nehal ibrahim | ASU - Academia.edu (original) (raw)

Papers by nehal ibrahim

Research paper thumbnail of Unveiling the Antimicrobial and Larvicidal Potential of Butyrolactones and Orsellinic Acid Derivatives from the <i>Morus alba‐</i>derived Fungus <i>Aspergillus terreus</i> via Integrated <i>In vitro</i> and <i>In silico</i> Approaches

Chemistry & biodiversity, Feb 9, 2024

Research paper thumbnail of Green preparation and evaluation of anti-psoriatic activity of vesicular elastic nanocarriers of kojic acid from Aspergillus oryzae N12; repurposing of dermo-cosmetic lead

Research Square (Research Square), Dec 11, 2023

Psoriasis is a skin disorder characterized by impaired epidermal differentiation that is regularl... more Psoriasis is a skin disorder characterized by impaired epidermal differentiation that is regularly treated by many systemic drugs with numerous side effects. Our present work aims to investigate an e cient topical bio-friendly vesicular system loaded with kojic acid as an alternative way for the management of psoriasis to avoid systemic toxicity. To achieve our goal, kojic acid was isolated from the endophytic fungus Aspergillus oryzae N12 obtained from the stems of Tecomaria capensis (Bignoniaceae). Kojic acid-loaded spanlastics were prepared by ethanol injection technique; employing span 60 along with birj35 and cremophor rh40 as edge activators with the complete in vitro characterization of kojic acidloaded spanlastics. The optimal formulation displayed spherical morphology under transmission electron microscopy, optimum particle size of 234.2 ± 1.65 nm and high entrapment e ciency (87.4 ± 0.84%). The selected formulation demonstrated signi cant sustained drug release compared with the drug solution. Kojic acid-loaded spanlastics demonstrated superior relief of psoriasis symptoms and the ability to maintain healthy skin with the least changes in mRNA expression of in ammatory cytokines compared to kojic solution in vivo studies. Moreover, in vivo, histopathological studies con rmed the safety of topically applied spanlastics. Concisely, our results suggest that a topically applied vesicular system loaded with kojic acid could lead to expansion in the dermo-cosmetic use of kojic acid as a natural bio-friendly alternative for occasionally used systemic anti-psoriatic drugs. Recent studies suggested the functional role of IL-23 /IL17A in the pathogenesis of psoriasis [68]. IL-22 can along with Interleukins (IL-23/IL17A) induce many of the pathogenic phenotypes from keratinocytes

Research paper thumbnail of Cytotoxic and antimicrobial mycophenolic acid derivatives from an endophytic fungus Penicillium sp. MNP–HS–2 associated with Macrozamia communis

Research paper thumbnail of GC/MS Profiling of Becium grandiflorum Essential Oil and Evaluation of Its Antiviral Activity

Archives of Pharmaceutical Sciences Ain Shams University

Genus Becium of the Lamiaceae family encounters numerous medicinally and economically valued arom... more Genus Becium of the Lamiaceae family encounters numerous medicinally and economically valued aromatic plants. The hydrodistilled essential oil of Becium grandiflorum (Lam.) Pic. Serm. aerial part was analyzed using GC/MS. A total of 32 compounds amounting to 99.68% of the essential oil were identified. Oxygenated diterpenes constituted the largest share (43.45%) in the studied oil followed by sesquiterpenes hydrocarbons (34.24%). Pimara-7,15-dien-3-ol (20.58%), 3-α-hydroxymanool (14.07%), caryophyllene (8.17%), sandaracopimaradiene (7.98%), Selina-3,7 (11)-diene (5.61%), and germacrene D (4.95%) are the chief identified compounds in B. grandiflorum essential oil. The essential oil was assessed for its antiviral potential against herpes simplex virus 1 (HSV-1) at a non-cytotoxic concentration using a cytopathic effect (CPE) inhibition assay on the Vero cell line. B. grandiflorum essential oil exhibited a pronounced in vitro cytotoxicity against Vero cells with 50 % cytotoxic concentration (CC 50) of 7.75 ± 0.84 µg/mL and weak anti-HSV-1 potency with percent inhibition of 21.36 ± 2.13 at a maximum non-toxic concentration of 1 µg/mL.

Research paper thumbnail of New Meroterpenoid Derivatives from the Pomegranate-Derived Endophytic Fungus Talaromyces purpureogenus

Molecules

In this study, we report the isolation of two new meroterpenoids, miniolutelide D (1) and miniolu... more In this study, we report the isolation of two new meroterpenoids, miniolutelide D (1) and miniolutelide E (13-epi-miniolutelide C) (2), along with two meroterpenoidal analogues (3 and 4) and two phenolic compounds (5 and 6) from the endophytic fungus Talaromyces purpureogenus derived from Punica granatum fruits. Their structures were elucidated using extensive MS, 1D, and 2D NMR spectroscopic analyses as well as by comparing with data in the literature. The absolute configurations of 1 and 2 were determined using TDDFT-ECD calculations. Antimicrobial activity was evaluated. Compound 5 displayed significant activity against methicillin-resistant Staphylococcus aureus strain ATCC 700699 and moderate activity against S. aureus strain ATCC 29213.

Research paper thumbnail of Unearthing the fungal endophyte Aspergillus terreus for chemodiversity and medicinal prospects: a comprehensive review

Fungal Biology and Biotechnology

Aspergillus terreus microorganism represents a promising prospective source for drug discovery si... more Aspergillus terreus microorganism represents a promising prospective source for drug discovery since it is rich in diverse kinds of bioactive secondary metabolites. It contributed to many biotechnological applications and its metabolites are used in the synthesis of certain pharmaceuticals and food products, in addition to its useful uses in fermentation processes. There are about 346 compounds identified from marine and terrestrial-derived A. terreus from 1987 until 2022, 172 compounds of them proved a vast array of bioactivity. This review aimed to create an up-to-date comprehensive literature data of A. terreus’s secondary metabolites classes supported by its different bioactivity data to be a scientific record for the next work in drug discovery.

Research paper thumbnail of Phytochemical screening and radioprotective potential of Jasminum grandiflorum methanol extract against gamma irradiation-induced oxidative damage and diverse inflammatory mediators in lungs of male Swiss Albino Rats

Natural Product Research

Rising awareness about the ecological burden of agricultural by-products and their potential indu... more Rising awareness about the ecological burden of agricultural by-products and their potential industrial and medicinal applications spurred the research of waste valorization. Egypt is a chief producer of jasmine oils. However, jasmine dense foliage is an agricultural waste that merits exploitation. Herein, Jasminum grandiflorum leaves were profiled using UPLC-MS, revealing a promising phytochemical composition rich in secoiridoids. Good safety profile was confirmed in vitro on cancerous and normal cell lines and in vivo (LD50>4000 mg/kg). The radioprotective effect of 3500 mg/kg jasmine leaves extract against irradiation-induced lung injury was demonstrated. Biochemical analysis indicated that jasmine extract decreased malondialdehyde level and enhanced the endogenous antioxidants GSH-Px, SOD and CAT levels. Jasmine alleviated the inflammatory response by downregulating the expression of COX-2 and iNOS and reducing the inflammatory mediators, TNF-α, IL-6, NO, and PGE2.Jasmine leaves offer interesting application prospects that add economic and industrial value to agricultural waste.

Research paper thumbnail of A new approach to improve solubility, targeting and efficacy of antimalarials

HAL (Le Centre pour la Communication Scientifique Directe), May 5, 2013

Research paper thumbnail of Strong enhancement of antimalarial activity of indolone-N-oxides by biodegradable albumin bound nanoparticles

HAL (Le Centre pour la Communication Scientifique Directe), Mar 1, 2012

Research paper thumbnail of Utilisation de nanoparticules pour la préparation de compositions antipaludéennes solubles dans l'eau et injectables

HAL (Le Centre pour la Communication Scientifique Directe), May 22, 2013

Research paper thumbnail of Neuroprotective Effect of Artichoke-Based Nanoformulation in Sporadic Alzheimer’s Disease Mouse Model: Focus on Antioxidant, Anti-Inflammatory, and Amyloidogenic Pathways

Pharmaceuticals

The vast socio-economic impact of Alzheimer’s disease (AD) has prompted the search for new neurop... more The vast socio-economic impact of Alzheimer’s disease (AD) has prompted the search for new neuroprotective agents with good tolerability and safety profile. With its outstanding role as antioxidant and anti-inflammatory, alongside its anti-acetylcholinesterase activity, the artichoke can be implemented in a multi-targeted approach in AD therapy. Moreover, artichoke agricultural wastes can represent according to the current United Nations Sustainable Development goals an opportunity to produce medicinally valuable phenolic-rich extracts. In this context, the UPLC-ESI-MS/MS phytochemical characterization of artichoke bracts extract revealed the presence of mono- and di-caffeoylquinic acids and apigenin, luteolin, and kaempferol O-glycosides with remarkable total phenolics and flavonoids contents. A broad antioxidant spectrum was established in vitro. Artichoke-loaded, chitosan-coated, solid lipid nanoparticles (SLNs) were prepared and characterized for their size, zeta potential, morp...

Research paper thumbnail of Antimalarial Activity of 2 -Aryl- 3H-indol-3-one Formulated in Albumin-based Nanosuspensions

International audienceBioreducible indolone-N-oxides have demonstrated their potent antimalarial ... more International audienceBioreducible indolone-N-oxides have demonstrated their potent antimalarial activities with, however, a short half-life. The deox-ygenated analogues, 2-aryl-3H-indol-3-ones, a reduced chemical form obtained by synthesis, have similar antiplasmodial prop-erties against the blood stages of Plasmodium falciparumin vitro, with, however, a low aqueous solubility in vivo. Albumin-based nanosuspensions were used to solubilize these new compounds to conduct experiments in vivo using the P. berghei ANKA mu-rine model to determine the antimalarial activity of the most active derivative of this deoxygenated series, the 5-methoxy-2-(4-methoxyphenyl)-3H-indol-3-one (IND-1). Results were compared with its oxygenated analogue tested in the same conditions. Albumin-based nano-suspensions were prepared by precipitation, high-pressure homogenization and lyophilisation to yield nanoparticles of controlled diameter (350 nm) and polydispersity index (0.223) suitable for intravenous ...

Research paper thumbnail of Séries bioréductibles antipaludiques issues des indolone-N-oxydes

HAL (Le Centre pour la Communication Scientifique Directe), Jun 1, 2015

International audienc

Research paper thumbnail of Powerful Antioxidant and Pro-Oxidant Properties of Cassia roxburghii DC. Leaves Cultivated in Egypt in Relation to Their Anti-Infectious Activities

Journal of Herbs, Spices & Medicinal Plants, 2015

OATAO is an open access repository that collects the work of some Toulouse researchers and makes ... more OATAO is an open access repository that collects the work of some Toulouse researchers and makes it freely available over the web where possible.

Research paper thumbnail of Macrocyclic Spermidine Alkaloids from Androya decaryi L. Perrier

Molecules, 2013

Three new spermidine alkaloids and two known compounds were isolated from the leaves of Androya d... more Three new spermidine alkaloids and two known compounds were isolated from the leaves of Androya decaryi. Their structures were elucidated on the basis of their spectroscopic data (NMR and mass spectrometry), by X-Ray diffraction and by comparison with literature values. Evaluation of the in vitro antiplamosdial properties of the isolated compounds revealed they did not possess any significant activity.

Research paper thumbnail of Albumin-bound nanoparticles of practically water-insoluble antimalarial lead greatly enhance its efficacy

International Journal of Pharmaceutics, 2014

We recently showed that the indolone-N-oxides can be promising candidates for the treatment of ch... more We recently showed that the indolone-N-oxides can be promising candidates for the treatment of chloroquine-resistant malaria. However, the in vivo assays have been hampered by the very poor aqueous solubility of these compounds resulting in poor and variable activity. Here, we describe the preparation, characterization and in vivo evaluation of biodegradable albumin-bound indolone-N-oxide nanoparticles. Nanoparticles were prepared by precipitation followed by high-pressure homogenization and characterized by photon correlation spectroscopy, transmission electron microscopy, differential scanning calorimetry and X-ray powder diffraction. The process was optimized to yield nanoparticles of controllable diameter with narrow size distribution suitable for intravenous administration, which guarantees direct drug contact with parasitized erythrocytes. Stable nanoparticles showed greatly enhanced dissolution rate (complete drug release within 30 min compared to 1.5% of pure drug) preserving the rapid antimalarial activity. The formulation achieved complete cure of Plasmodium berghei-infected mice at 25 mg/kg with parasitemia inhibition (99.1%) comparable to that of artesunate and chloroquine and was remarkably more effective in prolonging survival time and inhibiting recrudescence. In 'humanized' mice infected with Plasmodium falciparum, the same dose proved to be highly effective: with parasitemia reduced by 97.5% and the mean survival time prolonged. This formulation can help advance the preclinical trials of indolone-N-oxides. Albumin-bound nanoparticles represent a new strategic approach to use this most abundant plasma protein to target malaria-infected erythrocytes.

Research paper thumbnail of A new cytotoxic ceramide from Heteroxenia ghardaqensis and protective effect of chloroform extract against cadmium toxicity in rats

Arabian Journal of Chemistry, 2016

A new ceramide 2S,3R-4E,8E-2-(hexadecanoylamino)-docosa-4,8-diene-1,3-diol (1), along with two kn... more A new ceramide 2S,3R-4E,8E-2-(hexadecanoylamino)-docosa-4,8-diene-1,3-diol (1), along with two known ceramides, namely, 2S,3R-4E,8E-2-(octadecanoylamino)-octadeca-4,8-diene-1,3-diol (2) and 2S,3R-4E-2-(octadecanoylamino)-octadec-4-ene-1-ol (3) were isolated from the chloroform extract of the Egyptian Red Sea soft coral Heteroxenia ghardaqensis. Additionally, cholesterol, cholesterol-3b-acetate, 7b-hydroxy cholesterol, cosanyl octadecanoate, and hexadecanyl octadecanoate were also isolated. The isolated compounds were identified by spectroscopic methods involving 1D, 2D-NMR and ESI-MS. The ceramides (1) and (2) showed moderate cytotoxic activity as growth inhibitors of human hept-G2 cancer cell lines. The protective action of the chloroform extract on cadmium-induced adrenal toxicity was observed by the decrease of the hydropic degeneration in the cortex and normal medulla.

Research paper thumbnail of Interactions between Antimalarial Indolone-N-oxide Derivatives and Human Serum Albumin

Biomacromolecules, 2010

The binding affinity of human serum albumin (HSA) to three antimalarial indolone-N-oxide derivati... more The binding affinity of human serum albumin (HSA) to three antimalarial indolone-N-oxide derivatives, INODs, was investigated under simulated physiological conditions using fluorescence spectroscopy in combination with UV-vis absorption and circular dichroism (CD) spectroscopy. Analysis of fluorescence quenching data of HSA by these compounds at different temperatures using Stern-Volmer and Lineweaver-Burk methods revealed the formation of a ground state indolone-HSA complex with binding affinities of the order 10 4 M-1. The thermodynamic parameters ∆G, ∆H, and ∆S, calculated at different temperatures, indicated that the binding reaction was endothermic and hydrophobic interactions play a major role in this association. The conformational changes of HSA were investigated qualitatively using synchronous fluorescence and quantitatively using CD. Site marker competitive experiments showed that the binding process took place primarily at site I (subdomain IIA) of HSA. The number of binding sites and the apparent binding constants were also studied in the presence of different ions.

Research paper thumbnail of Chemical Composition, Antiaging Activities and Molecular Docking Studies of Essential Oils from Acca sellowiana (Feijoa)

Chemistry & Biodiversity

Research paper thumbnail of Rosmarinus officinalis L. hexane extract: phytochemical analysis, nanoencapsulation, and in silico, in vitro, and in vivo anti-photoaging potential evaluation

Scientific Reports

A shift towards natural anti-aging ingredients has spurred the research to valorize traditionally... more A shift towards natural anti-aging ingredients has spurred the research to valorize traditionally used plants. In this context, Rosmarinus officinalis L. was evaluated for its photoprotective, antioxidant, anti-inflammatory, and anti-wrinkling properties. GC/MS and LC-ESI-HRMS based phytochemical profiling of rosemary leaves hexane extract resulted in the identification of 47 and 31 compounds, respectively and revealed rich content in triterpenoids, monoterpenoids and phenolic diterpenes. In vitro assays confirmed the antioxidant, anti-aging, and wound healing potential of rosemary extract along with a good safety profile, encouraging further development. A systematic molecular modelling study was conducted to elucidate the mechanistic background of rosemary anti-aging properties through the inhibitory effects of its major constituents against key anti-aging targets viz. elastase, collagenase, and hyaluronidase. Development of rosemary extract lipid nanocapsules-based mucoadhesive g...

Research paper thumbnail of Unveiling the Antimicrobial and Larvicidal Potential of Butyrolactones and Orsellinic Acid Derivatives from the <i>Morus alba‐</i>derived Fungus <i>Aspergillus terreus</i> via Integrated <i>In vitro</i> and <i>In silico</i> Approaches

Chemistry & biodiversity, Feb 9, 2024

Research paper thumbnail of Green preparation and evaluation of anti-psoriatic activity of vesicular elastic nanocarriers of kojic acid from Aspergillus oryzae N12; repurposing of dermo-cosmetic lead

Research Square (Research Square), Dec 11, 2023

Psoriasis is a skin disorder characterized by impaired epidermal differentiation that is regularl... more Psoriasis is a skin disorder characterized by impaired epidermal differentiation that is regularly treated by many systemic drugs with numerous side effects. Our present work aims to investigate an e cient topical bio-friendly vesicular system loaded with kojic acid as an alternative way for the management of psoriasis to avoid systemic toxicity. To achieve our goal, kojic acid was isolated from the endophytic fungus Aspergillus oryzae N12 obtained from the stems of Tecomaria capensis (Bignoniaceae). Kojic acid-loaded spanlastics were prepared by ethanol injection technique; employing span 60 along with birj35 and cremophor rh40 as edge activators with the complete in vitro characterization of kojic acidloaded spanlastics. The optimal formulation displayed spherical morphology under transmission electron microscopy, optimum particle size of 234.2 ± 1.65 nm and high entrapment e ciency (87.4 ± 0.84%). The selected formulation demonstrated signi cant sustained drug release compared with the drug solution. Kojic acid-loaded spanlastics demonstrated superior relief of psoriasis symptoms and the ability to maintain healthy skin with the least changes in mRNA expression of in ammatory cytokines compared to kojic solution in vivo studies. Moreover, in vivo, histopathological studies con rmed the safety of topically applied spanlastics. Concisely, our results suggest that a topically applied vesicular system loaded with kojic acid could lead to expansion in the dermo-cosmetic use of kojic acid as a natural bio-friendly alternative for occasionally used systemic anti-psoriatic drugs. Recent studies suggested the functional role of IL-23 /IL17A in the pathogenesis of psoriasis [68]. IL-22 can along with Interleukins (IL-23/IL17A) induce many of the pathogenic phenotypes from keratinocytes

Research paper thumbnail of Cytotoxic and antimicrobial mycophenolic acid derivatives from an endophytic fungus Penicillium sp. MNP–HS–2 associated with Macrozamia communis

Research paper thumbnail of GC/MS Profiling of Becium grandiflorum Essential Oil and Evaluation of Its Antiviral Activity

Archives of Pharmaceutical Sciences Ain Shams University

Genus Becium of the Lamiaceae family encounters numerous medicinally and economically valued arom... more Genus Becium of the Lamiaceae family encounters numerous medicinally and economically valued aromatic plants. The hydrodistilled essential oil of Becium grandiflorum (Lam.) Pic. Serm. aerial part was analyzed using GC/MS. A total of 32 compounds amounting to 99.68% of the essential oil were identified. Oxygenated diterpenes constituted the largest share (43.45%) in the studied oil followed by sesquiterpenes hydrocarbons (34.24%). Pimara-7,15-dien-3-ol (20.58%), 3-α-hydroxymanool (14.07%), caryophyllene (8.17%), sandaracopimaradiene (7.98%), Selina-3,7 (11)-diene (5.61%), and germacrene D (4.95%) are the chief identified compounds in B. grandiflorum essential oil. The essential oil was assessed for its antiviral potential against herpes simplex virus 1 (HSV-1) at a non-cytotoxic concentration using a cytopathic effect (CPE) inhibition assay on the Vero cell line. B. grandiflorum essential oil exhibited a pronounced in vitro cytotoxicity against Vero cells with 50 % cytotoxic concentration (CC 50) of 7.75 ± 0.84 µg/mL and weak anti-HSV-1 potency with percent inhibition of 21.36 ± 2.13 at a maximum non-toxic concentration of 1 µg/mL.

Research paper thumbnail of New Meroterpenoid Derivatives from the Pomegranate-Derived Endophytic Fungus Talaromyces purpureogenus

Molecules

In this study, we report the isolation of two new meroterpenoids, miniolutelide D (1) and miniolu... more In this study, we report the isolation of two new meroterpenoids, miniolutelide D (1) and miniolutelide E (13-epi-miniolutelide C) (2), along with two meroterpenoidal analogues (3 and 4) and two phenolic compounds (5 and 6) from the endophytic fungus Talaromyces purpureogenus derived from Punica granatum fruits. Their structures were elucidated using extensive MS, 1D, and 2D NMR spectroscopic analyses as well as by comparing with data in the literature. The absolute configurations of 1 and 2 were determined using TDDFT-ECD calculations. Antimicrobial activity was evaluated. Compound 5 displayed significant activity against methicillin-resistant Staphylococcus aureus strain ATCC 700699 and moderate activity against S. aureus strain ATCC 29213.

Research paper thumbnail of Unearthing the fungal endophyte Aspergillus terreus for chemodiversity and medicinal prospects: a comprehensive review

Fungal Biology and Biotechnology

Aspergillus terreus microorganism represents a promising prospective source for drug discovery si... more Aspergillus terreus microorganism represents a promising prospective source for drug discovery since it is rich in diverse kinds of bioactive secondary metabolites. It contributed to many biotechnological applications and its metabolites are used in the synthesis of certain pharmaceuticals and food products, in addition to its useful uses in fermentation processes. There are about 346 compounds identified from marine and terrestrial-derived A. terreus from 1987 until 2022, 172 compounds of them proved a vast array of bioactivity. This review aimed to create an up-to-date comprehensive literature data of A. terreus’s secondary metabolites classes supported by its different bioactivity data to be a scientific record for the next work in drug discovery.

Research paper thumbnail of Phytochemical screening and radioprotective potential of Jasminum grandiflorum methanol extract against gamma irradiation-induced oxidative damage and diverse inflammatory mediators in lungs of male Swiss Albino Rats

Natural Product Research

Rising awareness about the ecological burden of agricultural by-products and their potential indu... more Rising awareness about the ecological burden of agricultural by-products and their potential industrial and medicinal applications spurred the research of waste valorization. Egypt is a chief producer of jasmine oils. However, jasmine dense foliage is an agricultural waste that merits exploitation. Herein, Jasminum grandiflorum leaves were profiled using UPLC-MS, revealing a promising phytochemical composition rich in secoiridoids. Good safety profile was confirmed in vitro on cancerous and normal cell lines and in vivo (LD50>4000 mg/kg). The radioprotective effect of 3500 mg/kg jasmine leaves extract against irradiation-induced lung injury was demonstrated. Biochemical analysis indicated that jasmine extract decreased malondialdehyde level and enhanced the endogenous antioxidants GSH-Px, SOD and CAT levels. Jasmine alleviated the inflammatory response by downregulating the expression of COX-2 and iNOS and reducing the inflammatory mediators, TNF-α, IL-6, NO, and PGE2.Jasmine leaves offer interesting application prospects that add economic and industrial value to agricultural waste.

Research paper thumbnail of A new approach to improve solubility, targeting and efficacy of antimalarials

HAL (Le Centre pour la Communication Scientifique Directe), May 5, 2013

Research paper thumbnail of Strong enhancement of antimalarial activity of indolone-N-oxides by biodegradable albumin bound nanoparticles

HAL (Le Centre pour la Communication Scientifique Directe), Mar 1, 2012

Research paper thumbnail of Utilisation de nanoparticules pour la préparation de compositions antipaludéennes solubles dans l'eau et injectables

HAL (Le Centre pour la Communication Scientifique Directe), May 22, 2013

Research paper thumbnail of Neuroprotective Effect of Artichoke-Based Nanoformulation in Sporadic Alzheimer’s Disease Mouse Model: Focus on Antioxidant, Anti-Inflammatory, and Amyloidogenic Pathways

Pharmaceuticals

The vast socio-economic impact of Alzheimer’s disease (AD) has prompted the search for new neurop... more The vast socio-economic impact of Alzheimer’s disease (AD) has prompted the search for new neuroprotective agents with good tolerability and safety profile. With its outstanding role as antioxidant and anti-inflammatory, alongside its anti-acetylcholinesterase activity, the artichoke can be implemented in a multi-targeted approach in AD therapy. Moreover, artichoke agricultural wastes can represent according to the current United Nations Sustainable Development goals an opportunity to produce medicinally valuable phenolic-rich extracts. In this context, the UPLC-ESI-MS/MS phytochemical characterization of artichoke bracts extract revealed the presence of mono- and di-caffeoylquinic acids and apigenin, luteolin, and kaempferol O-glycosides with remarkable total phenolics and flavonoids contents. A broad antioxidant spectrum was established in vitro. Artichoke-loaded, chitosan-coated, solid lipid nanoparticles (SLNs) were prepared and characterized for their size, zeta potential, morp...

Research paper thumbnail of Antimalarial Activity of 2 -Aryl- 3H-indol-3-one Formulated in Albumin-based Nanosuspensions

International audienceBioreducible indolone-N-oxides have demonstrated their potent antimalarial ... more International audienceBioreducible indolone-N-oxides have demonstrated their potent antimalarial activities with, however, a short half-life. The deox-ygenated analogues, 2-aryl-3H-indol-3-ones, a reduced chemical form obtained by synthesis, have similar antiplasmodial prop-erties against the blood stages of Plasmodium falciparumin vitro, with, however, a low aqueous solubility in vivo. Albumin-based nanosuspensions were used to solubilize these new compounds to conduct experiments in vivo using the P. berghei ANKA mu-rine model to determine the antimalarial activity of the most active derivative of this deoxygenated series, the 5-methoxy-2-(4-methoxyphenyl)-3H-indol-3-one (IND-1). Results were compared with its oxygenated analogue tested in the same conditions. Albumin-based nano-suspensions were prepared by precipitation, high-pressure homogenization and lyophilisation to yield nanoparticles of controlled diameter (350 nm) and polydispersity index (0.223) suitable for intravenous ...

Research paper thumbnail of Séries bioréductibles antipaludiques issues des indolone-N-oxydes

HAL (Le Centre pour la Communication Scientifique Directe), Jun 1, 2015

International audienc

Research paper thumbnail of Powerful Antioxidant and Pro-Oxidant Properties of Cassia roxburghii DC. Leaves Cultivated in Egypt in Relation to Their Anti-Infectious Activities

Journal of Herbs, Spices & Medicinal Plants, 2015

OATAO is an open access repository that collects the work of some Toulouse researchers and makes ... more OATAO is an open access repository that collects the work of some Toulouse researchers and makes it freely available over the web where possible.

Research paper thumbnail of Macrocyclic Spermidine Alkaloids from Androya decaryi L. Perrier

Molecules, 2013

Three new spermidine alkaloids and two known compounds were isolated from the leaves of Androya d... more Three new spermidine alkaloids and two known compounds were isolated from the leaves of Androya decaryi. Their structures were elucidated on the basis of their spectroscopic data (NMR and mass spectrometry), by X-Ray diffraction and by comparison with literature values. Evaluation of the in vitro antiplamosdial properties of the isolated compounds revealed they did not possess any significant activity.

Research paper thumbnail of Albumin-bound nanoparticles of practically water-insoluble antimalarial lead greatly enhance its efficacy

International Journal of Pharmaceutics, 2014

We recently showed that the indolone-N-oxides can be promising candidates for the treatment of ch... more We recently showed that the indolone-N-oxides can be promising candidates for the treatment of chloroquine-resistant malaria. However, the in vivo assays have been hampered by the very poor aqueous solubility of these compounds resulting in poor and variable activity. Here, we describe the preparation, characterization and in vivo evaluation of biodegradable albumin-bound indolone-N-oxide nanoparticles. Nanoparticles were prepared by precipitation followed by high-pressure homogenization and characterized by photon correlation spectroscopy, transmission electron microscopy, differential scanning calorimetry and X-ray powder diffraction. The process was optimized to yield nanoparticles of controllable diameter with narrow size distribution suitable for intravenous administration, which guarantees direct drug contact with parasitized erythrocytes. Stable nanoparticles showed greatly enhanced dissolution rate (complete drug release within 30 min compared to 1.5% of pure drug) preserving the rapid antimalarial activity. The formulation achieved complete cure of Plasmodium berghei-infected mice at 25 mg/kg with parasitemia inhibition (99.1%) comparable to that of artesunate and chloroquine and was remarkably more effective in prolonging survival time and inhibiting recrudescence. In 'humanized' mice infected with Plasmodium falciparum, the same dose proved to be highly effective: with parasitemia reduced by 97.5% and the mean survival time prolonged. This formulation can help advance the preclinical trials of indolone-N-oxides. Albumin-bound nanoparticles represent a new strategic approach to use this most abundant plasma protein to target malaria-infected erythrocytes.

Research paper thumbnail of A new cytotoxic ceramide from Heteroxenia ghardaqensis and protective effect of chloroform extract against cadmium toxicity in rats

Arabian Journal of Chemistry, 2016

A new ceramide 2S,3R-4E,8E-2-(hexadecanoylamino)-docosa-4,8-diene-1,3-diol (1), along with two kn... more A new ceramide 2S,3R-4E,8E-2-(hexadecanoylamino)-docosa-4,8-diene-1,3-diol (1), along with two known ceramides, namely, 2S,3R-4E,8E-2-(octadecanoylamino)-octadeca-4,8-diene-1,3-diol (2) and 2S,3R-4E-2-(octadecanoylamino)-octadec-4-ene-1-ol (3) were isolated from the chloroform extract of the Egyptian Red Sea soft coral Heteroxenia ghardaqensis. Additionally, cholesterol, cholesterol-3b-acetate, 7b-hydroxy cholesterol, cosanyl octadecanoate, and hexadecanyl octadecanoate were also isolated. The isolated compounds were identified by spectroscopic methods involving 1D, 2D-NMR and ESI-MS. The ceramides (1) and (2) showed moderate cytotoxic activity as growth inhibitors of human hept-G2 cancer cell lines. The protective action of the chloroform extract on cadmium-induced adrenal toxicity was observed by the decrease of the hydropic degeneration in the cortex and normal medulla.

Research paper thumbnail of Interactions between Antimalarial Indolone-N-oxide Derivatives and Human Serum Albumin

Biomacromolecules, 2010

The binding affinity of human serum albumin (HSA) to three antimalarial indolone-N-oxide derivati... more The binding affinity of human serum albumin (HSA) to three antimalarial indolone-N-oxide derivatives, INODs, was investigated under simulated physiological conditions using fluorescence spectroscopy in combination with UV-vis absorption and circular dichroism (CD) spectroscopy. Analysis of fluorescence quenching data of HSA by these compounds at different temperatures using Stern-Volmer and Lineweaver-Burk methods revealed the formation of a ground state indolone-HSA complex with binding affinities of the order 10 4 M-1. The thermodynamic parameters ∆G, ∆H, and ∆S, calculated at different temperatures, indicated that the binding reaction was endothermic and hydrophobic interactions play a major role in this association. The conformational changes of HSA were investigated qualitatively using synchronous fluorescence and quantitatively using CD. Site marker competitive experiments showed that the binding process took place primarily at site I (subdomain IIA) of HSA. The number of binding sites and the apparent binding constants were also studied in the presence of different ions.

Research paper thumbnail of Chemical Composition, Antiaging Activities and Molecular Docking Studies of Essential Oils from Acca sellowiana (Feijoa)

Chemistry & Biodiversity

Research paper thumbnail of Rosmarinus officinalis L. hexane extract: phytochemical analysis, nanoencapsulation, and in silico, in vitro, and in vivo anti-photoaging potential evaluation

Scientific Reports

A shift towards natural anti-aging ingredients has spurred the research to valorize traditionally... more A shift towards natural anti-aging ingredients has spurred the research to valorize traditionally used plants. In this context, Rosmarinus officinalis L. was evaluated for its photoprotective, antioxidant, anti-inflammatory, and anti-wrinkling properties. GC/MS and LC-ESI-HRMS based phytochemical profiling of rosemary leaves hexane extract resulted in the identification of 47 and 31 compounds, respectively and revealed rich content in triterpenoids, monoterpenoids and phenolic diterpenes. In vitro assays confirmed the antioxidant, anti-aging, and wound healing potential of rosemary extract along with a good safety profile, encouraging further development. A systematic molecular modelling study was conducted to elucidate the mechanistic background of rosemary anti-aging properties through the inhibitory effects of its major constituents against key anti-aging targets viz. elastase, collagenase, and hyaluronidase. Development of rosemary extract lipid nanocapsules-based mucoadhesive g...