Lipase-mediated synthesis of ricinoleic acid vanillyl ester and evaluation of antioxidant and antibacterial activity.

Castor oil extracted from castor bean has antibacterial property, and has been used in various folk remedies. The major structural component of castor oil, ricinoleic acid, has actual antibacterial activity. Some phenolic compounds derived from plants have antioxidant property. Among them, vanillyl alcohol from vanilla bean has strong antioxidant activity. As vanillyl alcohol has low solubility in hydrophobic solvents and castor oil has low solubility in hydrophilic solvents, there is practical difficulty in using them. We performed lipase-mediated transesterification using vanillyl alcohol and castor oil, and synthesized ricinoleic acid vanillyl ester (RAVE). 2,2-Diphenyl-1-picrylhydrazyl assay and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) assay revealed that RAVE had a strong antioxidant activity in various organic solvents. RAVE also had antibacterial activity against some food spoilage bacteria. It showed more powerful antibacterial activity for gram positive bacteria than for gram negative bacteria. The critical micelle concentration of RAVE was measured at 7.36 µM and it partitioned exclusively into emulsion phase in water-emulsion system. Zeta potential measurement, membrane release test, and fluorescent microscopy showed that RAVE inserted itself into the bacterial cell membrane, destroyed membrane permeability, and induced cell death. As such, RAVE is a novel multi-functional compound with antioxidant and antibacterial activity, so it can be used as a functional material in the food and cosmetic industries.

Vitamin d status and response to initial vitamin d supplementation in korean women with osteoporosis.

BACKGROUND: The aim of this study is to evaluate whether the optimal vitamin D level is achieved after taking recommended dose in vitamin D deficient patients. METHODS: This was a retrospective study. Women (n=52) first diagnosed with osteoporosis were recruited in outpatient clinic. They were recommended to be exposed to sun light for more than 30 min a day. Subjects were divided into 3 groups according to serum 25-hydroxy-vitamin D3 (25-[OH]D3) status: deficiency (less than 20 ng/mL), insufficiency (20-30 ng/mL) and sufficiency (30 ng/mL or more). Insufficient and sufficient patients received the recommended dose (1,000 IU/day) but deficient patients received recommended or double dose (1,800-2,000 IU/day). We compared 25-(OH)D levels at baseline and after vitamin D supplementation for 3 months. RESULTS: Median (interquartile range) serum 25-(OH)D concentration at baseline was 15.10 (13.30-16.97) ng/mL and the proportion of deficient, insufficient and sufficient groups were 69.2%, 23.1%, and 7.7% respectively. The optimal 25-(OH)D level (30 ng/mL or more) was achieved in 83.3% of insufficient patients with the recommended dose and was did in 55.6% of deficient patients with recommended dose (P=0.117). However, 88.9% of the deficient patient with double dose achieved optimal level (P=0.030). CONCLUSIONS: About 44% of vitamin D deficient patients did not attain the optimal level of serum 25-(OH)D despite recommended daily intake of vitamin D to 1,000 IU in patients with osteoporosis. Follow-up of serum 25-(OH)D levels may be required for vitamin D supplementation in vitamin D deficient patients with osteoporosis.

Nobiletin suppresses MMP-9 expression through modulation of p38 MAPK activity in human dermal fibrobalsts.

We aimed to identify a novel flavonoid from the in-house natural products to suppress matrix metalloproteases (MMPs), which is responsible for degradation of collagen and other extracellular matrix proteins. Total eight natural products were screened for identification of a novel MMP-9 suppressor using MMP-9 reporter system, where the prompt initial screening with multiple samples is readily examined. Among the extracts used in the present study, one extract (Citrus unshiu) was found active in this assay system. Furthermore, three representative flavonoids in this active extract of Citrus unshiu peel were tested in MMP-9 reporter system. Nobiletin (NB) of the tested flavonoids suppressed MMP-9 expression without cytotoxicity, which was validated by both real-time polymerase chain reaction (PCR) and zymography analyses. Sustained p38 mitogen activated protein kinase (MAPK) activity, closely associated with induction of MMP-9 under stress condition, was markedly reduced by NB treatment, which implies that modulation of p38MAPK by nobiletin is responsible for reduction of MMP9 expression. Hence, nobiletin, identified from MMP-9 reporter system based screening, may be further applied for the purpose of delaying collagen degradation in skin fibroblasts.

Extract of Aneilema keisak inhibits transforming growth factor-ß-dependent signalling by inducing Smad2 downregulation in keloid fibroblasts.

Keloids are characterised by the excessive accumulation of extracellular matrix (ECM), especially overabundant collagen formation. In keloid fibroblasts (KFs), transforming growth factor (TGF)-ß-dependent signalling is closely associated with a variety of keloid pathologic responses such as ECM production and fibroblast overgrowth. Thus, inhibition of TGF-ß signalling would be a potential therapeutic approach to prevent keloid scar formation. Thereby, we aimed to identify a novel TGF-ß signalling blocker among natural products using a simplified screening approach. We discovered that the extract of Aneilema keisak (A.K-Ex) lowered TGF-ß-dependent signalling by reducing Smad2 protein levels. Given that KFs showed altered dependency on TGF-ß for survival and proliferation, A.K-Ex-mediated reduction in Smad2 protein levels significantly inhibited the major characteristics of KFs such as cell growth, migration and collagen synthesis, suggesting that A.K-Ex exhibits possible therapeutic activity on keloids.