Background/Objectives: Trans-resveratrol (Res) has been reported to possess many biological activities, including neuroprotective effects, owing to its anti-inflammatory and antioxidant properties. However, Res has very low water solubility, which limits its therapeutic application. In this work, we formulated water-soluble micellar formulations incorporating Res using polyethylene glycol monostearate (stPEG). Methods: These formulations (stPEG/Res) were developed using five types of stPEG containing 10, 25, 40, 55 and 140 PEG repeat units. The formulations were characterized for Res content, water solubility, particle size, zeta potential, precipitation, biodistribution, and efficacy against neuronal and motor dysfunction in intracerebral hemorrhage (ICH). Results: Intravenous administration of stPEG40/Res, which demonstrated particle size, water solubility, and biodistribution properties suitable for intravenous administration, suppressed neurological and motor dysfunction following in a collagenase-induced ICH mouse model. These effects were inhibited by zinc protoporphyrin-9, an inhibitor of the antioxidant enzyme heme oxygenase-1, suggesting that Res contributes to antioxidant enzyme expression and anti-inflammatory activity. Conclusions: The stPEG/Res micellar formulation developed in this study may offer a promising therapeutic approach for ICH treatment.

Carnosic acid is a naturally occurring, plant-derived polyphenolic abietane diterpene with antitumor properties. However, its underlying mechanisms are still unclear. Therefore, we investigated the effects of carnosic acid on lung metastasis in a murine melanoma model. C57BL/6 mice were intravenously injected with B16-BL6 cells, followed by carnosic acid treatment. Lung weights were recorded, and tumor cell colonies were counted at the end of the experiment. Integrin expression was evaluated using flow cytometry and cell adhesion assays. Lung weights were significantly lower in the carnosic acid group than in the control group, indicating the suppression of metastasis. Carnosic acid suppressed α4 integrin expression in B16-BL6 cells and inhibited α4 and α9 integrin-dependent cell adhesion. Thus, our data suggest that carnosic acid prevents lung metastasis, possibly by suppressing integrin expression. Our findings support the clinical application of carnosic acid as a potential natural antitumor agent, offering a complementary approach to conventional therapies.

In 2007, the Japanese Orthopaedic Association proposed the concept of locomotive syndrome, a comprehensive description of conditions involving the functional decline of the locomotor system. Locomotive syndrome includes bone-related diseases such as osteoporosis, joint cartilage and disc-related diseases such as osteoarthritis and lumbar spondylosis, and sarcopenia and locomotive syndrome-related diseases. If left untreated, these diseases are likely to reduce mobility, necessitating nursing care. To prevent the progression of locomotive syndrome, a daily exercise routine and well-balanced diet are important, in addition to recognizing one’s own decline in mobility. Therefore, research on the effectiveness of functional ingredients in the prevention and suppression of locomotive syndrome progression is ongoing. In this review, we summarize the latest reports on the effectiveness of five functional ingredients, namely, epigallocatechin gallate, resveratrol, curcumin, ellagic acid, and carnosic acid, in the treatment of osteoarthritis, osteoporosis, and rheumatoid arthritis, which are considered representative diseases of the locomotive syndrome.

Background:Dry eye disease (DED) is a multifactorial ocular surface condition that causes damage and discomfort, significantly impairing the quality of life of patients. Recently, phytochemicals such as trans-resveratrol (Res) have attracted growing interest due to their potential therapeutic effects against the DED-related pathophysiology. To enable the therapeutic application of water-insoluble Res, this study aimed to evaluate the efficacy of a previously developed water-soluble micelle formulation (stPEG/Res) containing polyethylene glycol monostearate (stPEG) in treating DED.Methods:The antioxidant activity of stPEG/Res was assessed using the 2,2-diphenyl-1-picrylhydrazyl radical-scavenging assay, and its cytotoxicity was evaluated in a human corneal epithelial cell line. Furthermore, an in vivo efficacy study was performed using a mouse model of DED induced by lacrimal gland excision. Tear volume, corneal histopathological changes, inflammatory responses, and apoptosis in the cornea were evaluated.Results:The stPEG/Res formulation exhibited antioxidant activity and a cytotoxicity profile against corneal epithelial cells comparable to that of free Res. Furthermore, in the mouse model of DED, stPEG/Res alleviated dry eye symptoms not by restoring tear volume, but by suppressing inflammation and apoptosis in the cornea.Conclusions:These findings indicate that stPEG/Res has potential as a novel therapeutic option for corneal disorders associated with DED.