Search

Bioactive peptides (BPs) are protein fragments that benefit human health. To assess whether leftover green tea residues (GTRs) can serve as a resource for new BPs, we performed in silico proteolysis of GTRs using the BIOPEP database, revealing a wide range of BPs embedded in GTRs. Comparative genomics and the percentage of conserved protein analyses enabled us to select a few probiotic strains for GTR hydrolysis. The selected probiotics digested GTRs anaerobically to yield GTR-derived peptide fractions. To examine whether green tea (GT) peptide fractions could be potential mediators of host-microbe interactions, we comprehensively screened agonistic and antagonistic activities of 168 human G protein-coupled receptors (GPCRs). NanoLC-MS/MS analysis and thin-layer chromatography allowed the identification of peptide sequences and the composition of glycan moieties in the GTRs. Remarkably, GT peptide fractions produced by Lactiplantibacillus plantarum APsulloc 331261, a strain isolated from GT, showed a potent-binding activity for P2RY6, a GPCR involved in intestinal homeostasis. Therefore, this study suggests the potential use of probiotics-aided GTR hydrolysates as postbiotic BPs, providing a biological process for recycling GTRs from agro-waste into renewable resources as health-promoting BPs.

Background In aged skin, reactive oxygen species (ROS) induces degradation of the extracellular matrix (ECM), leading to visible aging signs. Collagens in the ECM are cleaved by matrix metalloproteinases (MMPs). Syringaresinol (SYR), isolated from Panax ginseng berry, has various physiological activities, including anti-inflammatory action. However, the anti-aging effects of SYR via antioxidant and autophagy regulation have not been elucidated. Methods The preventive effect of SYR on skin aging was investigated in human HaCaT keratinocytes in the presence of H2O2, and the keratinocyte cells were treated with SYR (0–200 μg/mL). mRNA and protein levels of MMP-2 and -9 were determined by real-time PCR and Western blotting, respectively. Radical scavenging activity was researched by 2,2 diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. LC3B level was assessed by Western blotting and confocal microscopy. Results SYR significantly reduced gene expression and protein levels of MMP-9 and -2 in both H2O2-treated and untreated HaCaT cells. SYR did not show cytotoxicity to HaCaT cells. SYR exhibited DPPH and ABTS radical scavenging activities with an EC50 value of 10.77 and 10.35 μg/mL, respectively. SYR elevated total levels of endogenous and exogenous LC3B in H2O2-stimulated HaCaT cells. 3-Methyladenine (3-MA), an autophagy inhibitor, counteracted the inhibitory effect of SYR on MMP-2 expression. Conclusion SYR showed antioxidant activity and up-regulated autophagy activity in H2O2-stimulated HaCaT cells, lowering the expression of MMP-2 and MMP-9 associated with skin aging. Our results suggest that SYR has potential value as a cosmetic additive for prevention of skin aging.

The purpose of the current study was to investigate the effect of various characterized green tea extracts (GTEs) according to extraction methods on enzymatic starch hydrolysis and intestinal glucose transport. Codigestion of wheat starch with water extract (WGT) or ethanol extract formulated with green tea polysaccharides and flavonols (CATEPLUS) produced 3.4-3.5 times higher resistant starch (RS) than wheat starch only. Its microstructures were changed to spherical shapes and smooth surfaces as shown by scanning electron microscopy (SEM) results. According to Fourier transform infrared (FT-IR) spectra, the absorption peak of O-H stretching was red-shifted in WGT or CATEPLUS. The results confirmed that hydrogen bonds were formed between starch granules and polysaccharides in WGT or CATEPLUS. Intestinal glucose transport subsequently measured after in vitro digestion was mostly suppressed in CATEPLUS. Gene expression of the glucose transporter protein, particularly SGLT1, was significantly inhibited by addition of CATEPLUS (

The purpose of the current study was to investigate the effect of green tea ethanol extract (GTE) and polysaccharide fractions from green tea (PFGs) on the hydrolysis of wheat starch, microstructural changes, and intestinal transport of glucose. The amount of resistant starch (RS) was significantly lowered in the water-soluble polysaccharide (WSP), water-soluble polysaccharide-pectinase (WSP-P), and water-insoluble polysaccharide-alkali soluble (WISP-Alk-Soluble; p < 0.05). The microstructures of gelatinized wheat starch granules with WSP, WSP-P, and WISP-Alk-Soluble were spherical with small cracks. The amount of intestinal transported glucose from digested wheat starch was 2.12-3.50 times lower than the control group. The results from the current study suggest that water- and alkali-soluble PFGs could be potential ingredients to lower starch hydrolysis as well as to control the postprandial blood glucose level when foods that contain starch are consumed.

Skin aging is a major risk factor for the dermal diseases, and interventions to attenuate cellular senescence are expected to reduce the risk for age-related diseases involving skin atrophy. However, blocking cell death or extending proliferation causally results in side effects and an increased cancer risk. For identification of a safer approach, we focused on PDK1 inhibition, which could revert cellular senescence and reduce senescence factors in skin in vitro, in a human skin equivalent model and in an exploratory, placebo-controlled, interventional trial. Natural phytochemical kaempferol tetrasaccharides resulted in a significant reduction in cellular senescence, and an increase in collagen fiber was observed in the skin cell and human skin equivalent. Clinical enhancement in skin appearance was noted in multiple participants, and an immunohistochemical study revealed improvement in the histological appearance of skin tissue and extracellular matrix. This change was associated with relative improvement in histological markers of senescence and clinical appearance of the aged skin and an increase in collagen fiber, an essential factor for preventing skin atrophy and consistency of the basement membrane. These results indicate that PDK1 inhibition is a potentially effective antiaging intervention, suggesting a diagnostic role and preventive actions of PDK1 in senescence-associated skin atrophy.

Background: Panax ginseng Meyer (Araliaceae) is a highly valued medicinal plant in Asian regions, especially in Korea, China, and Japan. Chemical and biological studies on P. ginseng have focused primarily on its roots, whereas the seeds remain poorly understood. This study explores the phytochemical and biological properties of compounds from P. ginseng seeds. Methods: P. ginseng seeds were extracted with methanol, and 16 compounds were isolated using various chromatographic methods. The chemical structures of the isolates were determined by spectroscopic data. Antiinflammatory activities were evaluated for triterpene and steroidal saponins using lipopolysaccharide-stimulated RAW264.7 macrophages and THP-1 monocyte leukemia cells. Results: Phytochemical investigation of P. ginseng seeds led to the isolation of a novel triterpene saponin, pseudoginsenoside RT8, along with 15 known compounds. Pseudoginsenoside RT8 exhibited more potent antiinflammatory activity than the other saponins, attenuating lipopolysaccharide-mediated induction of proinflammatory genes such as interleukin-1β, interleukin-6, inducible nitric oxide synthase, cyclooxygenase-2, and matrix metalloproteinase-9, and suppressed reactive oxygen species and nitric oxide generation in a dose-dependent manner. Conclusion: These findings indicate that pseudoginsenoside RT8 has a pharmaceutical potential as an antiinflammatory agent and that P. ginseng seeds are a good natural source for discovering novel bioactive molecules. Keywords: Antiinflammatory activity, Panax ginseng seeds, Pseudoginsenoside RT8

Plant exosomes are nanosized (30–150 nm) membrane vesicles that contain biomolecules and influence the development of a plant and protect the plant from pathogens. Recently, plant exosomes are in the spotlight as a new biologically active substance. However, whether plant exosomes have similar efficacy to conventional secondary metabolites of plants is unknown. In this study, the difference in efficacy between plant exosomes and conventional secondary metabolites was analyzed with three or four types of plant extracts, including ginseng (Panax ginseng) and green tea (Camellia sinensis). After 6 h of treatment, the analysis of gene expression pattern of each sample showed that the exosome treatment group and the extract treatment group were clearly distinguished. After selecting the genes that showed differential expression of > twofold change, the number of genes that were up- or downregulated appeared to be 398 or 438 for the extract and 861 or 648 for the exosome, on average. This suggests that the change in transcriptome is more expressed in the exosome treatment group than in the extract treatment group. In addition, in the comparative analysis of expression of genes that are known to affect aging, regeneration, skin barrier, and moisturization—MMP12, MMP13, NOTCH3, FGF12, HS3ST3A1, LOX, VIM, ELOVL3, and KRTI—the exosome treatment group was predicted to more effectively contribute to maintaining a healthy skin when compared to the extract treatment group. The number of genes that were identified to specifically react to the Panax ginseng or Camellia sinensis treatment group during the transcriptome change phase was 11 and 8, respectively. This suggests that exosomes bear its specific effect according to the plant it is derived from. In conclusion, the results of this study indicate that plant exosomes, as natural biologically active substances, have different effects from conventional plant extracts, and have the potential to be commercialized as a cosmeceutical product.

Caragana rosea Turcz, which belongs to the Leguminosae family, is a small shrub found in Northern and Eastern China that is known to possess anti-inflammatory properties and is used to treat fever, asthma, and cough. However, the underlying molecular mechanisms of its anti-inflammatory effects are unknown. Therefore, we used lipopolysaccharide (LPS) in RAW264.7 macrophages to investigate the molecular mechanisms that underlie the anti-inflammatory activities of a methanol extract of Caragana rosea (Cr-ME). We showed that Cr-ME reduced the production of nitric oxide (NO) and mRNA levels of iNOS, TNF-α, and IL-6 in a concentration-dependent manner. We also found that Cr-ME blocked MyD88- and TBK1-induced NF-κB and IRF3 promoter activity, suggesting that it affects multiple targets. Moreover, Cr-ME reduced the phosphorylation levels of IκBα, IKKα/β and IRF3 in a time-dependent manner and regulated the upstream NF-κB proteins Syk and Src, and the IRF3 protein TBK1. Upon overexpression of Src and TBK1, Cr-ME stimulation attenuated the phosphorylation of the NF-κB subunits p50 and p65 and IRF3 signaling. Together, our results suggest that the anti-inflammatory activity of Cr-ME occurs by inhibiting the NF-κB and IRF3 signaling pathways.

Several Cissus species have been used and reported to possess medicinal benefits. However, the anti-inflammatory mechanisms of Cissus subtetragona have not been described. In this study, we examined the potential anti-inflammatory effects of C. subtetragona ethanol extract (Cs-EE) in vitro and in vivo, and investigated its molecular mechanism as well as its flavonoid content. Lipopolysaccharide (LPS)-induced macrophage-like RAW264.7 cells and primary macrophages as well as LPS-induced acute lung injury (ALI) and HCl/EtOH-induced acute gastritis mouse models were utilized. Luciferase assays, immunoblotting analyses, overexpression strategies, and cellular thermal shift assay (CETSA) were performed to identify the molecular mechanisms and targets of Cs-EE. Cs-EE concentration-dependently reduced the secretion of NO and PGE2, inhibited the expression of inflammation-related cytokines in LPS-induced RAW264.7 cells, and decreased NF-κB- and AP-1-luciferase activity. Subsequently, we determined that Cs-EE decreased the phosphorylation events of NF-κB and AP-1 pathways. Cs-EE treatment also significantly ameliorated the inflammatory symptoms of HCl/EtOH-induced acute gastritis and LPS-induced ALI mouse models. Overexpression of HA-Src and HA-TAK1 along with CETSA experiments validated that inhibited inflammatory responses are the outcome of attenuation of Src and TAK1 activation. Taken together, these findings suggest that Cs-EE could be utilized as an anti-inflammatory remedy especially targeting against gastritis and acute lung injury by attenuating the activities of Src and TAK1.

There is a growing need to develop anti-inflammatory drugs to regulate inflammatory responses. An extract of Huberia peruviana Cogn. had the best inhibitory effect on nitric oxide (NO) production in screening process undertaken in our laboratory. However, the anti-inflammatory effect of Huberia peruviana Cogn. methanol extract (Hp-ME) has not been studied. In this study, the anti-inflammatory effect of Hp-ME was assessed by using an NO assay, RT-PCR, luciferase reporter gene activity assay, western blotting assay, HCl/EtOH-induced acute gastritis model, and LPS-induced acute lung injury model. The phytochemical components of Hp-ME were determined through LC-MS/MS analysis. When RAW264.7 and HEK293T cells were treated with Hp-ME, NO production was decreased dose-dependently without cytotoxicity and the mRNA levels of iNOS, COX-2, and TNF-α were decreased. In a luciferase assay, the activity of transcription factors, NF-κB in TRIF or MyD88-overexpressing HEK293T cells was extremely reduced by Hp-ME. The western blotting analysis indicated that Hp-ME has anti-inflammatory effects by inhibiting the phosphorylation of Src. Hp-ME showed anti-inflammatory effects on in vivo models of HCl/EtOH-induced gastritis and LPS-induced acute lung injury. LC-MS/MS revealed that Hp-ME contains several anti-inflammatory flavonoids. The final findings of this study imply that Hp-ME could be used as an anti-inflammatory drug in several inflammatory diseases.

Particulate matter 2.5 (PM2.5), an atmospheric pollutant with an aerodynamic diameter of

Theasinensin A (TSA) is a major group of catechin dimers mainly found in oolong tea and black tea. This compound is also manufactured with epigallocatechin gallate (EGCG) as a substrate and is refined after the enzyme reaction. In previous studies, TSA has been reported to be effective against inflammation. However, the effect of these substances on skin melanin formation remains unknown. In this study, we unraveled the role of TSA in melanogenesis using mouse melanoma B16F10 cells and normal human epidermal melanocytes (NHEMs) through reverse transcription polymerase chain reaction (RT-PCR), Western blotting analysis, luciferase reporter assay, and enzyme-linked immunosorbent assay analysis. TSA inhibited melanin formation and secretion in α-melanocyte stimulating hormone (α-MSH)-induced B16F10 cells and NHEMs. TSA down-regulated the mRNA expression of tyrosinase (Tyr), tyrosinase-related protein 1 (Tyrp1), and Tyrp2, which are all related to melanin formation in these cells. TSA was able to suppress the activities of certain proteins in the melanocortin 1 receptor (MC1R) signaling pathway associated with melanin synthesis in B16F10 cells: cyclic adenosine monophosphate (cAMP) response element-binding protein (CREB), protein kinase A (PKA), tyrosinase, and microphthalmia-associated transcription factor (MITF). We also confirmed α-MSH-mediated CREB activities through a luciferase reporter assay, and that the quantities of cAMP were reduced by TSA in the enzyme linked immunosorbent assay (ELISA) results. Based on these findings, TSA should be considered an effective inhibitor of hyperpigmentation.

In aged skin, reactive oxygen species (ROS) induces degradation of the extracellular matrix (ECM), leading to visible aging signs. Collagens in the ECM are cleaved by matrix metalloproteinases (MMPs). Syringaresinol (SYR), isolated fromThe preventive effect of SYR on skin aging was investigated in human HaCaT keratinocytes in the presence of HSYR significantly reduced gene expression and protein levels of MMP-9 and -2 in both HSYR showed antioxidant activity and up-regulated autophagy activity in H

Background Cocculus hirsutus (L.) W. Thedo., a traditionally well-known plant, has confirmed antitumor properties as well as acute and chronic diuretic effects. However, little is known about its inflammatory activities and the potential effect on inflammatory disease treatment. Purpose Our aim in this study was to explore additional beneficial properties of C. hirsutus ethanol extract (Ch-EE) such as anti-inflammatory activity in vitro and in vivo as well as its underlying mechanisms and to provide a theoretical basis for its role as a candidate natural drug in clinical gastritis and lung disease therapy. Study Design RAW264.7 cells, HEK293T cells, peritoneal macrophages, and mouse models of acute gastritis and acute lung injury were used to assess the anti-inflammatory activity of Ch-EE. Methods Decreases in LPS-induced nitric oxide (NO) production and cytokine expression by RAW264.7 cells after Ch-EE treatment were evaluated by Griess assays and PCR, respectively. Transcription factor activity was assessed through luciferase reporter gene assay, and protein expression was determined by Western blotting analysis. Overexpression assays and cellular thermal shift assays were executed in HEK293T cells. Our two in vivo models were an HCl/EtOH-induced gastritis model and an LPS-induced lung injury model. Changes in stomach lesions, lung edema, and lung histology were examined upon treatment with Ch-EE. Components of Ch-EE were determined by liquid chromatography-mass spectrometry. Results LPS-induced nitric oxide production and Pam3CSK4- and L-NAME-induced NO production were inhibited by Ch-EE treatment of RAW264.7 cells. Furthermore, LPS-induced increases in transcript levels of iNOS, COX2, CCL12, and IL-1β were reduced by Ch-EE treatment. Ch-EE decreased both MyD88- and TRIF-induced NF-κB promotor activity. Proteins upstream of NF-κB, namely p-p50, p-p65, p-IκBα, p-AKT1, p-Src, and p-Syk, were all downregulated by Ch-EE. Moreover, Src and Syk were targets of Ch-EE. Ch-EE treatment reduced the size of inflammatory stomach lesions induced by HCl/EtOH, lung edema, and accumulation of activated neutrophils caused by LPS. Conclusions These results strongly suggest that Cocculus hirsutus can be developed as a promising anti-inflammatory remedy with Src- and Syk-inhibitory functions targeting diseases related to gastritis and lung injury.

Green tea is reported to exert beneficial effects on metabolic disorders through the regulation of lipid metabolism. On the contrary, fermented food products have been introduced to improve human health by modulating immune response and energy metabolism. To maximize health benefit, we applied fermentation processing to green tea. Fermented green tea extract (FGT) inhibited adipogenesis and lipogenesis in cultured adipocytes, whereas it augmented mRNA expression of fatty acid oxidation-related genes in differentiated myocytes. In diet-induced obese mice, FGT blunted body weight and fat mass gain by 69.7% and 56.7%, respectively. FGT also improved circulating triglyceride concentrations by 32.6%. Similar to in vitro results, FGT suppressed lipogenesis and promoted lipid catabolism in peripheral tissues. In addition, FGT administration modulated the composition of certain gut microbiota which are associated with obesity and related metabolic disorders. Among the various components of FGT, gallocatechin gallate is suggested to mediate the effect of FGT on lipid metabolism. Taken together, we propose FGT as a novel functional food to benefit human health by controlling adiposity and lipid metabolism.

Precise measurement of particulate matter (PM) on skin is important for managing and preventing PM-related skin diseases. This study aims to directly visualize the deposition and penetration of PM into human skin using a multimodal nonlinear optical (MNLO) imaging system. We successfully obtained PM particle signals by merging two different sources, C–C vibrational frequency and autofluorescence, while simultaneously visualizing the anatomical features of the skin via keratin, collagen, and elastin. As a result, we found morphologically dependent PM deposition, as well as increased deposition following disruption of the skin barrier via tape-stripping. Furthermore, PM penetrated more and deeper into the skin with an increase in the number of tape-strippings, causing a significant increase in the secretion of pro-inflammatory cytokines. Our results suggest that MNLO imaging could be a useful technique for visualizing and quantifying the spatial distribution of PM in ex vivo human skin tissues.

The purpose of the current study was to examine the effect of adding secondary ingredients such as green tea derived water-soluble polysaccharides (GTP) and flavonol aglycone rich fractions derived from cellulase treated green tea extract (FVN) into catechin rich green tea extracts (GTE) on wheat starch digestion and intestinal glucose transport using in vitro digestion with Caco-2 cells. Co-digestion of wheat starch with GTE (16.88 g L(−1)) or GTE + GTP + FVN (16.69 g L(−1)) appeared to promote starch hydrolysis compared to control (15.49 g L(−1)). In case of major flavonoids, addition of epigallocatechin gallate (EGCG), EGCG + myricetin (M) into wheat starch significantly increased the digestion of starch into glucose. Glucose transport rate decreased by 22.35% in wheat starch + GTE + GTP + FVN (1.39%), while the least amount of glucose (1.70%) was transported in EGCG mixed with M (1% of EGCG) as secondary ingredients among individual flavonoids formulation. It indicated that inhibitory effect on glucose transport was higher in addition of GTE, GTP, and FVN as excipients ingredients rather than targeted major flavonoids. Results from the current study suggest that whole green tea including flavonoid rich fractions could enhance hypoglycemic potential of GTE. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s13197-021-05140-2.

Ethnopharmacological relevance Melicope accedens (Blume) Thomas G. Hartley is a plant included in the family Rutaceae and genus Melicope. It is a native plant from Vietnam that has been used for ethnopharmacology. In Indonesia and Malaysia, the leaves of M. accedens are applied externally to decrease fever. Aim of the study The molecular mechanisms of the anti-inflammatory properties of M. accedens are not yet understood. Therefore, we examined those mechanisms using a methanol extract of M. accedens (Ma-ME) and determined the target molecule in macrophages. Materials and methods We evaluated the anti-inflammatory effects of Ma-ME in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and in an HCl/EtOH-triggered gastritis model in mice. To investigate the anti-inflammatory activity, we performed a nitric oxide (NO) production assay and ELISA assay for prostaglandin E2 (PGE2). RT-PCR, luciferase gene reporter assays, western blotting analyses, and a cellular thermal shift assay (CETSA) were conducted to identify the mechanism and target molecule of Ma-ME. The phytochemical composition of Ma-ME was analyzed by HPLC and LC-MS/MS. Results Ma-ME suppressed the production of NO and PGE2 and the mRNA expression of proinflammatory genes (iNOS, IL-1β, and COX-2) in LPS-stimulated RAW264.7 cells without cytotoxicity. Ma-ME inhibited NF-κB activation by suppressing signaling molecules such as IκBα, Akt, Src, and Syk. Moreover, the CETSA assay revealed that Ma-ME binds to Syk, the most upstream molecule in the NF-κB signal pathway. Oral administration of Ma-ME not only alleviated inflammatory lesions, but also reduced the gene expression of IL-1β and p-Syk in mice with HCl/EtOH-induced gastritis. HPLC and LC-MS/MS analyses confirmed that Ma-ME contains various anti-inflammatory flavonoids, including quercetin, daidzein, and nevadensin. Conclusions Ma-ME exhibited anti-inflammatory activities in vitro and in vivo by targeting Syk in the NF-κB signaling pathway. Therefore, we propose that Ma-ME could be used to treat inflammatory diseases such as gastritis.

The outer epidermal skin is a primary barrier that protects the body from extrinsic factors, such as ultraviolet (UV) radiation, chemicals and pollutants. The complete epithelialization of a wound by keratinocytes is essential for restoring the barrier function of the skin. However, age-related alterations predispose the elderly to impaired wound healing. Therefore, wound-healing efficacy could be also considered as a potent function of an anti-aging reagent. Here, we examine the epidermal wound-healing efficacy of the fourth-generation retinoid, seletinoid G, using HaCaT keratinocytes and skin tissues. We found that seletinoid G promoted the proliferation and migration of keratinocytes in scratch assays and time-lapse imaging. It also increased the gene expression levels of several keratinocyte proliferation-regulating factors. In human skin equivalents, seletinoid G accelerated epidermal wound closure, as assessed using optical coherence tomography (OCT) imaging. Moreover, second harmonic generation (SHG) imaging revealed that seletinoid G recovered the reduced dermal collagen deposition seen in ultraviolet B (UVB)-irradiated human skin equivalents. Taken together, these results indicate that seletinoid G protects the skin barrier by accelerating wound healing in the epidermis and by repairing collagen deficiency in the dermis. Thus, seletinoid G could be a potent anti-aging agent for protecting the skin barrier.

It was revealed that excipient ingredients such as flavonols (FVN) or polysaccharides (GTP) which could be derived from green tea enhanced catechin absorption. We hypothesized that the addition of FVN or GTP as excipient ingredients into epicatechin rich green tea extracts (GTE) may improve the health benefits that accompany its consumption. When FVN8.7 (8.7% of GTE, w/w) was added to the GTE (20 mg) as an excipient ingredient, the bioaccessibility and intestinal absorption of total epicatechins was 1.2 and 1.5 times higher than that of only GTE, respectively. This was due to the free radical scavenging capacity of flavonols, showing 114.23 ± 3.07 μmol TE per g for GTE 100 + FVN8.7 and 113.64 ± 1.61 μmol TE per g for GTE 100 + FVN2, respectively. This was significantly higher than the GTE or GTE 100 + OW2 (onion peel and whangchil extracts, 2% of GTE, w/w) which have the same amount of total flavonols. Regarding potential hypoglycemic effects, co-digestion of GTE (20 mg) + green tea polysaccharides (2 mg) + FVN (5 mg) with wheat starch significantly reduced glucose intestinal absorption by 41.85 ± 1.75% compared to only the wheat starch. The results from the current study suggest that whole green tea components rich in flavonols and polysaccharides could be potential hypoglycemic excipient ingredients for green tea catechins.

Increased fat mass, which is induced by the storage of excess nutrients, is considered a causal factor for various metabolic disorders, including insulin resistance, type 2 diabetes, hyperlipidemia, hyperglycemia, hypertension, atherosclerosis, and non-alcoholic fatty liver disease. Therefore, it is necessary to prevent hyperadiposity to sustain a healthy life. Recently, uncoupling proteins (UCPs) were suggested to be molecular targets for curing obesity and its complications. In this study, green satsuma mandarin orange (Citrus unshiu) extract (GME) increased UCP3 expression in cultured myocytes. In a diet-induced obese animal model, administration of GME reduced fat mass and average fat cell size. Similar to in vitro experiments, GME restored expression of UCP3 in skeletal muscle. Moreover, GME also induced UCP2 expression in skeletal muscle. In conclusion, GME is suggested to be a novel functional dietary supplement for adiposity control through induction of UCPs.

The aim of this study was to evaluate the transport of gallocatechin gallate (GCG), catechin gallate (CG) and their metabolites in high-temperature-processed green tea extract (HTP_GTE) from the gastrointestinal tract to blood-brain barrier (BBB) with an in vitro bio-mimic model system with sequential cell cultures including Caco-2, HepG2 and HBMECs. Transports from the GI to BBB, the final concentrations of GCC and CG were 18.95 ± 3.24 μM and 5.11 ± 0.83 μM, respectively. Metabolites detected in BBB after systemic circulation were identified as glucuronide or sulfate conjugated form. Results suggest that GCG, CG and their metabolites in HTP_GTE are capable of reaching the brain by oral intake of HTP_GTE, implying that HTP_GTE could be utilized as a natural functional material for the prevention of degenerative brain diseases.

The current study was investigated the effect of catechin rich green tea extracts (GTE) formulated with excipient components, crude tea polysaccharides (CTP), and flavonols (FVN) derived from green tea on sucrose hydrolysis and intestinal transport of monosaccharides using an in vitro digestion system with Caco-2 cell. Sucrose (10 mg) co-digested with GTE (1 mg) + FVN (0.01 mg) or GTE (1 mg) + CTP (0.1 mg) + FVN (0.01 mg) was less hydrolyzed into glucose and fructose, which showed 90.4 ± 1.36% and 91.75 ± 1.48% for the control (sucrose), respectively. Approximately 65.59% of the glucose released from the sucrose digested with GTE (1 mg) + CTP (0.1 mg) + FVN (0.01 mg) was subsequently transported by Caco-2 cell, which was significantly lower than other treatments (p

It is well known that Panax ginseng (PG) has various pharmacological effects such as anti-aging and anti-inflammation. In a previous study, the authors identified that PG extract induced hair growth by means of a mechanism similar to that of minoxidil. In the present study, the inhibitory effect of PG extract on Dickkopf-1 (DKK-1)-induced catagen-like changes in hair follicles (HFs) was investigated in addition to the underlying mechanism of action. The effects of PG extract on cell proliferation, anti-apoptotic effect, and hair growth were observed using cultured outer root sheath (ORS) keratinocytes and human HFs with or without DKK-1 treatment. The PG extract significantly stimulated proliferation and inhibited apoptosis, respectively, in ORS keratinocytes. PG extract treatment affected the expression of apoptosis-related genes Bcl-2 and Bax. DKK-1 inhibited hair growth, and PG extract dramatically reversed the effect of DKK-1 on ex vivo human hair organ culture. PG extract antagonizes DKK-1-induced catagen-like changes, in part, through the regulation of apoptosis-related gene expression in HFs. These findings suggested that PG extract may reduce hair loss despite the presence of DKK-1, a strong catagen inducer via apoptosis.

BACKGROUND Water soluble polysaccharide derived from green tea (WSP) is produced as byproducts when catechins were extracted from green tea. Although inhibitory effect of green tea catechins on the glucose transport in small intestine has been studied, the hypoglycemic efficacy of the WSP or its combinational effect has not been studied. In order to investigate hypoglycemic efficacy of the WSP or its combinational effect with green tea extract (GTE), co-consumption of GTE and WSP with wheat starch was investigated using in vitro digestion coupled with Caco-2 cells. The mechanism of the intestinal glucose transport was elucidated throughout the gene expression of the intestinal glucose transporters, which included sodium dependent glucose transporter (SGLT1) and glucose transporter 2 (GLUT2), using quantitative real-time polymerase chain reaction (qRT-PCR). RESULTS The co-digestion of wheat starch with GTE during the small intestinal phase was the most rapidly digested into reducing sugar (73.96 g L-1 ) compared to itself (48.44 g L-1 ), WSP (60.35 g L-1 ), and GTE + WSP (61.81 g L-1 ). Intestinal glucose transport was 11.82, 7.59, 4.49, and 2.40% for wheat starch, wheat starch with GTE, WSP, and GTE + WSP, respectively. The highest decreased expression pattern in SGLT1 was observed when cells treated with wheat starch + GTE + WSP (0.66-fold) compared to GTE or WSP treatment. CONCLUSION The results suggested that co-consumption of green tea derived products with wheat starch could delay the intestinal absorption of glucose. Results from the current study suggested that GTE and WSP could be the useful supplements of dietary therapy for hyperglycemia to delay glucose absorption. © 2020 Society of Chemical Industry.

The aim of this study was to profile the bioaccessibility and intestinal absorption of epicatechins and flavonols in different forms of green tea and its formulation: loose leaf tea, powdered tea, 35% catechins containing GTE, and GTE formulated with green tea-derived polysaccharide and flavonols (CATEPLUS™). The bioaccessibillity and intestinal absorption of epicatechins and flavonols was investigated by using an in vitro digestion model system with Caco-2 cells. The bioaccessibility of total epicatechins in loose leaf tea, powdered tea, GTE, and CATEPLUS™ was 1.27%, 2.30%, 22.05%, and 18.72%, respectively, showing that GTE and CATEPLUS™ had significantly higher bioaccessibility than powdered tea and loose leaf tea. None of the flavonols were detected in powdered tea and loose leaf tea, but the bioaccessibility of the total flavonols in GTE and CATEPLUS™ was 85.74% and 66.98%, respectively. The highest intestinal absorption of epicatechins was found in CATEPLUS™ (171.39 ± 5.39 ng/mg protein) followed by GTE (57.38 ± 9.31), powdered tea (3.60 ± 0.67), and loose leaf tea (2.94 ± 1.03). The results from the study suggest that formulating green tea extracts rich in catechins with second components obtained from green tea processing could enhance the bioavailability of epicatechins.

The hypothesis of the current study was that flavonol and polysaccharides obtained during catechins extraction from green tea may enhance the effect of catechins on preventing pancreatic lipase activity, free glycerol absorption and accumulation in adipocytes co-cultured with Caco-2 cell after in vitro digestion. Catechins rich extract from green tea (GCT: 10 mg), GCT formulated with polysaccharides (GTP: 1 mg) and flavonol extract (GFV: 0.1 mg) strongly inhibited lipase activity during digestion while increasing lipolysis in adipocytes. Lipid accumulation in adipocytes was significantly reduced in GCT (10 mg) + GTP (1 mg) + GFV (1 mg) (100–87.27%) compared to control (p

Ethnopharmacological relevance Seed of Torreya nucifera (L.) Siebold & Zucc is used to treat several diseases in Asia. Reports document that T. nucifera has anti-cancer, anti-inflammatory, anti-oxidative activities. In spite of numerous findings on its pharmacological effects, the understanding of the molecular inhibitory mechanisms of the plant remains to be studied. Therefore, we aimed to explore in vitro anti-inflammatory mechanisms of ethyl acetate fraction (Tn-EE-BF) prepared from the seed of T. nucifera in LPS-stimulated macrophage inflammatory responses. Materials and methods For this purpose, we measured nitric oxide (NO) and prostaglandin E2 (PGE2) in LPS-stimulated macrophages. Additionally, using RT-PCR, luciferase reporter gene assay, immunoblotting analysis, and kinase assay, the levels of inflammatory genes, transcription factors, and inflammatory signal-regulatory proteins were investigated. Finally, the constituent of Tn-EE-BF was identified using HPLC. Results Tn-EE-BF inhibits NO and PGE2 production and also blocks mRNA levels of inducible NO synthase (iNOS), tumor necrosis factor (TNF)-α, and cyclooxygenase (COX)-2 in a dose dependent manner. Tn-EE-BF reduces nuclear levels of the transcriptional factors NF-κB (p65) and AP-1 (c-Jun and FRA-1). Surprisingly, we found that Tn-EE-BF inhibits phosphorylation levels of Src and Syk in the NF-κB pathway, as well as, IRAK1 at the protein level, part of the AP-1 pathway. By kinase assay, we confirmed that Src, Syk, and IRAK1 are suppressed directly. HPLC analysis indicates that arctigenin, amentoflavone, and quercetin may be active components with anti-inflammatory activities. Conclusion Tn-EE-BF exhibits anti-inflammatory activities by direct inhibition of Src/Syk/NF-κB and IRAK1/AP-1.

Thirty-three phenolic compounds were identified from the extract of fermented tea (Camellia sinensis L.), including three undescribed flavonoids, namely quamoreokchaside I–II and kamoreokchaside I, along with thirty known compounds. All isolates were tested to evaluate their inhibitory effects against amyloid-beta (Aβ) aggregation through thioflavin-T (ThT) fluorescence-based assay and transmission electron microscopy (TEM). Among the isolates, three tea polyphenols, including (–)-catechin gallate (CG), (–)-epicatechin gallate (ECG), and (–)-epigallocatechin gallate (EGCG), significantly decreased Aβ aggregation at a concentration of 10 μg ml−1, compared to the positive control, Aβ alone. The anti-Aβ aggregation effects of CG, ECG, and EGCG were confirmed again via TEM, which were consistent with the ThT fluorescence-based assay. Moreover, CG and ECG provided stronger protection on SH-SY5Y cells against Aβ-induced cytotoxicity than EGCG. Remarkably, CG showed more potent inhibitory activity than EGCG, the best-known anti-Aβ aggregation agent from tea products.

Dehydrotrametenolic acid (DTA) is a lanostane-type triterpene acid isolated from Poria cocos Wolf (Polyporaceae). Several studies have reported the anti-inflammatory and antidiabetic effects of DTA, however, its effects on the skin are poorly understood. In this study, we investigated the effects of DTA on skin barrier function in vitro and its regulatory mechanism in human keratinocyte cell line HaCaT cells. DTA increased the microRNA (mRNA) expression of natural moisturizing factor-related genes, such as HAS-2, HAS-3, and AQP3 in HaCaT cells. DTA also upregulated the mRNA expression of various keratinocyte differentiation markers, including TGM-1, involucrin, and caspase-14. Moreover, the protein expression of HAS-2, HAS-3, and TGM-2 were significantly increased by DTA. To examine the regulatory mechanisms of DTA, Western blotting, luciferase-reporter assays, and RT-PCR were conducted. The phosphorylation of mitogen-activated protein kinases (MAPKs) and I&kappa, B&alpha, were increased in DTA-treated HaCaT cells. In addition, AP-1 and NF-&kappa, B transcriptional factors were dose-dependently activated by DTA. Taken together, our in vitro mechanism studies indicate that the regulatory effects of DTA on skin hydration and keratinocyte differentiation are mediated by the MAPK/AP-1 and I&kappa, /NF-&kappa, B pathways. In addition, DTA could be a promising ingredient in cosmetics for moisturizing and increased skin barrier function.

This study demonstrates an effective one-pot regioselective synthesis of 3,7-diarylpyrazolo [1,5-α]pyrimidines. Moreover, the derivatives obtained were effective CB1R antagonists. These pyrazolo [1,5-α]pyrimidines with diaryl groups at the 3,7-positions are potential pharmacophores for CB1R candidates.