Flavones, Flavonols, Lignans, and Caffeic Acid Derivatives from Dracocephalum moldavica and Their In Vitro Effects on Multiple Myeloma and Acute Myeloid Leukemia.

Phenolic plant constituents are well known for their health-promoting and cancer chemopreventive properties, and products containing such constituents are therefore readily consumed. In the present work, we isolated 13 phenolic constituents of four different compound classes from the aerial parts of the Moldavian dragonhead, an aromatic and medicinal plant with a high diversity on secondary metabolites. All compounds were tested for their apoptotic effect on myeloma (KMS-12-PE) and AML (Molm-13) cells, with the highest activity observed for the flavone and flavonol derivatives. While diosmetin (6) exhibited the most pronounced effects on the myeloma cell line, two polymethylated flavones, namely cirsimaritin (1) and xanthomicrol (3), were particularly active against AML cells and therefore subsequently investigated for their antiproliferative effects at lower concentrations. At a concentration of 2.5 µM, cirsimaritin (1) reduced proliferation of Molm-13 cells by 72% while xanthomicrol (3) even inhibited proliferation to the extent of 84% of control. In addition, both compounds were identified as potent FLT3 inhibitors and thus display promising lead structures for further drug development. Moreover, our results confirmed the chemopreventive properties of flavonoids in general, and in particular of polymethylated flavones, which have been intensively investigated especially over the last decade.

Effects of Crude Fucus distichus Subspecies evanescens Fucoidan Extract on Retinal Pigment Epithelium Cells-Implications for Use in Age-Related Macular Degeneration.

Fucoidan extracts may have beneficial effects in age-related macular degeneration(AMD). Over-the-counter fucoidan preparations are generally undefined, crude extracts. In thisstudy, we investigated the effect of a crude fucoidan extract from Fucus distichus subspeciesevanescens (Fe) on the retinal pigment epithelium (RPE). Fe extract was investigated for chemicalcomposition and molar mass. It was tested in primary RPE and RPE cell line ARPE19. Oxidativestress was induced with tert-butyl hydroperoxide, cell viability evaluated with MTT assay, VEGFsecretion assessed in ELISA. Phagocytosis was evaluated in a fluorescence microscopic assay.Wound healing ability was tested in a scratch assay. Additionally, the inhibition of elastase andcomplement system by Fe extract was studied. The Fe extract contained about 61.9% fucose andhigh amounts of uronic acids (26.2%). The sulfate content was not as high as expected (6.9%). It wasnot toxic and not protective against oxidative stress. However, Fe extract was able to reduce VEGFsecretion in ARPE19. Phagocytosis was also reduced. Concerning wound healing, a delay could beobserved in higher concentrations. While some beneficial effects could be found, it seems tointerfere with RPE function, which may reduce its beneficial effects in AMD treatment.