Comparison among Activities and Isoflavonoids from Pueraria thunbergiana Aerial Parts and Root.

: Kudzu (Pueraria thunbergiana Benth.) has long been used as a food and medicine for many centuries. The root is the most commonly used portion of the plant, but the aerial parts are occasionally used as well. In this study, we investigated the constituent compounds and biological activities of the aerial parts, leaves, stems, and sprouts, and compared their constituents and activities with those of roots. Leaf extract showed a significantly higher TPC level at 59 ± 1.6 mg/g and lower free radical scavenging (FRS) values under 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), and NO inhibition at 437 ± 11, 121 ± 6.6 µg/mL and 107 ± 4.9 µg/mL, respectively, than those of sprout, stem, and root extract. Leaf extract also significantly suppressed lipopolysaccharide (LPS)-mediated gene expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). The main components of leaf extract were found to be genistin and daidzin. This study suggests that the leaves of kudzu are a good source of biological activities and isoflavones that can be used in functional or medicinal foods and cosmetics for the prevention or treatment of diseases related to inflammation and oxidative stress.

CopA3 peptide prevents ultraviolet-induced inhibition of type-I procollagen and induction of matrix metalloproteinase-1 in human skin fibroblasts.

Ultraviolet (UV) exposure is well-known to induce premature aging, which is mediated by matrix metalloproteinase-1 (MMP-1) activity. A 9-mer peptide, CopA3 (CopA3) was synthesized from a natural peptide, coprisin, which is isolated from the dung beetle Copris tripartitus. As part of our continuing search for novel bioactive natural products, CopA3 was investigated for its in vitro anti-skin photoaging activity. UV-induced inhibition of type-I procollagen and induction of MMP-1 were partially prevented in human skin fibroblasts by CopA3 peptide in a dose-dependent manner. At a concentration of 25 µM, CopA3 nearly completely inhibited MMP-1 expression. These results suggest that CopA3, an insect peptide, is a potential candidate for the prevention and treatment of skin aging.

The elastase and melanogenesis inhibitory and anti-inflammatory activities of phosvitin phosphopeptides produced using high-temperature and mild-pressure (HTMP) pretreatment and enzyme hydrolysis combinations.

This study aimed to determine the skin protective effect of egg yolk phosvitin phosphopeptides (PPPs). Phosvitin was separated from the egg yolk, and PPPs were produced using high-temperature and mild-pressure (HTMP) pretreatment and enzyme-sterilization hydrolysis combinations. The elastase and melanogenesis inhibitory activities and anti-inflammatory effects of egg yolk PPPs were determined. All PPPs significantly inhibited elastase activity, but the PPPs prepared with HTMP pretreatment and trypsin-sterilization (HTMP-T-S) combination suppressed the tyrosinase activity the most. PPPs (3 mg/mL) inhibited the α-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells by 31.18 to 38.58%. In addition, PPPs effectively inhibited nitric oxide (NO) production in the LPS (lipopolysaccharide)-stimulated RAW 264.7 macrophages, and the PPPs from HTMP-T-S exhibited the highest inhibitory activity. The protein expressions of pro-inflammatory enzymes, inducible nitric oxide synthase, and cyclooxygenase-2 were down-regulated by the PPPs from the HTMP-T-S. Therefore, PPPs could be used as an anti-melanogenic, anti-elastase, and anti-inflammatory agent for humans and skin care products.

Potential effect of compounds isolated from Coffea arabica against UV-B induced skin damage by protecting fibroblast cells.

Ultraviolet (UV) radiation has adverse effects on extracellular matrix (ECM) proteins, leading to formation of wrinkles a hallmark of premature skin aging. The adverse effects of UV radiation are associated with induction of matrix metalloproteinases (MMPs) expression and degradation of collagen and elastin. The present study investigated anti-wrinkle effects of chlorogenic acid (CGA), pyrocatechol (PC) and 3,4,5-tricaffeoyl quinic acid (TCQ), isolated from beans of Coffea arabica, against UV-B stimulated mouse fibroblast cells (CCRF) by measuring expression levels of MMP-1, 3, 9, and type-I procollagen. The three compounds were isolated and purified from coffee grounds using column chromatography and structural examination was evaluated by nuclear magnetic resonance (NMR) analysis. Among the three isolated compounds, CGA effectively suppressed the expression of the MMP-1, 3, and 9 and increased synthesis of type-I procollagen as compared UV-B-stimulated CCRF cells. In addition, CGA dose-dependently inhibited intracellular reactive oxygen species (ROS) production in CCRF cells stimulated by UV radiation. Moreover, CGA displayed a good sun protection factor (SPF) and in vitro DNA damage protection together with inhibition of enzyme xanthine oxidase. The enzyme inhibitory kinetic behavior of CGA was determined by Lineweaver-Burk plot, displayed a mixed type enzyme inhibition with 260.3±4.5µM, Ki value. The results indicate that CGA has potential to be used as a preventive agent against premature skin aging induced by UV radiation.

Anti-Inflammatory Activity of Pinus koraiensis Cone Bark Extracts Prepared by Micro-Wave Assisted Extraction.

In this study, we compared the anti-inflammatory activity of Pinus koraiensis cone bark extracts prepared by conventional extraction and microwave-assisted extraction (MAE). Water extracts and 50% ethanol extracts prepared using MAE were applied to RAW 264.7 cell at 5, 10, 25, and 50 µg/mL of concentrations, and tested for cytoxicity. The group treated with 50 µg/mL of 50% ethanol extracts showed toxicity. In order to investigate the inhibition of nitric oxide (NO) production in RAW 264.7 cells, extracts of water and ethanol were treated with 5, 10, and 25 µg/mL concentrations. The inhibitory activity of water and 50% ethanol extracts groups were determined as 40% and 60% at 25 µg/mL concentration, respectively. We found concentration dependent decreases on inducible NO synthase. The inhibitory effect against forming inflammatory cytokines, prostaglandin E2, tumor necrosis factor-α, interleukin (IL)-6, and IL-1ß, was also superior in the 25 µg/mL treated group than the control group. According to these results, the water extracts and 50% ethanol extracts both inhibited inflammatory mediators by reducing the inflammatory response. Therefore, The MAE extracts of P. koraiensis cone bark can be developed as a functional ingredient with anti-inflammatory activity.

Anti-inflammatory Potential of Quercetin-3-O-ß-D-("2"-galloyl)-glucopyranoside and Quercetin Isolated from Diospyros kaki calyx via Suppression of MAP Signaling Molecules in LPS-induced RAW 264.7 Macrophages.

Diospyros kaki (DK) contains an abundance of flavonoids and has been used in folk medicine in Korea for centuries. Here, we report for the first time the anti-inflammatory activities of Quercetin (QCT) and Quercetin 3-O-ß-("2"-galloyl)-glucopyranoside (Q32G) isolated from DK. We have determine the no cytotoxicity of Q32G and QCT against RAW 264.7 cells up to concentration of 50 µM. QCT and Q32G demonstrated potent anti-inflammatory activities by reducing expression of nitric oxide (NO), tumor necrosis factor (TNF)-α, interleukin (IL)-1ß, IL-6 inducible NO synthase (iNOS), cyclooxygenase (COX)-2, and mitogen-activated protein kinase (MAPKs) in mouse RAW 264.7 macrophages activated with lipopolysaccharide (LPS). Both QCT or Q32G could decrease cellular protein levels of COX-2 and iNOS as well as secreted protein levels of NO, PGE2 , and cytokines (TNF-α, IL-1ß, and IL-6) in culture medium of LPS-stimulated RAW 264.7 macrophages. Immunoblot analysis showed that QCT and Q32G suppressed LPS-induced MAP kinase pathway proteins p-p38, ERK, and JNK. This study revealed that QCT and Q32G have anti-inflammatory potential, however Q32G possess comparable activity as that of QCT and could be use as adjuvant to treat inflammatory diseases.

Physiological activity of irradiated green tea polyphenol on the human skin.

Physiological activity of irradiated green tea polyphenol on the human skin was investigated for further industrial application. The green tea polyphenol was separated and irradiated at 40 kGy by y-ray. For an anti-wrinkle effect, the collagenase inhibition effect was higher in the irradiated sample (65.3%) than that of the non-irradiated control (56.8%) at 200 ppm of the concentration (p < 0.05). Collagen biosynthesis rates using a human fibroblast were 19.4% and 16.3% in the irradiated and the non-irradiated polyphenols, respectively. The tyrosinase inhibition effect, which is related to the skin-whitening effect, showed a 45.2% and 42.9% in the irradiated and the non-irradiated polyphenols, respectively, at a 100 ppm level. A higher than 90% growth inhibition on skin cancer cells (SK-MEL-2 and G361) was demonstrated in both the irradiated and the non-irradiated polyphenols. Thus, the irradiation of green tea polyphenol did not change and even increased its anti-wrinkle, skin-whitening and anticancer effects on the human skin. The results indicated that irradiated green tea polyphenol can be used as a natural ingredient with excellent physiological functions for the human skin through cosmetic or food composition.

Quercetin-3-O-ß-d-glucopyranosyl-(1 → 6)-ß-d-glucopyranoside suppresses melanin synthesis by augmenting p38 MAPK and CREB signaling pathways and subsequent cAMP down-regulation in murine melanoma cells.

In this study, the effect of purified quercetin-3-O-ß-d-glucopyranosyl-(1 â†’ 6)-ß-d-glucopyranosid (QCGG) on melanogenesis was investigated. QCGG was isolated from the calyx of a traditional Korean medicinal herb, Persimmon (Diospyros kaki). The hypopigmentation effects of QCGG were determined by examination of cellular melanin contents, tyrosinase activity assay, cAMP assay, and Western blotting of α-MSH-stimulated B16F10 mouse melanoma cells. Our results showed that QCGG inhibited both melanin synthesis and tyrosinase activity in a concentration-dependent manner as well as significantly reduced the expression of melanogenic proteins such as microphthalmia-associated transcription factor (MITF), tyrosinase-related protein-1, tyrosinase-related protein-2, and tyrosinase. Moreover, QCGG inhibited intracellular cAMP levels, cAMP response element-binding protein (CREB), and p38 MAPK expression in α-MSH-stimulated B16F10 cells. Taken together, the suppressive effects of QCGG on melanogenesis may involve down-regulation of MITF and its downstream signaling pathway via phosphorylation of p38 MAPK and CREB along with reduced cAMP levels. These results indicate that QCGG reduced melanin synthesis by reducing expression of tyrosine and tyrosine-related proteins via extracellular signal-related protein kinase (ERK) activation, followed by down-regulation of CREB, p38, and MITF.

Inhibition of enzyme activities and the antiwrinkle effect of polyphenol isolated from the persimmon leaf (Diospyros kaki folium) on human skin.

BACKGROUND: Many studies have been conducted to find a natural material that has high biologic functions for human skin without any side effects. Persimmon leaf has a substantial amount of tannins in different forms; therefore, it was selected as a target material. OBJECTIVE: The biosynthesis rate of the collagen was also investigated to clarify the beneficial functions for the human skin. METHODS: Persimmon leaves were obtained, extracted with 80% ethanol, and isolated into PFs I, II, and III after column chromatography using a Sephadex LH-20 column followed by thin-layer chromatography. RESULTS: The xanthine oxidase inhibition effect of both PFs II and III was over 40% at a 100 ppm concentration. PF II, containing higher flavonoids levels, had a significantly higher tyrosinase inhibition than that of PF III. Collagenase inhibition was 16.3 and 8.1% for PF III and PF II, respectively, at 100 ppm. On the other hand, elastase inhibition activity was significantly higher in PF II than PF III. Collagen biosynthesis rates of PF III were over 25% from a 1 to 10 ppm concentration. Consequently, PFs isolated from the persimmon leaf can be used as natural materials or additives for human skin owing to their beneficial biologic functions, including the antiwrinkle effect and the inhibition of skin problems, for food or cosmetic compositions.