ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors

Verdoni, Marion; Roudaut, Hermine; Pomyers, Harold De; Gigmès, Didier; Luis, José; Bengeloune, Abd Haq; Mabrouk, Kamel

doi:10.1016/j.bmc.2016.08.023

Cited by 18 publications

(8 citation statements)

References 20 publications

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“…There is some evidence that a secretion of the mollusk Cryptomphalus aspersa possesses an antioxidant property in vitro and induces fibroblast proliferation by promoting the extracellular matrix assembly that can be applied for wound healing (Brieva et al, 2008). Spider venom (Argiope lobate) was recently studied as a potential inhibitor of melanogenesis in skin aging and a polyamine ArgTX-636 was identified as the novel class of melanogenesis inhibitors both in vitro and in B16F10 cells (Verdoni et al, 2016). In other studies, venoms from Hymenoptera were recently reported as a potential source for pharmacology and cosmetic applications while bee venom was found to possess significant antimicrobial activity on different bacterial species (Morais et al, 2011;Surendra et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Asian hornet Vespa velutina nigrithorax venom: Evaluation and identification of the bioactive compound responsible for human keratinocyte protection against oxidative stress

Silva

Colas

et al. 2020

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The present study aimed to explore the potential use of antioxidant molecules of the Asian hornet venom (Vespa velutina nigrithorax) to prevent or reduce skin aging. We developed a first technical platform that combined a DPPH radical scavenging chemical assay and cytotoxicity and ROS (reactive oxygen species) production in HaCaT keratinocyte cells exposed to UVB to evaluate the antioxidant property of V. velutina venom. We further employed Thin Layer Chromatography (TLC) combined with the DPPH assay as a targeted separation approach to isolate the antioxidant compounds responsible for the free radical scavenging property of V. velutina venom. In parallel, the latter was fractionated by a HPLC-DAD non-targeted separation approach. From this experiment, nine fractions were generated which were again evaluated separately for their antioxidant properties using DPPH assays. Results showed that only one fraction exhibited significant antioxidant activity in which serotonin was identified as the major compound by a UHPLC-ESI-QTOF HRMS/MS approach. We finally demonstrated, using purified serotonin molecule, that this bioactive structure is mostly responsible for the free radical scavenging property of the crude venom as evidenced by DPPH and ROS assays in HaCaT cells exposed to UVB.

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Section: Introductionmentioning

confidence: 99%

Asian hornet Vespa velutina nigrithorax venom: Evaluation and identification of the bioactive compound responsible for human keratinocyte protection against oxidative stress

Silva

Colas

et al. 2020

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“…Venoms are thus precious sources of bioactive components with various valuable activities [ 7 , 21 ]. We previously isolated from the Argiope lobata spider venom a compound able to regulate melanin production through the inhibition of tyrosinase [ 22 ]. In the present paper, we show for the first time that snake venom contains microtubule-targeting activity.…”

Section: Discussionmentioning

confidence: 99%

Myotoxin-3 from the Pacific Rattlesnake Crotalus oreganus oreganus Venom Is a New Microtubule-Targeting Agent

et al. 2022

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Microtubule targeting agents (MTA) are anti-cancer molecules that bind tubulin and interfere with the microtubule functions, eventually leading to cell death. In the present study, we used an in vitro microtubule polymerization assay to screen several venom families for the presence of anti-microtubule activity. We isolated myotoxin-3, a peptide of the crotamine family, and three isoforms from the venom of the Northern Pacific rattlesnake Crotalus oreganus oreganus, which was able to increase tubulin polymerization. Myotoxin-3 turned out to be a cell-penetrating peptide that slightly diminished the viability of U87 glioblastoma and MCF7 breast carcinoma cells. Myotoxin 3 also induced remodeling of the U87 microtubule network and decreased MCF-7 microtubule dynamic instability. These effects are likely due to direct interaction with tubulin. Indeed, we showed that myotoxin-3 binds to tubulin heterodimer with a Kd of 5.3 µM and stoichiometry of two molecules of peptide per tubulin dimer. Our results demonstrate that exogenous peptides are good candidates for developing new MTA and highlight the richness of venoms as a source of pharmacologically active molecules.

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“…For example, the anti-wrinkling effect of the botulinum toxin (Botox ® ), a toxin isolated from Clostridium botulinum bacteria, accounts for striking global sales of about $3 billion per year ( Clark et al., 2019 ). Among the biologically active compounds from animal venoms showing cosmeceuticals applications, we can cite the use of bee venom-containing cosmetics on facial wrinkles in human skin ( Han et al., 2015 ), and the inhibitory activity of melanogenesis of Argiotoxine-636 (ArgTX-636), a polyamine isolated from Argiope lobata spider venom ( Verdoni et al., 2016 ), including a deposited patent (US10064814B2) for skin whitening/depigmenting ( Mabrouk et al., 2018 ). Another example is the synthetic tripeptide [dipeptide diaminobutyroyl benzylamide diacetate (H-β-Ala-Pro-Dab-NHBzl x 2 AcOH)], commercialized as the cosmeceutical SYN ® -AKE (Pentapharm).…”

Section: Achievements With Animal Toxin-based Moleculesmentioning

confidence: 99%

From Animal Poisons and Venoms to Medicines: Achievements, Challenges and Perspectives in Drug Discovery

et al. 2020

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ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors

Cited by 18 publications

References 20 publications

Asian hornet Vespa velutina nigrithorax venom: Evaluation and identification of the bioactive compound responsible for human keratinocyte protection against oxidative stress

Asian hornet Vespa velutina nigrithorax venom: Evaluation and identification of the bioactive compound responsible for human keratinocyte protection against oxidative stress

Myotoxin-3 from the Pacific Rattlesnake Crotalus oreganus oreganus Venom Is a New Microtubule-Targeting Agent

From Animal Poisons and Venoms to Medicines: Achievements, Challenges and Perspectives in Drug Discovery

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