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Omic techniques have become key tools in the development of systems biology. As the holistic approaches underlying the practice of traditional Chinese medicine (TCM) and new tendencies in Western medicine towards personalised medicine require in-depth knowledge of mechanisms of action and active compounds, the use of omic techniques is crucial for understanding and interpretation of TCM development, especially in view of its expansion in Western countries. In this short review, omic applications in TCM research are reviewed which has allowed some speculation regarding future perspectives for these approaches in TCM modernisation and standardisation. Guidelines for good practice for the application of omics in TCM research are also proposed.

Plant extracts traditionally used for male impotence (Tribulus terrestris, Ferula hermonis, Epimedium breVicornum, Cinnamomum cassia), and the individual compounds cinnamaldehyde, ferutinin, and icariin, were screened against phosphodiesterase-5A1 (PDE5A1) activity. Human recombinant PDE5A1 was used as the enzyme source. Only E. breVicornum extract (80% inhibition at 50 µg/mL) and its active principle icariin (1) (IC 50 5.9 µM) were active. To improve its inhibitory activity, 1 was subjected to various structural modifications. Thus, 3,7-bis(2-hydroxyethyl)icaritin (5), where both sugars in 1 were replaced with hydroxyethyl residues, potently inhibited PDE5A1 with an IC 50 very close to that of sildenafil (IC 50 75 vs 74 nM). Thus, 5 was 80 times more potent than 1, and its selectivity versus phosphodiesterase-6 (PDE6) and cyclic adenosine monophosphate-phosphodiesterase (cAMP-PDE) was much higher in comparison with sildenafil. The improved pharmacodynamic profile and lack of cytotoxicity on human fibroblasts make compound 5 a promising candidate for further development.The inability to achieve or maintain an erection sufficient for satisfactory sexual function is an increasing problem with a considerable impact on interpersonal relationships and quality of life for men.1 During erection, nitric oxide is released from the axon terminals of the parasympathetic nerves and diffuses into smooth muscle cells of the arterial walls of the corpus cavernosum. The consequent activation of guanyl cyclase, converting guanosine triphosphate (GTP) into cyclic guanosine monophosphate (cGMP), causes smooth muscle relaxation, leading to dilation and increased influx of blood into the penile tissue. The trapping of blood in the penis results in an erection.2 Selective inhibitors of cGMPphosphodiesterase-5 (PDE5) such as sildenafil (Viagra), tadalafil, and vardenafil are currently used for erectile dysfunction (ED). However, several adverse effects have been recorded in clinical trials, including priapism and visual disturbances.3 Furthermore, therapy with PDE5 inhibitors is cost-effective. Thus, the search for new compounds of this type for drug development could be worthwhile. A variety of natural plant products, including berberine, forskolin, papaverine, and yohimbine, are claimed to be useful for improving sexual performance. Extracts from Lepidium meyenii Walp. (maca), Panax ginseng C.A. Meyer, Ginkgo biloba L., Ferula hermonis Boiss., and many other herbal remedies, alone or in combination, have been promoted for the treatment of sexual problems. 4,5 With the aim of looking for new leads for selective PDE5 inhibitors, plant extracts and their putative active principles were selected for screening against human PDE5 activity in vitro. Our attention focused on Tribulus terrestris L., Ferula hermonis, Epimedium breVicornum Maxim., and Cinnamomum cassia L., since these extracts are claimed traditionally to improve sexual performance. T. terrestris caused vasodilating and antihypertensive effects in rats 6 and a pro-erectile eff...

The Mediterranean diet reduces the risk of coronary artery disease as a consequence of its high content of antioxidants, namely, hydroxytyrosol (HT) and oleuropein aglycone (OleA), typical of virgin olive oil. Because intercellular and vascular cell adhesion molecules (ICAM-1 and VCAM-1) and E-selectin are crucial for endothelial activation, the role of the phenolic extract from extra virgin olive oil (OPE), OleA, HT, and homovanillyl alcohol (HVA) on cell surface and mRNA expression in human umbilical vascular endothelial cells (HUVEC) was evaluated. OPE strongly reduced cell surface expression of ICAM-1 and VCAM-1 at concentrations physiologically relevant (IC50 < 1 microM), linked to a reduction in mRNA levels. OleA and HT were the main components responsible for these effects. HVA inhibited cell surface expression of all the adhesion molecules, whereas the effect on mRNA expression was weaker. These results supply new insights on the protective role of olive oil against vascular risk through the down-regulation of adhesion molecules involved in early atherogenesis.