Rhamnetin Attenuates Melanogenesis by Suppressing Oxidative Stress and Pro-inflammatory Mediators

Kim, You Jung

doi:10.1248/bpb.b13-00276

Cited by 27 publications

(16 citation statements)

References 33 publications

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“…Melanogenesis involves the enzyme tyrosinase for catalyzing the oxidative reaction of tyrosine to dihydroxy-phenylalanine (DOPA) and Dopaquinone, a common intermediate to both eumelanogenic and pheomelanogenic pathways [ 61 – 63 ]. Conventionally, L-tyrosine and L-DOPA are regarded as positive regulators of melanogenesis [ 64 ].…”

Section: Resultsmentioning

confidence: 99%

Protective Effects of Triphala on Dermal Fibroblasts and Human Keratinocytes

Varma¹,

Sivaprakasam²,

Mishra³

et al. 2016

PLoS ONE

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Human skin is body’s vital organ constantly exposed to abiotic oxidative stress. This can have deleterious effects on skin such as darkening, skin damage, and aging. Plant-derived products having skin-protective effects are well-known traditionally. Triphala, a formulation of three fruit products, is one of the most important rasayana drugs used in Ayurveda. Several skin care products based on Triphala are available that claim its protective effects on facial skin. However, the skin protective effects of Triphala extract (TE) and its mechanistic action on skin cells have not been elucidated in vitro. Gallic acid, ellagic acid, and chebulinic acid were deduced by LC-MS as the major constituents of TE. The identified key compounds were docked with skin-related proteins to predict their binding affinity. The IC50 values for TE on human dermal fibroblasts (HDF) and human keratinocytes (HaCaT) were 204.90 ± 7.6 and 239.13 ± 4.3 μg/mL respectively. The antioxidant capacity of TE was 481.33 ± 1.5 mM Trolox equivalents in HaCaT cells. Triphala extract inhibited hydrogen peroxide (H2O2) induced RBC haemolysis (IC50 64.95 μg/mL), nitric oxide production by 48.62 ± 2.2%, and showed high reducing power activity. TE also rescued HDF from H2O2-induced damage; inhibited H2O2 induced cellular senescence and protected HDF from DNA damage. TE increased collagen-I, involucrin and filaggrin synthesis by 70.72 ± 2.3%, 67.61 ± 2.1% and 51.91 ± 3.5% in HDF or HaCaT cells respectively. TE also exhibited anti-tyrosinase and melanin inhibition properties in a dose-dependent manner. TE increased the mRNA expression of collagen-I, elastin, superoxide dismutase (SOD-2), aquaporin-3 (AQP-3), filaggrin, involucrin, transglutaminase in HDF or HaCaT cells, and decreased the mRNA levels of tyrosinase in B16F10 cells. Thus, Triphala exhibits protective benefits on skin cells in vitro and can be used as a potential ingredient in skin care formulations.

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Section: Resultsmentioning

confidence: 99%

Protective Effects of Triphala on Dermal Fibroblasts and Human Keratinocytes

Varma¹,

Sivaprakasam²,

Mishra³

et al. 2016

PLoS ONE

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“…Sakuranetin is the major flavonoid found in rice [45] and it has been primarily studied for its anti-inflammatory [46], anti-diabetic [47], and anti-bacterial [48] properties. Rhamnetin is found in most buckthorns (rhamnus genus) [49] and has been primarily studied for its anti-cancer [50], antioxidant [51] and anti-inflammatory properties [41]. Thus, both rhamnetin and sakuranetin have been found to be anti-inflammatory.…”

Section: Discussionmentioning

confidence: 99%

A nicotinic receptor-mediated anti-inflammatory effect of the flavonoid rhamnetin in BV2 microglia

et al. 2014

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The alpha7 nicotinic acetylcholine receptor (nAChR) is a potential target in neuroinflammation. Screening a plant extract library identified Solidago nemoralis as containing methyl-quercetin derivatives that are relatively selective ligands for the alpha7 nAChR. Flavonoids are not known for this activity, so we screened a small library of pure flavonoids to confirm our findings. Some flavonoids, e.g. rhamnetin, displaced a selective alpha7 nAChR radioligand from rat brain membranes whereas similar structures e.g. sakuranetin, did not. To evaluate the contribution of this putative nAChR activity to the known anti-inflammatory properties of these flavonoids, we compared their effects on lipopolysaccharide induced release of inflammatory mediators from BV2 microglia. Both rhamnetin and sakuranetin reduced mediator release, but differed in potency (rhamnetin>sakuranetin) and the Hill slope of their concentration response curves. For rhamnetin the Hill coefficient was >3.0 whereas for sakuranetin the coefficient was 1.0, suggesting that effects of rhamnetin are mediated through more than one mechanism, whereas sakuranetin has a single mechanism. nACHR antagonists decreased the Hill coefficient for rhamnetin toward unity, which suggests that a nAChR-mediated mechanism contributes cooperatively to its overall anti-inflammatory effect. In contrast nAChR antagonists had no effect on the potency or Hill coefficient for sakuranetin, but a concentration of nicotine (1μM) that had no effect alone, significantly increased the Hill coefficient of this flavonoid. In conclusion, the anti-inflammatory effects of rhamnetin benefit cooperatively from a nAChR-mediated mechanism. This action, together with potent free radical scavenging activity, suggests that flavonoids with alpha7 nAChR activity have therapeutic potential in neuroinflammatory conditions.

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“…It exhibited significant cytotoxicity against HeLa cells [35]. Astragalin was shown to be cytotoxic to cultured human hepatocellular carcinoma HepG2 cells, but not human breast cancer cell line MCF-7 [57]. It also decreased cell viability and increased apoptosis of cultured human lung cancer cell lines (A549 and H1299), but not the normal (BEAS-2B) lung cells [58].…”

Section: Bioactive Compounds In Beetrootmentioning

confidence: 99%

Red Beetroot and Betalains as Cancer Chemopreventative Agents

Lechner

Stoner

2019

Molecules

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Carcinogenesis is the process whereby a normal cell is transformed into a neoplastic cell. This action involves several steps starting with initiation and followed by promotion and progression. Driving these stages are oxidative stress and inflammation, which in turn encompasses a myriad of aberrant gene expressions, both within the transforming cell population and the cells within the surrounding lesion. Chemoprevention of cancer with bioreactive foods or their extracted/purified components occurs via normalizing these inappropriate gene activities. Various foods/agents have been shown to affect different gene expressions. In this review, we discuss whereby the chemoprevention activities of the red beetroot itself may disrupt carcinogenesis and the activities of the water-soluble betalains extracted from the plant.

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Rhamnetin Attenuates Melanogenesis by Suppressing Oxidative Stress and Pro-inflammatory Mediators

Abstract: Rhamnetin is a naturally occurring polyphenolic compound. In this report, experimental evidence is presented on the suppression of melanogenesis by rhamnetin using B16 murine melanoma cells (

Cited by 27 publications

References 33 publications

Protective Effects of Triphala on Dermal Fibroblasts and Human Keratinocytes

Protective Effects of Triphala on Dermal Fibroblasts and Human Keratinocytes

A nicotinic receptor-mediated anti-inflammatory effect of the flavonoid rhamnetin in BV2 microglia

Red Beetroot and Betalains as Cancer Chemopreventative Agents

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