In vivo schistosomicidal activity of 7-epiclusianone and its quantification in the plasma of healthy and Schistosoma mansoni infected mice using UPLC-MS/MS

Castro, Aline Pereira; Kawano, Taila; Spelta, Lídia Emmanuela Wiazowski; Castro, Andreísa Teixeira de; Pereira, Neusa Araújo; Couto, Flávia Fernanda Búbula; Santos, Marcelo H. dos; Boralli, Vanessa Bergamin; Marques, Marcos José

doi:10.1016/j.phymed.2017.11.001

Cited by 11 publications

(8 citation statements)

References 23 publications

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“…In combination, these effects suggest that 7- epi -clusianone could be used to slow the progression of many variations of cancer, but it will not be cytotoxic to all types of cells. As 7- epi -clusianone is likely to be safe in vivo at relatively high concentrations [30] and the compound is selective in inducing cell death, has the potential to be safely used for the treatment of a diverse group of cancers. In particular, renal cancer, melanoma, central nervous system tumors, colon cancer, and non-small cell lung cancer appear to be sensitive to the cytotoxic effects of 7- epi -clusianone.…”

Section: Discussionmentioning

confidence: 99%

“…7- epi -clusianone and its configurational isomers are natural products that have been demonstrated to feature antimicrobial, anti-allergenic, schistosomicidal, and anti-inflammatory effects [30,31,32,33]. Additionally, these compounds have been shown to induce cell death in glioblastoma, as well as lung, melanoma, breast, prostate, renal, cervical, and tongue cancer [34,35,36,37].…”

Section: Introductionmentioning

confidence: 99%

“…It is likely that multiple molecules are targeted by 7- epi -clusianone and its isomers due to the so-called “privileged structures” typically possessed by natural products. Limited in vivo studies have demonstrated the safety of a 7-epiclusianone in vivo in administrations of up to 300 mg/kg of body weight in female albino mice [30]. Additionally, the chemical synthesis of 7- epi -clusianone has been explored, allowing for a high availability of the compounds in the future [39].…”

Section: Introductionmentioning

confidence: 99%

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7-epi-Clusianone, a Multi-Targeting Natural Product with Potential Chemotherapeutic, Immune-Modulating, and Anti-Angiogenic Properties

et al. 2019

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Targeted therapies have changed the treatment of cancer, giving new hope to many patients in recent years. The shortcomings of targeted therapies including acquired resistance, limited susceptible patients, high cost, and high toxicities, have led to the necessity of combining these therapies with other targeted or chemotherapeutic treatments. Natural products are uniquely capable of synergizing with targeted and non-targeted anticancer regimens due to their ability to affect multiple cellular pathways simultaneously. Compounds which provide an additive effect to the often combined immune therapies and cytotoxic chemotherapies, are exceedingly rare. These compounds would however provide a strengthening bridge between the two treatment modalities, increasing their effectiveness and improving patient prognoses. In this study, 7-epi-clusianone was investigated for its anticancer properties. While previous studies have suggested clusianone and its conformational isomers, including 7-epi-clusianone, are chemotherapeutic, few cancer types have been demonstrated to exhibit sensitivity to these compounds and little is known about the mechanism. In this study, 7-epi-clusianone was shown to inhibit the growth of 60 cancer cell types and induce significant cell death in 25 cancer cell lines, while simultaneously modulating the immune system, inhibiting angiogenesis, and inhibiting cancer cell invasion, making it a promising lead compound for cancer drug discovery.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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7-epi-Clusianone, a Multi-Targeting Natural Product with Potential Chemotherapeutic, Immune-Modulating, and Anti-Angiogenic Properties

et al. 2019

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“…Matrix effect variation was expressed as a coefficient of variation (CV %) of the normalised matrix factor (NMF) values (Table S3). For each concentration tested, the CV % value was low and acceptable according to the required validation limits guidelines 29,30 . The plasma matrix did not interfere in the detection of both substances (PGE 2 and IS) since there was no sign in the chromatogram regarding the correspondent RTs in the blank plasma sample (Figure 1).…”

Section: Resultsmentioning

confidence: 69%

In vivo anti‐inflammatory activity of Fabaceae species extracts screened by a new ex vivo assay using human whole blood

Rosa

Domingos

Salem

et al. 2021

Phytochemical Analysis

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Introduction Plants have been considered a promising source for discovering new compounds with pharmacological activities. The Fabaceae family comprises a large variety of species that produce substances with diverse therapeutic potential, including anti‐inflammatory activity. The limitations of current anti‐inflammatories generate the need to research new anti‐inflammatory structures with higher efficacy as well as develop methods for screening multiple samples, reliably and ethically, to assess such therapeutic properties. Objective Validate and apply a quantification method for prostaglandin E2 (PGE2) production from an ex vivo assay in human blood in order to screen anti‐inflammatory activity present in many Fabaceae species extracts. Methods Human blood was incubated with extracts from 47 Fabaceae species. After lipopolysaccharide (LPS)‐induced inflammation, PGE2 was quantified in the plasma by liquid chromatography with tandem mass spectrometry (LC–MS/MS). The extracts that presented PGE2 production inhibition were further assessed through in vivo assay and then chemically characterised through an analysis of ultra‐performance liquid chromatography electrospray ionisation quadrupole time‐of‐flight tandem mass spectrometry (UPLC‐ESI‐QTOF‐MS2) data. Results The new ex vivo anti‐inflammatory assay showed that five out of the 47 Fabaceae species inhibited PGE2 production. Results from an in vivo assay and the metabolic profile of the active extracts supported the anti‐inflammatory potential of four species. Conclusion The quantification method for PGE2 demonstrated fast, sensitive, precise, and accurate results. The new ex vivo anti‐inflammatory assay comprised a great, reliable, and ethical approach for the screening of a large number of samples before an in vivo bioassay. Additionally, the four active extracts in both ex vivo and in vivo assays may be useful for the development of more efficient anti‐inflammatory drugs.

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“…The benzophenones (guttiferone E, isoxanthochymol, and guttiferone H) isolated from G. xanthochymus exhibited antiplasmodial activity with IC 50 values in the range of 4.71-11.40 µM [23]. The tetraprenylated benzophenone 7-epiclusianone (7-epi) was isolated from the fruits of G. brasiliensis showed effective against Schistosoma mansoni [24]. In addition, bi avanones (GB-1a, GB-1, and GB-2), another active compounds, were isolated from G. kola.…”

Section: Discussionmentioning

confidence: 99%

Synergistic Effect of Garcinia Mangostana Combined With Chlorhexidine on Acanthamoeba Triangularis Trophozoites and Cysts

Sangkanu

Mitsuwan

Mahabusarakam

et al. 2020

Preprint

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Background: Various parts of Garcinia mangostana Linn, including its pericarp have been traditionally used to treat different types of diseases. This study was carried out to determine the anti-Acanthamoeba activity of G. mangostana pericarp extract against Acanthamoeba triangularis. Methods: The G. mangostana ethanolic pericarp extract was screened for the anti-Acanthamoeba activity and determined its minimal inhibition concentrations (MICs) by the microdilution method. Then, the time-kill kinetic assay of the extract was determined. The synergistic effect of G. mangostana extract and chlorhexidine was performed using the checkerboard method. Parasite morphology was detected by scanning electron microscopy (SEM).Results: The MICs of extract were assessed on trophozoites and cysts with 250 and 4000 µg/mL, respectively. More so, at 2×MIC of extract exhibited inhibitory activity against trophozoites and cyst of A. triangularis for up to 7 days. Checkerboard assays showed synergistic activity of extract (500-1000 μg/mL) plus chlorhexidine (3.90-15.62 μg/mL) at a fractional inhibitory concentration index (FICI) of 0.18-0.37. The lowest FICI (0.18) displayed good synergism resulting in up to 16-fold reduction of drug MIC and reducing to 8-fold of extract MIC. The viability of cysts decreased to 12.28±3.03 cells/mL. FICI interpretation equal to 1 is considered an additive effect on Acanthamoeba trophpzoites. The SEM results clearly showed that Acanthamoeba cells treated with a single drug of chlorhexidine and its combination with G. mangostana extract caused cell membrane damage and irregular cell shapes comparing with the control. Conclusion: A good combinatorial relationship displayed by G. mangostana extract and chlorhexidine suggest a more reliable evidenced based therapeutic strategy. Therefore, this approach is promising and could be employed as an alternative treatment method for the management of Acanthamoeba infection.

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In vivo schistosomicidal activity of 7-epiclusianone and its quantification in the plasma of healthy and Schistosoma mansoni infected mice using UPLC-MS/MS

Cited by 11 publications

References 23 publications

7-epi-Clusianone, a Multi-Targeting Natural Product with Potential Chemotherapeutic, Immune-Modulating, and Anti-Angiogenic Properties

7-epi-Clusianone, a Multi-Targeting Natural Product with Potential Chemotherapeutic, Immune-Modulating, and Anti-Angiogenic Properties

In vivo anti‐inflammatory activity of Fabaceae species extracts screened by a new ex vivo assay using human whole blood

Synergistic Effect of Garcinia Mangostana Combined With Chlorhexidine on Acanthamoeba Triangularis Trophozoites and Cysts

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