Analysis of the toxicological and pharmacokinetic profile of Kaempferol-3-O-β-D-(6”-E-p-coumaryl) glucopyranoside - Tiliroside: in silico, in vitro and ex vivo assay

Sousa, Aleson Pereira de; Fernandes, Diégina Araújo; Ferreira, Maria Denise Leite; Cordeiro, Laísa Vilar; Souza, M. F. V.; Pêssoa, Hilzeth L. F.; Filho, Abrahão Alves de Oliveira; Sá, R. C. S.

doi:10.1590/1519-6984.244127

Cited by 4 publications

(1 citation statement)

References 36 publications

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“…A variação hemolítica mesmo que de forma discreta demostra uma tendência de melhor interação entre o extrato etanólico nas hemácias do tipo O e B; essa ação sugere menor relação citotóxica das moléculas desse composto frente a porção antigênica nestas hemácias. Os monossacarídeos específicos na superfície de membrana eritrocitária: tipo A (N-acetilgalactosamina), tipo B (D-galactose), tipo O que não possuí nenhum antígeno de superfície [22].…”

Section: Resultsunclassified

Avaliação da citotoxicidade em hemácias de humanos do extrato etanólico de Praxelis clematidea (Griseb.)

Pereira,

Medeiros

et al. 2022

Rev. Colomb. Cienc. Quím. Farm.

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Introdução: espécies da família Asteraceae são conhecidas por apresentarem propriedadesaromática, cosmética e terapêutica; tendo diversas pesquisas que evidencioupotencial medicinal dessa família. Dentre as espécies de Asteraceae, está Praxelis clematidea,que é rica em substâncias químicas como flavonoides, terpenóides e esteroides,as quais podem desempenhar uma série de atividades biológicas. Objetivo: verificar opotencial tóxico do extrato etanólico das folhas de P. clematidea frente à células sanguíneashumanas, afim de determinar a toxicidade teórica dessa espécie. Métodos: paraa realização do teste de atividade citotóxica foram preparadas suspensões sanguíneasdos tipos A, B e O, que posteriormente foram misturadas a concentrações distintas doextrato etanólico por 1 (uma) hora. A hemólise foi quantificada por espectrofotometriaem comprimento de onda de 540 nm. Resultados: o extrato etanólico das folhasde P. clematidea em diferentes concentrações apresentou baixa citoxicidade contra oseritrócitos humanos in vitro, enfatizando o produto como uma possível opção viável para a indústria de medicamentos fitoterápicos. No entanto, é importante elucidarque mais estudos in vivo precisam ser realizados para confirmar esse perfil toxicológicodo extrato.

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Section: Resultsunclassified

Avaliação da citotoxicidade em hemácias de humanos do extrato etanólico de Praxelis clematidea (Griseb.)

Pereira,

Medeiros

et al. 2022

Rev. Colomb. Cienc. Quím. Farm.

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Citrus Flavonoids: Biological Activities, Implementation in Skin Health, and Topical Applications: A Review

Sebghatollahi

Ghanadian

Agarwal

et al. 2022

ACS Food Sci. Technol.

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Citrus fruits are one of the most popular sources of dietary flavonoids, such as hesperidin, hesperetin, naringin, naringenin, quercetin, rutin, diosmin, diosmetin, kaempferol, myricetin, nobiletin, tangeretin, and so on. Flavonoids are polyphenols and aromatic bioactive compounds occurring in plants as secondary metabolites. These participate in various biochemical processes in the human body and help in promoting health. Citrus flavonoids are well-known for their antioxidant and anti-inflammatory properties. They promote wound healing and antimelanoma in addition to free radical scavenging, apoptosis, modulation of lipid metabolism, improvement of insulin sensitivity, and endothelial dysfunction. Citrus flavonoids serve as efficient therapeutics for treating various skin-related issues, such as skin aging/photoaging, skin pigmentation, and maintenance of overall healthy skin. This review is an attempt to compile relevant information from recently published articles addressing the roles of Citrus flavonoids in health-promoting activities, particularly skin health. In addition, it also provides a discussion on the recent progress in developing efficient topical delivery techniques to solve the challenge of flavonoids’ poor water solubility and limited permeability into the skin. The review aims to provide a better understanding of the current trends in research and development in Citrus flavonoid biochemistry and their usage in the production of plant-based medicinal and pharma-/nutraceuticals for topical applications.

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Family Malvaceae: a potential source of secondary metabolites with chemopreventive and anticancer activities supported with in silico pharmacokinetic and pharmacodynamic profiles

Sameh,

Elissawy,

Al-Sayed

et al. 2024

Front. Pharmacol.

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IntroductionCancer is the second most widespread cause of mortality following cardiovascular disorders, and it imposes a heavy global burden. Nowadays, herbal nutraceutical products with a plethora of bioactive metabolites represent a foundation stone for the development of promising chemopreventive and anticancer agents. Certain members of the family Malvaceae have traditionally been employed to relieve tumors. The literature concerning the chemopreventive and anticancer effects of the plant species along with the isolated cytotoxic phytometabolites was reviewed. Based on the findings, comprehensive computational modelling studies were performed to explore the pharmacokinetic and pharmacodynamic profiles of the reported cytotoxic metabolites to present basis for future plant-based anticancer drug discovery.MethodsAll the available information about the anticancer research in family Malvaceae and its cytotoxic phytometabolites were retrieved from official sources. Extensive search was carried out using the keywords Malvaceae, cancer, cytotoxicity, mechanism and signalling pathway. Pharmacokinetic study was performed on the cytotoxic metabolites using SWISS ADME model. Acute oral toxicity expressed as median lethal dose (LD50) was predicted using Pro Tox 3.0 web tool. The compounds were docked using AutoDock Vina platform against epidermal growth factor receptor (EGFR kinase enzyme) obtained from the Protein Data Bank. Molecular dynamic simulations and MMGBSA calculations were performed using GROMACS 2024.2 and gmx_MMPBSA tool v1.5.2.ResultsOne hundred forty-five articles were eligible in the study. Several tested compounds showed safe pharmacokinetic properties. Also, the molecular docking study showed that the bioactive metabolites possessed agreeable binding affinities to EGFR kinase enzyme. Tiliroside (25), boehmenan (30), boehmenan H (31), and isoquercetin (22) elicited the highest binding affinity toward the enzyme with a score of −10.4, −10.4, −10.2 and −10.1 Kcal/mol compared to the reference drug erlotinib having a binding score equal to −9 Kcal/mol. Additionally, compounds 25 and 31 elicited binding free energies equal to −42.17 and −42.68 Kcal/mol, respectively, comparable to erlotinib.DiscussionOverall, the current study presents helpful insights into the pharmacokinetic and pharmacodynamic properties of the reported cytotoxic metabolites belonging to family Malvaceae members. The molecular docking and dynamic simulations results intensify the roles of secondary metabolites from medicinal plants in fighting cancer.

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Analysis of the toxicological and pharmacokinetic profile of Kaempferol-3-O-β-D-(6”-E-p-coumaryl) glucopyranoside - Tiliroside: in silico, in vitro and ex vivo assay

Cited by 4 publications

References 36 publications

Avaliação da citotoxicidade em hemácias de humanos do extrato etanólico de Praxelis clematidea (Griseb.)

Avaliação da citotoxicidade em hemácias de humanos do extrato etanólico de Praxelis clematidea (Griseb.)

Citrus Flavonoids: Biological Activities, Implementation in Skin Health, and Topical Applications: A Review

Family Malvaceae: a potential source of secondary metabolites with chemopreventive and anticancer activities supported with in silico pharmacokinetic and pharmacodynamic profiles

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