Erufosine Induces Autophagy and Apoptosis in Oral Squamous Cell Carcinoma

Kapoor, Vaishali; Zaharieva, Maya M.; Berger, Martin R.

doi:10.1016/b978-0-12-405529-2.00016-0

Cited by 3 publications

(4 citation statements)

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“…In contrast to MLT, which forms micellar aqueous solutions and cannot be applied intravenously due to hemolytic properties, ERF forms lamellar aqueous solutions, and is suitable for intravenous administration [4,5,33]. ERF exerts remarkably strong antineoplastic activity in vitro against various types of neoplasias related to bacterial infections, such as oral squamous cell carcinoma [30,34,35] and cutaneous T-cell lymphoma [36,37]. Bacterial infections may compromise the anticancer therapy outcome due to inflammation in the tissue microenvironment and accelerated carcinogenesis [38][39][40][41][42].…”

Section: Introductionmentioning

confidence: 99%

Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenicStaphyloccocus aureusstrains

Zaharieva

Kroumov

Dimitrova

et al. 2019

Biotechnology & Biotechnological Equipment

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2019) Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenic Staphyloccocusaureus strains, Biotechnology & Biotechnological Equipment, 33:1,[38][39][40][41][42][43][44][45][46][47][48][49][50][51][52][53] ABSTRACT In the light of the emerging bacterial resistance to broad-spectrum antibiotics, the search for new antibacterial therapeutics and drug combinations is one of the most challenging topics nowadays. In the present study, we investigated for the first time the antibacterial and biofilm inhibitory effects of the third generation anticancer alkylphosphocholine (APC) erufosine against pathogenic Staphylococcus aureus strains in comparison to the prototype of this pharmacological class of drugs, miltefosine. We also searched for synergistic antibacterial combinations between both APCs and curcumin incorporated in copolymeric micelles based on PluronicV R P123 or a mixture of Pluronic V R P123 and Pluronic V R F127 (P123/F127). The obtained quantitative redoxactivity experimental data and drug-drug interactions were evaluated by using mathematical models in the MAPLE software. Similar to miltefosine, erufosine showed a moderate bacteriostatic effect in clinically relevant concentrations (50 Ä 60 lmol/L) and inhibited the redox activity of the treated bacteria up to 90% at minimal inhibitory concentrations. The effect of both APCs towards methicillin resistant staphylococci was enhanced by combinations with P123/F127 micellar CRM at a ratio of 1:1. Erufosine showed a stronger median biofilm inhibition at lower concentrations (MBIC 50 ¼ 1.87 lmol/L) than miltefosine (MBIC 50 ¼ 6.0 lmol/L) and curcumin (MBIC 50 ¼ 24.84 lmol/L) as demonstrated by quantification of biofilm-bound bacteria. In conclusion, the estimated antibacterial activity of erufosine widens the spectrum of its useful pharmacological effects, which is important for its clinical development. The established synergistic and additive drug combinations could be beneficial for the application of both APCs in cancer therapy, since numerous malignancies are accompanied by bacterial infections. ARTICLE HISTORY

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Section: Introductionmentioning

confidence: 99%

Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenicStaphyloccocus aureusstrains

Zaharieva

Kroumov

Dimitrova

et al. 2019

Biotechnology & Biotechnological Equipment

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“…Abirami et al 2018, evaluated the expression pattern of p-mTOR in various grades of OSCC in comparison to normal tissue to identify the dyspegulation in PI3K/Akt/mTOR pathway and identified p-mTOR as an effective prognostic marker [56]. Kapoor et al 2014, studied the anti-cancer activity of Erufosine by inducing autophagy via modulation of mTOR. Apart from autophagy, the compound showed effective therapeutic effect on the entire PI3K/Akt/mTOR pathway causing cell cycle arrest by downregulation of cyclin D1 and also induced apoptosis [57].…”

Section: Pi3k/akt Autophagy In Oral Squamous Cell Carcinomamentioning

confidence: 99%

“…Kapoor et al 2014, studied the anti-cancer activity of Erufosine by inducing autophagy via modulation of mTOR. Apart from autophagy, the compound showed effective therapeutic effect on the entire PI3K/Akt/mTOR pathway causing cell cycle arrest by downregulation of cyclin D1 and also induced apoptosis [57]. Inui et al 2013, studied the expression pattern of p62 and its association with the survival rate by modulating PI3K/Akt pathway [58].…”

Section: Pi3k/akt Autophagy In Oral Squamous Cell Carcinomamentioning

confidence: 99%

PI3K/AKT Signaling Pathway Mediated Autophagy in Oral Carcinoma - A Comprehensive Review

Rajendran,

Sekar,

Dhayasankar

et al. 2024

Int. J. Med. Sci.

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Oral cancer is the most heterogeneous cancer at clinical and histological levels. PI3K/AKT/mTOR pathway was identified as one of the most commonly modulated signals in oral cancer, which regulates major cellular and metabolic activity of the cell. Thus, various proteins of PI3K/AKT/mTOR pathway were used as therapeutic targets for oral cancer, to design more specific drugs with less off-target toxicity. This review sheds light on the regulation of PI3K/AKT/mTOR, and its role in controlling autophagy and associated apoptosis during the progression and metastasis of oral squamous type of malignancy (OSCC). In addition, we reviewed in detail the upstream activators and the downstream effectors of PI3K/AKT/mTOR signaling as potential therapeutic targets for oral cancer treatment.

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“…The solubility of LPC was reported to be higher when a mixture of organic solvents, chloroform: methanol (2:1), was used, compared to its solubility in methanol or chloroform alone [ 45 ]. LPCs are metabolically stable compared to the parent PC compound [ 46 ]. Pure LPC from egg yolk at −0 °C has been reported to be stable for up to 1 year [ 45 ].…”

Section: Properties Of Lpcmentioning

confidence: 99%

Marine Fish-Derived Lysophosphatidylcholine: Properties, Extraction, Quantification, and Brain Health Application

et al. 2023

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Long-chain omega-3 fatty acids esterified in lysophosphatidylcholine (LPC-omega-3) are the most bioavailable omega-3 fatty acid form and are considered important for brain health. Lysophosphatidylcholine is a hydrolyzed phospholipid that is generated from the action of either phospholipase PLA1 or PLA2. There are two types of LPC; 1-LPC (where the omega-3 fatty acid at the sn-2 position is acylated) and 2-LPC (where the omega-3 fatty acid at the sn-1 position is acylated). The 2-LPC type is more highly bioavailable to the brain than the 1-LPC type. Given the biological and health aspects of LPC types, it is important to understand the structure, properties, extraction, quantification, functional role, and effect of the processing of LPC. This review examines various aspects involved in the extraction, characterization, and quantification of LPC. Further, the effects of processing methods on LPC and the potential biological roles of LPC in health and wellbeing are discussed. DHA-rich-LysoPLs, including LPC, can be enzymatically produced using lipases and phospholipases from wide microbial strains, and the highest yields were obtained by Lipozyme RM-IM®, Lipozyme TL-IM®, and Novozym 435®. Terrestrial-based phospholipids generally contain lower levels of long-chain omega-3 PUFAs, and therefore, they are considered less effective in providing the same health benefits as marine-based LPC. Processing (e.g., thermal, fermentation, and freezing) reduces the PL in fish. LPC containing omega-3 PUFA, mainly DHA (C22:6 omega-3) and eicosapentaenoic acid EPA (C20:5 omega-3) play important role in brain development and neuronal cell growth. Additionally, they have been implicated in supporting treatment programs for depression and Alzheimer’s. These activities appear to be facilitated by the acute function of a major facilitator superfamily domain-containing protein 2 (Mfsd2a), expressed in BBB endothelium, as a chief transporter for LPC-DHA uptake to the brain. LPC-based delivery systems also provide the opportunity to improve the properties of some bioactive compounds during storage and absorption. Overall, LPCs have great potential for improving brain health, but their safety and potentially negative effects should also be taken into consideration.

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Erufosine Induces Autophagy and Apoptosis in Oral Squamous Cell Carcinoma

Cited by 3 publications

References 44 publications

Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenicStaphyloccocus aureusstrains

Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenicStaphyloccocus aureusstrains

PI3K/AKT Signaling Pathway Mediated Autophagy in Oral Carcinoma - A Comprehensive Review

Marine Fish-Derived Lysophosphatidylcholine: Properties, Extraction, Quantification, and Brain Health Application

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