Ginsenosides Conversion and Anti-Oxidant Activities in Puffed Cultured Roots of Mountain Ginseng

CRMG (Cultured Roots of Mountain Ginseng) have the advantages in scale-up production, safety, and pharmacological efficacies. Though several methods are available for the conversion of major to minor ginsenosides, which has more pharmacological activities, a single step process with high temperature and pressure as a puffing method took place in this study to gain and produce more pharmacologically active compounds. Puffed CRMG exhibited an acceleration of major ginsenosides to minor ginsenosides conversions, and released more phenolic and flavonoid compounds. HPLC analysis was used to detect a steep decrease in the contents of major ginsenosides (Re, Rf, Rg1, Rg2, Rb1, Rb2, Rb3, Rc and Rd) with increasing pressure; on the contrary, the minor ginsenosides (20 (S, R)-Rg3, Rg5, Rk1, Rh1, Rh2, Rg6, F4 and Rk3) contents increased. Minor ginsenosides, such as Rg6, F4 and Rk3, were firstly reported to be produced from puffed CRMG. After the puffing process, phenolics, flavonoids, and minor ginsenoside contents were increased, and also, the antioxidant properties, such as DPPH inhibition and reducing the power of puffed CRMG, were significantly enhanced. Puffed CRMG at 490.3 kPa and 588.4 kPa had a low toxicity on HaCaT (immortalized human epidermal keratinocyte) cells at 200 μg/mL, and could significantly reduce ROS by an average of 60%, compared to the group treated with H2O2. Therefore, single step puffing of CRMG has the potential to be utilized for functional food and cosmeceuticals.

Effects of Carissa carandas Linn. Fruit, Pulp, Leaf, and Seed on Oxidation, Inflammation, Tyrosinase, Matrix Metalloproteinase, Elastase, and Hyaluronidase Inhibition

In this study, the potential of Carissa carandas Linn. as a natural anti-aging, antioxidant, and skin whitening agent was studied. Various parts of C. carandas, including fruit, leaf, seed, and pulp were sequentially extracted by maceration using n-hexane, ethyl acetate, and ethanol, respectively. High-performance liquid chromatography, Folin–Ciocalteu, and Dowd method were used to investigate their chemical compositions. The inhibitory activities of oxidation process, matrix metalloproteinases (MMPs), elastase, hyaluronidase, and tyrosinase were analyzed. Cytotoxicity was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrazolium bromide assay in a human epidermal keratinocyte line (HaCaT). The results exhibited that ethyl acetate could extract the most ursolic acid from C. carandas, while ethanol could extract the most phenolics and flavonoids. The leaf extract had the highest content of ursolic acid, phenolics, and flavonoids. The leaf extracted with ethyl acetate (AL) had the highest ursolic acid content (411.8 mg/g extract) and inhibited MMP-1, NF-kappa B, and tyrosinase activity the most. Ursolic acid has been proposed as a key component in these biological activities. Although several C. carandas extracts are beneficial to human skin, AL has been proposed for use in cosmetics and cosmeceuticals due to its superior anti-wrinkle, anti-inflammation, and whitening properties.

In vitro investigation of metabolic fate of α-mangostin and gartanin via skin permeation by LC-MS/MS and in silico evaluation of the metabolites by ADMET predictor™

Background Mangosteen, Garciniam angostana L., is a juicy fruit commonly found in Thailand. The rinds of Garciniam angostana L.have been used as a traditional medicine for the treatment of trauma, diarrhea and skin infection. It is also used in dermatological product such as in cosmetics. The mangosteen pericarp can be used to extract valuable bioactive xanthone compounds such as α-mangostin and gartanin. This study is aimed to predict the metabolism of α-mangostin and gartanin using in silico and in vitro skin permeation strategies. Methods Based on their 2D molecular structures, metabolites of those compounds were predicted in silico using ADMET Predictor™. The Km and Vmax, for 5 important recombinant CYP isozymes 1A2, 2C9, 2C19, 2D6 and 3A4 were predicted. Moreover, the in vitro investigation of metabolites produced during skin permeation using human epidermal keratinocyte cells, neonatal (HEKn cells) was performed by LC-MS/MS. Results It was found that the results derived from in silico were in excellent alignment with those obtained from in vitro studies for both compounds. The prediction referred that gartanin and α-mangostin were the substrate of CYP1A2, 2C9, 2C19 and 3A. In the investigation of α-mangostin metabolites by LC-MS/MS system, the MW of the parent compound was increased from 411.200 to 459.185 Da. Therefore, α-mangostin might be metabolized via tri-oxidation process. The increased molecular weight of parent compound (397.200 to 477.157 Da) illustrated that gartanin might be conjugated to sulfated derivatives. Conclusions In all the studies, α-mangostin and gartanin were predicted to be. metabolized via phase I and phase II metabolism (sulfation), respectively.