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Giant Indian Gooseberry (GIG) or Phyllanthus indofischeri Bennet are commercially cultivated and commonly used herbs in Traditional medicine, especially in Thailand. The aim of this study was to assess the potential of the GIG extracts in anti-aging activities to be a dermatological application. The juice, meat residues, and seeds of GIG collected from Sra Kaeo Province, Thailand, were extracted by the Boiling method (B) and the Maceration process (M) by using 95% ethanol as a solvent. The GIG extracts gave the total phenolic, total flavonoid contents and quercetin contents, as well as exhibited anti-oxidative activities. The GIG-R-B extract inhibited tyrosinase activity and had the highest anti-melanogenesis activity on B16F10 cells at 31.63 ± 0.70%. The GIG-S-B, GIG-S-M, and GIG-R-M extracts demonstrated the highest collagen biosynthesis, which was comparable to vitamin C (p < 0.05), whereas the GIG-R-B extracts gave the highest stimulation of anti-aging genes (SIRT1 and FOXO1). All extracts at the concentration of 0.1 mg/mL showed no cytotoxicity on human skin fibroblasts. Therefore, the GIG-S-B extract was discovered to be a promising natural anti-aging agent for dermatological health and aesthetic applications that can be further developed in cosmetic, functional food and food supplement industries.

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Skin ageing is characterized by features such as wrinkles, loss of elasticity, laxity, rough-textured appearance, melasma and freckles. Several researches have focused for preventing, and treating skin ageing by many natural ingredients. This study aimed to assess the anti-ageing activities for anti-skin ageing of the ethanolic extracts of Pink rambutan (PR) (Nephelium lappaceum Linn.) from leaves (L), branches (B), seeds (S), and peels from ripe (R) and young (Y) fruits. The extraction yields of all Pink Rambutan (PR) extracted by the Maceration (M) and the Soxhlet extraction (Sox) using 95% ethanol as a solvent, ranged from 10.62% to 30.63%. Flavonoids were found as the main phytochemicals in almost all the PR extracts. The PR-Y-M and PR-Y-Sox extracts gave the highest total phenolic contents by the Folin-Ciocalteu assay of 67.60 ± 4.38 mgGAE/g, and total flavonoid contents by the modified aluminum chloride colorimetric assay of 678.72 ± 23.59 mgQE/g, respectively. The PR-L-M extracts showed the highest three anti-oxidative activities; the free radical scavenging (SC50 of 0.320 ± 0.070 mg/mL), the lipid peroxidation inhibition (LC50 of 0.274 ± 0.029 mg/mL), and the metal chelation activity (MC50 of 0.203 ± 0.021 mg/mL). All the PR extracts at 0.01 and 0.1 mg/mL showed no cytotoxicity on B16F10 cells, and human skin fibroblasts, respectively. Likewise, the PR-R-Sox extract exhibited the highest anti-melanogenesis on B16F10 cells (52.7 ± 0.9%) and, the mushroom tyrosinase inhibition activity (IC50 of 0.04 ± 0.02 mg/mL), which was significantly comparable to kojic acid (p < 0.05). The PR-Y-Sox extract showed the collagen biosynthesis by the Sirius Red method, and the stimulation of anti-ageing genes (Sirt1 and Foxo1) on human skin fibroblasts by the RT-PCR method, which were similar to standards ʟ-ascorbic acid and resveratrol, respectively. This study suggests that the PR-R-Sox and PR-Y-Sox extracts can be further developed as natural anti-ageing agents for whitening and anti-wrinkle in the cosmetics, cosmeceutical, and pharmaceutical industries.

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CONTEXT: Bambara groundnut (BG), originally from Africa, is widely distributed in Asian countries, especially in southern Thailand, and is used for food and functional foods. There is no report on the use of BG for ethnomedicine or cosmetics. OBJECTIVE: To investigate collagen biosynthesis stimulation and anti-melanogenesis of the BG extracts. MATERIALS AND METHODS: The hulls (H) and seeds (S) of BG were collected from Trang province, Thailand and extracted by Soxhlet (S) and maceration (M) using ethanol, and boiled with distilled-water (B). Total phenolic (TPC) and total flavonoid (TFC) contents were quantified. The three antioxidant and tyrosinase inhibition activities were determined by DPPH, FIC and FTC; and the modified dopachrome methods, respectively. The collagen biosynthesis and the anti-melanogenesis activities were investigated by Sirius-Red and the melanin content assay. RESULTS: The yields of BG extracts ranged from 1.72% to 9.06%. The BG-SS extract gave the highest TPC and TFC. The BG-HM extract showed the highest antioxidant activities (SC50 of 0.87 ± 0.02 mg/mL, MC50 of 1.83 ± 0.09 mg/mL and LC50 of 0.70 ± 0.06 mg/mL), tyrosinase inhibition activity (IC50 of 0.45 ± 0.23 mg/mL), and anti-melanogenesis activities (72.9 ± 0.08%), whereas the BG-SB extract exhibited the highest stimulation of collagen biosynthesis (18.04 ± 0.03%). All BG extracts at 0.1 mg/mL showed no cytotoxicity on human dermal fibroblasts. DISCUSSION: The biological activities of BG extracts might be from their phytochemicals, especially phenolic and flavonoid contents. CONCLUSION: The BG-HB and BG-HM extracts might be promising novel active sources for anti-aging and whitening cosmeceuticals.

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Activated macrophages produce various pro-inflammatory mediators such as inducible nitric oxide synthase (iNOS)-derived nitric oxide (NO) and cyclooxygenase (COX)-2-derived prostaglandin E2 (PGE2) during inflammatory response. However, overproduction of NO and PGE2 appears to be involved in pathogenesis of various inflammatory diseases. Therefore, inhibition of NO and PGE2 production might be useful for the treatment of inflammatory-related diseases. In this study, the bis[(5-methyl)2-furyl](4-nitrophenyl)methane or BFNM was evaluated for the anti-inflammatory activity and mechanism of action in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage. BFNM inhibited NO and PGE2 production in a concentration-dependent manner and down-regulated the expression of iNOS and COX-2 at mRNA and protein levels. BFNM suppressed nuclear translocation of NF-κB p65 subunit only very slightly, and failed to decrease NF-κB DNA binding activity. In contrast, the compound significantly reduced phosphorylation of p38 MAPK and ATF-2, a component of AP-1 known to be involved in the transcriptional regulation of iNOS and COX-2, in a dose-dependent manner in LPS-induced cells. Collectively, these results suggest that BFNM has an anti-inflammatory effect in RAW 264.7 macrophages, at least in part, by suppression of NO and PGE2 production. The inhibitory effect of BFNM is mediated mainly via the p38 MAPK/ATF-2 signaling pathway. Thus, BFNM would be a lead compound for the development of novel anti-inflammatory agents.

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Molecular iodine has been used as an efficient catalyst for a double Friedel-Crafts reaction of various heteroarenes, i.e. 2-methylfuran, 2-ethylfuran, 2-methylthiophene, pyrrole, N-methylpyrrole and indole, using aldehydes as alkylating agents under "open-flask" conditions with toluene or water as the reaction media. In the presence of 10 mol% iodine in toluene at room temperature, both aliphatic and aromatic aldehydes reacted smoothly to give the corresponding bis(heteroaryl)alkanes in good to excellent yields. Interestingly, with water as the solvent, the bis(heteroaryl)alkane adducts were obtained in moderate to good yields. The use of mild reaction conditions, low catalyst loadings, and eco-friendly reagents in a single step synthesis are the advantages of the present procedure. In an effort to discover novel non-steroidal anti-inflammatory agents, the synthesized bis(heteroaryl)alkanes were evaluated for the anti-inflammatory activity in the lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage model. These compounds (50 µM) significantly inhibited NO production and did not exhibit significant cytotoxic effects on macrophage cells. Among them, bis[(5-methyl)2-furyl](4-nitrophenyl) methane exhibited the most potent inhibition of NO with IC50 value of 42.4 ± 1.9, which is similar to that of the positive control, aminoguanidine (43.3 ± 2.5 µM). Thus, the bis[(5-methyl)2-furyl](4-nitrophenyl) methane could be considered a lead compound for the development of novel anti-inflammatory agents.

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