Cytotoxic and leishmanicidal properties of garcinielliptone FC, a prenylated benzophenone from<i>Platonia insignis</i>

Júnior, Joaquim Soares Costa; Almeida, Antônia Amanda Cardoso de; Ferraz, Alexandre de Barros Falcão; Rossatto, Raíssa Rebés; Silva, Teresinha G.; Silva, Paulo B.N.; Militão, Gardênia Carmen Gadelha; Citó, Antônia Maria das Graças Lopes; Santana, Lorena Citó Lopes Resende; Carvalho, Fernando Aécio de Amorim; Freitas, Rivelilson Mendes de

doi:10.1080/14786419.2012.695363

Cited by 37 publications

(21 citation statements)

References 16 publications

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“…In turn, GFC 20 and 30 lg/mL induced cell viability below 70% after exposure for 6 and 24 hr. The results of the present study confirm the findings published in a previous study [19], when GFC 25 lg/mL was shown to inhibit growth of NCI-H292 cells (mucoepidermoid carcinoma in human lung) by approximately 88% in the MTT test after 72 hr of exposure. Other benzophenones, such as 2,2 0 ,5,6 0 -tetrahydroxybenzophenone, isogarcinol, isoxanthochymol and guttiferone E, have been shown to be cytotoxic to the HCT116 colon carcinoma and leukaemia CCRF cell lines [37].…”

Section: Discussionsupporting

confidence: 92%

Evaluation of DNA Damage in HepG2 Cells and Mutagenicity of Garcinielliptone FC, A Bioactive Benzophenone

Prado

Silva

Garcia

et al. 2017

Basic Clin Pharma Tox

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Garcinielliptone FC (GFC) is a polyprenylated benzophenone isolated from the hexanic extract of Platonia insignis seeds with potential pharmacological effects on the central nervous system. In a pre-clinical study, this compound showed anticonvulsant action, becoming a candidate to treat epilepsy disorders. However, genotoxicological aspects of GFC should be known to ensure its safe use. This study investigated the cytotoxic, genotoxic, and mutagenic effects of GFC. Cytotoxicity was evaluated using the colorimetric assay of MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) in human hepatoma cells (HepG2) (2-100 μg/mL) for 3, 6 and 24 hr. The genotoxic and mutagenic potentials were analysed using the alkaline version of the comet assay, the cytokinesis-block micronucleus cytome assay in HepG2 cells, and the Salmonella/microsome assay with the strains TA98, TA97a, TA100, TA102 and TA1535, with and without metabolic activation. GFC concentrations above 50 μg/mL were cytotoxic at all experimental times. Viability of HepG2 cells was higher than 70% after exposure to GFC 2-30 μg/mL for 3 hr in the MTT test. No GFC concentration was mutagenic or genotoxic in the Salmonella/microsome and comet assays. Nuclear division index decreased, indicating the cytotoxic effect of the compound, while micronucleus and nuclear bud frequencies rose after treatment with the highest GFC concentration tested (30 μg/mL). Nucleoplasmatic bridges were not observed. The results indicate that GFC is cytotoxic and mutagenic to mammalian cells, pointing to the need for further studies to clarify the toxicological potentials of this benzophenone before proceeding to clinical studies.

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Section: Discussionsupporting

confidence: 92%

Evaluation of DNA Damage in HepG2 Cells and Mutagenicity of Garcinielliptone FC, A Bioactive Benzophenone

Prado

Silva

Garcia

et al. 2017

Basic Clin Pharma Tox

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“…Its fruits are known for their pleasant taste and aroma and are highly appreciated by the Amazonian people [15]. Some studies have reported the biological activity of different extracts of P. insignis and the chemical components, such as Garcinielliptone FC, responsible for the biological activity, have already been isolated and identified [12,13,16]. However, the ethnopharmacological use of P. insignis is related to the use of the extracts of its seeds, bark, or fruit pulp because of its ability to heal, anti-inflammatory effects, leishmanicidal agents, antioxidants, and cytotoxic activities.…”

Section: Discussionmentioning

confidence: 99%

“…Native to the Brazilian Amazon forests, P. insignis is a fruit-bearing and woody plant with a dense and diverse distribution throughout the country [11]. Traditionally, it has been used to treat various ailments related to the digestive tract and rapid wound healing, and was also reported to have diuretic and antitumor properties [12,13].…”

Section: Introductionmentioning

confidence: 99%

“…Previous natural product studies have focused on the characterization of fats extracted from seeds used in folk medicine to treat diarrhea, skin problems, earaches, rheumatism, arthritis, and scarring [12][13][14]. There have been some reports investigating the effects of P. insignis seed compounds as antioxidants, anti-inflammatory agents, cytotoxic agents, and leishmanicidal agents.…”

Section: Introductionmentioning

confidence: 99%

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Antifungal and Antivirulence Activities of Hydroalcoholic Extract and Fractions of Platonia insignis Leaves against Vaginal Isolates of Candida Species

Silva

Rocha

Silva³

et al. 2020

Pathogens

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Vulvovaginal candidiasis is a common fungal infection in women. In this study, Platonia insignis hydroalcoholic extract (PiHE) and its fractions were evaluated for antifungal and antivirulence activities against vaginal Candida species. Dichloromethane (DCMF) and ethyl acetate fractions (EAF) obtained from PiHE effectively inhibited the pathogen. Electrospray ionization mass spectrometry was used for identifying the main compounds in extracts. Minimal inhibitory and fungicidal concentrations (MIC and MFC, respectively) were determined by a broth microdilution assay. Furthermore, we evaluated the effect of the extract and fractions on the virulence properties of Candida albicans, and their cytotoxicity effect was determined on RAW 264.7 cells. Compounds found in extracts were flavonoid glycosides, mainly derivatives of quercetin and myricetin. Extracts showed antifungal potential, with the lowest MIC value for EAF (1.3 mg/mL) and inhibited Candida adherence and biofilm formation. EAF disrupted 48 h biofilms with an inhibition rate of more than 90%. The extract and its fractions exhibited no cytotoxicity. The antifungal effects were attributed to the ability of these extracts to alter the mitochondrial membrane potential for the release of pro-apoptotic factors in the cytosol. In conclusion, our data suggest that PiHE and EAF could act as novel candidates for the development of new therapeutic treatments against fungal infections.

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“…The species P. insignis cannot be considered an herbal yet, but the GFC isolated from the hexane extract of its seeds has been used in various experimental protocols and has demonstrated several biological properties such as anti-inflammatory [28], antioxidant [1,29], antileishmanial, cytotoxic [30] and vasorelaxing properties in rat mesenteric artery [31]. These data and the present study are useful to provide more information to strengthen the rational therapy and safety margins of pharmaceutical, cosmetic and/or food products originated from this species, such as, folk juices, ice creams, jellies, among others by the Brazilian Northeast population.…”

Section: Discussionmentioning

confidence: 99%

Toxicological Study Employing Repeated Doses of Garcinielliptone FC, a Polyisoprenylated-Benzophenone Isolated from Seed of Platonia Insignis Mart

Silva¹,

Filho²,

Júnior³

et al. 2015

JPP

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Abstract:The major constituent from the hexane extract of the seeds of P. insignis is GFC (garcinielliptone FC). Doses of 25, 50 and 75 mg/kg of GFC were aseptically suspended in 0.05% Tween 80 dissolved in 0.9% saline (vehicle) and orally administered for 30, 90 and 120 consecutive days to adult Swiss mice. In this work, the repeated oral administration, in animals of both sexes, demonstrates that this compound is not able to induce mortality and/or behavioral changes in adult mice. In addition, body weight gain, feed intake and disposal of excreta were not altered by the administration of this compound with repeated doses. Furthermore, no differences in weight and macroscopic structure of the brain, liver, kidney, lung, heart and spleen between groups of male and female adult mice were observed after treatment. During the periods of treatment, GFC produced no significant changes on haematological and biochemical parameters in male and female mice treated with all doses used. The aim of this study was to investigate the toxicological potential of GFC through behavioral, hematological, biochemical and morphological parameters in animals in order to ensure the safe use of Platonia insignis in folk medicine.

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Cytotoxic and leishmanicidal properties of garcinielliptone FC, a prenylated benzophenone fromPlatonia insignis

Cited by 37 publications

References 16 publications

Evaluation of DNA Damage in HepG2 Cells and Mutagenicity of Garcinielliptone FC, A Bioactive Benzophenone

Evaluation of DNA Damage in HepG2 Cells and Mutagenicity of Garcinielliptone FC, A Bioactive Benzophenone

Antifungal and Antivirulence Activities of Hydroalcoholic Extract and Fractions of Platonia insignis Leaves against Vaginal Isolates of Candida Species

Toxicological Study Employing Repeated Doses of Garcinielliptone FC, a Polyisoprenylated-Benzophenone Isolated from Seed of Platonia Insignis Mart

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