Citrus aurantium 'Changshan-huyou'-An ethnopharmacological and phytochemical review.

Citrus fruits are composed of oil cells layer, white membrane layer, pulp and seeds. The cultivar Citrus aurantium 'Changshan-huyou' (CACH) is a hybridization of Citrus grandis Osbeck and C. sinensis Osbeck. It is a rutaceae plant, and mainly grows in Changshan, Zhejiang, China. With the exploration of its high traditional values, it has been paid more and more attention by the scientific community in recent years. At present, one hundred and two chemical constituents have been identified from the pulp and peel of CACH, including volatile oils, terpenoids, phenols, limonins, sugars, etc., As the representative active component of CACH, phenols have been widely investigated. Studies have shown that CACH shows a variety of significant pharmacological activities, such as anti-inflammatory, antioxidant, hepatoprotective activity, respiratory system protection and intestinal regulation activity. This review mainly introduces the chemical constituents and pharmacological activities of CACH, and discusses its future research and development directions. It will provide theoretical basis for further research of its pharmacodynamic substances, functional mechanism and rational utilization.

Identification of Sorafenib as a Treatment for Type 1 Diabetes.

Th1 cell activation is considered a key mediator of the pathogenesis of type 1 diabetes. Targeting IL-12-induced Th1 cell differentiation seems to be an effective way to block the development of type 1 diabetes. However, given the critical function of Th1 in the immune system, the potential side effects hinder the application of anti-Th1 therapy in the treatment of type 1 diabetes. To identify safe anti-Th1 treatment(s), we screened the FDA-approved tyrosine kinase inhibitor (TKI) drug library using an IL-12-induced Th1 differentiation cell model. We found that among the TKIs with little effect on T cell viability, sorafenib is the top contender for the inhibition of Th1 differentiation. Treatment of NOD mice with sorafenib significantly impeded the development of type 1 diabetes and ameliorated insulitis, which coincided with a specifically decreased accumulation of Th1 cell population in the pancreas but not in peripheral immune organs. Mechanistically, sorafenib indirectly inhibited janus kinase 2 (JAK2) activity and blocked IL-12-induced phosphorylations of JAK2 and signal transducer and activator of transcription 4 (STAT4). Since sorafenib is classified as an FDA-approved drug, it serves as a preliminary lead point for additional experimentation and may be a promising therapy for type 1 diabetes in humans.

A new antibacterial 3,5-dimethylorsellinic acid-based meroterpene from the marine fungus Aspergillus sp. CSYZ-1.

Chemical investigation of the extracts of Aspergillus sp. CSYZ-1 resulted in the identification of compound 1, aspergillactone, a new 3,5-dimethylorsellinic acid-based meroterpenoid, together with four known metabolites (2-5). The structure and relative configuration of 1 were unambiguously determined by nuclear magnetic resonance (NMR), mass spectrometry. The absolute configuration of 1 was defined by quantum chemical TDDFT calculated and the experimental ECD spectra. The possible biosynthetic pathway of compound 1 was also proposed. The new compound exhibited potent antimicrobial activity against Helicobacter pylori and Staphylococcus aureus with MIC values of around 1-4 and 2-16 µg/mL, respectively.

[Study on original plant species and geographical distribution of Fructus Aurantii].

The original plant species of Fructus Aurantii are multitudinous and complex, and their requirements to the growing environment is strict. In order to clarify the original plant species and geographical distribution of Fructus Aurantii which recorded in the standards and circulated, used in commodity. The national and local standards of Chinese medicinal materials were collected and the original plants of Fructus Aurantii recoded in standards were found. Ten original plant species of Fructus Aurantii (including varieties of cultivars, the same below) were recorded in the Chinese pharmacopoeia and six local standards of Zhejiang, Yunnan and Guizhou etc. The producing areas and commodity in markets of Fructus Aurantii were investigated. The growth environment and geographical distribution of them were analyzed. There are six types of Fructus Aurantii i.e., Fructus Aurantii Chuan, Fructus Aurantii Xiang, Fructus Aurantii Jiang, Fructus Aurantii Qu, Fructus Aurantii Su, Fructus Aurantii Wen, and nineteen species of original plants in the practical commodities. There are four major Fructus Aurantii producing areas: Sichuan Basin, Dongting Lake Plain, Poyang Lake Plain, Jinqu Basin and its surrounding hilly areas. All of them are located in the area of the east longitude 104° to 121° and the northern latitudes 27° to 31°. There is a certain difference between the actual commodity and the standards of medicinal materials. It is suggested that the traditional mainstream types of Fructus Aurantii with fine quality should be accepted into Chinese Pharmacopoeia, and the types with poor quality should be withdrawn from Chinese Pharmacopoeia.