Newly Generated Atractylon Derivatives in Processed Rhizomes of Atractylodes macrocephala Koidz.

Thermally processed rhizomes of Atractylodes macrocephala (RAM) have a long history of use in traditional Chinese medicine (TCM) for treating various disorders, and have been an integral part of various traditional drugs and healthcare products. In TCM, herbal medicines are, in most cases, uniquely processed. Although it is thought that processing can alter the properties of herbal medicines so as to achieve desired functions, increase potency, and/or reduce side effects, the underlying chemical changes remain unclear for most thermally processed Chinese herbal medicines. In an attempt to shed some light on the scientific rationale behind the processes involved in traditional medicine, the RAM processed by stir-frying with wheat bran was investigated for the change of chemical composition. As a result, for the first time, five new chemical entities, along with ten known compounds, were isolated. Their chemical structures were determined by spectroscopic and spectrometric analyses. The possible synthetic pathway for the generation of such thermally-induced chemical entities was also proposed. Furthermore, biological activity evaluation showed that none of the compounds possessed cytotoxic effects against the tested mammalian cancer and noncancer cell lines. In addition, all compounds were ineffective at inhibiting the growth of the pathogenic microorganisms.

The Chemical Characterization of Eleutherococcus senticosus and Ci-wu-jia Tea using UHPLC-UV-QTOF/MS.

Eleutherococcus senticosus Maxim. belongs to the Araliaceae family. Phytochemical studies reveal that E. senticosus leaves contain triterpene glycosides along with organic acid derivatives and flavonoid compounds. It is believed that E. senticosus is similar to ginseng because they come from same family and both contain triterpene saponins. E. senticosus leaves have been developed as a functional beverage called ci-wu-jia tea in recent years. Triterpene glycosides are difficult to identify by ultraviolet (UV) detection and contents of these compounds are low in E. senticosus leaves. In this study, a sensitive ultra-high performance liquid chromatographic (UHPLC) method combining UV and tandem mass spectrometry (MS/MS) was developed to characterize the triterpene glycosides from E. senticosus leaves and related commercial products. Fragmentation patterns of three sub-groups of triterpene glycosides in E. senticosus leaves were investigated. Additionally, fragmentation pathways and UV characteristics of organic acid derivatives and flavonoids were also characterized. A compound screening library, including 241 compounds reported in the literature, was created and used to confirm the compounds in the samples. In this study, a total of 24 samples, including 13 plant samples of E. senticosus and 11 ci-wu-jia tea products, were analyzed. Out of the 11 commercial products, three products were discovered to contain green tea (Camellia sinensis) that was considered to be an adulterant since it was not an ingredient on the labels. The developed UHPLC-UV-MS/MS analytical method combined with the UNIFI processing method can simultaneously characterize organic acid derivatives, flavonoids, and triterpene saponins from E. senticosus. It provides a simple and sensitive way to perform quality control of E. senticosus and related ci-wu-jia tea products.

Benzophenone glycosides from the flower buds of Aquilaria sinensis.

Four new benzophenone glycosides named as aquilaside A-D (1-4) along with five known compounds (5-9) were isolated from the methanol extract of the flower buds of Aquilaria sinensis. Their structures were elucidated on the basis of 1D and 2D NMR and mass spectroscopic analyses. All purified compounds were evaluated for their anti-inflammatory and cytotoxic activities. Aquilasides B and C displayed moderate cytotoxicity against SK-MEL cells with IC50 of 17.0 and 12.0µM and weak NF-κB inhibitive activity at 100µM with 30% and 60%, respectively.

Eleutherococcus senticosus (Araliaceae) Leaf Morpho-Anatomy, Essential Oil Composition, and Its Biological Activity Against Aedes aegypti (Diptera: Culicidae).

The roots of Eleutherococcus senticosus (Rupr. & Maxim.) Maxim., a well-known medicinal plant from Eastern Asia, are used worldwide for their known beneficial medicinal properties. Recently, the leaves have been used as an alternative to the roots. The present study was aimed at exploring the leaf essential oil as a potential source of compounds for mosquito management. Gas chromatography/mass spectrometry analysis of the leaf essential oil revealed 87 compounds, constituting 95.2% of the oil. α-Bisabolol (26.46%), ß-caryophyllene (7.45%), germacrene D (6.87%), ß-bisabolene (4.95%), and α-humulene (3.50%) were five of the major constituents. The essential oil was subjected to biting deterrence and repellent activity against mosquito Aedes aegypti. The biting deterrence of the oil produced a proportion not biting (PNB) value of 0.62 at 10 µg/cm2 as compared with 0.86 of control DEET (N,N-diethyl-3-methylbenzamide) at a standard dose of 25 nmol/cm2. Among individually selected compounds present in the oil (α-bisabolol, ß-caryophyllene, α-humulene, and caryophyllene oxide), only α-bisabolol produced a PNB value of 0.80, equivalent to DEET at 25 nmol/cm2, whereas the others were not repellent. The artificial mixture (AMES-1) of these four selected compounds produced a relatively high PNB value of 0.80. The repellent activity measured by minimum effective dosage (MED) for α-bisabolol and α-humulene produced MED values of 0.094 and 0.104 mg/cm2, respectively, as compared with 0.023 mg/cm2 of DEET. The leaf essential oil, the artificial mixture (AMES-1), and other binary and tertiary combinations of major compounds showed no repellent activity. In addition, morpho-anatomical features of the leaf are provided for correct identification of the species.

[Nrf2-NF-κB pathway axes, epigenetic regulation and traditional Chinese medicine (natural medicine) to treat type 2 diabetes].

Diabetes mellitus is a characterized by high blood sugar metabolic disease, is a lifelong disease with a high incidence of major hazards. Prevention and treatment of diabetes and its complications has become a serious challenge and arduous task facing the world pharmaceutical researchers. Oxidative stress, Nfr2-NF-κB signaling axis related epigenomic genes have the apparent close relationship with type 2 diabetes,those have become one of the key focus and effective way to explore its pathogenesis, mechanism and drug screening. This paper systematically summarizes the current stage research regulating the key proteins, mRNA about Nrf2-NF-κB axis pathway and epigenomics for treatment of type 2 diabetes and the mechanism of traditional Chinese medicine and natural medicine (component) in the treatment of type 2 diabetes, hoping to provide some innovative research ideas for finding new drugs of the treatment of diabetes from traditional Chinese medicine and natural medicine.