Computed determination of the in vitro optimal chemocombinations of sphaeropsidin A with chemotherapeutic agents to combat melanomas

Ingels, Aude; Dinhof, Carina; Garg, Abhishek D.; Maddau, Lucia; Masi, Marco; Berger, Walter; Dejaegher, Bieke; Mathieu, Véronique

doi:10.1007/s00280-017-3293-x

Cited by 12 publications

(12 citation statements)

References 54 publications

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“…92 The authors found that 75 μM of cisplatin and 850 μM of temozolamide (DNA damaging agents) combined with 4 to 6 μM of sphaeropsidin A provided the maximum in vitro cytotoxic response with >90% of cellular lethality. 92 The authors found that 75 μM of cisplatin and 850 μM of temozolamide (DNA damaging agents) combined with 4 to 6 μM of sphaeropsidin A provided the maximum in vitro cytotoxic response with >90% of cellular lethality.…”

Section: Icacina Trichanthamentioning

confidence: 99%

“…Furthermore, a very recent 2017 article describes a positive synergistic effect of sphaeropsidin A with cisplatin and temozolamide against the predictive kinase biomarkers for the melanoma tumors serine/threonine protein kinase B-raf, mitogen activated protein kinase, and a receptor tyrosine kinase, to increase their vitro efficiency. 92 The authors found that 75 μM of cisplatin and 850 μM of temozolamide (DNA damaging agents) combined with 4 to 6 μM of sphaeropsidin A provided the maximum in vitro cytotoxic response with >90% of cellular lethality. This combination chemotherapy with different mechanisms of action (ion transport inhibitor with DNA damaging agents) could lead to a lower therapeutic dose of these cytotoxic anticancer agents with reduced side effects.…”

Section: Icacina Trichanthamentioning

confidence: 99%

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Pimarane diterpenes: Natural source, stereochemical configuration, and biological activity

et al. 2018

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Plants and fungi are seemingly inexhaustible sources of interesting natural products with remarkable structural and biological diversity. One of the most important groups is the terpenes, ubiquitous natural products that are generated by 2 now well-established biosynthetic pathways: the older mevalonate and the more recently discovered 1-deoxyxylulose-5-phosphate. Among the diterpenes, the pimarane diterpenes are a very representative subgroup with several and interesting biological activities resulting from different functional group modifications. In this review, we outline the method of their structure determination, mainly spectroscopic results, their absolute configuration, and structure-activity relationships, were reported, as well as the mode of action for selected examples from plants, marine organisms, and fungi. The pimarane, isopimarane, and ent-pimarane diterpenes covered in this review have a wide range of biological activities including antimicrobial, antifungal, antiviral, phytotoxic, phytoalexin, cytotoxicity, and antispasmodic and relaxant effects.

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Section: Icacina Trichanthamentioning

confidence: 99%

Section: Icacina Trichanthamentioning

confidence: 99%

Pimarane diterpenes: Natural source, stereochemical configuration, and biological activity

et al. 2018

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“…Compound 20 exhibited in vitro antibacterial activity towards Xanthomonas oryzae pv. oryzae , the causal agent of rice bacterial blight [ 43 ] and showed promising anticancer activity against drug-resistant melanoma cells [ 44 , 45 ]. Given that the absolute configuration (AC) is strictly linked to biological activity [ 46 , 47 ], the AC of 12 – 14 , 19 and 20 was determined using different methods [ 48 , 49 , 50 ].…”

Section: Resultsmentioning

confidence: 99%

Anti-Biofilm Activity of the Fungal Phytotoxin Sphaeropsidin A against Clinical Isolates of Antibiotic-Resistant Bacteria

Roscetto

Masi²,

Esposito

et al. 2020

Toxins

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Many pathogens involved in human infection have rapidly increased their antibiotic resistance, reducing the effectiveness of therapies in recent decades. Most of them can form biofilms and effective drugs are not available to treat these formations. Natural products could represent an efficient solution in discovering and developing new drugs to overcome antimicrobial resistance and treat biofilm-related infections. In this study, 20 secondary metabolites produced by pathogenic fungi of forest plants and belonging to diverse classes of naturally occurring compounds were evaluated for the first time against clinical isolates of antibiotic-resistant Gram-negative and Gram-positive bacteria. epi-Epoformin, sphaeropsidone, and sphaeropsidin A showed antimicrobial activity on all test strains. In particular, sphaeropsidin A was effective at low concentrations with Minimum Inhibitory Concentration (MIC) values ranging from 6.25 μg/mL to 12.5 μg/mL against all reference and clinical test strains. Furthermore, sphaeropsidin A at sub-inhibitory concentrations decreased methicillin-resistant S. aureus (MRSA) and P. aeruginosa biofilm formation, as quantified by crystal violet staining. Interestingly, mixtures of sphaeropsidin A and epi-epoformin have shown antimicrobial synergistic effects with a concomitant reduction of cytotoxicity against human immortalized keratinocytes. Our data show that sphaeropsidin A and epi-epoformin possess promising antimicrobial properties.

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“…In vitro combinations of sphaeropsidin A (Sph A) (66) with either cisplatin or temozolomide, showed that combining 4 µM Sph A with 75 µM cisplatin for 72 h had a synergistic cytotoxic effect independent of BRAF or NRAS mutations [96].…”

Section: Combination Therapiesmentioning

confidence: 99%

Natural Cytotoxic Diterpenoids, a Potential Source of Drug Leads for Melanoma Therapy

Prieto

Silveira

2019

CPD

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Diterpenes present complex structure and due to their unique carbon skeleton and interesting biological activities, have been the focus of continuous studies for the development of new anticancer agents. Phorbol esters have been known for their activity against skin malignancies since ancient times. Taxol was first studied in melanoma cells, and recently ingenol mebutate has been approved for the chemoprevention of melanoma in actinic keratosis patients. Therefore, there is scope for research on this class of compounds. We here aim to review the relevant original research reporting on isolated diterpenes with cytotoxic and/or antitumoral activities upon melanoma cells. By collating and discussing the implications of past and current developments on diterpenes, we hope to steer further interest on this field and facilitate the drug discovery activities of the scientific community towards finding potential alternatives to current melanoma chemotherapy.

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Computed determination of the in vitro optimal chemocombinations of sphaeropsidin A with chemotherapeutic agents to combat melanomas

Cited by 12 publications

References 54 publications

Pimarane diterpenes: Natural source, stereochemical configuration, and biological activity

Pimarane diterpenes: Natural source, stereochemical configuration, and biological activity

Anti-Biofilm Activity of the Fungal Phytotoxin Sphaeropsidin A against Clinical Isolates of Antibiotic-Resistant Bacteria

Natural Cytotoxic Diterpenoids, a Potential Source of Drug Leads for Melanoma Therapy

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