Publications by authors named "Raphael Grougnet"

This study explores the potential of polymethoxyflavones (PMFs) and polyacetylated flavones (PAFs) as novel analgesic and anti-inflammatory agents. Eight derivatives, isolated from Gardenia oudiepe bud exudate or semi-synthesized from commercial kaempferol, underwent evaluations in various in vivo, in vitro, and in silico models. Acetic acid-, formalin-induced pain, and hot-plate tests were conducted in mice (n = 6).

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causes destructive ear rot diseases in maize and wheat. New antifungals are essential to combat this pathogen, and aerial parts of species (Acanthaceae) are a potential source. We investigated the antifungal activity of extracts from stems and leaves of five species native to Northwest Argentina.

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Background: Endotoxemia is a severe and dangerous clinical syndrome that results in elevated morbidity, especially in intensive care units. Neonates are particularly susceptible to endotoxemia due to their immature immune systems. There are few effective treatments for neonatal endotoxemia.

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This study provides a comprehensive overview of the current knowledge regarding phototoxic terrestrial plants and their phototoxic and photosensitizing metabolites. Within the 435,000 land plant species, only around 250 vascular plants have been documented as phototoxic or implicated in phototoxic occurrences in humans and animals. This work compiles a comprehensive catalog of these phototoxic plant species, organized alphabetically based on their taxonomic family.

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Invited for this month's cover, the researchers from UTCBS and CiTCoM from Université Paris Cité (Paris, France), as well as Materia Nova (Mons, Belgium). The image emphasizes the deep eutectic solvent preparation thanks to hydrogen bond acceptor and donor interactions for drugs formulation and therapeutic applications. The Review itself is available at 10.

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In the spirit of circular economy and sustainable chemistry, the use of environmentally friendly chemical products in pharmacy has become a hot topic. In recent years, organic solvents have been the subject of a great range of restriction policies due to their harmful effects on the environment and toxicity to human health. In parallel, deep eutectic solvents (DESs) have emerged as suitable greener solvents with beneficial environmental impacts and a rich palette of physicochemical advantages related to their low cost and biocompatibility.

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Article Synopsis
  • Melanoma cells are known for their aggressive behavior and resistance to multiple drugs, often due to genetic changes like BRAF mutations, making long-term treatment difficult.
  • Recent research has focused on carotenoids derived from microalgae as a promising addition to melanoma therapy because they are safe and well-tolerated.
  • Studies show that microalgal carotenoids can inhibit the growth and spread of melanoma cells, induce cell death, and enhance the effectiveness of traditional chemotherapy treatments.
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For more than 40 years, marine microorganisms have raised great interest because of their major ecological function and their numerous applications for biotechnology and pharmacology. Particularly, Archaea represent a resource of great potential for the identification of new metabolites because of their adaptation to extreme environmental conditions and their original metabolic pathways, allowing the synthesis of unique biomolecules. Studies on archaeal carotenoids are still relatively scarce and only a few works have focused on their industrial scale production and their biotechnological and pharmacological properties, while the societal demand for these bioactive pigments is growing.

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Marine halophytes are an outstanding reservoir of natural products and several species have anti-infectious traditional uses. However, reports about their potential use against neglected tropical ailments, such as Chagas disease, are scarce. This work evaluated for the first time the in vitro anti- activity of extracts from the aromatic and medicinal species subsp.

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The chemical composition and in vitro biological activities of the essential oil (EO) of Micromeria macrosiphon Coss. and M. arganietorum (J.

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(Lam) Pers. (Crassulaceae) is widely used in folk medicine as leaf juice, aqueous, or hydro-ethanolic extracts. It is also listed as a medicinal plant in several countries such as France and Brazil.

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Article Synopsis
  • The essential oil (EO) of Chiliadenus antiatlanticus, a plant native to southwest Morocco, was analyzed for its chemical composition and biological activities.
  • The EO yielded 1.07% and contained 27 metabolites, with camphor, borneol, and intermedeol being the primary components.
  • It exhibited antibacterial properties against 24 out of 71 strains (mostly Gram-positive) and showed significant cytotoxic effects on liver and melanoma tumor cell lines at a concentration of 100 μg/mL.
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(Burseraceae) is a medicinal plant native to Brazil which is popularly used for treating oral and vaginal infections. There has been no scientific evidence pointing to its efficacy in the treatment of these infections. Thus, this study sought to investigate the cytotoxic, antifungal, and antibiofilm activity of against spp.

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is an important multidrug-resistant human pathogen by dint of its high intrinsic, acquired, and adaptive resistance mechanisms, causing great concern for immune-compromised individuals and public health. Additionally, resilience lies in the production of a myriad of virulence factors, which are known to be tightly regulated by the quorum sensing (QS) system. Anti-virulence therapy has been adopted as an innovative alternative approach to circumvent bacterial antibiotic resistance.

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Bryophyllum pinnatum (Lam.) Oken (Crassulaceae) is widely used as leaf juice or extracts in traditional medicine all over tropical areas, especially in Brazil, to relieve inflammation-associated symptoms. Flavonol glycosides with unusual sugar moiety are among the major metabolites.

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A library of 33 polymethoxylated flavones (PMF) was evaluated for heme-binding affinity by biomimetic MS assay and in vitro antiplasmodial activity on two strains of P. falciparum. Stability of heme adducts was discussed using the dissociation voltage at 50% (DV).

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Background: Limonene (LIM) and its main metabolite perillyl alcohol (POH) are ingredients found in food with promising chemical entities due to their pharmacological profile. In this study, we hypothesized that LIM and POH are two molecules capable of accelerating the regenerative process and alleviating neuropathic pain.

Methods: Animals were treated daily (LIM, POH and saline) for 28 days and during this period evaluated for mechanical hyperalgesia, astrocyte participation by immunofluorescence for GFAP, and ELISA was used to quantify IL-1β and TNF-α in the spinal cord.

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is capable to deploy a collection of virulence factors that are not only essential for host infection and persistence, but also to escape from the host immune system and to become more resistant to drug therapies. Thus, developing anti-virulence agents that may directly counteract with specific virulence factors or disturb higher regulatory pathways controlling the production of virulence armories are urgently needed. In this regard, this study reports that L.

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A series of 10 natural and semisynthetic flavonoids (1 to 10) were obtained from Gardenia oudiepe (Rubiaceae), an endemic plant from New Caledonia. Most of them were polymethoxylated flavones (PMFs) of rare occurrence. After a cell viability screening test, PMFs 2 and 3 showed significant cytotoxic activity against A2058 human melanoma cells (IC = 3.

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Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i.e., dihydroartemisinin, artemether, arteether, and artemisone) were synthesized from dihydroartemisinin.

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Natural products are considered an important source of bioactive compounds especially in biodiversity-rich countries like Brazil. The identification of potential targets is crucial to the development of drugs from natural sources. In this context, methodologies, such as inverse virtual screening (target fishing), are interesting tools as they are a rational and direct method that reduces costs and experimental time.

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This Data Descriptor announces the submission to public repositories of the monoterpene indole alkaloid database (MIADB), a cumulative collection of 172 tandem mass spectrometry (MS/MS) spectra from multiple research projects conducted in eight natural product chemistry laboratories since the 1960s. All data have been annotated and organized to promote reuse by the community. Being a unique collection of these complex natural products, these data can be used to guide the dereplication and targeting of new related monoterpene indole alkaloids within complex mixtures when applying computer-based approaches, such as molecular networking.

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Cutaneous melanoma has a high capacity to metastasize and significant resistance to conventional therapeutic protocols, which makes its treatment difficult. The combination of conventional drugs with cytostatic molecules of low toxicity has been shown to be an interesting alternative for sensitization of tumor cells to chemotherapy. In this study, we evaluated the effect of bixin, an abundant apocarotenoid present in Bixa orellana, on the sensitization of human melanoma cells (A2058) to dacarbazine treatment, an anticancer agent clinically used for the therapy of metastatic melanoma.

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Extracts from aerial parts of , , and were assayed against toxigenic species. They were obtained by sequential extraction of the aerial parts with hexane (fHex), dichloromethane (fDCM), ethyl acetate (fEtOAc) and methanol (fMeOH). The fMeOH from showed the highest antifungal spectrum (MIC = 750-1500 µg mL; MID = 50-200 µg; DI = 1.

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Twenty four extracts from Bignoniaceae plants of northwest Argentina were tested for antifungal activity against species responsible of the grape black rot. Stems and leaves of and were separately extracted with solvents of increasing polarity to obtain the dichloromethane (fCHCl), ethyl acetate (fEtOAc) and methanol extracts (fMeOH). The fCHCl from stem of had the lowest IC (1.

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