The Research of Toxicity and Sensitization Potential of PEGylated Silver and Gold Nanomaterials.

Polyethylene glycol (PEG) is a polymer used for surface modification of important substances in the modern pharmaceutical industry and biopharmaceutical fields. Despite the many benefits of PEGylation, there is also the possibility that the application and exposure of the substance may cause adverse effects in the body, such as an immune response. Therefore, we aimed to evaluate the sensitization responses that could be induced through the intercomparison of nanomaterials of the PEG-coated group with the original group. We selected gold/silver nanomaterials (NMs) for original group and PEGylated silver/gold NMs in this study. First, we measured the physicochemical properties of the four NMs, such as size and zeta potential under various conditions. Additionally, we performed the test of the NM's sensitization potential using the KeratinoSens™ assay for in vitro test method and the LLNA: 5-bromo-2-deoxyuridine (BrdU)-FCM for in vivo test method. The results showed that PEGylated-NMs did not lead to skin sensitization according to OECD TG 442 (alternative test for skin sensitization). In addition, gold nanomaterial showed that cytotoxicity of PEGylated-AuNMs was lower than AuNMs. These results suggest the possibility that PEG coating does not induce an immune response in the skin tissue and can lower the cytotoxicity of nanomaterials.

Stability Evaluation of National Reference Standards for Blood Products in Korea.

National reference standards (NRSs) for biologics are established through potency estimation by a multicenter joint study of standard materials used in the approval process for national lot release and quality control of vaccines, blood products, and other biologics. In this study, a stability evaluation was conducted to determine whether the potency of NRSs for six blood products was being maintained at a consistent level in Korea. The present study conducted real-time stability tests via in-vivo/in-vitro bioassay on NRSs for blood coagulation factor VIII concentrate (2nd standard), antithrombin concentrate, prekallikrein activator, anti-hepatitis B immunoglobulin, blood coagulation factor IX concentrate, and anti-tetanus human immunoglobulin, as well as a trend analysis using cumulative annual results. The real-time stability test results showed that the mean potency of six NRSs was all within the control limit. In the trend analysis, the potency of NRS for blood coagulation factor VIII concentrate (2nd standard) showed a decreasing trend, while the potency of all other products had been stably maintained. The present study confirmed that the mean potency of NRSs for six blood products had been stably maintained in Korea. The findings of the present study establish a foundation that can ensure the quality of NRSs for biologics in Korea, and it is expected to make a major contribution to the supply of high-quality biologics.

Potent acetylcholinesterase inhibitory compounds from Myristica fragrans.

The anti-cholinesterase activity was evaluated of the ethyl acetate fraction of the methanol extract of Myristica fragrans Houtt (Myristicaceae) seeds and of compounds isolated from it by various chromatographic techniques. The chemical structures of the compounds were determined from spectroscopic analyses (NMR data). Thirteen compounds (1-13) were isolated and identified. Compound 8 { [(7S)-8'-(4'-hydroxy-3'-methoxyphenyl)-7-hydroxypropyl]benzene-2,4-diol) showed the most effective activity with an IC50 value of 35.1 microM, followed by compounds 2 [(8R,8'S)-7'-(3',4'-methylenedioxyphenyl)-8,8'-dimethyl-7-(3,4-dihydroxyphenyl)-butane] and 11 (malabaricone C) with IC50 values of 42.1 and 44.0 pM, respectively. This is the first report of significant anticholinesterase properties of M. fragrans seeds. The findings demonstrate that M. fragrans could be used beneficially in the treatment of Alzheimer's disease.

Cycloartane-type triterpene glycosides from the rhizomes of Cimicifuga heracleifolia and their anticomplementary activity.

Seven known triterpene glycosides, 23-O-acetylshengmanol 3-O-α-L-arabinopyranoside (1), 23-O-acetylshengmanol 3-O-ß-D-xylopyranoside (2), 24-epi-24-O-acetylhydroshengmanol 3-O-ß-D-xylopyranoside (3), cimiaceroside B (4), (23R,24S)-cimigenol 3-O-ß-D-xylopyranoside (5), (23R,24R)-25-O-acetylcimigenol 3-O-ß-D-xylopyranoside (6) and (23R,24S)-25-O-anhydrocimigenol 3-O-ß-D-xylopyranoside (7) were isolated from the rhizomes of Cimicifuga heracleifolia. Their chemical structures were determined on the basis of spectroscopic analyses including 2D NMR. All isolates were investigated for their inhibitory effects on the classical pathway of the complement system. Among them, compound 6 showed strong inhibitory activity with an IC50 value of 7.7 µM while compound 3 was moderately active with an IC50 value of 195.6 µM.