In vitro and in vivo anti-aging effects of compounds isolated from Artemisia iwayomogi

In Korean folk medicine, Artemisia iwayomogi has largely been employed for the improvement of diabetic complications and hepatic function as well as in the treatment of female diseases and skin whitening. Accordingly, the present study sought to assess cosmeceutical activity of Artemisia iwayomogi. Through activity-guided fractionation, scopolin (AI-1), 2,4-dihydroxy-6-methoxy-acetophenone 4-O-β-D-glucoside (AI-2), scopoletin (AI-3), kaempferol-3-O-methyl ether (AI-4) and luteolin (AI-5) were isolated from ethyl acetate and water fractions of Artemisia iwayomogi. Of them, AI-4 and AI-5 exhibited strong antioxidative and whitening effects. In addition, AI-1, AI-3, AI-4, and AI-5 demonstrated considerable anti-wrinkle performances. According to results of quantitative analysis of compounds isolated from Artemisia iwayomogi, scopolin (AI-1) is a major component of Artemisia iwayomogi. Moreover, O/W type cream made by water fraction which included scopolin showed unwrinkling effect for 8 weeks when it was applied to face in an in vivo study. Specific contributions of Artemisia iwayomogi were as follows: AI-1, 1.21 mg/g; AI-2, 0.26 mg/g; AI-3, 0.38 mg/g; AI-4, 0.01 mg/g; and AI-5, 0.04 mg/g.

Isoamericanoic Acid B from Acer tegmentosum as a Potential Phytoestrogen

Phytoestrogens derived from plants have attracted the attention of the general public and the medical community due to their potentially beneficial role in relieving menopausal symptoms. The deciduous tree Acer tegmentosum Maxim (Aceraceae) has long been utilized in Korean folk medicine to alleviate many physiological disorders, including abscesses, surgical bleeding, and liver diseases. In order to explore structurally and/or biologically new constituents from Korean medicinal plants, a comprehensive phytochemical study was carried out on the bark of A. tegmentosum. One new phenolic compound with a 1,4-benzodioxane scaffold, isoamericanoic acid B (1), as well as with nine known phenolic compounds (2–10), were successfully isolated from the aqueous extracts of the bark of A. tegmentosum. A detailed analysis using 1D and 2D NMR spectroscopy, electronic circular dichroism (ECD) spectral data, and LC/MS afforded the unambiguous structural determination of all isolated compounds, including the new compound 1. In addition, compounds 2, 4, 5, and 9 were isolated and identified from the bark of A. tegmentosum for the first time. All isolated compounds were tested for their estrogenic activities using an MCF-7 BUS cell proliferation assay, which revealed that compounds 1, 2, and 10 showed moderate estrogenic activity. To study the mechanism of this estrogenic effect, a docking simulation of compound 1, which showed the best estrogenic activity, was conducted with estrogen receptor (ER) -α and ER-β, which revealed that it interacts with the key residues of ER-α and ER-β. In addition, compound 1 had slightly higher affinity for ER-β than ER-α in the calculated Gibbs free energy for 1:ER-α and 1:ER-β. Thus, the present experimental evidence demonstrated that active compound 1 from A. tegmentosum could be a promising phytoestrogen for the development of natural estrogen supplements.

Inhibition effects of the classical pathway complement of isolated compounds from Quercus glauca

Species of the Quercus species is an evergreen broadleaf tree found not only in Korea but also in China, Taiwan, and Japan. Quercus species is the most commonly occurring plant among the 50 native species of the family Fagaceae in Korea, China, and Taiwan. Quercus species have been used for diarrhea, dysentery, dermatitis, and hemorrhagia in Korean folk medicine. The present study evaluated the anticomplement effect of constituents from Quercus species (Fagaceae) in classical pathway complement system. We have evaluated leaves of five species of the Quercus genus with regard to its anticomplement activity and have identified its active principles following activity-guided isolation. Bioactivity-guided fractionation of the 80% methanol extracts of the stem barks of Quercus glauca Thunberg has led to the isolation of galloyl derivatives, displaying high anticomplement activity. Four galloyl derivatives isolated from the leaves of Q. glauca, namely 6′- O-galloyl salidroside (1), methyl gallate (2), 1,2,3,6-tetragalloylglucose (3), and 1,2,6-trigalloylglucose (4). 1, 2, 3 and 4 showed inhibitory activity against complement system with 50% inhibitory concentrations (IC50) values of 224 μM, 362.4 μM, 32.3 μM, and 138.3 μM. Among the compounds tested, 3 showed the most potent anticomplement activity (IC50, 32.3 μM). This is the first report of the isolation and anticomplement activity from Q. glauca.