Corneal Epithelial Wound Healing Promoted by Verbascoside-Based Liposomal Eyedrops

Ambrosone, Luigi; Guerra, Germano; Cinelli, Mariapia; Filippelli, Mariaelena; Mosca, Monica; Vizzarri, Francesco; Giorgio, Dario; Costagliola, Ciro

doi:10.1155/2014/471642

Cited by 18 publications

(15 citation statements)

References 34 publications

(26 reference statements)

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“…Despite the claimed antioxidant activity, the highly hydrophilic character of the active ingredient represents a limit for its application in different types of formulations. It has been shown that Verbascoside has neuropathic activity [34] and wound healing properties in corneal epithelia when delivered in a lyposome system [35]. In the present work we tested Verbascoside Pentapropionate (ES2) a more lipid-soluble Verbascoside formulation that has been previously synthetized in our laboratory [15].…”

Section: Discussionmentioning

confidence: 99%

ES2 as a Novel Verbascoside-Derived Compound in the Treatment of Cutaneous Wound Healing

et al. 2018

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Several pathologies are characterized by chronic wounds and often resistant to many of the common therapies, leading to chronic infections that can become even life-threatening for patients. For this reason, the identification of new products able to ameliorate the healing process is still an on-going research. Natural compounds have been used to improve skin conditions due to their dermo-cosmetic and therapeutic activities including anti-inflammatory, antioxidant and cell-migratory properties. Among these compounds, it has been recently demonstrated that Verbascoside, a phenyl propanoid glycoside widely used in the cosmetic field, can improve keratinocytes proliferation. Because of its high hydrophilic character, Verbascoside has a limited range of possible topical applications and the synthesis of ES2, a semi-synthetic derivative of Verbascoside was performed to bypass some of the drawback aspects of this molecule. In the present study, the wound healing properties of Verbascoside and ES2 were compared in both keratinocytes “in vitro” wound scratch and in wounded SKH1 mice. The results showed that both compounds were not cytotoxic and ES2 showed an efficient ability to promote the proliferation of human keratinocytes compared to Verbascoside. The findings were also confirmed in vivo but only at early time points (2/3 days). Taken together, these data suggest that the Verbascoside-derivative ES2 could be considered a novel and promising candidate for the topical treatment of wounds.

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Section: Discussionmentioning

confidence: 99%

ES2 as a Novel Verbascoside-Derived Compound in the Treatment of Cutaneous Wound Healing

et al. 2018

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“…28 Several therapeutics against corneal injury have been explored; and some cytokines, such as basic fibroblast growth factor (bFGF), epidermal growth factor (EGF), keratinocyte growth factor, vascular endothelial factor (VEGF), and pigment epithelium-derived factor (PEDF), have been found to stimulate corneal epithelial cell migration and wound closure in vivo. [29][30][31] However, with bFGF or EGF acting as the main therapeutics, bFGF-or EGF-induced corneal angiogenesis, which is currently untreatable, is a significant side effect. Thus for repair of corneal injury, effectively promoting wound closure, adequate corneal innervation, and neovascularization inhibition is key to restoring normal function.…”

Section: Discussionmentioning

confidence: 99%

A New Recombinant PACAP-Derived Peptide Efficiently Promotes Corneal Wound Repairing and Lacrimal Secretion

Zhao

Wang

et al. 2015

Invest. Ophthalmol. Vis. Sci.

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PURPOSE.A new recombinant pituitary adenylate cyclase-activating polypeptide (PACAP)-derived peptide, MPAPO, which has higher stability and PAC1-specific potency, was generated. The actions of MPAPO on corneal wound repairing and lacrimal secretion were examined.METHODS. MPAPO was prepared and identified by gene recombination, high-performance liquid chromatography (HPLC), and electrospray ionization mass spectrometry (ESI-MS). Stability assay was performed by HPLC-ESI-MS. PAC1-specific binding and potency assays were performed using PAC1-CHO cells. C57BL/6 mice and Japanese white rabbits were respectively used to analyze the effects of MPAPO on corneal wound repairing and lacrimal fluid secretion. Tetrazolium-based colorimetric assay (MTT), immunofluorescence, gene microarrays, and Western blot assay were performed to measure the effects of MPAPO on corneal epithelial cell proliferation, synapse growth, and gene differential expression of trigeminal ganglion cells. RESULTS.As compared with the wild PACAP, the in vitro stability and PAC1-specific potency of MPAPO with four mutations (M17L, L27K and M, K, respectively, added to the N-and Cterminus) were increased approximately 31-and 2-fold, respectively. MPAPO can significantly promote the proliferation of mouse corneal epithelium cells and the synapse growth of trigeminal ganglion cells. In experimental animals, MPAPO performed a complete corneal epithelial wound closure in 30 hours and significantly inhibited corneal neovascularization, and the effects were obviously stronger than for wild PACAP and recombinant bovine (rb)-bFGF (an anti-corneal wound drug). Furthermore, MPAPO can increase the lacrimal secretion, which may efficiently improve dry eye.CONCLUSIONS. MPAPO may represent a promising external therapeutic peptide for corneal wound repairing or dry eye.Keywords: gene recombination, pituitary adenylate cyclase activating polypeptide (PACAP)-derived peptide, PAC1 receptor, high stability, corneal wound repairing P ituitary adenylate cyclase-activating polypeptide (PACAP) is one of the important neuropolypeptides and a new member in the secretin/glucagon/vasoactive intestinal peptide (VIP) family.1 Pituitary adenylate cyclase-activating polypeptide is present in two forms, PACAP38 and PACAP27 in vivo, and has 60% homology with VIP, but the capacity of PACAP for stimulating brain pituicytes to generate adenylate cyclase is 1000-fold that of VIP.2 The biological actions of PACAP are mediated through three G protein-coupled receptors, namely, PAC1, VPAC1, and VPAC2. PAC1 is the specific 7-transmembrane receptor and exhibits high affinity for PACAP, but much lower affinity for VIP. VPAC1 and VPAC2 receptors display similar affinity for PACAP and VIP. 3 In mammals, PAC1 and VPAC receptors are expressed in the nervous, gastrointestinal, reproductive, and immune systems. However, PAC1 is mainly expressed in endocrine glands, such as the pituitary and adrenal, in the eye, and in the peripheral nervous system (PNS). In the PNS, especially in many ganglia and axons...

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“…It has been reported that verbascoside liposome can not only increase the stability, but also promote verbascoside accumulation into the stratum corneum 255 and improve the efficacy of a verbascoside based liposomal eyedrops. 256 Moreover, salidroside liposome formulation can be used in vaccine delivery systems to realize the controlled release of salidroside. 257 respectively, while that of CPhGs was 193.17 ng/ml and 15 min respectively.…”

Section: Nanotechnologymentioning

confidence: 99%

Therapeutic potential of phenylethanoid glycosides: A systematic review

Georgiev

Cao

et al. 2020

Medicinal Research Reviews

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Phenylethanoid glycosides (PhGs) are generally watersoluble phenolic compounds that occur in many medicinal plants. Until June 2020, more than 572 PhGs have been isolated and identified. PhGs possess antibacterial, anticancer, antidiabetic, anti-inflammatory, antiobesity, antioxidant, antiviral, and neuroprotective properties. Despite these promising benefits, PhGs have failed to fulfill their therapeutic applications due to their poor bioavailability. The attempts to understand their metabolic pathways to improve their bioavailability are investigated. In this review article, we will first summarize the number of PhGs compounds which is not accurate in the literature. The latest

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Corneal Epithelial Wound Healing Promoted by Verbascoside-Based Liposomal Eyedrops

Cited by 18 publications

References 34 publications

ES2 as a Novel Verbascoside-Derived Compound in the Treatment of Cutaneous Wound Healing

ES2 as a Novel Verbascoside-Derived Compound in the Treatment of Cutaneous Wound Healing

A New Recombinant PACAP-Derived Peptide Efficiently Promotes Corneal Wound Repairing and Lacrimal Secretion

Therapeutic potential of phenylethanoid glycosides: A systematic review

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