstrate that various drimanes potent inhibitors MCL‐1 and BCL‐xL, two proteins the BCL‐2 family overexpressed in cancers, including lymphoid malignancies. Subtle changes structure significantly modified activity on target proteins. The most active selective bind BH3 binding groove protein. Complementary studies by...
OSBP ligands from the ORPphilin family are chemically complex natural products with promising anticancer properties. Here, we describe macarangin B, a racemic flavonoid selective for OSBP, which stands out other ORPphilins due to its structural simplicity and distinct biological activity. Using bioinspired strategy, synthesized both (R,R,R) (S,S,S)-macarangin B enantiomers, enabling us study their interaction based on unique optical Experimental computational analyzes revealed that...
ATP wasting is recognized as an efficient strategy to enhance metabolic activity and productivity of specific metabolites in several microorganisms . However, such has been rarely implemented Streptomyces species whereas antibiotic production by members this genus known be triggered condition phosphate limitation that correlated with a low content. In consequence, assess the effects spilling on primary specialized metabolisms , gene encoding small synthetic protein DX, high affinity for...
Quinoline derivatives and especially quinolones are considered as privileged structures in medicinal chemistry often associated with various biological properties. We recently isolated a series of original monoterpenyl from the bark Codiaeum peltatum. As this extract was found to have significant inhibitory activity against Leishmania species, we decided study anti-leishmanial potential type compound. Leishmaniasis is serious health problem affecting more than 12 million people world....
Leishmaniasis is a vector-borne disease caused by the protozoan parasite Leishmania found in tropical and sub-tropical areas, affecting 12 million people around world. Only few treatments are available against this all of them present issues toxicity and/or resistance. In context, development new antileishmanial drugs specifically directed therapeutic target appears to be promising strategy. The GDP-Mannose Pyrophosphorylase (GDP-MP) has been previously shown an attractive Leishmania. study,...
Dengue and Zika viruses are identified as the most medically important arthropod-borne viral pathogens. Over past 20 years, global dengue incidence has dramatically increased with epidemics of severe where case fatality rate can reach up to 20% in untreated patients. The association between virus infection congenital anomalies was first reported 2015. Today no specific antiviral therapies available for infections, accentuating need adapted strategies based on medicinal plant drug discovery....