Christian Haug’s research while affiliated with Solvay (Shanghai) Co., Ltd. and other places

Inflammation plays a major role in many diseases, for instance in arteriosclerosis, rheumatoid arthritis, autoimmune disorders and cancer. Since many plants contain compounds with anti-inflammatory activity, their consumption may be able to prevent the development of inflammatory-based diseases. Edible ferns are some of the most important wild vegetables in China and have traditionally been used both for dietary and therapeutic purposes. In this study we investigated the anti-inflammatory and antioxidant potential of fern extracts from Matteuccia struthiopteris, Osmundajaponica, Matteuccia orientalis and Pteridium aquilinum intended for use as nutraceuticals. Two modes of action were investigated: the inhibition of the pro-inflammatory gene expression of interleukin-1 beta (IL1-β) and interleukin-6 (IL6), and the gene expression of iNOS by LPS-elicited macrophages. The results showed a decrease of IL1-β gene expression for the five fern extracts. This effect was more pronounced for the extracts prepared from the roots of O. japonica (IC50 of 17.8 µg/mL) and the young fronds of M orientalis (50.0 µg/mL). Regarding the indirect measurement of NO, via iNOS gene expression, an interesting decrease of 50% was obtained with the extract of M. orientalis fronds at a low concentration (20 µg/mL) compared with P. aquilinum fronds (160 µg/mL) and leaves of O. japonica. The latter showed a higher decrease but at a high concentration of extract (160 µg/mL). The five fern extracts were also evaluated for their ability to scavenge 2,2-diphenyl-l-picrylhydrazyl (DPPH) radicals and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). All fern extracts exhibited antioxidant effects but the roots of O. japonica and the fronds of M orientalis were most efficient. The HPLC-MS analysis of the constituents of the fern extracts confirmed the presence of chlorogenic acid, caffeic acid, p-coumaric acid, ferulic acid, kaempferol and apigenin, molecules known to exhibit antiinflammatory and/or antioxidant properties.

Plants represent a tremendous structural diversity of natural compounds that bind to many different human disease targets and are potentially useful as starting points for medicinal chemistry programs. This resource is, however, still underexploited due to technical difficulties with the identification of minute quantities of active ingredients in complex mixtures of structurally diverse compounds upon raw phytomass extraction. In this work, we describe the successful identification of a novel class of potent RAR-related orphan receptor alpha (RORα or nuclear receptor NR1F1) agonists from a library of 12,000 plant extract fractions by using an optimized, robust high-throughput cell-free screening method, as well as an innovative hit compound identification procedure through further extract deconvolution and subsequent structural elucidation of the active natural compound(s). In particular, we demonstrate that neoruscogenin, a member of the steroidal sapogenin family, is a potent and high-affinity RORα agonist, as shown by its activity in RORα reporter assays and from its effect on RORα target gene expression in vitro and in vivo. Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors, its excellent microsomal stability, good bioavailability, and significant peripheral exposure in mouse. Full paper download for free under: http://jbx.sagepub.com/content/19/3/399.full.pdf+html

China is getting into focus for building up and conducting pharmaceutical R&D and outsourcing activities. The reason for turning towards China is mostly politically or economically motivated. Scientific aspects often do not play an important role, but China with its huge plant biodiversity is an ideal site for drug discovery and development starting with natural compounds. This article gives an overview about advantages and disadvantages of natural product strategies in drug discovery. The authors describe how to deal with small molecules from plants as valuable source for successful drug discovery campaigns and how to meet the demands and standards of Western pharmaceutical industries.

Bicoll is the first Sino-German biopharmaceutical enterprise. It was founded in 2001 with two legal entities: Bicoll GmbH in Munich, Germany, and Bicoll Biotechnology (Shanghai) Co. Ltd. in Zhangjiang Hi-Tech Park, P.R. China. Technology development, cooperation management and marketing are functions in Munich, while facilities for research and development are located in Shanghai. The company is specialized in high-tech natural product chemistry and drug discovery services. The focus is on making compounds from natural resources compatible with customers' (drug) discovery systems in Europe and North America. More under: https://link.springer.com/chapter/10.1007/3-540-26561-9_16